Transepithelial transport of rosuvastatin and effect of ursolic acid on its transport in Caco-2 monolayers

被引：19

作者：

Hua, Wen Jin ^{[1
]}

Fang, Hu Jin ^{[1
]}

Hua, Wei Xiao ^{[1
]}

机构：

[1] Nanchang Univ, Dept Pharm, Affiliated Hosp 1, Nanchang, Peoples R China

来源：

EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS | 2012年 / 37卷 / 03期

关键词：

Rosuvastatin; Ursolic acid; Caco-2 cell monolayers; ADULT MALE-VOLUNTEERS; PHARMACOKINETICS;

D O I：

10.1007/s13318-012-0094-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The aim of this study was to determine transepithelial transport characteristics of rosuvastatin and effect of ursolic acid (P-gp potential inhibitor) and ko143 (ABC transporters selective inhibitor) on its transport in Caco-2 monolayers. A reliable Caco-2 cell monolayers model was established. The TEER value was used to inspect integrity of cell model. Apparent permeability coefficients (Papp(BL-AP) and Papp(AP-BL)) were used to analyze transepithelial transport of rosuvastatin. Uptake of rosuvastatin was time- and concentration-dependent in Caco-2 cell. The ko143 but not ursolic acid had effect on the uptake of rosuvastatin in Caco-2 cell monolayer model and affected apparent permeability coefficient and apparent permeability of rosuvastatin. Active transport and passive diffusion absorption existed in transepithelial transport of rosuvastatin in Caco-2 cell model. Ursolic acid had no effect on transport of rosuvastatin in Caco-2 cell monolayer. The result indicated that ursolic acid may not cause effect on intestinal absorption of rosuvastatin.

引用

页码：225 / 231

页数：7

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