Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal
A novel cocrystal of the potent H<sub>2</sub> 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 connect...
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MDPI AG
2019-07-01
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| Online Access: | https://www.mdpi.com/2073-4352/9/7/360 |
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| author | Yan Zhang Zhao Yang Shuaihua Zhang Xingtong Zhou |
| author_facet | Yan Zhang Zhao Yang Shuaihua Zhang Xingtong Zhou |
| author_sort | Yan Zhang |
| collection | DOAJ |
| description | A novel cocrystal of the potent H<sub>2</sub> 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) Å<sup>3</sup>, 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. |
| first_indexed | 2024-04-11T18:18:36Z |
| format | Article |
| id | doaj.art-28f354d2b9d34c70beac48f47567fd40 |
| institution | Directory Open Access Journal |
| issn | 2073-4352 |
| language | English |
| last_indexed | 2024-04-11T18:18:36Z |
| publishDate | 2019-07-01 |
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| spelling | doaj.art-28f354d2b9d34c70beac48f47567fd402022-12-22T04:09:49ZengMDPI AGCrystals2073-43522019-07-019736010.3390/cryst9070360cryst9070360Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine CocrystalYan Zhang0Zhao Yang1Shuaihua Zhang2Xingtong Zhou3School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, ChinaQingdao Institute for Food and Drug Control, Qingdao 266071, ChinaSchool of Pharmacy, Qingdao University, Qingdao 266071, ChinaQingdao Institute for Food and Drug Control, Qingdao 266071, ChinaA novel cocrystal of the potent H<sub>2</sub> 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) Å<sup>3</sup>, 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.https://www.mdpi.com/2073-4352/9/7/360cocrystalfamotidinemalonic acidcrystal structuresolubility |
| spellingShingle | Yan Zhang Zhao Yang Shuaihua Zhang Xingtong Zhou Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal Crystals cocrystal famotidine malonic acid crystal structure solubility |
| title | Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal |
| title_full | Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal |
| title_fullStr | Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal |
| title_full_unstemmed | Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal |
| title_short | Synthesis, Crystal Structure, and Solubility Analysis of a Famotidine Cocrystal |
| title_sort | synthesis crystal structure and solubility analysis of a famotidine cocrystal |
| topic | cocrystal famotidine malonic acid crystal structure solubility |
| url | https://www.mdpi.com/2073-4352/9/7/360 |
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