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Modified Polysaccharides as Fast Disintegrating Excipients for Orodispersible Tablets of Roxithromycin

机译:改性多糖作为罗红霉素口腔分散片的快速崩解赋形剂

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摘要

The purpose of this study was to develop a dosage form that was easy to administer and provides rapid release of the drug roxithromycin, using modified polysaccharides as rapidly disintegrating excipients. Modified polysaccharides co grinded treated agar (C-TAG) and co grinded treated guar gum (C-TGG) were prepared by subjecting pure polysaccharides namely agar and guar gum respectively to sequential processes of wetting, drying and co grinding with mannitol (1:1). The modified polysaccharides were characterized by Scanning Electron Microscopy and Diffuse Reflectance Spectroscopy and evaluated for particle size distribution, derived properties, swelling index and biodegradability. Optimization studies based on 22 factorial designs, with friability and disintegration time as response parameters were used to formulate orodispersible tablets of roxithromycin and evaluated for wetting time, water absorption ratio and in vitro drug release at salivary pH 6.4 and physiological pH 7.4. Results indicated that lower levels of modified polysaccharides namely C-TAG in F3 and C-TGG in F7 and higher levels of microcrystalline cellulose, exhibited least disintegration times without friability concerns. In vitro release of optimized formulations F3 and F7, both at salivary pH and physiological pH was found to be more than 90% within 30 min as compared to 27.82% at the same time point of conventional formulation. Stability studies carried out as per ICH Q1A guidelines suggested the formulations to be stable for a period of 6 months. Thus the approach of using modified polysaccharides as fast disintegrating excipient can be used to formulate a stable orodispersible formulation.
机译:这项研究的目的是开发一种易于使用的剂型,并使用修饰的多糖作为快速崩解的赋形剂提供罗红霉素的快速释放。通过分别对纯多糖即琼脂和瓜尔豆胶进行润湿,干燥和与甘露醇共研磨的顺序过程(1:1),制备共研磨处理的琼脂(C-TAG)和瓜研磨的瓜尔豆胶(C-TGG)的改性多糖。 )。通过扫描电子显微镜和漫反射光谱对改性的多糖进行表征,并评估其粒度分布,衍生性质,溶胀指数和生物降解性。以2 2 因子设计为基础的优化研究,以脆性和崩解时间为响应参数来制备罗红霉素的口腔分散片,并评估其在唾液pH值6.4下的润湿时间,吸水率和体外药物释放和生理pH值7.4。结果表明,较低水平的修饰多糖,即F3中的C-TAG和F7中的C-TGG,以及较高水平的微晶纤维素,具有最短的崩解时间,而无需担心脆性。发现在唾液pH值和生理pH值下,优化配方F3和F7的体外释放在30分钟内超过90%,而常规配方同时达到27.82%。根据ICH Q1A指南进行的稳定性研究表明,该制剂在6个月内稳定。因此,使用修饰的多糖作为快速崩解赋形剂的方法可用于配制稳定的口腔分散制剂。

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