Please use this identifier to cite or link to this item: https://doi.org/10.1021/cg500245e
Title: Pharmaceutical salts of haloperidol with some carboxylic acids and artificial sweeteners: Hydrate formation, polymorphism, and physicochemical properties
Authors: Aitipamula, S.
Wong, A.B.H.
Chow, P.S.
Tan, R.B.H. 
Issue Date: 7-May-2014
Citation: Aitipamula, S., Wong, A.B.H., Chow, P.S., Tan, R.B.H. (2014-05-07). Pharmaceutical salts of haloperidol with some carboxylic acids and artificial sweeteners: Hydrate formation, polymorphism, and physicochemical properties. Crystal Growth and Design 14 (5) : 2542-2556. ScholarBank@NUS Repository. https://doi.org/10.1021/cg500245e
Abstract: We report novel pharmaceutical salts of an important neuroleptic drug haloperidol (HAL) with some carboxylic acids and artificial sweeteners. The pKa difference between HAL and the selected carboxylic acids and sweeteners suggests salt formation. All the salts were obtained from conventional solvent evaporative crystallization experiments at ambient conditions. Except formic acid, all the carboxylic acids form salt hydrates. Crystal structure analysis revealed an isostructural crystal packing in succinate, fumarate, and acetate salt hydrates. This study reports a stable polymorph of the known HAL-saccharinate, and two polymorphs of a novel salt with acesulfame. Both polymorphic sets feature significant differences in hydrogen bonding and conformations of HAL. Stability of the polymorphs was deduced by thermal analysis, comparison of the calculated density, and slurry experiments in the case of the HAL-acesulfame salt. The reported salts with artificial sweeteners could offer advantages in terms of masking the bitter taste of the parent HAL base. All the salts showed higher solubility and intrinsic dissolution rate in 10% EtOH-water medium compared to HAL. These salts provide a means of increasing the number of solid forms for HAL that facilitate selection of a suitable salt form for development of fast-dissolving HAL formulations. © 2014 American Chemical Society.
Source Title: Crystal Growth and Design
URI: http://scholarbank.nus.edu.sg/handle/10635/89762
ISSN: 15287505
DOI: 10.1021/cg500245e
Appears in Collections:Staff Publications

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

SCOPUSTM   
Citations

25
checked on Oct 16, 2018

WEB OF SCIENCETM
Citations

23
checked on Oct 8, 2018

Page view(s)

70
checked on Oct 12, 2018

Google ScholarTM

Check

Altmetric


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