甲磺酸加替沙星胶囊与片剂的相对生物利用度研究

RelatiVe bioavailability of gatinoxacin methane-sulfonate capSUles versus tablets in healthy male volunteers

目的:评价甲磺酸加替沙星胶囊剂对片剂的相对生物利用度。方法:选择24例18～40岁健康成年男性受试者,随机分为2组,自身前后交叉依次口服甲磺酸加替沙星胶囊剂与片剂400mg,应用高效液相色谱法测定各受试者给药后不同时间点的血药浓度,采用3P97软件进行数据处理,计算药动学参数,应用STAT进行统计分析。结果:甲磺酸加替沙星胶囊剂与片剂药-时曲线符合二房室模型,胶囊剂与片剂达峰时间(T_(max))分别为(1.16±0.40)和(1.10±0.40)h;峰浓度(C_(max))分别为(3.91±0.61)和(3.85±0.83)mg·L^(-1);血浆生物半衰期(t_(1/2))分别为(6.77±1.65)和(7.28±1.20)h;血药浓度-时间曲线下面积(AUC_(0～t))分别为(28.23±4.77)和(26.88±6.54)mg·h·L^(-1)。胶囊剂与片剂主要药动学参数无显著差异。结论:甲磺酸加替沙星胶囊剂相对于片剂的相对生物利用度为105.4%。

Objective: To assess the relative bioavailability of gatifioxacin methane-sulfonate capsules versus tablets. Methods: 24 healthy male volunteers were randomized orally to receive a single crossover dose of either 400mg gatifloxacin capsules or tablets (400mg/each). The plasma gatifloxacin concentrations at certain timepoints after the administration of the gatifloxacin were measured using HPLC. The pharmacokinetic parameters of both gatifoxacins were evaluated using 3P97 program. Results: Ceneralized plot of gatifoxacin concentration versus time showed drug distribution and equilibration for a two-compartment model. No statistical difference of the gatifoxacin capsules versus tablets was found in the pharmacokinetie profiles, i. e. , T_(max) (1.16± 0.40) versus (1.10±0.40)h; C_(max)(3.91±0.61) versus (3.85±0.83)mg·L^(-1); t_(1/2) (6.77±1.65 ) versus (7.28±1.20) h; AUC_(0-t)(28.23±4.77) versus (26.88±6.54)mg·h·L^(-1). Conclusion: The relative bioavailability of the gatifloxacin capsules was 105.4 %.