齐墩果酸自微乳化给药系统的制备及其体外溶出度考察

目的:制备齐墩果酸-自微乳化给药系统(OA-SMEDDS)并考察其体外溶出度。方法:以聚氧乙烯(35)蓖麻油等为辅料制备OA-SMEDDS;采用高效液相色谱法测定制剂中OA含量;以0.5%十二烷基硫酸钠为溶出介质、转速100r·min-1、桨法测定制剂的体外溶出度,并与上市OA片剂比较。结果:所制微乳液滴呈圆球形,平均粒径为48.5nm,平均含量为9.29mg·mL-1;OA-SMEDDS软胶囊15min累积溶出度达85%以上,而上市片剂60min时未达60%。结论:与上市片剂相比,SMEDDS显著改善了药物的溶出度,为进一步提高OA制剂的口服生物利用度奠定了基础。

Preparation and in Vitro Dissolution of Oleanolic Acid Self-Microemulsifying Drug Delivery System

OBJECTIVE： To prepare oleanolic acid self-microemulsifying drug delivery system （OA-SMEDDS） and to study its dissolution in vitro. METHODS： OA-SMEDDS was prepared using PEO （35） castor oil as excipients. The content of OA was determined by HPLC. The paddle method was used to detected the in vitro dissolution of preparations with 0.5% sodium lauryl sulfate as dissolution medium at rotation speed of 100 r·min-1. The dissolution of OA-SMEDDS was compared with that of OA tablets on the market. RESULTS： Prepared microemulsion drops assumed as spherosome with mean particle size of 48.5 nm and mean content of 9.29 mg·mL-1. The accumulative dissolution rates of OA-SMEDDS soft capsules at 15 minute were above 85%, while that of tablets on the market were less than 60% at 60 min. CONCLUSION： The dissolution of oleanolic acid is significantly increased with self-microemulsifying drug delivery system as carrier, compared with tablets on the market. It provides a foundation for the improvement of bioavailability of OA.