硫酸长春新碱传递体的制备及其离体透皮研究  

Preparation of transfersomes of vincristine sulfate and study on its prcutaneous penetration

作　　者：卢懿[1] 侯世祥[1] 陈彤[1] 孙毅毅[1] 杨本霞[1] 袁子雁[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《中国中药杂志》2005年第12期900-903,共4页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金资助项目(30472194)

摘　　要：目的:筛选制备硫酸长春新碱传递体(VCR-T)的最佳工艺,预测其作为VCR新制剂的可行性。方法:采用干膜超声法通过正交试验优化制备工艺;激光散射粒径分析仪测量粒径及其分布,透射电镜观察形态,HPLC测定包封率;改良的Franz扩散池进行体外透皮试验。结果:最优处方及工艺:卵磷脂:去氧胆酸钠为70:20,载体:VCR为45:10;pH7.3,水合30min;制备的硫酸长春新碱传递体为淡黄色透明胶体溶液,平均粒径94nm,外形圆整光滑,分布均匀,包封率为90%;以零级速率透过皮肤,24h累积透皮吸收率为63.8%。结论:VCR-T有望成为VCR临床给药的一种新给药系统。Objective: To select the best preparation method of vincristine transfersomes( VCR-T) and predict its possibility of being a new formulation of VCR. Method: Orthogonal design was used to optimize the preparation methods on the basis of single factor pretests; and the permeation tests in vitro were performed in modified Franz diffusion cells.Result: The optimum formula was: pH was equal to 7.3, the ratio of lecithin to sodium deoxycholate is 70/20, the weight of VCR is 10 mg, hydrating time is 30 minutes. The optimized solution was light yellow and transparent colloid solution. The VCR-T are spherical and smooth with average diameters of 94 run and an encapsulation ratio of 90% . The test in vitro showed that VCR-T could permeat through mouse skin at zero rate with the cumulative penetrating quality amounting to 63.8%. Conclusion: Transfersomes may become a promising carrier of VCR for clinic use.

关 键 词：传递体 制备工艺 长春新碱 透皮给药 

分 类 号：R943[医药卫生—药剂学]