COMPARATIVE, OPEN LABEL, SINGLE DOSE CLINICAL TRIAL OF BIOAVAILABILITY OF FORMULATION CONTAINING AMBROXOL, TRIMETHOPRIM AND SULFAMETHOXAZOLE IN HEALTHY VOLUNTEERS.

Abstract

Author(s): J. Pérez-Urizar*,I. Torres-Roque, D. Torres-Tirado, JR. Zapata-Morales, AEscobedo-Moratilla, ACovarrubias-Pinedo, ASMares-García, O. Patiño-Rodríguez

Acute exacerbation of chronic bronchitis is a consequence of augmentation in air pathways secretions, often complicated by bacterial infections. Then, a clinical benefit can be anticipated with the join therapy of antimicrobial and mucolytic agents. In this study we aimed to compare the bioavailability and safety of an oral formulation containing ambroxol (AMBX), trimethoprim (TMP) and sulfamethoxazole (SMZ) in 24 healthy volunteers. Subjects were randomized to receive a tablet of (A) AMBX-TMP-SMZ (160, 800mg and 30mg); (B) TMP-SMZ (160mg and 800mg) and (C) AMBX (30mg), in a crossover way with 3 sequences in 3 periods (ABC, BCA, CAB) and 7 days of washout between each period. No significant changes were observed in the absorption indicators Cmax, Tmax, AUC0-t and AUC0-∞, and the elimination parameter T1/2 of SMZ, TMP or AMBX. Also Westlake 90% Confidence Intervals calculated for Cmax and AUC’s were included in the bioequivalence range of 0.80-1.25 suggesting that the bioavailability of all agents in the new combined formulation is not different to that obtained following the individual administration of each. Volunteers claimed minimal side effects following all treatments. These results show the pharmacokinetic properties of a formulation containing TMP SMZ-AMBX that could contribute to improve the therapeutic adherence.