Please use this identifier to cite or link to this item: http://idr.nitk.ac.in/jspui/handle/123456789/12519
Title: Pharmaceutical salts of ethionamide with GRAS counter ion donors to enhance the solubility
Authors: Nechipadappu, S.K.
R., Trivedi, D.
Issue Date: 2017
Citation: European Journal of Pharmaceutical Sciences, 2017, Vol.96, , pp.578-589
Abstract: Pharmaceutical salts of BCS class II second line anti-tuberculosis drug ethionamide (ETH) with various counter ions namely, 2-chloro-4-nitrobenzoic acid (CNB), 2,6-dihydroxybenzoic acid (2,6HBA), 2,3-dihydroxybenzoic acid (2,3HBA) and 2,4-dinitrobenzoic acid (DNB) were synthesized by crystal engineering approach. All the synthesized salts were characterized by various spectroscopic (NMR, FT-IR,), thermal (DSC & TGA) and PXRD techniques. The crystal structure of the synthesized salts was determined by single-crystal X-ray diffraction techniques. All the reported salts, except ETH-2,3HBA exhibited charge assisted acid pyridine heterosynthon. In ETH-2,3HBA hydoxyl pyridine heterosynthon is observed. In ETH-CNB salt, both ionic and neutral acid pyridine heterosynthon were observed in the asymmetric unit. ETH-DNB salt consists of both partial and complete proton transfer from DNB to ETH in the asymmetric unit. All the synthesized salts were found to be non-hygroscopic at accelerated humid condition (~ 75% RH). Solubility experiment has been performed in purified water and in 0.1 N HCl (pH = 1) solution and found that the solubility of ETH-CNB salt was about eight-fold higher soluble than ETH in purified water. The solubility of synthesized salts follows the order of ETH < ETH-2,3HBA < ETH-2,6HBA < ETH-CNB in purified water. 2016 Elsevier B.V.
URI: http://idr.nitk.ac.in/jspui/handle/123456789/12519
Appears in Collections:1. Journal Articles

Files in This Item:
There are no files associated with this item.


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.