Kovacevic Jovana, Mladenovic Aleksandar, Djuris Jelena, Ibric Svetlana
Department of Pharmaceutical Technology, Faculty of Pharmacy, Belgrade, Serbia.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Belgrade, Serbia.
Eur J Pharm Sci. 2016 Mar 31;85:84-93. doi: 10.1016/j.ejps.2016.01.018. Epub 2016 Jan 18.
Gastro-resistant pellets were prepared by use of three different drug loading techniques (powder layering, solution layering and suspension layering) and two different enteric coating techniques (powder layering and suspension layering). Pellets produced by different layering techniques were compared in terms of morphological characteristics, content of drug, release properties and stability. Drug loaded pellets produced by the use of powder layering had much more pronounced surface roughness in comparison to other tested techniques. Higher weight gains of enteric polymer were needed to achieve the same level of gastric resistance when powder layering was employed to apply enteric layer than when it was applied by suspension layering. Both tested techniques of enteric coating application enabled complete dissolution of drug in buffer stage of dissolution test. Suspension layering proved to be superior to other techniques both in drug loading and enteric layering phase.
采用三种不同的载药技术(粉末层积法、溶液层积法和混悬液层积法)和两种不同的肠溶包衣技术(粉末层积法和混悬液层积法)制备了胃内滞留微丸。比较了不同层积技术制备的微丸在形态特征、药物含量、释放特性和稳定性方面的差异。与其他测试技术相比,采用粉末层积法制备的载药微丸表面粗糙度更为明显。采用粉末层积法包衣肠溶层时,要达到相同的抗胃酸性水平,需要更高的肠溶聚合物增重,而采用混悬液层积法时则不然。两种测试的肠溶包衣应用技术均能使药物在溶出试验的缓冲阶段完全溶解。混悬液层积法在载药和肠溶包衣阶段均优于其他技术。