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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)
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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MDPI and ACS Style

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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