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建立并验证一个简单和快速的血浆中罗格列酮RP-HPLC分析方法和提取方法,并将该法应用于罗格列酮体内药动学和组织分布研究.在大鼠给药前和给药后0.083,0.25,0.50,1,2,3,4,6,8,10和24h通过尾静脉采集血样检测,并检测给药1h后各组织的罗格列酮的分布情况.给药后1h,采集大鼠脑脊液,检测脑脊液内罗格列酮是否存在.结果显示,大鼠灌胃给药3mg/kg时,AUC(0-∞)为(1 574.419±332.731)mg.min.L-1,Tmax为(40±10)min,CL/F为0.002L.min-1.kg-1,t1/2为(150.314±44.209)min,Cmax为(6.974±0.877)mg/L.给药1h后,各个组织均有分布.罗格列酮能够透过血脑屏障,给药后1h,通过率为0.004 5%.由此得出结论,罗格列酮在大鼠体内吸收迅速,分布广泛,且能够通过血脑屏障.
To establish and validate a simple and rapid RP-HPLC method for the determination of rosiglitazone in plasma and its application in the pharmacokinetics and tissue distribution of rosiglitazone in vivo.Methods: Blood samples were collected via the tail vein at 0.083, 0.25, 0.50, 1, 2, 3, 4, 6, 8, 10 and 24 h after drug administration and the distribution of rosiglitazone in each tissue was determined after 1 h 1h, collecting cerebrospinal fluid (CSF) and detecting the presence of rosiglitazone in the cerebrospinal fluid.The results showed that the AUC (0-∞) was (574.419 ± 332.731) mg.min.L- 1, Tmax was (40 ± 10) min, CL / F was 0.002L.min-1.kg-1, t1 / 2 was (150.314 ± 44.209) min and Cmax was (6.974 ± 0.877) mg / After 1h, all the tissues were distributed.Roglitazone was able to penetrate the blood-brain barrier, and the passing rate was 0.004 5% at 1h after administration.The conclusion was that rosiglitazone absorbed rapidly and distributed in rats Broad, and can pass the blood-brain barrier.