| 引用本文: | 王琼,钟优艳,叶丛丛,林玉仙,陈连国.阿魏酸长期给药后对大鼠灌服氯沙坦钾的药动学影响[J].中国现代应用药学,2017,34(4):575-578. |
| WANG Qiong,ZHONG Youyan,YE Congcong,LIN Yuxian,CHEN Lianguo.Effects of Ferulic Acid on the Pharmacokinetics of Intragastrically Administered Losartan in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2017,34(4):575-578. |
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| 摘要: |
| 目的 研究长期给药阿魏酸对大鼠体内氯沙坦及其代谢物E-3174的药动学影响。方法 12只健康♂ SD大鼠随机分成2组（每组6只），试验组每天灌胃50 mg·kg-1阿魏酸，连续诱导7 d；对照组灌胃等体积0.5%CMC-Na。第8天给药30 min后，给予氯沙坦钾（5 mg·kg-1）。分别于给药前和给药后0.25，0.5，0.75，1，1.5，2，3，4，6，8，10，12，24 h大鼠尾静脉取血，血样处理后采用UPLC-MS/MS检测大鼠血浆中氯沙坦及E-3174的浓度。结果 虽然2组大鼠体内氯沙坦各项药动学参数对比均无统计学意义，但是试验组大鼠体内E-3174的AUC（0-t）、AUC（0-∞）和Cmax显著增高（P<0.05）；CL/F、Tmax显著降低（P<0.05）。结论 大鼠长期给药阿魏酸后虽然未能引起氯沙坦原形药物药动学的变化，但可使其活性代谢产物E-3174代谢减慢，浓度增高，药时曲线下面积增大。 |
| 关键词: 阿魏酸 氯沙坦 E-3174 UPLC-MS/MS |
| DOI：10.13748/j.cnki.issn1007-7693.2017.04.022 |
| 分类号: |
| 基金项目:温州市科技计划项目（2015Y0271） |
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| Effects of Ferulic Acid on the Pharmacokinetics of Intragastrically Administered Losartan in Rats |
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WANG Qiong, ZHONG Youyan, YE Congcong, LIN Yuxian, CHEN Lianguo
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Department of Pharmacy, People's Hospital of Wenzhou, Wenzhou 325000, China
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| Abstract: |
| OBJECTIVE To study the influence of ferulic acid on the pharmacokinetics of losartan and E-3174 in rats. METHODS Twelve rats (six for each group) were administered orally with 50 mg·kg-1 ferulic acid (experimental group) or 0.5% CMC-Na (control group) every day for 7 d. On the eighth day, losartan (5 mg·kg-1) was given to all rats orally 30 min after taking ferulic acid or CMC-Na. Blood samples were collected from the tail vein before giving losartan and at the time points of 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24 h after administration. The plasma concentrations of losartan and E-3174 were determined by UPLC-MS/MS. RESULTS There was no significant difference on the pharmacokinetic parameters of losartan between the control group and the experimental group. However, the pharmacokinetic parameters of E-3174 in the experimental group, such as AUC(0-t), AUC(0-∞), Cmax were significantly rose (P<0.05) while CL/F and Tmax were significantly decreased (P<0.05) compared with the control group. CONCLUSION This study indicates that the pharmacokinetics of E-3174 in rats can be greatly changed by ferulic acid, slow down the metabolism and increase the concentration. However, ferulicacid has no effect on that of losartan. |
| Key words: ferulic acid losartan E-3174 UPLC-MS/MS |
