Selecting efficient pharmaceutical binder for developing robust extended release matrices of Compritol ® 888ATO prepared using wet granulation technique
Part 1 Studying impact on granule & tablet properties
Part 2 Studying impact on dissolution profiles of ER tablets of different API’s
K. Deshmukh, A. Shrivastava, S. Banerjee, R. Tiwari, S. Bambarkar, N. Farah
This study evaluates the binding efficiency of four commonly used pharmaceutical binders to hold hydrophilic API’s of different solubilities with hydrophobic, waxy ER matrices of Compritol ® 888 ATO as sustained release agent by studying their impact on the granule and tablet properties formulated using the same.
Softer Skin Stick (2613-1.17) is a 99% natural origin scrub in the practical form of a stick. It is possible to use it on dry skin or on wet skin for a more slippery application. Its texture, stabilized with Emulium® Dolcea MB, emulsify on contact with water, for an easy rinsing.
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Everything Balm (2620-1.02) is a 99% natural origin anhydrous multifunctional balm that takes care of the skin of the face, the body, the hands and also the lips and the hair. It contains Acticire® MB which allows the incorporation of aqueous ingredients such as active ingredients or colorants, for more customization!
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Magma Mask (2618-2.52) is a 98% natural origin mask in the form of surprising solid black pellets, obtained thanks to Geleol™ MB and Emulium® Kappa MB. One pellet represents a unique dose of a product, making it possible to take only the needed quantity. First, crush a pellet of the Magma Mask in your palm, then take a bit of 2620-1.02 Everything Balm (or alternatively hot water). Mix to form a thick black mask to spread directly onto the skin and rinse after 10 minutes.
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Scalp & Body Scrub (2628-1.07) is a 94% natural origin anhydrous wax with grains of sodium bicarbonate that gently exfoliates and cleanses the scalp, then rinses easily as grains will be dissolved by water, leaving no particles in the hair. The presence of Emulium® Kappa MB helps to improves rinsing while Acticire® MB boosts foam formation. It can also be used on the body for a 2-in-1 application.
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Slide n’ Foam (2621-2.09) is a 92% natural origin solid face cleanser that invites to a new gesture! Apply the product directly onto dry skin, then rub the skin with wet hands to create foam, boosted by Acticire® MB, and clean the skin. Thus, the product is not damaged by water and is gentler for the skin. Indeed, only the right amount is applied thanks to its melting texture obtained with the help of Lipocire™ A SG.
A non-ionic pure surfactant for lipid-based formulation to solubilize and increase oral bioavailability of poorly soluble API. Forms micellar solution in aqueous media.
\n","names_kv":[{"keys":"USP NF Name","value":"
Polyoxyl-32 stearate (type I) NF
\n"},{"keys":"EP Name","value":"
Macrogol-32 stearate (type I) EP
\n"},{"keys":"UNII Code (FDA)","value":"
33GX5WQC0M
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PEG-32 STEARATE
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Polyoxylethylene stearates
\n"},{"keys":"Chemical description","value":"
Consists of PEG-32 (MW 1500) esters of palmitic (C16) and stearic (C18) acids
Solubilizer for low log P APIs and bioavailability enhancer. Single excipient formulation system: self-emulsifies in aqueous fluid into micellar solution—LFCS Type IV. Use in melt processes (granulation, extrusion), granulation, and compression. Wetting agent. Safety of use is inferred by precedence of use in approved pharmaceutical products.
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Daily"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":36,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"","_yoast_wpseo_metadesc":""},"categories":[56],"tags":[],"acf":{"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false,"main_img_article":{"id":28468,"alt":"","title":"Inspiration2023-daring-on-the-daily","caption":"","description":"","mime_type":"image/png","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35.png","width":1536,"height":510,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-150x150.png","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-300x100.png","medium-width":300,"medium-height":100,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-768x255.png","medium_large-width":474,"medium_large-height":157,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-1024x340.png","large-width":474,"large-height":157,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-672x372.png","post-thumbnail-width":672,"post-thumbnail-height":372,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2023/01/Sans-titre-35-1038x510.png","twentyfourteen-full-width-width":1038,"twentyfourteen-full-width-height":510}},"component":"PageGenericContentCos","title":"INSPIRATION 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Sensorial experts for more than 20 years, Gattefossé consistently surprises and delights with innovative cosmetic textures.
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Five years ago, Gattefossé created INSPIRATION; a tool to discover new sensorial experiences and galvanize creativity. This creative concept provides pleasure, a sense of astonishment, and motivation to awaken formulators’ innermost imaginations.
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INSPIRATION highlights one or more topics, each of which offers a refreshing take through novel textures and visuals. The prototypes that illustrate each idea will encourage formulators to rediscover Gattefossé’s ingredients outside of their comfort zone.
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INSPIRATION for 2023 presents a new topic: DARING ON THE DAILY
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This year, Gattefossé invites customers to re-enchant their daily lives and dare to be unique. Due to a world in constant flux, consumers are reinventing their routines, rather than following normal conventions.
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For this new INSPIRATION, Gattefossé sets the tone for 2023 by giving a new narrative called: DARING ON THE DAILY! It is a joyful invitation that shakes up everyday conventions to celebrate life as a manifesto and assert your uniqueness.
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This new expression of beauty is highlighted by 3 main themes – I.D. Manifesto, Playground, and Experience the Unexpected – encouraging disruptive & playful cosmetics.
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Inspired by these trends, Gattefossé’s application lab has developed a collection of 7 innovative formulas that break the norms and explore new territories. Surprising & delightful, this new collection invites everyone to have fun, be bold, and be whimsical!
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Be “daring on the daily”!
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7 new formulas to shake up your daily routine and dare you to be yourself!
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I.D. Manifesto
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It is no longer a question of trying to hide imperfections; but letting them be a pathway to individuality. This trend anchors a desire for self-acceptance and self-expression.
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Primer-to-Powder (2479-2.04) is a makeup base featuring Emulium® Illustro. It starts with a rich, creamy texture that dries down to a powdery, matte finish, and leaves a silky smooth, even skin tone with long-lasting comfort and moisturization. \n (99.6% natural origin)
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Let’s now discover the Glittering Gummies (2745-3.04), a surprising travel-friendly format for a highlighter, made possible by Emulium® Kappa MB! Compact and easy to carry, this solid O/W emulsion is perfect for touch-ups on the go.
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It offers an ultra-bouncy effect and melting sensation thanks to Lipocire® A SG and creates a fresh and watery effect upon application. \n (97.4% natural origin)
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Craving uniqueness? The Holo Eye Liner (2758-1.11) has been designed to reveal the eccentricity living in you while reamining smudge-free and waterproof. Creamy and quick-drying, it melts seamlessly thanks to Lipocire® A SG to leave an intense purple, holographic line with long-wear properties! Emulium® Dolcea MB shows unfailing efficiency and robustness with this formula rich in pigments. \n (92% natural origin)
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Playground
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What if everyday life became a playground (again)? Gattefossé encourages more playful cosmetic application with our Cottage Cheese cream (2748-1.11) and its Squid Ink Topping (2748-2.04)! With Emulium® Dolcea MB, Acticire® MB, and EnergiNius® this creamy, yogurt-like texture delivers moisturizing and energizing benefits, perfect for daily application. Recommended once a week or once a month, mix it with 2 drops of the Squid Ink Topping, enriched with Original Extract® Ginger, to create your own detox mask! \n (99.5% natural origin)
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Experience the unexpected
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It’s time to discover new territories! Between the real and imaginary, appearances can be misleading… \n Like the Chayote-Kiwi Sorbet (2694-3.03), is it a beauty sorbet or a granita? With its light green color, you first see a food-like texture that you would love to eat. Upon initial application, you’ll feel a fresh, creamy yet powdery sensation, that leaves a dry, soft, non-tacky after-feel due to Emulium® Mellifera MB. This cushion cream brings a refreshing and intense moisturization, acts as a blur, and protects the skin from photoaging with Solastemis™. The skin appears radiant, even, and healthy. \n (99.4% natural origin)
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Alien Slime (2614-3.01) is another optical illusion! is it slime, or is it a cosmetic? Try it and you’ll be surprised by its comfortable, stringy, but non-sticky after-feel thanks to Emulium® Dolcea MB & Acticire® MB.
