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采用正交实验筛选法制备99 Tcm Q3 (99 Tcm N, N亚乙基二(乙酰丙酮亚胺)二[三(3甲氧基1丙基)膦]);家兔注射99 Tcm Q3 后定时采血,绘制血药时间放射性曲线并分析其体内药代动力学。结果显示,制备99 Tcm Q3 的最佳配方为 K O H 溶液(1 m ol/ L,溶于 50% 乙醇)30 μ L、 Sn Cl2·2 H2 O 溶液(2 g/ L,溶于无水乙醇)20 μ L、 N, N′亚乙基二(乙酰丙酮亚胺)20 m g 和三(2甲氧基1丙基)膦5 m g。这些因素对标记物放化纯度的影响均具有显著性差异( P< 0.01),且各因素间不存在交互作用。99 Tcm Q3 兔血清除动力学符合一次静脉给药的二室药代动力学模型,并且99 Tcm Q3 血浆蛋白结合率低((7.13±0.42)% ))。
The 99 Tcm N, Nethylene bis (acetylacetoneimine) bis [tris (3methoxy1propyl) phosphine]) was prepared by orthogonal experiment. Rabbits were injected with 99 Tcm Q3 at regular intervals to draw blood timeradiation curves and to analyze their in vivo pharmacokinetics. The results showed that the optimal formulation of 99 Tcm Q3 was 30 μL of K O H solution (1 mol / L, 50% ethanol), 2 g / L of Sn Cl2 · 2 H 2 O solution Water ethanol) 20 μ L, 20 m g N and N’-ethylene-bis (acetylacetoneimine) and 5 m g tris (2-methoxy-1-propyl) phosphine. The effects of these factors on the radiochemical purity of the markers were significantly different (P <0.01), and there was no interaction between the factors. The kinetics of 99 Tcm Q3 rabbit serum was in accordance with the two - compartment pharmacokinetic model of single intravenous injection, and the plasma protein binding rate of 99 Tcm Q3 was low (7.13 ± 0.42)%).