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脱水穿心莲内酯在大鼠的药代动力学

Pharmacokinetics of Anhydroandrographolide in Rats

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【作者】 李克敏刘文清朱治本

【Author】 Li Kemin Liu Wenqing Zhu Zhiben(Department of Pharmacology and Research Laboratory ofClinical Pharmacology of First Affiliated Hospital, Chongqing University of Medical Sciences, Chongqing 630041)

【机构】 重庆医科大学药理教研室第一附属医院临床药理研究室 重庆 630041重庆 630041重庆 630041

【摘要】 脱水穿心莲内酯二琥珀酸半酯单钾盐(DASK,商品名炎琥宁)100mg/kgiv后的药时数据可拟合开放性二室模型,分布相很短。150mg/kg im后所得药时数据可拟合开放性一室模型,吸收较快而完全。iv与im后求得的Vd、CL和消除相t1/2无明显差别。本品与血浆蛋白的结合率较低。im后24h内DASK原形物尿中仅排出24.9±18.1%,由胆汁和粪中排出量还要少些。

【Abstract】 Anhydroandrographolide is a constituent of the Chinese herbal drug Andrographis paniculata Nees. The injectable preparation monopotassium anhydroandrog-rapholide disuccinate (DASK) is used clinically. Some pharmacokinetic characteristics of DASK in rats were reported in present paper.The plasma concentration-time data obtained after iv 100 mg/kg were fitted with the open two compartment model and the ch- ief kinetic parameters were as follows: and After im 150mg/kg the plasma concentration-time data were fitted with the one compartment model and the important kinetic parameters were as follows: .There was no significant difference in the values of Vd,CL and elimination obtained after both routes of administration. The plasma protein binding of DASK was found to be 36.5+3.0%. The excretion of unchanged DASK in 24h after im 150mg/kg was amounted to 24.9+18.1% in urine, 14.9+0.7% in bile and 13.9+3.6% in feces.

  • 【文献出处】 中药药理与临床 ,Pharmacology and Clinics of Chinese Materia Medica , 编辑部邮箱 ,1990年01期
  • 【被引频次】7
  • 【下载频次】225
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