氢溴酸东莨菪碱微乳的制备及其体外透皮吸收研究
Studies on preparation and skin permeation in-vitro of scopolamine hydrobromide microemulsion
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摘要: 目的:探讨微乳组分对其理化性质及其体外透皮吸收性质的影响。方法:以聚氧乙烯氢化蓖麻油(CremophorRH-40)-乙醇-油酸聚乙二醇甘油酯(LabrafilM 1944 CS)-水作为微乳的组成成分,制备水包油型微乳。考察各微乳粒径、黏度值,同时考察微乳水相含量、油相含量、乳化剂含量和Km值对其透皮吸收性质的影响。结果:氢溴酸东莨菪碱微乳粒径、黏度值及透皮吸收率受多种因素的影响,包括Km值、水相含量、油相含量等结论:具有最大透皮渗透量及适宜粒径、黏度值的微乳体系处方为:乳化剂(CremophorRH-40+无水乙醇,Km=2:1)30%,油相Labrafil 10%,三蒸水58.5%,氢溴酸东莨菪碱1.5%。Abstract: Objective :To investigate the physico-chemical properties of scopolamine hydrobromide micromulsion and its transdermal delivery effect in vitro. Methods : The O/W microemulsion was prepared with the system contained of Cremophor RH-40-ethanol-Labrafil-water according to the pseudo-ternary phase diagrams.The values of droplet diameter and viscosity were investigated and the permeation flux of scopolamine hydrobromide was determined in vitro using Franz difusion cel1 with nude rats skin.The content of scopolamine hydrobromide was determined by HPLC. Results :The results indicated that the values of droplet diameter and viscosity and the permeation rate were influenced by the Km value and the contents of oil and water. Conclusion : The highest percutaneous scopolamine hydrobromide absorption microemulsion system with suitable diameter and viscosity contains 30%Cremophor RH-40+ethanol、10%Labrafil M 1944 CS 、1.5% scopolamine hydrobromide and 58.5% water,Km=21.
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Key words:
- microemulsion /
- scopolamine hydrobromide /
- transdermal delivery
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