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Adapted for sensitive skin, it has a long playtime which is perfect for a soothing massage! It can also be used as a leave-on so that you can appreciate its nourishing properties. \n (98.2% natural origin)
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Bi-gels consist of an intimate mixture of an aqueous gel and an oily gel.
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Due to their dual nature, bi-gels are associated with the following advantages:
Improves the texture and enables a smooth and easy application on the body
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Numerous studies have shown that poor texture and sensorial properties negatively impact patient experience and adherence to treatment. The good news is there is plenty of scope for innovation and improvement in topical dosage forms if the patient’s experience of texture and sensorial properties is taken into consideration during formulation development. \r\n \r\nSensory analysis is a scientific discipline that applies the principles of experimental design and statistical analysis to measure, analyze, and interpret the characteristics of a product as they are perceived by the senses. \r\n \r\nGattefossé has developed validated methods and established an in-house sensorial analysis panel. Using this approach, we can evaluate the sensorial properties of our prototype formulations to \r\n•\tevaluate the influence of new raw materials in formulation, \r\n•\tevaluate the main texture characteristics of our emulsifiers, \r\n•\tcompare prototypes with market references, \r\n•\tunderstand market preferences, \r\n•\tconstruct a broad texture database. \r\n","":false,"content":[{"wysiwyg":"
A trained panel and validated methods for reliable results
\n
\n
Our sensory panel brings together over a dozen trained staff members, both men and women. They test new formulations approximately twice a week. The assessments are carried out using specific protocols and standardized procedures, and the results are statistically analyzed.
\n
Tests cover vision and touch, and they evaluate the following criteria:
\n
\n\n
\n
Initial touch \n
\n
pick-up
\n
texture
\n
creaminess
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\n
\n
\n
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During application\n
\n
spreadability
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tackiness
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play time
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greasiness
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softness
\n
absorption
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\n
\n
After absorption\n
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residual film
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tackiness
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greasy after-feel
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soft after-feel
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shine
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\n\n
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The power of sensorial mapping
\n
\n
\n
\n
This sensorial map shows the results with cream formulations formulated with different Gattefossé pharmaceutical-grade emulsifiers. It enables direct and visual comparison and can help to select the emulsifier or appropriate prototype formulation.
\n
Click on the image to enlarge.
\n
\n
For more information on how to develop formulas for optimized texture and sensory properties, please see our topical formulation section.
Incorporated in France as a “Société par actions simplifiée” with a capital of 4,650,000 euros, registered with the Lyon Trade and Companies Register under No. 389 586 900,
\n
Publishing Director: Ségolène Moyrand-Gros, Group Director – Corporate Development
\n
Hosted by:
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\n GATTEFOSSE SAS
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While requirements for sustainably driven product development have never been so real, the importance of natural actives as a key part of cosmetic formulations increases greatly.
\n
Consumer expects powerful efficacy from natural products. The challenge therefore is to find extraction methods that are both natural and effective in extracting the key active molecules from plants.
\n
When extracting active metabolites from botanicals, some molecules are more challenging than others. Despite perfect solubility in plant tissues, many of these molecules are poorly soluble in water or lipids, and even in the most efficient known solvents. Additionally, traditional solvents such as butylene glycol or alcohol are no longer acceptable to many consumers.
\n
Since 2012, Gattefossé scientists’ teams have been working on the design of a new generation of 100% natural solvents to create highly functional active ingredients: they are called Natural Deep Eutectic solvents or NaDES.
\n
\n
\n
A nature-inspired solution
\n
This new category of green solvents is directly inspired by botanicals and the way in which metabolites are solubilized inside the plant – through eutectic combinations of simple chemicals such as sugars, nitrogen compounds, and organic acids. \n Working with researchers from Leiden University, Gattefossé has developed and patented several natural eutectic solvents, perfectly adapted for the extraction of cosmetic active ingredients (1). This exciting class of solvents uses all-natural components such as sugars, polyols, amino acids.
\n
\n
But what does NaDES mean?
\n
\n
A NaDES can be defined as a eutectic mixture formed by a combination of natural compounds with specific molar ratio. It melts at a single, sharp unique temperature named the “eutectic point” (the lowest melting point for a specific composition) and is characterized by a supramolecular structure.
\n
This homogenous liquid is stable once the eutectic point is reached, making possible its use for extraction applications.
\n
\n
NaDES by Gattefossé
\n
\n
Through an ambitious research program, Gattefossé revealed many advantages linked to this extraction technology.
\n
\n
Completely natural, NaDES combinations benefits from a perfect affinity with plants enabling to reach high extraction potential. The botanical extracts obtained unveil unique phytochemical signature, and performance that would be impossible to reach using conventional solvents. \n Gattefossé thus makes the most of this technology to rediscover well known plants in cosmetics (Calendula, Mallow, Rose, Horse Chesnut…), and opens therefore new fields of possibility. \n 2 applications patents have already been granted (2).
\n
\n
Bright perspectives
\n
\n From plants and solvents selection to industrialization stage, we master in house all the steps of the development and manufacturing process. \n Our research teams are committed to continue exploring the potential of NaDES. \n Our research perspectives are still wide, and the coming years will surely see the rise of new NaDES active ingredients. \n Natural, non-toxic and efficient at low temperatures, the NaDES technology is perfectly aligned with Gattefossé commitments to provide high-performance sustainable active ingredients.
\n\n
Want to know more about the NaDES technology? Do not hesitate to contact your local sales representative.
\n
\n (1) Patent FR3036618B1, GATTEFOSSE SAS, CAPRIN B, CHARTON V, DEMARNE F: Vegetable extracts for cosmetics, solvents and methods for obtaining same \n (2) Patent FR3053890B1, US10363212B2, GATTEFOSSE SAS, CHARTON V, CAPRIN B, BECHETOILE N: Aesculus Hippocastanum extract \n (2) Patent FR3067939A1, GATTEFOSSE SAS, BECHETOILE N, LOPIS-PRESLE S: Extract of Whitania Somnifera to fight against the harmful effects of visible light on skin
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Highest-purity solvent and solubilizer for solubility and bioavailability enhancement for oral and alternative routes.
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Diethylene glycol monoethyl ether
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Diethylene glycol monoethyl ether
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DIETHYLENE GLYCOL MONOETHYL ETHER
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Diethylene glycol monoethyl ether
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The North American region is a leading market for pharmaceuticals and personal care with important local production, consumption and a major influence on global trends. Within this favorable context, Gattefossé North America has enjoyed continuous growth in its business activity since its creation in 1982.
\n
To expand its presence in the region, the Gattefossé Group has decided to establish its fourth Technical Center of Excellence in Paramus, New Jersey. Mr. Jacques Moyrand, Gattefossé Group Chairman, Mr. Olivier Midler, Gattefossé Group CEO and Mr. Eric Brun, President and CEO of Gattefossé USA and Canada, will inaugurate the North America Technical Center of Excellence on Wednesday, April 26th 2017. This center brings together pharmaceutical and personal care application laboratories in a 5,300 ft² (492 m²) space with state-of-the-art equipments.
