Spécialisé dans le développement, la fabrication et la commercialisation d’ingrédients cosmétiques et d’excipients pharmaceutiques, le groupe Gattefossé explore ce que la nature et la science ont de meilleur à offrir depuis 1880.
Poor solubility, poor permeability, and pre-systemic elimination are factors that can limit absorption of somedrugs. Lipid excipients have the capability to overcome these hurdles and enhance oral bioavailability throughdifferent mechanisms.
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How to develop lipid-based formulation?
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An optimized LBF enables solubilization of the entire therapeutic dose andmaintains the drug in solubilized state throughout the digestion process.
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To speed up LBF development, we have produced tools to guide you at each stageof development:
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1 – methods for saturation solubility screening
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2 – database of solubility of drugs in common pharmaceutical excipients
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3 – methods for miscibility and dispersability testing
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4 – miscibility table
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5 – in vitro lipolysis procedure
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6 – guideline for preclinical studies
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What are the different types of lipid-based formulations?
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Depending on their composition, LBF exhibit different in vivo behaviors. They typically consist of biocompatible excipients falling into four main categories: oils, low-HLB surfactants, high HLB surfactants and co-solvents. To facilitate their identification, Poutonet al. introduced the Lipid Formulation Classification System based on the composition, size of the droplets generated after the dispersion of the formulation in aqueous media, and the impact of natural lipid digestion process on the in vivo performance of the formulation classes.
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What functional excipients for oral bioavailability enhancement do Gattefossé deliver?
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Our range of functional excipients includes oils, low HLB surfactants, high HLB surfactants and solvents. They can be combined to formulate all types of lipid-based formulations
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What are self-emulsifying formulations?
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Self-emulsifying lipid formulations form emulsions upon contact with aqueous fluids without the need for mechanical or thermal energy.The size of the dispersion depends on the composition of excipients in the formulation.
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How to use lipid excipients and lipid-based formulations in early stage development?
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A vehicle or formula intended for preclinical studies must allow adequate administration of the test compound with little or no effect on the test species. The vehicle or formulation must be suitable for the intended route of administration, maintain the stability of the active ingredient, and preferably, maximize the systemic bioavailability of the drug. Lipid excipients provide a solution to these challenges and have proven utility in preclinical studies. Further information is available from Gattefossé guideline
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Exposed to environmental stress, the skin’s barrier function is altered, facilitating the penetration of irritants, and increasing Trans Epidermal Water Loss (TEWL). As a result, the skin becomes dry and presents sensitivity, associated with redness and a stinging sensation. There is a growing need for mild, soothing texture ingredients that reduce skin sensitivity to aggression and enable the use of skincare and make-up products without reaction and discomfort.
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Emulium® Dermolea MB, an O/W emulsifier, reduces skin stress and brings long-term soothing thanks to its unique lipidic composition rich in sterols and triterpenes. Highly moisturizing and protective, it is shown to reinforce the skin barrier function. Used at up to 4%, it is suitable for all skin types, in both humid and dry climates.
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Emulium® Dermolea MB was obtained using Gattefossé’s proprietary knowledge on the wax butter technology. Candelilla wax, rice bran wax, and jojoba wax have been selected for their complementary properties and functionalized with polyglycerol-3.
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Composed of plant lipids close to those of the skin’s surface, rich in anti-inflammatory pentacyclic triterpenes and sterols, Emulium® Dermolea MB forms a fine skin-compatible film, proven to reduce environmental skin stress. Highly moisturizing and protective, it reinforces the skin barrier function and brings long-term soothing.
Capable of emulsifying oil phases up to 40%, Emulium® Dermolea MB can create sprays to thick butters suitable for skin care, suncare, makeup and hair/scalp care. In the form of pellets, it is very easy to formulate and forms stable emulsions. The use of a gelling agent is recommended for better stability, particularly at high temperatures.
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Adapted to all climates:
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Similar sensory profile in temperate and tropical humid conditions
A nonionic water-dispersible surfactant for lipid-based formulations to solubilize and increase oral bioavailability of poorly water-soluble APIs. Self-emulsifies in aqueous media forming a fine dispersion, i.e., microemulsion (SMEDDS).
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Caprylocaproyl Polyoxyl-8 glycerides
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Caprylocaproyl macrogol-8 glycerides
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00BT03FSO2
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PEG-8 CAPRYLIC/CAPRIC GLYCERIDES
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Polyoxylglycerides
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Consists of a small fraction of mono-, di- and triglycerides and mainly PEG-8 (MW 400) mono- and diesters of caprylic (C8) and capric (C10) acids
Solubilizer for poorly-soluble APIs and bioavailability enhancer. Single excipient formulation system: self-emulsifies in aqueous fluid into microemulsion—LFCS Type III (SMEDDS). High purity guaranteed for stability and capsule compatibility. Safety of use is inferred by extensive toxicological data and precedence of use in approved pharmaceutical products.
