Abdelkader Hamdy, Abdalla Ossama Youssef, Salem Hesham
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.
AAPS PharmSciTech. 2007 Nov 30;8(4):E100. doi: 10.1208/pt0804100.
This work aims at investigating different types and levels of hydrophilic matrixing agents, including methylcellulose (MC), sodium alginate (Alg), and sodium carboxymethylcellulose (CMC), in an attempt to formulate controlled-release matrix tablets containing 25 mg baclofen. The tablets were prepared by wet granulation. Prior to compression, the prepared granules were evaluated for flow and compression characteristics. In vitro, newly formulated controlled-release tablets were compared with standard commercial tablets (Lioresal and baclofen). The excipients used in this study did not alter physicochemical properties of the drug, as tested by the thermal analysis using differential scanning calorimetry. The flow and compression characteristics of the prepared granules significantly improved by virtue of granulation process. Also, the prepared matrix tablets showed good mechanical properties (hardness and friability). MC- and Alg-based tablet formulations showed high release-retarding efficiency, and good reproducibility and stability of the drug release profiles when stored for 6 months in ambient room conditions, suggesting that MC and Alg are good candidates for preparing modified-release baclofen tablet formulations.
本研究旨在考察不同类型和水平的亲水性基质剂,包括甲基纤维素(MC)、海藻酸钠(Alg)和羧甲基纤维素钠(CMC),以制备含25 mg巴氯芬的控释基质片。片剂采用湿法制粒制备。在压片前,对制备的颗粒进行流动性和压缩特性评估。在体外,将新制备的控释片与标准市售片(力奥来素和巴氯芬)进行比较。本研究中使用的辅料未改变药物的理化性质,这通过差示扫描量热法的热分析得到验证。通过制粒过程,制备颗粒的流动性和压缩特性得到显著改善。此外,制备的基质片表现出良好的机械性能(硬度和脆碎度)。基于MC和Alg的片剂配方显示出高缓释效率,并且在室温条件下储存6个月时药物释放曲线具有良好的重现性和稳定性,这表明MC和Alg是制备巴氯芬缓释片剂配方的良好候选材料。