Qiu Chenxu, Zhang Yancui, Fan Yingsai, Li Shupeng, Gao Jianting, He Xin, Zhao Xinghua
College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China.
Pharmaceutics. 2024 Feb 22;16(3):306. doi: 10.3390/pharmaceutics16030306.
Genistein (GEN) is an active pharmaceutical ingredient that presents the challenges of poor water solubility and low oral bioavailability. To tackle these challenges, a GEN solid dispersion was prepared by solvent rotary evaporation using polyvinylpyrrolidone K30 (PVP K30) as a carrier. The optimal formulation was determined by drug loading efficiency and in vitro release. The physical state of the solid dispersion was characterized by DSC, XRD, SEM and FT-IR. And the results of the in vitro release study indicate that the drug release of SD (1:7) increased 482-fold that of pure GEN at 60 min. Following oral administration to rats, the C and AUC of SD (1:7) was increased 6.86- and 2.06-fold to that of pure GEN. The adipose fat index and body weight of the SD (1:7) group were significantly lower than those of the GEN group ( < 0.05). Meanwhile, the levels of TC and TG in the serum were significantly decreased in the SD (1:7) group compared with the GEN group ( < 0.05). All experiments revealed that solid dispersion could be a promising formulation approach to improve the dissolution rate, oral bioavailability, and effect on the reduction of lipid accumulation in high-fat diet-induced obesity mice.
染料木黄酮(GEN)是一种活性药物成分,存在水溶性差和口服生物利用度低的问题。为应对这些挑战,以聚乙烯吡咯烷酮K30(PVP K30)为载体,通过溶剂旋转蒸发法制备了GEN固体分散体。通过载药效率和体外释放确定了最佳配方。采用差示扫描量热法(DSC)、X射线衍射法(XRD)、扫描电子显微镜(SEM)和傅里叶变换红外光谱法(FT-IR)对固体分散体的物理状态进行了表征。体外释放研究结果表明,在60分钟时,SD(1:7)的药物释放量比纯GEN增加了482倍。大鼠口服给药后,SD(1:7)的Cmax和AUC分别比纯GEN增加了6.86倍和2.06倍。SD(1:7)组的脂肪指数和体重显著低于GEN组(P<0.05)。同时,与GEN组相比,SD(1:7)组血清中总胆固醇(TC)和甘油三酯(TG)水平显著降低(P<0.05)。所有实验表明,固体分散体可能是一种有前景的制剂方法,可提高高脂饮食诱导的肥胖小鼠的溶解速率、口服生物利用度以及减少脂质积累的效果。