A method for improving the properties of famotidine
According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were chara...
| Main Authors: | , , , , , , |
|---|---|
| 格式: | 文件 |
| 语言: | English |
| 出版: |
Elsevier
2023-06-01
|
| 丛编: | Heliyon |
| 主题: | |
| 在线阅读: | http://www.sciencedirect.com/science/article/pii/S2405844023047023 |
| _version_ | 1827917686467723264 |
|---|---|
| author | Yongfeng Zhao Ying Fan Yan Zhang Hong Xu Min Li Yunjie Zhu Zhao Yang |
| author_facet | Yongfeng Zhao Ying Fan Yan Zhang Hong Xu Min Li Yunjie Zhu Zhao Yang |
| author_sort | Yongfeng Zhao |
| collection | DOAJ |
| description | According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, powder X-ray diffraction and X-ray single crystal diffraction. A single crystal structure of FMT–MNBA (1:1) was successfully obtained, and then the solubility and permeability of the newly synthesized salt cocrystal were studied. The results showed that, compared with free FMT, the FMT from the FMT–MNBA cocrystal showed improved permeability. This study provides a synthetic method to improve the permeability of BCS III drugs, which will contribute to the development of low-permeability drugs. |
| first_indexed | 2024-03-13T03:31:58Z |
| format | Article |
| id | doaj.art-00c552da451345c28ab7baa70ab123ff |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-03-13T03:31:58Z |
| publishDate | 2023-06-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-00c552da451345c28ab7baa70ab123ff2023-06-24T05:18:10ZengElsevierHeliyon2405-84402023-06-0196e17494A method for improving the properties of famotidineYongfeng Zhao0Ying Fan1Yan Zhang2Hong Xu3Min Li4Yunjie Zhu5Zhao Yang6College of Pharmacy, Qingdao University, Qingdao, 266071, ChinaPharmacy Department, Qingdao Special Servicemen Recuperation Center of CPLA Navy, Qingdao, 266071, ChinaQingdao Institute for Food and Drug Control, Qingdao, 266073, ChinaShandong University of Science and Technology, Qingdao, 266590, ChinaAnqiu People's Hospital, Weifang, 262199, ChinaQingdao Institute for Food and Drug Control, Qingdao, 266073, ChinaCollege of Pharmacy, Qingdao University, Qingdao, 266071, China; Qingdao Institute for Food and Drug Control, Qingdao, 266073, China; Corresponding author. College of Pharmacy, Qingdao University, Qingdao, 266071, China.According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, powder X-ray diffraction and X-ray single crystal diffraction. A single crystal structure of FMT–MNBA (1:1) was successfully obtained, and then the solubility and permeability of the newly synthesized salt cocrystal were studied. The results showed that, compared with free FMT, the FMT from the FMT–MNBA cocrystal showed improved permeability. This study provides a synthetic method to improve the permeability of BCS III drugs, which will contribute to the development of low-permeability drugs.http://www.sciencedirect.com/science/article/pii/S2405844023047023FamotidineM-nitrobenzoic acidCrystal structureAqueous solubilityPermeability |
| spellingShingle | Yongfeng Zhao Ying Fan Yan Zhang Hong Xu Min Li Yunjie Zhu Zhao Yang A method for improving the properties of famotidine Heliyon Famotidine M-nitrobenzoic acid Crystal structure Aqueous solubility Permeability |
| title | A method for improving the properties of famotidine |
| title_full | A method for improving the properties of famotidine |
| title_fullStr | A method for improving the properties of famotidine |
| title_full_unstemmed | A method for improving the properties of famotidine |
| title_short | A method for improving the properties of famotidine |
| title_sort | method for improving the properties of famotidine |
| topic | Famotidine M-nitrobenzoic acid Crystal structure Aqueous solubility Permeability |
| url | http://www.sciencedirect.com/science/article/pii/S2405844023047023 |
| work_keys_str_mv | AT yongfengzhao amethodforimprovingthepropertiesoffamotidine AT yingfan amethodforimprovingthepropertiesoffamotidine AT yanzhang amethodforimprovingthepropertiesoffamotidine AT hongxu amethodforimprovingthepropertiesoffamotidine AT minli amethodforimprovingthepropertiesoffamotidine AT yunjiezhu amethodforimprovingthepropertiesoffamotidine AT zhaoyang amethodforimprovingthepropertiesoffamotidine AT yongfengzhao methodforimprovingthepropertiesoffamotidine AT yingfan methodforimprovingthepropertiesoffamotidine AT yanzhang methodforimprovingthepropertiesoffamotidine AT hongxu methodforimprovingthepropertiesoffamotidine AT minli methodforimprovingthepropertiesoffamotidine AT yunjiezhu methodforimprovingthepropertiesoffamotidine AT zhaoyang methodforimprovingthepropertiesoffamotidine |