中国药理学通报
中國藥理學通報
중국약이학통보
CHINESE PHARMACOLOGICAL BULLETIN
2010年
3期
392-396
,共5页
沈金芳%孙黎%苏克剑%刘瑾
瀋金芳%孫黎%囌剋劍%劉瑾
침금방%손려%소극검%류근
注射用法罗培南钠%药代动力学%高效液相色谱法%单剂量%多剂量%人类实验
註射用法囉培南鈉%藥代動力學%高效液相色譜法%單劑量%多劑量%人類實驗
주사용법라배남납%약대동역학%고효액상색보법%단제량%다제량%인류실험
faropenem sodium for injection%pharmacokinetics%HPLC%single-dose%multiple-dose%human experimentation
目的 研究12名健康志愿者按400 mg单剂量和多剂量静脉滴注注射用法罗培南钠后的药代动力学.方法 多剂量给药方案为每天2次,连续5次.采用高效液相色谱法测定法罗培南钠的血药浓度及尿药浓度.血药浓度-时间数据用3p87软件处理,按两室模型拟合并求算药代动力学参数.尿药排泄数据采用尿药速率法.结果 单剂量给药后的药代动力学参数分别为: C_(max) 为(45.20±8.73) mg·L~(-1);T_(1/2α)为(0.401±0.096) h; T _(1/2β)为(1.419±0.267) h;AUC_(0-12) (以梯形法计算)分别为(59.216±11.886) mg·h·L~(-1);尿累积排泄率为(30.48±12.77)%, T_((1)/(2)) 为(0.993±0.088) h, K_e为(0.227±0.097)h~(-1).多剂量给药达稳态后的药代动力参数分别为:C~(ss)_(min)为(0.03±0.02)mg·L~(-1);C~(ss)_(max)为(44.60±9.08) mg·L~(-1);C_(av) 为(4.939±1.048) mg·L~(-1); T_(1/2α)为(0.340±0.105) h;T_(1/2β)为(1.257±0.173) h;AUC~(ss)_(0-τ)为(59.268±12.571) mg·h·L~(-1) ;尿累积排泄率为(40.55±17.53)% , T_(1/2)为(1.085±0.069) h, K_e为(0.296±0.136) h~(-1).结论 该药在人体内的分布和消除速度不随连续给药而变化.按400 mg ,每天2次的给药方案,在体内可达到有效血药浓度,且安全性好,适合临床推广应用.
目的 研究12名健康誌願者按400 mg單劑量和多劑量靜脈滴註註射用法囉培南鈉後的藥代動力學.方法 多劑量給藥方案為每天2次,連續5次.採用高效液相色譜法測定法囉培南鈉的血藥濃度及尿藥濃度.血藥濃度-時間數據用3p87軟件處理,按兩室模型擬閤併求算藥代動力學參數.尿藥排洩數據採用尿藥速率法.結果 單劑量給藥後的藥代動力學參數分彆為: C_(max) 為(45.20±8.73) mg·L~(-1);T_(1/2α)為(0.401±0.096) h; T _(1/2β)為(1.419±0.267) h;AUC_(0-12) (以梯形法計算)分彆為(59.216±11.886) mg·h·L~(-1);尿纍積排洩率為(30.48±12.77)%, T_((1)/(2)) 為(0.993±0.088) h, K_e為(0.227±0.097)h~(-1).多劑量給藥達穩態後的藥代動力參數分彆為:C~(ss)_(min)為(0.03±0.02)mg·L~(-1);C~(ss)_(max)為(44.60±9.08) mg·L~(-1);C_(av) 為(4.939±1.048) mg·L~(-1); T_(1/2α)為(0.340±0.105) h;T_(1/2β)為(1.257±0.173) h;AUC~(ss)_(0-τ)為(59.268±12.571) mg·h·L~(-1) ;尿纍積排洩率為(40.55±17.53)% , T_(1/2)為(1.085±0.069) h, K_e為(0.296±0.136) h~(-1).結論 該藥在人體內的分佈和消除速度不隨連續給藥而變化.按400 mg ,每天2次的給藥方案,在體內可達到有效血藥濃度,且安全性好,適閤臨床推廣應用.
목적 연구12명건강지원자안400 mg단제량화다제량정맥적주주사용법라배남납후적약대동역학.방법 다제량급약방안위매천2차,련속5차.채용고효액상색보법측정법라배남납적혈약농도급뇨약농도.혈약농도-시간수거용3p87연건처리,안량실모형의합병구산약대동역학삼수.뇨약배설수거채용뇨약속솔법.결과 단제량급약후적약대동역학삼수분별위: C_(max) 위(45.20±8.73) mg·L~(-1);T_(1/2α)위(0.401±0.096) h; T _(1/2β)위(1.419±0.267) h;AUC_(0-12) (이제형법계산)분별위(59.216±11.886) mg·h·L~(-1);뇨루적배설솔위(30.48±12.77)%, T_((1)/(2)) 위(0.993±0.088) h, K_e위(0.227±0.097)h~(-1).다제량급약체은태후적약대동력삼수분별위:C~(ss)_(min)위(0.03±0.02)mg·L~(-1);C~(ss)_(max)위(44.60±9.08) mg·L~(-1);C_(av) 위(4.939±1.048) mg·L~(-1); T_(1/2α)위(0.340±0.105) h;T_(1/2β)위(1.257±0.173) h;AUC~(ss)_(0-τ)위(59.268±12.571) mg·h·L~(-1) ;뇨루적배설솔위(40.55±17.53)% , T_(1/2)위(1.085±0.069) h, K_e위(0.296±0.136) h~(-1).결론 해약재인체내적분포화소제속도불수련속급약이변화.안400 mg ,매천2차적급약방안,재체내가체도유효혈약농도,차안전성호,괄합림상추엄응용.
Aim To study the pharmacokinetics of faropenem sodium for injection after a single and multiple intravenous dose in 12 healthy volunteers.Methods Multiple-dose regiments used 12-hour dosing intervals for 5 doses.Plasma and urine faropenem sodium concentrations were measured using high-performance liquid chromatography.The concentration-time curves of faropenem sodium were fitted to a two-compartment open model.The excretion data in urine were disposed by the method of excretion rate in urine.Results The pharmacokinetic parameters obtained from the single-dose study were as follows: C_(max) =(45.20±8.73) mg·L ~(-1); T_(1/2α) =(0.401±0.096) h; T_(1/2β) =(1.419±0.267) h;AUC_(0-12) =(59.216±11.886) mg·h·L~(-1) .The steady-state pharmacokinetic parameters were: C ss min =(0.03±0.02) mg·L~(-1) ; C ss max =(44.60±9.08) mg·L~(-1) ; C_(av)=(4.939±1.048) mg·L~(-1) ; T_(1/2α) =(0.340±0.105) h; T_(1/2β) =(1.257±0.173) h;AUC~(ss)_(0-12) =(59.268±12.571) mg·h·L~(-1) .The amount of cumulative recovery of faropenem sodium in urine for single and multiple dose within 12 h was(30.48±12.77)% and (40.55±17.53)%, respectively.The pharmacokinetic parameters in urine of the single-dose study were: T_(1/2) =(0.993±0.088) h, K_e=(0.227±0.097) h~(-1) .The steady-state pharmacokinetic parameters in urine were: T_(1/2) =(1.085±0.069) h, K_e=(0.296±0.136) h~(-1) .Conclusions The distribution and elimination rates of faropenem sodium for injection are not changed after multiple intravenous administrations.Effective concentrations in vivo can be achieved after the repeated administration with 400 mg twice a day regiment.The dosing schedule can be recommended.
