Preparation and characterization of salt forms of enalapril

Pharmaceutical Development and Technology
Lokesh KumarArvind K Bansal

Abstract

Selection of an optimal salt form of a drug candidate is a vital component of preformulation stage of drug development. In this study, six salts of enalapril--citrate, mesylate, tartrate, malate, besylate and tosylate--were prepared and characterized by Mass Spectroscopy, Differential Scanning Calorimetry, Thermogravimetric Analysis, Microscopy, Powder X-ray Diffraction, Karl Fischer Titration, High Performance Liquid Chromatography, Fourier-Transform Infra-red Spectroscopy and Head Space Gas Chromatography. All the six salts were subjected to a tiered screening involving five stages in the following order: crystallinity, hygroscopicity, solubility, stability and flow/compactability. Enalapril malate showed encouraging profile because of its lower hygroscopicity, higher solubility, good solid state stability, and better flow and compactability, in comparison to the marketed maleate salt.

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Citations

Jun 7, 2012·AAPS PharmSciTech·Neeraj KumarAsim Kumar Jana
Dec 20, 2012·AAPS PharmSciTech·Lokesh KumarArvind K Bansal
Oct 25, 2014·Drug Development and Industrial Pharmacy·Shashank JainSenshang Lin
Jan 18, 2011·Journal of Pharmaceutical and Biomedical Analysis·Norman ChiengJaakko Aaltonen
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter
Jul 6, 2018·Acta Crystallographica. Section C, Structural Chemistry·Alex N ManinGerman L Perlovich

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