ABSOLUTE BIOAVAILABILITY OF CEFIXIME IN MAN
ABSOLUTE BIOAVAILABILITY OF CEFIXIME IN MAN
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DOI：
10.1002/j.1552-4604.1988.tb03203.x
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发表时间：
1988-08-01
影响因子：
2.9
通讯作者：
SILBER, BM
中科院分区：
文献类型：
--
作者：
FAULKNER, RD;FERNANDEZ, P;SILBER, BM
在一项四方交叉研究中，头孢克肟在16名健康志愿者中的绝对生物利用度被测定。每个受试者接受一次200毫克的静脉注射和口服液，以及200毫克和400毫克的胶囊剂量的药物。每次给药后24小时采集血样和尿样。静脉注射和口服头孢克新后耐受性良好，未观察到严重的药物相关不良反应。口服200 mg口服液、200 mg和400 mg胶囊后，头孢克肟的最大血药浓度(Cmax)分别为3.22、2.92和4.84微克/毫升。静脉注射、200毫克口服液、200毫克和400毫克胶囊后的平均血药浓度时间曲线下面积(AUC)分别为47.0、26.0、23.6和39.4微克。HR/m L。口服和静脉注射后，该药物的平均消除半衰期相当，范围为3.2至3.5小时。口服200 mg口服液、200 mg胶囊和400 mg胶囊后，头孢克肟的绝对生物利用度分别为52.3%、47.9%和40.2%。基于24小时尿恢复数据的比率分别为44.7%、41.7%和40.5%。因此，结果表明，200 mg和400 mg口服给药后头孢克肟的吸附百分率是相似的。
In a four-way cross-over study, the absolute bioavailability of cefixime was determined in 16 healthy volunteers. Each subject received a single 200-mg dose as an intravenous (IV) and oral solution, and 200-mg and 400-mg capsule doses of the drug. Blood and urine samples were collected for 24 hours after each dose. Cefixime was well tolerated after IV and oral doses of the drug and no serious drug related adverse effects were observed. The maximal serum concentration (Cmax) of cefixime following the 200-mg oral solution and 200-mg and 400-mg capsule doses were 3.22, 2.92, and 4.84 .mu.g/mL, respectively. Mean area under the serum concentration time curves (AUC) following the IV, 200-mg oral solution, and 200-mg and 400-mg capsule doses were 47.0, 26.0, 23.6, and 39.4 .mu.g .cntdot. hr/mL, respectively. Mean elimination half-life values of the drug were comparable after oral and IV doses, ranging from 3.2 to 3.5 hours. Based on serum AUC values, the absolute bioavailability of cefixime was 52.3%, 47.9%, and 40.2% after the 200-mg oral solution, 200-mg capsule and 400-mg capsule doses, respectively. Respective ratios based on 24-hour urinary recovery data were 44.7%, 41.7%, and 40.5%. Therefore, the results show that the percent of cefixime adsorbed after 200-mg and 400-mg oral doses was similar.