| 陈仕云,何勇,于艳英,等.富含铁元素食物对非洛地平片在Beagle犬体内药动学的影响[J].安徽医药,2019,23(9):1737-1740. |
| 富含铁元素食物对非洛地平片在Beagle犬体内药动学的影响 |
| Effects of foods rich in Fe3+ on pharmacokinetics of felodipine tablets in Beagle dogs |
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| DOI：10.3969/j.issn.1009-6469.2019.09.010 |
| 中文关键词: 非洛地平 药代动力学 高效液相色谱-串联质谱法 食物药物相互作用 |
| 英文关键词: Felodipine Pharmacokinetics HPLC-MS/MS Food-drug interaction |
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| 中文摘要: |
| 目的 研究高铁饮食对非洛地平在Beagle犬体内药动学影响。方法 采用随机、开放、单剂量给药、双交叉试验设计。12条健康Beagle犬采用随机数字表法分为两组，每组6条，分别空腹和餐后服用5 mg非洛地平片，给药前后按不同采血时间点采集血样，采用液相色谱-质谱联用(HPLC-MS/MS)法测定血浆中非洛地平浓度，用DAS3.2.8软件计算药动学参数。结果 空腹与餐后主要药动学参数如下:Cmax(12.59±2.17)、(7.13±2.96)ng/mL，tmax(1.25±0.24)、(1.32±0.35)h，t1/2(1.1±0.69)、(1.2±0.72)h，AUC0-12(19.46±5.23)、(11.87±3.85)ng·h-1·mL-1，AUC0-∞(20.69±5.75)、(12.76±4.18)ng·h-1·mL-1。以AUC0-12计算，实验组的相对生物利用度F为(61.0±12.7)%。与对照组相比，实验组Beagle犬的生物利用度偏低，而且达峰浓度也降低，说明食物中Fe3+抑制了非洛地平药物的吸收。结论 高铁饮食可显著降低非洛地平片在Beagle犬体内的吸收程度，但不影响其吸收速度。 |
| 英文摘要: |
| Objective To investigate the effect of ferrum diets on pharmacokinetics of Felodipine in Beagle dogs.Methods A randomized，open-label，single dose and two-way crossover clinical study was conducted.Twelve healthy Beagle dogs were randomly divided into two groups，then 5 mg of felodipine were admitted respectively before and after meal.Blood samples were collected at different time points before and after drug administration.The concentration of felodipine in plasma was determined by HPLC-MS / MS.The pharmacokinetic parameters were calculated by DAS3.2.8.Results The main pharmacokinetic parameters were as follows:Cmax(12.59±2.17) and (7.13±2.96)ng·mL-1，tmax(1.25±0.24) and (1.32±0.35)h，t1/2(1.1±0.69) and (1.2±0.72)h，AUC0-12h(19.46±5.23) and (11.87±3.85) ng·h-1·mL-1，AUC0-∞(20.69±5.75) and (12.76±4.18) ng·h-1·mL-1，Respectively according to AUC0-12h，the relative bioavailability of felodipine in the experimental group was (61.0±12.7)%.Compared to the control group，the bioavailability of felodipine in the experimental group was low and the peak concentration decreased.Conclusion High ferrum Diets can significantly reduce the extent of absorption of felodipine -in Beagle dogs，however，with no influence on the absorption rate of felodipine. |
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