Strausbaugh L J, Bolton W K, Dilworth J A, Guerrant R L, Sande M A
Antimicrob Agents Chemother. 1976 Sep;10(3):450-6. doi: 10.1128/AAC.10.3.450.
Two macrolide antibiotics, josamycin and erythromycin stearate, were administered orally to healthy, adult male volunteers for a comparative study of their pharmacological properties. In comparable doses, josamycin and erythromycin produced similar plasma concentrations, with similar half-lives and elimination constants. An initial loading dose of 1.5 g of josamycin produced greater peak concentrations of antibiotic throughout a 10-day period with a regimen of every 6 h. In addition, josamycin tended to reach higher peak and trough concentrations after regimens of every 6 or 8 h were maintained for 2 days. Josamycin penetrated into saliva, sweat, and tears, and it was better tolerated in fasting subjects than was erythromycin stearate.
给健康成年男性志愿者口服两种大环内酯类抗生素,交沙霉素和硬脂酸红霉素,以对它们的药理特性进行比较研究。在相当剂量下,交沙霉素和红霉素产生相似的血浆浓度,半衰期和消除常数也相似。在每6小时给药一次的方案下,1.5克交沙霉素的初始负荷剂量在10天内产生了更高的抗生素峰值浓度。此外,在每6或8小时给药一次的方案维持2天后,交沙霉素往往能达到更高的峰浓度和谷浓度。交沙霉素可渗透到唾液、汗液和泪液中,并且在禁食受试者中比硬脂酸红霉素耐受性更好。