高原环境对大鼠体内呋塞米和醋甲唑胺血浆蛋白结合率的影响

发布时间：2018-03-17 09:05

本文选题：急进高原　切入点：蛋白结合率　出处：《中国医院药学杂志》2015年20期 　论文类型：期刊论文

【摘要】：目的:对平原与高原组大鼠体内呋塞米和醋甲唑胺的血浆蛋白结合率差异进行比较。方法:Wistar大鼠于平原地区禁食12 h后分别将呋塞米0.001 7 g、醋甲唑胺0.004 9 g片剂灌胃给药,清洗期后,急进高原灌胃给药。给药后0.66、2、4 h由眼眶后静脉丛取血(呋塞米),醋甲唑胺采血时间点为0.66、2、8 h,采用超滤法测定呋塞米和醋甲唑胺血浆蛋白结合率,LCMS/MS方法测定呋塞米和醋甲唑胺血浓度。结果:急进高原后呋塞米蛋白结合率略有增高,但无显著性差异。而醋甲唑胺组蛋白结合率增高明显,平原组和急进高原组血浆蛋白结合率值分别为(21.52±1.22)%、(73.98±2.09)%。结论:本研究发现急进高原后大鼠体内呋塞米和醋甲唑胺血浆蛋白结合率变化不同,血浆蛋白结合率的变化可能会影响药物药动学特征。
[Abstract]:Objective: to compare the difference of plasma protein binding rates of furosemide and methazolamide between plain and high altitude rats. Methods: after fasting in plain area for 12 hours, rats were given furosemide 0.001 g and methazolamide 0.004 9 g respectively. After the cleaning period, The blood was collected from the posterior orbital venous plexus (furosemide, mezolamide) for 8 h. The plasma protein binding rate of furosemide and mezolamine was determined by ultrafiltration method and the LCMS- / MS method was used to determine furosemide and furosemide plasma protein binding rate. Results: the binding rate of furosemide protein increased slightly after rapid entry into high altitude. However, there was no significant difference between the two groups. The plasma protein binding rates in plain group and acute plateau group were 21.52 卤1.22 and 73.98 卤2.09, respectively. Conclusion: the changes of plasma protein binding rates of furosemide and oxazolamine in rats after rapid entry into high altitude were different. Changes in plasma protein binding rates may affect pharmacokinetic characteristics.
【作者单位】：全军高原损伤防治重点实验室;兰州军区兰州总医院药材科;
【基金】：国家自然科学基金项目(编号81403004) 国家科技部重大专项资助项目(编号2008ZXJ09014-010)
【分类号】：R965

【参考文献】