Revolutionizing oral bioavailability: powdered lipid surfactants for tablets and capsules

To answer the rising need for oral solid dosage forms, Gattefossé innovates and creates new grades from its existing surfactants portfolio. Along these new grades, Gattefossé also partnered with PMC Isochem to offer vitamin E TPGS in powder form. Summary of the products and their characteristics is listed in table below.

GSolid™ 50/13 and 48/16 are powders obtained by grinding existing Gelucire® grades: they keep the excellent solubilizing properties of Gelucire®, in addition to being easily used in compression or granulation (wet or dry) processes. A preliminary study focuses on GSolid™ 50/13, the powder grade of Gelucire® 50/13 (stearoyl polyoxyl-32 glycerides), in fenofibrate tablets. Fenofibrate is a BCS class II API, hence needing solubility enhancement. Reference drug in Europe is Lipanthyl®, existing in two different dosages: 67 and 160 mg. A tablet formula was developed by Gattefossé and successful tablets were produced on the Styl’One Nano Compaction Simulator. The tablets were then tested in dissolution in a USP II dissolution bath containing a FeSSIF V2 biorelevant media, at 100 rpm, in 1000 mL. Dissolution of pure fenofibrate, of Lipanthyl® market reference and of a tablet without GSolid™ 50/13 were also performed for comparison. Results below show a rapid dissolution, and a similar if not better dissolution profile than the market reference.

LabraSolid™ products are powders consisting of Labrasol® ALF adsorbed on a mineral carrier: the obtained powdered surfactants act both as solubilizers and intestinal permeation enhancers. In our lab, we tested LabraSolid™ 2 in ticagrelor hard capsules. Ticagrelor is a BCS class IV API, which means it has both low solubility and low permeability. A ticagrelor hard capsule formula was co-developed with Syntegon, equipment manufacturer. Hard capsules were then manufactured using Syntegon’s small batch scale equipment, the GKF 720 automatic capsule filling machine with APD technology and KKE 2500 capsule checkweigher. They showed good processability and weight uniformity across trials. The hard capsules were then tested in dissolution in a USP II dissolution bath containing a FaSSIF V2 biorelevant media, at 50 rpm, in 900 mL. Dissolution of pure ticagrelor and ticagrelor formulated with polysorbate 80 were also performed for comparison. Results below show a 2.5-fold bioavailability enhancement when ticagrelor is formulated with LabraSolid™ 2 hard capsules. LabraSolid™ 2 formula is also better in terms of ticagrelor dissolution compared to the polysorbate 80 formula.