Abstract
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.
Highlights
We have isolated a fungus of Paecilomyces bainer sp.229, which could effectively produce compound K (CK) by the biotransformation pathway of Rb1 → Rd → F2 → CK, and found a new approval of CK in treating rheumatoid arthritis (RA) [4,5,6]
Three techniques were used for the polymorphs preparation in the present study: (1) rapid solvent evaporation in a vacuum and high-temperature condition; (2) gradual solvent evaporation in a small opening glass tube at room temperature, and (3) anti-solvent precipitation in water
Form IV showed a big block appearance and had a wavy surface under an optical microscope (Figure S1). These results indicated forms I, II, III, and IV displayed the apparent differences due to the different molecular arrangements in different solvents, respectively
Summary
Triterpene saponins, commonly known as ginsenosides, are the major pharmacologically active ginseng components [1,2]. We have isolated a fungus of Paecilomyces bainer sp.229, which could effectively produce compound K (CK) by the biotransformation pathway of Rb1 → Rd → F2 → CK, and found a new approval of CK in treating rheumatoid arthritis (RA) [4,5,6].
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