5种土霉素注射液在山羊体内的药动学比较

Comparative Pharmacokinetics of Various Oxytetracycline Injection in Goats

为了研究5种土霉素注射液肌肉注射后在山羊体内的药动学特征,给临床用药及其研究提供参考依据,选取30只山羊为靶动物,将其随机分为5组,分别注射不同品种的土霉素注射液(10%A、B、C)和(20%D、E),然后采用高效液相色谱法对山羊体内的土霉素含量进行测定,3 P97软件拟合血药浓度-时间曲线,计算药动学参数。结果显示,5种土霉素注射液均符合一级吸收二室模型,10%A、10%B、10%C、20%D和20%E主要药动学参数分别为:消除半衰期(t1/2β)为7.13μg/mL、6.62μg/mL、6.97μg/mL、21.16μg/mL和27.32μg/mL;达峰浓度(Cmax)为(2.71±0.37)μg/mL、(3.11±0.81)μg/mL、(3.60±0.83)μg/mL、(5.52±0.53)μg/mL和(4.69±1.20)μg/mL;达峰时间(Tmax)为(2.08±1.52)h、(2.17±2.2)h、(3.05±2.30)h、(2.05±0.80)h和(2.80±1.01)h;药时曲线下面积(AUC)为(61.41±20.94)h·μg/mL、(50.34±8.74)h·μg/mL、(58.57±7.31)h·μg/mL、(124.23±7.23)h·μg/mL和(109.47±22.35)h·μg/mL。表明高浓度(20%)的土霉素注射液具有半衰期长,峰浓度高,药时曲线下面积大等特点,与低浓度(10%)土霉素注射液之间差异显著,可能与有机溶媒的用量和种类有关,此结论为临床合理使用剂型提供依据和指导。

To study the pharmacokinetics of five kinds of oxytetracycline injection on goats and to provide reference for clinical guidance and research.Thirty goats were selected as target animals and randomly divided into five groups,which received different doses of oxytetracycline injection(10%A、B、C)and(20%D、E).And then use high performance liquid chromatography to determine oxytetracycline content in goats,3P97 to determine plasma concentration-time curve,calculate the pharmacokinetic parameters.Results showed that the five oxytetracycline injections were in accordance with the first-order absorption two-compartment model.The main pharmacokinetic parameters of 10%A、10%B、10%C、20%D and 20%E were as follows:t1/2βwas 7.13μg/mL,6.62μg/mL,6.97μg/mL,21.16μg/mL and 27.32μg/mL;Cmax was(2.71±0.37)μg/mL,(3.11±0.81)μg/mL,(3.60±0.83)μg/mL,(5.52±0.53)μg/mL and(4.69±1.20)μg/mL;Tmax was(2.08±1.52)h,(2.17±2.2)h,(3.05±2.30)h,(2.05±0.80)h and(2.80±1.01)h;AUC was(61.41±20.94)h·μg/mL,(50.34±8.74)h·μg/mL,(58.57±7.31)h·μg/mL,(124.23±7.23)h·μg/mL和(109.47±22.35)h·μg/mL.There is no significant difference in the pharmacokinetic parameters of oxytetracycline injection at same concentrations,while the pharmacokinetic parameters of oxytetracycline injection at different concentrations have significant differences.This conclusion provides basis and guidance for rational use of dosage forms in clinical practice.