Bioequivalence study of montelukast tablets in healthy Pakistani volunteers

Montelukast is a leukotrien receptor antagonist used for asthma treatment. Objective of this study was to evaluate the bioequivalence of two montelukast 10mg tablets, Innovator drug (Singulair) as reference and other locally manufactured drug (Montiget) in 12 healthy volunteers. It was randomized, single dose, two-period crossover study with 1 week washout period. Blood samples (4-5 ml) were collected before and after drug administration and plasma was separated for analysis. Concentrations of montelukast at different time intervals were determined by validated UV-HPLC method at 345nm wavelength. Bioequivalence was assessed by using non compartmental approach and also calculated the 90% confidence interval of the least-squared pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞). On average, Cmax, AUC0-t, AUC0-inf, was 2.35μg/ml, 1.28μg.h./ml, 1.67μg.h./ml, for innovator drug and 2.53μg/ml, 1.53μg.h./ml, 1.96μg.h./ml, for test drug, respectively. Confidence interval (90%) for Cmax, AUC0-t and AUC0-inf was 89-97%, 85–91% and 81-98% respectively. No statistical difference was found between the Cmax and AUC values of test and reference drugs. The confidence intervals for Cmax, AUC0-t and AUC0-∞ are fully laid within the acceptable range of FDA (80-125%), thus two formulations are considered to be bioequivalent.