Ricevuti G, Pasotti D, Mazzone A, Gazzani G, Fregnan G B
Department of Internal Medicine and Therapeutics, University of Pavia, Italy.
Chemotherapy. 1988;34(5):374-9. doi: 10.1159/000238595.
Serum and bronchial concentrations of erythromycin were determined in 30 chronic bronchitic patients during an exacerbation phase of bacterial infections. The levels were measured after single and multiple oral treatments with erythromycin-propionate-N-acetylcysteinate (EPAC) or erythromycin stearate (ES) in a double-blind design. EPAC showed higher and longer-lasting erythromycin levels in serum, sputum and pure bronchial mucus than ES. It is believed that EPAC is better absorbed because of its greater stability in the gastrointestinal juices. Higher concentrations in bronchial secretions not always depend on the blood levels. It seems to be possible that the N-acetylcysteine moiety in the molecule of EPAC drug can facilitate antibiotic penetration because of its mucolytic activity. The clinical response (disappearance of fever, clearance of bacterial pathogens from sputum, reduction of quantity and viscosity of sputum) also occurred faster in the EPAC than in the ES group.
在30例慢性支气管炎患者细菌感染加重期测定了血清和支气管中的红霉素浓度。采用双盲设计,在单次和多次口服丙酰基-N-乙酰半胱氨酸红霉素(EPAC)或硬脂酸红霉素(ES)后测量这些水平。与ES相比,EPAC在血清、痰液和纯支气管黏液中显示出更高且更持久的红霉素水平。据信,由于EPAC在胃肠液中具有更高的稳定性,其吸收更好。支气管分泌物中的较高浓度并不总是取决于血液水平。EPAC药物分子中的N-乙酰半胱氨酸部分因其黏液溶解活性可能有助于抗生素渗透。EPAC组的临床反应(发热消退、痰液中细菌病原体清除、痰液量和黏稠度降低)也比ES组出现得更快。