【摘要】 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%。更多还原

【Abstract】 A comparative pharmacokinetics between the single andcombination preparations of acetaminophen was studied in 6 male normalvolunteers. According to the cross-over design, each volunteer was giventwo tablets of acetaminophen (500mg per tablet) or the combination prepara-tion of acetaminophen-codeine phosphate (500mg+8. 4mg per tablet) afteran overnight fast. The samples of plasma and urine were determined byHPLC and the results showed: 1. The pharmacokinetics of single and combination preparations of acu- taminophen was different, A individual difference among the volunteers wasalso observed. 2. Absorption of single acetaminophen in two-third of the volunteerswas fast and the drug lever-time curves were two-compartment model. Themaximum level was 15. 96mg/l at 0. 56 hour after administration. One-thirdof the volunteers absorbed slowly and the drug level-time curves wereone-compartment model, The maximum level was 8. 89mg/l at 3 hours afteradministration. The drug level-time curve of the combination acetaminophenin one of the volunteers was a double-peak curve. That of other five volun-teers were two compartment model and absorption rate was between theformer two. The maximum level was 9. 38 mg/l at 1.5 hours after adminis-tration. The total amount of acetaminophen absorbed in the single and thecombination preparations was similar. 3. Acetaminophen widely distributed in the body. The apperent volumeof distribution of single and combination preparations were 0.90 l/kg and1. 29 l/kg, respectively. 4. The half-life of single acetaminophen in the fast absorption groupwas 3. 22 hours, and 4. 04 hours, in the slow absorption group. That ofcombination acetaminophen was 3. 56 hours. The renal clearance of the twopreparations were slow, that were 0.84 l/h and 1. 17 l/h, respectively. Therecovery of anchanged acetaminophen of the two preparations during 24 hoursafter administration were 4. 71% and 5. 84% of the dose, respectively.更多还原