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

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(英文)

作　　者：全东琴[1] 徐贵霞[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《Journal of Chinese Pharmaceutical Sciences》2005年第2期105-109,共5页中国药学（英文版）

摘　　要：Aim In vitro dissolution test and pharmacokinetics in beagle dogs wereconducted to assess the formulation of tretinoin in self-emulsifying systems. Methods Theconcentrations of tretinoin were determined by HPLC. A crossover study was performed in four fastingbeagle dogs with the formulation of self-emulsifying systems and commercial capsules. Results Theresults showed that the dissolution rate in 15 min of tretinoin in self-emulsifying systems washigher than 80% while that of the commercial capsules was lower than 5% . The area under the plasmaconcentration-time curve (AUC) of the self-emulsifying formulation was significantly higher andC_(max) was approximately two times greater than those of commercial capsule, respectively, Inaddition, the time taken to reach peak was shorter (2 h to 1.25 h) for self-emulsifying formulationof tretinoin. Conclusion The self-emulsifying drug delivery systems.can significantly increasetretinoin in vitro dissolution and in vivo absorption.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：self-emulsifying systems TRETINOIN BIOAVAILABILITY DISSOLUTION 

分 类 号：R965[医药卫生—药理学]