维甲酸自乳化给药系统的体外溶出及比格犬药物动力学研究

维甲酸自乳化给药系统的体外溶出及比格犬药物动力学研究

全东琴^*, 徐贵霞

军事医学科学院毒物药物研究所, 北京 100850;

收稿日期:2004-09-18 修回日期:2005-05-10 出版日期:2005-06-15 发布日期:2005-06-15
通讯作者: 全东琴*

In vitro Dissolution and Pharmacokinetics in Beagle Dogs of a Self-Emulsifying Formulation of Tretinoin

QUAN Dong-qin^*, XU Gui-xia

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China

Received:2004-09-18 Revised:2005-05-10 Online:2005-06-15 Published:2005-06-15
Contact: QUAN Dong-qin*

摘要/Abstract

摘要： 目的评价维甲酸(RA)自乳化释药系统的体外溶出及在比格犬体内的药动学。方法采用HPLC法测定比格犬血浆药物浓度.用四条比格犬交叉实验考察RA自乳化制剂与市售胶囊体内药动学。结果实验表明与市售胶囊剂相比:以水为溶出介质, 维甲酸RA自乳化制剂15 min可以溶出80%以上; 而市售胶囊只溶出不到5%.比格犬体内药动学研究结果表明: 与市售胶囊剂相比, 自乳化制剂达峰时间提前, tmax = 1.25 h 而市售胶囊 tmax = 2 h; 最大血药浓度达到市售胶囊剂的近两倍, AUC(0~∞)提高了67%。结论自乳化制剂可以显著提高RA的体外溶出及体内吸收。

关键词: 自乳化, 自乳化, 自乳化, 维甲酸, 维甲酸, 维甲酸, 生物利用度, 生物利用度, 生物利用度, 溶出, 溶出, 溶出

Abstract: Aim In vitro dissolution test and pharmacokinetics in beagle dogs were conducted to assess the formulation of tretinoin in self-emulsifying systems. Methods The concentrations of tretinoin were determined by HPLC. A crossover study was performed in four fasting beagle dogs with the formulation of self-emulsifying systems and commercial capsules. Results The results showed that the dissolution rate in 15 min of tretinoin in self-emulsifying systems was higher than 80% while that of the commercial capsules was lower than 5%. The area under the plasma concentration-time curve (AUC) of the self-emulsifying formulation was significantly higher and Cmax was approximately two times greater than those of commercial capsule, respectively. In addition, the time taken to reach peak was shorter (2 h to 1.25 h) for self-emulsifying formulation of tretinoin. Conclusion The self-emulsifying drug delivery systems can significantly increase tretinoin in vitro dissolution and in vivo absorption.

Key words: self-emulsifying systems, self-emulsifying systems, tretinoin, tretinoin, bioavailability, bioavailability, dissolution, dissolution

中图分类号:

R969.1

Supporting: ^*Corresponding author. Tel.: 86-10-66931636

全东琴^*, 徐贵霞. 维甲酸自乳化给药系统的体外溶出及比格犬药物动力学研究[J]. .

QUAN Dong-qin^*, XU Gui-xia. In vitro Dissolution and Pharmacokinetics in Beagle Dogs of a Self-Emulsifying Formulation of Tretinoin[J]. .

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