\n
The technical team will offer an essential interface with both pharmaceutical and personal care customers throughout North America by providing formulation troubleshooting, inspiration and technical support.
\n
For pharmaceuticals, high priority will be given to oral bioavailability enhancement and modified release applications. For personal care, the laboratory will develop specific formulas to answer local needs and to capture local trends.“The latest sign of our investment in this strategic market is the creation of the Gattefossé North America Technical Center of Excellence. These state-of-the-art application laboratories located in Paramus, New Jersey, will ensure our customers responsive service adapted to their market”.
\n
Eric Brun, President and CEO of Gattefossé USA and Canada
\n
\n
About Gattefossé North America
\n
\n\n
The USA and Canadian affiliates of Gattefossé (created respectively in 1982 and 1997) were established to provide local service and support to the.pharmaceutical and personal care industries in North America. Since its creation, Gattefossé North America has enjoyed continuous growth, expanding its presence as a provider of innovative solutions involving performance ingredients.
\n
Under the leadership of Eric Brun, Ph. D, a specialized team of professionals, including marketing, customer service, supply chain, quality, and technical support, is fully committed to servicing customers from the corporate offices in Paramus, NJ, Toronto, ON and Montreal, QC. Local service is also provided by long-term partners in the US Midwest and West Coast, as well as Mexico.
\n
Today, Gattefossé has 34 employees and 3 offices in North America as well as 3 warehouses in Edison (NJ), La Mirada (CA) and Toronto (Canada).
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We all know that naturalness is no longer just a trend, it is a prerequisite for any new cosmetic product launch. Indeed, it is one of the main consumer expectations, not only in Europe but also throughout the world.
\n
\n
Formulation of natural cosmetics is not so easy
\n
\n
Formulating a natural cosmetic product is not that simple, for various reasons:
\n
\n
The naturality of the cosmetic ingredients is not always clearly indicated, and the calculation methods used vary from one supplier to another (ISO 16128, COSMOS…)
\n
The formula stability is an essential point to check before launching a new product
\n
The formula must be perfectly tolerated by all skin types
\n
Textures must be always more innovative to attract consumers’ attention
\n
Sensoriality is a key factor that drives purchase intention
\n
\n
Formulating a natural cosmetic product therefore takes longer, whereas development times decrease year after year.
\n
\n
The wax butter technology is the solution
\n
\n
This technology leads to the creation of 100% natural origin emulsifiers and texture ingredients which bring moisturizing benefits due to the vegetable waxes and true sensory identities.
\n
It maximizes the advantages of vegetable waxes while overcoming their disadvantages:
\n
\n
\n
\n
A patented technology
\n
\n\n
For over 30 years, Gattefossé has developed a strong expertise in the transformation and functionalization of natural waxes according to the rules of green chemistry. This environment-friendly chemistry enables the creation of new texture ingredients with particularly interesting properties. Gattefossé holds a number of patents on this technology, the most recent of which describe the reaction of solid and liquid waxes in presence of vegetable polyglycerol1. The subject of several scientific papers, communications and recognized as an innovation in textures, this chemistry has been used to create a wide range of texture ingredients.
\n
\n
\n
How does it work?
\n
\n\n
Natural waxes contain fatty acids, fatty alcohols and esters with reactive groups. Adding polyglycerol-3 enables the creation of new sensorial esters though a succession of transesterifications.
\n
\n\n
1) Transesterification between polyglycerol-3 and ester of solid wax:
\n
\n
\n
\n
2) Transesterification between polyglycerol-3 monoester and jojoba wax ester:
\n
\n
\n
\n
3) Transesterification between fatty alcohol of solid wax and polyglycerol-3 diester:
\n
\n
\n
\n
4) Transesterification between polyglycerol-3 monoester and fatty alcohol of jojoba wax:
\n
\n
\n
\n
Summary of all the reactions:
\n
\n
\n
\n
These transesterifications create new jojoba esters that combine the rigidity of the saturated carbon chain with the flexibility of the unsaturated one.
\n
These mixed esters show intermediate physico-chemical properties between solid and liquid waxes. Transforming the waxes improves their behavior and functionality. These new properties include a better solubilization in the lipid phase, amphiphilic behavior, good moisturizing properties and enhanced sensory attributes.
\n
\n
\n
\n
Water absorption capacity
\n
\n\n
The reactions described above create a homogeneous soft wax butter. It has the ability to absorb up to 4 times its weight in water and is central to the moisturizing properties of the ingredients created with this technology.
\n
\n
\n
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Our products range based on the wax butter technology
\n
\n
By varying the types of waxes used, Gattefossé has developed a wide range of emulsifiers and texturizing ingredients with very distinct functional and sensory properties.
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\n
\n
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1 EP1933806, GATTEFOSSÉ SAS, Support comprising a wax derivative for making topical cosmetic formulations, filed on 10 September 2006
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A radiant complexion is an essential characteristic of beautiful skin. Complexion indeed plays a key role in perceptions of youth and beauty around the globe. Gatuline® Radiance enhances microcirculation, bringing blood flow to the surface layers of the skin. This in turn enhances all aspects of a radiant complexion, including skin color and luminosity. Skin brightness is visibly enhanced even under heavy pollution.
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Gatuline® Radiance is obtained from Evodia rutaecarpa, also known as “Wu-Zhu-Yu”, a flowering shrub member of the Rutaceae family. Evodia rutaecarpa is widely cultivated in southeast China for Traditional Chinese Medicine. In addition to its medicinal uses, the Chinese would traditionally wear Evodia on the ninth day of the ninth Chinese lunar month (Double Ninth Festival). The plant was thought to bring luck. Preservative free.
Anti-pollution (the skin is less reactive, durably soothed)
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Alphabet creams
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Skin perfectors
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Illuminating products
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Global antiaging lines
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Lip products (reveals natural rosy color of lips)
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New strategic step for the Group
\n
This new production site will enable the Group to respond to several strategic challenges: \n • Deepen its presence in North America to better meet local customers’ needs, \n • Increase its global production capacity, \n • Provide back-up solutions on 3 continents and bring more supply flexibility to all \n customers. \n Construction will begin in 2021 and the plant should deliver its first customers in 2024.
\n
United States: a key choice for the Group development
\n
“North America is a leading region for the global pharmaceutical and personal care industries in terms of innovation, production and consumption, and has therefore a major impact on worldwide trends. The opening of a manufacturing unit represents an essential milestone in our strategy to enhance our local presence and commitment to this important and influential market. The label “Made in USA” will satisfy a strong demand expressed by our customers and the geographical location of this new site will facilitate logistics and supply chain. Production in Texas is first intended to serve the North American market but will gradually be extended to other regions” says Eric Brun, President and CEO of Gattefossé USA and Canada.
\n
Today, the Gattefossé Group operates 2 production sites, in Europe (France) and Asia (Singapore).
\n
The opening of a third manufacturing plant in the United States will improve the Group’s ability to better serve the American market and represents an extra step in the deployment of its industrial operations. The company chose to set up a plant in Lufkin, Texas, because of its central position in North America, close to the important industrial pole in Houston. Lufkin is a dynamic up and coming city of 35,000 inhabitants located in the heart of a free trade zone.
\n
A project in line with the Group’s social responsibility
\n
“The international expansion of industrial operations is an essential step in the development of our Group. This project meets the economic and environmental challenges set by the company as part of its global strategy: innovation, customer intimacy, geographic expansion and social responsibility. Controlling our environmental impact is a priority: Gattefossé headquarters will be ISO 14001 certified in 2021 and the new American site will also meet this requirement” explains Eduardo De Purgly, Gattefossé Group CEO.
