Harding S M, Williams P E, Ayrton J
Antimicrob Agents Chemother. 1984 Jan;25(1):78-82. doi: 10.1128/AAC.25.1.78.
Cefuroxime axetil is a new orally absorbed prodrug of the antibiotic cefuroxime. The results of pharmacological studies in 52 healthy volunteers are presented. Intact cefuroxime axetil was not detected in the systemic circulation, indicating that deesterification to yield cefuroxime occurs rapidly after absorption. The bioavailability as measured by urinary recovery of cefuroxime was 40 to 50% if the drug was taken after food and 30% if the drug was taken after overnight fasting. Absorption was similar for three different formulations at 500 mg and independent of dose over the range of 250 mg to 1 g. When the drug was taken after food, serum levels and urinary recoveries were significantly greater for cefuroxime than for ampicillin, but when the drug was taken after fasting the values were similar for the two drugs. The kinetic behavior of cefuroxime axetil and ampicillin was not influenced by repeated dosing at 250 mg. Cefuroxime axetil was well tolerated. Although changes in bowel flora and habit were noted during repeated dosing, these changes were no greater than with ampicillin.
头孢呋辛酯是抗生素头孢呋辛一种新的口服吸收前体药物。本文展示了对52名健康志愿者进行的药理学研究结果。在体循环中未检测到完整的头孢呋辛酯，这表明吸收后迅速发生脱酯反应生成头孢呋辛。如果在进食后服用该药物，以头孢呋辛尿回收率衡量的生物利用度为40%至50%；如果在空腹过夜后服用，则为30%。三种不同剂型的500毫克药物吸收情况相似，在250毫克至1克范围内吸收与剂量无关。当在进食后服用该药物时，头孢呋辛的血清水平和尿回收率显著高于氨苄西林，但在空腹服用时，两种药物的值相似。250毫克重复给药对头孢呋辛酯和氨苄西林的动力学行为没有影响。头孢呋辛酯耐受性良好。虽然在重复给药期间注意到肠道菌群和排便习惯的变化，但这些变化不大于氨苄西林引起的变化。
