Gohel M C, Amin A F, Patel K V, Panchal M K
Department of Pharmaceutics and Pharmaceutical Technology, L. M. College of Pharmacy, Navrangpura, India.
Boll Chim Farm. 2002 Jan-Feb;141(1):21-8.
(Hydroxypropyl)methyl cellulose and xanthan gum were used as hydrophilic matrixing agents for preparing modified release tablets of diltiazem HCl. The amount of (Hydroxypropyl)methyl cellulose and xanthan gum exhibited significant effect on drug release from the tablets prepared by direct compression technique. Xanthan gum showed a higher ability to retard the drug release than (Hydroxypropyl)methyl cellulose. A 2(2) + 1 factorial design was adopted to study the effect of amount of (Hydroxypropyl)methyl cellulose and xanthan gum on percent drug released in first hour (Y60) and the time required for 90% drug dissolution (t90). A response surface plot is generated for investigating the effect of the independent variables on t90. The tablets containing 90 mg diltiazem HCl, 45 mg (Hydroxypropyl)methyl cellulose and 45 mg xanthan gum showed drug release upto 12 h. The value of similarity factor, f2, for the selected batch was found to be 85.1 when the dissolution study was carried out in water or simulated gastric fluid, indicating pH independent drug dissolution. The selected batch also showed a comparable release profile with a market product (f2 = 60.2). Linear relationship was observed between percent drug released and degree of swelling. The kinetics of the drug release fitted well to the Hixson-Crowell equation. It can be concluded that by using a suitable blend of (Hydroxypropyl)methyl cellulose and xanthan gum desired modified drug release can be achieved.
羟丙基甲基纤维素和黄原胶被用作制备盐酸地尔硫卓缓释片的亲水性基质剂。羟丙基甲基纤维素和黄原胶的用量对采用直接压片技术制备的片剂的药物释放有显著影响。黄原胶比羟丙基甲基纤维素表现出更高的延缓药物释放的能力。采用2(2)+1析因设计研究羟丙基甲基纤维素和黄原胶用量对第一小时药物释放百分比(Y60)和90%药物溶解所需时间(t90)的影响。生成响应面图以研究自变量对t90的影响。含有90mg盐酸地尔硫卓、45mg羟丙基甲基纤维素和45mg黄原胶的片剂显示药物释放长达12小时。当在水或模拟胃液中进行溶出度研究时，所选批次的相似因子f2值为85.1，表明药物溶出与pH无关。所选批次与市售产品也显示出相当的释放曲线(f2 =
