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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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