联合应用氨氯地平对缬沙坦在大鼠体内药动学的影响研究

许金红,宋建国*,李永霞

中国药学杂志 ›› 2014, Vol. 49 ›› Issue (14) : 1243-1246.

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中国药学杂志 ›› 2014, Vol. 49 ›› Issue (14) : 1243-1246. DOI: 10.11669/cpj.2014.14.016
论著

联合应用氨氯地平对缬沙坦在大鼠体内药动学的影响研究

  • 许金红1,宋建国2*,李永霞1
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Effects of Combination of Amlodipine and Valsartan on in Vivo Pharmacokinetics of Valsartan in Rats

  • XU Jin-hong1,SONG Jian-guo2*,LI Yong-xia1
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摘要

目的 研究氨氯地平与缬沙坦联合用药对缬沙坦在大鼠体内药动学的变化,探讨联合用药对降压作用的影响,为临床合理用药提供参考。方法 12只SD雄性大鼠随机分成2组,分别灌胃给予缬沙坦(16 mg·kg-1)及倍博特(含缬沙坦16 mg·kg-1,氨氯地平1 mg·kg-1),于给药前0 h及给药后0.33、0.67、1、2、4、8、12及24 h眼内眦静脉取血。HPLC紫外法测定血浆缬沙坦浓度。结果 缬沙坦在大鼠体内ρ-t曲线呈一室模型,服药后2 h达血药峰值,联用氨氯地平后血药浓度增高,ρmax、AUC显著增大(P<0.05),VdCL显著降低(P<0.01)。结论 缬沙坦与氨氯地平联用,可使缬沙坦血药浓度增高,AUC增大,CLVd降低,比单独用药时降压作用更高。

Abstract

OBJECTIVE To study the phamackinetics of amlodipine and valsartan for valsartan in rats, and to investigate the antihypertensive effect of combined treatment.METHODS Twelve male SD rats were divided into two groups.The valsartan (16 mg穔g-1)and Exforge(containing valsartan 16 mg穔g-1,amlodipine 1 mg穔g-1) were given by using stomach tube respectively to rats.Blood samples were taken for detecting plasma concentration before dosing and at 0, 0.33, 0.67, 1, 2, 4, 8, 12 and 24 h after a single intrauenous administration.A HPLC method was used to assay the valsartan concentration in plasma.RESULTS The plasma concentration-time course showed one compartment model of valsartan plasma in rats, with the increased dose after 2 h,Cmax and AUC has a significant increase(P<0.05),while Vd and CL has a significant decrease(P<0.01).CONCLUSION Combination of valsartan and amlodipine could increase the plasma concentration and AUC,while decrease CL and Vd, higher than single antihypertensive effect.

关键词

缬沙坦 / 氨氯地平 / 药动学

Key words

valsartan / amlodipine / pharmacokinetics

引用本文

导出引用
许金红,宋建国*,李永霞. 联合应用氨氯地平对缬沙坦在大鼠体内药动学的影响研究[J]. 中国药学杂志, 2014, 49(14): 1243-1246 https://doi.org/10.11669/cpj.2014.14.016
XU Jin-hong,SONG Jian-guo*,LI Yong-xia. Effects of Combination of Amlodipine and Valsartan on in Vivo Pharmacokinetics of Valsartan in Rats[J]. Chinese Pharmaceutical Journal, 2014, 49(14): 1243-1246 https://doi.org/10.11669/cpj.2014.14.016
中图分类号: R285   

参考文献

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