ABSTRACT

The present investigation aims at development of extended release (ER) pellets using κ-carrageenan-montmorillonite (κ-Carr-MMT) polyelectrolyte complex (PEC) hydrogel. The PEC was used as binder and ER polymer, whereas tapentadol was a model drug. The hydrogels were optimised using 32 full factorial design and characterised by FTIR, DSC, XRPD, and SEM analyses. The pelletisation was done using extrusion-spheronization procedure. The prepared pellets were further characterised for yield, FTIR, DSC, XRPD, pellet morphology, flow characteristics, mucoadhesion, and in vitro drug release studies. The interactions between the cationic silicate hydroxylated edge groups of MMT with the anionic sulphate group of κ-carrageenan leads to the formation of κ-Carr-MMT PEC hydrogel and these interactions were confirmed by FTIR analysis. The optimised pellet formulation containing 2.25:1.00 ratio of κ-Carr and MMT exhibited sustained drug release upto 12 h, in vitro. Present ER pellet formulation could be a best alternative to the conventional formulations for pain management.

摘要

本研究旨在开发使用 κ-角叉菜胶-蒙脱石 (κ-Carr-MMT) 聚电解质复合物 (PEC) 水凝胶的缓释 (ER) 微丸。PEC用作粘合剂和ER聚合物，而他喷他多是模型药物。使用 32 个全因子设计对水凝胶进行优化，并通过 FTIR、DSC、XRPD 和 SEM 分析对其进行表征。使用挤出-滚圆程序进行造粒。制备的微丸进一步表征了产量、FTIR、DSC、XRPD、微丸形态、流动特性、粘膜粘附和体外药物释放研究。MMT 的阳离子硅酸盐羟基化边缘基团与 κ-角叉菜胶的阴离子硫酸盐基团之间的相互作用导致形成 κ-Carr-MMT PEC 水凝胶，这些相互作用通过 FTIR 分析得到证实。含有 2.25:1.00 比例的 κ-Carr 和 MMT 的优化微丸制剂在体外表现出长达 12 小时的持续药物释放。目前的缓释颗粒配方可能是传统疼痛管理配方的最佳替代品。