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首页> 外文期刊>The Journal of the South African Veterinary Association >The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs
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The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs

机译：肌内给药对健康犬体内醋酸曲美那嗪的药代动力学

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The pharmacokinetics of diminazene aceturate following intramuscular (i.m.) administration at 4.2 mg/kg was evaluated in 8 healthy German Shepherd dogs. Blood samples were collected at 19 intervals over a period of 21 days. Diminazene plasma concentrations were measured using a validated HPLC method with UV detection and a sensitivity of 25 ng/m . The in vitro and in vivo binding of diminazene to blood elements was additionally determined. Diminazene pharmacokinetics showed a large inter-individual variation after i.m. administration. It had a short absorption half-life (K01-HL of 0.11 + 0.18 h), resulting in a Cmax of 1849 + 268.7 ng/m? at Tmax of 0.37 h and a mean overall elimination half-life (T1/2??) of 5.31 + 3.89 h. A terminal half-life of 27.5 + 25.0 h was measured. At 1 h after i.m. injection, 75% of the diminazene in whole blood was in the plasma fraction. The results of this study indicate that diminazene is rapidly distributed and sequestered into the liver, followed by a slower terminal phase during which diminazene is both redistributed to the peripheral tissues and/or renally excreted. It is recommended that diminazene administered i.m. at 4.2 mg/kg should not be repeated within a 21-day period.
机译：在8只健康的德国牧羊犬中，以4.2mg / kg的肌内（i.m.）给药后，评估了乙酸地米那嗪的药代动力学。在21天的时间内以19个间隔采集血样。使用经过验证的HPLC方法（具有紫外线检测功能）和灵敏度为25 ng / m的二咪唑血浆浓度进行测量。另外确定了地米那嗪与血液元素的体外和体内结合。二咪唑药代动力学在i.m.之后显示很大的个体间差异。行政。它的吸收半衰期很短（K01-HL为0.11 + 0.18 h），Cmax为1849 + 268.7 ng / m2。在Tmax为0.37小时时，平均总消除半衰期（T1 / 2′）为5.31±3.89小时。测量的终末半衰期为27.5 + 25.0 h。凌晨1点注射后，全血中75％的二咪唑存在于血浆中。这项研究的结果表明，地米那嗪迅速分布并被隔离在肝脏中，随后是一个较慢的终末期，在此期间，地米那嗪既重新分布到周围组织和/或肾脏排泄。建议地米那明静脉内给药。 4.2 mg / kg的剂量不应在21天之内重复使用。

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