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制备方法对无定形盐酸西那卡塞的影响

王闪闪, 樊伟明, 陈娟, 高缘

王闪闪, 樊伟明, 陈娟, 高缘. 制备方法对无定形盐酸西那卡塞的影响[J]. 中国药科大学学报, 2016, 47(3): 317-323. DOI: 10.11665/j.issn.1000-5048.20160312
引用本文: 王闪闪, 樊伟明, 陈娟, 高缘. 制备方法对无定形盐酸西那卡塞的影响[J]. 中国药科大学学报, 2016, 47(3): 317-323. DOI: 10.11665/j.issn.1000-5048.20160312
WANG Shanshan, FAN Weiming, CHEN Juan, GAO Yuan. Influence of preparation methods on amorphous cinacalcet hydrochloride[J]. Journal of China Pharmaceutical University, 2016, 47(3): 317-323. DOI: 10.11665/j.issn.1000-5048.20160312
Citation: WANG Shanshan, FAN Weiming, CHEN Juan, GAO Yuan. Influence of preparation methods on amorphous cinacalcet hydrochloride[J]. Journal of China Pharmaceutical University, 2016, 47(3): 317-323. DOI: 10.11665/j.issn.1000-5048.20160312

制备方法对无定形盐酸西那卡塞的影响

基金项目: 江苏省自然科学基金资助项目(No.BK20141351);江苏高校优势学科建设工程资助项目;浙江省微生物发酵与合成制药工程技术中心资助项目(No.2013E10030)

Influence of preparation methods on amorphous cinacalcet hydrochloride

  • 摘要: 采用溶液介导的减压旋转蒸发法(旋蒸法)、熔融液体介导的熔融冷却法(熔融法)及冷冻干燥法(冻干法)制备了无定形态的盐酸西那卡塞,并考察了制备方法对所制得的无定形物的理化性质(热行为、溶出度、稳定性等)的影响。结果表明,这3种方法制备的盐酸西那卡塞无定形物在溶出度和化学稳定性方面无差异,但在热力学行为和物理稳定性上表现出差异:虽玻璃化转变温度(Tg)相似,但转晶温度(Tc)有显著差异(旋蒸法、冻干法和熔融法制备的无定形盐酸西那卡塞的转晶温度分别为135.2、129.6和153.9 ℃);旋蒸法和冻干法所得无定形物在高温、高湿条件下的稳定性显著优于熔融法制备的无定形物。本研究为筛选无定形物的制备方法提供了实验基础。
    Abstract: In the present study, amorphous cinacalcet hydrochloride was prepared by three different approaches including rotary evaporation, quench-cooling and lyophilization. Physicochemical properties of prepared amorphous cinacalcet hydrochloride such as thermal behavior, dissolution and stability were investigated. Results showed that there was no difference in dissolution and chemical stability for amorphous cinacalcet hydrochloride prepared by these three different methods; however, these amorphous materials exhibited significant difference in thermodynamic behavior and physical stability: (1)They had similar Tg but with significant difference in Tc(135. 2, 129. 6 and 153. 9 °C for the amorphous products prepared by rotary evaporation, lyophilization and quench-cooling, respectively); (2)These amorphous products were easy to recrystallize under an environment with high temperature and humidity, especially that prepared by quench-cooling. This study provides an experimental basis for screening preparation methods of amorphous materials.
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  • 刊出日期:  2016-06-24

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