Ferrero-Cafiero Juan Manuel, Gich Ignasi, Puntes Montse, Martínez Joan, Ballester Maria R, Coimbra Jimena, Mathison Yaira, Tarré Maite, Font Xavier, Antonijoan Rosa M
Int J Clin Pharmacol Ther. 2015 Nov;53(11):972-9. doi: 10.5414/CP202368.
To assess and compare the bioavailability of ibuprofen enantiomers (R and S) of two different pediatric suspensions: the first one with ibuprofen lysinate (Algidrin® Pediátrico, FARDI S.A., Barcelona, Spain) and the second one with ibuprofen base (Dalsy®, Abbott Laboratories S.A., Madrid, Spain).
A randomized, open-label, single-dose, balanced, crossover study under fasting conditions was performed at the CIM-Sant Pau. 24 healthy volunteers received a single dose of ibuprofen lysinate (Algidrin® Pediátrico, FARDI S.A.) and ibuprofen base (Dalsy®, Abbott Laboratories S.A.) equivalent to 400 mg of ibuprofen. 18 blood samples were drawn and ibuprofen enantiomer plasma concentrations were determined using an enantioselective analytical method. An analysis of variance (ANOVA) model was used, and the 90% confidence intervals (CI) were calculated; further analyses were made regarding rate of absorption and variability.
The pharmacokinetic parameters (Algidrin® Pediátrico vs. Dalsy® (Mean±SD)) were: S-enantiomer: Cmax=22.39±5.33 vs. 19.97±3.19 μg/mL; AUC0t=74.83±16.69 vs. 74.64±14.80 μg×h/mL, and AUC0∞=77.46±19.33 vs. 76.98±17.13 μg×h/mL; and for R-enantiomer: Cmax=21.74±3.76 vs. 15.20±2.03 μg/mL; AUC0t=57.55±10.17 vs. 46.13±9.61 μg×h/mL, and AUC0∞ value was 58.49±10.57 vs. 47.03±10.02 μg×h/mL. The tmax (Median) for S-enantiomer (active) were: 0.5 vs. 1.33 hours (p=0.001) and for R-enantiomer: 0.5 vs. 1.0 hours (p=0.004). Ibuprofen pharmacokinetic values may vary under fed state and in pediatric population.
While S-ibuprofen shows a similar bioavailability for AUC0t, AUC0∞, and Cmax, R-ibuprofen shows suprabioavailability for the lysinate formulation. The rate of absorption of the ibuprofen lysinate suspension is quicker and less variable than that of the ibuprofen base reference suspension and it exhibits a shorter tmax, which is of particular interest for achieving a rapid and homogeneous analgesic and antipyretic effect.
评估并比较两种不同儿科混悬液中布洛芬对映体（R和S）的生物利用度：第一种为赖氨酸布洛芬（Algidrin® Pediátrico，FARDI S.A.，巴塞罗那，西班牙），第二种为布洛芬原料药（Dalsy®，雅培实验室西班牙公司，马德里，西班牙）。
在圣保禄医院临床研究与创新中心（CIM-Sant Pau）进行了一项随机、开放标签、单剂量、平衡、交叉的空腹条件下研究。24名健康志愿者分别单次服用相当于400 mg布洛芬的赖氨酸布洛芬（Algidrin® Pediátrico，FARDI S.A.）和布洛芬原料药（Dalsy®，雅培实验室西班牙公司）。采集18份血样，采用对映体选择性分析方法测定布洛芬对映体的血浆浓度。使用方差分析（ANOVA）模型，并计算90%置信区间（CI）；进一步分析吸收速率和变异性。
药代动力学参数（Algidrin® Pediátrico与Dalsy®（均值±标准差））如下：S-对映体：Cmax = 22.39±5.33 vs. 19.97±3.19 μg/mL；AUC0t = 74.83±16.69 vs. 74.64±14.80 μg×h/mL，AUC0∞ = 77.46±19.33 vs. 76.98±17.13 μg×h/mL；R-对映体：Cmax = 21.74±3.76 vs. 15.20±2.03 μg/mL；AUC0t = 57.55±10.17 vs. 46.13±9.61 μg×h/mL，AUC0∞值为58.49±10.57 vs. 47.03±10.02 μg×h/mL。S-对映体（活性）的tmax（中位数）分别为：0.5 vs. 1.33小时（p = 0.001），R-对映体为：0.5 vs. 1.0小时（p = 0.004）。布洛芬的药代动力学值在进食状态和儿科人群中可能会有所不同。
虽然S-布洛芬在AUC0t、AUC0∞和Cmax方面显示出相似的生物利用度，但R-布洛芬在赖氨酸盐制剂中显示出超生物利用度。赖氨酸布洛芬混悬液的吸收速率比布洛芬原料药参比混悬液更快且变异性更小，并且其tmax更短，这对于实现快速且均匀的镇痛和解热效果尤为重要。
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