甲磺酸培氟沙星多次给药的药代动力学与合理给药方案研究  

Multiple-dose pharmacokinetics of pefloxacin in normal volunteers and study of reasonable regimen

作　　者：李华[1] 陆红[1] 张朴[1] 赵彩云[1] 李家泰[1] 

机构地区：[1]北京医科大学临床药理研究所

出　　处：《中国药学杂志》1996年第1期37-40,共4页Chinese Pharmaceutical Journal

摘　　要：目的：通过测定连续口服甲磺酸培氟沙星后的健康志愿者体内的稳态血药浓度，提出该药用于抗感染治疗的给药方案。方法：选择男性健康志愿者，ＨＰＬＣ测定血药浓度，用３Ｐ８７和Ｓｃｈｉｍ程序处理数据。结果：连续６ｄ给药（４００ｍｇｂｉｄ）后可达稳态血药浓度，其中Ｃ_（ｓｓｍａｘ）＝１２．２４±３．８７ｍｇ／Ｌ，Ｃ_（ｓｓｍｉｎ）＝７．４７±２．３６ｍｇ／Ｌ，积蓄比Ｒ＝２．３６。结论：该药的积蓄情况比较严重，但４００ｍｇｂｉｄ给药方式是安全的。同时建议４００ｍｇｂｉｄ用于重度感染，２００ｍｇｂｉｄ用于中轻度感染，８００ｍｇｂｉｄ的方案不予考虑。To determines the steady-state plasma concentration of pefloxacin in normal volunteers after multiple doses,and to suggest a therapeutic regimen in the treatment of various infections.METHOD:6 health male volunteers were orally given 400 mg pefloxacin every 12 h in 14 doses.HPLC was used for the determination of concentration of pefloxacin in plasma. Statistical software's 3P87 and Schim were used for the calculation of results.RESULTS:Steady-state plasma concentration was achieved after pefloxacin was continuously given for six days (400 mg bid).Calculated results were:Cssmax=12.24±3.87 mg/L,Cssmin=7.47±2.36 mg/L,cumulative ratio R=2.36.CONCLUSIONS:The cumulative ratio of pefloxacin indicated it might cause severe side effects during multiple doses,however the use of 400 mg dose(bid)was safe and a 400 mg (bid) dose was recommended for the treatment of severe infections,a 200 mg (bid)dose for modest infections;a 800 mg(bid)dose regimen was not recommended.

关 键 词：药代动力学 甲碘酸培氟沙星 高效液相色谱 

分 类 号：R978.19[医药卫生—药品]