Raulston J E
Department of Microbiology and Immunology, University of North Carolina School of Medicine, Chapel Hill 27599-7290.
J Antimicrob Chemother. 1994 Nov;34(5):765-76. doi: 10.1093/jac/34.5.765.
The pharmacokinetics of azithromycin and erythromycin were examined in uninfected and Chlamydia trachomatis infected human endometrial epithelial cells in vitro. Cells which were grown in a polarized orientation showed a three-fold higher quantity of azithromycin uptake than did non-polarized cells. Cellular penetration profiles of azithromycin exceeded erythromycin by as much as eight-fold. In addition, approximately 20% of azithromycin remained cell-associated after 24 h in drug-free medium whereas erythromycin was not retained beyond 3 h. Hormone-responsive primary human endometrial gland epithelial cells, cultured directly after hysterectomy, showed enhanced uptake of both antimicrobials compared with laboratory adapted epithelial cell lines. Cells infected with a genital serovariant of C. trachomatis showed no significant difference in antibiotic uptake during the early stages of the chlamydial developmental cycle, and only a slight decrease in azithromycin uptake in the late stage of infection compared with non-infected cells. Morphological evidence of the bactericidal activity of azithromycin was evident in infected cells at most stages of the chlamydial developmental cycle, whereas the same concentration of erythromycin produced less evidence of marked bactericidal activity as observed by transmission electron microscopy.
在体外对未感染和沙眼衣原体感染的人子宫内膜上皮细胞中阿奇霉素和红霉素的药代动力学进行了研究。以极化方向生长的细胞对阿奇霉素的摄取量比未极化细胞高三倍。阿奇霉素的细胞穿透率比红霉素高出多达八倍。此外，在无药培养基中培养24小时后，约20%的阿奇霉素仍与细胞结合，而红霉素在3小时后就不再保留。直接在子宫切除术后培养的激素反应性原代人子宫内膜腺上皮细胞，与实验室适应的上皮细胞系相比，对两种抗菌药物的摄取均增强。感染沙眼衣原体生殖器血清型的细胞在衣原体发育周期早期的抗生素摄取上无显著差异，与未感染细胞相比，仅在感染后期阿奇霉素摄取略有下降。在衣原体发育周期的大多数阶段，感染细胞中都有阿奇霉素杀菌活性的形态学证据，而通过透射电子显微镜观察，相同浓度的红霉素产生的明显杀菌活性证据较少。
