Olson N Z, Otero A M, Marrero I, Tirado S, Cooper S, Doyle G, Jayawardena S, Sunshine A
Analgesic Development, Ltd, New York NY 10022-1009, USA.
J Clin Pharmacol. 2001 Nov;41(11):1238-47. doi: 10.1177/00912700122012797.
Ibuprofen is a peripherally acting nonsteroidal anti-inflammatory drug indicated fo ranalgesia, antipyresis, and various arthritic conditions. A solubilized 200 mg liquigel formulation of ibuprofen has been shown to have a more rapid rate of absorption compared with ibuprofen 200 mg tablets. Ibuprofen liquigels have a kinetic profile similar to ibuprofen suspension, with both a higher Cmax and an earlier tmax than any solid tablet. The objective of this single-dose, double-blind, triple-dummy, parallel-group study was to assess the time to onset of relief and overall analgesic efficacy of liquigel ibuprofen 400 mg, ketoprofen 25 mg compared with acetaminophen 1000 mg, and placebo in 239 patients with moderate or severe pain following third molar extractions. Treatments were compared over 6 hours using standard scales for pain intensity and relief and stopwatch onset of meaningful relief. All active treatments provided meaningful relief significantly faster compared with placebo. Ibuprofen provided significantly faster relief compared with acetaminophen and ketoprofen. By the end of the study (6 h), onset of meaningful relief was achieved by 36%, 99%, 96%, and 88% of the patients in the placebo, ketoprofen, ibuprofen, and acetaminophen groups, respectively. The median times to onset of relief were > 6 hours for placebo, 25.5 minutes for ketoprofen, 24.2 minutes for ibuprofen, and 29.9 minutes for acetaminophen. In addition, both ibuprofen and ketoprofen showed statistical superiority over acetaminophen at earlier time points on the time-effect curves for pain relief and pain intensity difference. Consistent results were seen with respect to the 6-hour summary efficacy variables: the three active treatments were significantly better than placebo, and ibuprofen was significantly better than both acetaminophen and ketoprofen. Liquigel ibuprofen 400 mg was shown to provide faster relief and superior overall efficacy compared with ketoprofen 25 mg, acetaminophen 1000 mg, and placebo. No serious adverse effects were reported in this single-dose study.
布洛芬是一种外周作用的非甾体抗炎药,用于止痛、退热及治疗各种关节炎。与布洛芬200毫克片剂相比,已证明一种布洛芬200毫克的增溶液体制剂吸收速度更快。布洛芬液体制剂的动力学特征与布洛芬混悬液相似,其Cmax更高,tmax比任何固体片剂都更早。这项单剂量、双盲、三模拟、平行组研究的目的是评估400毫克布洛芬液体制剂、25毫克酮洛芬与1000毫克对乙酰氨基酚及安慰剂相比,在239例拔除第三磨牙后出现中度或重度疼痛患者中的起效时间和总体镇痛效果。使用疼痛强度和缓解的标准量表以及秒表记录有意义缓解的开始时间,在6小时内对各治疗组进行比较。与安慰剂相比,所有活性治疗组均显著更快地提供了有意义的缓解。与对乙酰氨基酚和酮洛芬相比,布洛芬提供缓解的速度明显更快。到研究结束时(6小时),安慰剂组、酮洛芬组、布洛芬组和对乙酰氨基酚组分别有36%、99%、96%和88%的患者实现了有意义的缓解。安慰剂组缓解的中位时间>6小时,酮洛芬组为25.5分钟,布洛芬组为24.2分钟,对乙酰氨基酚组为29.9分钟。此外,在疼痛缓解和疼痛强度差异的时间效应曲线上,布洛芬和酮洛芬在较早时间点均显示出优于对乙酰氨基酚的统计学优势。关于6小时总疗效变量观察到一致的结果:三种活性治疗组均显著优于安慰剂,布洛芬显著优于对乙酰氨基酚和酮洛芬。与25毫克酮洛芬、1000毫克对乙酰氨基酚及安慰剂相比,400毫克布洛芬液体制剂显示出更快的缓解速度和更优的总体疗效。在这项单剂量研究中未报告严重不良反应。