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β-榄香烯在大鼠体内的药代动力学及体内过程

PHARMACOKINETICS AND DISPOSITION OF β-ELEMENE IN RATS

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【作者】 王堃苏成业

【Author】 WT4”,5BZ]WANG Kun, SU Cheng-ye (Department of Pharmacology, Dalian Medical University, Dalian 116027, China) [WT4”,5HZ]

【机构】 大连医科大学药理学教研室!辽宁大连116027

【摘要】 目的 研究β 榄香烯在大鼠体内的药代动力学及其体内过程。 方法 用GC法测定生物样品中β 榄香烯浓度。结果 大鼠ivβ 榄香烯 5 0 ,75 ,10 0mg·kg-1的时量曲线属二室模型 ,药物自血浆消除较快 ,且呈线性动力学。大鼠ip本品 10 0mg·kg-1的时量曲线属一室模型 ,但其消除慢于iv。本品自大鼠尿、粪、胆汁的排出量均很少。β 榄香烯的平均血浆蛋白结合率为 97 7%。结论 β 榄香烯在大鼠体内吸收快、分布广、消除快、蛋白结合率高 ,经尿、粪、胆汁排泄不是本品的主要消除途径。

【Abstract】 AIM To study the pharmacokinetics, absorption, distrbution and excretion of β-elemene obtained from the roots and stems of Curcuma wenynjin Y.H Chen et C.Ling. in rats. METHODS A GC method for isolation and determination of β-elemene in biological specimens was used. RESULTS After a single iv dose to rats, the plasma concentration-time course of β-elemene fitted well to a two-compartment open model. With regard to ip administration of a single dose of 100 mg·kg -1 to rats, the absorption of the drug was rapid. Elimination of the drug from plasma was found to be in accord with linear kinetics, whereas the elimination half-lives were longer than that of iv administration. Only small amount of unchanged β-elemene was excreted in urine, feces and bile after iv and ip administration. Plasma protein binding ratio was obtained from two different levels of β-elemene, 97 7% from 60 μg·mL -1 and 96 5% from 100 μg·mL -1 . CONCLUSION β-elemene was eliminated at a rapid rate and distributed widely in the body. The protein binding was found to be high. Unchanged β-elemene excreted via urine, feces and bile were very few.

【关键词】 β榄香烯气相色谱法药代动力学
【Key words】 elemenegas chromatographypharmacokinetics
  • 【文献出处】 药学学报 ,ACTA PHARMACEUTICA SINICA , 编辑部邮箱 ,2000年10期
  • 【分类号】R965
  • 【被引频次】38
  • 【下载频次】421
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