新型协同加工辅料对阿司匹林片剂快速崩解的评价

O. Olayemi, Sophie Nock-Anyebe
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引用次数: 1

摘要

协同加工是一种确保单个赋形剂的亚颗粒相互作用,从而导致最终赋形剂的整体功能的技术。以香附淀粉和甘露醇为原料,采用融合法制备香附淀粉,考察其对片剂崩解和体外溶出度的影响。以香附淀粉和甘露醇为原料,以1:1、1:2和2:1的比例(分别为CM2、CM2和CM3)融合制备共加工辅料,并对其流动和膨胀性能进行评价。采用FM1、FM2、FM3直接压缩法,以5% w/w的比例加入阿司匹林片剂中。以乙醇酸淀粉钠(FSG)为原料制备了类似的片剂,并对其硬度、脆度、湿润时间、崩解时间和体外溶出度进行了评价。所有辅料均具有良好的流动性,Carr指数在17.31 ~ 20.78之间,Hausner比值在1.21 ~ 1.26之间。CM3肿胀剖面最高(1.491),CM2肿胀剖面最低(1.321)。配方FM1的抗拉强度最高(14.12 N/cm2),但润湿时间较FM3慢(34.33秒),其抗拉强度为11.32 N/cm2,润湿时间为9.00秒,崩解时间为4.26 min,与FSG相当(4.01 min);它们的溶出谱也很相似。以2:1的比例融合处理香附淀粉和甘露醇,影响片剂的崩解和体外溶出度,有潜力用于速溶片剂的生产。关键词:Co-processing;香柏淀粉;甘露醇;解体;解散
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Evaluation of Novel co-processed excipient for fast disintegration of aspirin tablet formulations
Co-processing is a technique that ensures sub-particulate interaction of individual excipients leading to overall functionality of the resulting excipient. The aim of this study is to co-process Cyperus esculentus starch with mannitol by fusion and evaluate its effect on tablet disintegration and in vitro dissolution. Co-processed excipients were prepared from Cyperus esculentus starch and mannitol by fusion in ratios of 1:1, 1:2 and 2:1 (CM1, CM2, and CM3 respectively) and evaluated for flow and swelling properties. The excipients were incorporated into Aspirin tablet formulations at 5 %w/w by direct compression (FM1, FM2, FM3 respectively). Similar tablets were prepared using sodium starch glycolate (FSG) and the formulations were assessed for hardness, friability, wetting time, disintegrationtime and in vitro dissolution profile. All the prepared excipients possessed excellent flow with Carr’s index between 17.31 and 20.78 and Hausner ratio between 1.21 and 1.26. CM3 had the highest swelling profile (1.491) while CM2 had the lowest (1.321). Formulation FM1 had the highest tensile strength (14.12 N/cm2 ) but slower wetting time (34.33 sec) compared to FM3 with tensile strength of 11.32 N/cm2 and wetting time of 9.00 sec. Disintegration time of CM3 (4.26 min) was comparable to that of FSG (4.01 min); their dissolution profile was also found to be similar. Coprocessing Cyperus esculentus starch and mannitol by fusion (2:1) influenced tablet  disintegration and in vitro dissolution and has potential to be used in manufacture of fast dissolving tablet formulations. Keywords: Co-processing; Cyperus esculentus starch; Mannitol; Disintegration; Dissolution
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