替加环素和万古霉素对正常肺和囊性纤维化肺支气管上皮穿透性差异的测定

N. Gunay, F. Akar, C. Gokbulut, S. Sakarya, Tip Fakultesi Tibbi Farmakoloji Anabilim Dali Balikesi Balikesir Universitesi
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引用次数: 0

摘要

目的:探讨替加环素和万古霉素对正常肺和囊性纤维化肺支气管上皮细胞内有效浓度的影响。方法:采用体外细胞培养和高效液相色谱技术测定万古霉素和替加环素在剂量和时间依赖性细胞内浓度方面的差异。结果:囊性纤维化细胞中替加环素的穿透性明显高于正常支气管细胞。替加环素的最佳给药剂量为30 μg/mL,作用时间为8 h。为了使万古霉素渗透到细胞的最小程度,需要给予的万古霉素剂量远远高于指南中描述的最小抑制剂浓度。结论:替加环素对囊性纤维化肺细胞的渗透高于正常肺细胞,而万古霉素对正常肺细胞和囊性纤维化肺细胞的渗透均有限。这些数据表明,替加环素在囊性纤维化患者肺部感染中具有很高的治疗潜力。Klimik Dergisi 2018;31(2): 139 - 43。
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Determination of the Differences in Penetration of Tigecycline and Vancomycin Into Bronchial Epithelium of Normal and Cystic Fibrosis Lung
Objective: We aimed to investigate the dose and time course of tigecycline and vancomycin for effective intracellular concentration in bronchial epithelium of normal and cystic fibrosis lung. Methods: Differences between vancomycin and tigecycline in terms of their doseand time-dependent intracellular concentrations were determined with in vitro cell culture and the high performance liquid chromatography techniques. Results: The penetration of tigecycline was found significantly higher in cystic fibrosis cells compared to normal bronchial cells. The optimal dose for tigecycline was 30 μg/mL and the optimal time was 8 h in comparison to given dose and penetrating amount into the cells. Vancomycin dose needed to be given for minimal penetration into the cell was extremely higher than the minimum inhibitor concentration described in the guidelines. Conclusions: Penetration of tigecycline into cells of cystic fibrosis lung was found higher than normal lung cells, whereas cell penetration of vancomycin into both normal and cystic fibrosis cells was limited. These data suggest that tigecycline has a high therapeutic potential in lung infections of patients with cystic fibrosis. Klimik Dergisi 2018; 31(2): 139-43.
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