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Strongly reinforced, the skin is visibly revived in favor of a healthy glow."},"categories":[6],"tags":[],"acf":{"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false,"component":"PageCosmeticProduct","":false,"product_codes":[{"code":"5911"}],"bandeau_image":{"id":13742,"alt":"","title":"EnergiNius","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius.jpg","width":1144,"height":400,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-300x105.jpg","medium-width":300,"medium-height":105,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-768x269.jpg","medium_large-width":474,"medium_large-height":166,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-1024x358.jpg","large-width":474,"large-height":166,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-672x372.jpg","post-thumbnail-width":672,"post-thumbnail-height":372,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/EnergiNius-1038x400.jpg","twentyfourteen-full-width-width":1038,"twentyfourteen-full-width-height":400}},"image_product_finder":{"id":9011,"alt":"EnergiNius","title":"","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","width":244,"height":163,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","medium-width":244,"medium-height":163,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","medium_large-width":244,"medium_large-height":163,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","large-width":244,"large-height":163,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","post-thumbnail-width":244,"post-thumbnail-height":163,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2018/04/iStock-617394368_vignette.jpg","twentyfourteen-full-width-width":244,"twentyfourteen-full-width-height":163}},"title":"EnergiNius®","tagline":"Recharge the skin's battery","description_product_finder":"","introduction":"
EnergiNius® protects skin cells from screen-emitted artificial visible light, an added environmental stress induced by a modern lifestyle. Strongly reinforced, the skin is visibly revived and the signs of fatigue disappear in favor of a healthy glow.
Derived from Indian Ginseng (Withania somnifera) roots, EnergiNius® is organic certified and obtained using the innovative NaDES technology. Sourced in Oregon, USA, Withania somnifera is an emblematic plant of Ayurvedic medicine and has been used in traditional medicine for millennia. EnergiNius® contains amino acids and withanolids; the synergetic action of these two phytochemical families supports its high level of efficacy.
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Watch the video to get a comprehensive overview of EnergiNius®: \n
For the first time, the screen emitted artifical visible light (AVL) has been precisely characterized and Gattefossé has developed unique equipment accurately recreating the light emitted by screens.
A nonionic oil-in-water emulsifier for topical formulations that provides high stability in topical fluid lotions and light emulsions over a wide pH range.
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Mixture of PEG-6 stearate and PEG-32 stearate
\n"},{"keys":"EP Name","value":"
Pending
\n"},{"keys":"UNII Code (FDA)","value":"
8LQC57C6B0 33GX5WQC0M
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PEG-6 STEARATE PEG-32 STEARATE
\n"},{"keys":"Handbook of Pharmaceutical Excipients","value":"
Polyoxylethylene stearates
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Consists of a mixture of PEG-6 (MW 300) esters of stearic (C18) acid and PEG-32 (MW 1500) esters of stearic (C18) acid
Polyvalent emulsifier compatible with all types of oils and ideal for topical lotions. Stabilizes and improves sensorial and texture properties. Safety of use is inferred by precedence of use in approved pharmaceutical products.
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and conditions"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":1,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"","_yoast_wpseo_metadesc":""},"categories":[48],"tags":[],"acf":{"component":"PageGenericContentCorporate","oneLoad":false,"title":"Terms and conditions","content":"
General Terms and Conditions of Use for the gattefosse.com website :
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Purpose
\n\n
These General Terms and Conditions of Use (“General Terms and Conditions of Use”) apply to the browsing of the website www.gattefosse.com (the “Website”) and the use of its features.
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By accessing the Website, the user (the “User”) acknowledges having read and accepted without reservation all the General Terms and Conditions of Use herein and undertakes to comply with them.
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These General Terms and Conditions of Use may be revised by Gattefossé at any time without any formality other than the online publication of a new amended version, the latter prevailing over any previous version.
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Access to the Website
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The Website is accessible free of charge in any place to any User with internet access.
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Any costs involved in accessing the Website (computer hardware, software, internet connection, etc.) are borne by the User.
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In the event of maintenance work, an event beyond the control of Gattefossé, an outage or in the event of force majeure, access to the Website may be interrupted or suspended without notice or justification and without Gattefossé being held liable.
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In addition, Gattefossé reserves the right to interrupt or definitively cease publication of the Website, at any time, without notice or justification and without being held liable.
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Members’ Section
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Any User who wishes to access the members’ section of the Website (the “Members’ Section”) must register by filling in the form.
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When registering in the Members’ Section, the User undertakes to provide accurate information concerning their civil status, contact details (email address), the company for which they work, their field of activity and the position they hold there,
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Registration is subject to validation by Gattefossé, who are free to refuse a User’s registration, without justification and without being held liable.
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Access to the Members’ Section is controlled by entering the email address provided upon registration and the password selected by the User.
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These identifiers are strictly personal and must not be conveyed to third parties. In all events, the User remains responsible for the use made of them.
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Without prejudice to its other rights and remedies, Gattefossé reserves the right to suspend or delete, without notice, the account of any User who does not comply with these General Terms and Conditions of Use.
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The User may request that their account be deleted by sending an email to: contact@gattefosse.com specifying their first and last names, email address and the reason for their request. Account deletion will be effective within a reasonable timeframe.
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Any deletion of an account, for any reason whatsoever, shall result in the definitive deletion of all the User’s personal information.
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Intellectual Property
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The registered or unregistered trademarks, logos and signs represented on the Website as well as all its content (texts, icons, photographs, illustrations, layouts, etc.), including the content of the Members’ Section, are protected by the French Intellectual Property Code and more specifically by copyright.
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Any reproduction, representation, publication, redistribution or copying of all or part of these elements is subject to the express prior authorisation of Gattefossé and/or the holders of the rights for these elements.
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Non-compliance with this obligation may constitute an act of infringement punishable under Articles L335-2 et seq. of the French Intellectual Property Code.
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Access to the Website shall not be interpreted as conferring on the User any licence or intellectual property right whatsoever over the Website and/or its content other than that of viewing and browsing the Website.
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All Users are also prohibited from using a robot or any other automatic process that enables them to access, vacuum or extract the data contained or presented on the Website.
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Without prejudice to the above, any User duly registered in the Members’ Section may download the media made available in the members’ section. These media may only be used for personal and informational purposes, to the exclusion of any commercial and/or advertising use. The User shall also refrain from (i) deleting or modifying the copyright notices and any other proprietary notices affixed or contained in these media (ii) modifying or altering these media and their content (iii) publishing and distributing, in any manner whatsoever, for consideration or free of charge, these media and their content. More generally, the User shall refrain from directly, indirectly or through third parties, in any way whatsoever, infringing the rights of Gattefossé and/or the rights of third parties on these media.
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Personal data
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Gattefossé may collect and process personal data that Users provide during their browsing of the Website.
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Gattefossé undertakes to collect and process this data in accordance with applicable law and the provisions of its Personal Data Protection Policy.
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Cookies
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When browsing the Website, cookies may be placed on the User’s device (computer, tablet, smartphone). A cookie is a small computer file deposited on the User’s device through their internet browser that allows certain data to be stored in order to facilitate browsing on a website and enable certain functionalities.
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Gattefossé’s use of these cookies is governed by the provisions of its Personal Data Protection Policy.
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Liability
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Gattefossé does not provide any warranty, whether express or implied, concerning the Website and/or all or part of its content.
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Gattefossé will make every effort to ensure that the information presented on the Website is accurate, up-to-date and reliable, but will not be held responsible for any error or omission in this respect.
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The information presented on the Website is provided for information purposes only.
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Consequently, Gattefossé may not be held liable for any damage, direct or indirect, of any kind whatsoever, resulting from the use by the User of the information presented on the Website.
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Gattefossé declines all responsibility for any viruses that may infect the User’s computer hardware due to access to, or use of, the Website.
