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首页> 外文期刊>薬物動態 >Pharmacokinetic Studies of [~14C]Urea (2); Absorption, Distribution, Metabolism and Excretion after Administration of [~14C] Urea in Non-Fasted Rats
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Pharmacokinetic Studies of [~14C]Urea (2); Absorption, Distribution, Metabolism and Excretion after Administration of [~14C] Urea in Non-Fasted Rats

机译：[〜14c]尿素的药代动力学研究（2）; 在非禁食大鼠施用[〜14C]尿素后的吸收，分布，代谢和排泄

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Absorption, distribution, metabolism and excretion after a single intravenous and oral administration of [~14C] urea at a main dose of 2 mg/kg were investigated in non-fasted rats. Comparison of the pharmackinetics in rats between under non-fasted and fasted conditions was also investigated.1. The radioactivity levels in plasma were decreased biphasically with t_(1/2#alpha#) of 2-3 hr and t_(1/2#beta#) of 6-11 hr, irrespective of administration routes and doses. After oral administration at odes of 2,62.5,250 and 1000 mg/k, the C_max and AUC_(0-infinity) were virtually proportional to the administered doses, suggesting linear-pharmacokinetics within the examined dose range.2. The radioactivity levels in plasma and tissues reached C_max at 0.5-1 hr after oral dministration. The concentration in the kidney, which was 2.4 times as high as that in plasma, was the highest in the examined tissues. The concentrations in other tissues were similar to, or lower than the plasma concentration. After the C_max, the concentrations in most tissues decreased in almost parallel with the plasma concentration.3. In plasma at 1 hr after oral administration, only the unchanged drug was observed in the plasma radioactivity. On the other hand, at 8 hr, about 70% and 30% of the plasma radioactivity wre unchanged drug and unknown components, respectively. In urine for 24 hr after dosing, only the unchanged drug was also observed, irrespective of administration routes.4. Within 96 hr, 73.1%,1.6% and 20.1% of dosed radioactivity were excreted in urine, feces and expired air after intravenous administration, and 54.0%, 1.0% and 42.9% after oral administration, respectively. The bioavailability estimated from the ratio of urinary excretion of urea after oral administration to that after intravenous administration was 74%.Feeding condition in rats enhanced metabolism / decomposition of urea and influenced its plasma concentration-time profiles and excretion profile.
机译：在非捕获大鼠中研究了在单个静脉内和口服尿尿嘧啶中的吸收，分布，代谢和排泄后的[〜14c]尿素。还研究了在非禁食和禁食条件下的大鼠中药物的比较.1。无论给药路线和剂量如何，血浆中的血浆中的放射性水平与2-3小时和T_（1/2＃β＃）的T_（1/2＃α＃）减小。在2,62.5,250和1000mg / k的ODES中口服给药后，C_max和Auc_（0-无穷大）几乎与给药剂量成比例，表明在检查剂量范围内的线性药代动力学。血浆和组织中的放射性水平在口服Dministration后在0.5-1小时达到C_max。肾脏中的浓度为血浆中的2.4倍，是检查组织中最高的。其他组织中的浓度类似于或低于等离子体浓度。在C_max之后，大多数组织中的浓度几乎与血浆浓度几乎平行降低。在口服给药后1小时的血浆中，在血浆放射性中仅观察到不变的药物。另一方面，在8小时，分别在8小时，血浆放射性的约70％和30％，分别不变的药物和未知的组分。在给药后24小时尿液中，不管给药途径，也只观察到不变的药物.4。在96小时内，73.1％，1.6％和20.1％的剂量放射性分别在静脉内给药后的尿液，粪便和过期空气中排出，分别在口服给药后的54.0％，1.0％和42.9％。在口服给药后尿素排泄比率估计的生物利用度在静脉内给药后的尿液中的比例为74％。大鼠中的再现条件增强了尿素的代谢/分解，影响了其血浆浓度 - 时间谱和排泄谱。

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