Faulkner R D, Fernandez P, Lawrence G, Sia L L, Falkowski A J, Weiss A I, Yacobi A, Silber B M
Medical Research Division, American Cyanamid Co., Pearl River, New York.
J Clin Pharmacol. 1988 Aug;28(8):700-6. doi: 10.1002/j.1552-4604.1988.tb03203.x.
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 micrograms/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 micrograms.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.
在一项四交叉研究中，测定了16名健康志愿者体内头孢克肟的绝对生物利用度。每位受试者接受单次200毫克剂量的静脉注射（IV）溶液、口服溶液，以及200毫克和400毫克胶囊剂型的该药物。每次给药后收集24小时的血液和尿液样本。静脉注射和口服该药物后，头孢克肟耐受性良好，未观察到严重的药物相关不良反应。200毫克口服溶液、200毫克和400毫克胶囊剂型给药后，头孢克肟的最大血清浓度（Cmax）分别为3.22、2.92和4.84微克/毫升。静脉注射、200毫克口服溶液、200毫克和400毫克胶囊剂型给药后，血清浓度-时间曲线下的平均面积（AUC）分别为47.0、26.0、23.6和39.4微克·小时/毫升。口服和静脉给药后，该药物的平均消除半衰期值相当，范围为3.2至3.5小时。根据血清AUC值，200毫克口服溶液、200毫克胶囊和400毫克胶囊剂型给药后，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小时尿液回收数据的相应比率分别为44.7%、41.7%和40.5%。因此，结果表明，200毫克和400毫克口服剂量后头孢克肟的吸附百分比相似。
