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Trials to evaluate the biotransformation activity of the liver in calves using a simplified paracetamol test.

机译:使用简化的扑热息痛试验评估小牛肝脏的生物转化活性。

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The aim of this investigation is to examine the use of paracetamol (as a model drug) test for calves. We examined if a precise determination of the pharmacokinetics of paracetamol (indirectly the activity of enzymes catalyzing the reaction of phase II of hepatic biotransformation) was possible using a simplified paracetamol test. The experiment was carried out on 15 healthy calves of BW (Black-and-White) breed. Paracetamol (5 mg/kg bw.) was administered per os on the tenth, twentieth and fourteenth days of the calves' lives. The concentration of a model drug in plasma was determined by the spectrophotometric method in 10, as well as 3 and 4 samples. Pharmacokinetic parameters were estimated using a non-compartmental method, via the TopFit computer program. The values of pharmacokinetic parameters of paracetamol estimated in "simplified variants" significantly correlated (r=0.874-0.985) with data obtained in a full test. The highest coefficients of the correlation was observed when the concentration of paracetamol was determined at 3, 4, 6 and 8 hours after the model drug administration. Summing up, it was determined that it is possible to evaluate precisely and indirectly the biotransformation activity in calves (activity of UDP-glucuronyltransferase and sulfonyltransferase) using a simplified variant of paracetamol test, based on the determination of the concentration of the model drug in 3-4 blood samples..
机译:这项研究的目的是检查对乙酰氨基酚(作为模型药物)在犊牛中的使用。我们检查了使用简化的扑热息痛试验能否精确测定扑热息痛的药代动力学(间接催化肝生物转化II期反应的酶活性)。实验是对15头BW(黑白)品种的健康小牛进行的。在小牛生命的第十,二十和十四天,口服口服扑热息痛(5 mg / kg体重)。通过分光光度法测定10个样品,3个和4个样品中血浆中模型药物的浓度。药代动力学参数通过TopFit计算机程序使用非隔室方法进行估算。在“简化的变体”中估计的扑热息痛的药代动力学参数值与在完全测试中获得的数据显着相关(r = 0.874-0.985)。当在模型药物施用后3、4、6和8小时确定对乙酰氨基酚的浓度时,观察到最高的相关系数。综上所述,已确定可以使用扑热息痛简化试验的简化变体,基于对3种模型药物浓度的测定,精确和间接地评估犊牛的生物转化活性(UDP-葡萄糖醛酸转移酶和磺酰转移酶的活性)。 -4血样

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