螺内酯样品和对照品大鼠长期毒性比较试验

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目的观察连续ig给予螺内酯样品及对照品30d对大鼠所产生的毒性反应,比较两个受试物之间毒性反应的差别,提供不良反应的靶器官及其恢复情况。方法设螺内酯样品及对照品20、60、180mg/kg3个剂量组和对照组,连续ig给药30d,停药观察15d,观察药物对动物精神行为、饮食、饮水、体质量等影响;在给药结束和恢复后进行血液学、血液生化、尿液生化及病理学检查。结果螺内酯样品及对照品ig给药30d,一般检查中螺内酯样品及对照品180mg/kg组雄性大鼠体质量增长均受到一定程度的抑制;血液学检查可见螺内酯样品和对照品均可引起雌雄大鼠血小板数升高,雄性大鼠凝血酶原时间增加,雌性大鼠凝血酶原时间和单核细胞比例降低;血液生化学检查可见螺内酯样品和对照品均可引起雄性大鼠丙氨酸氨基转移酶活性和钾离子明显升高,总胆红素明显降低;雌性大鼠丙氨酸氨基转移酶活性、尿素氮、总胆固醇和三酰甘油水平明显升高,总胆红素明显降低。脏器系数统计结果可见螺内酯样品及对照品可引起雌雄大鼠肝脏质量和系数升高;组织病理学检查未见明显由受试药物引起的病理改变。螺内酯样品和对照品对上述变化指标的影响趋势及程度基本一致,同剂量组间比较均无明显差异。停药恢复15d,螺内酯样品对动物血小板的影响恢复速度略慢于螺内酯对照品,两药各组其他各项指标的恢复情况基本一致。结论螺内酯样品及对照品ig给药30d,主要毒性靶器官为肝脏。螺内酯样品和对照品对上述变化指标的影响趋势及程度基本一致。 Objective To observe the toxic effects of continuous ig given spironolactone and reference substance for 30 days in rats and to compare the difference in toxicity between the two test substances and provide target organs for adverse reactions and their recovery. Methods The spironolactone 20 mg / kg and 20 mg / kg 3 dose group and the control group were treated with continuous ig administration for 30 days and drug withdrawal for 15 days. The effects of the drugs on the animal mental behavior, diet, drinking water and body weight were observed. Hematology, blood biochemistry, urine biochemistry and pathology after drug termination and recovery. Results Spironolactone and reference substance ig administration 30d, the general examination of the spirolactone sample and the reference substance 180mg / kg group of male rats body weight growth are subject to a certain degree of inhibition; hematology examination showed spironolactone samples and reference substance can cause male and female large The number of rat platelets increased, the prothrombin time of male rats increased, and the proportion of prothrombin time and mononuclear cells decreased in female rats. The results of blood biochemistry showed that both spironolactone and reference substance could induce alanine aminotransferase Enzyme activity and potassium ion were significantly increased, total bilirubin was significantly reduced; alanine aminotransferase activity, urea nitrogen, total cholesterol and triglyceride levels were significantly increased and total bilirubin was significantly decreased in female rats. Organ coefficient statistics show that spironolactone samples and reference substance can cause livers and male and female rats to improve the quality and coefficient; histopathological examination showed no obvious pathological changes caused by the test drug. Spirolactone samples and controls on the changes in the trend and extent of the indicators are basically the same, the same dose groups were no significant differences. Recovery of withdrawal 15d, spironolactone samples of animal platelets recovery rate of slightly slower than spironolactone reference substance, the two groups of the rest of the rest of the indicators were basically the same. Conclusion Spironolactone samples and reference substance administered ig 30d, the main toxic target organ for the liver. Spirolactone samples and controls on the above changes in the trend and extent of indicators are basically the same.
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