和厚朴酚自微乳结冷胶钙微丸的制备及其特性研究  

Preparation and characterization of calcium-gellan beads containing honokiol selfmicroemulsifying drug delivery system

作　　者：甘露[1] 田睿[2] 贾运涛[3] 郭锋[1] 邓萍[1] 张良珂[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆400016 [2]重庆医科大学实验教学中心,重庆400016 [3]重庆医科大学附属儿童医院药剂科,重庆400010

出　　处：《第三军医大学学报》2014年第22期2263-2266,共4页Journal of Third Military Medical University

基　　金：重庆市自然科学基金(CSTC2012jj A10021);高等学校博士学科点专项科研基(20125503120003);重庆市卫生局医学科研项目(2013-2-060);重庆医科大学大学生科研与创新实验项目(201432;201244;201217);重庆市教育委员会科学技术研究项目(KJ120307);海扶之星学生科研基金项目(XS201309)~~

摘　　要：目的制备载和厚朴酚自微乳结冷胶钙微丸(calcium-gellan beads containing honokiol self-microemulsifying drug delivery system,GB-HSMEDDS),研究其特性。方法采用离子凝胶法制备GB-HSMEDDS,以包封率为指标,单因素实验考察结冷胶浓度、钙离子浓度、交联时间、投药量对药物包封率的影响,对优化后的微丸在HCl(p H 1.2)及PBS(p H 6.8)溶液中的溶胀及释放特性进行研究。结果通过优化,选取结冷胶浓度为1.25%,Ca Cl2浓度8%,和厚朴酚自微乳化给药系统(self-microemulsifying drug delivery system,SMGDDS)与结冷胶溶液质量比(g/g)为0.15,交联时间15 min为制备条件,包封率为(64.0±2.8)%,微丸在PBS中的溶胀度大于在HCl溶液中的,药物在HCl溶液中2 h的累积释放超过50%,而在PBS中的不足20%。结论成功制备了含和厚朴酚SMEDDS的结冷胶钙微丸,有望成为SMEDDS固体化的良好载体。Objective To study the preparation and characterization of calcium-gellan beads containing honokiol self-microemulsifying drug delivery system（ GB-HSMEDDS）. Methods GB-HSMEDDS were prepared by ionotropic gelation. With the encapsulation efficiency as indicators,the concentration of gellan gum and Ca^2 ＋,cross-linking time and amount of added drug were selected as variables for single-factor experiment design. The swelling and release characteristics of the beads at p H 1. 2 and 6. 8 were investigated. Results The optimal preparation method included： gellan gum concentration 1. 25%,Ca Cl2 concentration 8%,the weight ratio of honokiol microemulsifying drug delivery system（ SMEDDS） to gellan gum solution 0. 15,and the cross-linking time 15 min. The encapsulation efficiency of GB-HSMEDDS was（ 64. 0 ± 2. 8） %. The swelling degree of GB-HSMEDDS in PBS was greater than those in HCl solution. The cumulative release of honokiol was more than 50% in HCl solution but less than 20% in PBS for 2 h. Conclusion We successfully prepare gellan gum beads containing honokiol SMEDDS,a good carrier for producing solid SMEDDS.

关 键 词：和厚朴酚 自微乳给药系统 结冷胶钙微丸 固体化 

分 类 号：R282.71[医药卫生—中药学] R943[医药卫生—中医学]