基于孟鲁司特钠咀嚼片渗透速率分析初步预测制剂的生物等效性

Preliminary Prediction of Bioequivalence of Montelukast Sodium Chewable Tablets Based on Permeability Analysis

目的研究孟鲁司特钠咀嚼片体外溶出及渗透过程,并建立体内外相关性模型对仿制制剂的生物等效性进行预测。方法采用Macro Flux型药物溶出度与渗透速率测试系统,以饱腹小肠模拟液(p H 5. 0)为介质,分别比较参比制剂和受试制剂的溶出及渗透行为,通过关键质量参数考察药物的释放与吸收过程,预测受试制剂的生物利用度,进而预测制剂间是否生物等效。结果在饱腹小肠模拟液中,孟鲁司特钠咀嚼片受试制剂与参比制剂的溶出行为和渗透速率基本一致,ρmax和AUC0-t无显著性差异,生物利用度约为参比制剂的97%。结论初步预测孟鲁司特钠咀嚼片受试制剂与参比制剂在体内生物等效。

OBJECTIVE To study the in vitro dissolution and permeation process of montelukast sodium chewable tablets,and establish the in vivo-in vitro correlation models to predict the bioequivalence of the generic preparations.METHODS The Macro Flux drug dissolution absorption test system was used,and the satiety intestinal simulated liquid(p H 5.0)was used as the medium to compare the penetration of the reference preparation and test preparation.The rate,release and absorption process of the drug were examined by the quality parameters,and the bioavailability of the test preparation was predicted,thereby predicting whether the preparation was bioequivalent.RESULTS In the satiety small intestine simulating solution,the permeation rate,ρmaxand AUC0-tof the test preparation and the reference preparation were basically the same.The bioavailability was approximately 97%of the reference formulation.CONCLUSION It is preliminarily predicted that the test preparation of montelukast sodium chewable tablets is bioequivalent with the reference preparation.