加替沙星胶囊的药代动力学及生物等效性评价
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[摘要] 目的：评价加替沙星胶囊在健康男性体内的药代动力学和生物等效性。方法：40例健康男性试验者随机平分为两组，分别口服国产与进口加替沙星胶囊试验制剂或参比制剂，采用高效液相色谱法测定血浆中加替沙星的浓度，计算主要药代动力学参数，评价两制剂的生物等效性。结果：口服国产和进口加替沙星后两组的半衰期、峰时间、峰浓度和滞后时间相比无显著性差异。同时生物等效性相比也无显著性差异，可认为两种制剂具有生物等效性。结论：国产与进口加替沙星胶囊试验制剂或参比制剂在健康志愿者体内具有生物等效性和类似的药代动力学。
[关键词] 加替沙星胶囊；高效液相色谱法；药代动力学；生物等效性
[中图分类号] R968 [文献标识码]A[文章编号]1673-7210(2011)03(c)-036-02
Pharmacokinetics and bioequivalence evaluation of Gatifloxacin Capsules
SU Jihong1, LI Qiju2
1.Pharmacy Department, Maternal and Child Health Hospital of Changsha City, Changsha 410007, China; 2.Pharmacy Department, Hu′nan Province People′s Hospital, Changsha 410005, China
[Abstract] Objective: To evaluate the pharmacokinetics and bioequivalence of Gatifloxacin Capsules in the healthy male. Methods: 40 healthy male were randomly divided into two groups, there were respectively given domestic and imported oral Gatifloxacin Capsules, used the high performance liquid chromatography method for detected the Gatifloxacin concentrations in plasma, and analyzed the major drug pharmacokinetic parameters and evaluated the bioequivalence of two formulations. Results: The oral administration of domestic and imported in the two groups after gatifloxacin′s half-life, peak time, peak concentration and the lag time had not significant different. Bioequivalence compared with the same time had no significant difference, so we thought that the two formulations were bioequivalent. Conclusion: Domestic and imported Gatifloxacin Capsules preparation or reference test preparation in healthy volunteers are bioequivalent and similar pharmacokinetics.
[Key words] Gatifloxacin Capsules; Performance liquid chromatography; Pharmacokinetics; Bioequivalence
加替沙星是新一代日本杏林制药公司研发的氟喹诺酮类广谱抗菌药物，现将其专利权已转让给美国施贵宝制药公司，有口服与静脉注射两种规格，已在全球多个国家等获得许可上市[1]。它抗菌谱广，抗菌活性强，不但对革兰阴性菌包括大肠埃希菌、流感嗜血杆菌、克雷伯菌属、铜绿假单胞菌、不动杆菌属、沙门菌属等具有较好的抗菌活性，而且对革兰阳性球菌包括金黄色葡萄球菌、溶血性链球菌、肺炎链球菌及厌氧菌也有较好的抗菌活性，对非典型病原体作用增强，并具有良好的药代动力学特性[2]。本实验比较了在我国健康成年男性志愿者中口服国产和进口加替沙星片剂的药代动力学参数，以评估两者的生物等效性，现报道如下：
1 材料与方法
1.1 仪器
HPLC 1100高压液相色谱仪，美国Agilent，配备自动进样器和二极管阵列检测器；Agilent化学高级色谱数据工作站；分析天平，上海生工电子；高速冷冻离心机，日本Olympus；HY-4多用调速振荡器；北京医用仪器厂：GL-88B旋涡混合器，上海医用仪器厂。
1.2 试剂
乙腈为色谱纯，四丁基溴化铵、为分析纯。受试制剂国产加替沙星(规格：200 mg/片，重庆赛维药业有限公司，批号：060701)；参比制剂进口加替沙星(规格：200 mg/片 ......
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