水飞蓟宾自微乳给药系统的体内外评价

水飞蓟宾自微乳给药系统的体内外评价

李馨儒, 裴宇盛, 黄燕清, 周艳霞, 张雨辰, 刘艳^*

1. 北京大学药学院药剂学系, 北京 100191
2. 中国药品生物制品检定所药理室, 北京 100050
3. 北京大学药学院药学教学实验中心, 北京 100191

收稿日期:2009-07-30 修回日期:2009-10-15 出版日期:2009-11-30 发布日期:2009-11-30
通讯作者: 刘艳*

In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for silybin

Xin-Ru Li, Yu-Sheng Pei, Yan-Qing Huang, Yan-Xia Zhou, Yu-Chen Zhang, Yan Liu^*

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
2. Division of Pharmacology, National Institute for the Control of Pharmaceutical and Biological Products, Beijing 100050, China
3. Pharmaceutical Teaching Laboratory Center, Peking University, Beijing 100191, China

Received:2009-07-30 Revised:2009-10-15 Online:2009-11-30 Published:2009-11-30
Contact: Yan Liu*

摘要/Abstract

摘要： 本文为提高难溶性药物水飞蓟宾的口服吸收, 以亚油酸乙酯、聚氧乙烯蓖麻油和聚乙二醇400为处方制备自微乳化给药系统, 并对其理化性质和生物利用度进行评价。体外释放实验和分散实验结果表明自微乳化给药系统相对于市售品可显著提高药物溶出和释放速度; 体内实验表明, 自微乳化给药系统的药时曲线下面积 (AUC)和达峰浓度都明显高于市售品, 生物利用度为市售品的2.3倍。这些实验结果表明自微乳化给药系统可用于难溶性药物的口服吸收。

关键词: 自微乳化给药系统, 水飞蓟宾, 微乳, 生物利用度

Abstract: To enhance the oral absorption of the poorly water-soluble drug silybin, a self-microemulsifying drug delivery system (SMEDDS) composed of ethyl linoleate, Cremophor EL and PEG 400 for oral administration of silybin was formulated, and its physicochemical properties and bioavailability of silybin were evaluated. The in vitro release of silybin from microemulsion and dispersion of silybin from SMEDDS were significantly faster than those from the commercial silybin hard capsule, respectively. The area under the drug concentration-time curve (AUC) and the mean maximum plasma level (Cmax) of the SMEDDS were remarkably greater than those of the hard capsule after oral administration to rats. The absorption of silybin formulated in SMEDDS exhibited a 2.3-fold increase in bioavailability as compared with the hard capsule. These results demonstrated that SMESDDS might be a useful drug delivery system for the oral delivery of the poorly water-soluble drug silybin.

Key words: Self-microemulsifying drug delivery system, Silybin, Microemulsion, Bioavailability

中图分类号:

R945

Supporting: ^*Corresponding author. Tel.: 86-10-82801508; e-mail: yanliu@bjmu.edu.cn

李馨儒, 裴宇盛, 黄燕清, 周艳霞, 张雨辰, 刘艳^*. 水飞蓟宾自微乳给药系统的体内外评价[J]. .

Xin-Ru Li, Yu-Sheng Pei, Yan-Qing Huang, Yan-Xia Zhou, Yu-Chen Zhang, Yan Liu^*. In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for silybin[J]. .

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