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目的 探讨曲马多在小鼠体内的药物代谢动力学。方法 采用药效—药代统一模型 ,以小鼠腹腔注射醋酸后扭体反应次数为镇痛效应指标 ,测定时—效、量—效关系 ,进一步求时间—体存生物相当药量曲线及相应药代动力学参数。结果 曲马多在小鼠的镇痛作用呈显著的时—效、量—效关系 ,其镇痛作用效量半衰期(T1 /2 ,ED)为 4 68min ,消除速率常数K为 0 1 4 8。结论 曲马多母核药物与多种代谢产物均有镇痛作用 ,此法比单纯测定曲马多的血药浓度更能科学地反映药物在作用部位的药效变化规律
Objective To investigate the pharmacokinetics of tramadol in mice. Methods Pharmacodynamic - pharmacokinetic model was used to determine the time-effect-dose-response relationship of mice writhing reaction after intraperitoneal injection of acetic acid into mice. Pharmacokinetic parameters. Results Tramadol had a significant effect on the analgesic effect in mice. The half-life (T1 / 2, ED) of the analgesic effect was 4 68 min and the elimination rate constant K was 0 1 48 . Conclusion Tramadol mother-daughter drug and a variety of metabolites have analgesic effect than the simple determination of plasma concentration of tramadol can more scientifically reflect the law of drug action at the site of change