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Gattefossé cannot be held liable for any difficulties in accessing the Website and/or disruptions to Internet connections. Similarly, the liability of Gattefossé is excluded in the event of force majeure.
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In general, Gattefossé declines all liability in the event of direct or indirect damage, regardless of the causes, origins, nature or consequences that would result from access to and/or use of the Website and/or its content, the User taking sole responsibility for the resulting risks.
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Links to other websites
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The Website may have hypertext links directing the User to other websites. Gattefossé declines all responsibility regarding access to and use of these websites and/or their content, the User alone assuming full responsibility and the resulting risks.
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Applicable law, competent courts
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These General Terms and Conditions of Use are governed by French law. In the event of a dispute, the courts of Lyon shall have sole jurisdiction, including in the event of summary proceedings, third-party claims or multiple defendants.
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General Terms & Conditions of Sale :
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Please find below the General Terms & Conditions of Sale (“T&C’s”) applicable to all sales of products and/or services by the corresponding affiliate of the Gattefossé Group:
Hard fat pessary base with emulsifier to improve dispersibility and wettability of hydrophobic APIs.
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Mixture of hard fat and ethoxylated fatty alcohols
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Mixture of hard fat and ethoxylated fatty alcohols
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8334LX7S21 YRC528SWUY
\n"},{"keys":"Preferred Substance Name (FDA)","value":"
Hard fat Polyoxyl 20 cetostearyl ether
\n"},{"keys":"Handbook of Pharmaceutical Excipientsitory bases, hard fat","value":"
/
\n"},{"keys":"Chemical description","value":"
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Understanding The Role Of In Vitro And In Vivo Evaluation Techniques In Determining the Performance of Lipid-Based Formulations
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Elise Dauphin-Chanard ; Jean-Marie Girard ; Carole Deleglise ; Philippe Caisse
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Fiona Mc Cartney ; David Brayden
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Selecting efficient pharmaceutical binder for developing robust extended release matrices of Compritol ® 888ATO prepared using wet granulation technique
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Part 1 Studying impact on granule & tablet properties
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Part 2 Studying impact on dissolution profiles of ER tablets of different API’s
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K. Deshmukh, A. Shrivastava, S. Banerjee, R. Tiwari, S. Bambarkar, N. Farah
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This study evaluates the binding efficiency of four commonly used pharmaceutical binders to hold hydrophilic API’s of different solubilities with hydrophobic, waxy ER matrices of Compritol ® 888 ATO as sustained release agent by studying their impact on the granule and tablet properties formulated using the same.
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K. Deshmukh, A. Shrivastava, S. Banerjee, R. Tiwari, S. Bambarkar, N. Farah
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Providing texture and stability
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A short video to explain how Gattefossé all-in-one emulsifiers help simplify topical formulations and enable to obtain a wide range of sensorial textures
A short video to understand the three formulation rules, ie solubility, partition, diffusion, for safe skin penetration enhancement with Gattefossé solubilizers. \n
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Transcutol® P: A high-purity solvent and powerful solubilizer associated with skin penetration enhancement in topical dosage forms.
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Lauroglycol™ FCC: Cosurfactant and solubilizer in topical dosage forms associated with skin penetration enhancement.
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Patches are efficient systems to deliver drug to and through the skin. A permeation enhancer is often used to help the percutaneous passage of the drug. With a very high solubilizing capacity for both CBD and THC, Transcutol® P is the ideal permeation enhancer.
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The mechanism of action of Transcutol® P for penetration and permeation enhancement can be explained as follows:
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Increasing drug solubility in the vehicle Increasing drug solubility and partitioning in the stratum corneum
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Maintaining hydrated dynamics in the stratum corneum without disturbing the lipid bilayer structures
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More information on the use of Transcutol® P for transdermal patches is available:
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A SG","tagline":"Sustainable texturizing","description_product_finder":"","introduction":"
Agent de texture naturel et durable, Lipocire™ A SG donne du corps aux formules cosmétiques et leur confère un toucher plus onctueux, ultra fondant.
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Une expérience sensorielle unique dans de nombreuses applications soin et maquillage.
Beurre végétal texturant, Lipocire™ A SG est issu de l’hydrogénation et de l’inter-estérification d’huiles de palme et de palmiste, extraites des fruits et des graines du palmier à huile. Relipidants et nourrissants, ces lipides filmogènes présentent une excellente affinité avec la peau et permettent de reconstituer le film protecteur hydrolipidique. Ils apportent douceur et confort à la peau et aux formulations.
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Gattefossé n’utilise que des huiles de palme et de palmiste certifiées RSPO Segregated (SG) (Roundtable on Sustainable Palm Oil). Cette certification garantit que les huiles proviennent exclusivement de plantations gérées durablement.
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Le fruit du palmier a la peau rouge foncé et la chair jaune-orange, il est particulièrement riche en éléments nutritifs. La pulpe du fruit et l’amande dans son noyau ont tous deux une teneur élevée en triglycérides (> 50%).
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Autres grades disponibles :
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Lipocire ™ CM SG a un point de fusion légèrement supérieur et est préconisé pour les formulations de plus grande rigidité : par exemple, sticks ou poudres pressées.
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Lipocire ™ DM SG a un point de fusion supérieur aux deux autres grades. Il est conseillé de l’utiliser pour les formulations avec une solidité encore plus grande, comme les crayons de maquillage.
Maquillage : mascaras, rouges à lèvres, brillant à lèvres, bâtons, eye-liner, ombres à paupières, rougeurs, poudres en vrac
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Thermal Activity Monitoring
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Formulation forum – A Quick Approach for Evaluation of Drug-Excipient Compatibility: Case of Acetylsalicylic Acid
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Dr. Masumi Dave, Rollie Fuller – Gattefossé USA \n
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In this study, the authors monitor acetylsalicylic acid (ASA) hydrolysis in different formulations using UPLC and TAM with the objective of comparing these methods for agreement, speed, and efficiency in predicting drug stability. In parallel, we assess the impact of the excipient choices on the stability of the ASA. \n
TAM Technique for Identifying API-Lipid Excipient Compatibility Issues Upstream in the Development Process
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Masumi Dave, M.S., Jason Le Pree, Ph.D., R.Ph. – Gattefossé USA
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AAPS PharmSci 360 – 2018
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In this study the authors showed that Thermal Activity Monitoring is a useful technique to detect at early stage potential interaction between APi and excipients, using less time and resources than conventional techniques. \n TAM technique is used routinely in Gattefossé North America Technical Center of Excellence to speed up formulation development. \n Download the poster
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PIT deviation for fast and accurate measure of HLB
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An efficient method to determine the Hydrophile-Lipophile Balance of surfactants using the phase inversion temperature deviation of Ci Ej /n-octane/water emulsions.
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Nollet M, Boulghobra H, Calligaro E, Rodier JD
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Int J Cosmet Sci. 2019 Apr; 41(2):99-108. doi: 10.1111/ics.12516. Epub 2019 Mar 7.
Size characterization of lipid-based self-emulsifying pharmaceutical excipients during lipolysis using Taylor dispersion analysis with fluorescence detection
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Joseph Chamieh, Habib Merdassi, Jean-Christophe Rossi, Vincent Jannin, Frédéric Demarne, Hervé Cottet
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International Journal of Pharmaceutics, Volume 537, Issues 1–2, 15 February 2018, Pages 94–101
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In this work, the lipolysis of Labrasol® and Gelucire® 44/14 , two lipid based self-emulsifying drug delivery systems, by pancreatic enzymes and under conditions mimicking the gastrointestinal tract is followed by Taylor dispersion analysis. Results show that, Labrasol® droplets decrease exponentially in size with lipolysis time, whereas Gelucire® 44/14 droplets increased sigmoïdally in size. Even after 120 min lipolysis, both systems maintain a solubilizing capacity of the hydrophobic marker.
