来曲唑的经皮扩散动力学参数及其滞留时间法评价  

The letrozole's kinetics parameter of percutaneous permeation and the evaluation of the lag time method

作　　者：齐瑗晶[1] 卢霞[1] 刘拥军[1] 刘爱芹[1] 于胜海[1] 

机构地区：[1]山东省医学科学院药物研究所,山东济南250062

出　　处：《中国医院药学杂志》2009年第24期2086-2088,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的:获取来曲唑的经皮扩散参数,以确定其能否研发成经皮给药新剂型。方法:用4个不同处方制备成的来曲唑霜剂进行离体动物皮肤的主药经皮扩散试验,用HPLC法检测并统计各样品的累计释放量,计算经皮扩散的动力学参数,并用滞留时间法验证、评价这些参数的可信度。结果:来曲唑的Tlag为1.23 h,Jss为4.73×10^(-5)mmol·cm^(-2)·h^(-1),D为1.658×10~6cm^2·h^(-1),Kp为1.35×10^(-6)cm·h^(-1)。结论:来曲唑的皮肤滞留时间较短(小于2h),稳态通量较大,适宜制备成经皮肤给药系统。OBJECTIVE To make it sure whether a percutaneous administration system of letrozol can be developed by studying the kinetic parameters of percutaneous permeation. METHODS The permeation experiment of four letrozole＇s cream were carried out by using rabbit skin in vitro. To determine the diffusion media by HPLC, then calculate the kinetic parameters and evaluate the reliability coefficient of these parameters by the lag time method. RESULTS The Tlag = 1. 23 h. ;The Jss = 4. 49 10^-5mmol·cm^-2·h^-1 ;The D= 1. 658 10^-6cm^-2·h^-1 ;The Km= 0. 0027;The Kp = 1. 283 10-^6cm·h^-1 CONCLUSION On account of letrozole＇s tlag and steady-state flux, it is concluded that letrozole can developed to be Transdermal drug deliver systems.

关 键 词：来曲唑 经皮扩散 动力学参数 滞留时间法 高效液相色谱法 

分 类 号：R943[医药卫生—药剂学]