奥沙普秦凝胶剂体外透皮实验条件及促渗剂的选择

The Selection of Transdermal Release Condition and Percutaneous Enhancer of Oxaprozin Gel in Vitro

目的 :考察载药量、介质组成、促渗剂月桂醇(LA)和氮酮(AZ)对奥沙普秦(OXP)凝胶剂体外透皮作用的影响。方法 :采用改良Franz双室渗透装置 ,以离体小鼠皮肤为透皮屏障 ,进行体外渗透试验。结果 :在有效透过面积5 77cm2条件下 ,载药量大于1 2g ,接收液乙醇∶生理盐水=7∶3(v∶v)时 ,实验结果稳定 ,重现性好 ;月桂醇促渗作用强于氮酮 ,混合促渗剂3 %AZ +10 %LA效果最佳。结论 :通过对OXP凝胶最佳透皮实验条件和促渗剂的选择 ,为研究OXP透皮给药提供了参考依据 ,同时对凝胶剂体外透皮试验的标准化进行了初步探讨。

OBJECTIVE:To observe the effect of drug loading,medium composition,transdermal enhancer,lauryl alcohol and azone on percutaneous permeation of oxaprozin gel in vitro METHODS:Drug permeation test was carried out by using modified Franz-type double compartment diffusion cell and isolated mice skin in vitro as transdermal barrier RESULTS:Under the condition of an effective area of 5 77cm2,it was found that the result was stable and the reproducibility was well with drug loading more than 1 2g,the receiver solution ethanol to normal saline=7∶3(v∶v);The transdermal enhancing effect of lauryl alcohol was superior to that of azone,the effect of mixed transdermal enhancer 3%AZ+10%LA was the best CONCLUSION:The selection of both the optimum release condition and the best penetration enhancers provided reference for oxaprozin transdermal delivery The standardization of gel percutaneous test in vitro was discussed preliminarily