A Comparative Study of Solubility Enhancement of Aceclofenac by Solid Dispersion Technique Using Several Polymers

M. Sarangi, Neha Singh
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引用次数: 10

Abstract

The attempt has been made to compare the aqueous solubility and dissolution characteristics of Aceclofenac (ACE) enhanced by solid dispersion technique using several water soluble carriers PEG 6000, β-Cyclodextrin (β –CD) and Sodium Carboxy methyl cellulose (Na-CMC). Solid dispersions of ACE were prepared with solvent evaporation method. Solid dispersions with carriers were prepared in drug: carrier (1:1, 1:2, 1:3 and 1:4) ratios. The prepared dispersions were evaluated by solubility, in vitro dissolution studies and X-Ray diffraction studies (XRD). The results from XRD analysis showed that ACE might exist in an amorphous state in the solid dispersion. Considerably improved dissolution profile was obtained by PEG ratios (1:2), whereas there was no significant improvement in dissolution of ACE along with β-CD at higher carrier ratios. Na- CMC showed least dissolution improvement among all carriers. The solid dispersion prepared as AC: PEG 6000 (1:2), exhibited the fastest dissolution among all solid dispersions, was formulated into tablets using direct compression method and further compared with immediate release marketed brands of ACE. The results indicated that formulated tablets displayed better dissolution profiles as compared to existing commercial tablets.
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几种聚合物固体分散技术增强乙酰氯芬酸溶解度的比较研究
以PEG 6000、β-环糊精(β -CD)和羧甲基纤维素钠(Na-CMC)为载体,对固相分散技术增强的乙酰氯芬酸(ACE)的水溶性和溶出特性进行了比较。采用溶剂蒸发法制备了ACE的固体分散体。以药物与载体(1:1、1:2、1:3、1:4)的比例制备载体固体分散体。通过溶解度、体外溶出度和x射线衍射(XRD)对所制备的分散体进行了评价。XRD分析结果表明,ACE在固体分散体系中可能以非晶态存在。PEG比(1:2)显著改善了β-CD的溶出,而在较高的载体比下,ACE和β-CD的溶出没有显著改善。Na- CMC在所有载体中溶出改善最小。制备的固体分散体为AC: PEG 6000(1:2),在所有固体分散体中溶出最快,采用直接压缩法配制成片剂,并与即刻释放的ACE市售品牌进行比较。结果表明,与现有的市售片剂相比,该制剂具有更好的溶出度。
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