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A glyceride with an intermediate melting point used as a lipidic vehicle and modified release agent.
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Mono and Diglycerides
\n"},{"keys":"EP Name","value":"
Glycerol Monostearate 40-55 (Type I)
\n"},{"keys":"UNII Code (FDA)","value":"
KC98RO82HJ
\n"},{"keys":"Preferred Substance Name (FDA)","value":"
Glyceryl Monostearate
\n"},{"keys":"Handbook of Pharmaceutical Excipients","value":"
Glyceryl Monostearate
\n"},{"keys":"Chemical description","value":"
Consists of mono-, di- and triesters of palmitic (C16) and stearic (C18) acids
Modified release matrix former for capsule. Coating agent for taste masking. Consistency agent. Safety of use is inferred by GRAS status and precedence of use in approved pharmaceutical products.
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publications"},"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":"An exhaustive list of all the scientific publications from Gattefossé experts","_yoast_wpseo_metadesc":"Find out the scientific articles and posters written by our pharmaceutical scientists about lipid-based excipients and formulation technologies."},"categories":[63],"tags":[],"acf":{"component":"Brochures","title":"Gattefossé publications","introduction":"Find below the list of all publications (articles and posters) of Gattefossé scientists.Posters are available to download after log-in.","":false,"content":[{"wysiwyg":"
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/about-us/wp-json/wp/v2/pages/3753"}],"collection":[{"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/users/9"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/comments?post=3753"}],"version-history":[{"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/pages/3753/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/media?parent=3753"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/categories?post=3753"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/about-us/wp-json/wp/v2/tags?post=3753"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"publications-solid-lipid-nanoparticles":{"id":6592,"date":"2017-10-03T11:32:31","date_gmt":"2017-10-03T09:32:31","guid":{"rendered":"https://www.gattefosse.com:443/?page_id=6592"},"modified":"2022-03-16T13:20:33","modified_gmt":"2022-03-16T11:20:33","slug":"publications-solid-lipid-nanoparticles","status":"publish","type":"page","link":"https://www.gattefosse.com/fr/pharmaceuticals-special-content/publications-solid-lipid-nanoparticles/","title":{"rendered":"Publications on solid lipid nanoparticles"},"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 solid lipid nanoparticles | Gattefossé","_yoast_wpseo_metadesc":"Find out Gattefossé publications on solid lipid nanoparticles."},"categories":[36],"tags":[],"acf":{"component":"PageSpecialContentPharma","title":"Publications on solid lipid nanoparticles","introduction":"","":false,"content":[{"wysiwyg":"
Lipid-based nanocarriers for oral delivery of peptides
Solid lipid Nanocarriers diffuse effectively through mucus and enter intestinal cells – but where is my peptide?
\n
Camille Dumont, Ana Beloqui, Cédric Miolane, Sandrine Bourgeois, Véronique Préat, Hatem Fessi, Vincent Jannin
\n
International Journal of Pharmaceutics, Volume 586, 30 August 2020
\n
This study aimed to evaluate the potential of Hydrophobic Ion Pairing combined with Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) to improve peptide transport across the intestinal border using Caco-2 cell monolayers (enterocyte-like model) and Caco-2/HT29-MTX co-cultured monolayers (mucin-secreting model).
\n
This study showed that hydrophobic ion pairing enabled high encapsulation efficiency of peptide in SLN and NLC. The lipid-based nanocarriers were highly internalized by Caco-2 cell monolayers and were able to cross the mucus barrier (Caco-2/HT29-MTX cell model). However, the peptide intestinal transport was limited by an extensive release from the carriers.
Solid lipid nanocarrier development toolbox for increasing oral bioavailability of API
\n
Dr Camille Dumont
\n
American Pharma Review, May-June 2020 issue, pp 69-75
\n
In this comprehensive article, the author describes the latest tools available to develop solid lipid nanoparticles: how to prepare and characterize solid lipid nanoparticles, how to evaluate encapsulation efficiency and intestinal permebility.
Journal of Drug Delivery Science and Technology (article in press)
\n
In this study, the authors developed a protocol to produce reproducible solid lipid nanoparticles by high pressure homogeneization. The possibility to encapsulate peptides was also investigated.
