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去氢骆驼蓬碱衍生物DH-004大鼠在体肠吸收动力学研究
引用本文:李玉玲,高惠静,冉鑫,马桂芝,滕亮. 去氢骆驼蓬碱衍生物DH-004大鼠在体肠吸收动力学研究[J]. 中国临床药理学杂志, 2021, 0(7): 878-882
作者姓名:李玉玲  高惠静  冉鑫  马桂芝  滕亮
作者单位:新疆医科大学药学院;新疆医科大学第一附属医院药学部省部共建中亚高发病成因与防治国家重点实验室
基金项目:中华医学会临床药学分会吴阶平医学基金会科研专项基金资助项目(320.6750.19090-9)。
摘    要:目的 考察去氢骆驼蓬碱衍生物DH-004大鼠在体肠吸收动力学特征,探讨其可能的吸收机制.方法 建立UPLC法测定灌流液中DH-004浓度,用大鼠在体单向肠灌流模型考察不同质量浓度的DH-004在不同肠段的吸收特征.结果 DH-004在全肠段均有吸收.20.0μg·mL-1 DH-004在十二指肠、空肠、回肠和结肠的吸收...

关 键 词:DH-004  去氢骆驼蓬碱衍生物  肠吸收  单向灌流法  UPLC

Study on the absorption kinetics of harmine derivative DH-004 in rat intestine
LI Yu-ling,GAO Hui-jing,RAN Xin,MA Gui-zhi,TENG Liang. Study on the absorption kinetics of harmine derivative DH-004 in rat intestine[J]. The Chinese Journal of Clinical Pharmacology, 2021, 0(7): 878-882
Authors:LI Yu-ling  GAO Hui-jing  RAN Xin  MA Gui-zhi  TENG Liang
Affiliation:(College of Pharmacy,Xinjiang Medical University,Urumqi 830011,Xinjiang Uygur Autonomous Region,China;State Key Laboratory of Pathogenesis,Prevention and Treatment of High Incidence Diseases in Central Asia,Department of Pharmacy,The First Affiliated Hospital of Xinjiang Medical University,Urumqi 830054,Xinjiang Uygur Autonomous Region,China)
Abstract:Objective To investigate the absorption characteristics of harmine derivative DH-004 in rat intestine and its possible absorption mechanism.Methods The concentration of DH-004 in perfusion solution was determined by UPLC,and in situ rats single pass perfusion model was used to investigate the absorption characteristics of different concentrations of DH-004 in different intestinal segments.Results DH-004 can be absorbed in all intestinal segments of rats.The absorption rate constants(Ka)of DH-00420.0μg·mL-1 in duodenum,jejunum,ileum and colon were(11.66±3.84)×10-2,(10.85±2.65)×10-2,(7.48±1.70)×10-2 and(4.75±1.14)×10-2 min,separately.The apparent permeability coefficients(Papp)were(1.47±0.33)×10-2,(1.55±0.20)×10-2,(1.25±0.10)×10-2 and(0.98±0.22)×10-2 cm·min-1,separately.Ka of DH-004 in duodenum and jejunum were significantly higher than those in ileum and colon(all P<0.05)Conclusion DH-004 can be absorbed in all segments of the rat intestine with different degrees.The main absorption segments for DH-004 may be the duodenum and jejunum.
Keywords:DH-004  harmine derivative  intestinal absorption  in situ rats single pass perfusion model  UPLC
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