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Solubility and Dissolution Enhancement of Etoricoxib by Solid Dispersion Technique Using Sugar Carriers

机译:糖载体的固体分散技术提高依托考昔的溶解度和溶解度

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摘要

The aim of the present study was to improve solubility and dissolution of the poorly aqueous soluble drug, etoricoxib by solvent evaporation technique using various sugar carriers, such as lactose, sucrose, and mannitol. Etoricoxib solid dispersions and their respective physical mixtures using lactose, sucrose, and mannitol were prepared in different ratios by solvent evaporation technique. The percent yield, drug content, saturation solubility, and in vitro dissolution of etoricoxib solid dispersions and physical mixtures were analyzed. Etoricoxib solid dispersions were characterized by FTIR spectroscopy, XRD, and DSC analysis. The FTIR spectroscopic analysis revealed the possibility of intermolecular hydrogen bonding in various solid dispersions. The XRD and DSC studies indicated the transformation of crystalline etoricoxib (in pure drug) to amorphous etoricoxib (in solid dispersions) by the solid dispersion technology. Both the aqueous solubility and dissolution of etoricoxib were observed in all etoricoxib solid dispersions as compared with pure etoricoxib and their physical mixtures. The in vitro dissolution studies exhibited improved dissolution in case of solid dispersion using lactose than the solid dispersions using both sucrose and mannitol. The in vitro dissolution of etoricoxib from these solid dispersions followed Hixson-Crowell model.
机译:本研究的目的是通过使用各种糖载体(例如乳糖,蔗糖和甘露醇)的溶剂蒸发技术来改善水溶性差的药物依托考昔的溶解度和溶解度。通过溶剂蒸发技术以不同的比例制备了依托考昔固体分散体及其使用乳糖,蔗糖和甘露醇的物理混合物。分析了依托昔布固体分散体和物理混合物的百分产率,药物含量,饱和溶解度和体外溶出度。依托昔布固体分散体通过FTIR光谱,XRD和DSC分析表征。 FTIR光谱分析揭示了各种固体分散体中分子间氢键的可能性。 XRD和DSC研究表明,通过固体分散技术将结晶的依托昔布(在纯药物中)转变为无定形的依托昔布(在固体分散物中)。与纯依托昔布及其物理混合物相比,在所有依托昔布固体分散体中均观察到了依托昔布的水溶性和溶解性。体外溶出度研究显示,与使用蔗糖和甘露醇的固体分散体相比,使用乳糖的固体分散体的溶出度更高。依托昔布从这些固体分散体中的体外溶解遵循Hixson-Crowell模型。

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