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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 amphetamine hydrochloride tablets in fasting and postprandial single-dose Chinese healthy subjects. Methods Randomized, open, single-dose (200,400,600 mg) fasting and postprandial oral administration of the design method. Each dose group of eight subjects (4 males and 4 females) under oral and postnatal conditions, oral administration of the prescribed dose of amphetamine hydrochloride tablets. Collect blood and urine samples at different time points and determine the concentration by HPLC. Results The main pharmacokinetic parameters of 200, 400 and 600 mg of the anortho-salbutamol hydrochloride tablets for fasting and postprandial oral administration were as follows: The Cmax values of fasting and postprandial oral administration were (2.35 ± 0.28), (3.78 ± 0.84) and (4.77 ± 1.29) (1.27 ± 0.86), (2.75 ± 1.65), (2.42 ± 1.65) and (2.42 ± 1.26) mg / L, respectively; t 1/2 was 13.89 ± 2.83, 18.71 ± 1.98 and 16.47 ± 3.61 h respectively ± 1.30) h; AUC0-t were (31.66 ± 5.93), (76.87 ± 25.96) and (92.93 ± 22.79) mg · L -1 · h respectively; AUC 0- ∞ were (32.99 ± 6.12 (P <0.01), (79.01 ± 26.27) and (95.24 ± 23.37) mg · L -1 · h, respectively. The postprandial oral C max were 2.03 ± 0.34, 3.57 ± 0.74 and 4.68 ± 1.01 mg · L (-1) and t1 / 2β were (14.54 ± 2.08), (18.86 ± 2.20) and (16.91 ± 2.19) h, respectively; tmax were (2.64 ± 2.01), (3.46 ± 2.26) and (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 respectively; AUC 0- ∞ were 31.17 ± 4.13, (79.40 ± 14.00) and (109.66 ± 17.73) mg · L -1 · h, respectively. The cumulative excretion rates of urinary excretion of prototype drug from 0 to 96 h were (41.88 ± 11.00)%, (46.31 ± 13.23)% and (36.87 ± 10.64)% respectively after oral administration of 200, 400 and 600 mg of ampicillin hydrochloride. CONCLUSION: The tmax of 200,400,600 mg of amphetamines hydrochloride after oral administration was significantly prolonged compared with that of the fasting foods. However, the effect of diet on pharmacokinetic parameters was insignificant, and the effect of diet was not considered in clinic.