Hydrodynamic size characterization of a self-emulsifying lipid pharmaceutical excipient by Taylor dispersion analysis with fluorescent detection
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Vincent Jannin, Frédéric Demarne, Hervé CottetInternational Journal of Pharmaceutics, Volume 513, Issues 1–2, 20 November 2016, Pages 262-269
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In this study the size of microemulsion droplets is carried out using Tailor Dispersion Analysis in comparison to Dynamic Light Scattering. The size evolution of a Labrasol® self emulsifying drug delivery system as a function of concentration and temperature is evaluated. The influence of physical parameters and polydispersity is discussed.
Toward the Establishment of Standardized in Vitro Tests for Lipid-Based Formulations. 5. Lipolysis of representative formulations by gastric lipase.
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Bakala-N’Goma, J.C., Williams, H.D., Sassene, P., Kleberg, K., Calderone, M., Jannin, V., Igonin, A., Partheil, A., Marchaud, D., Jule, E., Vertommen, J., Maio, M., Blundell, R., Benameur, H., Müllertz, A., Pouton, C.W., Porter, C.J.H., Carrière, F. Pharm Res. 2015 Apr; 32(4):1279-87. doi: 10.1007/s11095-014-1532-y. Epub 2014 Oct 7.
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This research article focuses on the effect of gastric lipases on various LFCS formulation types. Gastric lipase is active on all formulations tested but presents the highest activity on self (micro)emulsifying drug delivery systems composed of medium chain lipids (LFCS type II & III).
Toward the Establishment of Standardized In Vitro Tests for Lipid-Based Formulations, Part 6: Effects of Varying Pancreatin and Calcium Levels.
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Sassene, P.J., Kleberg, K., Williams, H.D., Bakala-N’Goma, J.C., Carrière, F., Calderone, M., Jannin, V., Igonin, A., Partheil, A., Marchaud, D., Jule, E., Vertommen, J., Maio, M., Blundell, R., Benameur, H., Porter, C.J.H., Pouton, C.W., Müllertz, A.
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AAPS J. 2014 Nov;16(6):1344-57. doi: 10.1208/s12248-014-9672-x. Epub 2014 Oct 2.
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This article continues a series of publication on the establishment of a standardized method of lipolysis. In this article the effect of varying quantities of pancreatin (the selected enzyme) and calcium on the extent of lipolysis and drug repartition (precipitation / micellar phase / lipid phase) has been evaluated. The repartition of the drug is not significantly affected by these two parameters, hence physiological levels of enzyme and calcium (1.4 mM) are recommended.
Biorelevant media resistant co-culture model mimicking permeability of human intestine.
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Delphine Antoine, Yann Pellequer, Camille Tempesta, Stefan Lorscheidt, Bernadette Kettel, Lana Tamaddon, Vincent Jannin, Frédéric Demarne, Alf Lamprecht, Arnaud Béduneau
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International Journal of Pharmaceutics, Volume 481, Issues 1–2, 15 March 2015, Pages 27-36
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Cell culture models are currently used to predict absorption pattern of new compounds and formulations in the human gastro-intestinal tract (GIT). One major drawback is the lack of relevant apical incubation fluids allowing mimicking luminal conditions in the GIT. Here, we suggest a culture model compatible with biorelevant media, namely Fasted State Simulated Intestinal Fluid (FaSSIF) and Fed State Simulated Intestinal Fluid (FeSSIF).
\n"}],"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false},"_links":{"self":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/6857"}],"collection":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/users/9"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/comments?post=6857"}],"version-history":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/6857/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/media?parent=6857"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/categories?post=6857"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/tags?post=6857"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"publications-on-skin-drug-delivery":{"id":13112,"date":"2019-04-11T08:38:12","date_gmt":"2019-04-11T06:38:12","guid":{"rendered":"https://www.gattefosse.com/?page_id=13112"},"modified":"2022-04-04T11:09:34","modified_gmt":"2022-04-04T09:09:34","slug":"publications-on-skin-drug-delivery","status":"publish","type":"page","link":"https://www.gattefosse.com/fr/pharmaceuticals-special-content/publications-on-skin-drug-delivery/","title":{"rendered":"Publications on skin drug delivery"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":9,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"Publications on skin drug delivery | Gattefossé","_yoast_wpseo_metadesc":"Find out Gattefossé Publications on skin drug delivery"},"categories":[36],"tags":[],"acf":{"component":"PageSpecialContentPharma","title":"Publications on skin drug delivery","introduction":"List of Gattefossé publications on skin drug delivery","":false,"content":[{"wysiwyg":"
Critical Criteria for Assessing the Permeation Performance of Topical Formulas on Animal Skin: Standardization of IVPT Protocols
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E. Dauphin-Chanard; A. Forest; C. Deleglise; D. Hoste; P. Caisse
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Poster PBP 2022
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To assess the performance of dermal/transdermal formulation, in vitro permeation test (IVPT) with Franz cells is a reliable, reproducible, and widely used technique1. Due to its histological similarity, pig skin is a common model used as an alternative to human skin2. However, careful consideration should be given to the pig skin preparation, as both permeability and lag time can be greatly affected. The main variation sources are pig skin storage time, skin integrity and thickness, sample quantity and methodology to apply the formulation on the membrane. This study aims to investigate the critical parameters affecting the data’s accuracy by evaluating the permeation of a lidocaine hydrochloride-based gel (LID HCl) on pig skin.
Investigation of the permeation enhancer strategy on benzoylaconitine transdermal patch: the relationship between transdermal enhancement strength and physicochemical properties of permeation enhancer
In this study several permeation enhancers are evaluated for their ability to permeate high molecular weight benzoylaconitine. The results showed that Plurol® Oleique CC 497 enabled the highest permeation. FT-IR studies demonstrated that the enhancer had strong interactions with the Stratum corneum, both in the hydrophilic and lipophilic regions. The optimized patch formulation showed excellent analgesic and antiinflammatory effect.
Synergising excipients to boost skin delivery. A case study with lidocaine hydrochloride
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E. Dauphin-Chanard; A. Forest; C. Deleglise; M. Ducros; D. Marchaud
\n
Poster Skin Forum 2019
\n
In this study the authors showed that combining an efficient solubilizer and penetration enhancer achieves a synergic effect which enhances the passive diffusion of LID HCl through the Strat-M membrane in this Franz cell model.
Development of a daphnetin transdermal patch using chemical enhancer strategy: insights of the enhancement effect of Transcutol P and the assessment of pharmacodynamics.
\n
Shen M, Liu C, Wan X, Farah N, Fang L.
\n
Drug Dev Ind Pharm. 2018 Oct;44(10):1642-1649. doi: 10.1080/03639045.2018.1483391. Epub 2018 Jul 2.
\n
A patch for transdermal delivery of daphnetin was developped using Transcutol® P as permeation enhancer.
\n
The study showed:
\n
\n
10% Transcutol® P led to a significant increase in drug release from the patch.
\n
Patch exhibited analgesic and anti-inflammatory activity
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For nearly 140 years, our strategy of continuous investment in research, development, and applications has driven our capacity to innovate. Gattefossé customers benefit from the company’s unique know-how and ability to stay one step ahead of market trends in the personal care and pharmaceutical sectors.
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for Solubility and Bioavailability Enhancement"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":9,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"Excipients for solubility and bioavailability enhancement | Gattefossé","_yoast_wpseo_metadesc":"Discover our range of excipients to increase solubility and oral bioavailability of BCS class II poorly soluble drugs."},"categories":[49],"tags":[],"acf":{"component":"PageGenericContentPharma","title":"Excipients for Solubility and Bioavailability Enhancement","content":"
Active pharmaceutical ingredients (APIs) exhibiting low aqueous solubility or poor intestinal permeability will be associated with poor or variable drug absorption. Lipid-based drug delivery (LBDD) has emerged as a successful approach to improve drug solubilization in the dosage form and, more importantly, in the gastrointestinal (GI) tract, leading to normalized drug absorption and increased bioavailability.
