温控型胰岛素液体直肠栓的制备及处方筛选  

Preparation and Prescription Screening of Thermosensitive Insulin Rectal Liquid Suppository

作　　者：肖秋生[1] 杨文慧 姜宗文[1] 肖金宝[1] 

机构地区：[1]解放军第208医院461临床部,长春130021 [2]内蒙古林业总医院,内蒙古牙克石022150

出　　处：《中国药房》2014年第41期3892-3895,共4页China Pharmacy

基　　金：吉林省科技发展计划项目(No.201205033)

摘　　要：目的:制备温控型胰岛素液体直肠栓。方法:以胰岛素含量为指标,以泊洛沙姆407-泊洛沙姆188的比例、壳聚糖含量、p H为因素,采用正交设计试验筛选温控型胰岛素液体直肠栓的处方;并采用无膜、动物黏膜溶出法考察所制栓剂的体外释药机制。结果:所制温控型胰岛素液体直肠栓的胰岛素含量为0.35%;泊洛沙姆407-泊洛沙姆188的比例对栓剂中胰岛素含量影响显著(P<0.05);最优处方为泊洛沙姆407-泊洛沙姆188比例为15%∶25%、壳聚糖含量为0.4%、p H为5;使用无膜和牛肠黏膜时是通过溶蚀方式释放,使用羊肠黏膜时是通过扩散与溶蚀相结合的方式释放。结论:成功制得温控型胰岛素液体直肠栓。OBJECTIVE：To prepare Thermosensitive insulin rectal liquid suppository. METHODS：The formulation of Thermosensitive insulin rectal liquid suppository was optimized by orthogonal test with the ratio of poloxamer P407-P188,the content of chitosan and p H value as factors using the content of insulin as index. The in vitro release mechanism of the suppository was investigated by membraneless dissolution model and animal mucosal dissolution model. RESULTS：The content of insulin was 0.35%,and was influenced by the ratio of poloxamer P407-P188 significantly（P〈0.05）. The optimal formulation was as follows：the ratio of poloxamer P407-P188 was 15% ∶ 25%;the content of chitosan was 0.4%;p H value was 5. In vitro release test confirmed that the drug entered membraneless and bovine intestinal mucosa through erosion;entered the ovine intestinal mucosa through a combination of diffusion and erosion. CONCLUSIONS：Thermosensitive insulin rectal liquid suppository has been prepared successfully.

关 键 词：温控型胰岛素 液体直肠栓 制备 释放机制 

分 类 号：R965[医药卫生—药理学]