荆芥油-苦参素阴道用脂质体温敏凝胶的制备及其性质考察  

Preparation and properties of nepeta oil-oxymatrine lipidosome pro vagina thermosensitive gel

作　　者：张朵朵[1] 吴艳丽[1] 危红华[1] 李莎莎[1] 宋艳丽[1] 郝保华[1] 

机构地区：[1]西北大学生命科学学院,陕西西安710069

出　　处：《中草药》2014年第7期929-934,共6页Chinese Traditional and Herbal Drugs

基　　金：陕西省教育厅产业培育项目(2010JC20);陕西省重点科技创新团队:基于秦巴优势中草药资源的新药创制创新团队(2013KCT-24)

摘　　要：目的制备荆芥油-苦参素(OMT)阴道用脂质体温敏凝胶并考察其体外释放特征。方法以泊洛沙姆407(P-407)和泊洛沙姆188(P-188)为凝胶基质,以凝胶的胶凝温度为考察指标对处方进行优化;复乳法制备OMT脂质体,冷溶法制备荆芥油-OMT阴道用脂质体温敏凝胶;采用HPLC法测定OMT的量,透析法研究荆芥油-OMT脂质体温敏凝胶的体外释放特性。结果温敏凝胶基质最佳处方为18%P-407、5%P-188和0.2%羟丙基甲基纤维素(HPMC),所制备的荆芥油-OMT阴道用脂质体温敏凝胶胶凝温度为(36.8±0.2)℃。体外释放结果显示,荆芥油-OMT阴道用脂质体温敏凝胶24 h内累积释放率为(58.89±0.34)%,48 h内累积释放率为(66.38±0.12)%,具有明显的缓释作用。结论制得的荆芥油-OMT脂质体温敏凝胶具有温敏特性和缓释作用,能有效延缓药物在阴道中的释放速率,提高其在阴道中的滞留时间。Objective To prepare the nepeta oil-oxymatrine （OMT） lipidosome pro vagina thermosensitive gel, and to investigate its in vitro drug release behavior. Methods P-407 and P-188 were used as gel matrix to prepare the gel, and gelatinization temperature was applied as a target to optimize the prescription. The OMT lipidosome was prepared based on the multiple emulsion method, and the nepeta oil-OMT lipidosome pro vagina thermosensitive gel was obtained by cold-dissolving method. The content of OMT was determined by HPLC, and in vitro release properties of nepeta oil-OMT lipidosome thermosensitive in situ gel was investigated by dialysis method. Results After optimization, the gel prescription was finally confirmed as 18% P-407, 5% P-188, and 0.2% hydroxy-propyl methyl cellulose （HPMC）. The gelatination temperature for nepeta oil-OMT lipidosome thermosensitive gel was （36.8 ± 0.2） ℃, and the in vitro accumulating release ratio of sinomenine in the nepeta oil-OMT lipidosome gel system was （58.89 ± 0.34） % and （66.38 ± 0.12） % after 48 h. Conclusion The prepared nepeta oil-OMT lipidosome thermosensitive gel has the temperature sensitivity and sustained release effect, can effectively delay the release of the drug in vagina and improve the residence time inthe vagina.

关 键 词：苦参素 阴道给药 脂质体 温敏凝胶 体外释放度 

分 类 号：R283.6[医药卫生—中药学]