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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15min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=1.25h而市售胶囊tmax=2h;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。
Objective To evaluate the in vitro dissolution of retinoic acid (RA) self-emulsifying drug delivery system and its pharmacokinetics in beagle dogs. Methods HPLC was used to determine plasma drug concentration in beagle dogs. Four Beagle dogs were crossed with each other to examine the pharmacokinetics of RA self-emulsifying formulations and commercial capsules. Results Experiments show that compared with the commercial capsules: water as the dissolution medium, retinoic acid RA self-emulsifying formulations 15min can be dissolved more than 80%; while the commercially available capsules only less than 5%. Beagle dog pharmacokinetic study results show that: compared with the commercial capsules, self-emulsifying formulations peak time ahead, tmax = 1.25h while the commercially available capsules tmax = 2h; the maximum plasma concentration of commercially available capsules near Twice, AUC (0 ~ ∞) increased 67%. Conclusion Self-emulsifying formulations can significantly improve the in vitro dissolution and absorption of RA.