利托那韦对舒芬太尼在家兔体内药动学的影响
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篇名: 利托那韦对舒芬太尼在家兔体内药动学的影响
TITLE:
摘要: 目的:研究利托那韦对舒芬太尼在家兔体内药动学的影响。方法:将24只家兔随机分为两组,每组12只,实验组ig利托那韦10 mg/kg,5 min后iv舒芬太尼2 μg/kg;对照组ig同等容量生理盐水后iv舒芬太尼2 μg/kg。分别于ig前和iv后0、0.25、0.5、1、2、3、4、6、8、10、12、14、24 h自兔耳中央动脉取血0.3 ml,采用液相色谱-串联质谱法(LC-MS/MS)测定血浆中舒芬太尼的浓度,DAS2.0软件计算药动学参数。结果:两组家兔体内舒芬太尼药动学过程均符合二室模型;对照组与实验组家兔体内舒芬太尼的药动学参数t1/2分别为(22.0±6.59)、(26.4±1.41) h,MRT0-24 h分别为(8.6±2.08)、(12.1±3.70) h,AUC0-∞分别为(16.1±5.17)、(38.1±12.95) mg·h/L;两组间MRT0-24 h、AUC0-∞差异均有统计学意义(P<0.05)。结论:利托那韦可提升舒芬太尼在家兔体内的分布,延长舒芬太尼滞留时间。
ABSTRACT: OBJECTIVE: To study the effects of ritonavir on the pharmacokinetics of sufentanil in rabbits. METHODS: 24 rabbits were randomly divided into 2 groups, with 12 rabbits in each group. Trial group was given ritonavir 10 mg/kg by gavage and then injected sufentanil 2 μg/kg intravenously after 5 min. Control group was given equal volume of normal saline by gavage and then injected sufentanil 2 μg/kg intravenously. Arterial blood samples 0.3 ml were taken before gavage and 0, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 14, 24 h after intravenous administration. The plasma concentrations of sufentanil were determined by LC-MS/MS, and DAS 2.0 software was adopted to calculate pharmacokinetic parameters. RESULTS: The pharmacokinetic change of sufentanil conformed to two-compartment model in 2 groups. The pharmacokinetic parameters of sufentanil in control group vs. trial group were that t1/2 were (22.0±6.59) and (26.4±1.41) h; MRT0-24 h were (8.6±2.08) and (12.1±3.70) h; AUC0-∞ were (16.1±5.17) and (38.1±12.95) mg·h/L, respectively. There was statistical significance in MRT0-24 h and AUC0-∞ between 2 groups (P<0.05). CONCLUSIONS: Ritonavir can elevate distribution of sufentanil in rabbits, and prolong retention time of sufentanil.
期刊: 2016年第27卷第22期
作者: 张雪松,张莹,张雪岩
AUTHORS: ZHANG Xuesong,ZHANG Ying,ZHANG Xueyan
关键字: 舒芬太尼;利托那韦;药动学;液相色谱-串联质谱法;药物相互作用;家兔
KEYWORDS: Sufentanil; Ritonavir; Pharmacokinetics; LC-MS/MS; Drug interactions; Rabbits
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