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大鼠经阴道和口服给予[14C]甲硝唑后的处置情况。

The disposition of [14C]metronidazole in rats following vaginal and oral administration.

作者信息

Buttar H S, Siddiqui W H, Moffatt J H

出版信息

J Pharm Pharmacol. 1979 Aug;31(8):542-4. doi: 10.1111/j.2042-7158.1979.tb13580.x.

Abstract

The absorption, tissue distribution and excretion of [17C]metronidazole (14C-MTZ) were compared during the first 4 h after administration of 10 mg kg-1 of 14C-MTZ either orally or intravaginally (i.v.g.) to rats. Peak 14C blood concentrations were reached at 1 h in both groups. Blood samples collected at 0.5, 3 and 4 h had a higher 14C concentration in orally dosed rats (P less than 0.05) than in i.v.g.-treated animals. About 3% of the i.v.g. applied dose remained in the vagina at 4 h. After 4 h, the plasma, liver, kidney, brain, lung and uterus concentrations of 14C were similar in both groups, whereas the blood, skeletal muscle and fat 14C values were significantly greater in the orally dosed rats. The total recoveries of 14C in the urine and faeces did not differ (ca 38% over 4 h) between the two groups. These results suggest that the kinetics of metronidazole are similar after the administration of equal amounts of this drug by either route.

摘要

在给大鼠口服或经阴道给予(经阴道给予)10 mg/kg的[17C]甲硝唑(14C-MTZ)后的前4小时内,比较了14C-MTZ的吸收、组织分布和排泄情况。两组在给药1小时时均达到14C血药浓度峰值。在0.5、3和4小时采集的血样中,口服给药大鼠的14C浓度高于经阴道给药的动物(P<0.05)。在4小时时,约3%经阴道给予的剂量残留在阴道中。4小时后,两组的血浆、肝脏、肾脏、大脑、肺和子宫中的14C浓度相似,而口服给药大鼠的血液、骨骼肌和脂肪中的14C值明显更高。两组尿液和粪便中14C的总回收率无差异(4小时内约为38%)。这些结果表明,通过两种途径给予等量该药物后,甲硝唑的动力学相似。

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