Jasiecka-Mikołajczyk A, Ziółkowski H, Jaroszewski J J
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Warmia and Mazury, Olsztyn, Poland.
J Vet Pharmacol Ther. 2018 Feb;41(1):e22-e29. doi: 10.1111/jvp.12447. Epub 2017 Aug 19.
The aim of this research had been to determine the pharmacokinetics of tigecycline (TIG) in turkey after intravenous (i.v.), intramuscular (i.m.), subcutaneous (s.c.), and oral (p.o.) administration at a dose of 10 mg/kg. TIG concentrations in plasma were determined using high-performance liquid chromatography with tandem mass spectrometry. Mean concentrations of TIG in turkey plasma in the i.v. group were significantly higher than concentrations of this drug obtained after using the other administration routes. No significant differences were demonstrated in respect to the concentrations achieved after i.m. and s.c. administration. The bioavailability of TIG after i.m., s.c., and p.o. administration was 32.59 ± 5.99%, 34.91 ± 9.62%, and 0.97 ± 0.57%, respectively. Values of half-life in the elimination phase were 23.49 ± 6.51 hr, 25.42 ± 4.42 hr, and 26.62 ± 5.19 hr in i.v., i.m., and s.c. groups, respectively, values of mean residence time were 7.92 ± 1.41 hr, 19.62 ± 2.82 hr, and 17.55 ± 2.59 hr in i.v., i.m., and s.c. groups, respectively, whereas the volume of distribution was 14.85 ± 5.71 L/kg, 14.68 ± 2.56 L/kg, and 15.37 ± 3.00 L/kg in i.v., i.m., and s.c. groups, respectively. Because TIG is not absorbed from the gastrointestinal tract in turkeys to a clinically significant degree, this drug given p.o. could find application in commercial turkey farms only to treat gastrointestinal tract infections.
本研究的目的是确定替加环素(TIG)以10mg/kg的剂量经静脉注射(i.v.)、肌肉注射(i.m.)、皮下注射(s.c.)和口服(p.o.)给药后在火鸡体内的药代动力学。使用高效液相色谱串联质谱法测定血浆中的替加环素浓度。静脉注射组火鸡血浆中替加环素的平均浓度显著高于其他给药途径后的该药物浓度。肌肉注射和皮下注射后所达到的浓度方面未显示出显著差异。替加环素经肌肉注射、皮下注射和口服给药后的生物利用度分别为32.59±5.99%、34.91±9.62%和0.97±0.57%。消除相的半衰期值在静脉注射、肌肉注射和皮下注射组中分别为23.49±6.51小时、25.42±4.42小时和26.62±5.19小时,平均驻留时间值在静脉注射、肌肉注射和皮下注射组中分别为7.92±1.41小时、19.62±2.82小时和17.55±2.59小时,而分布容积在静脉注射、肌肉注射和皮下注射组中分别为14.85±5.71L/kg、14.68±2.56L/kg和15.37±3.00L/kg。由于替加环素在火鸡胃肠道中吸收程度未达到具有临床意义的水平,口服该药物仅可在商业火鸡养殖场用于治疗胃肠道感染。