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首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Pharmacokinetics of 18Ffleroxacin in healthy human subjects studied by using positron emission tomography.
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Pharmacokinetics of 18Ffleroxacin in healthy human subjects studied by using positron emission tomography.

机译：18F氟沙星在健康人体内的药动学通过正电子发射断层扫描技术进行研究。

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Positron emission tomography (PET) with [18F]fleroxacin was used to study the pharmacokinetics of fleroxacin, a new broad-spectrum fluoroquinolone, in 12 healthy volunteers (9 men and 3 women). The subjects were infused with a standard therapeutic dose of fleroxacin (400 mg) supplemented with approximately 20 mCi of [18F]fleroxacin. Serial PET images were made and blood samples were collected for 8 h, starting at the initiation of the infusion. The subjects were then treated with unlabeled drug for 3 days (400 mg/day). On the fifth day, infusion of radiolabeled drug, PET imaging, and blood collection were repeated. In most organs, there was rapid accumulation of radiolabeled drug, with stable levels achieved within 1 h after completion of the infusion. Especially high peak concentrations (in micrograms per gram) were achieved in the kidney (> 34), liver (> 25), lung (> 20), myocardium (> 19), and spleen (> 18). Peak concentrations of drug more than two times the MIC for 90% of Enterobacteriaceae strains tested (> 10-fold for most organisms) were achieved in all tissues except the brain and remained above this level for more than 6 to 8 h. The plateau concentrations in tissues (2 to 8 h, in micrograms per gram +/- standard error of the mean) of drug were as follows: brain, 0.83 +/- 0.032; myocardium, 4.53 +/- 0.24; lung, 5.80 +/- 0.48; liver, 7.31 +/- 0.33; spleen, 6.00 +/- 0.47; bowel, 3.53 +/- 0.74; kidney, 8.85 +/- 0.64; bone, 2.87 +/- 0.29; muscle, 4.60 +/- 0.33; prostate, 4.65 +/- 0.48; uterus, 3.87 +/- 0.39; breast, 2.68 +/- 0.11; and blood, 2.35 +/- 0.09. Concentrations of fleroxacin in tissue were similar in males and females, before and after pretreatment with unlabeled drug.
机译：正电子发射断层扫描（PET）与[18F]氟罗沙星用于研究氟罗沙星（一种新型的广谱氟喹诺酮）在12名健康志愿者（9名男性和3名女性）中的药代动力学。给受试者输注标准治疗剂量的氟沙星（400 mg），补充约20 mCi的[18F]氟沙星。从开始输液开始，连续拍摄PET图像，并采集血样8 h。然后将受试者用未标记的药物治疗3天（400毫克/天）。在第五天，重复输注放射性标记药物，PET成像和采血。在大多数器官中，放射性标记药物迅速积累，在输注完成后1小时内达到稳定水平。在肾脏（> 34），肝脏（> 25），肺（> 20），心肌（> 19）和脾脏（> 18）中达到了特别高的峰值浓度（以微克/克为单位）。在除脑外的所有组织中，所测试的肠杆菌科菌株90％的药物峰值浓度均超过MIC的两倍（大多数生物体> 10倍），并保持高于此水平6至8小时以上。药物在组织中的平台浓度（2至8小时，以微克每克+/-平均值的标准误为准）如下：脑，0.83 +/- 0.032；心肌4.53 +/- 0.24;肺5.80 +/- 0.48;肝脏7.31 +/- 0.33；脾脏6.00 +/- 0.47;肠3.53 +/- 0.74;肾脏8.85 +/- 0.64;骨2.87 +/- 0.29;肌肉4.60 +/- 0.33；前列腺4.65 +/- 0.48;子宫3.87 +/- 0.39;乳房2.68 +/- 0.11;和血液，2.35 +/- 0.09。在未标记药物预处理之前和之后，男性和女性的组织中氟罗沙星的浓度相似。

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