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猪体内有机磷杀虫剂的经皮吸收——不同载体的影响

Percutaneous absorption of organophosphorus insecticides in pigs--the influence of different vehicles.

作者信息

Gyrd-Hansen N, Brimer L, Rasmussen F

机构信息

Department of Pharmacology and Pathobiology, Royal Veterinary and Agricultural University, Frederiksberg, Denmark.

出版信息

J Vet Pharmacol Ther. 1993 Jun;16(2):174-80. doi: 10.1111/j.1365-2885.1993.tb00161.x.

Abstract

In 40 experiments on 20 pigs three different organophosphorus insecticides (OPs), parathion (n = 6), phoxim (n = 7) and phosmet (n = 7), were administered both intravenously (i.v.) and dermally (d.) as 'pour-ons' in a crossover design in order to determine the dermal bioavailability of the OPs. As percutaneous absorption of drugs may be affected by the vehicle used, three chemically different vehicles--DMSO, 1-octanol and macrogol 400-were used for the dermal administration of each of the OPs. The pharmacokinetic parameters measured showed that 15-30% of dermally applied parathion is absorbed when administered in DMSO or octanol, but only 4-5% when administered in macrogol. Absorption was fastest with DMSO and slowest with macrogol. For the two ectoparasiticides, phoxim and phosmet, only between 0.5 and 3% of the dermal dose was absorbed with little difference in the absorption rate between the three vehicles. On the basis of the very limited dermal bioavailability for these two OPs it seems doubtful whether sufficient concentrations can reach the ectoparasites through the systemic route.

摘要

在对20头猪进行的40项实验中,采用交叉设计,静脉注射(i.v.)和皮肤给药(d.,即浇泼剂)三种不同的有机磷杀虫剂(OPs),即对硫磷(n = 6)、辛硫磷(n = 7)和亚胺硫磷(n = 7),以确定这些OPs的皮肤生物利用度。由于药物的经皮吸收可能受所用赋形剂的影响,每种OPs皮肤给药时使用了三种化学性质不同的赋形剂——二甲基亚砜(DMSO)、1-辛醇和聚乙二醇400。所测得的药代动力学参数表明,对硫磷经皮肤给药于DMSO或辛醇中时,有15% - 30%被吸收,但经皮肤给药于聚乙二醇中时,只有4% - 5%被吸收。DMSO吸收最快,聚乙二醇吸收最慢。对于两种外用杀虫剂辛硫磷和亚胺硫磷,经皮肤给药剂量只有0.5% - 3%被吸收,三种赋形剂之间的吸收速率差异不大。基于这两种OPs非常有限的皮肤生物利用度,似乎怀疑是否有足够浓度的药物能通过全身途径到达体外寄生虫。

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