盐酸雷诺嗪结晶水及其对晶体稳定性的影响  

Crystalline Water of Ranolazine Hydrochloride and the Influence on its Crystallization

作　　者：邹文博[1] 胡昌勤[1] 

机构地区：[1]中国食品药品检定研究院,北京100050

出　　处：《中国药事》2013年第8期859-863,共5页Chinese Pharmaceutical Affairs

摘　　要：目的通过研究盐酸雷诺嗪结晶水及其对晶体稳定性的影响,探讨盐酸雷诺嗪半水合物水分含量不稳定的原因及可能对其质量产生的影响。方法利用单晶X-射线衍射、热重分析和动态水分吸附法,分析盐酸雷诺嗪半水合物中结晶水分子在晶体中的稳定性;采用粉末X-射线衍射分析结合卡尔-费休氏法测定水分含量,分析盐酸雷诺嗪半水合物中的结晶水分子对晶体结构的影响。结果结晶水在晶体中不稳定,极易脱去,仅约0.3%的水分可以与盐酸雷诺嗪分子稳定结合,盐酸雷诺嗪半水合物的生产工艺稳定,结晶水分子的丢失对其晶体结构影响不大。结论可以根据产品的长期稳定性试验结果调整水分限度。Objective To discuss the reason for the instability of water content of ranolazine hydrochloride and the possible influence to its quality by studying the impact on the crystal lattice of crystalline water of ranolazine hydrochloride. Methods Analyze the stability of crystalline water in the crystal lattice of ranolazine hydrochloride by means of single crystal X-ray diffraction, TGA and dynamic vapor sorption. Analyze the influence to crystal lattice by crystalline water using X-ray powder diffraction and Karl-Fischer method. Results The crystalline water in the ranolazine molecule was found to be unstable and easily released from the lattice. About 0.3% of water content combines tightly with the ranolazine molecular. Nevertheless, the releasing of the crystalline water nearly has no impact on the crystal lattice. Conclusion The limit of water content needs to be revised according to the results of long term stability test.

关 键 词：盐酸雷诺嗪 结晶水 稳定性 单晶X-射线衍射 粉末X-射线衍射 卡尔-费休氏法 热重分析 动态水分吸附法 

分 类 号：R927.11[医药卫生—药学]