阿维菌素凝胶微球的制备及其缓释性能  

Preparation and Release Behavior of Avermectin Microspheres

作　　者：辛露露 张雨 刘宝传[2] 张保华[1] XIN Lu-lu1 , ZHANG Yu1, LIU Bao-chuan2, ZHANG Bao-hua1(1. College of Chemistry and Pharmaceutical Sciences, Qingdao Agricultural University, Qingdao 266109, Shandong China ;2. Linyi Agriculture Bureau, Linyi 276001, Shandong , China)

机构地区：[1]青岛农业大学化学与药学院,山东青岛266109 [2]山东省临沂市农业局,山东临沂276001

出　　处：《精细化工》2018年第4期652-657,共6页Fine Chemicals

基　　金：国家自然科学基金(31501682);山东省自然科学基金(ZR2014CM039,ZR2014EL012);青岛农业大学高层次人才科研基金(631333)~~

摘　　要：以壳聚糖（CS）和海藻酸钠（ALG）为包封材料,以阿维菌素（AVM）为芯材,采用锐孔法制备了阿维菌素-海藻酸钠-壳聚糖微球,考察了海藻酸钠质量分数、壳聚糖质量分数、氯化钙质量分数和芯壁体积比（质量分数1%的阿维菌素乳液与质量分数3%海藻酸钠溶液的体积比）对微球形态及包埋率的影响,利用SEM、FTIR等对微球结构及性质进行了表征,并考察了其在土壤中的缓释性能和释药机制。结果表明,经优化的制备条件为：海藻酸钠、壳聚糖及氯化钙的质量分数分别为3%、0.6%及5%,芯壁体积比为1∶2,制备的载药微球形状规整,成球性良好,粒径约0.7 mm,载药量31.65%,包埋率83.81%;红外光谱分析显示,芯壁材料之间除氢键外,没有发生化学作用。所制备的阿维菌素微球在土壤中具有缓释特性,42 h累积释药率达到82.06%,之后药物释放减缓。药物释放特性符合Riger-Peppas模型,释放机理为Fick扩散。Chitosan（CS） and sodium alginate（ALG） were used as wall materials,and avermectin（AVM） was used as core material to prepare avermectin sodium alginate/chitosan microspheres through sharp hole method. The effects of sodium alginate mass fraction,chitosan mass fraction,calcium chloride mass fraction and core-wall volume ratio（volume ratio of mass fraction 1% avermectin emulsion and mass fraction 3% sodium alginate solution） on the microsphere morphology and encapsulation efficiency were investigated. The as-prepared microspheres were characterized by SEM and FTIR,and their release properties and mechanism in soil were discussed. The results showed that the optimized preparation conditions were obtained as follows： mass fraction of sodium alginate,chitosan and calcium chloride 3%,0. 6% and 5%,respectively,core-wall volume ratio 1 ∶ 2. Under these conditions,the resulting microspheres had good spherical shape with an average diameter of about0. 7 mm. The drug content and the encapsulation efficiency were 31. 65% and 83. 81%,respectively.FTIR analysis displayed that there was no chemical interaction between core and wall materials except hydrogen bonding. The avermectin sodium alginate/chitosan microspheres exhibited slow release properties in soil the cumulative release rate reached 82. 06% in 42 h,and then the release of the drug decreased. The avermectin release characteristics of microspheres was in accord with Riger-Peppas model,and the release mechanism was Fick diffusion.

关 键 词：阿维菌素 海藻酸钠 壳聚糖 微球 医药原料 

分 类 号：TQ424.2[化学工程]