A method for improving the properties of famotidine

Yongfeng Zhao; Ying Fan; Yan Zhang; Hong Xu; Min Li; Yunjie Zhu; Zhao Yang

doi:10.1016/j.heliyon.2023.e17494

A method for improving the properties of famotidine

Heliyon. 2023 Jun 21;9(6):e17494. doi: 10.1016/j.heliyon.2023.e17494. eCollection 2023 Jun.

Authors

Yongfeng Zhao¹, Ying Fan², Yan Zhang³, Hong Xu⁴, Min Li⁵, Yunjie Zhu³, Zhao Yang^{1

3}

Affiliations

¹ College of Pharmacy, Qingdao University, Qingdao, 266071, China.
² Pharmacy Department, Qingdao Special Servicemen Recuperation Center of CPLA Navy, Qingdao, 266071, China.
³ Qingdao Institute for Food and Drug Control, Qingdao, 266073, China.
⁴ Shandong University of Science and Technology, Qingdao, 266590, China.
⁵ Anqiu People's Hospital, Weifang, 262199, China.

Abstract

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.

Keywords: Aqueous solubility; Crystal structure; Famotidine; M-nitrobenzoic acid; Permeability.