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

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.

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

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 C_ max 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.