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Lipid excipients have proven utility for BCS Class II APIs and are potentially useful for Classes III and IV, due to their ability to:
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improve API solubility in the dosage form;
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maintain APIs in a solubilized state within the GI tract;
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work in synergy with in vivo physiological lipid digestion and absorption, which facilitate drug absorption.
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Lipid excipients: Solubilizers of poorly water-soluble drugs
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Drug solubility depends on many physicochemical properties and is therefore a complex phenomenon. When addressing poor aqueous solubility, a drug molecule is often described as lipophilic or hydrophobic. Lipophilic molecules are insoluble in aqueous solution but exhibit a degree of solubility in lipid excipients. In contrast, hydrophobic molecules are insoluble in aqueous solution and can also be poorly soluble in lipids (i.e., hydrophobic/lipophobic).
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The lipophilicity of an API is described as the log P value, which can be a useful starting point in selecting lipid excipients for solubility screening.
Lipide excipients should be able to solubilize APIs in the dosage form, and it is crucial that they maintain API solubility in vivo when exposed to an aqueous environment. Therefore, the behavior of the excipients in aqueous fluid is an important factor.
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The hydrophilic/lipophilic balance (HLB) is commonly used to categorize the degree of affinity of the lipid excipient for the aqueous phase. At Gattefossé, the HLB of excipients is determined by analytical methods and called practical HLB.
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Each API has a complex chemical space. As such we recommend solubility screening of the API for a range of excipients. Depending on API characteristics, one or more lipid excipients may be required to solubilize the target dose. Generally, excipients that provide the highest solubilizing power are selected for formulation development. For information about formulation, consult our section“Lipid-based drug delivery systems.”
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Lipid excipients maintain APIs in solubilized state during digestion
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Digestive enzymes play a well-known role in food transformation within the GI tract. They digest fats (triglycerides) by the hydrolysis of ester bonds, which releases free fatty acids and monoglycerides. These are naturally emulsified by bile salts into mixed micelles and transported to the GI membrane for absorption. Lipid excipients comprise fatty acid esters (e.g., glycerides and PEG esters) and are therefore subject to lipolysis by the same endogenous enzymes.
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The in vivo digestion of lipid excipients can further enhance drug solubility in mixed micelles, presenting the drug in a solubilized state at the GI membrane.
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Lipid excipients naturally promote drug absorption
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With lipid-based formulations, API bioavailability may be improved by:
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facilitating drug permeability through the intestinal epithelium;
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stimulating chylomicron secretion, which results in enhanced drug uptake through the lymphatic pathway, bypassing initial metabolism in the liver.
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Medium chain lipids (C<12) diffuse across the enterocyte directly into blood vessels. Long unsaturated chain lipids (C18:1, C18:2) are absorbed via the lymphatic pathway.
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Ethanol-resistant ethylcellulose/guar gum coatings – importance of formulation parameters
\n
In vitro digestion of the self-emulsifying lipid excipient Labrasol® by gastro-intestinal lipases and influence of its colloidal structure on lipolysis rate
\n
Ethanol-resistant polymeric film coatings for controlled drug delivery
Compartmentalization of the human stratum corneum by persistent tight junction-like structures
\n
\n"},{"wysiwyg":"
2010
\n
\n
Diluent effects on drug release from sustained release Compritol® 888 ATO tablets
\n
Gastro-intestinal lipolysis of lipid-based excipients intended for oral drug delivery of poorly water soluble drugs
\n
Specific assay of carboxyl ester hydrolase using PEG esters as substrate
\n
An investigation into the mechnism of dissolution rate enhancement of poorly water soluble drugs from spray chilled Gelucire® 50/13 microspheres
\n
\n"},{"wysiwyg":"
2009
\n
\n
Lauroyl polyoxylglycerides, functionalized coconut oil, enhancing the bioavailability of poorly soluble active substances
\n
Vaginal cream formulation for the prevention of HIV infection for women in developing countries
\n
In vitro gastrointestinal lipolysis of four formulations of piroxicam and cinnarizine with the self-emulsifying excipients Labrasol® and Gelucire® 44/14
\n
Influence of drug polarity upon the solid-state structure and release properties of self-emulsifying drug delivery systems in relation with water affinity
Bibliography on Gattefossé’s products. 2004-2005 review.
\n
\n
Systèmes auto-emulsionnables et émulsions sèches [Self emulsifying drug delivery systems]
\n
\n"},{"wysiwyg":"
2004
\n
\n
Structural and thermal characterization of lipidic excipients and carriers by X-ray diffraction coupled to differential microcalorimetry
\n
Structural and thermal characterization of mono and diacyl polyoxyethylene glycol by infrared spectroscopy and X-ray diffraction coupled to differential calorimetry
\n
\n"},{"wysiwyg":"
2003
\n
\n
Enhanced bioavailability of simvastatin in a self-emulsifying drug delivery system (SMEDDS)
Ethanol-resistant ethylcellulose/guar gum coatings – importance of formulation parameters
\n
In vitro digestion of the self-emulsifying lipid excipient Labrasol® by gastro-intestinal lipases and influence of its colloidal structure on lipolysis rate
\n
Ethanol-resistant polymeric film coatings for controlled drug delivery
Lauroyl polyoxylglycerides, functionalized coconut oil, enhancing the bioavailability of poorly soluble active substances
\n
Vaginal cream formulation for the prevention of HIV infection for women in developing countries
\n
In vitro gastrointestinal lipolysis of four formulations of piroxicam and cinnarizine with the self-emulsifying excipients Labrasol® and Gelucire® 44/14
\n
Influence of drug polarity upon the solid-state structure and release properties of self-emulsifying drug delivery systems in relation with water affinity
Structural and thermal characterization of lipidic excipients and carriers by X-ray diffraction coupled to differential microcalorimetry
\n
Structural and thermal characterization of mono and diacyl polyoxyethylene glycol by infrared spectroscopy and X-ray diffraction coupled to differential calorimetry
\n","link":""}]},"_links":{"self":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/3753"}],"collection":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/users/9"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/comments?post=3753"}],"version-history":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/3753/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/media?parent=3753"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/categories?post=3753"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/tags?post=3753"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"olivine":{"id":1682,"date":"2017-04-17T12:23:41","date_gmt":"2017-04-17T12:23:41","guid":{"rendered":"/?page_id=1682"},"modified":"2019-05-03T15:26:15","modified_gmt":"2019-05-03T13:26:15","slug":"olivine","status":"publish","type":"page","link":"https://www.gattefosse.com/personal-care-actives/olivine/","title":{"rendered":"Oli’Vîne™"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":36,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"Oli'Vîne™ | Energizing mineral active | Gattefossé","_yoast_wpseo_metadesc":"Oli’Vîne™ is an energizing magnesium complex that helps skin cells fight stress, and simultaneously oxygenates and energizes the skin."},"categories":[6],"tags":[],"acf":{"component":"PageCosmeticProduct","product_codes":[{"code":"5779"}],"bandeau_image":{"id":13772,"alt":"","title":"Olivine","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine.jpg","width":1144,"height":400,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-300x105.jpg","medium-width":300,"medium-height":105,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-768x269.jpg","medium_large-width":474,"medium_large-height":166,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-1024x358.jpg","large-width":474,"large-height":166,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-672x372.jpg","post-thumbnail-width":672,"post-thumbnail-height":372,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/Olivine-1038x400.jpg","twentyfourteen-full-width-width":1038,"twentyfourteen-full-width-height":400}},"image_product_finder":{"id":2681,"alt":"Rock climber gathering strength to climb higher while he is hanging from mountain, secured by a climbing rope.","title":"Olivine","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","width":244,"height":163,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","medium-width":244,"medium-height":163,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","medium_large-width":244,"medium_large-height":163,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","large-width":244,"large-height":163,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","post-thumbnail-width":244,"post-thumbnail-height":163,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/olivine-1.jpg","twentyfourteen-full-width-width":244,"twentyfourteen-full-width-height":163}},"title":"Oli'Vîne™","tagline":"Energizing mineral complex","description_product_finder":"","introduction":"
Nature is a constant inspiration for cosmetics ingredients, but plants are not the only sources of natural actives. Mineral Matters™ liquid stone extracts apply special technology to extract important minerals from precious stones and make them bioavailable to the skin. The result is a unique line of substantiated stone actives that enhance and protect. Oli’Vîne™ is an energizing magnesium complex extracted from peridot. It increases cellular activity, helps skin cells fight stress, and simultaneously oxygenates and energizes the skin for an antiaging, antistress effect. See the other actives in this Mineral Matters™ line:
Peridot is an ancient gemstone. An earlier term for it was chrysolite, whose Greek roots mean “golden stone,” an allusion to its gold-green brilliance. Peridot was also used in Egyptian jewelry dating to the time of the pharaohs.
