摘要

酒石酸美托洛尔基质缓释片配方的研制及体外评价

作者(年代):Ramesh V. Shinde, Dattatreya B. Udgirkar和K. Sreenivasa Rao

在本研究中，选择酒石酸美托洛尔(MT)作为模型药物，它是一种-1选择性肾上腺素能阻滞剂，广泛用于高血压等多种心血管疾病;但因其半衰期短(3 ~ 4小时)、水溶性高，被选为缓释基质片的合适候选制剂。以羟丙基甲基纤维素(hpmc15cps)、羧甲基纤维素钠(NaCMC)、瓜尔胶(GG)等亲水聚合物为缓释剂，配制成基质片。所有预压参数如休止角、豪斯纳比和卡尔指数均在标准范围内。对片剂进行硬度、脆性、厚度、药物含量、体外释放度、溶胀和稳定性评价。研究了聚合物浓度、二元聚合物混合物和湿法制粒方法对药物释放谱的影响。观察到聚合物的种类和浓度对基质片的释药效果有影响。含有HPMC和羧甲基纤维素钠混合物的基质片成功地维持了酒石酸美托洛尔12小时的释放。挤压前参数表明，用于制备片剂的颗粒是自由流动的。压缩后的硬度、脆性、厚度、药物含量等参数均在可接受范围内。 The concentration of metoprolol tartrate was kept constant (100 mg) Formulation containing only a single polymer could not control the release of metoprolol tartrate. The sustained release from sodium carboxy methyl cellulose and hydroxy propyl methyl cellulose combination was due to interaction between ionic polymer and non-ionic polymer, which resulted in favorable increase in the water uptake capacity and gel viscosity leading to a better control over the release of metoprolol tartrate. HC1 and HC2 showed the sustained release of metoprolol tartrate as desired. Model fitting data showed good correlation coefficient with Higuchi’s kinetics. The study revealed that the combination of NaCMC and HPMC can be used for the formulation of sustained release matrix tablets of metoprolol tartrate.