泰地罗新注射液在藏系羊体内的药物代谢动力学研究
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摘要
为研究泰地罗新注射液在藏系羊体内的药物动力学特征,了解其在藏系羊体内的吸收、分布、转化及排泄规律,为泰地罗新注射液的临床合理用药提供参考,选取8只藏系羊,泰地罗新4 mg/kg体重单剂量肌内注射给药,不同时间点采集藏系羊血液,利用高效液相色谱法测定血浆中药物浓度。结果显示:给药后泰地罗新在藏系羊体内的药-时曲线符合有吸收三室开放模型,其主要药动学参数为:达峰时间(T_(max))为(0.723±0.186)h,最高血药浓度(C_(max))为(0.769±0.231)μg/m L,半衰期(t_(1/2))为(86.525±10.547)h,表观分布容积(Vd)为(15.298±2.564)m L/kg,药时曲线下面积(AUC)为(28.738±3.452)μg·h/m L。结果表明:泰地罗新注射给药后,在藏系羊体内吸收迅速,消除较为缓慢。
The experiment mainly focused on studying the pharmacokinetic characteristics of tildipirosin injection in Tibetan sheep to provide the guidance for clinical rational use of tildipirosin injection in sheep. Eight Tibetan sheep were selected and administrated with intramuscular injection of tildipirosin with single dose and the blood samples were collected at different time points. The drug concentrations in plasma were determined by HPLC. The results showed that the pharmacokinetic behavior of tildipirosin in the Tibetan sheep conformed to the curve in the three compartment open model. The main pharmacokinetic parameters were as follows: The T_(max),C_(max),t_(1/2),Vd and AUC were( 0. 723±0. 186) h,( 0. 769±0. 231) g/m L,( 86. 525±10. 547) h,( 15. 298±2. 564) m L/kg and( 28. 738±3. 452) μg·h/m L,respectively. These results indicated that tildipirosin injected could be quickly absorbed but slowly eliminated in Tibetan sheep.
The experiment mainly focused on studying the pharmacokinetic characteristics of tildipirosin injection in Tibetan sheep to provide the guidance for clinical rational use of tildipirosin injection in sheep. Eight Tibetan sheep were selected and administrated with intramuscular injection of tildipirosin with single dose and the blood samples were collected at different time points. The drug concentrations in plasma were determined by HPLC. The results showed that the pharmacokinetic behavior of tildipirosin in the Tibetan sheep conformed to the curve in the three compartment open model. The main pharmacokinetic parameters were as follows: The T_(max),C_(max),t_(1/2),Vd and AUC were( 0. 723±0. 186) h,( 0. 769±0. 231) g/m L,( 86. 525±10. 547) h,( 15. 298±2. 564) m L/kg and( 28. 738±3. 452) μg·h/m L,respectively. These results indicated that tildipirosin injected could be quickly absorbed but slowly eliminated in Tibetan sheep.
引文
[1]Jacob P,Niels M A,Ralf W,et al.Visualizing the 16-membered ring macrolides tidipirosin and tilmicosin bound to their ribosomal site[J].ACS Chem Biol,2012,7(8):1351-1355.
[2]李伟岭,杨芳.泰地罗新研究进展[J].中国兽药杂志,2012,46(10):50-53.
[3]Watts J L,Sweeney M T.Antimierobial resistance in bovine respiratory disease pathogens:measures,trends,and impact on eficacy[J].Vet Clin North Am Food Anim Pract,2010,26(1):79-88.
[4]Miyake T,Takita T,Hamada M,et al.16-membered ring macrolide antibioticsand the treatment or prophylaxis of pasteurellosis of mammalian livestock orpoultry using the same as an active ingredient:U.S.Patent 6,514,946[P].2003-2-4.
[5]Menge M,Rose M,Bohland C et al.Pharmacokinetics of tildipirosin in bovine plasma,lung tissue,and bronchial fluid(from live,nonanesthetizedcattle)[J].J Vet Pharmacol Ther,2012,35(6):550-559.
[6]Rose M,Menge M,Bohland,C et al.Pharmacokinetics of tildipirosin in porcine plasma,lung tissue,and bronchial fluid and effects of test conditions on in vitro activity against reference strains and field isolates of Actinobacillus pleuropneumoniae[J].J Vet Pharmacol Ther,2013,36(2):140-153.
[7]廖远军.泰地罗新注射液在猪体内的药代动力学研究[D].长春:吉林大学,2015.
[2]李伟岭,杨芳.泰地罗新研究进展[J].中国兽药杂志,2012,46(10):50-53.
[3]Watts J L,Sweeney M T.Antimierobial resistance in bovine respiratory disease pathogens:measures,trends,and impact on eficacy[J].Vet Clin North Am Food Anim Pract,2010,26(1):79-88.
[4]Miyake T,Takita T,Hamada M,et al.16-membered ring macrolide antibioticsand the treatment or prophylaxis of pasteurellosis of mammalian livestock orpoultry using the same as an active ingredient:U.S.Patent 6,514,946[P].2003-2-4.
[5]Menge M,Rose M,Bohland C et al.Pharmacokinetics of tildipirosin in bovine plasma,lung tissue,and bronchial fluid(from live,nonanesthetizedcattle)[J].J Vet Pharmacol Ther,2012,35(6):550-559.
[6]Rose M,Menge M,Bohland,C et al.Pharmacokinetics of tildipirosin in porcine plasma,lung tissue,and bronchial fluid and effects of test conditions on in vitro activity against reference strains and field isolates of Actinobacillus pleuropneumoniae[J].J Vet Pharmacol Ther,2013,36(2):140-153.
[7]廖远军.泰地罗新注射液在猪体内的药代动力学研究[D].长春:吉林大学,2015.