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以甲氨基阿维菌素苯甲酸盐(以下简称甲维盐)为芯材,以生物可降解材料聚乳酸(PLA)为壁材,采用溶剂挥发法制备了甲维盐缓释微球,分别考察了反应温度、芯壁材质量比、聚乳酸质量浓度对微球形态、粒径、载药量和包封率的影响。结果表明:在聚乳酸质量浓度和芯壁材质量比值固定不变时,温度保持20℃,微球的粒径、载药量、包封率均达到最佳;而固定其他条件不变,若增加聚乳酸的质量浓度,则微球的载药量、包封率和粒径也随之增加;当芯壁材质量比由1∶1变化到1∶5时,微球粒径和载药量均逐渐减小,而包封率则在芯壁材质量比为1∶1至1∶4之间逐渐增大,最大值为97.8%。电镜扫描结果显示,当芯壁材质量比在1∶3至1∶5之间时,微球呈现光滑完整的球形。差示扫描量热检测结果显示,甲维盐和聚乳酸能够有机地结合为一体。微球释药性研究表明,甲维盐聚乳酸微球具备明显的缓释性能。
The emamectin benzoate (hereinafter referred to as carbazole salt) as the core material, polylactic acid (PLA) as the biodegradable material for the wall material, the use of solvent evaporation prepared a dimension sustained-release microspheres, The effects of reaction temperature, mass ratio of core material and polylactic acid concentration on microsphere morphology, particle size, drug loading and entrapment efficiency were investigated. The results showed that when the mass concentration of polylactic acid and the ratio of core wall material were constant, the particle size, drug loading and entrapment efficiency of the microspheres reached the best when the temperature was kept at 20 ℃, while the other conditions were unchanged. Increasing the mass concentration of polylactic acid, the drug loading, entrapment efficiency and particle size of microspheres also increased. When the ratio of core material to wall material was changed from 1: 1 to 1: 5, the microsphere size and drug loading The volume decreases gradually, while the entrapment efficiency increases gradually with the mass ratio of core wall material between 1: 1 and 1: 4, and the maximum value is 97.8%. Electron microscopy results showed that when the mass ratio of core wall material was between 1: 3 and 1: 5, the microspheres showed a smooth and complete sphere. Differential Scanning Calorimetry results showed that the carbaryl and polylactic acid can be organically combined into one. Studies on drug release of microspheres showed that the carbaryl polylactic acid microspheres had obvious sustained release properties.