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比格犬对乙酸2-丙氧基乙酯和乙酸2-乙氧基乙酯的肺部及经皮吸收情况

Pulmonary and percutaneous absorption of 2-propoxyethyl acetate and 2-ethoxyethyl acetate in beagle dogs.

作者信息

Guest D, Hamilton M L, Deisinger P J, DiVincenzo G D

出版信息

Environ Health Perspect. 1984 Aug;57:177-83. doi: 10.1289/ehp.8457177.

Abstract

A comparison was made of the absorption and elimination rates of 2-propoxyethyl acetate (PEA) and 2-ethoxyethyl acetate (EEA) following inhalation, dermal application or IV administration. Male beagle dogs were exposed to 50 ppm PEA or EEA for 5 hr, and breath samples were collected during the exposure and a 3-hr recovery period. Both compounds were rapidly absorbed through the lungs. After 10 min of exposure, the concentrations of the parent compounds in the expired breath were 5 to 10 ppm (80-90% absorption) and reached plateau values at about 3 hr of 13 ppm for PEA (74% absorption) and 16 ppm for EEA (68% absorption). Post-exposure breath samples declined exponentially to 0.5 ppm and 2 ppm after 3 hr for PEA and EEA, respectively. Expired concentrations of PEA were slightly, but significantly (p less than 0.025), lower than those of EEA at corresponding times during the exposure. After IV dosing with 1 mg/kg [ethyl-1,2-14C]PEA, the urine contained 61% and 88% of the dose in 4 and 24 hr, respectively. [14C]EEA was eliminated more slowly, with 20% and 61% of the dose appearing in the urine in 4 and 24 hr, respectively. Blood elimination half-lives were 1.6 hr for [14C]PEA and 7.9 hr for [14C]EEA. Only trace amounts of 14CO2 (less than 1%) or volatile materials (less than 0.1%) were detected in the expired air with either compound. For studies of percutaneous absorption, [14C]PEA or [14C]EEA was added to undiluted compound and applied in a glass cell to a shaved area on a dog's thorax for 30 or 60 min.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

对吸入、经皮给药或静脉注射后乙酸2-丙氧基乙酯(PEA)和乙酸2-乙氧基乙酯(EEA)的吸收和消除速率进行了比较。雄性比格犬暴露于50 ppm的PEA或EEA中5小时,在暴露期间和3小时恢复期收集呼吸样本。两种化合物均通过肺部迅速吸收。暴露10分钟后,呼出气体中母体化合物的浓度为5至10 ppm(吸收80-90%),约3小时时达到平台值,PEA为13 ppm(吸收74%),EEA为16 ppm(吸收68%)。暴露后呼吸样本在3小时后分别呈指数下降至PEA的0.5 ppm和EEA的2 ppm。在暴露期间的相应时间,呼出的PEA浓度略低于EEA,但差异显著(p小于0.025)。静脉注射1 mg/kg [乙基-1,2-14C]PEA后,尿液在4小时和24小时分别含有剂量的61%和88%。[14C]EEA消除较慢,在4小时和24小时分别有20%和61%的剂量出现在尿液中。[14C]PEA的血液消除半衰期为1.6小时,[14C]EEA为7.9小时。两种化合物在呼出气体中仅检测到痕量的14CO2(小于1%)或挥发性物质(小于0.1%)。对于经皮吸收研究,将[14C]PEA或[14C]EEA添加到未稀释的化合物中,并在玻璃池中应用于犬胸部的剃毛区域30或60分钟。(摘要截断于250字)

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