Journal of Bioequivalence & Bioavailability

Abstract

Bioequivalence Study of Two 10 mg Montelukast Immediate-Release Tablets Formulations: A Randomized, Single-Dose, Open-Label, Two Periods, Crossover Study

Enrique Muñoz, Daniel Horacio Ocampo, Edgar Emilio Espinal and Natalia Yépes

tablets in twenty-four healthy volunteers. The Test product was Montelukast* manufactured by Tecnoquímicas S.A. (Jamundí – Colombia) and the Reference product was Singulair® (Montelukast) made by Merck Sharp & Dohme Ltd. (Northumberland - United Kingdom). A crossover design 2 x 2 of single-dose, with two treatments, two periods, two sequences and with a washout period of one week was used. Blood samples were collected from 0, 5 to 24 hours after dosing. The determination of Montelukast in plasma was performed using a previously validated bio-analytical method of high-performance liquid chromatography with fluorescence detector (HPLC-FLD). Through Montelukast concentration curves versus time measured in the volunteers’ plasma, the pharmacokinetic parameters and bioequivalence were determined for both products. The pharmacokinetic parameters determined in this study for both the reference and test products were Cmax 440.6 ± 227.4 ng/ml, 460.5 ± 170.9 ng/ml, AUC0→∞ 3196.5 ± 1546.8 ng/h.ml, 3284.9 ± 1270.0 ng/h.ml and AUC0→24 3162.5 ± 1537.6 ng/h.ml, 3251.6 ± 1221.8 ng/h.ml respectively. For Montelukast, with a confidence interval of 90%, the ratio of the logarithmic transformation test product / reference product for AUC0→∞ was from 94.5 to 110.9 and the ratio test product/reference product for Cmax was from 89.0 to 110.4. These intervals are within the established bioequivalence range and therefore determined that the test formulation is interchangeable or bioequivalent to the reference.