国产洛美沙星胶囊临床药代动力学和生物利用度  

CLINICAL PHARMACOKINETICS AND BIOAVILABILTY OF LOMEFLOXACIN IN CHINESE VOLUNTEERS

作　　者：娄建石[1] 张京玲[1] 张才丽[1] 刘德孟[1] 魏殿军[1] 李立津[1] 吴瑾[1] 胡文芝[1] 

机构地区：[1]天津医学院药理教研室,天津医学院第二附属医院感染疾病研究室

出　　处：《中国抗生素杂志》1994年第4期253-258,共6页Chinese Journal of Antibiotics

摘　　要：健康成年男性志望者１２名，随机分为２组，分别一次空腹口服进口或国产洛美沙星胶囊３００ｍｇ。２周后进行交叉试验。分别于给药前和给药后不同时间取血、尿标本，记录尿量。采用微生物法测定血、尿药物浓度。测试菌为大肠杆菌ＡＴＣＣ２５９２２。结果表明，进口和国产洛美沙星均符合口服一级吸收动力学的二房室开放模型。主要药代参数有：Ｔｌａｇ０．１７±０．１２和０．２６±０．０９ｈ，Ｔｍａｘｌ，１２±０．２８和０．７７±０．３７ｈ，Ｃｍａｘ１．５２±０．５３和１．８１±０．９１μｇ／ｍｌ，Ｖ／Ｆ１３６．７４±８６．６５和１３１．５８±５５．００Ｌ，Ｔβ１／２９．９２±２．４０和９８±２．５１ｈ，ＡＵＣ１２．９７±２．８９和１１．７８±３．３０μｇ／ｍｌ．ｈ，Ｃｌｓ／Ｆ２４．３３±６．０５和２７·６０±８·５３Ｌ／ｈ。尿药浓度采用平均排泄速率法计算后各药基本符合一级消除动力学的二房室开放模型。Ｒｔｎａｘ为２６．３１±１１，３６和２１．６２±１６．１０ｍｇ／ｈ，Ｃｌｒ为２６９．０±８３．４和３８０．２±２３２．４ｍｌ／ｍｉｎ。４８ｈ内尿中排泄药物总量分别为１９９．３±５８．７和２１０．２±８５．０ｍｇ，各占投药量的６７·９５±１９?iu Demeng;Wei Dianjun; Li Lijin; Wu Jin; Hu Wenzhi(Department of Infectious Disease, The Second Teaching Hospital,Tianjin Medical College,Tianjin 300211)ABST RACT The clinical pharmacokinetics and bioavailability of Lomefloxacin were studied in 12 Chinese male healthy volunteers with randomised crossover oral dose of 300 mg capsule made in Japan and China respectiveiy. The serum and urine concentrations of Lomefloxacin were measured by microbiological assay,The serum concentration-time curves appeared to fit the two-compartment open model,The results sho-wed that T lag were 0.17± 0.12 and 0.26±0.09 h;Tmax 1.12± 0.28 and 0.77 ± 0.37 h;max 1.52± 0.53 and 1.81± 0.91 μg/ml;tβ1/2 9.92 ±2.40 and 9.88±2.51 h;AUC 12.97±2.89 and 11.78 ±3.30 (μg/ml)h;V/F 136.74±86.65and 131.58±55.00 L; CLs/24.33± 6.05 and 27.60± 8.53 L/h,The urine concentration excretion parameters were Rmax 26.31±11.36 and 21.62± 16.10mg/h; Clr 269.0±83.4 and 380.2±232.4 ml /min; The renal excretion of unchanged Lomefloxacin 67.95 ±19.94 and 79.88 ± 33. 12%of dose,The relative bioavailability of Lomefloxacin made in China is 90.99± 17.74%。

关 键 词：洛美沙星 药代动力学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]