Moeremans Ilse, Devreese Mathias, De Baere Siegrid, Croubels Siska, Hermans Katleen
Department of Pathology, Bacteriology and Avian Diseases, Division of Poultry, Exotic Companion Animals, Wildlife and Experimental Animals, Faculty of Veterinary Medicine, Ghent University, Merelbeke, Belgium.
Department of Pharmacology, Toxicology and Biochemistry, Faculty of Veterinary Medicine, Ghent University, Merelbeke, Belgium.
Vet Anaesth Analg. 2019 Jul;46(4):548-555. doi: 10.1016/j.vaa.2018.11.011. Epub 2019 Mar 23.
To investigate the pharmacokinetics and absolute oral bioavailability of meloxicam in guinea pigs.
Prospective crossover study.
A group of six healthy male Dunkin Hartley guinea pigs.
A single dose of meloxicam (1.5 mg kg) was administered orally and intravenously (IV) to six healthy male guinea pigs. A wash-out period of 48 hours was taken into account between administrations (oral and IV) in the same animal. Blood was sampled through a central venous catheter before administration (t = 0 hours) and at 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 20, 24 and 28 hours post administration. After centrifugation, plasma concentrations of meloxicam were measured by high-performance liquid chromatography with UV detection, and pharmacokinetic parameters were calculated using noncompartmental analysis.
Meloxicam in guinea pigs exhibited a moderate absorption rate after oral dosing (time to maximal plasma concentration 3.7 ± 1.7 hours) and maximal plasma concentration was 0.92 ± 0.30 μg mL. After IV administration, total body clearance and volume of distribution were 0.13 ± 0.04 and 0.72 ± 0.36 L kg, respectively. Terminal half-life was 3.7 ± 0.7 hours and 3.5 ± 1.1 hours after IV and oral administration, respectively. Body extraction ratio was 0.0087 and mean absorption time was 3.8 ± 1.7 hours. The absolute oral bioavailability was 0.54 ± 0.14 in unfasted guinea pigs.
This study reported the pharmacokinetics of meloxicam in guinea pigs. Studies concerning efficacy and safety are the next step towards a rational use of this drug in guinea pigs.
研究美洛昔康在豚鼠体内的药代动力学及绝对口服生物利用度。
前瞻性交叉研究。
一组6只健康雄性邓金·哈特利豚鼠。
对6只健康雄性豚鼠分别口服和静脉注射单剂量美洛昔康（1.5 mg/kg）。同一动物在口服和静脉注射给药之间设置48小时的洗脱期。给药前（t = 0小时）以及给药后0.5、1、2、3、4、6、8、10、12、16、20、24和28小时通过中心静脉导管采集血液。离心后，采用高效液相色谱-紫外检测法测定血浆中美洛昔康的浓度，并使用非房室分析法计算药代动力学参数。
豚鼠口服美洛昔康后吸收速率适中（达最大血浆浓度时间为3.7±1.7小时），最大血浆浓度为0.92±0.30μg/mL。静脉注射后，总体清除率和分布容积分别为0.13±0.04和0.72±0.36 L/kg。静脉注射和口服给药后的末端半衰期分别为3.7±0.7小时和3.5±1.1小时。机体提取率为0.0087，平均吸收时间为3.8±1.7小时。非禁食豚鼠的绝对口服生物利用度为0.54±0.14。
本研究报道了美洛昔康在豚鼠体内的药代动力学。关于其疗效和安全性的研究是在豚鼠中合理使用该药物的下一步。
