Siahi Mohammad Reza, Barzegar-Jalali Mohammad, Monajjemzadeh Farnaz, Ghaffari Fatemeh, Azarmi Shirzad
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran.
AAPS PharmSciTech. 2005 Dec 7;6(4):E626-32. doi: 10.1208/pt060477.
The present study was performed to design oral controlled delivery systems for the water-soluble drug, verapamil hydrochloride, using natural and semisynthetic polymers as carriers in the forms of 1- and 3-layer matrix tablets. Verapamil hydrochloride 1-layer matrix tablets containing hydroxypropylmethylcellulose, tragacanth, and acacia either alone or mixed were prepared by direct compression technique. 3-layer matrix tablets were prepared by compressing the polymers as release retardant layers on both sides of the core containing the drug. The prepared tablets were subjected to in vitro drug release studies. Tragacanth when used as the carrier in the formulation of 1- and 3-layer matrices produced satisfactory release prolongation either alone or in combination with the other 2 polymers. On the other hand, acacia did not show enough prolonging efficiency in 1- and 3-layer matrix tablets. The results also showed that the location of the polymers in the 3-layer tablets has a pronounced effect on the drug release. Kinetic analysis of drug release from matrices exhibiting sustained release indicated that release was predominantly attributable to the contribution made by Fickian diffusion, while the erosion/relaxation mechanisms had a minor role in the release.
本研究旨在以天然和半合成聚合物为载体,采用单层和三层基质片剂的形式,设计用于水溶性药物盐酸维拉帕米的口服控释系统。通过直接压片技术制备了单独或混合含有羟丙基甲基纤维素、黄芪胶和阿拉伯胶的盐酸维拉帕米单层基质片剂。三层基质片剂是通过将聚合物作为缓释层压在含有药物的核心两侧来制备的。对制备的片剂进行体外药物释放研究。黄芪胶在单层和三层基质制剂中单独或与其他两种聚合物组合用作载体时,均可产生令人满意的释放延长效果。另一方面,阿拉伯胶在单层和三层基质片剂中未显示出足够的延长效率。结果还表明,聚合物在三层片剂中的位置对药物释放有显著影响。对表现出缓释的基质的药物释放进行动力学分析表明,释放主要归因于菲克扩散的贡献,而侵蚀/松弛机制在释放中起次要作用。