葛根黄酮自微乳化给药系统的体内外评价  

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

作　　者：崔升淼[1] 赵春顺[2] 何仲贵[3] 

机构地区：[1]广东药学院中药学院,广东广州510006 [2]中山大学药学院,广东广州510080 [3]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中药材》2007年第6期684-687,共4页Journal of Chinese Medicinal Materials

摘　　要：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。Objective： To evaluate the self-mieroemulsifying ability and dissolution behavior of pueraria lobata isoflavone in vitro and the pharmaeokinetie behavior in rats. Methods： The self-mieroemulsifying rate was evaluated by the self-mieroemulsifying time and the self-mieroemulsifying efficiency was evaluated by the particle size of resultant mieroemulsions. The plasma concentrations were evaluated by HPLC and dissolution and pharmaeokinetie behavior of self-mieroemulsifying drug delivery systems were evaluated by comparison with commercial tablets. Results ： The system was self-mieroemulsified in 2 rain 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. Con- clusion： The self-microemulsifying drug delivery systems can increase drug dissolution in vitro and absorption in vivo significantly.

关 键 词：葛根黄酮 自微乳化 溶出度 生物利用度 

分 类 号：R943.3[医药卫生—药剂学] R969.1[医药卫生—药学]