In-vitro evaluation of solid lipid nanoparticles: Ability to encapsulate, release and ensure effective protection of peptides in the gastrointestinal tract
\n
Camille Dumont, Sandrine Bourgeois, Hatem Fessib, Pierre-Yves Dugas, Vincent Jannin
\n
International Journal of Pharmaceutics, Volume 565, 30 June 2019, Pages 409-418
In vitro evaluation of leuprolide-containing solid lipid-based nanosuspensions: ability to encapsulate, release, protect and permeate in the gastrointestinal tract
\n
Dumont C., Jannin V., Beloqui A., Préat V., Fessi H.c, Bourgeois S.
\n
In this study the authors obtained solid lipid nanoparticles using high pressure homogeneization, in which leuprolide was included as an ion pair. The nanoparticles were shown to be internalized by Caco-2 and Caco-2/HT29-MTX cell monolayers.
Evaluation of the digestibility of solid lipid nanoparticles of glyceryl dibehenate produced by two techniques: Ultrasonication and spray-flash evaporation
\n
Published online October 2017
\n
European Journal of Pharmaceutical Sciences , Volume 111, 1 January 2018, Pages 91-95
\n
In this study, solid lipid nanoparticles (SLN) of glyceryl dibehenate are produced by two methods and evaluated for digestion using the in vitro lipolysis test.
\n
\n
By ultrasonication, SLN have a mean particle size of 180 nm and showed a limited digestion by lipase.
\n
By spray-flash evaporation, SLN particle size ranges from 235 to 411 nm, depending on process conditions and were not digested by lipase.
\n"}],"content_not_translated":false,"equivalent_fr":false,"equivalent_en":false},"_links":{"self":[{"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/pages/6592"}],"collection":[{"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/users/9"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/comments?post=6592"}],"version-history":[{"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/pages/6592/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/media?parent=6592"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/categories?post=6592"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/fr/wp-json/wp/v2/tags?post=6592"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"excipients-for-lubrication":{"id":3558,"date":"2017-04-27T14:05:33","date_gmt":"2017-04-27T14:05:33","guid":{"rendered":"https://www.gattefosse.com:443/?page_id=3558"},"modified":"2019-05-13T17:46:45","modified_gmt":"2019-05-13T15:46:45","slug":"excipients-for-lubrication","status":"publish","type":"page","link":"https://www.gattefosse.com/pharmaceuticals-content/excipients-for-lubrication/","title":{"rendered":"Excipients for lubrication"},"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 Lubrication | Range of lipid-based lubricants | Gattefossé","_yoast_wpseo_metadesc":"Discover our range of lipid-based lubricants to help you formulate challenging pharmaceutical and nutraceutical tablets and capsules."},"categories":[49],"tags":[],"acf":{"component":"PageGenericContentPharma","title":"Excipients for lubrication","content":"
During tablet and capsule production, lubricants are necessary to improve powder flow and reduce friction and adherence. Lubrication is a critical step since over- or underlubrication is responsible for many production and quality issues. Therefore, lubricant type, quantity, and conditions of use are critical parameters to take into account when developing a formulation.
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Advantages of Gattefossé lubricants:
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Gattefossé lubricants are recommended for challenging formulations. They are also able to resolve production and quality issues due to these qualities:
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chemical inertness: no reactive groups and no incompatibility with APIs or other excipients
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robustness: resistant particles of homogeneous size ensure constant surface area; mixing time and speed do not change the quality of the lubrication or tablet properties
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effective lubrication that preserves tablet attributes: hardness, disintegration time, and drug release
improved powder blend flow due to glidant properties
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recommended for use at proportion 1%–3% (w/w)
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GRAS status and precedence of use with many APIs (FDA IID)
\n
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\n W/O Meets Market Trends
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W/O (water-in-oil) emulsions are becoming more and more preferred in the personal care space, particularly regarding color cosmetics and sun care. In color cosmetics, W/O foundations offer better water resistance, long-wear, and high coverage – all the performance qualities a consumer desires – compared to O/W (oil-in-water) formulations. And though W/Si (water-in-silicone) formulations may offer great performance and texture, they do not qualify as natural makeup, making them a less desirable option among younger shoppers. When it comes to sun care, consumers are moving towards mineral options. Sunscreen launches containing zinc oxide increased by 45% from 2014-15 to 2018-19 in North America(1). Zinc oxide is easier to formulate in a W/O than an O/W system. In fact, most inorganic sunscreens are either anhydrous or W/O formulations.
\n
However, formulating can be easier said than done, as there are many challenges that come with making a stable W/O product. W/O systems are more sensitive to other ingredients and require more energy in their processing to ensure stability. There are two key factors to consider when it comes to W/O formulation: oil polarity and electrolyte addition, which may not have any influence or not even be necessary for O/W formulations.
