美洛昔康血药浓度的测定及其人体药代动力学

Determination of meloxicam in plasma by HPLC and study on its pharmacokinetics in man

目的 :建立血浆中美洛昔康的测定方法 ,并研究美洛昔康在中国人体内的药代动力学。方法 :采用 HPL C方法测定 18名健康志愿者口服美洛昔康片剂后的血药浓度。色谱柱为 C18柱 ,15 0 mm× 4.6 m m,5 μm,流动相为 2 0 mm ol· L- 1磷酸盐缓冲液 -乙腈 40∶ 6 0 ,流速为 1.5 0 m l· min- 1 ,检测波长 :U V2 2 5 nm。结果 :测定方法在 0 .10～ 5 .0 0 mg· L- 1范围内具良好的线性关系 ,回收率为 90 .0 0～ 10 5 .0 0 % ,日内、日间 RSD小于 15 % ,最低检测浓度为 0 .0 5 m g· L- 1。药代动力学参数 tmax为 4.33± 1.2 8h;Cmax为 1.5 3± 0 .2 7mg· L- 1 ;t1 /2 为 2 1.2 2± 6 .2 5 h;AU C0 -∞ 为 5 5 .33± 16 .84h· mg· L- 1 。结论 :测定方法具灵敏、准确、快速的优点 ,适用于药代动力学和生物利用度等的研究。美洛昔康片剂在人体的吸收较慢 。

OBJECTIVE:To develop an HPLC method for the determination of meloxicam in human plasma,and to study the pharmacokinetics of meloxicam in healthy Chinese subjects.METHOD:A liquid chromatographic assay has been developed for the determination of meloxicam in plasma from 18 healthy Chinese male volunteers orally administered 15 mg meloxicam. The UV detector was set at 255 nm,and a 250mm×4.6mm ID column packed with C18(5μm) was used.The mobile phase consisted of acetonitrile-20 mmol·L -1 potassium dihydrogenphosphate solution (60∶40)with a flow rate of 1.50 ml·min -1 . Piroxicam was used as the internal standard.RESULTS:A good linearity was obtained in the rang of 0.10～5.00 mg·L -1 . The recovery was more than 90%. The relative standard deviation of within day and between day were less than 10% and 15%,respectively. The minimal detectable concentration in plasma was 0.05mg·L -1 . The main pharmacokinetic parameters were:t max =(4.33±1.28)h;C max =(1.53±0.27)mg·L -1 ;t 1/2 =(21.22±6.25)h;AUC 0-∞ =55.33±16.84)h·mg·L -1 .CONCLUSION:The established method was shown to be sensitive,accurate and fast for the determination of meloxicam levels in human plasma. It is suitable for its pharmacokinetic and bioavailability study. The absorption of meloxicam tablets was slow,and the half life of elimination was long in man.