贵州医科大学学报

2019, v.44;No.231(12) 1401-1407

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灯盏花乙素磷脂复合物固体分散体的离体小肠吸收研究
Study on Intestinal Absorption of Scutellarin Ethylphospholipid Complex Solid Dispersion in Vitro

周威;薛雨晨;贺智勇;肖婷;姜丰;周雪;吴林菁;沈祥春;陶玲;
ZHOU Wei;XUE Yuchen;HE Zhiyong;XIAO Ting;JIANG Feng;ZHOU Xue;WU Linjing;SHEN Xiangchun;TAO Ling;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University, Engineering Center for Efficient Utilization of Natural Drug Resources in Guizhou Province, Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Drugs in Colleges and Universities in Guizhou Province, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Optimal U

摘要(Abstract):

目的:分析灯盏花乙素磷脂复合物固体分散体的离体小肠吸收。方法:采用溶剂法制备不同处方和工艺的灯盏花乙素磷脂复合物固体分散体(DZ-PC-SD)等制剂,以体外累积释放百分率为指标,单因素试验方法优选处方和制备工艺;SD大鼠随机分成灯盏花乙素(DZ)组、灯盏花乙素磷脂复合物(DZ-PC)组、DZ-PC-SD(PEG6000)组和DZ-PC-SD(PVPK17)组,每组6只,考察DZ、DZ-PC及DZ-PC-SD在大鼠十二指肠、空肠、回肠的吸收速率常数。结果:DZ-PC-SD的最佳制备工艺为DZ-PC∶PEG6 000是1∶2,二氯甲烷10 mL,有机溶剂挥发温度为40℃;DZ-PC-SD在240 min体外累积释放百分率为(99.35±1.14)%,DZ-PC和DZ-PC-SD在肠道各吸收部位的吸收速率常数K_a均大于DZ,其中在十二指肠的吸收最多, DZ-PC-SD (PEG6000)的小肠吸收速率常数达到(24.48±0.65)×10~(-2)μg/(min·cm~2)。结论:溶剂法成功制备得到DZ-PC-SD,该制备工艺简便、稳定,DZ-PC和DZ-PC-SD均能有效促进灯盏花乙素在肠道的吸收。
Objective: Analysis of in vitro small intestine absorption of scutellarin A phospholipid complex solid dispersion. Methods: Solvent method is used to obtain preparations of breviscapine phospholipid complex solid dispersion(DZ-PC-SD) with different prescriptions and processes, and the single factor test method was used to optimize its formulation and preparation process with in-vitro cumulative dissolution as evaluation index. SD rats were randomly divided into 4 groups, breviscapine(DZ) group, breviscapine phospholipid complex(DZ-PC) group, DZ-PC-SD(PEG6000) group, and DZ-PC-SD(PVPK17) group. There were 6 rats of each group. The absorption rate constants of DZ, DZ-PC and DZ-PC-SD in rat duodenum, jejunum and ileum were investigated. Results: The best preparation process of DZ-PC-SD is DZ-PC, PEG6 000 is 1 ∶2, dichloromethane is 10 mL, and the evaporation temperature of organic solvent is 40 ℃. The cumulative release rate of DZ-PC-SD in vitro at 240 minutes was(99.35±1.14)%. The absorption rate constants Ka of DZ-PC and DZ-PC-SD at the absorption sites of the intestinal tract are greater than DZ, and the absorption in the duodenum is the highest. And DZ-PC-SD(PEG6000) has a small intestine absorption rate constant of(24.48±0.65)×10~(-2) μg/(min·cm~2). Conclusion: The solvent method to prepare the DZ-PC-SD was successful. The preparation process is simple and stable. DZ-PC and DZ-PC-SD can effectively promote the absorption of breviscapine in the intestine.

关键词(KeyWords): 肠吸收;灯盏花乙素;磷脂复合物;固体分散体;体外释放;天然药物
Intestinal absorption;Scutellarin;phospholipid complex;solid dispersions;in vitro release;natural medicine

Abstract:

Keywords:

基金项目(Foundation): 贵州省天然药物成药性人才基地[黔人领发(2018)3];; 贵州省高层次创新型人才“百层次”人才项目[黔科合人才(2015)4029];; 贵州医科大学药学国际科技合作基地[黔科合平台人才(2017)5802];; 贵州省科技厅国际合作项目[黔科合外G字(2012)7041]

作者(Author): 周威;薛雨晨;贺智勇;肖婷;姜丰;周雪;吴林菁;沈祥春;陶玲;
ZHOU Wei;XUE Yuchen;HE Zhiyong;XIAO Ting;JIANG Feng;ZHOU Xue;WU Linjing;SHEN Xiangchun;TAO Ling;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University, Engineering Center for Efficient Utilization of Natural Drug Resources in Guizhou Province, Key Laboratory of Pharmacology and Pharmacological Evaluation of Natural Drugs in Colleges and Universities in Guizhou Province, Guizhou Medical University-Guiyang Joint Key Laboratory, Key Laboratory of Optimal U

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DOI: 10.19367/j.cnki.1000-2707.2019.12.007

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