【摘要】 <正> 桔酰苯胺即N-(β-二乙氨乙基)-N-邻甲苯基-3′,4′,5′-三甲氧基苯甲酰胺马来酸盐(代号603)是一种有抗心律失常作用的新型化合物。试验证明,对各种心律失常动物模型有一定的预防和治疗作用,治疗指数也较大,现已进入临床试验阶段。关于桔酰苯胺的药代动力学研究报道甚少,体内生物转化尚未阐明。为了解它对药酶的影响,以及在药物代谢上的种属差异,本研究用安替比林血浆半衰期(t(1/2))为指标,用双波长薄层扫描定量测更多还原

【Abstract】 Gallanilide, N- (β-diethylaminoethyl) -N- (o-methylphenyl) -3’, 4’, 5’, -trimethyloxycarboxylamide maleate (603), is a new synthetic compound with antiarrhythmic action. Antipyrine plasma half-life (t(1/2)) was used as an indicator by quantitative TLC scanning technique for studying the effects of gallanilide and phenobarbital on hepatic drug metabolizing enzymes in hybrid and inbred rats. I.p administration of gallanilide (8 mg/kg, twice a day) or phenobarbital (40 mg/kg, once daily) to both hybrid and inbred rats for three days, caused significant prolongation or shortening of antipyrine plasma t(1/2), respectively. The results showed that gallanilide probably inhibited hepatic drug metabolizing enzymes and that phenobarbital induced them, significantly. But it was found that there was no statistical difference between the two species of animals. The results suggest that hybrid rats could be used for primary investigation.更多还原