黄芩素固体分散体的制备、表征及体内外释药研究

doi:10.16431/j.cnki.1671-7236.2024.05.037

Abstract

Abstract: 【Objective】 The aim of this study was to improve the solubility of baicalein (BAI),enhance its dissolution and bioavailability,and expand its clinical application.【Method】 Solid dispersion of baicalein (BAI-ASD) was prepared by rotary evaporation using polyethylene caprolactam-polyethylene acetate-polyethylene glycol graft copolymer (Soluplus) as the carrier,and it was characterized including that:Using the position and intensity of the characteristic diffraction peaks in powder X-ray diffraction (PXRD) to preliminarily determine whether the solid dispersion was successfully prepared;Differential scanning calorimetry (DSC) was used to study thermal properties;Fourier transform infrared spectroscopy (FT-IR) was used to analyze intermolecular interactions;Scanning electron microscopy (SEM) was used to observe the microscopic topography.The in vitro release performance was investigated by dissolution test,and the pharmacokinetic characteristics of oral BAI-ASD in chickens were investigated.【Result】 There was no crystal diffraction peak of BAI baicalein in PXRD and no obvious endothermic peak in DSC,indicating that the baicalein solid dispersion BAI-ASD was successfully prepared,and BAI baicalein existed in an amorphous form in the solid dispersion ASD.The results of in vitro dissolution showed that the cumulative dissolution of baicalein BAI within 240 min was only 6.62%,and the cumulative dissolution of solid dispersion ASD was significantly increased when the ratio was 1∶9 and 2∶8,and the cumulative dissolution within 240 min was 29.89% and 52.67%,respectively.The stability study results showed that BAI-ASD had good stability within 90 days at 45 ℃ and 75% RH.The pharmacokinetic results showed that the peak concentration (C_max(0-24)) and area under the curve (AUC_(0-24)) of BAI-ASD within 24 h of intragastric administration were (5.20±0.82) μg/mL and (17.03±0.67) μg·h/mL,respectively,which were 1.91 and 2.64 times of BAI,respectively.【Conclusion】 BAI-ASD,a solid dispersion of baicalein prepared by rotary evaporation with Soluplus as the carrier,had good stability,which could effectively improve the cumulative dissolution and oral bioavailability of BAI.

Key words: baicalein(BAI); amorphous solid dispersion; Soluplus; cumulative dissolution; bioavailability

CLC Number:

S859.7

GAO Jianting, LU Chenyue, SHI Xinchao, HE Xin. Preparation,Characterization and in vitro and in vivo Drug Release of Baicalein Solid Dispersion[J]. China Animal Husbandry and Veterinary Medicine, 2024, 51(5): 2169-2177.

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Preparation,Characterization and in vitro and in vivo Drug Release of Baicalein Solid Dispersion

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