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.
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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