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Amorphous solid dispersion of berberine with absorption enhancer demonstrates a remarkable hypoglycemic effect via improving its bioavailability 期刊论文

编号：

01c348d8-ba7e-4a21-8407-c947e21faa87
作者：

Meng Zhaojie#^[1]Zhang Ming(张明)#^[1]Wei Shengnan^[1];Bi Xiaojia^[1];Hatch, Grant M.^[3];Gu Jingkai(顾景凯)*^[2]Chen Li(陈立)*^[1]
语种：

英文
期刊：

INTERNATIONAL JOURNAL OF PHARMACEUTICS ISSN：0378-5173 2014 年 467 卷 1-2 期 (50 - 59) ; JUN 5
收录：
关键词：

Berberine Sodium caprate Amorphous solid dispersion Bioavailability Hypoglycemic effect Type 2 diabetes
摘要：

Low oral bioavailability of berberine due to poor solubility and membrane permeability limits its clinical use for treatment of diabetes. We developed an amorphous solid dispersion of berberine with absorption enhancer sodium caprate, referred to as Huang-Gui Solid Dispersion (HGSD) preparations, and examined them for improvement of dissolution and oral bioavailability. HGSDs were prepared by solvent evaporation, and the formulations of amorphous solid dispersions were characterized by X-ray diffraction, differential scanning calorimetry and scanning electron microscopy. According to in vitro solubility and dissolution studies, P9, the 9th production of HGSDs based on orthogonal test, was sorted out. Then pharmacokinetic behavior of P9 was evaluated by in vitro membrane permeation, in situ intestinal perfusion, and in vivo bioavailability in rats. Furthermore, the anti-diabetic effect of P9 was examined in a type 2 diabetic rat model. It was found that majority of berberine in P9 existed in an amorphous form, and its solubility and dissolution rate were significantly increased. Pharmacokinetic studies demonstrated a 3-fold increase in in vitro membrane permeation, a 4-fold increase in in situ intestinal perfusion and a 5-fold increase in vivo bioavailability of P9 compared to berberine or berberine tablets. In addition, oral administration of P9 (100 mg/kg) improved glucose and lipid metabolism in diabetic rats compared to pure berberine (100 mg/kg), berberine tablets (100 mg/kg) or metformin (300 mg/kg) treatment. These findings indicate that P9 enhances oral bioavailability of berberine and may be a potential candidate drug for treatment of diabetes. (C) 2014 Published by Elsevier B. V.
推荐引用方式
GB/T 7714：

Meng Zhaojie,Zhang Ming,Wei Shengnan, et al. Amorphous solid dispersion of berberine with absorption enhancer demonstrates a remarkable hypoglycemic effect via improving its bioavailability [J].INTERNATIONAL JOURNAL OF PHARMACEUTICS,2014,467(1-2):50-59.
APA：

Meng Zhaojie,Zhang Ming,Wei Shengnan,Bi Xiaojia,&Chen Li.(2014).Amorphous solid dispersion of berberine with absorption enhancer demonstrates a remarkable hypoglycemic effect via improving its bioavailability .INTERNATIONAL JOURNAL OF PHARMACEUTICS,467(1-2):50-59.
MLA：

Meng Zhaojie, et al. "Amorphous solid dispersion of berberine with absorption enhancer demonstrates a remarkable hypoglycemic effect via improving its bioavailability" .INTERNATIONAL JOURNAL OF PHARMACEUTICS 467,1-2(2014):50-59.
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