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三甲双酮和二甲双酮用于溶解胰腺结石的比较药代动力学研究。

Comparative pharmacokinetic study of trimethadione and dimethadione for lysis of pancreatic stones.

作者信息

Noda A, Yamamoto K, Nakanishi Y

出版信息

Gastroenterol Jpn. 1986 Apr;21(2):167-71. doi: 10.1007/BF02774835.

Abstract

In order to investigate the biological equivalence of dimethadione (DMO) and its precursor trimethadione (TMO), comparative pharmacokinetic studies were performed in 6 beagle dogs. DMO and TMO power was given orally at the same molar dose of 1.0 g and 1.11 g (7.7 mM), respectively. Plasma concentration of DMO and TMO was determined at an appropriate interval. Four pharmacokinetic parameters were calculated from the plasma concentration-time curves of DMO and TMO; the peak plasma concentration (Cmax), the time to the peak concentration of Cmax (Tmax), the area under the plasma concentration-time curve (AUC), and the biological half-life (t 1/2). In the plasma concentration-time curve of DMO, Tmax after oral administration of TMO was longer than that after administration of DMO. This resulted from the presence of the conversion process of TMO to DMO in the body, because of the very short Tmax observed in the plasma concentration-time curve of TMO. Cmax, AUC and t 1/2 did not differ significantly between the drugs. The results obtained indicate that TMO is biologically equivalent to DMO in regard to plasma concentration of DMO.

摘要

为研究二甲双酮(DMO)及其前体三甲双酮(TMO)的生物等效性,对6只比格犬进行了比较药代动力学研究。分别以1.0 g和1.11 g(7.7 mM)的相同摩尔剂量口服给予DMO和TMO。在适当的时间间隔测定DMO和TMO的血浆浓度。根据DMO和TMO的血浆浓度-时间曲线计算四个药代动力学参数;血浆峰浓度(Cmax)、达到Cmax峰浓度的时间(Tmax)、血浆浓度-时间曲线下面积(AUC)和生物半衰期(t 1/2)。在DMO的血浆浓度-时间曲线中,口服TMO后的Tmax长于口服DMO后的Tmax。这是由于体内存在TMO向DMO的转化过程,因为在TMO的血浆浓度-时间曲线中观察到Tmax非常短。两种药物之间的Cmax、AUC和t 1/2没有显著差异。所得结果表明,就DMO的血浆浓度而言,TMO与DMO具有生物等效性。

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