尼莫地平过饱和自微乳的研制

Preparation of supersaturatable self-microemulsifying drug delivery system containing nimodipine

目的制备尼莫地平过饱和自微乳化给药系统(NMP S-SMEDDS),并对其体外特性进行考察。方法以平均粒径、平均电位、乳化时间为评价指标,通过星点设计-效应面优化法优化自微乳化给药系统(SMEDDS)处方;以PVPK30为促饱和物质,制备NMP S-SMEDDS,并通过考察PVPK30用量对SSMEDDS体外溶出行为的影响,筛选PVPK30的适用量。结果 SMEDDS的最优处方为油酸乙酯∶吐温-80∶Transcutol P=17.25∶49.16∶44.76(质量比);以PVPK30质量分数为2%,尼莫地平质量分数为2.5%制备得到的NMP S-SMEDDS的粒径为(33.41±0.48)nm,Zeta电位为(-9.62±1.49)mV,60 min的体外溶出度达90.4%,比市售尼莫地平片的溶出度明显提高。结论 NMP S-SMEDDS可提高尼莫地平的体外溶出度。

Objective To prepare supersaturatable self-microemulsifying drug delivery system （S-SMEDDS） of nimodipine （NMP） and study its characteristics in vitro.Methods With degree of average particle size, Zeta potential and emulsifying time as indexes, the formulation of self-microemulsifying drug delivery systems was optimized by central composite design-response surface methodology.The dissolution of NMP was determined in the different formulations of S-SMEDDS to screen the usage of PVPK30 as supersaturated promoter.Results The composition of the optimized formulation was as follows： ethyl oleate ：tween-80 ： Transcutol P = 17.25 ： 49.16 ： 44.76. The S-SMEDDS was prepared by using 2% PVPK30 and 2.5% nimodipine.The average particle size and Zeta potential were （33.41±0.48） nm and （-9.62± 1.49） mV. The dissolution was 90.4% in 60 min, and it was much faster than the reference formulation. Conclusion The dissolution of NMP was enhanced by S-SMEDDS.