Estudo da estabilidade e do perfil de liberação de comprimidos de maleato de enalapril e determinação da concentração plasmática em pacientes

AUTOR(ES)
DATA DE PUBLICAÇÃO

2008

RESUMO

The stability of a pharmaceutical formulation can be a major factor in assuring the quality of a drug product and, as a consequence, the efficacy of the treatment. Enalapril is an anti-hypertensive pro-drug that, after being absorbed, is hydrolised into enalaprilat, an agent responsible for blocking the conversion of angiotensin I into angiotensin II. Stability of formulations containing enalapril maleate can be affected when exposed to high levels of temperature and humidity, with the formation of two degradation products: enalaprilat and diketopiperazine. In this work, the quality of different commercially available tablets of 20mg of enalapril maleate (Reference, generic and similar products) was evaluated by both an accelerated stability study and by monitoring the plasma concentration of this drug in patients. Previous indications that enalapril can be easily decomposed under adverse environmental conditions were proven by the results of the accelerated stability studies obtained in this work, in which five out of the nine samples analyzed did not exhibit the specified amount of drug. In addition, the evaluation of the dissolution profile of the tables showed marked differences in the drug release mechanism. Also, at the end of 30 minutes of the test, the dissolution was altered by the degradation of the drug. During the clinical study, lower plasma concentrations were found in patients under treatment with generic and similar products. Changes observed in the drug concentration and dissolution profile for some of the samples in this study may be an indication of a compromised bioavailability.

ASSUNTO(S)

stability estabilidade equivalency dissolution comprimidos farmacia tablets enalapril enalapril dissolução equivalência

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