Pharmacokinetics and metabolism of ketoprofen after intravenous and intramuscular administration in camels
Pharmacokinetics and metabolism of ketoprofen after intravenous and intramuscular administration in camels
复制标题
DOI：
10.1046/j.1365-2885.1999.00193.x
复制
发表时间：
1999-04-01
影响因子：
1.3
通讯作者：
Lambert, M
中科院分区：
文献类型：
--
作者：
Alkatheeri, NA;Wasfi, IA;Lambert, M
使用气相色谱/质谱 (GC/MS) 对五只骆驼 (Camelus dromedarius) 进行静脉内 (i.v.) 和肌内 (i.m.) 剂量 2.0 mg/kg 体重后测定酮洛芬的药代动力学。静脉注射后获得的数据（中位数和范围）给药如下：消除半衰期（t（1/2β））为4.16（2.65-4.29）h，稳态分布容积（V-ss）为130.2（103.4-165.3）mL/kg，分布容积（面积法）（Vd（area））为321.5（211.4-371.0）mL/kg，全身清除率(CI) 为 1.00 (0.88-1.08) mL/min.kg，肾清除率为 0.01 (0.003-0.033) mL/min.kg。肌内给药后，药物被迅速吸收，1.50（1.00-2.00）小时时血清峰值浓度为12.2（4.80-14.4）μg/mL。酮洛芬的全身可用性是完全的。表观半衰期为 3.28 (2.56-4.14) h。在电子轰击 (EI) 和化学电离 (CI) 扫描模式下通过 (GC/MS) 鉴定了酮洛芬的羟基化代谢物。静脉注射（i.v.）剂量为 3.0 mg/kg 体重后，尿液中酮洛芬和羟基酮洛芬的检测时间分别为 24.00 和 70.00 小时。 20 μg/mL 酮洛芬的血清蛋白结合广泛； （99.1 +/- 0.15%）。
The pharmacokinetics of ketoprofen were determined after an intravenous (i.v.) and intramuscular (i.m.) dose of 2.0 mg/kg body weight in five camels (Camelus dromedarius) using gas chromatography/mass spectrometry (GC/MS). The data obtained (median and range) following i.v. administration was as follows: the elimination half-life (t(1/2 beta)) was 4.16 (2.65-4.29) h, the steady state volume of distribution (V-ss) was 130.2 (103.4-165.3) mL/kg, volume of distribution (area method) (Vd(area)) was 321.5 (211.4-371.0) mL/kg, total body clearance (CI) was 1.00 (0.88-1.08) mL/min.kg and renal clearance was 0.01 (0.003-0.033) mL/min.kg. Following i.m, administration, the drug was rapidly absorbed with peak serum concentration of 12.2 (4.80-14.4) mu g/mL at 1.50 (1.00-2.00) h. The systemic availability of ketoprofen was complete. The apparent half-life was 3.28 (2.56-4.14) h. A hydroxylated metabolite of ketoprofen was identified by (GC/MS) under electron impact (EI) and chemical ionization (CI) scan modes. The detection times for ketoprofen and hydroxy ketoprofen in urine after an intravenous (i.v.) dose of 3.0 mg/kg body weight was 24.00 and 70.00 h, respectively. Serum protein binding of ketoprofen at 20 mu g/mL was extensive; (99.1 +/- 0.15%).