氟罗沙星片剂、胶囊剂的人体药物动力学和相对生物利用度研究(英文)  

Studies on the pharmacokinetics and relative bioavailability of fleroxacin preparations in healthy volunteers

作　　者：洪诤[1] 薛京会[1] 朱浩[1] 李章万[1] 王浴生[2] 梁德荣 范爱兰 

机构地区：[1]华西医科大学药学院 [2]成都临床药理研究所,成都610041

出　　处：《中国抗生素杂志》1997年第1期31-36,70,共7页Chinese Journal of Antibiotics

摘　　要：9名男性健康自愿受试者采用三交叉单剂口服国产氛罗沙星片剂、胶囊和进口氟罗沙星片剂各400mg的药代动力学参数比较。血、尿药浓度用HPLC检测．结果表明：体内过程符合一室模型，主要药代动力学参数分别为：AUC：82.30±14．30、81．13±8．45与83．92±14.27h·mg／L；Cmax：4．71±0．83、4．67±0．51与4．86±0．89mg／L；Tmax：1．88±0．44、1．90±0．39与1．92±0．23h；T1／2ke：11．02±0．96、10．93±0．68与10．86±0．82h；V／F（c）：79．08±13．31、78.42±8．70与76．39±12．93L；Cl／F：5．00±0．98、4．98±0．52与4．88±0．73L／h。服药48h的尿中原型药排出率分别为给药量的57．4％，55．9％和60．7％。国产氧罗沙星片剂和胶囊口服后药物动力学参数与进口片剂相仿．其相对生物利用及分别为98.07％与96．68％。The following studies were undertaken to evaluate thecomparative pharmacokinetic profiles and their relative bioavailabilities offleroxacin preparations (CFT, CFC and SFT). Nine heralthy young Chinesevolunteers were given a single dose of 400mg fleroxacin according to a triplecross-over design. The drug concentration in plasma and urine were assayed byHPLC method. The plasma concentration-time curve of fleroxacin administeredorally could be best described by an open one-compartment model. Their mainmean parameters were as follows: AUC: 82. 30±14. 30, 81. 13±8. 45 and 83. 92±14. 2 h·mg/L; Cmax: 4. 71 ±0. 83, 4. 67±0. 51 and 4. 86±0. 89mg/L; Tmax:1. 88±0. 44, 1.90±0.39 and 1. 92±0.23h; T1/2ke: 11. 02±0. 96, 10.93±0.68and 10. 86±0. 82h;V/F(c): 79. 08±13. 31, 78. 42±8. 70 and76. 39±12. 93L;Cl/F: 5. 00±0. 98, 4. 98±0. 52 and 4. 88±0. 73L/h. The drug excreted in urinewithin 48h was approximately 57. 4%, 55. 9% and 60. 7%, respectively. Thepharmacokinetic parameters of f1eroxacin China-made tablets, capsules and Swissmade tablets were closely similar. The relative bioavailability of China-madefleroxacin tablets and capsules were 98. 07% and 96. 68%, respectively.

关 键 词：氟罗沙星 片剂 胶囊剂 药物动力学 生物利用度 

分 类 号：R978.19[医药卫生—药品] R944[医药卫生—药学]