Kyllönen Matti, Olkkola Klaus T, Seppälä Timo, Ryhänen Pauli
Department of Anesthesia and Intensive Care, Oulu University Hospital, Oulu, Finland.
Paediatr Anaesth. 2005 Jul;15(7):566-73. doi: 10.1111/j.1460-9592.2005.01499.x.
Ibuprofen is a nonsteroidal anti-inflammatory drug which has both peripheral and central analgesic effects. Ibuprofen has been shown to be an effective antipyretic and postoperative analgesic drug both in adults and children with few side effects. Pharmacokinetics of rectal ibuprofen has not been studied, although suppositories are frequently used for perioperative pain control in children.
There were four study groups: full-term infants aged 1-7 weeks (n = 9), infants aged 8-25 weeks (n = 8), and infants aged 26-52 weeks (n = 7). Adult patients were 20-40 years old (n = 7). Ibuprofen suppository 20 mg.kg(-1) was administered after induction of anesthesia. Blood samples were collected from 20 min to 10 h after dosing and pharmacokinetic analysis of ibuprofen enantiomers were done.
Both ibuprofen enantiomers were detectable in blood in 20 min. Total ibuprofen plasma concentrations >10 mg.l(-1) were seen from 40 min to 8 h. Values for T(max) of ibuprofen enantiomers and total ibuprofen were higher in the adult group than any of the infant groups (P < 0.05). In addition, values for physiological (standardized) t(1/2) of (R)-(-)- and (S)-(+)-ibuprofen were higher in infants aged 1-7 weeks than the adults (P < 0.05). None of the other pharmacokinetic variables, C(max), AUC, chronological t(1/2) or AUC ratio differed between the groups.
A single dose of ibuprofen suppository 20 mg.kg(-1) after induction of anesthesia guarantees analgesic plasma concentrations during the early postoperative period. Except for the delayed absorption of ibuprofen in adults and higher physiological t(1/2) in infants aged 1-7 weeks, no major pharmacokinetic differences were observed between study groups.
布洛芬是一种非甾体抗炎药，具有外周和中枢镇痛作用。布洛芬已被证明是一种有效的解热药和术后镇痛药，在成人和儿童中均有应用，且副作用较少。尽管栓剂常用于儿童围手术期疼痛控制，但直肠用布洛芬的药代动力学尚未得到研究。
共有四个研究组：1 - 7周的足月儿（n = 9）、8 - 25周的婴儿（n = 8）以及26 - 52周的婴儿（n = 7）。成年患者年龄在20 - 40岁（n = 7）。麻醉诱导后给予20 mg·kg⁻¹的布洛芬栓剂。给药后20分钟至10小时采集血样，并对布洛芬对映体进行药代动力学分析。
给药20分钟后血液中即可检测到两种布洛芬对映体。在40分钟至8小时期间，布洛芬血浆总浓度>10 mg·L⁻¹。布洛芬对映体和布洛芬总量的T(max)值在成年组中高于任何婴儿组（P < 0.05）。此外，1 - 7周龄婴儿的（R）-（-）-和（S）-（+）-布洛芬的生理（标准化）t(1/2)值高于成年人（P < 0.05）。其他药代动力学变量，如C(max)、AUC、按时间计算的t(1/2)或AUC比值在各组之间没有差异。
麻醉诱导后单次给予20 mg·kg⁻¹的布洛芬栓剂可确保术后早期血浆镇痛浓度。除了成人中布洛芬吸收延迟以及1 - 7周龄婴儿中生理t(1/2)较高外，研究组之间未观察到主要的药代动力学差异。
