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通过溶剂旋转蒸发法制备染料木黄酮固体分散体以改善高脂饮食诱导肥胖小鼠的溶解度、生物利用度及改善效果

Solid Dispersions of Genistein via Solvent Rotary Evaporation for Improving Solubility, Bioavailability, and Amelioration Effect in HFD-Induced Obesity Mice.

作者信息

Qiu Chenxu, Zhang Yancui, Fan Yingsai, Li Shupeng, Gao Jianting, He Xin, Zhao Xinghua

机构信息

College of Veterinary Medicine, Hebei Agricultural University, Baoding 071000, China.

出版信息

Pharmaceutics. 2024 Feb 22;16(3):306. doi: 10.3390/pharmaceutics16030306.

DOI:10.3390/pharmaceutics16030306
PMID:38543200
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10975362/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/a73e50a2dd83/pharmaceutics-16-00306-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/9b646bacf191/pharmaceutics-16-00306-g010.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/3c53f5d32db7/pharmaceutics-16-00306-g004.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/4455bcd31472/pharmaceutics-16-00306-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/1c3dae6911e9/pharmaceutics-16-00306-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/dec8acb223ca/pharmaceutics-16-00306-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/9b646bacf191/pharmaceutics-16-00306-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5e7a/10975362/a73e50a2dd83/pharmaceutics-16-00306-g011.jpg

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