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脂质载体中环孢素肠道吸收的体内模型。

In vivo model for ciclosporin intestinal absorption in lipid vehicles.

作者信息

Reymond J P, Sucker H, Vonderscher J

机构信息

Pharma Development, Sandoz AG, Basel, Switzerland.

出版信息

Pharm Res. 1988 Oct;5(10):677-9. doi: 10.1023/a:1015939307478.

Abstract

The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vivo. The model takes into account the effect of the intestinal lipid digestion on the absorption after intraduodenal administration of [3H]Ciclosporin in olive oil or middle-chain triglyceride (MCT) to the bile duct-cannulated rat. Digested vehicles significantly promoted the absorption compared to nondigested vehicles. In the nondigested state, olive oil was a significantly better vehicle than MCT, whereas the difference between both lipids was only a trend in the digested state. Further studies with variants of this in vivo model should determine the influence of abnormalities of fat digestion and absorption on the pharmacokinetics and pharmacodynamics of a drug with a low therapeutical index.

摘要

在体内研究了脂质载体对环孢素肠道吸收的影响。该模型考虑了十二指肠内给予[3H]环孢素于橄榄油或中链甘油三酯(MCT)至胆管插管大鼠后,肠道脂质消化对吸收的影响。与未消化的载体相比,消化后的载体显著促进了吸收。在未消化状态下,橄榄油作为载体明显优于MCT,而在消化状态下,两种脂质之间的差异仅为一种趋势。对该体内模型变体进行的进一步研究应确定脂肪消化和吸收异常对治疗指数低的药物的药代动力学和药效学的影响。

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