王堃, 苏成业. β-榄香烯在大鼠体内的药代动力学及体内过程J. 药学学报, 2000, 35(10): 725-728.
引用本文: 王堃, 苏成业. β-榄香烯在大鼠体内的药代动力学及体内过程J. 药学学报, 2000, 35(10): 725-728.
WANG Kun SU Cheng-ye, . PHARMACOKINETICS AND DISPOSITION OF β-ELEMENE IN RATSJ. Acta Pharmaceutica Sinica, 2000, 35(10): 725-728.
Citation: WANG Kun SU Cheng-ye, . PHARMACOKINETICS AND DISPOSITION OF β-ELEMENE IN RATSJ. Acta Pharmaceutica Sinica, 2000, 35(10): 725-728.

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

  • 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iv β-榄香烯50,75,100 mg.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100 mg.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.

     

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