不同掩味技术在分散片剂配方设计与评价中的实施与比较

Alaa E. Elawni, Zuheir A. Osman, M. Salih, Waleed Elballa, Mohammed E. A. Shayoub
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摘要

本研究的目的是评估几种掩味技术的效果,并研究不同配方变量对以雷尼替丁为模型药物的分散片理化性质的影响。采用多种方法对雷尼替丁粉末进行味掩盖。采用因子设计(24)设计片剂配方。考察了制备方法、填料类型、超崩解剂类型和超崩解剂浓度四个因素。制备方法选择的水平为直接压缩和湿造粒,稀释型为微晶纤维素和甘露醇,超崩解型为乙醇酸淀粉钠和交联纤维素钠,超崩解浓度为2%和10%。用碳酸钙造粒(比例为1:8)是优选的掩味方法。结果表明,制备方法对片剂的重量变化、硬度、脆性、崩解时间等理化指标均有显著影响(p值< 0.05)。交联纤维素钠比乙醇酸淀粉钠效果更好。采用交联棉糖钠浓度为2%的直接压缩法和交联棉糖钠浓度为10%的湿造粒法,两种填料均获得了良好的性能。交联棉糖钠浓度的增加也促进了药物的释放。这些发现代表了一种简单的制造过程,使用相对低成本的材料,可以用于配制苦味药物的分散片,这将提高患者的依从性,并导致更快的起效。
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Implementation and comparison of different taste masking techniques to design and assess dispersible tablet formulations
The objective of this study was to assess the efficacy of several taste-masking techniques and to study the impact of different formulation variables on the physicochemical properties of dispersible tablets containing Ranitidine as a model drug. Ranitidine powder was taste masked using various techniques. Factorial design (24) was applied to design the set of tablet formulations. The four factors implemented were the manufacturing method, filler type, superdisintegrant type and superdisintegrant concentration. Levels selected were direct compression and wet granulation for the manufacturing method, microcrystalline cellulose and mannitol for the diluent type, sodium starch glycolate and croscarmellose sodium for superdisintegrant type, and 2% and 10% for superdisintegrant concentration. Granulation with calcium carbonate (ratio of 1:8) was the taste-masking method of choice to be implemented. The formulated tablets results revealed that the manufacturing method has a significant influence on all the tested physicochemical properties (p-values < 0.05) such as tablet’s weight variation, hardness, friability, and disintegration time. Croscarmellose sodium obtained better results than sodium starch glycolate. Both fillers obtained good properties when implementing direct compression method with croscarmellose sodium concentration of 2%, or wet granulation method with croscarmellose sodium concentration of 10%. Drug release was also increased by increasing concentration of croscarmellose sodium. These findings represent an easy manufacturing procedure with relatively low-cost materials that can be implemented to formulate dispersible tablets of bitter tasting drugs that will enhance patient compliance and lead to faster onset of action.
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