<sup>99</sup>Tc<sup>m</sup>-环丙沙星一步法药盒的制备及其动物体内的分布

⁹⁹Tc^m-环丙沙星一步法药盒的制备及其动物体内的分布

摘要: 采用国产盐酸环丙沙星原料药，研究确定了99Tcm-环丙沙星（ciprofloxacin ，CPF）的最佳标记条件，在此基础上制备环丙沙星冻干品药盒，并初步研究了99Tcm-CPF在炎症模型小鼠体内的分布。结果显示最佳标记条件为：盐酸环丙沙星的用量大于4 mg；SnCl2•2H2O的用量大于100μg；体系pH为3.0~3.5；反应时间约10 min。最佳标记条件下制备的99Tcm-CPF放化纯度>95%，室温放置6 h，其放化纯度无明显变化；药盒分别在0~8 ℃冷藏及－18 ℃冷冻保存3个月后再标记，标记物的放化纯度仍>95%；小鼠炎症模型实验结果显示，注射后4 h脓肿与肌肉放射性摄取比为4.30±0.31。

Abstract: Ciprofloxacin (CPF) made in China is labeled with 99Tcm and the factors affecting the labeling efficiency are determined. Accordingly, a new CPF cold kit is developed and the biodistribution of 99Tcm-CPF in infected animal is evaluated. Under the optimal condition of pH 3.0～3.5, CPF contents above 4 mg, SnCl2•2H2O contents over 100μg, 10 minutes after injection of 99TcmO4-, the radiochemical purity of 99Tcm-CPF is above 95% and remained >95% at 6 h after preparation at room temperature. The kit is stored at 0~8℃ or at -18℃ in refrigerator, theradiochemical purity of 99Tcm-CPF keeps up with over 95% after 3 months. Mice with infectious lesions injected with 99Tcm-CPF show a mean abscess-to-muscle ratio of 4.30±0.31at 4h post injection.