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1、甲磺酸帕珠沙星注射液人体药动学探究■二作者:沈奇梁德荣苗佳余勤梁茂植徐楠郑莉罗柱吴松泽毕业论文【摘要】;目的研究单次及多次静脉滴注甲磺酸帕珠沙星注射液的药动学特点。方法筛选健康受试者12名,q12h静脉滴注甲磺酸帕珠沙星注射液每次500mg,连续5d,共9次;用反向高效液相色谱?紫外法测定血药浓度,用DASverl.O软件拟合药动学参数。结果受试者静脉滴注甲磺酸帕珠沙星注射液后体内过程符合二室模型;单次给药后的药动学参数:Tmax为(0.47±0.09)h,cmax为(13.71±1.81)mg/L,AUCO-t^(24.60±4.15)mg-h/L,t1/2为(1.46±0.64)h,
2、MRT、CL和Vd分别为(2.14±0.33)h.(0.09±0.04)L/(h・kg)和(0•仃±0・03)L/kg。q12h静脉滴注帕珠沙星500mg连续5d(共9次),第2、3、4、5d晨测得谷浓度分别为0.13.0.16,0.17和0.14mg/L,提示血药浓度已达稳态。末剂给药后的药动学参数:Tmax为(0.48±0.10)h,cmax为(15.41±1.67)mg/L,AUCO-t为(28・42±4・90)mg・h/L,t1/2为(1.33±0.49)h,CL为(0.09±0.06L/)h,(css)av为(2.34±0.43)mg/L,DF为(99.48±0.38)%,以上
3、参数与单次给药比较除cmax外均无统计学差异,且累积系数小,说明本品多次给药无体内蓄积。女性和男性受试者主要药动学参数比较均无统计学差异。受试者给药期间未出现严重不良反应。结论500mgq12h静脉滴注,在人体内可达到有效血药浓度,可以作为临床应用的推荐方案。毕业论文【关键词】;甲磺酸帕珠沙星;反向高效液相色谱?紫外法;药动学毕业论文Studyonpharmacokineticsofpazufloxacinmesylateinjectioninhealthyvolunteers毕业论文ABSTRACT;Objective;Toinvestigatethepharmacokineticso
4、fpazufloxacinmesylateinjectionaftersingleandmultiple?dosesintravenously.;Methods;Twelvehealthyvolunteerswereadministrated500mgpazufloxacinmesylatetwiceadayfor5days.TheplasmaconcentrationsweredeterminedbyRP?HPLC?UVmethodandthepharmacokineticparameterswerecalculatedbyDASverl.Osoftware.;Results;Thep
5、harmacokineticsofpazufloxacinisfittotwocompartmentmodel.Thepharmacokineticparametersaftersingleadministration:Tmaxwas(0.47±0.09)h,cmaxwas(13.71±1.81)mg/L,AUCO-twas(24.60±4.15)mg-h/L,t1/2was(1.46±0.64)h,MRTwas(2.14±0.33)h,CLwas(0.09±0.04)L/(h-kg)andVdwas(0.17±0.03)L/kg・Thepharmacokineticparameters
6、aftersuccessiveadministration:Tmaxwas(0.48±0.10)h,cmaxwas(15.41±1.67)mg/L,AUCO-twas(8.42±4.90)mg・h/L,t1/2was(1.33±0.49)h,CLwas(0.09±0.06)L/h,(css)avwas(2.34±0.43)mg/L,DFwas(99・48±0.38)%・Therewerenosignificantdifferencesinallpharmacokineticparametersexceptcmaxbetweenthefirstandthelastadministraion
7、ofpazufloxacinandcumulationcoefficientwasverysmall.Itsuggestedthattherewasnoaccumulationaftersuccessiveadministration.Noseriousadverseeffectwasobservedinvolunteers.;Conclusion;Effectiveconcentrationinvivocouldbeachieve