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Issue 26, 2017
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Bringing new life into old drugs: a case study on nifuroxazide polymorphism

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Abstract

This paper describes the rational search for and the synthesis of eight new polymorphs, solvates or hydrates of the well-known drug nifuroxazide. By selecting the appropriate polymorph, a 50% increase in solubility was obtained, compared to the commercially available solid form. The target molecule was chosen using hydrogen bond propensity models as a rational approach. All new forms were characterized by X-ray powder diffraction and thermal methods, and, in three cases, by single crystal X-ray diffraction. Two new solid anhydrous polymorphs were discovered and showed a significant increase in solubility and dissolution rates in water over the known solid form.

Graphical abstract: Bringing new life into old drugs: a case study on nifuroxazide polymorphism

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Article information


Submitted
13 Feb 2017
Accepted
15 May 2017
First published
15 May 2017

CrystEngComm, 2017,19, 3584-3591
Article type
Paper

Bringing new life into old drugs: a case study on nifuroxazide polymorphism

O. Covaci, R. Mitran, L. Buhalteanu, D. G. Dumitrescu, S. Shova and C. Manta, CrystEngComm, 2017, 19, 3584
DOI: 10.1039/C7CE00303J

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