Volume 16, Number 4-5-6, Juillet-Décembre 2009Lipides tropicaux (Actes des Journées Chevreul de l'AFECG 2009)
|Page(s)||267 - 272|
|Section||Nutrition – Santé|
|Published online||15 July 2009|
Lauroyl polyoxylglycerides, functionalized coconut oil, enhancing the bioavailability of poorly soluble active substances
Pharmaceutical R&D, Gattefossé S.A.S., Saint-Priest, 69804, France
Gelucire® 44/14, a lauroyl polyoxylglycerides obtained by polyglycolysis of hydrogenated coconut oil with PEG-32, is used to increase the oral bioavailability of poorly-water soluble drugs. It is a solid dispersion composed of a PEG ester fraction under a lamellar phase of 120 Å with a helical conformation and an acylglycerol fraction under a hexagonal packing. This excipient spontaneously evolves to its most stable phase of 120 Å after storage at 25 °C for 21 hours leading to physically stable formulations. Gelucire® 44/14 is a hydrophilic system that hydrates and swells in contact with water and forms cubic mesophases before complete erosion/emulsification. It is also lipolyzed by various enzymes such as gastric lipase or carboxyl ester hydrolase. After an in vitro gastrointestinal lipolysis simulation, the main components remaining are mono and diesters of PEG-32. These amphiphilic metabolites can explain the beneficial role of Gelucire® 44/14 on the solubility of poorly-water soluble drugs such as cinnarizine even after partial lipolysis of the lipid-based system. Finally that excipient can also increase the bioavailability of active substances by interacting with enterocyte-based proteins like P-glycoprotein or cytochromes P450.
Key words: coconut oil / crystalline structure / emulsification / lauroyl polyoxylglycerides / lipolysis / poorly-water / soluble drug
© John Libbey Eurotext 2009
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