Safety Monitoring

Improving photostability of nifedipine by cocrystal synthesis

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  • 1. Qingdao Institute for Food and Drug Control, Qingdao 266071, China;
    2. National Institutes for Food and Drug Control, Beijing 100050, China;
    3. Qingdao Women and Children's Hospital, Qingdao 266011, China

Revised date: 2022-06-11

  Online published: 2024-06-24

Abstract

Objective: To improve the light stability of nifedipine by cocrystal synthesis. Methods: Isonicotinamide was selected as the cocrystal former to produce cocrystal with nifedipine by solution evaporation. The components and structure of cocrystal were determined by single crystal X-ray diffraction. Meanwhile, the eutectic was characterized by infrared spectroscopy(IR),differential scanning calorimetry (DSC) and thermogravimetric analyze (TGA). In addition, the stability under illumination conditions of cocrystal was studied. Results: Nifedipine-isonicotinamide cocrystalcrystallized in space group P21/n, and the asymmetric unit consisted of one nifedipine molecule and one isonicotinamide molecule, which were connected by three kinds of H-bond. In the stability test, subsequent to the exposures of nifedipine and cocrystal under the light for 10 d, the contents of nifedipine decreased from 97.6% to 10.5%, while the contents of nifedipine in cocrystal decreased from 96.0% to 61.0%, comparing with initial content. Conclusion: This study reveals that the photostability of nifedipine is significantly improved through the synthesis of cocrystal with isonicotinamide.

Cite this article

ZHANG Yan, NING Bao-ming, ZHOU Xing-tong, YANG Zhao, WANG Zun-wen . Improving photostability of nifedipine by cocrystal synthesis[J]. Chinese Journal of Pharmaceutical Analysis, 2022 , 42(7) : 1241 -1246 . DOI: 10.16155/j.0254-1793.2022.07.18

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