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目的:研究壳多糖(几丁质)庆大霉素缓释药体内动力学行为,为其临床应用提供理论依据。方法:将缓释药棒植入兔胫骨干骺端,监测术后不同时间血药浓度、血尿素氮(BUN)和肌酐(Cr)值,局部骨组织和血肿中庆大霉素浓度。结果:血药浓度峰值(0.92μg/ml)在24h出现,维持时间为3周。术后血BUN和Cr值无增加。术后第1天离药棒0.5cm处的血肿、1cm处的皮质骨和松质骨中庆大霉素浓度分别为:62.00,40.38,29.78μg/g,其后下降;第10周时,庆大霉素浓度仍为金葡菌最小抑菌浓度数倍以上。结论:壳多糖庆大霉素缓释药具有良好体内缓释作用,有望为临床治疗骨感染提供一种无需二期取出的简便而有效的方法。
OBJECTIVE: To study the in vivo kinetics of chitosan (chitin) gentamicin sustained release drug in order to provide a theoretical basis for its clinical application. Methods: The drug-resistant rods were implanted into the metaphysis of the tibia of rabbits. Blood concentration, blood urea nitrogen (BUN) and creatinine (Cr), local bone tissue and gentamicin concentration in the hematoma were measured at different time points after operation. Results: The peak plasma concentration (0.92μg / ml) appeared in 24h, the maintenance time was 3 weeks. Postoperative blood BUN and Cr values did not increase. On the first day after operation, hematoma 0.5 cm away from the drug stick, cortical bone at 1 cm and cancellous bone were respectively 62.00, 40.38 and 29.78 μg / g, and then decreased ; The 10th week, the concentration of gentamicin is still several times more than the minimum inhibitory concentration of S. aureus. CONCLUSION: The chitosan gentamycin sustained-release drug has a good sustained-release effect in vivo and is expected to provide a simple and effective method for clinical treatment of bone infection without second-phase removal.