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硝酸氰胺静注混悬剂的药代动力学和急性毒性

THE PHARMACOEINETICS AND ACUTE TOXICITY OF MICRONIZED NITRODIPHENYLAMINOISOTHIOCYANATE(7505)AQUEOUS SUSPENSION FOR INTRAVENOUS INJECTION

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【作者】 陈古荣; 涂植光; 全钰珠;

【Author】 Department of Pharmacology:Chen Gurong Tu Zhiguang Quan Yuzhu

【机构】 四川省中药研究所; 重庆医学院药理教研室; 重庆医学院药理教研室 进修员;

【摘要】 <正> 硝硫氰胺(Nithiocyamine,“7505”),为一新型抗血吸虫药,由于本品难溶于水,故药代动力学的研究,受到一定限制。最近,上海医药工业研究院试制出供家畜静脉注射用的硝硫氰胺混悬剂。本文乃采用该制剂给健康家兔进行静脉注射,观察硝硫氰

【Abstract】 The pharmacokinetics of Nitrodiphenylaminoisothiocyanate(7505)in the healthy rabbits was studied.The micronized 7505 aqueous suspension was given to rabbits by intravenous injection.The plasma C-T curve indicated that the data fitted a two-compartment open model. The pharmacokinetic parameters are:t1/2α,1.253hr;t1/2β,13.509hr;K12,0.258hr-1;K21, 0.214hr-1;K10,0.133hr-1;V1,3.687 1/kg;V2,4.441 1/kg;VB,9.520 1/kg;QB,0.488 1/kg/ hr;AUC0-16,11.091 mg.hr/1. The mice acute LD50 of micronized 7505 in aqueous suspension by intravenous or intraperitoneal injection was 169.99±13.77mg/kg(P=0.95)or 180.50±21.13mg/kg(P=0.95)respectively.It seems that the formulated dosage form given intravenusly is not more toxic significantly than given intraperitoneally.

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