国产氟罗沙星正常人体耐受性及药代动力学比较研究  

TOLERANCE TRIALS AND PHARMACOKINETICS STUDY OF FLEROXACIN IN NORMAL VOLUNTEERS

作　　者：李华[1] 侯杰[1] 刘彦[1] 梁远军[1] 李家泰[1] 

机构地区：[1]北京医科大学临床药理研究所,航天医学工程研究所

出　　处：《中国临床药理学杂志》1995年第1期20-27,共8页The Chinese Journal of Clinical Pharmacology

摘　　要：本研究对国产氟罗沙星进行了片剂的５０，１００，２００，４００，６００ｍｇ５个剂量的耐受性试验，１００，２００，４００ｍｇ３个剂量的药代动力学试验和与２００ｍｇ进口洛美沙星胶囊的药代动力学对比试验。耐受性试验结果表明直至６００ｍｇ试验结束不论是受试者主观感觉、还是血尿生化指标均无改变。证明单次口服氟罗沙星６００ｍｇ以下均可耐受。药代动力学结果表明：分别口服１００，２００，４００ｍｇ氟罗沙星片剂以后用ＨＰＬＣ法测定血尿药浓度，所得主要药代动力学参数分别为：Ｃ＿ｍａｘ＝１．１８±０．２１ｍｇ／１，２．２２±０．４２ｍｇ／１，４．５８±０．８７ｍｇ／１。Ｔｐｅａｋ＝１．３８±０．８８ｈ，１．５６±０．８６ｈ，２．１９±１．２２ｈ。ＡＵＣ＝１６．１±６．１ｍｇ·ｈ￣－１·Ｌ￣－１，３８．５±７．１ｍｇ·ｈ￣－１·Ｌ￣－１，７３．３±９．３１ｍｇ·ｈ￣－１·Ｌ￣－１。Ｔ＿１／２β＝１１．８±５．７ｈ，１４．４±２．９ｈ，１３．３±７．５ｈ。微生物法测定血尿药浓度，所得主要药代动力学参数分别为：Ｃ＿ｍａｘ＝１．２３±０．２８ｍｇ／ｌ，２．３４±０．４４ｍｇ／ｌ，４．３５±１．２５ｍｇ／ｌ。Ｔｐｅａｋ＝１．４８±０．８７ｈ?Fleroxacin is a new member of the class of fluoroquinolones. The drug has good activity (i.e. MIC at less than 2 mg/l against 90% of strains)against a wide range of Gram-positive and Gram-negative bacterial. Both high performance liquid chromatography and bioassay were used to determine concentration of fleroxacin in serum and urine. Below studies were carried out. Tolerance trails of 5 dosages from 50 mg to 600 mg.Pharmacokinetics studies of serial single dose 100 mg, 200 mg and 400 mg. The result shows: 1.The volunteers tolerated single dose fleroxacin well from 50 mg to 600 mg. 2. After single dose fleroxacin 100 mg, 200 mg and 400 mg, the mean values for maximum concentration of drug in serum were 1.18, 2.22 and 4.58mg /l. The times to maximum concentration were 1.38, 1.56 and 2.19 h. .The elimination half-lives were 11.8,14.4 and 13.3h.. The area under curve of concentration-time were 16.1,38.5 and 73.3mg·h-1·L-1. We also recovered 39.79%,32.3% and 38.59% of the administered fleroxacin from the urine as unchanged drug within 24 h after dosing with 100 mg, 200 mg and 400 mg tablets.The results were not significant different compared determined by bioassay and using HPLC.

关 键 词：氟罗沙星 耐受性 药代动力学 微生物测定法 

分 类 号：R978.19[医药卫生—药品]