厄贝沙坦片在大鼠体内血药浓度的测定及药动学研究

目的:建立厄贝沙坦片给药后大鼠血药浓度的高效液相色谱测定法并进行药动学研究。方法:色谱柱为Consmosil-C18,流动相为磷酸-甲醇-乙腈(7∶80∶13,V/V/V),流速为1.0mL·min-1,检测波长为272nm;大鼠灌胃给予厄贝沙坦水溶液30mg·kg-1后分别在在给药前及给药后0、5、10、20、30、45、60、120、180、240、360、480min测定血浆中厄贝沙坦的浓度,计算药动学参数。结果:厄贝沙坦的检测浓度线性范围为0.5～50μg.mL-(1r=0.999 1);回收率为93.89%,RSD小于4.14%;t1/2、tmax、Cmax、AUC0～t分别为(48.71±4.037)h、(0.33±0.12)h、(1.33±0.18)μg·mL-1、(23.10±1.56)mg·L·h-1。结论:所建立的血药浓度测定方法简单、灵敏、专一,能够满足血药浓度和药动学研究的需要。

Determination of Plasma Concentration and Pharmacokinetics Study of Irbesartan Tablets in Rats

OBJECTIVE： To establish an HPLC method for the determination of plasma concentration of Irbesartan tablets in rats and its pharmacokinetics study.METHODS： The determination was performed on Cosmosil-C18 column with mobile phase consisted of phosphoric acid-methanol-acetonitrile（7 ∶ 80 ∶ 13,V/V/V） at flow rate of 1.0 mL·min^-1.The detection wavelength was set at 272 nm.Rats were given Irbesartan solution 30 mg·kg^-1 via i.g.gtt.The plasma concentration of irbesartan were determined before medication and at 0 min,5 min,10 min,20 min,30 min,45 min,60 min,120 min,180 min,240 min,360 min,480 min after medication.The pharmacokinetics parameters were estimated.RESULTS： The linear range of irbesartan was 0.5～50 μg·mL^-1（r=0.999 1） with an average recovery of 93.89%（RSD4.14%）.Main pharmacokinetic parameters of irbesartan were as follows： t1/2：（48.71±4.037） h;tmax：（0.33±0.12） h： Cmax：（1.33±0.18） μg·mL-1;AUC0～t：（23.10±1.56） mg·L·h^-1.CONCLUSION： Established method is simple,sensitive and exclusive,which meet the requirements of the plasma concentration and pharmacokinetic study.