• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

氟吡甲禾灵丁酯在人体志愿者中的药代动力学。II:经皮给药。

Pharmacokinetics of fluazifop-butyl in human volunteers. II: Dermal dosing.

作者信息

Ramsey J D, Woollen B H, Auton T R, Batten P L, Leeser J E

机构信息

ICI Central Toxicology Laboratory, Macclesfield, Cheshire, UK.

出版信息

Hum Exp Toxicol. 1992 Jul;11(4):247-54. doi: 10.1177/096032719201100402.

DOI:10.1177/096032719201100402
PMID:1354971
Abstract
  1. The absorption of the herbicide fluazifop-butyl (f-b), has been determined from plasma and urine measurements in groups of six male volunteers following dermal administration of 2.5, 25 and 250 micrograms cm-2 from standardized formulations containing 0.05, 0.5 and 5.0% (w/v) fluazifop-butyl to a skin area of 800 cm2. 2. Urinary excretion rate of the principal metabolite fluazifop, following dosing with the 5% formulation, was described by a two-compartment pharmacokinetic model; the average elimination half-lives of initial and terminal phases were 18 h and approximately 70 h, respectively. For the other dose levels the elimination half-life was estimated to be 17 h; urine concentrations at later time points were too low to characterize a second compartment. 3. The estimated total fluazifop-butyl absorbed was 8.0, 3.4 and 1.6% of the applied dose for the 0.05, 0.5 and 5.0% formulations, respectively. 4. Up to 50% of the applied fluazifop-butyl was readily removed by skin washing and the majority of the remainder was transferred to clothing during the 24 h following application. 5. When six volunteers were given a daily dermal dose of the 0.5% formulation for five consecutive days, the plasma and urinary excretion kinetics of fluazifop could be accurately predicted by simple mathematical extrapolation of the kinetic data from the single exposure study at the equivalent daily dose. 6. It is concluded that fluazifop-butyl is only slowly and poorly absorbed through human skin and has a low potential to accumulate in man.
摘要
  1. 对六组男性志愿者进行研究,在其800平方厘米的皮肤区域分别涂抹含0.05%、0.5%和5.0%(w/v)精稳杀得的标准制剂,剂量分别为2.5、25和250微克/平方厘米,之后通过检测血浆和尿液来测定除草剂精稳杀得(f-b)的吸收情况。2. 用5%制剂给药后,主要代谢物精稳杀得的尿排泄率可用二室药代动力学模型描述;初始阶段和终末阶段的平均消除半衰期分别为18小时和大约70小时。对于其他剂量水平,消除半衰期估计为17小时;后期时间点的尿液浓度过低,无法确定第二房室。3. 对于0.05%、0.5%和5.0%的制剂,估计精稳杀得的总吸收量分别为给药剂量的8.0%、3.4%和1.6%。4. 涂抹的精稳杀得中,高达50%可通过皮肤清洗轻易去除,其余大部分在涂抹后的24小时内转移到衣物上。5. 当六名志愿者连续五天每日经皮给予0.5%的制剂时,精稳杀得的血浆和尿排泄动力学可通过对单次暴露研究中同等日剂量的动力学数据进行简单数学外推来准确预测。6. 研究得出结论,精稳杀得通过人体皮肤的吸收缓慢且较差,在人体内蓄积的可能性较低。

相似文献

1
Pharmacokinetics of fluazifop-butyl in human volunteers. II: Dermal dosing.氟吡甲禾灵丁酯在人体志愿者中的药代动力学。II:经皮给药。
Hum Exp Toxicol. 1992 Jul;11(4):247-54. doi: 10.1177/096032719201100402.
2
Oral pharmacokinetics of fluazifop-butyl in human volunteers.氟吡甲禾灵丁酯在人体志愿者中的口服药代动力学。
Hum Exp Toxicol. 1991 Jan;10(1):39-43. doi: 10.1177/096032719101000107.
3
Modelling dermal pharmacokinetics using in vitro data. Part II. Fluazifop-butyl in man.利用体外数据模拟皮肤药代动力学。第二部分。氟吡甲禾灵丁酯在人体中的情况。
Hum Exp Toxicol. 1993 May;12(3):207-13. doi: 10.1177/096032719301200303.
4
Modelling dermal pharmacokinetics using in vitro data. Part I. Fluazifop-butyl in the rat.利用体外数据模拟皮肤药代动力学。第一部分。大鼠体内的氟吡甲禾灵丁酯。
Hum Exp Toxicol. 1993 May;12(3):199-206. doi: 10.1177/096032719301200302.
5
Oral and dermal pharmacokinetics of triclopyr in human volunteers.三氯吡氧乙酸在人体志愿者中的口服和皮肤药代动力学。
Hum Toxicol. 1989 Nov;8(6):431-7. doi: 10.1177/096032718900800602.
6
Effect of dosing vehicle on the dermal absorption of fluazifop-butyl and fomesafen in rats in vivo.给药载体对大鼠体内氟吡禾灵丁酯和乙羧氟草醚经皮吸收的影响。
Fundam Appl Toxicol. 1994 Jul;23(1):93-100. doi: 10.1006/faat.1994.1084.
7
Comparison of two methods for determining the toxicokinetics of fluazifop-butyl after intravenous dosing in rats.大鼠静脉给药后精稳杀得毒代动力学两种测定方法的比较
Hum Exp Toxicol. 1994 Feb;13(2):123-9. doi: 10.1177/096032719401300211.
8
Fate of fluazifop butyl in rat and human skin in vitro.氟吡甲禾灵丁酯在大鼠和人皮肤中的体外代谢情况。
Arch Toxicol. 1993;67(1):44-8. doi: 10.1007/BF02072034.
9
A physiologically based mathematical model of dermal absorption in man.人体皮肤吸收的基于生理学的数学模型。
Hum Exp Toxicol. 1994 Jan;13(1):51-60. doi: 10.1177/096032719401300108.
10
The pharmacokinetics and metabolism of 14C/13C-labeled ortho-phenylphenol formation following dermal application to human volunteers.对人类志愿者进行皮肤给药后,14C/13C标记的邻苯基苯酚形成的药代动力学和代谢情况。
Hum Exp Toxicol. 1998 Aug;17(8):411-7. doi: 10.1177/096032719801700801.

引用本文的文献

1
The ethics of human volunteer studies involving experimental exposure to pesticides: unanswered dilemmas.涉及实验性接触农药的人体志愿者研究的伦理学:未解决的困境。
Environ Health. 2010 Aug 18;9:50. doi: 10.1186/1476-069X-9-50.
2
Biological monitoring for pesticide exposure--the role of human volunteer studies.农药暴露的生物监测——人体志愿者研究的作用
Int Arch Occup Environ Health. 1993;65(1 Suppl):S189-92. doi: 10.1007/BF00381338.