Polymorphic Characterization, Pharmacokinetics, and Anti-Inflammatory Activity of Ginsenoside Compound K Polymorphs

Polymorphism exhibits different physicochemical properties, which can impact the bioavailability and bioactivity of solid drugs. This study focused on identifying the polymorphs of ginsenoside compound K (CK) and studying their different behaviors in pharmacokinetics (PK) and pharmacodynamics (PD)....

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-04, Vol.26 (7), p.1983
Main Authors: Kuang, Yun-Yan, Gao, Xuan, Niu, Yi-Jun, Shi, Xun-Long, Zhou, Wei
Format: Article
Language:English
Subjects:
anti-inflammatory
Anti-inflammatory agents
Bioavailability
Biological activity
Calorimetry
Carrageenan
Differential scanning calorimetry
Dimorphism
Drug development
Edema
Females
Fourier analysis
Fourier transforms
ginsenoside compound K
Inflammation
Infrared analysis
Infrared spectroscopy
Organic solvents
Pharmacodynamics
Pharmacokinetics
Pharmacology
Phase transitions
Physicochemical properties
polymorph
Polymorphism
Scanning electron microscopy
Sexual dimorphism
Solvents
Spectrum analysis
Thermogravimetric analysis
Vibration
X ray powder diffraction
X-ray diffraction
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Summary:Polymorphism exhibits different physicochemical properties, which can impact the bioavailability and bioactivity of solid drugs. This study focused on identifying the polymorphs of ginsenoside compound K (CK) and studying their different behaviors in pharmacokinetics (PK) and pharmacodynamics (PD). Four CK polymorphs (form I, II, III, and IV) from organic solvents were characterized by scanning electron microscope (SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), and powder X-ray diffraction (PXRD). A feasible LC-MS/MS method was exploited to determine the PK parameters. Form II displayed the most exposure, followed by form I, III, and IV. Notably, all forms showed sex dimorphism, and the bioavailability in the female group was about two-fold higher than in the male group. The PD properties were investigated in carrageenan-induced acute paw inflammation, and form II at 20 mg/kg showed significant inhibition of edema by 42.7%. This study clarified the polymorphic, PK, and PD characters of four crystal forms of CK, and the data suggested that form II had the best efficacy for drug development.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26071983