Tremblay D, Dupront A, Ho C, Coussediere D, Lenfant B
Roussel Uclaf, Direction Recherches Santé, Romainville, France.
J Antimicrob Chemother. 1990 Dec;26 Suppl E:21-8. doi: 10.1093/jac/26.suppl_e.21.
Three pharmacokinetic studies involving single oral doses of cefpodoxime proxetil in healthy volunteers are reported. The first study was to determine the absolute bioavailability of cefpodoxime, the second was to study the relationship between the oral dose of cefpodoxime proxetil and pharmacokinetic parameters of cefpodoxime, and the third was to compare the pharmacokinetics of cefpodoxime in healthy young and elderly volunteers. Half the dose of cefpodoxime orally administered as cefpodoxime proxetil in tablet form reaches the systemic circulation, while 80% of the cefpodoxime absorbed is excreted unchanged in urine. The volume of distribution is large (32.3 l). The pharmacokinetics of cefpodoxime were linear in young and elderly subjects after 100 and 200 mg oral doses, which are those used therapeutically. The Cmax was about 1.4 mg/l (after 100 mg) and 2.6 mg/l (after 200 mg). Deviation from linearity appeared at 400 mg and the effect was confirmed at 800 mg. The differences between young and elderly subjects were negligible, with the exception of the half-life which increased by only 14%, from 2.67 to 3 h. Dosage adjustment is therefore not necessary in the elderly.
本文报道了三项在健康志愿者中进行的关于单次口服头孢泊肟酯的药代动力学研究。第一项研究旨在测定头孢泊肟的绝对生物利用度，第二项研究是探究头孢泊肟酯口服剂量与头孢泊肟药代动力学参数之间的关系，第三项研究则是比较健康年轻志愿者和老年志愿者体内头孢泊肟的药代动力学情况。以片剂形式口服给药的头孢泊肟酯中，有一半剂量的头孢泊肟能够进入体循环，而吸收的头孢泊肟中有80%以原形经尿液排出。分布容积较大（32.3升）。在年轻和老年受试者中，口服100毫克和200毫克（治疗常用剂量）的头孢泊肟后，其药代动力学呈线性。Cmax分别约为1.4毫克/升（100毫克后）和2.6毫克/升（200毫克后）。在400毫克时出现非线性偏差，并在800毫克时得到证实。除半衰期仅增加14%（从2.67小时增至3小时）外，年轻和老年受试者之间的差异可忽略不计。因此，老年人无需调整剂量。
