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在大鼠中,亚慢性给予或不给予利福平后氯法齐明的组织分布与沉积情况。

Tissue distribution and deposition of clofazimine in rat following subchronic treatment with or without rifampicin.

作者信息

Mamidi N V, Rajasekhar A, Prabhakar M C, Krishna D R

机构信息

University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.

出版信息

Arzneimittelforschung. 1995 Sep;45(9):1029-31.

PMID:7488306
Abstract

Tissue distribution and deposition characteristics of clofazimine (CAS 2030-63-9), an antileprotic drug in rats have been investigated following controlled sub-chronic administration (p.o.) for a period of 1-2 months. The drug was administered alone at a dose of 20 mg/kg body weight and in combination with rifampicin (CAS 13292-46-1) (20 mg/kg p.o.). Various tissues (liver, lung, spleen, small intestine, brain, heart, kidney, skin, stomach and subcutaneous fat) were analyzed for clofazimine in all the treated groups. High levels (range 0.9-3.6 mg/g of wet tissue) were observed in tissues having reticuloendothelial components. In other tissues the levels were relatively lower (range 3-114 micrograms/g of wet tissue). Histopathological studies revealed that clofazimine is deposited in many tissues in the form of reddish-orange crystals. Concomitant treatment with rifampicin did not significantly alter tissue distribution or deposition profile of clofazimine nor did it influence the histopathology.

摘要

在对大鼠进行为期1 - 2个月的对照亚慢性口服给药后,研究了抗麻风病药物氯法齐明(CAS 2030 - 63 - 9)在大鼠体内的组织分布和沉积特征。该药物单独以20 mg/kg体重的剂量给药,或与利福平(CAS 13292 - 46 - 1)(口服20 mg/kg)联合给药。对所有治疗组的各种组织(肝脏、肺、脾脏、小肠、大脑、心脏、肾脏、皮肤、胃和皮下脂肪)进行了氯法齐明分析。在具有网状内皮成分的组织中观察到高水平(范围为0.9 - 3.6 mg/g湿组织)。在其他组织中,水平相对较低(范围为3 - 114微克/g湿组织)。组织病理学研究表明,氯法齐明以红橙色晶体的形式沉积在许多组织中。与利福平联合治疗并未显著改变氯法齐明的组织分布或沉积情况,也未影响组织病理学。

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