The role of formulation excipients in the development of lyophilised fast-disintegrating tablets
The role of formulation excipients in the development of lyophilised fast-disintegrating tablets
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DOI：
10.1016/j.ejpb.2008.11.011
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发表时间：
2009-05-01
影响因子：
4.9
通讯作者：
Mohammed, Afzal R.
中科院分区：
文献类型：
--
作者：
Chandrasekhar, Rahul;Hassan, Zahra;Mohammed, Afzal R.
尽管最近取得了成功，但许多快速崩解片(FDT)仍然面临机械强度低、口感差和崩解时间较长的问题。这项研究旨在使用渐进的三阶段方法来优化FDTS。在每个阶段对处方进行了一系列的硬度、可裂性和崩解时间测试。在第一阶段，制备浓度在2%至5%(w/w)之间的片剂，并在每个浓度下用75和225个BSG配制成单一和组合BSG(BSG)。分析表明，随着明胶浓度的增加，硬度和崩解时间都增加。5%明胶)FDT的50：50比例为75：225BSG(硬度：13.7+/-0.9N，崩解时间：24.1+/-0.6S)被认为是最理想的，并被延续到阶段II：添加浓度在10%至80%w/w的山梨醇、甘露醇和蔗糖。含有甘露醇的处方(50%-硬度：30.9+/-2.8N，崩解时间：13.3+/-2.1 S)表现出最好的性能，这些都延续到了下一个阶段：添加粘度调节聚合物以改善口感并帮助胃部前滞留。加入卡波姆974P-NF可增加片剂的粘度，但降低了片剂的硬度，而Pluronic F127(6%)的崩解时间和粘度随机械推进力的保持而增加。(C)2008爱思唯尔B.V.保留所有权利。
Despite recent Success, many fast-disintegrating tablets (FDTs) still face problems of low mechanical strength, poor mouth-feel and higher disintegration times. This Study aimed to optimise FDTS using a progressive three-stage approach. A series of hardness, fracturability and disintegration time tests were performed on the formulations at each stage. During Stage 1, tablets were prepared in concentrations between 2% and 5% w/w, and were formulated at each concentration as single and combination bloom strength gelatin (BSG) using 75 and 225 BSGs. Analysis revealed that both hardness and disintegration time increased with an increase in gelatin concentration. A combination (5% gelatin) FDT comprising a 50:50 ratio of 75:225 BSGs (hardness: 13.7 +/- 0.9 N and disintegration time: 24.1 +/- 0.6 s) was judged the most ideal, and was carried forward to Stage II: the addition of the saccharides sorbitol, mannitol and sucrose in concentrations between 10% and 80% w/w. The best properties were exhibited by mannitol-containing formulations (50%-hardness: 30.9 +/- 2.8 N and disintegration time: 13.3 +/- 2.1 s), which were carried forward to the next stage: the addition of viscosity-modifying polymers to improve mouth-feel and aid pre-gastric retention. Addition of carbopol 974P-NF resulted in the enhancement of viscosity with a compromise of the hardness of the tablet, whereas Pluronic F127 (6%) showed an increase in disintegration time and viscosity with retention of mechanical propel-ties. (C) 2008 Elsevier B.V. All rights reserved.