恩拉霉素自微乳制剂的研制及质量评价  

Preparation and Quality Evaluation of Enramycin Self-Microemulsifying Drug Delivery System

作　　者：陈浩[1] 陈敏[1] 刘蕊[1] 

机构地区：[1]浙江工商大学,杭州310018

出　　处：《中国药学杂志》2016年第14期1235-1240,共6页Chinese Pharmaceutical Journal

基　　金：浙江省新苗人才计划资助项目(2015R408073)

摘　　要：目的 研制恩拉霉素自微乳制剂,并进行质量评价。方法 测定恩拉霉素在各辅料中的溶解度,通过三相配伍实验筛选自微乳化基质;以微乳粒径作为效应值,应用D-最优混料设计进行处方优化,并对优化后的恩拉霉素自微乳制剂进行稳定性、释放度及抑菌活性考察。结果 恩拉霉素自微乳的最佳处方组成为20%油酸乙酯、40%聚氧乙烯氢化蓖麻油和40%丙二醇。1 g自微乳中较佳载药量20 mg,加水乳化后的平均粒径为（27.81±0.79）nm;体外溶出度10 min达90%以上,比原料药溶出度显著提高。在4-40℃循环条件下48 h,自微乳的粒径及载药量均无明显变化;自微乳化释药系统对恩拉霉素的抑菌活性没有影响。结论 恩拉霉素自微乳质量稳定,可显著提高恩拉霉素的溶出度,有望改善恩拉霉素口服生物利用度。OBJECTIVE To prepare enramycin self-microemulsifying drug delivery system （SMEDDS） and evaluate its quality. METHODS The formulations of enramycin SMEDDS were screened by solubility experiment and self-emulsifying grading test. The formulation was optimized using Design Expert Software, taking particle size as dependent variable and the usage amoumts of oil, sur- factant, and cosurfactant as independent variables. RESULTS The optimized formulation of enramycin SMEDDS consisted of 20% ethyl oleate, 40% RH40, and 40% 1,2-propylene glycol. 1.0 g mixture contained 20 mg enramycin, which dispersed rapidly into wa- ter and the particle size of the formed emulsion was （27.81 ± 0.79）nm. The enramycin SMEDDS dissolved by more than 90% within 10 min, much faster than that of enramycin API. The particle size and concentration of SMEDDS were stable at alternative temperature cycles （4 and 40 ℃ ） for 48 h, and the SMEDDS formulation had no effect on the bacteriostasis of enramycin. CONCLUSION The quality of enramycin SMEDDS is stable. The system increases the dissolution of enramycin significantly and could be advantageous to improve the oral bioavailability of enramycin.

关 键 词：恩拉霉素 自微乳药物传递系统 D-最优混料设计 质量评价 

分 类 号：R944[医药卫生—药剂学]