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\n
Oxygenating
\n
Energizing
\n
Combats cutaneous stress
\n
Helps fight dull, tired skin
\n
\n","applications":"
\n
Anti-fatigue day cream
\n
Fash radiance skin care
\n
Anti-stress youth masks
\n
Energizing body lotion
\n
\n","actives":["energizing"],"actives_secondary":["alcohol_free","bg_free"],"textures":"","textures_secondary":"","extract":false,"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false},"_links":{"self":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/1682"}],"collection":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/users/36"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/comments?post=1682"}],"version-history":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/1682/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/media?parent=1682"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/categories?post=1682"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/tags?post=1682"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"emulium-dolcea-mb":{"id":21135,"date":"2020-10-07T10:05:42","date_gmt":"2020-10-07T08:05:42","guid":{"rendered":"https://www.gattefosse.com/?page_id=21135"},"modified":"2021-07-05T14:20:50","modified_gmt":"2021-07-05T12:20:50","slug":"emulium-dolcea-mb","status":"publish","type":"page","link":"https://www.gattefosse.com/fr/personal-care-textures/emulium-dolcea-mb/","title":{"rendered":"Emulium® Dolcea MB"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":24,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"Emulium® Dolcea MB | Émulsionnant multifonctionnel | Gattefossé","_yoast_wpseo_metadesc":"Emulium® Dolcea MB est un émulsionnant H/E sans PEG, 100% d’origine naturelle, facile à formuler et flexible qui crée des textures fluides comme des beurres épais."},"categories":[14],"tags":[],"acf":{"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false,"component":"PageCosmeticProduct","product_codes":[{"code":"5898"}],"bandeau_image":{"id":21138,"alt":"","title":"1144x400px","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px.jpg","width":1144,"height":400,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-300x105.jpg","medium-width":300,"medium-height":105,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-768x269.jpg","medium_large-width":474,"medium_large-height":166,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-1024x358.jpg","large-width":474,"large-height":166,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-672x372.jpg","post-thumbnail-width":672,"post-thumbnail-height":372,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/1144x400px-1038x400.jpg","twentyfourteen-full-width-width":1038,"twentyfourteen-full-width-height":400}},"image_product_finder":{"id":21139,"alt":"","title":"244x163px","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","width":244,"height":163,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","medium-width":244,"medium-height":163,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","medium_large-width":244,"medium_large-height":163,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","large-width":244,"large-height":163,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","post-thumbnail-width":244,"post-thumbnail-height":163,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/244x163px.jpg","twentyfourteen-full-width-width":244,"twentyfourteen-full-width-height":163}},"title":"Emulium® Dolcea MB","tagline":"Soft by nature","description_product_finder":"","introduction":"
Emulium® Dolcea MB est un émulsionnant H/E sans PEG, 100% d’origine naturelle, facile à formuler et flexible qui crée des textures fluides comme des beurres épais.
\n
Emulium® Dolcea MB est parfaitement compatible avec les ingrédients cosmétiques et apporte une excellente stabilité en combinaison avec des agents gélifiants naturels.
\n
Avec son pouvoir hydratant immédiat et long-terme, cet ingrédient apporte de la fonctionnalité et de l’efficacité à une large gamme d’applications.
\n
Doté d’une signature sensorielle forte, il apporte une douceur extrême aux émulsions cosmétiques. Approuvé COSMOS, Emulium® Dolcea MB peut être utilisé dans des formulations certifiées bio, véganes et facilement biodégradables.
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Gattefossé a poussé les limites de sa technologie brevetée des beurres de cires pour développer la version la plus aboutie et robuste de ses émulsionnants naturels, Emulium® Dolcea MB.
\n
Les cires de jojoba et de tournesol utilisées dans Emulium® Dolcea MB réagissent avec du polyglycérol végétal pour créer un émulsionnant H/E 100% d’origine naturelle, qui apporte des propriétés hydratantes grâce aux cires végétales et une identité sensorielle unique.
Emulium® Dolcea MB peut être ajouté à la phase huileuse de préférence, ou à la phase aqueuse si nécessaire. Robuste, il est capable d’émulsionner et de stabiliser des émulsions contenant jusqu’à 40% de phase huileuse. Sous forme de pastilles, il est très facile à utiliser, ne nécessite pas d’agitation forte et permet la création d’émulsions très fines (5-10µm).
Avec Emulium® Dolcea MB, notre émulsionnant naturel le plus robuste, plusieurs process peuvent être utilisés pour répondre à différentes contraintes. Regardez cette vidéo pour découvrir chacun d’eux ainsi que leurs bénéfices !
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Pouvoir hydratant immédiat et long-terme:
\n
\n
Améliore significativement l’hydratation de la peau comparé à un émulsionnant avec PEG
\n
La peau est hydratée jusqu’à 48 heures
\n
Le niveau d’hydratation de la peau est amélioré sur l’ensemble du visage
\n
\n
\n","img":{"id":21144,"alt":"","title":"Close up of woman's face with freckles","caption":"Close up of woman's face with freckles","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2020/10/gettyimages-1023927920-170667a.jpg"},"video":""},{"content":"
Biodégradabilité :
\n
\n
La composition d’Emulium® Dolcea MB a été soigneusement choisie pour assurer une excellente biodégradabilité
\n
97% de la crème testée contenant Emulium® Dolcea MB a été biodégradée après seulement 28 jours
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Rectal route in the 21st century to treat children.
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Advanced Drug Delivery Reviews, 73 34-49. doi: 10.1016/j.addr.2014.05.012
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Selecting efficient pharmaceutical binder for developing robust extended release matrices of Compritol ® 888ATO prepared using wet granulation technique
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Part 1 Studying impact on granule & tablet properties
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This study evaluates the binding efficiency of four commonly used pharmaceutical binders to hold hydrophilic API’s of different solubilities with hydrophobic, waxy ER matrices of Compritol ® 888 ATO as sustained release agent by studying their impact on the granule and tablet properties formulated using the same.
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K. Deshmukh, A. Shrivastava, S. Banerjee, R. Tiwari, S. Bambarkar, N. Farah
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This study evaluates impact of four pharmaceutical binders on dissolution profile of ER tablets of different API’s formulated using Compritol ® 888 ATO as sustained release agent
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