Nix D E, Symonds W T, Hyatt J M, Wilton J H, Teal M A, Reidenberg P, Affrime M B
Clinical Pharmacokinetics Laboratory, Millard Fillmore Health System, Buffalo, New York, USA.
Pharmacotherapy. 1997 Jan-Feb;17(1):121-5.
To compare the pharmacokinetics of ceftibuten, cefixime, ceturoxime axetil, and cefaclor after oral administration.
Randomized, four-period, crossover study.
Hospital-based clinical research center.
Healthy adult men and women volunteers.
Single 400-mg doses of cefixime and ceftibuten, and 500-mg doses of cefuroxime axetil and cefaclor.
Serum concentrations were determined by high-performance liquid chromatography methods. The mean oral clearances of cefixime, cefuroxime axetil, and cefaclor were similar, ranging from 20.4-27.0 L/hour; clearance of ceftibuten was approximately 4-fold less, 5.45 L/hour. The serum half-lives of ceftibuten (2.35 hrs) and cefixime (2.38 hrs) were prolonged compared with those of cefuroxime axetil (1.30 hrs) and cefaclor (0.693 hr). These agents also differed in terms of time to maximum concentration, time to peak plasma level, area under the curve, and apparent volume of distribution, the last reflecting differences in biovailability.
Ceftibuten had a relatively high time to maximum concentration and long half-life, resulting in a 3.5-fold higher area under the curve than cefixime, cefuroxime axetil, and cefaclor. These pharmacokinetic data can be used as a basis to compare the four oral cephalosporins; however, comparative susceptibility data must also be considered.
比较口服头孢布烯、头孢克肟、头孢呋辛酯和头孢克洛后的药代动力学。
随机、四周期、交叉研究。
医院临床研究中心。
健康成年男女志愿者。
单次口服400毫克头孢克肟和头孢布烯，以及500毫克头孢呋辛酯和头孢克洛。
采用高效液相色谱法测定血清浓度。头孢克肟、头孢呋辛酯和头孢克洛的平均口服清除率相似，范围为20.4 - 27.0升/小时；头孢布烯的清除率约低4倍，为5.45升/小时。与头孢呋辛酯（1.30小时）和头孢克洛（0.693小时）相比，头孢布烯（2.35小时）和头孢克肟（2.38小时）的血清半衰期延长。这些药物在达峰浓度时间、血药峰浓度时间、曲线下面积和表观分布容积方面也存在差异，后者反映了生物利用度的差异。
头孢布烯的达峰浓度时间相对较长，半衰期较长，导致其曲线下面积比头孢克肟、头孢呋辛酯和头孢克洛高3.5倍。这些药代动力学数据可作为比较这四种口服头孢菌素的基础；然而，还必须考虑比较药敏数据。
