诺氟沙星缓释微球的制备及释放性能  

Preparation and release property of norfloxacin sustained-release microspheres

作　　者：原佳露 刘梅[1] 覃小龙 邱阳[1] 李菁 Yuan Jialu;Liu Mei;Qin Xiaolong;Qiu Yang;Li Jing(College of Chemistry&Chemical Engineering,Southwest Petroleum University,Chengdu 610500,Sichuan Province,China)

机构地区：[1]西南石油大学化学化工学院,四川省成都市610500

出　　处：《中国组织工程研究》2023年第30期4790-4795,共6页Chinese Journal of Tissue Engineering Research

基　　金：国家级大学生创新创业训练计划(202110615061),项目负责人:覃小龙。

摘　　要：背景:诺氟沙星在临床上应用广泛,将其制备成缓释微球能够在较长时间发挥作用,在很大程度上提高了药物的生物利用度与患者的顺应性,减少了药物的毒副作用与患者治疗周期内的不适感和服药剂量,具有重要的研究意义与应用价值。目的:以壳聚糖、纳米SiO_(2)和海藻酸钠为原料,制备诺氟沙星缓释微球,并对其制备条件、释放性能与微球结构进行考察和分析。方法:利用挤出-外源凝胶法制备诺氟沙星微球,通过单因素实验考察诺氟沙星浓度、m(SiO_(2))∶m(诺氟沙星)与交联时间对微球包封率的影响,确定最优制备条件,并在最佳制备条件下制备出海藻酸钙/壳聚糖及SiO_(2)-海藻酸钙/壳聚糖两种诺氟沙星缓释微球,对制得的微球进行表征和体外释放性能研究。结果与结论:①单因素实验结果表明,诺氟沙星质量浓度为1.5 g/L、m(SiO_(2))∶m(诺氟沙星)为4∶10、交联时间为20 min时,微球包封率较优,选择在此条件下制备微球;②通过对微球的红外光谱、扫描电镜、X射线衍射和热重分析表征得出,上述条件下制备的微球更倾向于非晶性物质,其外貌尺寸均一、形状规整,SiO_(2)与海藻酸钙、壳聚糖相容性好,形成了新的复合物,添加SiO_(2)对微球的形貌基本没有影响,且添加SiO_(2)的微球热稳定性较好;③对制得微球的缓释性能研究发现,微球具有一定缓释作用,释放时未出现突释现象,且添加SiO_(2)的微球抗盐性能更好。BACKGROUND:Norfloxacin is widely used in clinical practice.When it is used as the sustained-release microspheres,it can play a role in a long time,largely improve the bioavailability and elevate the compliance of patient’s medication,and also can decrease the adverse reaction,discomfort and medication dosage during the treatment period.It has important research significance and application value.OBJECTIVE:To prepare norfloxacin-loaded microspheres and investigate and analyze its preparation conditions,release properties and structure with chitosan,nano-SiO_(2)and sodium alginate as the raw materials.METHODS:Norfloxacin microspheres were prepared by extrusion-exogenous gel method.The effects of norfloxacin concentration,m(SiO_(2)):m(norfloxacin)and crosslinking time on the encapsulation rate of norfloxacin microspheres were investigated by single factor experiment.The optimal preparation conditions were determined and two types of norfloxacin sustained release microspheres,calcium alginate/chitosan and SiO_(2)-calcium alginate/chitosan,were prepared under the optimal preparation conditions.The microspheres were characterized and released in vitro.RESULTS AND CONCLUSION:(1)The single factor experiment results showed that the encapsulation rate of microspheres was better when the concentration of norfloxacin was 1.5 g/L,the concentration of m(SiO_(2)):m(norfloxacin)was 4:10,and the crosslinking time was 20 minutes.(2)Through the characterization of the microspheres by Fourier Transform Infrared Spectroscopy,scanning electron microscopy,X-ray diffraction and thermogravimetric analysis,it can be concluded that the microspheres prepared under the above conditions tended to be amorphous materials,with uniform appearance size and regular shape,and SiO_(2)had good compatibility with calcium alginate and chitosan,forming a new complex.The addition of SiO_(2)had no effect on the morphology of the microspheres.The thermal stability of SiO_(2)microspheres was better.(3)The sustained release performance of the prepared micro

关 键 词：缓释微球 诺氟沙星 壳聚糖 海藻酸钠 纳米SIO2 包封率 释放性能 挤出-外源凝胶法 

分 类 号：R459.9[医药卫生—治疗学] R318.08[医药卫生—临床医学] O636[理学—高分子化学]