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Open AccessArticle

Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal

1
School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
2
Qingdao Institute for Food and Drug Control, Qingdao 266071, China
3
School of Pharmacy, Qingdao University, Qingdao 266071, China
*
Author to whom correspondence should be addressed.
Crystals 2019, 9(7), 360; https://doi.org/10.3390/cryst9070360
Received: 15 May 2019 / Revised: 8 July 2019 / Accepted: 10 July 2019 / Published: 15 July 2019
(This article belongs to the Special Issue Pharmaceutical Crystals)
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Abstract

A novel cocrystal of the potent H2 receptor antagonist famotidine (FMT) was synthesized with malonic acid (MAL) to enhance its solubility. The cocrystal structure was characterized by X-ray single crystal diffraction, and the asymmetry unit contains one FMT and one MAL connected via intermolecular hydrogen bonds. The crystal structure is monoclinic with a P21/n space group and unit cell parameters a = 7.0748 (3) Å, b = 26.6502 (9) Å, c = 9.9823 (4) Å, α = 90, β = 104.2228 (12), γ = 90, V = 1824.42 (12) Å3, and Z = 4. The cocrystal had unique thermal, spectroscopic, and powder X-ray diffraction (PXRD) properties that differed from FMT. The solubility of the famotidine-malonic acid cocrystal (FMT-MAL) was 4.2-fold higher than FMT; the FAM-MAL had no change in FMT stability at high temperature, high humidity, or with illumination. View Full-Text
Keywords: cocrystal; famotidine; malonic acid; crystal structure; solubility cocrystal; famotidine; malonic acid; crystal structure; solubility
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Zhang, Y.; Yang, Z.; Zhang, S.; Zhou, X. Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal. Crystals 2019, 9, 360.

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