Sugai K, Imamura Y, Mihashi S, Mori N, Baba S
J Toxicol Sci. 1986 Aug;11(3):155-67. doi: 10.2131/jts.11.155.
125I-Labeled batroxobin was prepared and following its intravenous and subcutaneous administrations to rats and dogs, the blood radioactivity was determined. In the both species following the intravenous injections, the decrease in radioactivity was biexponential. Following subcutaneous administration, radioactivity became maximal at 6h and decreased in a manner similar to that of the beta-phase of the intravenous injection. The blood concentration of fibrinogen in dogs was also determined. After the intravenous injection, fibrinogen became undetectable 1h later, and appeared again in the blood at 24h. After the subcutaneous injection, the decrease was not so rapid. Fibrinogen resumed its original levels at 7 day after the administration in both the routes. Radioactivity after the both injections was excreted generally in the urine in about the same amounts. The total urinary and fecal excretions in rats and dogs were 80 and 95%, respectively. The distribution of radioactivity in the tissues was examined by counting technique and whole-body autoradiography. Radioactivity predominantly accumulated in the thyroid and stomach and could also be found in the kidneys and liver in fair amounts. The distribution patterns of radioactivity for both the routes of administrations and also for male and pregnant rats were basically the same. In fetus rats, a slight distribution was noted. From the results of gel filtration chromatography and trichloroacetic acid fractionation, [125I] batroxobin was metabolized soon after the administration to afford low molecular substances such as 125I-ion in the plasma and urine.
制备了125I标记的巴曲酶，并在对大鼠和犬进行静脉内和皮下给药后，测定了血液放射性。在这两个物种中，静脉注射后放射性的下降呈双指数形式。皮下给药后，放射性在6小时达到最大值，并以类似于静脉注射β相的方式下降。还测定了犬的血液纤维蛋白原浓度。静脉注射后，1小时后纤维蛋白原无法检测到，并在24小时再次出现在血液中。皮下注射后，下降没有那么快。两种给药途径在给药7天后纤维蛋白原恢复到原始水平。两种注射后的放射性一般以大致相同的量经尿液排出。大鼠和犬的尿液和粪便总排泄量分别为80%和95%。通过计数技术和全身放射自显影检查了组织中的放射性分布。放射性主要积聚在甲状腺和胃中，也可以在肾脏和肝脏中大量发现。两种给药途径以及雄性和妊娠大鼠的放射性分布模式基本相同。在胎鼠中，有轻微的分布。从凝胶过滤色谱和三氯乙酸分级分离的结果来看，[125I]巴曲酶在给药后很快被代谢，在血浆和尿液中产生低分子物质，如125I离子。
