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
CECIF (Centro de la ciencia y la investigación farmacéutica), Medellín, Colombia
- *Corresponding Author:
- Enrique Muñoz Carnago
CECIF (Centro de la Ciencia y la Investigación Farmacéutica)
Medellín, Antioquia, Colombia
Tel: 57-4-3778584 ext. 107/104
Fax: 57-4-3778584 ext. 102
E-mail: [email protected]
Received Date: May 02, 2014; Accepted Date: May 25, 2014; Published Date: May 31, 2014
Citation: Muñoz E, Ocampo DH, Espinal EE, Yépes N (2014) Bioequivalence Study of Two 10 mg Montelukast Immediate-Release Tablets Formulations: A Randomized, Single-Dose, Open-Label, Two Periods, Crossover Study. J Bioequiv Availab 6: 086-090. doi: 10.4172/jbb.10000186
Copyright: © 2014 Muñoz E, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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.