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小檗碱磷脂固体分散体改善氧化应激治疗2型糖尿病
引用本文:童帅,尹明星,马永贵,施春阳,方建国. 小檗碱磷脂固体分散体改善氧化应激治疗2型糖尿病[J]. 中国药学杂志, 2022, 57(5): 363-372. DOI: 10.11669/cpj.2022.05.006
作者姓名:童帅  尹明星  马永贵  施春阳  方建国
作者单位:1.华中科技大学同济医学院附属同济医院药学部, 武汉 430030;
2.华中科技大学同济-荣程生命科学与医学研究中心, 武汉 430030
基金项目:湖北省自然科学基金面上项目资助(2019CFB744)
摘    要:目的 制备包载小檗碱(BBR)的磷脂固体分散体促进药物吸收,增强降糖、降脂药效,并初步阐明其抗2型糖尿病(T2DM)作用机制.方法 溶剂挥发法制备小檗碱磷脂固体分散体(SD),对其粒径、形貌、体外释放、胃肠道吸收、治疗T2DM药效和作用机制进行了充分研究.结果 SD在水溶液中粒径约为118 nm,形貌为球形;相比于游离...

关 键 词:小檗碱  磷脂固体分散体  2型糖尿病  氧化应激
收稿时间:2021-06-21

Berberine Loaded Phospholipid Solid Dispersion for the Treatment of Type 2 Diabetes Mellitus by Ameliorating Oxidative Stress
TONG Shuai,YIN Ming-xing,MA Yong-gui,SHI Chun-yang,FANG Jian-guo. Berberine Loaded Phospholipid Solid Dispersion for the Treatment of Type 2 Diabetes Mellitus by Ameliorating Oxidative Stress[J]. Chinese Pharmaceutical Journal, 2022, 57(5): 363-372. DOI: 10.11669/cpj.2022.05.006
Authors:TONG Shuai  YIN Ming-xing  MA Yong-gui  SHI Chun-yang  FANG Jian-guo
Affiliation:1. Department of Pharmacy, Tongji Hospital Affiliated to Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China;
2. Tongji-Rongcheng Center for Biomedicine, Huazhong University of Science and Technology, Wuhan 430030, China
Abstract:OBJECTIVE To prepare berberine(BBR) loaded phospholipid solid dispersion and realize the enhanced drug absorption and antidiabetic effect.. METHODS Berberine (BBR) loaded phospholipid solid dispersion (SD) was prepared by solvent evaporation method. The particle size, morphology, in vitro release property, gastrointestinal absorption profile, antidiabetic effect and mechanism of SD were fully investigated. RESULTS SD was with a mean hydrodynamic diameter of ≈118 nm and a near spherical shape. SD exhibited faster in vitro BBR release, enhanced in vivo gastrointestinal absorption than free BBR, and thus resulted in significantly decreased fasting blood glucose, insulin, triglycerides, total cholesterol, low density lipoprotein and liver malondialdehyde levels, and significantly increased the liver superoxide dismutase, glutathione levels and expression of HO-1in T2DM mice compared with free BBR, which demonstrated tissue protection of SD. CONCLUSION SD can significantly increase the gastrointestinal absorption and antidiabetic effect of BBR via ameliorating oxidative stress in T2DM mice.
Keywords:berberine  phospholipid solid dispersion  type 2 diabetesmellitus  oxidative stress   
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