Le Mignon M M, Chambon C, Warrington S, Davies R, Bonnemain B
Research and Development Division, Laboratoire Guerbet, Aulnay-sous-Bois, France.
Invest Radiol. 1990 Aug;25(8):933-7.
The pharmacokinetics of Gd-DOTA meglumine in humans were evaluated in six healthy male volunteers. The agent was injected intravenously at 0.1 mmol/kg over approximately 2 minutes. Its behavior was found to be similar to that of urographic and angiographic iodinated contrast media with a plasma elimination half-life of 91 +/- 14 minutes (mean +/- standard deviation [SD]), a small distribution volume of 171.0 +/- 19.7 mL/kg and rapid urinary excretion. The results suggest rapid passive extravascular diffusion of gadolinium (Gd)-DOTA in the interstitial space without intracellular penetration, followed by a rapid urinary excretion via glomerular filtration. Furthermore, the results are consistent with animal data that showed that the compound does not cross the normal blood brain barrier. Its plasma pharmacokinetics appeared to be similar to those reported for Gd-DTPA. No relevant biological effects were seen with Gd-DOTA, especially in regard to serum iron and bilirubin levels.
在6名健康男性志愿者中评估了钆喷酸葡甲胺在人体中的药代动力学。该药物以0.1 mmol/kg的剂量在约2分钟内静脉注射。发现其行为与尿路造影和血管造影用碘化造影剂相似，血浆消除半衰期为91±14分钟（平均值±标准差[SD]），分布容积小，为171.0±19.7 mL/kg，且经尿液快速排泄。结果表明，钆（Gd）-DOTA在间质空间中快速被动血管外扩散，不穿透细胞内，随后通过肾小球滤过快速经尿液排泄。此外，这些结果与动物数据一致，动物数据表明该化合物不会穿过正常的血脑屏障。其血浆药代动力学似乎与报道的钆喷替酸葡甲胺相似。未观察到Gd-DOTA有相关生物学效应，尤其是对血清铁和胆红素水平而言。
