生物学的同等性とバイオアベイラビリティのジャーナル

概要

Bioequivalence Study of Two Formulations of Escitalopram Oxalate 20 mg Tablets in Healthy Volunteers

Enrique Muñoz, Daniel Ocampo and Natalia Yepes

A Bioequivalence study was developed to compare the bioavailability of two formulations of Escitalopram oxalate 20 mg tablets in twenty-four healthy volunteers. The Test product was Escitalopram made by Laboratorios Tecnoquímicas S.A. (Jamundí – Colombia) and the Reference product was Lexapro® (Escitalopram) made by H. Lundbeck A/S (Valby - Denmark). A crossover, 2 x 2, single-dose, two treatments, two periods, two sequences design was used, with a washout period of one week. Prior to dose administration a basal blood sample was taken and between 1 and 96 hours after the administration another 17 samples were collected. The determination of Escitalopram in plasma was performed using a bioanalytical method for ultra high resolution liquid chromatography coupled to a single quadrupole mass spectrometer (UHPLC-MS) and using ESI+, previously validated. Through Escitalopram concentration curves versus time obtained from measurements in the plasma of volunteers the pharmacokinetic parameters and Bioequivalence were determined for both products. The pharmacokinetic parameters determined in this study to the Reference and Test products were Cmax 15.7 ± 7.3 ng/ml, 14.5 ± 5.9 ng/ ml, AUC0→∞ 901.6 ± 389.2 ng.h/ml, 731.3 ± 257.1 ng.h/ml and AUC0→96 740.9 ± 354.0 ng.h/.ml, 612.7 ± 207.6 ng.h/ ml respectively. For Escitalopram, the ratio of the logarithmic transformation Test product / Reference product for AUC0→96 were from 94.6 to 103.1 and for Cmax were from 91.7 to 107.4; both ratios with confidence interval of 90%. These intervals are within the range of Bioequivalence established and therefore it can be concluded that the Test formulation is interchangeable or Bioequivalent to the Reference.