【摘要】 建立反相高效液相色谱法测定美洛昔康血药浓度方法。以 5-氯 -2 -氨基 -二苯甲酮为内标 ,乙醚 -正己烷 ( 2∶ 1 )为提取剂 ,紫外检测波长 3 55nm。该方法简单灵敏 ,线性范围为 0 .0 5～ 2 .50μg/ml,最小检测浓度0 .0 2μg/ml;日内、日间误差均小于 7.0 % ,方法绝对回收率大于 90 %。用该法测定了 1 8名健康志愿者随机交叉口服单剂量 1 5mg国产和进口美洛昔康片后的血药浓度 ,并计算药动学参数。结果表明 :美洛昔康的药时曲线下面积 AUC0→ 96 分别为 53 .55± 1 1 .74μg· h/ml和 54.53± 1 1 .1 8μg· h/ml,达峰时间 Tmax分别为 5.6± 2 .7h和5.6± 2 .3 h,峰浓度 Cmax分别为 1 .549± 0 .3 2 8μg/ml和 1 .580± 0 .3 4 2 μg/ml。上述药动学参数经三因素方差分析和双单侧检验统计分析 ,结果表明两种制剂生物等效。以进口片为标准参比制剂 ,国产片的相对生物利用度为98.5± 1 1 .2 %。更多还原

【Abstract】 A sensitive HPLC method for the determination of meloxicam in human plasma was established and the bioequivalence of two MLX was studied. HPLC system consisted of a discovery C\-\{18\} column (5 μm, 250 mm×\{4.6 mm)\} and a mobile phase of methanol H\-2O (75∶25, adjusted pH 4.5 with HOAc ). The UV detector was 355 nm. 5 chloro 2 amino benzophenone was setected as an internal standard. The drug was extracted with ether n hexane(2∶1) after acidification with HCl. The calibration curve was linear in the range from 0.05~2.50 μg/ml with r=0.9998. The relative standard deviations for within day and between day were all < 7.0%, and the recoveries of MLX were >90%. A single oral dose of 15 mg domestic and imported MLX tablet was given to 18 healthy volunteers in a randomized crossover study. The results showed that AUC 0→96 were 53.55±11.74 μg·h/ml and 54.53±11.18 μg·h/ml ; C max were 1.549±0.328 μg/ml and 1.580±0.342 μg/ml; T max were 5.6±2.7 h and 5.6±2.3 h for domestic and imported tablet respectively. Relative bioavailability was 98.5%±\{11.2%.\} The results showed that the two formulations were bioequivalent.更多还原