Martin W, Koselowske G, Töberich H, Kerkmann T, Mangold B, Augustin J
Pharmakin GmbH, Gesellschaft für Pharmakokinetik, Ulm, FRG.
Biopharm Drug Dispos. 1990 Apr;11(3):265-78. doi: 10.1002/bdd.2510110311.
The lysine salt of d,l-2-(4-isobutylphenyl)-propionic acid (ibuprofen lysine) was administered as a single oral dose of 500 mg by means of commercially available coated tablets (Imbun).* To assess the absolute bioavailability of ibuprofen after its oral application as a lysine salt, intravenous injections of ibuprofen solutions containing 200 mg and 400 mg of the drug served as reference application. In a partially randomized cross-over design, 8 healthy male volunteers received three different single dose administrations which were separated by wash-out periods of 4 days each. Ibuprofen plasma concentrations were determined by HPLC using direct injection, pre-column enrichment and column switching techniques. From the results of intravenous injections one can deduce linear ibuprofen pharmacokinetics within the considered dosage range, with corresponding AUC0-infinity values of 3786 micrograms * min ml-1 and 7260 micrograms * min ml-1 for the 200 mg and 400 mg doses, respectively. The values of plasma clearances as well as those of different volumes of distribution showed remarkable constancy after evaluation from both intravenous injections. The absorption of orally administered ibuprofen lysine proved to be rapid, resulting in a mean peak plasma level (Cmax) of 31 micrograms ml-1 ibuprofen and in a mean time to peak (tmax) of 45 min. The absolute bioavailability of ibuprofen amounts to 102.7 per cent, indicating a complete absorption of ibuprofen when administered as its lysine salt. Drug tolerability was excellent for the oral administration of ibuprofen lysine as well as for the intravenous treatments with ibuprofen free acid. Only mild and transient adverse drug reactions such as mild burning or dragging sensation during injection or mild redness at the site of injection were reported.
通过市售包衣片（Imbun）以500mg的单次口服剂量给予d，l-2-（4-异丁基苯基）-丙酸赖氨酸盐（布洛芬赖氨酸）。*为了评估布洛芬作为赖氨酸盐口服后的绝对生物利用度，静脉注射含200mg和400mg该药物的布洛芬溶液作为对照给药。在部分随机交叉设计中，8名健康男性志愿者接受了三种不同的单剂量给药，每次给药间隔4天的洗脱期。使用直接进样、柱前富集和柱切换技术，通过高效液相色谱法测定布洛芬血浆浓度。从静脉注射结果可以推断，在所考虑的剂量范围内，布洛芬的药代动力学呈线性，200mg和400mg剂量的相应AUC0-无穷大值分别为3786微克·分钟/毫升和7260微克·分钟/毫升。从两次静脉注射评估后，血浆清除率值以及不同分布容积值均显示出显著的稳定性。口服布洛芬赖氨酸的吸收迅速，布洛芬的平均血浆峰浓度（Cmax）为31微克/毫升，平均达峰时间（tmax）为45分钟。布洛芬的绝对生物利用度为102.7%，表明以赖氨酸盐形式给药时布洛芬可完全吸收。布洛芬赖氨酸口服给药以及布洛芬游离酸静脉治疗的药物耐受性均良好。仅报告了轻微和短暂的药物不良反应，如注射期间的轻微烧灼感或牵拉感，或注射部位的轻微发红。
