胡椒碱胶囊自乳化释药系统的处方筛选及体外质量评价  

Formula Screening and Quality Evaluation in vitro of Piperine Self-emulsifying Drug Delivery System

作　　者：邵兵[1,2] 崔超[1,2] 刘红梅[1,2] 纪宏宇[1,2] 唐景玲[3] 秦梦楠[1,2] 李欣[1,2] 吴琳华[1,2] 

机构地区：[1]哈尔滨医科大学附属第二医院药学部,哈尔滨150086 [2]黑龙江省高校重点试验室 [3]哈尔滨医科大学药学院

出　　处：《中国药师》2015年第10期1674-1678,共5页China Pharmacist

基　　金：黑龙江省教育厅科学技术研究项目(编号:12541482)

摘　　要：目的:研究胡椒碱自乳化释药系统的处方及其体外特性。方法:通过溶解度、处方配伍试验以及伪三元相图的绘制来筛选处方,并考察空白处方、含药处方对自乳化效率的影响以及自乳化后乳滴的粒度分布,考察了胡椒碱自乳化胶囊的溶出速率和稳定性。结果:胡椒碱自乳化胶囊的最终处方为油酸乙酯、Tween 80、Transcutol P,三者之比为30∶55∶15(w∶w∶w),药物为辅料总量的2.5%,粒径约为90 nm,胡椒碱自乳化胶囊60 min溶出度是自制的胶囊剂6倍;低温和常温稳定性考察药物含量无明显变化。结论:所制备的胡椒碱自乳化胶囊自乳化效率高、能力强、性质稳定,体外溶出率高。Objective：To study the optimized formula and characteristics in vitro of piperine self-emulsifying drug delivery system （ SEDDS） . Methods：Solubility test, formula compatibility test and ternary phase diagram were adapted to screen and optimize the for-mula. The effects of the blank formula and piperine-loaded formula on the self-emulsifying efficiency were examined. Meanwhile, the particle size distribution after self-emulsification, and the dissolution rate and stability of SEDDS were determined in vitro as well. Re-sults：The optimized formula was composed of ethyl oleate, Tween 80 and Transcutol P （30：55：15, w/w/w）, and the amount of pip-erine was 2. 5% （w/w） of the adjuvants. The mean droplet size was 90 nm approximately. The dissolution profile of SEDDS was 6-fold higher than that of the self-prepared capsules during the 60-minute incubation. There was no significant change in the stability test un-der sub-ambient and ambient temperature. Conclusion：The preparation efficiency of piperine SEDDS is high with promising stability, and the dissolution of the SEDDS capsules is improved obviously when compared with that of the self-prepared capsules.

关 键 词：胡椒碱 自乳化释药系统 伪三元相图 溶出度 

分 类 号：R944.9[医药卫生—药剂学]