Bioequivalence study of montelukast sodium chewable tablet in healthy volunteers by liquid chromatography-tandem mass spectrometry
Zhou Chun-hu · Chinese Journal of Hospital Pharmacy · 2014
OBJECTIVE To establish a LC/MS/MS method for measuring montelukast sodium in human plasma,and study the pharmacokinetic and bioavailability of montelukast sodium in healthy volunteers.And then compare the bioequivalence of montelukast sodium chewable tablet in human body.METHODS A single oral of 10 mg montelukast sodium test or reference tablets was given to 20 healthy volunteers in a randomized cross-over study.The plasma obtained was spiked with internal standard of simvastatin in the plasma,then the sample was treated by protein precipitating method,and the concentration of montelukast sodium in plasma was determined by LC/MS/MS.The pharmacokinetic parameters as well as the relative bioavailability were measured by DAS software.RESULTS The good linear range of montelukast sodium was 1.0-1000.0ng ml-1. The main pharmacokinetic parameters of test and reference montelukast sodium chewable tablets were as follows:AUC0-24 h were(3 404.7±2 248.5),(3 517.1±2 313.2)ng·ml-1·h;AUC0-∞were(3 516.0±2 302.3),(3 621.8±2 366.2)ng·ml-1· h;Cmaxwere(646.3±384.1),(612.4±409.2)ng·ml-1;tmaxwere(2.00±0.78),(2.13±0.76)h;t1/2were(5.31±1.16),(4.93±1.28)h.CONCLUSION The method was suitable for the pharmacokinetic study of montelukast sodium.The statistical analysis of the results showed that the reference and test montelukast sodium chewable tablets were bioequivalent.