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Enhancement of Loperamide Dissolution Rate by Liquisolid Compact Technique

机译:液固紧凑技术提高洛哌丁胺的溶出度

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摘要

>Purpose: The aim of present study was to improve the dissolution rate of poorly soluble drug Loperamide (LPM) by liquisolid compact technique. >Methods: Liquisolid compacts of LPM were prepared using Propylene glycol (PG) as a solvent, Avicel pH 102 as carrier, Aerosil as coating material and Sodium Starch Glycolate (SSG) as superdisintegrant. Interactions between the drug and excipients were examined by Fourier Transform Infrared (FTIR) spectroscopy. The dissolution studies for LPM liquisolid formulation, marketed product and pure drug were carried out in pH 1.2 HCl buffer as dissolution media. >Results: Results confirmed the absence of chemical interactions between the drug and excipients. From the solubility studies, it was observed the LPM was highly soluble in PG thereby it was selected as a solvent. The dissolution efficiency of LPM at 15 min was increased from 9.99 % for pure drug and 54.57% for marketed product to 86.81% for the tablets prepared by liquisolid compact technique. Stability studies showed no significant change in percent cumulative drug release, hardness, disintegration time, friability and drug content for 3 months. >Conclusion: Formulation F2 showed significant increase in dissolution rate compared to the marketed product at pH 1.2 where LPM is largely absorbed. Around 90% of the drug was released from F2 in 30 min compared to the marketed product and it might be due to the increased wetting and surface area of the particles. Hence, the liquisolid compact technique appears to be a promising approach for improving the dissolution rate of poorly soluble drug.
机译:>目的:本研究的目的是通过液固紧凑技术提高难溶性药物洛哌丁胺(LPM)的溶出度。 >方法:使用丙二醇(PG)作为溶剂,Avicel pH 102作为载体,Aerosil作为包衣材料以及乙醇酸淀粉钠(SSG)作为超崩解剂制备LPM液体固体压块。通过傅立叶变换红外(FTIR)光谱检查了药物与赋形剂之间的相互作用。 LPM液状固体制剂,市售产品和纯药物的溶出度研究是在pH 1.2 HCl缓冲液中作为溶出介质进行的。 >结果:结果证实了药物与赋形剂之间不存在化学相互作用。从溶解度研究中,观察到LPM在PG中高度可溶,因此被选择作为溶剂。 LPM在15分钟时的溶出效率从纯药物的9.99%和市售产品的54.57%提高到通过液固紧密技术制备的片剂的86.81%。稳定性研究表明3个月内累积药物释放百分比,硬度,崩解时间,易碎性和药物含量没有明显变化。 >结论:与市场上销售的LPM含量较高的pH 1.2相比,配方F2的溶出度显着提高。与市售产品相比,约有90%的药物在30分钟内从F2释放出来,这可能是由于颗粒的润湿性和表面积增加所致。因此,液固紧实技术似乎是改善难溶性药物的溶解速率的有前途的方法。

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