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几种制剂中氧氟沙星的生物利用度。 (注:原英文表述有误,多了一个of,正确表述应该是The bioavailability of ofloxacin from several formulations. )

The bioavailability of ofloxacin from several formulations.

作者信息

Flor S, Beals B

机构信息

R. W. Johnson Pharmaceutical Research Institute, Ortho Pharmaceutical Corporation, Raritan, NJ.

出版信息

Curr Med Res Opin. 1991;12(5):282-6. doi: 10.1185/03007999109112662.

Abstract

The bioavailability of ofloxacin after a single dose of one of two tablet formulations (200 or 400 mg) or a liquid formulation (1.67 mg/ml) was investigated in 24 healthy male volunteers in an open randomized, crossover design study with a 5-day wash-out period between doses. Plasma concentrations of ofloxacin were determined at various times after administration by a sensitive and specific High Pressure Liquid Chromatography (HPLC) method. Ofloxacin was well absorbed after each administration, although somewhat more slowly after the tablet formulations than the solution. Mean AUC values of 31.8, 31.3, and 31.3 micrograms.hr/ml were calculated after administration of the solution, 2 x 200 mg tablets and a 400 mg tablet, respectively. Thus, the bioavailability of the tablets was in excess of 98% that of the liquid reference. Mean Cmax values of 4.4, 3.7 and 3.7 micrograms/ml were observed at Tmax values of 0.8, 1.6 and 1.8 hours after administration of the solution, 2 x 200 mg tablets and a 400 mg tablet, respectively. The drug was well tolerated and no adverse effects necessitating subject withdrawal were noted during the study.

摘要

在一项开放随机交叉设计研究中,对24名健康男性志愿者进行了研究,以确定两种片剂剂型(200或400毫克)之一或液体制剂(1.67毫克/毫升)单次给药后氧氟沙星的生物利用度,给药间隔为5天的洗脱期。通过灵敏且特异的高压液相色谱(HPLC)法在给药后的不同时间测定血浆中氧氟沙星的浓度。每次给药后氧氟沙星均吸收良好,不过片剂剂型吸收速度比溶液剂型稍慢。分别给予溶液、2片200毫克片剂和1片400毫克片剂后,计算得到的平均AUC值分别为31.8、31.3和31.3微克·小时/毫升。因此,片剂的生物利用度超过液体制剂对照的98%。分别给予溶液、2片200毫克片剂和1片400毫克片剂后,在Tmax值分别为0.8、1.6和1.8小时时观察到的平均Cmax值分别为4.4、3.7和3.7微克/毫升。该药物耐受性良好,研究期间未发现需要受试者退出试验的不良反应。

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