大鼠静脉给药后阿霉素的药动学。

R. Nwankwoala, O. Georgewill, U. Georgewill
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引用次数: 6

摘要

用雄性Wister大鼠研究了阿霉素在睾丸、心脏和血浆中的药动学。对照组接受0。阿霉素治疗组大鼠静脉滴注阿霉素20mg/kg。第二组给予阿霉素1mg/kg,同时静脉注射。分别于1、3、12、24小时处死,取睾丸、心脏。血浆是从血液中提取出来的。采用荧光法定量测定组织和血浆中阿霉素的含量。药物在组织和血浆中的半衰期由阿霉素浓度(ug/g)与时间的对数曲线图计算。药代动力学研究中使用的两种剂量在心脏和血浆中的分布模式显示药物浓度随时间呈指数下降。另一方面,在睾丸中,在该器官中药物水平最初下降后,药物水平随着时间的推移而升高。睾丸积累阿霉素的这种能力使其极易受到阿霉素的致命影响,从而解释了观察到的药物引起的睾丸毒性。
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Pharmacokinetics Of Adriamycin After Intravenous Administration In Rat.
Pharmacokinetics of adriamycin in the rat testis, heart and plasma was Investigated using male Wister rats. The control group received 0. 9%saline Given I.V. One group of adriamycin treated rats received 20mg/kg adriamycin administered intravenously. The Second group received1mg/kg adriamycin also given I.V. Thereafter, the animals weresacrificed 1,3,12 and 24 hours and the testes, and hearts were removed.The plasma was recovered from the blood. Using fluorimetric method, the amount of adriamycin in the tissues and plasma was quantitated. The Half life of the drug in the tissues and plasma was calculated from the Graph of log adriamycin concentration (ug/g) vs. time. The pattern of distribution in the heart and plasma at the two doses used in the pharmacokinetic studies revealed an exponential fall in drug concentration with time. In the testis on the other hand, after the initial drop on the level of the drug in this organ, the level of the drug was elevated with time. This ability of the testis to accumulate adriamycin renders it highly susceptible to the lethal effects of adriamycin And thus accounts for the observed drug induced testicular toxicity.
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