依替米星骨水泥植入剂在兔体内的局部组织释放及肾脏安全性考察

发布时间：2018-03-05 17:33

本文选题：依替米星　切入点：骨水泥　出处：《中国药学杂志》2015年18期 　论文类型：期刊论文

【摘要】：目的研究依替米星骨水泥植入剂在家兔体内的局部释放及其全身浓度并评价其肾毒性。方法将自制定量的依替米星骨水泥药柱,手术植入兔股骨髓腔,测定植入依替米星骨水泥后不同时间的骨及周围组织浓度和全身血药浓度,应用Phoenix Win Nonlin 6.3软件进行药物动力学参数计算。应用全自动生化分析仪对给药前后兔的血肌酐和尿素氮进行测定,评价其肾毒性。结果依替米星骨水泥植入剂,t1/2(13.2±4.71)h,tmax(4.44±0.88)h,ρmax(7 163.15±1 673.62)ng·m L-1,术后1,2,4周骨髓局部浓度分别为(226.14±60.20),(16.00±11.40),(5.98±1.97)μg·g-1,骨皮质浓度(54.68±36.98),(3.95±1.73),(1.39±0.77)μg·g-1。结论依替米星骨水泥植入剂较全身注射给药可以达到较好的缓释作用。植入1个月后局部组织浓度仍能达到多数细菌MIC以上,而且肾毒性较全身用药低,可以为临床使用提供参考。
[Abstract]:Objective to study the local release and systemic concentration of etimicin bone cement implant in rabbits and evaluate its nephrotoxicity. Bone and surrounding tissue concentrations and systemic blood drug concentrations were measured at different time after implantation of Etimicin bone cement. The pharmacokinetic parameters of rabbits were calculated by Phoenix Win Nonlin 6.3 software. The serum creatinine and urea nitrogen were measured by automatic biochemical analyzer before and after administration. Results the renal toxicity was evaluated. Results the local bone marrow concentrations of etemicin cement implants were 226.14 卤60.20 卤11.40 卤1.97 渭 g 路g 路g -1 and 54.68 卤36.98 卤3.98 卤0.88 h, 蟻 max(7 163.15 卤1 673.62 ng 路ml -1, respectively. Conclusion the local bone marrow concentrations based on stellate bone cement implants are better than that of the whole body injection of mistrin cement implants (54.68 卤36.989.98 卤1.97) 渭 g 路g-1.Conclusion the local bone marrow concentrations of Etimicin cement implants are better than those of the whole body injection of pterylocycin-cement implants at 4 weeks after operation, and the bone cortex concentration is 54.68 卤36.98 卤0.88 卤0.88 卤0.78 卤0.77 渭 g 路g-1.Conclusion the local bone marrow concentrations at the 4th week after operation are 226.14 卤60.20 卤11.40 卤1.97 渭 g 路g 路g -1, respectively. Release. 1 month after implantation, the local tissue concentration can still reach more than most bacteria MIC, Moreover, the nephrotoxicity is lower than that of systemic medication, which can provide reference for clinical use.
【作者单位】：北京积水潭医院药剂科;北京积水潭医院病理科;北京积水潭医院创伤骨科;
【基金】：北京市优秀人才培养资助项目(2011D003034000018)
【分类号】：R965

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