盐酸加替沙星胶囊的人体相对生物利用度研究

Study on Relative Bioavailability of Gatifloxacin Hydrochloride Capsules

目的：比较两种国产盐酸加替沙星制剂的人体相对生物利用度。方法：18名健康志愿者按照两制剂两周期的随机交叉试验设计，分别单剂量口服受试制剂（盐酸加替沙星胶囊）和参比制剂（盐酸加替沙星片）400mg，采用HPLC-紫外检测法测定人血浆中加替沙星的浓度，用DAS1．0软件对所得药代动力学参数进行统计分析。结果：受试和参比制剂的主要药代动力学参数如下：cmax分别为（4．29±0．72）和（4．04±0．45）μg／ml；tmax分别为（1．5±0．7）和（1．5±0．6）h；AUC0-36b分别为（40．26±4．77）和（37．89±4．09）μg·h·ml^-1；AUC0-∞分别为（41．69±5．20）和（39．12±4．53）μg·h·ml^-1；t1／2分别为（7．1±0．8）和（7．1±0．8）h。受试制剂相对于参比制剂的相对生物利用度为（106．3±6．6）％。结论：两制剂各药代动力学参数均无显著差异，二者具有生物等效性。

Objective： To invetigate pharmaeokineties and relative bioavailability of two gatifloxaein preparations in healthy male volunteers. Methods：In a randomized crossover study, 18 healthy male volunteers were given a single oral dose of 400 mg test gatifloxaein hydrochloride capsules and reference tablets. The concentrations of gatifloxaein in human plasma were determined by a HPLC method with ultra-violet detector. The pharmaeokinetie parameters were processed with DAS 1.0 package for statistic analysis. Results ：The pharmaeokinetie parameters of the test and reference preparations were as follows： cmax were （4.29±0.72） and （4.04±0.45）μg/ml;tmax were （1.5±0.7） and （1.5±0.6）h,AUC0-36b were （40.26±4.77） and （37.89±4.09）μg· h· ml^-1;AUC0-∞：were （41.69±5.20） and （39.12±4.53）μg·h·ml^-1 ; t1/2 were （7.1±0.8） and （7.1±0.8 ） h, respectively. The relative bioavailability of the test capsules was （ 106.3±6.6） %. Conclusion：There was no significant difference in tmax,cmax ,AUC0-3b and AUC0-36b between the two preparations. The two preparations were bioequivalent.