中国健康志愿者单剂口服甲磺酸加替沙星片的药代动力学研讨.pdfVIP

中国健康志愿者单剂口服甲磺酸加替沙星片的药代动力学研究 王睿 裴斐 方翼 朱曼 王中孝 柴栋 王锡萍 解放军总医院临床药理药学研究室,北京 100853 摘要 目的 研究中国健康成年志愿者单剂口服甲磺酸加替沙星片的药代动力学 方法 按GCP 指导原则设计试验方案 选择9 名健康受试者分别依次单剂口服200mg 400mg 600mg 3 个剂量的甲磺酸加替沙星片后 应用HPLC 测定血药浓度 采用3P97 软件进行数 据处理 求出药代动力学参数 结果 受试者分别给药后 药- 时曲线符合二房室模型 主 . - 1 . - 1 要药代动力学参数 Cmax 分别为 2.028 0.362 mg L 3.749 0.446 mg L 4.876 0.569 . - 1 mg L t1/2 分别为7.489 0.806h 7.063 0.890h 7.735 0.8701h AUC0~t 分别为12.24 -1 -1 -1 1.51mg· h·L 26.02 3.38 mg· h·L 39.22 6.57 mg· h·L 原型药主要经肾排泄 48h 尿药累 积排泄率分别为61.90% 7.70% 60.90% 5.70% 和58.74% 13.49% 结论 9 名健康受试者分别口服给药后 药- 时曲线符合二房室模型 甲磺酸加替沙星在 200mg~600mg 剂量范围内药物体内过程呈线性动力学特征而无饱和性 主要排泄途径为肾 脏 关键词 加替沙星 HPLC 药代动力学 A Single Dose Pharmacokinetics of Gatifloxacin Mehanesulfanae tablets In Chinese Healthy Volunteers WANG Rui, PEI Fei, FANG Yi, ZHU Man, WANG ZhongXiao, CHAI Dong, WANG Xiping (Department of Clinical Pharmacology, Chinese PLA General Hospital,Beijing 100853) Abstract OBJECTIVE: To investigate the pharmacokinetics of oral single dose of Gatifloxacin mehanesulfanae tablets in Chinese healthy volunteers. METHODS: The protocal was designed according to GCP principle The plasma concentrations from the volunteers after oral 200mg 400mg 600mg gatifloxacin mehanesulfanae tablets were determined by HPLC method and the pharmacokinetcs parameters were calculated by 3P97 software. RESULTS: The plasma concentration –t