CAJ | 학술논문

目的确定普罗布考自微乳化给药系统(self micro-emulsifying drug delivery system,SMEDDS)的较优处方.方法以微乳粒径、zeta-电位、药物在空白自微乳给药系统的平衡溶解度及5 min时药物的溶出度为指标,采用星点设计-效应面优化法,确定较优处方.结果处方中橄榄油占油相比例、油相占处方比例及表面活性剂与助表面活性剂的比值分别为0.33、0.5和2.0时,为较优处方.此时微乳粒径为92.7 nm,zeta-电位为-17.38 mV,药物在空白自微乳给药系统中的平衡溶解度为65.17 mg/mL,5 min时药物的溶出度为63.46%.结论应用星点设计-效应面优化法能够快速方便的得到普罗布考自微乳化给药系统的较优处方,所建立的模型预测性良好.
목적 학정보라포고자미유화급약계통(self micro-emulsifying drug delivery system,SMEDDS)적교우처방.방법 이미유립경、zeta-전위、약물재공백자미유급약계통적평형용해도급5 min시약물적용출도위지표,채용성점설계-효응면우화법,학정교우처방.결과 처방중감람유점유상비례、유상점처방비례급표면활성제여조표면활성제적비치분별위0.33、0.5화2.0시,위교우처방.차시미유립경위92.7 nm,zeta-전위위-17.38 mV,약물재공백자미유급약계통중적평형용해도위65.17 mg/mL,5 min시약물적용출도위63.46%.결론 응용성점설계-효응면우화법능구쾌속방편적득도보라포고자미유화급약계통적교우처방,소건립적모형예측성량호.
Objective To determine the optimized self micro-emulsifying drug delivery system (SMEDDS) formulation of probucol. Methods According to the indexes of mean particle size, zeta-potential, solubility of probucol in blank SMEDDS and the dissolution percentage in 5 minutes of the preparations, the optimized formulation was determined by the central composite design-response surface methodology. Results When the correspondent percentage of olive oil in oil phase (W/W) was 0.33, the percentage of oil phase in formulation (W/W) was 0.5, and the ratio of surfactant to co-surfactant (W/W) was 2.0, respectively. The mean particle size, zeta-potential, solubility of probucol and dissolution percentage in 5 minutes of micro-emulsion was 92.7 nm, -17.38 mV, 65.17 mg/mL and 63.46%, respectively. Conclusions The optimized formulation of the probucol SMEDDS was obtained quickly and conveniently by the central composite design-response surface methodology. The method had a reliable predictability.