D-优化设计ZLR-8自乳化制剂的处方  

Study on D-Optimal Design for Self-emulsifying Formulation of ZLR-8

作　　者：李莉[1] 高缘[2] 张建军[2] 钱帅[3] 周建平[3] 张奕华[3] 

机构地区：[1]南京医科大学第二附属医院,江苏南京210011 [2]中国药科大学药剂学教研室,江苏南京210009 [3]中国药科大学新药研究中心,江苏南京210009

出　　处：《药物生物技术》2007年第5期339-344,共6页Pharmaceutical Biotechnology

基　　金：国家自然科学基金资助项目(NO.30271491);江办省自然科学基金项目(NO.BK2002119)

摘　　要：优化筛选极难溶性的氮氧供体型非甾体抗炎药ZLR-8自乳化制剂的处方。采用HPLC法测定ZLR-8在各溶剂中的溶解度,初步确定自乳化制剂中的油相、表面活性剂和助表面活性剂;采用水滴定法制备伪三相图,确定自乳化制剂中各组分的应用范围;再根据这些范围,采用Design Expert软件进行D-优化设计得到了ZLR-8自乳化制剂的优化处方,其自乳化性能及乳液粒径的预测值与实测值基本一致。D-优化设计对于ZLR-8自乳化制剂的处方优化是一种有效手段。To optimize the formulation ingredient of self-emulsifying drug delivery system of ZLR-8, a new NO-donor nonsteroidal anti inflammatory drug with Door absorption and insolubility in water. The solubility experiment of ZLR-8 in various vehicles was determined by HPLC and the solubility data were used to choose the appropriate type of oil phase, surfactant and Co-surfactant in SEDDS system. Water titration technique was performed to figure out the pseudo-ternary phase diagrams and to determine the concentration region of each vehicle used in SEDDS. The region was then adapted into Design-Expert software for D-Optimal design for formulation optimization of ZLR-8 SEDDS. The optimized formulation of ZLR-8 SEDDS was generated. No significant difference exists between the predicted values and the observed values of evaluated parameters. CONCLUSION： D-optimal design is a useful technique for the formulation optimization of SEDDS.

关 键 词：氮氧供体型非甾体抗炎药 ZLR-8 自乳化 处方优化 

分 类 号：R9[医药卫生—药学]