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农药制剂中惰性成分对西维因经皮吸收的影响。

Influence of inert ingredients in pesticide formulations on dermal absorption of carbaryl.

作者信息

Baynes R E, Riviere J E

机构信息

Cutaneous Pharmacology and Toxicology Center, College of Veterinary Medicine, North Carolina State University, Raleigh 27606, USA.

出版信息

Am J Vet Res. 1998 Feb;59(2):168-75.

PMID:9492931
Abstract

OBJECTIVES

To assess the influence of solvent plus various mixtures on percutaneous absorption and disposition of the carbamate insecticide, carbaryl (CA).

ANIMALS

Skin was obtained from the dorsum of 14 female weanling specific-pathogen-free Yorkshire pigs.

PROCEDURE

In this 8-hour in vitro flow-through diffusion study, porcine skin sections were dosed with 40 micrograms of CA/cm2 of surface area, different amounts of solvents (40 or 80% acetone or dimethyl sulfoxide [DMSO]), different amounts of a surfactant (0, 1, or 5% sodium lauryl sulfate [SLS]), an insect repellent (0 or 15% diethyl-m-toluamide [DEET]), an insecticide synergist (0 or 2% piperonyl butoxide [PB]), and a CA metabolite (40 micrograms/cm2 1-naphthol [1-NA]).

RESULTS

In general, CA absorption was greater from acetone than from DMSO mixtures, and CA penetration into skin and stratum corneum was greater from DMSO at 8 hours. This is consistent with the flux-time profiles, which depicted initial peak flux within 2 to 3 hours for most acetone mixtures, but a slow increase in flux for DMSO mixtures. Irrespective of the solvent, increasing water content in pesticide dosing mixtures significantly increased CA absorption from SLS mixtures only. The SLS also enhanced CA absorption, especially at low solvent concentrations. The DEET significantly reduced CA absorption from acetone, but not from DMSO mixtures, and 1-NA enhanced CA absorption from acetone, but not from DMSO mixtures. Piperonyl butoxide significantly enhanced CA absorption from acetone and DMSO mixtures. However, addition of PB or PB plus SLS did not significantly increase CA flux above that observed from solvent plus surfactant mixtures.

CONCLUSIONS

Inert ingredients can modulate percutaneous absorption of toxicologically important pesticides and their effect or activity on CA disposition is dependent on solvent specificity and solvent concentration. Whereas SLS, PB, and 1-NA can enhance pesticide absorption, DEET can reduce absorption.

摘要

目的

评估溶剂加各种混合物对氨基甲酸酯类杀虫剂西维因(CA)经皮吸收和分布的影响。

动物

从14只雌性断奶无特定病原体的约克夏猪的背部获取皮肤。

实验步骤

在这项8小时的体外流通扩散研究中,给猪皮肤切片的表面积每平方厘米施用40微克的CA、不同量的溶剂(40%或80%丙酮或二甲基亚砜[DMSO])、不同量的表面活性剂(0%、1%或5%十二烷基硫酸钠[SLS])、一种驱虫剂(0%或15%避蚊胺[DEET])、一种杀虫剂增效剂(0%或2%胡椒基丁醚[PB])以及一种CA代谢物(每平方厘米40微克1-萘酚[1-NA])。

结果

总体而言,CA从丙酮混合物中的吸收量大于从DMSO混合物中的吸收量,且在8小时时,CA从DMSO渗透到皮肤和角质层的量更大。这与通量-时间曲线一致,大多数丙酮混合物在2至3小时内呈现初始峰值通量,而DMSO混合物的通量则缓慢增加。无论使用何种溶剂,在农药给药混合物中增加含水量仅显著增加了CA从SLS混合物中的吸收。SLS也增强了CA的吸收,尤其是在低溶剂浓度下。DEET显著降低了CA从丙酮中的吸收,但未降低从DMSO混合物中的吸收,而1-NA增强了CA从丙酮中的吸收,但未增强从DMSO混合物中的吸收。胡椒基丁醚显著增强了CA从丙酮和DMSO混合物中的吸收。然而,添加PB或PB加SLS并没有使CA通量显著高于从溶剂加表面活性剂混合物中观察到的通量。

结论

惰性成分可调节具有毒理学重要性的农药的经皮吸收,它们对CA分布的影响或活性取决于溶剂特异性和溶剂浓度。虽然SLS、PB和1-NA可增强农药吸收,但DEET可降低吸收。

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