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作者研究了三硝基甘油(GTN)及其二硝基代谢物(1,2GDN和1,3GDN)的药物动力学和药效动力学。作者认为过去许多文献中的争论如:口服剂型的效能、长效硝基化合物等均以“三硝基甘油服用后产生足够量的二硝基代谢物及其药理作用”加以解释。作者的实验表明,口服与其它连续给药如透皮吸收、静脉滴注一样能产生足够量的二硝基代谢物,可以达到所期望的药效动力学目的,某些当前常用剂型的低效能亦可用此加以解释。此外作者论证,狗体内二硝基代谢物在血液流动学方面的明显有效性和初步药物动力学数据表明这些代谢物在持久痉挛性心绞痛患者身上具有明显活性。作者建议制备供人体口服、静脉给药、局部给药(舌下和外用)的二硝基化合物制剂,并提出所需的一些数据。
The authors studied the pharmacokinetics and pharmacodynamics of trinitroglycerol (GTN) and its dinitro metabolites (1, 2GDN, and 1,3GDN). The authors argue that many of the controversies in the past, such as the efficacy of oral dosage forms and long-acting nitro compounds, are explained by “a sufficient amount of dinitro metabolites and their pharmacological effects after administration of trinitroglycerol”. The authors’ experiments showed that orally administered dinitro metabolites in sufficient quantities, as well as other continuous administrations such as transdermal absorption and intravenous instillation, can achieve the desired pharmacodynamic goals and the efficacy of some currently available dosage forms Can also be used to explain this. In addition, the author argues that the significant efficacy of dinitro metabolites in dog blood flow dynamics and preliminary pharmacokinetic data suggest that these metabolites have significant activity in patients with persistent spastic angina. The authors recommend the preparation of dinitro compounds for oral, intravenous, topical (sublingual and topical) administration to humans and provide some of the data needed.