Bachmann K A, Schwartz J I, Jauregui L
Department of Pharmacology, University of Toledo College of Pharmacy, Ohio 43606.
Br J Clin Pharmacol. 1988 Aug;26(2):191-4. doi: 10.1111/j.1365-2125.1988.tb03387.x.
The effect of ciprofloxacin treatment on theophylline clearance was evaluated with a theophylline multiple dose, multiple sample protocol and with a single dose, single sample protocol. The object was to determine whether a single dose, single sample protocol for estimating theophylline clearance could be used as a screening strategy for evaluating host factor influences on theophylline clearance. Ciprofloxacin (750 mg per os) was administered every 12 h for nine doses in the multidose study and every 12 h for seven doses in the single dose protocol. Subjects were sixteen healthy, non-smoking young adult males. The oral clearance of theophylline at steady state, (CL/F)ss, decreased from a mean (+/- s.d.) value of 0.035 (+/- 0.008) 1 h-1 kg-1 to 0.024 (+/- 0.004) 1 h-1 kg-1 during ciprofloxacin treatment. Single sample estimates of theophylline clearance, CL/F, similarly decreased from 0.040 (+/- 0.014) 1 h-1 kg-1 to 0.018 (+/- 0.008) 1 h-1 kg-1. Mean theophylline clearances were significantly different when comparing control with ciprofloxacin treatment means (P less than 0.01), but were not different when comparing single sample vs multiple sample clearances for a given treatment (i.e. control or ciprofloxacin). It is concluded that a single dose, single sample strategy may be used in screening for host-factor influences on theophylline clearance.
采用茶碱多剂量、多样本方案以及单剂量、单样本方案评估环丙沙星治疗对茶碱清除率的影响。目的是确定用于估计茶碱清除率的单剂量、单样本方案是否可作为一种筛查策略,以评估宿主因素对茶碱清除率的影响。在多剂量研究中,每12小时口服给予环丙沙星(750毫克),共九剂;在单剂量方案中,每12小时给予七剂。受试者为16名健康、不吸烟的年轻成年男性。在环丙沙星治疗期间,茶碱稳态口服清除率(CL/F)ss从平均(±标准差)值0.035(±0.008)升/小时/千克降至0.024(±0.004)升/小时/千克。茶碱清除率的单样本估计值CL/F同样从0.040(±0.014)升/小时/千克降至0.018(±0.008)升/小时/千克。比较对照与环丙沙星治疗组的均值时,平均茶碱清除率有显著差异(P<0.01),但对于给定治疗(即对照或环丙沙星),比较单样本与多样本清除率时无差异。结论是,单剂量、单样本策略可用于筛查宿主因素对茶碱清除率的影响。