酮洛芬自乳化制剂的释药动力学研究

目的探讨酮洛芬自乳化制剂 (SEDDS)的体外释药性能。方法测定酮洛芬在不同释放介质中的表观油水分配系数 ,并用HPLC法测定经释放介质稀释后药物含量的变化。采用反向透析技术测定体外释药性能 ,并对其释药曲线进行拟和。结果酮洛芬在 pH 6. 8PBS中的表观油水分配系数较大 ,药物释放较快 ,1 5h释放可达 90 %。经稀释后 4h内药物含量未改变。释药曲线符合Hixson -Crowell方程。结论酮洛芬的油水分配系数与释药速率有关 ,释药过程中 ,酮洛芬SEDDs乳化后乳滴粒径和表面积均发生改变 ,药物透膜过程属于被动扩散机制。

Study on the release kinetics in vitro of the ketoprofen self-emulsifying drug delivery system

Objective To study the release in vitro of the ketoprofen self-emulsifying drug delivery system.Methods Apparent partition coefficients of ketoprofen and the variance of ketoprofen concentration after dilution were determined by HPLC.The release amount of ketoprofen SEDDS was determined by the bulk-equilibrium reverse dialysis bag technique.Results Apparent partition coefficients of ketoprofen in pH 6.8 PBS was larger,and the release of the drug was faster,which was 90% after 1.5 h.Ketoprofen concentration after dilution within 4 h wasn't altered.The profile curve fits the Hixson-Crowell equation.Conclusion The in vitro release of ketoprofen is interrelated with apparent partition coefficients of the drug.The particle diameter and surface area of the drops in the course of release in vitro are changing.The process of the drug penetrating membrane fits passive diffusion.