葛根黄酮自微乳化给药系统的体内外评价

目的:研究葛根黄酮自微乳化给药系统的自微乳化能力及在大鼠体内的药动学。方法:通过测定自微乳化所需的时间来评价自微乳化速度,测定自微乳化后药液的粒径来评价自微乳化效率,采用HPLC法测定大鼠血清药物浓度,与市售片剂比较,考察葛根黄酮自微乳化制剂体外溶出行为及体内药动学。结果:体系在2 min内已基本乳化完全,乳化后的粒径在50 nm以下,在水中10 min的溶出度可达90%以上,而愈风宁心片120 min的溶出度不足50%。大鼠体内药动学研究结果表明:与市售片剂相比,自微乳化制剂达峰时间提前,Tmax=15 min,而市售片剂Tmax=29 min;AUC0~∞提高了82%。结论:自微乳化制剂显著提高了葛根黄酮的体外溶出和体内吸收。

Assessment 0f Pueraria lobata isoflavone with Self-microemulsifying Drug Delivery Systems in Vitro and in Vivo

Objective: To evaluate the self-microemulsifying ability and dissolution behavior of pueraria lobata isoflavone in vitro and the pharmacokinetic behavior in rats.Methods: The self-microemulsifying rate was evaluated by the self-microemulsifying time and the self-microemulsifying efficiency was evaluated by the particle size of resultant microemulsions.The plasma concentrations were evaluated by HPLC and dissolution and pharmacokinetic behavior of self-microemulsifying drug delivery systems were evaluated by comparison with commercial tablets.Results: The system was self-microemulsified in 2 min and the particle size was less than 50 nm.The dissolution of SMESC in distilled water was more than 90% at 10 min,while those of the commercial tablet were less than 50% at 120 min.82% increase in the relative bioavailability was observed for the self microemulsifying drug delivery systems compared with Yufengningxin tablets.Tmax was smaller in the self-microemulsifying drug delivery systems compared with Yufengningxin tablets.Conclusion: The self-microemulsifying drug delivery systems can increase drug dissolution in vitro and absorption in vivo significantly.