星点设计-效应面法优化依托泊苷自微乳化释药系统  

Optimization of etoposide self-microemulsifying drug delivery system by central composite design-response surface methodology

作　　者：吴成杨[1,2] 尹东东[2] 王杏林[2] 王频[2] 

机构地区：[1]天津中医药大学,天津300193 [2]天津药物研究院释药技术与药代动力学国家重点实验室,天津300193

出　　处：《中南药学》2012年第10期721-725,共5页Central South Pharmacy

基　　金：国家重点基础研究发展计划(973计划)课题(编号:2010CB735602;2012CB724002)

摘　　要：目的研制稳定的依托泊苷自微乳制剂并评价其质量。方法通过溶解度试验、处方配比、三元相图的绘制及星点设计-效应面法的优化,以粒径、溶解度和zeta电位为指标,筛选各组分的最佳组合和处方配比,并对依托泊苷自微乳的理化性质和体外溶出进行测定。结果依托泊苷自微乳最佳处方为:依托泊苷(2.0%)、Capryol 90(15.1%)、Cremophor RH40(30.4%)、Transcutol HP(52.5%),平均粒径为18.31 nm,自乳化时间<1 min,乳化后载药量>25 mg mL-1。结论制备的依托泊苷自微乳稳定性好,载药量高。Objective To develop the stable formulation of etoposide self-microemulsifying system and evaluate its quality.Methods The optimum formulations of etoposide SMEDDS were screened by solubility,compatibility tests,tertiary phase diagrams and central composite design-response surface methodology,with the particle size,solubility and zeta electric potential as parameters.The physic-chemical property and dissolution characters of etoposide SMEDDS were also determined.Results The optimum self-microemulsifying drug delivery system was composed of etoposide（2.0%）,Capryol 90（15.1%）,Cremophor RH40（30.4%）,and Transcutol HP（52.5%）.The mean particle diameter after the emulsification was 18.31 nm,the self-microemulsifying time was less than 1 min,and the drug loading of emulsifying exceeded 25 mg · mL-1.Conclusion The prepared etoposide SMEDDS is stable with good drug loading.

关 键 词：依托泊苷 自微乳 伪三元相图 星点设计 

分 类 号：TQ460.60[化学工程—制药化工]