Srivastava A K, Wadhwa Saurabh, Ridhurkar D, Mishra B
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India.
Drug Dev Ind Pharm. 2005 May;31(4-5):367-74. doi: 10.1081/ddc-54313.
Floating matrix tablets of atenolol were developed to prolong gastric residence time and increase drug bioavailability. Atenolol was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by direct compression technique, using polymers such as hydroxypropyl methylcellulose (HPMC K15M, K4M), guargum (GG), and sodium carboxymethylcellulose (SCMC), alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, swelling index, floating capacity, thickness, and weight variation. Further, tablets were evaluated for in vitro release characteristics for 8 hr. The effect of effervescent on buoyancy and drug release pattern was also studied. In vitro release mechanism was evaluated by linear regression analysis. GG- and SCMC-based matrix tablets showed significantly greater swelling indices compared with other batches. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium.
开发阿替洛尔漂浮型骨架片是为了延长药物在胃内的滞留时间并提高药物的生物利用度。选择阿替洛尔作为模型药物是因为它在下消化道的吸收较差。该片剂采用直接压片技术制备,使用了诸如羟丙基甲基纤维素(HPMC K15M、K4M)、瓜尔胶(GG)和羧甲基纤维素钠(SCMC)等聚合物,单独使用或组合使用,以及其他标准辅料。对片剂的物理特性如硬度、膨胀指数、漂浮能力、厚度和重量差异进行了评估。此外,对片剂进行了8小时的体外释放特性评估。还研究了泡腾剂对浮力和药物释放模式的影响。通过线性回归分析评估体外释放机制。与其他批次相比,基于GG和SCMC的骨架片显示出显著更高的膨胀指数。该片剂在漂浮于溶出介质上方时呈现出可控且延长的药物释放曲线。