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热烧结:盐酸普萘洛尔胃滞留漂浮片设计中的一种新技术及其评价

Thermal sintering: a novel technique in the design of gastroretentive floating tablets of propranolol HCl and its evaluation.

作者信息

Meka Venkata Srikanth, Songa Ambedkar Sunil, Nali Sreenivasa Rao, Battu Janaki Ram, Kukati Latha, Kolapalli Venkata Ramana Murthy

机构信息

School of Pharmacy, International Medical University (IMU), Kuala Lumpur, Malaysia.

出版信息

Invest Clin. 2012 Sep;53(3):223-36.

Abstract

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.

摘要

本研究的目的是制备盐酸普萘洛尔热烧结漂浮片,并研究烧结条件对药物释放的影响及其体外漂浮特性。选择亲水性聚合物聚环氧乙烷作为烧结聚合物以延缓药物释放。通过直接压片法制备制剂,并通过体外溶出度研究进行评价。结果表明,烧结温度和暴露时间对漂浮性以及溶出特性有很大影响。随着烧结温度和暴露时间的增加,发现漂浮滞后时间缩短,总漂浮时间延长,药物释放受到抑制。基于其药物缓释特性,选择了优化的烧结制剂(烧结温度50℃,暴露时间4小时)。采用傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)对优化后的制剂进行了表征,未发现药物与所用聚合物之间存在相互作用。

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