健康兔子口服和静脉注射 D-ribose 后的药代动力学评价。

IF 3.1 Q2 PHARMACOLOGY & PHARMACY Clinical Pharmacology : Advances and Applications Pub Date : 2018-06-12 eCollection Date: 2018-01-01 DOI:10.2147/CPAA.S167150
Karem H Alzoubi, Zuhair Bani Ismail, Mohamed K Al-Essa, Osama Y Alshogran, Reem F Abutayeh, Nareman Abu-Baker
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摘要

简介:本研究探讨了健康兔子静脉注射(IV)和口服 D-核糖后的药代动力学:静脉注射 420 毫克/千克(4 只)或 840 毫克/千克(6 只)剂量的 D-核糖,或口服 420 毫克/千克(3 只)或 840 毫克/千克(3 只)剂量的 D-核糖。在给药后 210 分钟内的不同时间点采集血清。静脉注射后还收集了尿液。使用 Kinetica 软件根据药物浓度-时间数据确定药代动力学参数:结果:研究结果表明,D-核糖具有剂量依赖性动力学特征。静脉注射剂量增加一倍,AUCtotal 显著增加三倍,而清除率降低 44%。剂量增加时,半衰期延长了 1.7 倍。口服给药也观察到类似的非显著趋势。D-ribose 被迅速吸收(Tmax=36-44 分钟),并迅速从血浆中消失(在结论时间内):总之,D-核糖显示出剂量依赖性的动力学特征,其参数随剂量水平而变化。在低剂量时,D-核糖清除率似乎遵循一阶动力学。此后,消除系统达到饱和,继续快速消除。尿液只能部分恢复,这可能与戊糖的多种代谢途径有关。
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Pharmacokinetic evaluation of D-ribose after oral and intravenous administration to healthy rabbits.

Introduction: This study explored D-ribose pharmacokinetics after intravenous (IV) and oral administration to healthy rabbits.

Materials and methods: D-ribose was administered once as 420 mg/kg (N=4) or 840 mg/kg (N=6) dose intravenously, or as an oral dose of 420 mg/kg (N=3) or 840 mg/kg (N=3). Serum was obtained at various time points, up to 210 minutes after administration. Urine was also collected after IV administration. Pharmacokinetic parameters were determined from drug concentration-time data using Kinetica software.

Results: The findings showed that D-ribose follows a dose-dependent kinetic profile. With doubling the IV dose, AUCtotal was significantly increased by threefold, while the clearance was decreased by 44%. The half-life was 1.7-fold longer at the higher dose. Similar nonsignificant trends were also observed at oral administration. D-ribose was rapidly absorbed (Tmax=36-44 minutes) and rapidly disappeared from plasma (within <140 minutes). Additionally, D-ribose was partially (18-37.5%) recovered from urine.

Conclusion: Collectively, D-ribose showed a dose-dependent kinetic profile, where parameters change according to dosing levels. D-ribose clearance seems to follow first-order kinetics at low dose. Thereafter, elimination systems are saturated, and elimination continues in a fast manner. Urine recovery was partial, which could be attributed to the several metabolic pathways that pentose can undergo.

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来源期刊
CiteScore
4.60
自引率
0.00%
发文量
14
审稿时长
16 weeks
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