| 引用本文: | 林淑,潘佩佩,胡国新.格列吡嗪和格列本脲对氯沙坦药动学的影响[J].中国现代应用药学,2017,34(1):85-88. |
| LIN Shu,PAN Peipei,HU Guoxin.Effect of Glipizide and Glibenclamide on the Pharmacokinetics of Losartan[J].Chin J Mod Appl Pharm(中国现代应用药学),2017,34(1):85-88. |
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| 摘要: |
| 目的 研究格列吡嗪和格列本脲对氯沙坦在大鼠体内药动学的影响。方法 将15只大鼠随机分成对照组、格列吡嗪组和格列本脲组，分别灌胃给予0.5% CMC、10 mg·kg-1格列吡嗪和10 mg·kg-1格列本脲，0.5 h后灌胃给予5 mg·kg-1氯沙坦钾，经尾静脉予不同时间点采集血样，采用HPLC测定血样中氯沙坦及其代谢产物E-3174的浓度。采用DAS计算各组主要的药动学参数，并进行统计学分析。结果 合用格列吡嗪后，氯沙坦和E-3174的AUC、MRT和峰浓度均明显增加，氯沙坦的清除率减小；合用格列本脲后，氯沙坦的达峰时间提前，E-3174的MRT延长。结论 与同剂量的格列本脲相比，格列吡嗪对氯沙坦及其代谢产物在大鼠体内的药动学影响较大。临床上合用氯沙坦和格列吡嗪时，应注意潜在的药物相互作用所致的药物不良反应。 |
| 关键词: 氯沙坦 格列吡嗪 格列本脲 药动学 |
| DOI：10.13748/j.cnki.issn1007-7693.2017.01.020 |
| 分类号:R284.1；R917.101 |
| 基金项目:卫生行业科研专项项目（201302008） |
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| Effect of Glipizide and Glibenclamide on the Pharmacokinetics of Losartan |
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LIN Shu1, PAN Peipei2, HU Guoxin3
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1.Department of Pharmacy, Second Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China;2.Department of Pharmacy, Taizhou Central Hospital, Taizhou 318000, China;3.Department of Pharmacology, Wenzhou Medical University, Wenzhou 325000, China
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| Abstract: |
| OBJECTIVE To study the effect of glipizide and glibenclamide on the pharmacokinetics of losartan in rats. METHODS Fifteen rats were randomly divided into 3 groups(control group, glipizide group and glibenclamide group) and administrated orally with 0.5%CMC, 10 mg·kg-1 glipizide and 10 mg·kg-1 glibenclamide, respectively. The 5 mg·kg-1 losartan potassium was administrated orally to the rats 0.5 h later and blood samples were collected via tail vein at different time point, which were further processed and analyzed for the concentration of losartan and E-3174 by HPLC. The pharmacokinetic parameters were calculated by DAS, followed by statistical analysis. RESULTS When co-administrated with glipizide, the AUC, MRT and Cmax of losartan and E-3174 were significantly increased and the clearance of losartan was significantly decreased; when co-administrated with glibenclamide, only the Tmax of losartan and MRT of E-3174 were altered. CONCLUSION Glipizide significantly affected the pharmacokinetics of losartan and its metabolite E-3174 in rats. In clinic, when these two drugs are co-administrated, drug adverse reaction of losartan induced by drug-drug interaction should be paid attention to. |
| Key words: losartan glipizide glibenclamide pharmacokinetics |