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Oil Polarity
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\n
\n The emulsifier you choose has distinctive characteristics that will help you determine the profile of your other ingredients. One trait to consider, that is often overlooked, is polarity. If you are using a more polar emulsifying agent, then your oil phase should consist of more polar oils. Some medium to high polarity oils include C12-15 alkyl benzoate, caprylic/capric triglycerides, octyldodecyl myristate, castor oil, and coco-glycerides, among countless others. On the other hand, if the emulsifier is not very polar, then your oil phase should be more comprised of apolar oils, such as alkanes like squalane, or undecane, tridecane, or silicones if preferred.
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Electrolytes Are Included
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\n
\n The stability of W/O emulsions can be improved by adding a proper concentration of inorganic salts, such as CaCl2, NaCl, MgCl2, and MgSO4, in the aqueous phase(2). Adding salts to a W/O emulsion inhibits Ostwald ripening, which is where smaller droplets diffuse and deposit themselves onto larger droplets.
\n
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\n Inorganic salts can also lower the interfacial tension at an oil-water interface, thereby improving stability against coalescence and sedimentation(2).
\n
\n
\n Attractive forces exist within the dispersed phase and can increase their collision frequency(2). This can lead to either coalescence or sedimentation. However, by adding electrolytes to the system, you can lower the attractive forces between water droplets to ensure stability.
\n
Needless to say, electrolytes are absolutely necessary to ensure a stable formula, maintaining the smaller droplet sizes in a consistent, even dispersion.
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Easy to Use Emulium® Illustro
\n
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Emulium® Illustro is Gattefossé’s gold-winning, naturally derived, high performing, W/O emulsifier that can help you create a natural, stable, and sensorial make-up, sun care, or skincare product! You will notice that this ingredient has a very large, polar head group and long lipophilic chains that also have polar bonds, as seen by the hydroxide and ester groups:
\n
\n
Because of these polar properties, Emulium® Illustro is more compatible with medium to high polarity oils. But since we’ve engineered this ingredient to be highly compatible and flexible, you may still incorporate apolar oils at certain percentage levels. And as for electrolytes, our R&D team found this ingredient to work very well with 2% MgSO4 or 1% of MgSO4 and NaCl. Check out this video to see how you can make a 2-min emulsion using Emulium® Illustro!
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(1) Mintel GNPD
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(2) Qiaomei Zhu, Yijun Pan, Xin Jia, Jinlong Li, Min Zhang, Lijun Yin. Review on the Stability Mechanism and Application of Water‐in‐Oil Emulsions Encapsulating Various Additives. (2019)
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Identify easily the excipients you need with a (multi) criteria search. Alternatively, search by pharmacopoeia name, FDA IID preferred substance name or UNII code using the keyword tool.
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As the skin ages, a progressive disorganization of the dermal structure occurs and is responsible for reduced firmness and tonicity. Face and body contours lose their definition, décolleté and neck areas become wrinkled.
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Gatuline® In-Tense MB is an active ingredient of natural origin that acts deeply in the skin, in the extra-cellular matrix. By stimulating fibroblasts’ activity, it provides support to the collagen fiber network and restores firmness and smoothness of the face and the body.
Gatuline® In-Tense MB is a concentrated oily extract taken from the flower of the Acmella Oleracea plant also called Paracress or “Brède mafane”, a traditional spicy condiment. Acmella Oleracea is renowned for its high content in alkylamides, markers of the plant activity.
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Special attention is given to a selective harvest of the flowers (upper buds only), so that the plant can be used by local population for other applications, especially for cooking.
Oily phase for topical formulations. Oily vehicle and solubilizer for solutions. Safety of use is inferred by substantial toxicological data and precedence of use in approved human and veterinary pharmaceutical products.
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Modified- or sustained-release matrices are designed to release a drug slowly over an extended period of time. Formulations must be robust to ensure drug release over time and avoid dose-dumping. Lipid-based matrices are water-insoluble and do not swell or erode when in contact with aqueous media. When used as sustained-release agents, they form an inert matrix from which the drug diffuses slowly.
