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本文报告日本血吸虫病患者口服硝硫氰胺后,药物在体内的分布与清除及药物对大鼠肝胆系统的影响。 硝硫氰胺350 mg分3天口服的47例血吸虫病患者,首次给药后48小时的全血药浓度的平均值为1.56±0.18 μg/ml。末次给药后16天,血药浓度还维持在0.10 μg/ml。但药物主要存在于血浆中,血细胞与其它有形成分的含药量则较少。给药期原药经由尿的排泄量大于停药后的排泄量,药物的排出可持续到19天以上。在一例因其它疾病死亡的尸检脏器组织中,测得肝、肾、心、脾的药物含量均高于肌肉、脑、脂肪与血清中的含药量。 大鼠口服硝硫氰胺100 mg/kg/d×7,胆汁分泌量明显减少,与对照组比较胆汁量减少58.3％。药物能抑制肝脏分泌胆汁的能力,并使动物黄疸指数和胆红素升高。
This article reports the distribution of schistosomiasis japonica schistosomiasis in patients with oral administration of thiocyanic acid and drug clearance and the effect of drugs on the hepatobiliary system in rats. Forty-seven schistosomiasis patients treated with 350 mg of nitrofurazone for 3 days had a mean whole blood concentration of 1.56 ± 0.18 μg / ml at 48 hours after the first dose. 16 days after the last dose, plasma concentration was also maintained at 0.10 μg / ml. However, the drug is mainly present in the plasma, with less blood and other tangible components. Drug delivery through the urinary excretion is greater than the amount of excretion after drug withdrawal, the drug can be discharged to 19 days or more. In one case of autopsy organs that died of other diseases, the measured contents of liver, kidney, heart and spleen were higher than those in muscle, brain, fat and serum. Oral administration of 100 mg / kg / d × 7 of nitrosamine in rats significantly reduced bile secretion, compared with the control group decreased 58.3%. Drugs can inhibit the ability of the liver to secrete bile, and animal jaundice index and bilirubin.