Abstract

The aim of the present investigation is to develop zaltoprofen-loaded extended-release (ER) pellets formulation by an extrusion-spheronization technique using glyoxalated pre-gelatinized starch (GPS) complex as a novel matrix-forming polymer. The prime objective was to prepare an efficient and robust ER drug delivery system of zaltoprofen. Pellets were characterized by physicochemical, morphological, and solid-state characterization. The formulation was also analyzed for in-vitro drug release and in-vivo pharmacokinetic parameters. The FTIR analysis confirmed the GPS complex formation through the formation of the hemiacetal group while the ketone groups of glyoxal are abolished. Optimized formulation G5 containing 5:8 ratio of GPS complex and MCC showed 99.03 ± 2.12 percent cumulative drug releases in 14 h. The in-vivo study showed decreased C_max and increased t_1/2 compared to bulk zaltoprofen, and hence would be a viable alternative for ER-type formulations. In the author’s opinion, the GPS-based ER pellet formulation would be an excellent delivery system for zaltoprofen.

摘要

本研究的目的是通过使用乙二醛化预糊化淀粉 (GPS) 复合物作为新型基质形成聚合物的挤压滚圆技术开发载有扎托洛芬的缓释 (ER) 微丸制剂。主要目标是制备一种有效且强大的扎托洛芬 ER 药物递送系统。通过物理化学、形态学和固态表征来表征颗粒。还分析了制剂的体外药物释放和体内药代动力学参数。FTIR分析通过半缩醛基团的形成证实了GPS复合物的形成，而乙二醛的酮基团被消除。包含 5:8 比例的 GPS 复合物和 MCC 的优化配方 G5 在 14 小时内显示出 99.03 ± 2.12% 的累积药物释放。体内研究表明，与散装扎托洛芬相比，C max 降低，t _1/2增加_，因此将是 ER 型制剂的可行替代品。在作者看来，基于 GPS 的 ER 微丸制剂将是一种出色的 zaltoprofen 递送系统。