(99m)Tc(CO)3(NTA)：一种具有与健康志愿者中 (131)I-OIH 相当的药代动力学特性的 (99m)Tc 肾示踪剂。
(99m)Tc(CO)3(NTA): a (99m)Tc renal tracer with pharmacokinetic properties comparable to those of (131)I-OIH in healthy volunteers.
机构信息
Department of Radiology, Emory University, Atlanta, Georgia 30322, USA.
出版信息
J Nucl Med. 2010 Mar;51(3):391-6. doi: 10.2967/jnumed.109.070813. Epub 2010 Feb 11.
UNLABELLED
Studies in rats showed that the pharmacokinetics of the tricarbonyl core radiopharmaceutical (99m)Tc(CO)(3)-nitrilotriacetic acid, (99m)Tc(CO)(3)(NTA), were essentially identical to those of (131)I ortho-iodohippuran ((131)I-OIH), the clinical gold standard for the measurement of effective renal plasma flow. Our objective was to compare the pharmacokinetics of these 2 tracers in healthy volunteers.
METHODS
(99m)Tc(CO)(3)(NTA) was prepared with commercially available NTA and a commercially available kit and isolated by reversed-phase high-performance liquid chromatography. Approximately 74 MBq (2 mCi) of (99m)Tc(CO)(3)(NTA) were coinjected with 9.25 MBq (250 microCi) of (131)I-OIH in 9 volunteers, and simultaneous imaging of each tracer was performed for 24 min. Plasma clearances were determined from 8 blood samples obtained 3-90 min after injection using the single-injection, 2-compartment model. Plasma protein binding, red cell uptake, and percentage injected dose in the urine at 30 and 180 min were determined.
RESULTS
There was no difference in the plasma clearances of (99m)Tc(CO)(3)(NTA) and (131)I-OIH, 475 +/- 105 mL/min versus 472 +/- 108 mL/min, respectively. The plasma protein binding and red cell uptake of (99m)Tc(CO)(3)(NTA) were 43% +/- 5% and 9% +/- 6%, respectively; both values were significantly lower (P < 0.001) than the plasma protein binding (75% +/- 3%) and red cell uptake (17% +/- 5%) of (131)I-OIH. There was no significant difference in the percentage injected dose recovered in the urine at 30 min and at 3 h; for comparison, the percentage dose in the urine at 3 h was 91% +/- 4% for (99m)Tc(CO)(3)(NTA) and 91% +/- 6% for (131)I-OIH (P = 0.96). Image quality with (99m)Tc(CO)(3)(NTA) was excellent, and the renogram parameters were similar to those of (131)I-OIH.
CONCLUSION
Preliminary results in healthy volunteers suggest that the pharmacokinetic behavior of (99m)Tc(CO)(3)(NTA) is comparable to that of (131)I-OIH.
目的
比较这两种示踪剂在健康志愿者中的药代动力学。
方法
采用市售 NTA 和市售试剂盒制备[99mTc（CO）3（NTA）]，并通过反相高效液相色谱法分离。9 名志愿者同时注射约 74MBq（2mCi）[99mTc（CO）3（NTA）]和 9.25MBq（250μCi）[131I-OIH]，注射后 3-90min 采集 8 份血样，采用单注射双室模型计算血浆清除率。分别于 30min 和 180min 时测定血浆蛋白结合率、红细胞摄取率和尿中注入剂量的百分比。
结果
[99mTc（CO）3（NTA）]和[131I-OIH]的血浆清除率分别为 475±105mL/min 和 472±108mL/min，无差异。[99mTc（CO）3（NTA）]的血浆蛋白结合率和红细胞摄取率分别为 43%±5%和 9%±6%，均明显低于[131I-OIH]的血浆蛋白结合率（75%±3%）和红细胞摄取率（17%±5%）（均 P<0.001）。30min 和 3h 时尿中注入剂量的百分比无显著差异；相比之下，[99mTc（CO）3（NTA）]的尿中 3h 时剂量百分比为 91%±4%，[131I-OIH]为 91%±6%（P=0.96）。[99mTc（CO）3（NTA）]图像质量良好，肾图参数与[131I-OIH]相似。
结论
健康志愿者的初步结果表明，[99mTc（CO）3（NTA）]的药代动力学行为与[131I-OIH]相似。
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