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Inhibition of transformation from puerarin monohydrate to puerarin dihydrate by polyvinylpyrrolidones during dissolution
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Zhao-yi ZHONG1, Min WU1, Shuai QIAN1, Jian-jun ZHANG2, Yuan GAO1, *
Acta Pharmaceutica Sinica | 2017, 52(2) : 302 - 308
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Acta Pharmaceutica Sinica | 2017, 52(2): 302-308
• Pharmaceutics •
Inhibition of transformation from puerarin monohydrate to puerarin dihydrate by polyvinylpyrrolidones during dissolution
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Zhao-yi ZHONG1, Min WU1, Shuai QIAN1, Jian-jun ZHANG2, Yuan GAO1, *
Affiliations
  • 1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
  • 2. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
Published: 2017-02-12 doi: 10.16438/j.0513-4870.2016-1015
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Puerarin (PUE), an isoflavone with anti-inflammation, anti-oxidation and neuroprotection effects, has been widely applied to the treatment of cardiovascular diseases in clinics in China. In the current study, we reported that the active pharmaceutical ingredient (API) of marketed products was the PUE monohydrate (PUEMH). During its supersaturated dissolution, the PUE concentration quickly reached a plateau, followed by a gradually concentration decrease to another lower plateau. In order to explore the internal mechanism of above phenomenon, the solid residues after saturated dissolution test were characterized by powder X-ray diffraction (PXRD), thermal gravity analysis (TGA) and Karl Fisher titration (KFT). PXRD suggested that a novel PUE crystal different from PUEMH formed during its dissolution, the following TGA and KFT confirmed the generation of PUE dihydrate (PUEDH) with much lower solubility. Moreover, polyvinylpyrrolidones (PVPK12, PVPK30 and PVPK90) were added in the dissolution medium to investigate their potential inhibition effects on such crystal transformation during dissolution process. We observed that polymers could inhibit the transformation from PUEMH to PUEDH and result in much higher PUE concentration level than that in pure water.

puerarin  /  hydrate  /  polymer  /  dissolution  /  transformation
Zhao-yi ZHONG, Min WU, Shuai QIAN, Jian-jun ZHANG, Yuan GAO. Inhibition of transformation from puerarin monohydrate to puerarin dihydrate by polyvinylpyrrolidones during dissolution[J]. Acta Pharmaceutica Sinica, 2017 , 52 (2) : 302 -308 . DOI: 10.16438/j.0513-4870.2016-1015
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Article Info
doi: 10.16438/j.0513-4870.2016-1015
  • Receive Date：2016-10-01
  • Online Date：2026-01-14
  • Published：2017-02-12
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History
  • Received：2016-10-01
  • Revised：2016-11-24
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    1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
    2. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
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表12种不同金属材料的力学参数
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Number of
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Number of
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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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