Shuke N, Takashio T, Sato J, Ishikawa Y, Saito Y, Yamamoto W, Aburano T, Mizunaga M, Kaneko S, Yachiku S, Ogawa Y, Kikuchi K, Sasajima T, Kubo Y
Department of Radiology, Asahikawa Medical College Hospital.
Kaku Igaku. 1996 May;33(5):513-20.
We studied 50 patients with mild to moderate renal dysfunction to compare pharmacokinetics of 99mTc-MAG3 with that of 131I-OIH. After simultaneous bolus injection of both 99mTc-MAG3 and 131I-OIH, 8-point venous blood sampling was performed from 2 to 44 min post injection. Aliquoted plasma samples were counted for radioactivity along with the injected standard to obtain % injected dose/ml plasma for each tracer. Using obtained time-concentration data, classical 2 compartment model analysis was performed for both tracers to obtain various pharmacokinetic parameters, including distribution volumes (Vds), inter-compartmental rate constants, and plasma clearance. In these parameters, Vd of central compartment, Vd at steady state, central to peripheral inter-compartmental rate constant, and plasma clearance were significantly larger for 131I-OIH. In all parameters, significant correlation was found between 99mTc-MAG3 and 131I-OIH. The best correlation was seen in plasma clearance (r = 0.891, p < 0.0001). Plasma clearance ratio (99mTc-MAG3/131I-OIH), however, showed weak but significant negative correlation with serum creatinine, although this correlation was not likely to affect the overall correlation of clearance between 131I-OIH and 99mTc-MAG3. From these results, we confirmed that 99mTc-MAG3 clearance could be used as an alternative to 131I-OIH clearance, although pharmacokinetic behavior of 99mTc-MAG3 was not exactly the same as that of 131I-OIH.
我们研究了50例轻至中度肾功能不全患者，以比较99mTc-MAG3与131I-OIH的药代动力学。在同时推注99mTc-MAG3和131I-OIH后，于注射后2至44分钟进行8点静脉血采样。将等分的血浆样本与注射的标准品一起计数放射性，以获得每种示踪剂的每毫升血浆注射剂量百分比。利用获得的时间-浓度数据，对两种示踪剂进行经典的二室模型分析，以获得各种药代动力学参数，包括分布容积（Vds）、室间速率常数和血浆清除率。在这些参数中，131I-OIH的中央室Vd、稳态Vd、中央至外周室间速率常数和血浆清除率显著更大。在所有参数中，99mTc-MAG3与131I-OIH之间均存在显著相关性。血浆清除率的相关性最佳（r = 0.891，p < 0.0001）。然而，血浆清除率比值（99mTc-MAG3/131I-OIH）与血清肌酐呈弱但显著的负相关，尽管这种相关性不太可能影响131I-OIH与99mTc-MAG3之间清除率的总体相关性。从这些结果来看，我们证实99mTc-MAG3清除率可作为131I-OIH清除率的替代指标，尽管99mTc-MAG3的药代动力学行为与131I-OIH并不完全相同。