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Advantages of Gattefossé’s modified-release agents:
\n
• Drug release is a function of diffusion, which enables simple product design and offers both straightforward modulation of drug release and high reproducibility. • Tablets are biopharmaceutically robust as the lipid matrix is not sensitive to physiological variations (e.g., pH, digestive processes, alcohol level). • Agents are suitable for a wide range of processing techniques, including direct compression, granulation, melt coating, hot melt extrusion, and capsule molding.
finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
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used at proportion of 10%–40%, depending on drug solubility and diluent properties
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suitable for direct compression, granulation, and hot processes (i.e., hot melt coating, granulation, and extrusion)
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crystalline material with narrow melting range (∼70 °C) and rapid recrystallization, ideal for hot melt processes
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GRAS status and precedence of use with many APIs (FDA IID)
\n
\n
We can provide technical guidelines that offer useful tips on SR formulation development and numerous case studies with model drug molecules, e.g., bupropion HCl, levodopa, metformin HCl, metoprolol succinate, niacin, and theophylline.
finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
\n
crystalline material with narrow melting range (∼55 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
\n
GRAS status and precedence of use with many APIs (FDA IID)
crystalline material with narrow melting range (∼60 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
\n
GRAS status and precedence of use with many APIs (FDA IID)
\n
\n
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Some APIs present poor organoleptic properties; therefore, taste or odor need to be masked. Others are sensitive to water, oxidation, or temperature and need to be protected to maintain stability. Certain lipid excipients are used in melt processes to effectively protect the API from degradation or mask taste and odor.
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Advantages of Gattefossé’s taste-masking and API protection agents:
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• thermoplastic behavior conducive to processes used (high shear coating, hot melt coating, granulation, extrusion, and capsule molding) • solvent-free process • chemically inert—highly compatible with other excipients in the formulation • plastic deformation for high resistance to compaction • lipid coating that does not impact bioavailability
lipid excipient with intermediate melting point (43 °C)
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ideal for capsule molding process
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Suppocire® bases comprise chemically stable fatty acid esters with a narrow melting range. Their physicochemical properties provide numerous formulation and manufacturing advantages, including optimized solidification properties and straightforward scale-up with low, medium, and high throughput manufacturing equipment. Careful selection of the right Suppocire® base ensures optimal physicochemical stability and drug delivery properties, as defined by European Pharmacopeia requirements. In addition, Suppocire® formulations are usually simple binary mixtures of the API dissolved or dispersed in the suppository base. They do not require additional excipients to enhance performance, quality, or stability. Step 1: Suppocire® melting Suppocire® pellets are heated at 20 °C above the melting point—indicated in the product technical data sheet—while stirring to ensure the base is thoroughly melted and perfectly homogenized. Step 2: API addition The API is added at a temperature above the recrystallization temperature of the base, generally 30–45 °C. Stirring continues during addition of the API to ensure homogeneity. Step 3: Blister filling The melted, homogenized mixture is poured into the mold at a specific temperature, as determined by a thermorheogram. A thermorheogram plots viscosity versus temperature and allows you to find the optimal mold or blister filling temperature during production. Since viscosity is a function of the specific formulation ingredients, a thermorheogram is necessary for each formulation. Gattefossé has a thermorheogram for each grade of product in the product page section.
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Gattefossé can help you identify the appropriate suppository or pessary base optimized for your API and manufacturing equipment. We also provide advice on formulating to obtain physicochemical stability and performance and solve manufacturing or quality issues. For further information, please contact your local representative.
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This is the simplest process for the production of tablets. It consists of three main steps: powder blending, lubrication, and compression. Atomized lipid excipients are used as lubricants or modified-release agents in direct compression.
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Advantages of lipid excipients in direct compression:
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batch-to-batch composition uniformity, ensuring high quality and performance of final product (adequate for QbD development)
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chemical inertness, preventing incompatibilities with other excipients or with drug
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tablet hardness, resulting in robustness as product is not affected by compression
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Range of functional excipients for direct compression:
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Lubricants to decrease friction between particles and compression tools\n
We can provide technical guidelines on the use of Compritol® 888 ATO as lubricant for challenging pharmaceutical tablets that offer useful tips and numerous case studies.
Compritol® 888 ATO—a well-established sustained-release agent with precedence of use and numerous publicationsdemonstrating efficacy
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We can provide technical guidelines that offer useful tips on SR formulation development and numerous case studies with model drug molecules, e.g., bupropion HCl, levodopa, metformin HCl, metoprolol succinate, niacin, and theophylline.
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Sticking issue
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Sticking during tableting is a relatively common problem. It is often attributable to tooling and machine setup. However, the formulation, active ingredient, and excipients can play an important role. We conducted an in-house study to evaluate the cause of punch adhesion or “sticking,” which occasionally occurs during the compression of powder formulations containing Compritol® 888 ATO. Our study concludes that sticking is primarily due to a combination of factors, including formulation with a “sticky” API and use of ingredients with reduced interparticle bonding capacity.
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Contact Gattefossé for the full study report.
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\n
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Experts en chimie des lipides et en extraction végétale, nous fournissons à nos clients internationaux des produits de qualité et des solutions de formulation innovants. 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