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Bringing new life into old drugs. A case study on nifuroxazide polymorphism

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 show a significant increase in solubility and dissolution rates in water over the known solid form.

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Publication details

The article was received on 13 Feb 2017, accepted on 15 May 2017 and first published on 15 May 2017


Article type: Paper
DOI: 10.1039/C7CE00303J
Citation: CrystEngComm, 2017, Accepted Manuscript
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    Bringing new life into old drugs. A case study on nifuroxazide polymorphism

    O. I. Covaci, R. -. A. A. Mitran, L. Buhalteanu, D. Dumitrescu, S. Sova and C. M. Manta, CrystEngComm, 2017, Accepted Manuscript , DOI: 10.1039/C7CE00303J

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