Reymond J P, Sucker H
Pharma Development, Sandoz AG, Basel, Switzerland.
Pharm Res. 1988 Oct;5(10):673-6. doi: 10.1023/a:1015987223407.
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.
在体外研究了脂质载体对环孢素肠道吸收的影响。考虑了肠道脂质消化对药物从橄榄油或中链甘油三酯（MCT）分配到模拟肠内容物各相的影响。对超速离心后得到的各相进行环孢素含量分析，并对其脂质类别进行表征。对于两种脂质载体，脂解产物的存在均未促进药物分配到水相中。体内吸收与水相和油相中的药量无关。因此，体外相定量不能模拟在脂质载体中应用难溶性药物后体内吸收事件的动态过程。
