Kirkwood C K, Wilson S K, Hayes P E, Barr W H, Sarkar M A, Ettigi P G
Department of Pharmacy and Pharmaceutics, Virginia Commonwealth University-Medical College of Virginia (VCU-MCV), Richmond 23298-0533.
Am J Hosp Pharm. 1994 Feb 15;51(4):486-9.
The single-dose bioavailabilities of two extended-release lithium carbonate products and an immediate-release product were compared. Nonsmoking healthy volunteers ages 20-31 (n = 12) were randomly assigned to one of three groups and given three treatments, each separated by a one-week period. The treatments, which were given to each group in a different sequence, consisted of three 300-mg immediate-release lithium carbonate tablets (Lithotab), two 450-mg extended-release lithium carbonate tablets (Eskalith CR), and three 300-mg extended-release lithium carbonate tablets (Lithobid). Blood samples were collected just before drug administration and at intervals up to 48 hours afterward. Urine was collected for 96 hours. Plasma and urine lithium concentrations were determined by flame-emission spectrophotometry, and lithium pharmacokinetic values and the cumulative urinary excretion of lithium were computed. Mean maximum plasma lithium concentration (Cmax) differed significantly among all three lithium carbonate products. Eskalith CR produced a 40% lower Cmax and Lithobid a 25% lower Cmax than Lithotab; Lithobid produced a 23% higher Cmax than Eskalith CR. Lithotab had a significantly shorter mean time to maximum plasma lithium concentration than either extended-release product. Mean cumulative urinary excretion of lithium did not differ significantly among the three products. Two extended-release lithium carbonate products were not bioequivalent when given in single doses to healthy volunteers.
比较了两种缓释碳酸锂产品和一种速释产品的单剂量生物利用度。将年龄在20 - 31岁的非吸烟健康志愿者(n = 12)随机分为三组,分别给予三种治疗,每次治疗间隔一周。以不同顺序给予每组的治疗包括:三片300毫克速释碳酸锂片(Lithotab)、两片450毫克缓释碳酸锂片(Eskalith CR)和三片300毫克缓释碳酸锂片(Lithobid)。在给药前及给药后长达48小时的间隔时间采集血样。收集尿液96小时。通过火焰发射分光光度法测定血浆和尿液中的锂浓度,并计算锂的药代动力学值和锂的累积尿排泄量。所有三种碳酸锂产品的平均最大血浆锂浓度(Cmax)差异显著。与Lithotab相比,Eskalith CR的Cmax低40%,Lithobid的Cmax低25%;与Eskalith CR相比,Lithobid的Cmax高23%。Lithotab达到最大血浆锂浓度的平均时间明显短于任何一种缓释产品。三种产品的锂平均累积尿排泄量无显著差异。单剂量给予健康志愿者时,两种缓释碳酸锂产品不具有生物等效性。