目的:应用共晶技术提高硝苯地平的光稳定性。方法:选择异烟酰胺为共晶形成物与硝苯地平采用溶剂挥发法制备共晶,共晶的组成和结构通过X射线单晶衍射测定,同时通过红外光谱法(IR)、差示扫描量热法(DSC)、热重法(TGA)对共晶进行表征,并考察了共晶的光稳定性。结果:硝苯地平-异烟酰胺共晶结晶于P21/n空间群,不对称单元包含1个硝苯地平分子和1个异烟酰胺分子,通过3种氢键相互相连。稳定性考察试验将硝苯地平和共晶分别在光照条件下放置10 d后,分别与各自0 d的硝苯地平含量相比,硝苯地平含量从97.6%降至10.5%,共晶中硝苯地平含量从96.0%降至61.0%。结论:制备的硝苯地平-异烟酰胺共晶提高了硝苯地平的光稳定性。
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.
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ChP 2020. VolⅡ[S]. 2020: 1534
