载抗结核药吡嗪酰胺、卷曲霉素、莫西沙星及阿米卡星骨水泥的体外缓释性能  

Sustained releasing of pyrazinamide,capreomycin,moxifloxacin and amikacin loaded bone cement in vitro

作　　者：袁虎成 丁永国 马雪花 马文鑫[3] 孙建民 王自立 金卫东[3,5] Yuan Hucheng;Ding Yongguo;Ma Xuehua;Ma Wenxin;Sun Jianmin;Wang Zili;Jin Weidong(Pain Department of Ningxia Integrated Traditional Chinese and Western Medicine Hospital,Yinchuan 750021,Ningxia Hui Autonomous Region,China;DaxinCommunity Health Service Center of Yinchuan Third People’s Hospital,Yinchuan 750004,Ningxia Hui Autonomous Region,China;General Hospital of NingxiaMedical University,Yinchuan 750004,Ningxia Hui Autonomous Region,China;Xi’an International Medical Center Hospital,Xi’an 710000,Shaanxi Province,China;Ningxia Medical University,Yinchuan 750004,Ningxia Hui Autonomous Region,China)

机构地区：[1]宁夏中西医结合医院疼痛科,宁夏回族自治区银川市750021 [2]银川市第三人民医院大新社区卫生服务中心,宁夏回族自治区银川市750004 [3]宁夏医科大学总医院,宁夏回族自治区银川市750004 [4]西安国际医学中心医院,陕西省西安市710000 [5]宁夏医科大学,宁夏回族自治区银川市750004

出　　处：《中国组织工程研究》2023年第7期1017-1022,共6页Chinese Journal of Tissue Engineering Research

基　　金：宁夏医科大学校级科研项目资助(XY201828,XY201722),项目负责人:金卫东、王自立;宁夏自然科学基金项目(NZ17145),项目负责人:马文鑫。

摘　　要：背景:骨关节结核病灶清除术后口服抗结核药全身毒副作用大,寻求一种既能节约药物用量又能提高病灶局部药物浓度、降低全身血药浓度的药物缓释系统势在必行。目的:观察载抗结核药吡嗪酰胺、卷曲霉素、莫西沙星、阿米卡星的聚甲基丙烯酸甲酯骨水泥,在PBS人工模拟体液中的缓释性能。方法:将聚甲基丙烯酸甲酯骨水泥Palacos R粉剂分别与抗结核药吡嗪酰胺、卷曲霉素、莫西沙星、阿米卡星混合,每种药物与骨水泥粉剂有1.5 g∶40 g、2.5 g∶40 g两种比例,均加入20 mL液相单体,制备载抗结核药骨水泥标准试件8组,每组5个样本;对照组将40 g骨水泥粉剂与其20 mL液相单体混合,制备不含药骨水泥标准试件1组,共5个样本。将上述所有样本浸泡于PBS中,并置于37℃恒温水浴振荡器内,于设定的时间点取浸提液,采用高效液相色谱法检测药物浓度。结果与结论:①吡嗪酰胺1.5 g组、吡嗪酰胺2.5 g组、卷曲霉素1.5 g组、卷曲霉素2.5 g组、莫西沙星1.5 g组、莫西沙星2.5 g组、阿米卡星1.5 g组、阿米卡星2.5 g组在PBS中可测到最低释药浓度的时间分别为45,60,150,150,120,120,60,90 d,其中卷曲霉素1.5 g组、卷曲霉素2.5 g组、莫西沙星1.5 g组、莫西沙星2.5 g组、阿米卡星2.5 g组具有更长的释药周期,对照组无药物释出;②结果显示,载卷曲霉素(1.5,2.5 g)、莫西沙星(1.5,2.5 g)、阿米卡星(2.5 g)的聚甲基丙烯酸甲酯骨水泥释药周期长、缓释性能好。BACKGROUND:Oral anti-tuberculosis drugs have serious systemic side effects after removal of bone and joint tuberculosis lesions.It is imperative to seek a sustained-release drug system that can not only save drug dosage,but also increase local drug concentration in lesions and reduce systemic blood drug concentration.OBJECTIVE:To observe the sustained-release properties of polymethyl methacrylate bone cement loaded with antituberculosis drugs pyrazinamide,capreomycin,moxifloxacin,and amikacin in PBS artificial simulated body fluid.METHODS:Polymethyl methacrylate bone cement Palacos R powder was mixed with antituberculosis drugs pyrazinamide,capreomycin,moxifloxacin,and amikacin in the proportion of 40 g:1.5 g and 40 g:2.5 g,respectively.The 20 mL of liquid monomer were added to prepare 8 groups of anti-tuberculosis drugloaded bone cement standard specimens,with 5 samples in each group.In the control group,40 g bone cement powder and 20 mL liquid monomer were mixed in the same way to prepare 5 standard bone cement samples without drugs.The drug was soaked in PBS and placed in 37℃constant temperature water bath oscillator.The extract was taken at set time points.The drug concentration of each group was determined by high performance liquid chromatography.RESULTS AND CONCLUSION:(1)The time of the lowest drug release concentration in PBS artificial simulated body fluid of pyrazinamide 1.5 g group,pyrazinamide 2.5 g group,capreomycin 1.5 g group,capreomycin 2.5 g group,moxifloxacin 1.5 g group,moxifloxacin 2.5 g group,amikacin 1.5 g group and amikacin 2.5 g group was 45,60,150,150,120,120,60 and 90 days,respectively.Among these groups,the capreomycin 1.5 g group,capreomycin 2.5 g group,moxifloxacin 1.5 g group,moxifloxacin 2.5 g group,and amikacin 2.5 g group had a longer drug release period,while the control group had no drug release.(2)It is concluded that polymethyl methacrylate bone cement loaded with capreomycin(1.5 g and 2.5 g),moxifloxacin(1.5 g and 2.5 g),and amikacin(2.5 g)has a long release cycle and good

关 键 词：聚甲基丙烯酸甲酯 骨水泥 抗结核药 缓释性能 骨关节结核 病灶清除术 高效液相 缓释材料 

分 类 号：R459.9[医药卫生—治疗学] R318[医药卫生—临床医学] R529.2