盐酸安妥沙星片在健康受试者单次给药的药代动力学  

Pharmacokinetics of single dose of antofloxacin hydrochloride in Chinese healthy subjects

作　　者：赵彩芸[1] 魏敏吉[1] 吕媛[1] 李湘燕[1] 贺锐锐[1] 赵艺璇 李天云[1] 刘燕[1] 夏亚红[1] 田继红[1] 马雁[1] 

机构地区：[1]北京大学第一医院临床药理研究所,北京100034 [2]北京大学公共卫生学院,北京100191

出　　处：《中国临床药理学杂志》2016年第16期1477-1480,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价盐酸安妥沙星片在中国健康受试者空腹和餐后单次给药的药代动力学。方法按随机、开放、单剂量(200,400,600 mg)空腹和餐后口服给药的方法进行设计。每个剂量组各有8名受试者(男4例、女4例)在空腹和餐后条件下口服规定剂量的盐酸安妥沙星片。收集不同时间点的血、尿样本,用HPLC法测定浓度。结果 16名受试者空腹和餐后口服盐酸安妥沙星片200,400,600 mg的主要药代动力学参数如下:空腹口服的Cmax分别为(2.35±0.28),(3.78±0.84),(4.77±1.29)mg·L^(-1);t1/2β分别为(13.89±2.83),(18.71±1.98),(16.47±3.61)h;tmax分别为(1.27±0.86),(2.75±1.65),(2.42±1.30)h;AUC0-t分别为(31.66±5.93),(76.87±25.96),(92.93±22.79)mg·L^(-1)·h;AUC_(0-∞)分别为(32.99±6.12),(79.01±26.27),(95.24±23.37)mg·L^(-1)·h;餐后口服的Cmax分别为(2.03±0.34),(3.57±0.74),(4.68±1.01)mg·L^(-1);t1/2β分别为(14.54±2.08),(18.86±2.20),(16.91±2.19)h;tmax分别为(2.64±2.01),(3.46±2.26),(4.50±1.69)h;AUC0-t分别为(29.27±3.42),(77.30±13.73),(107.43±17.72)mg·L^(-1)·h;AUC_(0-∞)分别为(31.17±4.13),(79.40±14.00),(109.66±17.73)mg·L^(-1)·h。单剂量口服盐酸安妥沙星200,400,600 mg后,0~96 h原型药物尿中累积排泄百分率分别为(41.88±11.00)%,(46.31±13.23)%,(36.87±10.64)%。结论餐后单次口服盐酸安妥沙星片200,400,600 mg的tmax较空腹明显延长,但进食对药代动力学参数影响不明显,临床应用可不考虑饮食的影响。Objective To evaluate the pharmacokinetics of single dose of antofloxacin hydrochloride tablet under fasting and fed state in Chinese healthy subjects. Methods A randomized, open and single dose study was conducted. Three dose groups, 16 randomly selected subjects in each group were given the dose of 200, 400 and 600 mg antofloxacin hydrochloride tablet, respectively. 8 subjects （4 male and 4 female） were administrated under fasting state and 8 subjects （4 male and 4 female） under fed state in each dose. The concentrations of antofloxacin in plasma and urine were determined by a validated HPLC method. Results The main pharmacokinetics parameters of three dose （200,400 and 600 mg） groups under fast were as follows： Cmax were （2.35 ± 0.28 ）,（3.78 ±0.84） and（4.77 ±1.29）mg · L^-1; t1/2β were（13.89 ±2.83）,（18.71 ±1.98） and（16.47 ±3.61）h; tmax were （1.27 ±0.86）, （2.75 ± 1.65） and （2.42 ± 1.30） h; AUC0-t, were （31.66 ± 5.93）, （76.87 ± 25.96） and （92. 93 ± 22. 79） mg · L^- 1 · h ; AUC0-∞ were （ 32.99 ± 6. 12 ）, （ 79.01 ± 26. 27 ） and （ 95.24 ± 23.37 ） mg· L^- 1h, respectively. Under fed state, Cmax were （2. 03 ± 0. 34） , （3.57 ± 0. 74） and （4. 68 ± 1.01 ） mg · L^- 1 ; t1/2β were （14. 54 ±2.08）, （18.86 ±2. 20） and（ 16.91 ±2. 19）h; tmax were （2. 64 ±2.01 ）, （3.46 ±2.26）, （4. 50 ± 1.69）h; AUC0-t were（29.27 ±3.42） ,（77.30 ± 13.73） and（ 107.43 ± 17.72）mg · L^-1· h; AUC0-∞ were（31.17 ±4. 13）, （79.40 ± 14. 00） and （ 109.66 ± 17.73） mg· L^- 1 · h, respectively. Urinary recovery rates were（41.88 ± 11.00） %, （46. 31 ± 13.23 ）% and （36.87 ± 10.64 ）%, respectively. Conclusion Food had no obvious influence on the pharmacokineties parameters after a single oral dose of 200, 400 and 600 mg antofloxacin hydrochloride tablet under fasting and fed state, except that the tmax increased. It can be considered that food had no effect on its clinical us

关 键 词：盐酸安妥沙星片 药代动力学 空腹 餐后 高效液相色谱法 

分 类 号：R978.1[医药卫生—药品]