6例男性健康志愿者交叉口服2片扑热息痛片(每片含500mg)和2片氨酚待因片(每片含扑热息痛500mg和磷酸可待因8.4mg)进行药代动力学比较研究结果表明,二者存在较大差异。同一种剂型的个体之间也存在较大差异。口服单方制剂的药—时曲线,4例为二室模型,吸收快,达血浆峰浓度时间为0.56h,峰浓度也较高,为15.96mg/l。2例慢吸收的药—时曲线为一室模型,峰时间为3h峰浓度也较低,为8.89mg/l。口服复方制剂扑热息痛的药—时曲线有1例呈双峰曲线,其余5例为二室模型,吸收速度和峰浓度均居前二者之间,血浆峰浓度为9.38mg/l,于1.5h达到。单、复方制剂的吸收均有一个较短的迟滞时间。吸收速度的差异没有导致总吸收的差异,单、复方制剂的生物利用度相似,分别为84.73%和80.75%。扑热息痛在体内分布广泛,单、复方制剂的表现分布容积分别为0.90 l/kg和1.29l/kg。单方制剂的消除半衰期在快吸收者中为3.22h,慢吸收者为4.04h;复方制剂的消除半衰期更接近快吸收者,为3.56h。扑热息痛肾清除率低,单、复方制剂分别为0.84 l/h和1.17 l/h。24h尿中回收原型药物分别为给药剂量的4.71%和5.84%。 6 healthy volunteers crossed two tablets of paracetamol (500 mg per tablet) and two paracetamol tablets (each containing paracetamol 500 mg and codeine phosphate 8.4 mg) for pharmacokinetic studies at the crossover point. There is a big difference between the two. There is also a large discrepancy between individuals of the same dosage form. Oral unilateral formulations of drug-time curve, 4 cases of two-compartment model, fast absorption, peak plasma concentration reached a time of 0.56h, the peak concentration is higher at 15.96mg / l. Two cases of slow absorption of drug-time curve for the one-compartment model, peak time 3h peak concentration is also lower, 8.89mg / l. The oral compound prescription paracetamol drug-time curve of a bimodal curve in 1 case, the remaining 5 cases of two-compartment model, the absorption rate and peak concentration were among the former two peak plasma concentration of 9.38mg / l, at 1.5h achieve. Single, compound preparations have a shorter absorption of lag time. The difference of absorption rate did not lead to the difference of total absorption. The bioavailabilities of single and compound preparations were similar, 84.73% and 80.75% respectively. Paracetamol is widely distributed in the body, single and complex formulations of the performance distribution volume were 0.90 l / kg and 1.29l / kg. The elimination half-life of unilateral preparation was 3.22h in fast absorbers and 4.04h in slow absorbers; the elimination half-life of compound preparation was closer to fast absorbers, 3.56h. Paracetamol kidney clearance was low, single, compound preparations were 0.84 l / h and 1.17 l / h. Urine 24h recovery prototype drugs were administered dose of 4.71% and 5.84%.