Pharmacokinetics of single‐dose sildenafil administered orally in clinically healthy dogs: Effect of feeding and dose proportionality
Pharmacokinetics of single‐dose sildenafil administered orally in clinically healthy dogs: Effect of feeding and dose proportionality
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临床健康犬口服单剂量西地那非的药代动力学：喂养和剂量比例的影响
DOI：
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发表时间：
2018
影响因子：
1.3
通讯作者：
N. Takemura
中科院分区：
文献类型：
--
作者：
R. Akabane;T. Sato;A. Sakatani;Y. Miyagawa;H. Tazaki;N. Takemura
有关西地那非在狗体内的药代动力学的基本信息很少。本研究旨在描述口服西地那非的药代动力学特性，并确定喂养和剂量比例的影响。采用6只狗的交叉试验研究了饲喂对西地那非（1 mg/kg）药代动力学的影响。此外，在5只狗的禁食状态下，评估了西地那非1-4 mg/kg的剂量比例。采用高效液相色谱法测定西地那非的血药浓度，采用非区室分析计算药代动力学参数。在所有研究中，西地那非耐受良好。进料显著降低了外推曲线下的面积（AUCinf）和最大血浆浓度（Cmax）。消除半衰期（T1/2）在禁食和喂食状态之间没有差异。对于剂量比例，通过功率模型分析检测到1-4 mg/kg剂量下AUCinf和Cmax的非比例增加。
Basic information related to the pharmacokinetics of sildenafil in dogs is scarce. This study aimed to describe the pharmacokinetic properties of oral sildenafil and determine the effect of feeding and dose proportionality. The effect of feeding on pharmacokinetics of sildenafil (1 mg/kg) was investigated using a crossover study with six dogs. In addition, the dose proportionality of sildenafil ranging 1-4 mg/kg was evaluated using five dogs in the fasted states. The plasma concentrations of sildenafil were determined using high-performance liquid chromatography, and pharmacokinetic parameters were calculated using a noncompartmental analysis. Sildenafil administrations were well tolerated in all studies. Feeding reduced the area under the curve extrapolated to infinity (AUCinf ) and the maximum plasma concentration (Cmax ) significantly. The elimination half-life (T1/2 ) did not differ between the fasted and the fed states. For dose proportionality, nonproportional increases in AUCinf and Cmax at 1-4 mg/kg doses were detected by a power model analysis.
DOI：
10.1016/j.bbrc.2005.06.183
发表时间：
2005-09-02
影响因子：
3.1
作者：
Corbin, JD;Beasley, A;Francis, SH
通讯作者：
Francis, SH