薛明, 崔颖, 汪汉卿, 罗永江, 张彬, 周宗田. 隐丹参酮及其代谢物在猪体内的药代动力学研究J. 药学学报, 1999, 34(2): 81-84.
引用本文: 薛明, 崔颖, 汪汉卿, 罗永江, 张彬, 周宗田. 隐丹参酮及其代谢物在猪体内的药代动力学研究J. 药学学报, 1999, 34(2): 81-84.
Xue Ming, Cui Ying, Luo Yongjiang, Zhang Bin , Zhou Zongtian, Wang Hanqing, . PHARMACOKINETICS OF CRYPTOTANSHINONE AND ITS METABOLITE IN PIGSJ. Acta Pharmaceutica Sinica, 1999, 34(2): 81-84.
Citation: Xue Ming, Cui Ying, Luo Yongjiang, Zhang Bin , Zhou Zongtian, Wang Hanqing, . PHARMACOKINETICS OF CRYPTOTANSHINONE AND ITS METABOLITE IN PIGSJ. Acta Pharmaceutica Sinica, 1999, 34(2): 81-84.

隐丹参酮及其代谢物在猪体内的药代动力学研究

PHARMACOKINETICS OF CRYPTOTANSHINONE AND ITS METABOLITE IN PIGS

  • 摘要: 目的: 研究隐丹参酮(CT)及其代谢物丹参酮IIA(TS)在猪体内的药代动力学。方法: 实验猪5头, 单剂量(10 mg.kg-1) iv隐丹参酮后,采用反相 HPLC法检测CT及TS的血浆浓度。 以二苄基为内标, 流动相为甲醇—水(85∶15),检测波长254 nm。 结果: CT血药时程符合二室开放模型。im与po给药后, CT和TS的血药浓度很低。 少量原药及其代谢产物在胆汁中随着给药时间的延长逐渐增多。不同途径给药后(iv及po),隐丹参酮及丹参酮IIA在尿中的排泄量占给药剂量的比例很小。 结论: 猪CT及TS药代动力学数据为动物临床用药提供有价值的理论依据。

     

    Abstract: AIM: To study the pharmacokinetics and excretion of the antibacterial constituent cryptotanshinone (CT) isolated from the roots of Saliva przewaalskii maxim (Labiatae) and its metabolite tanshinone IIA(TS) in pigs. METHODS: Normal pigs were given CT iv 10 mg.kg-1. The concentrations of CT and TS in porcine plasma, urine and bile were determined by an HPLC method developed in our laberatory. A waters model 480 instrument was used throughout the experiment. Dibenyl was used as the internal standard at absorption wavelength of 254 nm. A mixture of methanol and water(85∶15) was used as the mobile phase with a flow rate of 1 ml.min-1, and YWG C18H37 as stationary phase. RESULTS: The method is simple, sensitive and available for pharmacokinetics studies. Plasma drug concentration-time course of CT after iv adminstration of CT was found to be fitted to a two compartment open model and its pharmacokinetic paremeters were as follows: T1/2α=2.36 min, T1/2β=64.78 min, AUC=23.83 mg.min.L-1. TS was detected simultaneously. Peak plasma concentration of TS was reached at about 4.6 minutes after dosing. Cmax=0.62 μg.ml-1, T1/2β=189.04 min, AUC=22.97 mg.min.L-1. The excretion of CT and TS in urine and bile in 24~48 hour was very few after iv and po administration of CT. CONCLUSION: The pharmacokinetics of CT and TS in pigs provided a useful index for clinical trial in animals.

     

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