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Taste masking of diclofenac sodium using microencapsulation

机译:使用微胶囊掩盖双氯芬酸钠的味道

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This study addresses how to mask the undesirable ttaste of diclofenas sodium (DS) without interfering with an adequate rate of drug release. DS microcapsules were successfully prepared using a system of ethylcellulose (EC) - toluene-petroleum ether. The system was optimized by the construction of the phase diagram and determination of the amount of EC precipitated under different solvent:non-solvent ratios to determine the most appropriate conditions for preparing good microcapsules. Microcrystalline cellulose (Avicel) and lactose were mixed with DS powder and conferted into spherical cores by the wet agglomeration technique which facilitated coacervation and formation of thin and uniform microcapsule walls. Diethylphthalate (DEP) and Polyethyleneglycol 600 (PEG) in different cocentrations (20 or 40% w/w) were used as plasticizers to impart better elasticity to the microcapsules. The microcapsules were evaluated for DS released against crushed commercial DS enteric coated tablet (Voltaren). The prepared microcapsules were taste evaluated by a taste panel of 10 volunteers. The results revealed that the optimum solvent:non-xolvent ratio required for microcapsule formation was 1:2 Microcapsules containing PEG 20% or DEP 40% showed a faster rate of DS release compared to that obtained from other microcapsules and crushed commercial enteric coated tablets (Voltaren). The palatability and the taste of DS were significantly improved by microencapsulation. The extent of taste masking was influenced by the microcapsule core:wall ratio, the presence of additives within the core, the type and concentrtion of plasticizer and initial core size.
机译:这项研究解决了如何在不干扰足够的药物释放速率的情况下掩盖双氯芬酸钠(DS)的不良味道。使用乙基纤维素(EC)-甲苯-石油醚系统成功制备了DS微胶囊。通过构建相图并确定在不同溶剂:非溶剂比率下沉淀的EC的量来确定最合适的条件,以制备好的微胶囊,从而对该系统进行了优化。将微晶纤维素(Avicel)和乳糖与DS粉混合,并通过湿附聚技术将其制成球形核,从而促进凝聚并形成薄而均匀的微胶囊壁。使用不同浓度(20或40%w / w)的邻苯二甲酸二乙酯(DEP)和聚乙二醇600(PEG)作为增塑剂,以赋予微胶囊更好的弹性。评估微胶囊相对于压碎的商业DS肠溶衣片剂(Voltaren)释放的DS。由10名志愿者的味觉小组对制备的微胶囊进行味觉评价。结果表明,微胶囊形成所需的最佳溶剂:非溶剂比为1:2,与从其他微胶囊和粉碎的市售肠溶衣片剂中获得的相比,含PEG 20%或DEP 40%的微胶囊的DS释放速率更快( Voltaren)。微囊化显着改善了DS的适口性和味道。掩味的程度受微胶囊核心:壁比,核心中添加剂的存在,增塑剂的类型和浓度以及初始核心尺寸的影响。

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