鸦胆子油微囊-原位凝胶的制备及体外释药机制的-天津中草药杂志社.pdfVIP

·1306 · 中草药 Chinese Traditional and Herbal Drugs 第 43 卷 第 7 期 2012 年 7 月 鸦胆子油微囊-原位凝胶的制备及体外释药机制的研究 1, 2 1 3 1 1 1 陈 钢 ，张 晓 ，卢 刚 ，邵阿丽 ，刘广泉 ，蔡 冰 1. 广东药学院药科学院，广东 广州 510006 2. 广东省药物新剂型重点实验室，广东 广州 510006 3. 上海博爱医院，上海 200031 摘 要：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 89.399 μm ，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。 关键词：鸦胆子油微囊；原位凝胶；体外释放；复凝聚法；无膜溶出模型 中图分类号：R283.6 文献标志码：A 文章编号：0253 - 2670(2012)07 - 1306 - 04 Preparation of Brucea javanica oil microcapsule in situ gel system and its in vitro release mechanism 1, 2 1 3 1 1 1 CHEN Gang , ZHANG Xiao , LU Gang , SHAO A-li , LIU Guang-quan , CAI Bing 1. School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China 2. Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangzhou 510006, China 3. Shanghai Humanity Hospital, Shanghai 200031, China Abstract: 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