RELATIVE BIOAVAILABILITY OF AN ORAL SOLUTION OF INDINAVIR: DEVELOPMENT OF PEDIATRIC FORMULATIONS OF ANTIRETROVIRAL DRUGS

CURRAS V.; HOCHT C.; CARCABOSO A.M.; CHIAPPETTA D.A.; BREGNI C.; BUONTEMPO F.; MATO G.; BRAMUGLIA G.F.; NISELMAN V.; RUBIO M.C.

MAR DEL PLATA, BUENOS AIRES, ARGENTINA

Congreso; XXXVII REUNION ANUAL DE LA SOCIEDAD ARGENTINA DE FARMACOLOGIA EXPERIMENTAL; 2005

SOCIEDAD ARGENTINA DE FARMACOLOGIA EXPERIMENTAL

Bioavailability studies are indispensable since pharmaceutical forms for administration to special populations, such as pediatric patients, are lacking. The aim of the present work was to compare the bioavailability of an oral solution of indinavir (INDs) with a capsule formulation (INDc) in adult volunteers and to develop pediatric formulations based on microencapsulated, taste-masked IND. Plasma concentrations of 6 volunteers were determined at 6 time points. Pharmacokinetic parameters were calculated using TOPFIT. Assessment of relative bioavailability (n=6) showed a Cmax of 3.3±1.2 ìg/ml and 3.8±1.0 ìg/ml after INDs and INDc administration, respectively. Tmax was significantly lower for the solution (0,5h) than for capsules (1.3±0.2h). No difference in AUC was found between both formulations (AUCs/AUCc=1.14). In addition, new IND formulations were prepared by a double emulsion-solvent evaporation technique. Their bioavailability will be assessed in further studies. This study demonstrated a faster absorption after INDs intake, achieving similar plasmatic levels as compared to INDc administration.