Issue 26, 2014

Modulating the solubility of sulfacetamide by means of cocrystals

Abstract

Sulfacetamide is a popular antibiotic prescribed for treating ocular infections. However, various physiological constraints are known to reduce its concentration at the site of action, thereby limiting its therapeutic efficacy. In this crystal engineering study, we report novel cocrystals of sulfacetamide with the objective to lower the solubility of the reference drug and improve its residence time at the site of action. Standard cocrystallization methods resulted in cocrystals with caffeine, isonicotinamide, theophylline, bipyridine and a salt with 4-aminopyridine. These crystalline forms were characterized by thermal, spectroscopic and diffraction techniques. In pH 7 phosphate buffer medium, sulfacetamide–caffeine cocrystal exhibited lower solubility (8.64 g L−1, 0.69 times) than the drug (12.5 g L−1). The dissolution of sulfacetamide–isonicotinamide and sulfacetamide–caffeine is 0.64 and 0.68 times lower, whereas sulfacetamide–theophylline is comparable to the reference drug. This study highlights a less explored application of pharmaceutical cocrystals to reduce the solubility and dissolution rate of the drug for improved therapeutic action.

Graphical abstract: Modulating the solubility of sulfacetamide by means of cocrystals

Supplementary files

Article information

Article type
Paper
Submitted
15 Jan 2014
Accepted
10 Mar 2014
First published
11 Mar 2014

CrystEngComm, 2014,16, 5859-5869

Author version available

Modulating the solubility of sulfacetamide by means of cocrystals

N. Rajesh Goud, R. A. Khan and A. Nangia, CrystEngComm, 2014, 16, 5859 DOI: 10.1039/C4CE00103F

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements