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阿斯巴甜的药代动力学——衰老的影响。

Aspartame pharmacokinetics - the effect of ageing.

作者信息

Puthrasingam S, Heybroek W M, Johnston A, Maskrey V, Swift C G, Turner P, Abrams S M, Jackson S H

机构信息

Department of Health Care of the Elderly, King's College School of Medicine and Dentistry, Dulwich Hospital, E. Dulwich Grove, London E22 8PT, UK.

出版信息

Age Ageing. 1996 May;25(3):217-20. doi: 10.1093/ageing/25.3.217.

Abstract

Aspartame is an intense sweetener which is increasingly used in the UK. It is registered at an acceptable daily intake (ADI) of 40 mg/kg, although there are no previous data relating to the metabolism of aspartame in older people. Twelve young and 12 elderly volunteers each received a single dose of approximately 40 mg/kg of aspartame. Baseline concentrations of phenylalanine (the main metabolite of aspartame) rose after ingestion with a significantly higher maximum concentration (Cmax) (81.3 vs. 63.3 micromol/1, p<0.01) and area under the plasma concentration-time curve extrapolated to infinity AUC 9(0-infinity)(518.7 vs. 353.5 micromol . h/l, p<0.01) in the elderly group. The higher concentrations reflected a significant fall in volume of distribution (V) from 2.03 to 1.59 1/kg (p <0.05) and clearance (CL) from 7.3 to 4.9 ml/min/kg (p <0.005) in the elderly group. The greater effect on CL than on V resulted in a small but non-significant rise in elimination half life (3.5 to 3.9 hours). The sizes of the differences were modest implying that there is no need on pharmacokinetic grounds for a change in the ADI for older people.

摘要

阿斯巴甜是一种高强度甜味剂,在英国的使用越来越广泛。它的每日可接受摄入量(ADI)为40毫克/千克,不过此前尚无关于老年人阿斯巴甜代谢的数据。12名年轻志愿者和12名老年志愿者各自服用了约40毫克/千克的单剂量阿斯巴甜。摄入后,苯丙氨酸(阿斯巴甜的主要代谢物)的基线浓度升高,老年组的最大浓度(Cmax)显著更高(81.3对63.3微摩尔/升,p<0.01),血浆浓度-时间曲线外推至无穷大时的曲线下面积(AUC9(0-无穷大))也显著更高(518.7对353.5微摩尔·小时/升,p<0.01)。较高的浓度反映出老年组的分布容积(V)从2.03降至1.59升/千克(p<0.05),清除率(CL)从7.3降至4.9毫升/分钟/千克(p<0.005)。对CL的影响大于对V的影响,导致消除半衰期略有但不显著的延长(从3.5小时至3.9小时)。差异幅度不大,这意味着从药代动力学角度来看,无需改变老年人的ADI。

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