糖载体固体分散技术增强依托昔布的溶解度和溶出度。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-09-05 DOI:10.5402/2011/819765
Abhisekh Das, Amit Kumar Nayak, Biswaranjan Mohanty, Satyabrata Panda
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引用次数: 54

摘要

本研究的目的是利用不同的糖载体,如乳糖、蔗糖和甘露醇,通过溶剂蒸发技术改善难溶性药物依托昔布的溶解度和溶出度。采用溶剂蒸发技术,以乳糖、蔗糖和甘露醇为原料,按不同配比制备了依托昔布固体分散体及其物理混合物。分析了依托昔布固体分散体和物理混合体的收率、药物含量、饱和溶解度和体外溶出度。采用FTIR、XRD和DSC对依托昔布的固体分散体进行了表征。红外光谱分析揭示了不同固体分散体分子间氢键形成的可能性。XRD和DSC研究表明,固体分散技术将结晶型(纯药物型)依托托昔布转化为无定形(固体分散体)依托托昔布。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观察到依托昔布的水溶性和溶解性。体外溶出研究表明,使用乳糖的固体分散体比使用蔗糖和甘露醇的固体分散体溶解性更好。依托昔布在这些固体分散体中的体外溶出符合Hixson-Crowell模型。
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Solubility and dissolution enhancement of etoricoxib by solid dispersion technique using sugar carriers.

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.

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