Abu-Basha E A, Gehring R, Hantash T M, Al-Shunnaq A F, Idkaidek N M
Department of Veterinary Basic Medical Sciences, Faculty of Veterinary Medicine, Jordan University of Science and Technology, Irbid, Jordan.
J Vet Pharmacol Ther. 2009 Jun;32(3):258-63. doi: 10.1111/j.1365-2885.2008.01036.x.
A pharmacokinetic and bioavailability study of sulfadiazine combined with trimethoprim (sulfadiazine/trimethoprim) was carried out in fifteen healthy young ostriches after intravenous (i.v.), intramuscular (i.m.) and oral administration at a total dose of 30 mg/kg body weight (bw) (25 and 5 mg/kg bw of sulfadiazine and trimethoprim, respectively). The study followed a single dose, three periods, cross-over randomized design. The sulfadiazine/trimethoprim combination was administered to ostriches after an overnight fasting on three treatment days, each separated by a 2-week washout period. Blood samples were collected at 0 (pretreatment), 0.08, 0.25, 0.50, 1, 2, 4, 6, 8, 12, 24 and 48 h after drug administration. Following i.v. administration, the elimination half-life (t(1/2beta)), the mean residence time (MRT), volume of distribution at steady-state (V(d(ss))), volume of distribution based on terminal phase (V(d(z))), and the total body clearance (Cl(B)) were (13.23 +/- 2.24 and 1.95 +/- 0.19 h), (10.06 +/- 0.33 and 2.17 +/- 0.20 h), (0.60 +/- 0.08, and 2.35 +/- 0.14 L/kg), (0.79 +/- 0.12 and 2.49 +/- 0.14 L/kg) and (0.69 +/- 0.03 and 16.12 +/- 1.38 mL/min/kg), for sulfadiazine and trimethoprim, respectively. No significant difference in C(max) (35.47 +/- 2.52 and 37.50 +/- 3.39 microg/mL), t(max) (2.47 +/- 0.31 and 2.47 +/- 0.36 h), t((1/2)beta) (11.79 +/- 0.79 and 10.96 +/- 0.56 h), V(d(z))/F (0.77 +/- 0.06 and 0.89 +/- 0.07 L/kg), Cl(B)/F (0.76 +/- 0.04 and 0.89 +/- 0.07) and MRT (12.39 +/- 0.40 and 12.08 +/- 0.36 h) were found in sulfadiazine after i.m. and oral dosing, respectively. There were also no differences in C(max) (0.71 +/- 0.06 and 0.78 +/- 0.10 microg/mL), t(max) (2.07 +/- 0.28 and 3.27 +/- 0.28 h), t((1/2)beta) (3.30 +/- 0.25 and 3.83 +/- 0.33 h), V(d(z))/F (6.2 +/- 0.56 and 6.27 +/- 0.77 L/kg), Cl(B)/F (21.9 +/- 1.46 and 18.83 +/- 1.72) and MRT (3.68 +/- 0.19 and 4.34 +/- 0.14 h) for trimethoprim after i.m. and oral dosing, respectively. The absolute bioavailability (F) was 95.41% and 86.20% for sulfadiazine and 70.02% and 79.58% for trimethoprim after i.m. and oral administration, respectively.
在15只健康的年轻鸵鸟中进行了磺胺嘧啶与甲氧苄啶（磺胺嘧啶/甲氧苄啶）联合用药的药代动力学和生物利用度研究，给药途径为静脉注射（i.v.）、肌肉注射（i.m.）和口服，总剂量为30mg/kg体重（bw）（磺胺嘧啶和甲氧苄啶分别为25mg/kg bw和5mg/kg bw）。该研究采用单剂量、三个阶段、交叉随机设计。在三个治疗日，鸵鸟禁食过夜后给予磺胺嘧啶/甲氧苄啶联合用药，每个治疗日间隔2周的洗脱期。给药后0（给药前）、0.08、0.25、0.50、1、2、4、6、8、12、24和48小时采集血样。静脉注射给药后，磺胺嘧啶和甲氧苄啶的消除半衰期（t(1/2β)）、平均驻留时间（MRT）、稳态分布容积（V(d(ss))）、基于终末相的分布容积（V(d(z))）和全身清除率（Cl(B)）分别为（13.23±2.24和1.95±0.19小时）、（10.06±0.33和2.17±0.20小时）、（0.60±0.08和2.35±0.14L/kg）、（0.79±0.12和2.49±0.14L/kg）以及（0.69±0.03和16.12±1.38mL/min/kg）。肌肉注射和口服给药后，磺胺嘧啶的C(max)（35.47±2.52和37.50±3.39μg/mL）、t(max)（2.47±0.31和2.47±0.36小时）、t((1/2)β)（11.79±0.79和10.96±0.56小时）、V(d(z))/F（0.77±0.06和0.89±0.07L/kg）、Cl(B)/F（0.76±0.04和0.89±0.07）以及MRT（12.39±0.40和12.08±0.36小时）均无显著差异。肌肉注射和口服给药后，甲氧苄啶的C(max)（0.71±0.06和0.78±0.10μg/mL）、t(max)（2.07±0.28和3.27±0.28小时）、t((1/2)β)（3.30±0.25和3.83±0.33小时）、V(d(z))/F（6.2±0.56和6.27±0.77L/kg）、Cl(B)/F（21.9±1.46和18.83±1.72）以及MRT（3.68±0.19和4.34±0.14小时）也无差异。肌肉注射和口服给药后，磺胺嘧啶的绝对生物利用度（F）分别为95.41%和86.20%，甲氧苄啶的绝对生物利用度分别为70.02%和79.58%。
