Preparation and in vitro-in vivo evaluation of intestinal retention pellets of Berberine chloride to enhance hypoglycemic and lipid-lowing efficacy

论文摘要

Berberine chloride（BBR） is a pharmacokinetic profile of drug with poor bioavailability but good therapeutic efficacy,which is closely related to the discovery of BBR intestinal target.The major aim of this paper is to develop BBR intestinal retention type sustained-release pellets and evaluate their in vivo and in vitro behaviors base on the aspect of local action on intestinal tract. Here,wet milling technology is used to improve dissolution and dissolution rate of BBR by decreasing the particle size and increasing the wettability. The pellets are prepared by liquid layer deposition technology,and then the core pellets are coated with Eudragit?L30 D-55 and Eudragit?NE30 D aqueous dispersion. The prepared pellets show high drug loading capacity,and the drug loading up to 93%. Meanwhile,it possesses significant sustained drug release effect in purified water which is expected to improve the pharmacokinetic behavior of BBR. The pharmacokinetics results demonstrate that the halflife of BBR was increased significantly from 24 h to 36 h and the inter-and intra-subject variability are decreased compared to commercial BBR tablets. The retention test results indicate that the pellet size and Eudragit?NE30 D plays an important role in retention time of the pellet,and it is found that the pellets with small particle size and high Eudragit?NE30 D coating content can stay longer in the intestine than the pellets with large particle size. All in all,BBR intestinal retention type pellets are prepared successfully in this study,and the pellets show satisfactory in vivo and in vitro behaviors.

论文目录

文章来源

类型: 期刊论文

作者: Guofei Li,Mingming Zhao,Xianying Su,Lin Song,Limei Zhao

来源: Asian Journal of Pharmaceutical Sciences 2019年05期

年度: 2019

分类: 医药卫生科技,工程科技Ⅰ辑

专业: 有机化工,药学

单位: Shengjing Hospital of China Medical University,Northeast Pharmaceutical Science & Technology Development Co.,Ltd.

分类号: R943;R96

页码: 559-568

总页数: 10

文件大小: 3960K

下载量: 18

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