加替沙星胶囊药代动力学及生物等效性评价.docVIP

加替沙星胶囊药代动力学及生物等效性评价[摘要] 目的:研究两种加替沙星药剂的药代动力学参数,同时评估两者的生物等效性。方法:采用随机交叉,将36例男性健康志愿者随机分为两组,分别单剂量口服加替沙星胶囊400 mg(国产)和加替沙星片400 mg(进口),以高效液相色谱法测定受试者服药后血浆中加替沙星的经时浓度,计算加替沙星药动学参数,以双单侧t检验统计法比较两种甲磺酸加替沙星制剂是否具有生物等效性。结果:进口药物AUCo-t的90%可信限为国内药物相应参数的95.8%左右,Cmax的90%可信限为国内药物相应参数的95.6%左右。结论:加替沙星胶囊口服吸收迅速,血药浓度高,组织分布广,消除半衰期长,国产与进口加替沙星为生物等效制剂。 [关键词] 加替沙星;药代动力学;生物等效性 [中图分类号] R96 [文献标识码]A [文章编号]1673-7210(2010)01(a)-056-02 Assessment on pharmacokinetics and bioavailability of Gatifloxacin Capsules JIANG Hongtao (Women and Children Hospital in Dandong City, Dandong 118002, China) [Abstract] Objective: To study pharmacokinetic parameters of two kinds of Gatifloxacin Capsules and assessment their bioavailability. Methods: An open, randomized, two-period crossover study was conducted in 36 healthy volunteers. Concentrations of gatifloxacin in plasma were assayed by HPLC after a single oral rose of 400 mg local Gatifloxacin Capsules or imported Gatifloxacin Capsules. The main pharmacokinetic parameters were analyzed by two one-sided t test. Results: Compared local Gatifloxacin Capsules, 90% confidence limit of AUCo-t and Cmax of imported Gatifloxacin Capsules was 95.8% times and 95.6% times, respectively. Conclusion: The Gatifloxacin Capsules has characteristic of quick absorption, high peak concentration in plasma and longer mean retention times. The restult of statistical analysis showed that two formulations were bioequivalent. [Key words] Gatifloxacin Capsules; Pharmacokinetics; Bioavailability 加替沙星(Gatifloxacin)是新一代的喹诺酮类抗菌药物,口服易吸收,静脉注射与口服具有生物等效性。其对革兰阳性菌、衣原体、支原体和分枝杆菌等都有很强的杀菌作用。本研究对扬子江药业研制的加替沙星胶囊在健康男性受试者中进行了药代动力学研究,并以进口加替沙星片为参比,并评价两种药剂的生物等效性,希望能为该药在临床合理应用提供参考依据。 1 材料与方法 1.1 材料 实验试剂:加替沙星胶囊[规格:200 mg/粒,批号:0810020,扬子江药业(A药物)];参比制剂:加替沙星片[规格:200 mg/片,批号:0305711,中美史克(B药物)];甲醇为色谱纯,磷酸二氢钠、三乙胺、二氯甲烷试剂均为分析纯。 1.2 受试对象 选择健康男性36名,平均年龄(36.2±2.5)岁,平均身高(1.70±0.05)m,平均体重(61.8±5.6)kg。经病史询问,并全面体检,血、尿常规、肝、肾功能等均无异常。受试者在试验前两周未服用过任何相关抗菌药物,同时受试者均签署受试者知情同意书。 1.3 分组与给药 本试验采用双周期自