Department of Pharmaceutics, Semmelweis University, 7-9 Hogyes E. Street, 1092 Budapest, Hungary.
AAPS PharmSciTech. 2010 Mar;11(1):383-91. doi: 10.1208/s12249-010-9396-x. Epub 2010 Mar 17.
The objective of the present study was to investigate the effect of the pellet core materials isomalt, sugar, and microcrystalline cellulose on the in vitro drug release kinetics of coated sustained-release pellets as well as to evaluate the influence of different ratios of polymethacrylate copolymers exhibiting different permeability characteristics on the drug release rate. For characterization of the drug release process of pellets, the effect of osmolality was studied using glucose as an osmotically active agent in the dissolution medium. The pellet cores were layered with diclofenac sodium as model drug and coated with different ratios of Eudragit RS30D and Eudragit RL30D (ERS and ERL; 0:1 and 0.5:0.5 and 1:0 ratio) in a fluid bed apparatus. Physical characteristics such as mechanical strength, shape, and size proved that the inert cores were adequate for further processing. The in vitro dissolution tests were performed using a USP Apparatus I (basket method). The results demonstrated that, besides the ratio of the coating polymers (ERS/ERL), the release mechanism was also influenced by the type of starter core used. Sugar- and isomalt-type pellet cores demonstrated similar drug release profiles.
本研究的目的是研究丸芯材料异麦芽酮糖醇、糖和微晶纤维素对包衣缓释丸的体外药物释放动力学的影响，并评估具有不同渗透特性的不同比例的多甲基丙烯酸酯共聚物对药物释放速率的影响。为了对丸剂的药物释放过程进行特征描述，使用葡萄糖作为溶出介质中的渗透活性物质研究了渗透压的影响。丸芯采用双氯芬酸钠作为模型药物，并在流化床设备中用不同比例的 Eudragit RS30D 和 Eudragit RL30D（ERS 和 ERL；0:1 和 0.5:0.5 和 1:0 比）进行包衣。机械强度、形状和尺寸等物理特性证明惰性丸芯足以进行进一步加工。体外溶解试验采用 USP 装置 I（篮法）进行。结果表明，除了包衣聚合物的比例（ERS/ERL）外，释放机制还受到起始丸芯类型的影响。糖型和异麦芽酮糖醇型丸芯表现出相似的药物释放曲线。
