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.