司帕沙星片在健康人体的药动学和生物等效性研究  

Pharmacokinetics and relative bioavailability of sparfloxacin in healthy volunteers

作　　者：高静[1] 孙喜东[2] 宋冬梅[1] 曹相林 王冬梅 

机构地区：[1]沈阳亿灵医药科技有限公司,沈阳110179 [2]中国人民解放军第二O八医院,长春130062 [3]北京四环科宝制药有限公司,北京100070

出　　处：《中南药学》2011年第3期182-185,共4页Central South Pharmacy

摘　　要：目的建立HPLC内标法测定血浆中司帕沙星含量,并研究司帕沙星片的相对生物利用度及生物等效性。方法 20名健康志愿者分2组,随机、交叉口服试验制剂与参比制剂的司帕沙星片0.4 g,测定其血药浓度,计算药物动力学参数及生物等效性评价。结果试验制剂与参比制剂血浆中司帕沙星的tmax为(4.68±0.44)和(4.55±0.51)h;Cmax为(1 560.4±243.9)和(1 584.1±273.9)ng.mL-1;t1/2为(20.92±4.85)和(19.81±3.75)h;用梯形法计算AUC0-t为(43 325±12 174)和(44 139±11 815)ng.h.mL-1;AUC0-∞为(45 452±12 884)和(45 999±12 629)ng.h.mL-1。以AUC0-t计算,试验制剂的平均相对生物利用度为(97.9±5.8)%。结论该法操作简便,快速灵敏,可用于测定血浆中的司帕沙星浓度;司帕沙星的两制剂具有生物等效性。Objective To develop an HPLC method to determine sparfloxacin concentrations in human plasma and to study the pharmacokinetics and relative bioavailability of sparfloxacin for suspension.Methods A single dose reference and test preparation was given to 20 healthy volunteers in a randomized 2-way cross-over study.The plasma sparfloxacin concentrations were determined by HPLC.The pharmacokinetics and relative bioavailability were measured.Results The main pharmacokinetic parameters of the two formulations,sparfloxacin in the test and reference preparation were as follows：tmax（4.68 ± 0.44）and（4.55±0.51）h;Cmax（1 560.4±243.9）and（1 584.1±273.9）ng·mL-1;t1/2（20.92±4.85）and（19.81±3.75）h;AUC0-t（43 325±12 174）and（44 139±11 815）ng·h·mL-1;AUC0-∞（45 452±12 884）and（45 999±12 629）ng·h·mL-1,respectively.The average bioavailability for test sparfloxacin was（97.9±5.8）%.Conclusion The method is simple,quick and sensitive,the reference and test sparfloxacin are bioequivalent.

关 键 词：司帕沙星 相对生物利用度 生物等效性 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]