In vitro model for ciclosporin intestinal absorption in lipid vehicles.
The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vitro. The effect of the intestinal lipid digestion was considered on the partition of the drug from olive oil or middle-chain triglyceride (MCT) into phases of simulated intestinal content. The phases obtained after ultracentrifugation were analyzed for their Ciclosporin content and characterized for their lipid classes. For both lipid vehicles the presence of lipolysis products did not promote the partition of the drug into the aqueous phase. The absorption in vivo was not related to the drug amount in the aqueous phase and in the oil phase. Therefore, phase quantification in vitro cannot simulate the dynamics of in vivo absorption events following application of a poorly water-soluble drug in a lipid vehicle.
Reymond
J P
JP
Pharma Development, Sandoz AG, Basel, Switzerland.
Sucker
H
H
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003524:Cyclosporins / Q000493:pharmacokinetics*; D005227:Fatty Acids; D007408:Intestinal Absorption; D008055:Lipids; D008954:Models, Biological; D000069463:Olive Oil; D014677:Pharmaceutical Vehicles; D010938:Plant Oils
D003524:Cyclosporins; D005227:Fatty Acids; D008055:Lipids; D000069463:Olive Oil; D014677:Pharmaceutical Vehicles; D010938:Plant Oils