环孢素A眼用乳剂原位凝胶的制备及体外释放机制考察  

Preparation of cyclosporine A ophthalmic emulsions trapped in situ gels and the release mechanism in vitro

作　　者：李实[1] 伊春芳[1] 王志昆[1] 薛晓[1] 王东凯[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2013年第18期2195-2200,共6页Chinese Journal of New Drugs

摘　　要：目的:制备环孢素A眼用pH敏感型乳剂凝胶并研究其体外释放机制。方法:采用Box-behnken响应面法对乳剂处方进行优化;比较不同比例凝胶组合的流动性及胶凝性确定凝胶处方;建立HPLC法测定制剂的体外释放量,并对其释药机制进行研究。结果:卡波姆与HPMC组成的混合凝胶符合pH敏感型凝胶的要求;该乳剂凝胶在48 h内可以稳定释放,其释放机制为药物扩散和凝胶溶蚀共同作用的结果。结论:环孢素A眼用pH敏感型乳剂凝胶可显著延迟药物释放。Objective： To prepare pH-sensitive cyclosporine A gel emulsions and to research its release mechanism in vitro. Methods ： Prescription of emulsions was optimized by the Box-behnken response surface meth- od. In order to determine the gel compositions suitable for use as in situ gelling, solutions of different concentrations of carbomer and HPMC were prepared to compare their flow ability and gelling capacity. HPLC methods were estab- lished to study the release rate of cyclosporine A gel emulsions in vitro and the drug release mechanism. Results： The mixed gel composed of carbomer and HPMC could be used as pH-sensitive gel, and the emulsions trapped in situ gels could achieve stable release within 48h. The drug release was operated by the combined action of drug dif- fusion and gel erosion. Conclusion： Cyclosporine A emulsions trapped in the gels is sensitive to pH and signifi- cantly delays drug release.

关 键 词：环孢素A 乳剂 pH敏感型凝胶 体外释放 

分 类 号：R943[医药卫生—药剂学] R979.5[医药卫生—药学]