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Establishment of a cocrystal characterization method for sacubitril valsartan sodium
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Jing XIONG1, 2, De-zhong XU1, Xin-yi XU3, Yang LU:4, Shi-ying YANG*, 4, Si-cen WANG*, 2
Acta Pharmaceutica Sinica | 2021, 56(2) : 577 - 584
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Acta Pharmaceutica Sinica | 2021, 56(2): 577-584
• Original Articles •
Establishment of a cocrystal characterization method for sacubitril valsartan sodium
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Jing XIONG1, 2, De-zhong XU1, Xin-yi XU3, Yang LU:4, Shi-ying YANG*, 4, Si-cen WANG*, 2
Affiliations
  • 1. National Institutes for Food and Drug Control, NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs, Beijing 102629, China
  • 2. School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China
  • 3. Chinese Pharmacopoeia Commission, Beijing 100061, China
  • 4. Beijing Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2021-02-12 doi: 10.16438/j.0513-4870.2020-1811
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Sacubitril valsartan sodium(LCZ696) is an ionic cocrystal drug. The purpose of this study was to explore the cocrystal features of LC696 by establishing a variety of characterization methods, and thus provide basic research data for effective quality control. The cocrystal characteristics of LCZ696 and its tablets were identified by applying analytical means including powder X-ray diffraction(PXRD), fourier transform infrared spectroscopy(FTIR), Raman spectra(RM), differential scanning calorimetry(DSC) and solid-state nuclear magnetic resonance spectroscopy(ssNMR). The crystalline water and hygroscopicity of LCZ696 were analyzed by thermogravimetric analysis(TGA), dynamic vapor sorption(DVS), hygroscopicity test and Karl Fischer reaction method.The results show that PXRD, FTIR, DSC and ssNMR can effectively distinguish the features of LCZ696 cocrystal, sacubitril monomer, valsartan monomer, and sacubitril-valsartan(1∶1) mixture. RM can be used as a supplementary approach. Combined with the analysis by TGA, DVS, hygroscopicity test and Karl Fischer reaction method results, LCZ696 contains 2.5 crystalline water molecules and is very hygroscopic; we recommend that LCZ696 be stored in an environment with a relative humidity below 60%. By characterizing the crystal features we can establish quality control measure and evaluate the stability of the drug tablets. This study provides data in support for the establishment of the LCZ696 quality standard.

heart failure  /  sacubitril valsartan sodium  /  cocrystal  /  characterization  /  powder X-ray diffraction  /  solid-state nuclear magnetic resonance spectroscopy  /  dynamic vapor sorption  /  hygroscopicity
Jing XIONG, De-zhong XU, Xin-yi XU, Yang LU:, Shi-ying YANG, Si-cen WANG. Establishment of a cocrystal characterization method for sacubitril valsartan sodium[J]. Acta Pharmaceutica Sinica, 2021 , 56 (2) : 577 -584 . DOI: 10.16438/j.0513-4870.2020-1811
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Year 2021 volume 56 Issue 2
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Article Info
doi: 10.16438/j.0513-4870.2020-1811
  • Receive Date：2020-11-25
  • Online Date：2025-12-18
  • Published：2021-02-12
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History
  • Received：2020-11-25
  • Revised：2021-01-05
Funding
Affiliations
    1. National Institutes for Food and Drug Control, NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs, Beijing 102629, China
    2. School of Pharmacy, Xi'an Jiaotong University, Xi'an 710061, China
    3. Chinese Pharmacopoeia Commission, Beijing 100061, China
    4. Beijing Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
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Family		 属数
Number of
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Number of
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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