法舒地尔复乳的制备及质量评价

Preparation and quality evaluation of fasudil multiple emulsions

目的:优选处方并制备法舒地尔复乳。方法:以离心药物保留率为指标,采用正交试验设计优化法舒地尔复乳处方;并对其形态、粒径、电导率、载药量进行考察。结果:复乳的最优处方为蓖麻油5.47 g,内相水2.73 g,乳化剂Ⅰ中司班80(Span 80)∶吐温(Tween 80)=7∶3,外相水8.3 g,乳化剂Ⅱ中Tween 80∶卵磷脂=2∶1,维生素E聚乙二醇琥珀酸酯(TPGS)占2%,法舒地尔复乳的离心保留率为99.46%,形态圆整,粒径为382.3 nm,电导率为428μs/cm,载药量为0.48%。结论:成功制备了法舒地尔复乳,为后续口服制剂开发提供制剂学基础。

Objective:To optimize prescription and prepare fasudil multiple emulsions.Methods:The content of fasudil was determined by high performance liquid chromatography,and the formulation of fasudil was optimized by orthogonal design with the centrifugal retention rate as the index.The morphology,particle size,electrical conductivity and drug loading were selected as variable factors.Results:The optimum formula of multiple emulsion was as follows:castor oil 5.47 g,internal phase 2.73 g,volume ratio of Span 80 to Tween 80 was 7:3 of emulsifier I,external phase of 8.3 g,volume ratio of Tween 80 to lecithin was 2:1 of emulsifier II,percentage of TPGS was 2%.The centrifugal retention of fasudil multiple emulsions was 99.46%.The emulsion was prepared with round shape,drug loading rate of 0.48%,particle size of 382.3 nm,electrical conductivity of 428μs/cm.Conclusion:The fasudil multiple emulsions was successfully prepared,which provides a pharmacological basis for the follow-up development of oral preparations.