Gerstenberg B, Schepers G, Voncken P, Völkel H
INBIFO Institut für Biologische Forschung, Köln, Germany.
Drug Metab Dispos. 1995 Jan;23(1):143-8.
This study was performed to assess the contribution of systemic and external uptake to nicotine accumulation in hair. The systemic nicotine uptake in hair was determined in pigmented rats (Brown Norway) and albino rats (Sprague-Dawley) after subcutaneous administration of 3 doses of nicotine with osmotic minipumps [5, 10, and 20 mg/(kg x day) for 3 weeks], the highest dose also following metabolic enzyme induction. The external nicotine uptake was determined in cut hair of both strains after exposure to room-aged cigarette sidestream smoke, a surrogate for environmental tobacco smoke (nicotine concentration: 5 micrograms/liter for 1, 2, and 3 weeks). Nicotine and its metabolite cotinine were determined using capillary GC after complete alkaline digestion of the hair sample and solvent extraction. Systemic uptake: Nicotine and cotinine concentrations in hair were dose-dependent and correlated with plasma concentrations. The nicotine concentration was approximately 20 times higher in pigmented than in unpigmented hair. The cotinine concentration was approximately 10 times lower than the nicotine concentration in pigmented hair. After enzyme induction before administration, nicotine and cotinine concentrations in hair were significantly reduced in parallel to the reduced plasma concentrations, showing the influence of metabolism. External uptake: Nicotine was found in the hair of both strains, the concentration in pigmented hair being a factor of 1.5 higher than in unpigmented hair. Thus, hair pigmentation had a major influence on systemic uptake in hair and a minor influence on external uptake in hair.(ABSTRACT TRUNCATED AT 250 WORDS)
本研究旨在评估全身吸收和外部吸收对毛发中尼古丁积累的贡献。在有色大鼠(棕色挪威大鼠)和白化大鼠(斯普拉格-道利大鼠)皮下植入渗透微型泵给予3种剂量的尼古丁[5、10和20毫克/(千克·天),持续3周]后,测定毛发中的全身尼古丁吸收情况,最高剂量组在给药前还进行了代谢酶诱导。在两种品系的剪发暴露于室内陈化香烟侧流烟雾(环境烟草烟雾的替代物,尼古丁浓度为5微克/升,持续1、2和3周)后,测定外部尼古丁吸收情况。在毛发样品完全碱性消化和溶剂萃取后,使用毛细管气相色谱法测定尼古丁及其代谢物可替宁。全身吸收:毛发中的尼古丁和可替宁浓度呈剂量依赖性,且与血浆浓度相关。有色毛发中的尼古丁浓度比无色毛发高约20倍。有色毛发中的可替宁浓度比尼古丁浓度低约10倍。给药前进行酶诱导后,毛发中的尼古丁和可替宁浓度与降低的血浆浓度平行显著降低,表明代谢的影响。外部吸收:在两种品系的毛发中均发现了尼古丁,有色毛发中的浓度比无色毛发高1.5倍。因此,毛发色素沉着对毛发中的全身吸收有主要影响,对毛发中的外部吸收有次要影响。(摘要截短为250字)