Inhibition of transformation from puerarin monohydrate to puerarin dihydrate by polyvinylpyrrolidones during dissolution
10.16438/j.0513-4870.2016-1015
- VernacularTitle:聚乙烯吡咯烷酮抑制葛根素一水合物在溶出过程中向二水合物的转变
- Author:
Zhao-yi ZHONG
1
;
Min WU
1
;
Shuai QIAN
1
;
Jian-jun ZHANG
2
;
Yuan GAO
1
Author Information
1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
2. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
puerarin;
hydrate;
polymer;
dissolution;
transformation
- From:
Acta Pharmaceutica Sinica
2017;52(2):302-308
- CountryChina
- Language:Chinese
-
Abstract:
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.
