论文部分内容阅读
目的:建立简便、灵敏、快速的高效液相柱切换法测定人血浆中盐酸左氧氟沙星浓度,比较两种剂型的盐酸左氧氟沙星主要药物动力学参数,进行生物等效性评价。方法:20名健康男性受试者进行随机双交叉试验,随机单剂量口服200 mg盐酸左氧氟沙星片参比制剂和试验制剂后采集血样,以环丙沙星为内标,采用柱切换荧光检测法测定盐酸左氧氟沙星血浆浓度,计算药动学参数及进行生物等效性评价。结果:单剂量口服受试制剂和参比制剂后血浆中的左氧氟沙星主要药动学参数:t_(1/2)分别为:(8.04±0.8)h和(8.3±1.02)h;t_(max)分别为(0.7±0.2)h和(0.8±0.4)h;C_(max)分别为(2 282.62±619.58)ng·ml~(-1)和(2 187.83±601.82)ng·ml~(-1);AUC_(0-36)分别为(17 682.78±3 191.45)ng·h·ml~(-1)和(16 768.09±3 161)ng·h·ml~(-1);AUC_(0～∞)分别为(18 455.6±3 289.1)ng·h·ml~(-1)和(17 571.92±2 915.07)ng·h·ml~(-1);受试药物的相对生物利用度(F)为:(105.4±9.0)%。结论:建立的高效液相柱切换技法在左氧氟沙星片生物等效性研究中的应用准确、灵敏,结果可靠;统计分析表明盐酸左氧氟沙星片试验制剂和参比制剂生物等效。
OBJECTIVE: To establish a simple, sensitive and rapid HPLC method for the determination of levofloxacin in human plasma. The main pharmacokinetic parameters of levofloxacin hydrochloride in two dosage forms were compared to evaluate the bioequivalence. Methods: Twenty healthy male subjects were randomized to receive a double crossover test. A single oral dose of 200 mg levofloxacin hydrochloride tablets and test preparations were taken and blood samples were taken. Ciprofloxacin was used as an internal standard and determined by column-switch fluorescence detection Levofloxacin Hydrochloride Plasma Concentration, Pharmacokinetic Parameters and Bioequivalence Assessment. Results: The main pharmacokinetic parameters of levofloxacin in plasma after single-dose oral administration of test preparation and reference preparation were: t 1/2 (8.04 ± 0.8) h and (8.3 ± 1.02) h, t max (0.7 ± 0.2) h and (0.8 ± 0.4) h respectively; C max were (2 282.62 ± 619.58) ng · ml -1 and (2 187.83 ± 601.82) ng · ml -1 ); AUC_ (0-36) were (17 682.78 ± 3 191.45) ng · h · ml -1 and 16 768.09 ± 3 161 ng · h · ml -1; ∞) were 18 455.6 ± 3 289.1 ng · h · ml -1 and 17 571.92 ± 2915.07 ng · h · ml -1, respectively. The relative bioavailability (F ) Was: (105.4 ± 9.0)%. Conclusion: The established HPLC method is effective and accurate in the bioequivalence study of levofloxacin tablets. The statistical analysis shows that the levofloxacin hydrochloride tablets test preparation and reference preparation are bioequivalent.