Scaglione F, Triscari F, Demartini G, Arcidiacono M, Cocuzza C, Fraschini F
Department of Pharmacology, University of Milan, Italy.
Chemotherapy. 1995 Jul-Aug;41(4):229-33. doi: 10.1159/000239349.
Ceftibuten is a broad-spectrum oral cephalosporin exhibiting antimicrobial activity against a wide range of gram-negative and some gram-positive pathogens. Pharmacokinetic studies have shown that the molecule has an oral bioavailability higher than 90% of the administered dose (reaching peak serum concentrations of 5-19 mg/l after a single dose of 200 and 400 mg). Moreover, ceftibuten has been shown to be useful in the treatment of acute lower respiratory tract infections. This study was performed to determine the distribution of ceftibuten in bronchial secretions from patients affected by the exacerbation of chronic bronchitis. Patients were treated with a single 400-mg oral dose of ceftibuten. Blood and bronchial-secretion samples were obtained just before, and at 0.5, 1, 2, 4, 8, 12, 16 and 24 h after dosing. Cells were separated from bronchial secretions by centrifugation. Ceftibuten in duplicate samples of both serum and bronchial secretion was quantified by HPLC. Ceftibuten reached peak levels 2 and 4 h after oral administration in serum and in bronchial secretions, respectively (18.12 +/- 2.13 and 9.19 +/- 3.1 mg/l, respectively). Falling curves after the peaks showed a monoexponential decay. The absorption was very rapid both in serum and bronchial secretions, but elimination was slower in bronchial secretions than in serum.
头孢布烯是一种广谱口服头孢菌素，对多种革兰氏阴性菌和一些革兰氏阳性病原体具有抗菌活性。药代动力学研究表明，该分子的口服生物利用度高于给药剂量的90%（单次服用200毫克和400毫克后，血清峰值浓度达到5-19毫克/升）。此外，头孢布烯已被证明可用于治疗急性下呼吸道感染。本研究旨在确定头孢布烯在慢性支气管炎急性加重患者支气管分泌物中的分布情况。患者口服单次400毫克剂量的头孢布烯进行治疗。在给药前以及给药后0.5、1、2、4、8、12、16和24小时采集血液和支气管分泌物样本。通过离心从支气管分泌物中分离细胞。血清和支气管分泌物的双份样本中的头孢布烯通过高效液相色谱法进行定量。头孢布烯在口服给药后血清和支气管分泌物中分别在2小时和4小时达到峰值水平（分别为18.12±2.13毫克/升和9.19±3.1毫克/升）。峰值后的下降曲线呈单指数衰减。血清和支气管分泌物中的吸收都非常迅速，但支气管分泌物中的消除比血清中慢。
