Cumberland Pharmaceuticals, 2525 West End Avenue, Nashville, TN 37203, USA.
Am J Health Syst Pharm. 2011 Jan 1;68(1):47-51. doi: 10.2146/ajhp100120.
The pharmacokinetics, safety, and tolerability of a rapid infusion of i.v. ibuprofen in healthy adults were evaluated. Methods In this randomized, double-blind, placebo-controlled, single-dose, crossover study, 12 healthy subjects age 18-65 years were randomized to receive a single dose of either 800 mg i.v. ibuprofen (infused over five to seven minutes) concomitantly with an oral placebo or 800 mg oral ibuprofen with concomitant i.v. placebo (0.9% sodium chloride injection). After a six-day washout period, subjects received the treatment not previously received. Blood samples were taken 1 hour before each dose of study medication was administered and throughout the 12 hours thereafter. Plasma ibuprofen concentrations were determined using validated liquid chromatography-tandem mass spectrometry methods. The frequency and severity of treatment-emergent adverse effects were monitored throughout the study.
The maximum plasma concentration (C(max)) of i.v. ibuprofen was approximately twice that of oral ibuprofen, and the (t(max)) of i.v. ibuprofen was 0.11 hour, compared with 1.5 hours for oral ibuprofen. However, the elimination half-life of i.v. and oral ibuprofen did not differ, both of which were approximately 2 hours. Oral ibuprofen was 100% bioavailable; therefore, the area under the concentration-time curve did not differ between i.v. and oral ibuprofen. In addition, i.v. ibuprofen infused over five to seven minutes did not differ in terms of safety or tolerability when compared with oral ibuprofen.
I.V. ibuprofen, when administered over five to seven minutes in healthy subjects, achieved a higher C(max) and a more-rapid t(max) than did oral ibuprofen and was found to be safe and well tolerated.
评估健康成年人静脉内快速输注布洛芬的药代动力学、安全性和耐受性。
在这项随机、双盲、安慰剂对照、单次交叉研究中，将 12 名年龄在 18-65 岁之间的健康受试者随机分为两组，分别接受静脉内 800mg 布洛芬（5-7 分钟内输注）和口服安慰剂或静脉内 800mg 布洛芬和口服安慰剂（0.9%氯化钠注射液）。在 6 天的洗脱期后，受试者接受了之前未接受的治疗。在每次给予研究药物前 1 小时和之后 12 小时内采集血样。使用经过验证的液相色谱-串联质谱法测定血浆中布洛芬的浓度。在整个研究过程中监测治疗中出现的不良事件的频率和严重程度。
静脉内布洛芬的最大血浆浓度（C(max)）约为口服布洛芬的两倍，静脉内布洛芬的（t(max)）为 0.11 小时，而口服布洛芬为 1.5 小时。然而，静脉内和口服布洛芬的消除半衰期没有差异，均约为 2 小时。口服布洛芬的生物利用度为 100%；因此，静脉内和口服布洛芬的浓度-时间曲线下面积没有差异。此外，静脉内输注 5-7 分钟的布洛芬在安全性和耐受性方面与口服布洛芬没有差异。
在健康受试者中，静脉内输注布洛芬 5-7 分钟可达到更高的 C(max)和更快的 t(max)，与口服布洛芬相比，静脉内输注布洛芬具有更高的安全性和耐受性。
