Bernareggi A, Cavenaghi L, Assandri A
Antimicrob Agents Chemother. 1986 Nov;30(5):733-8. doi: 10.1128/AAC.30.5.733.
The pharmacokinetic profile of [14C]teicoplanin was studied in male Sprague-Dawley rats given a single 10,000-U/kg intravenous dose. The disposition of the antimicrobial activity in the body was estimated by a three-compartment open model. Plasma concentration data were fitted to a three-exponent equation. The profile of total 14C in plasma was similar to that of the microbiological activity. The cumulative recovery of total 14C 5 days after drug administration averaged 76.3% of the administered dose in the urine and 8.7% in the feces. The residual dose remaining in the animal carcasses was 11.1%. Teicoplanin was widely distributed in the body. In almost all organs, the maximum concentration of [14C]teicoplanin was already reached at the first time of killing, which was 0.25 h after the administration of drug. The liver, kidneys, skin, and fat contained most of the residual dose found in the animal carcasses 120 h after administration and behaved as a deep compartment with the adrenal glands and spleen.
在给予单次10000 U/kg静脉注射剂量的雄性Sprague-Dawley大鼠中研究了[14C]替考拉宁的药代动力学特征。通过三室开放模型估计抗菌活性在体内的处置情况。血浆浓度数据拟合为三指数方程。血浆中总14C的曲线与微生物活性的曲线相似。给药后5天，尿液中总14C的累积回收率平均为给药剂量的76.3%，粪便中为8.7%。动物尸体中残留的剂量为11.1%。替考拉宁在体内广泛分布。在几乎所有器官中，[14C]替考拉宁的最大浓度在首次处死时（给药后0.25小时）就已达到。给药120小时后，肝脏、肾脏、皮肤和脂肪含有动物尸体中发现的大部分残留剂量，并与肾上腺和脾脏一起表现为深部隔室。
