鸦胆子油微囊-原位凝胶的制备及体外释药机制的研究

目的制备鸦胆子油微囊-原位凝胶,并探讨其体外释药性能。方法以复凝聚法制备鸦胆子油微囊,并将微囊载于泊洛沙姆407形成的原位凝胶中,采用无膜溶出模型考察其体外溶蚀及释放情况。结果制得的微囊大小均匀,平均粒径为89.399μm,包封率和载药量分别为94.5%～97.4%(n=3)和48.3%～52.6%(n=3);加入微囊后泊洛沙姆407凝胶的相变温度提高了6℃左右,微囊-原位凝胶的体外释药符合Higuchi方程,且持续释放可达96 h以上。结论鸦胆子油微囊-原位凝胶制备方法简便,载药量高,并有一定的缓释作用。

Preparation of Brucea javanica oil microcapsule in situ gel system and its in vitro release mechanism

Objective To prepare Brucea javanica oil microcapsule(BOM) in situ gel system and investigate its in vitro drug releasing properties.Methods BOM was prepared by complex coacervation method.The BOM in situ gel system was prepared by loading microcapsules to Poloxamer 407.A membraneless dissolution model was used to determine in vitro release and gel erosion of BOM in situ gel system.Results The microcapsules were with uniform size and the mean diameter was 89.399 μm.The entrapment efficiency and drug loading of the microcapsules were in the range of 94.5%—97.4%(n = 3) and 48.3%—52.6%(n = 3),respectively.The phase transition temperature of Poloxamer 407 gel loaded by microcapsules increased about 6 ℃.The in vitro release behavior of the BOM in situ gel system exhibited the characteristics of Higuchi equation and the drug could sustained-release for over 96 h.Conclusion It is easy to prepare BOM in situ gel system with suitable formulation.A high drug loading and sustained-release effect could be obtained.