Absolute bioavailability of imatinib (Glivec®) orally versus intravenous infusion
Absolute bioavailability of imatinib (Glivec®) orally versus intravenous infusion
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DOI：
10.1177/0091270003262101
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发表时间：
2004-02-01
影响因子：
2.9
通讯作者：
Lloyd, P
中科院分区：
文献类型：
--
作者：
Peng, B;Dutreix, C;Lloyd, P
本研究的目的是在健康受试者中研究伊马替尼（Glivec（R））400 mg（胶囊vs.口服溶液）单次口服给药与伊马替尼100 mg（静脉[i.v]输注）相比的绝对生物利用度。12例受试者在每个治疗阶段接受单次治疗：口服400 mg伊马替尼胶囊或溶液或100 mg伊马替尼静脉输注。在每次治疗后测量伊马替尼的血浆浓度;确定药代动力学参数和绝对生物利用度。伊马替尼胶囊和口服溶液的绝对生物利用度值（与静脉输注相比）分别为98.3%和97.2%。通过C-max、部分AUC和总AUC测量的伊马替尼吸收速率和程度，口服溶液和预期上市的伊马替尼胶囊相似。口服400 mg伊马替尼胶囊或溶液可完全吸收，几乎完全生物利用（>97%）。
The purpose of this study was to investigate the absolute bioavailability of a single oral dose of imatinib (Glivec(R)), 400 mg (capsules vs. oral solution), compared with imatinib, 100 mg (intravenous [i.v] infusion), in healthy subjects. Twelve subjects received a single treatment in each treatment period: a 400-mg oral dose of imatinib in capsule form or as a solution or a 100-mg i.v. infusion of imatinib. Plasma imatinib concentrations were measured following each treatment; pharmacokinetic parameters and absolute bioavailability were determined. Absolute bioavailability values (compared with i.v infusion) for the imatinib capsule and oral solution were 98.3% and 97.2%, respectively. Both the rate and extent of imatinib absorption, as measured by C-max, partial AUC, and total AUC, were similar for the oral solution and the imatinib capsule intended for the market. The 400-mg oral dose of imatinib, as a capsule or a solution, was completely absorbed and was; almost completely bioavailable (>97%).