普卢利沙星片在健康人体的药代动力学研究

目的研究单剂量口服普卢利沙星片在中国健康志愿者体内的药代动力学。方法12名健康成年受试者按3×3拉丁方随机分组,分别单次口服100、200、400mg普卢利沙星片,采用LC/MS/MS法测定给药后普卢利沙星代谢产物NM394的血药浓度,应用DAS ver2.0软件进行房室拟合及参数计算。结果血样中未检测到普卢利沙星,只能测定其代谢产物NM394。低、中、高3个剂量组均符合二室模型,在人体内的药动学过程符合一级动力学。男女受试者的主要药动学参数无显著性差异。试验期间未发现明显不良反应。结论普卢利沙星片单次3剂量口服给药后,其代谢产物NM394的Cmax和AUC呈良好的剂量依赖性,主要代谢参数在我国健康成人中无性别差异。检测方法灵敏、准确、可靠、特异性强,可满足普卢利沙星临床药动学试验要求。

Pharmacokinetics of Prulifloxacin Tablets in Healthy Volunteers

Aim To investigate the pharmaeokinetics of prulifloxacin tablets in Chinese healthy volunteers after a single oral administration of prulifloxacin tablets. Methods A total of 12 healthy adult subjects were randomly grouped by 3× 3 Latin square and assigned to receive a single oral dose of 100,200 and 400mg of prulifloxacin tablets. LC/MS/MS were used for the determination of NM394,the metabolite of prulifloxacin,in plasma after a single oral dose of prulifloxacin tablets. Important pharmaeokinetic parameters were caculated by DAS 2.0 software （compartment model）. Results No prtdifloxacin but its metabolite-NM394 was identified in the blood sample of subjects. All the three dosage groups （100,200,400rag） conformed to the two-compartment model. The pharmacokinetics fitted first-order kinetic process. No difference in pharmaeokineties of NM394 in male and female volunteers was observed. 12 subjects completed the single oral administration test, with no adverse drug reactions during the test. Conclusion The Cmax ,AUC of NM394 are highly correlated with given prulifloxacin doses. The established method is sensitive, accurate, reliable and specific, and it can meet the requirement of clinical pharmacokinetic trials.