Preliminary Prediction of Bioequivalence of Montelukast Sodium Chewable Tablets Based on Permeability Analysis
WANG Lin1, WU Bin1, WANG Tie-song1, WU Ke-chun1, HU Qin1, WANG Hao-tian2, DONG Da-wen3*, ZHANG Zhe1*
1. Beijing Key Laboratory of Analysis and Evaluation on Chinese Medicine, Beijing Institute for Drug Control, Beijing 102206, China; 2. American Pion Company, Billrika 01821, USA; 3. Yangzijiang Pharmaceutical Group Co., Ltd., Taizhou 225300, China
Abstract：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 (pH 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, ρmax and AUC0-t of 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.
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2019, Vol. 54 
