Improvement of water solubility and in vitro dissolution rate of gliclazide by complexation with β-cyclodextrin1

Yalçιn Özkan , Tamer Atay , Necati Di̇kmen , Aşkιn Işimer , Hassan Y Aboul-Enein
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引用次数: 86

Abstract

Inclusion complexes of gliclazide with β-cyclodextrin were prepared using different two methods: neutralization and recrysstalization. Host–guest interactions were studied in the solid state by X-ray diffractometry and infrared spectroscopy. The stability constant between gliclazide and β-cyclodextrin was calculated from the phase solubility diagram. It was found that the neutralization technique and a solid complex of gliclazide with β-cyclodextrin in a molar ratio of 1.5:1 could be used to prepare the amorphous state of drug inclusion complexes. The dissolution rates of gliclazide from the inclusion complex made by neutralization was much faster than the pure drug, physical mixture of drug and cyclodextrin, recyristalization system and also comparable to the data reported in literature. Results of this report indicate that β-cyclodextrin could be useful for the solid gliclazide formulations as it may results in a more rapid and uniform release of the drug.

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β-环糊精1络合改善格列齐特的水溶性和体外溶出率
采用中和法和重结晶法制备了格列齐特与β-环糊精的包合物。利用x射线衍射和红外光谱研究了固态中主客体相互作用。根据相溶解度图计算了格列齐特与β-环糊精之间的稳定常数。发现采用中和技术和格列齐特与β-环糊精的摩尔比为1.5:1的固体配合物可以制备无定形的药物包合物。中和法制备的包合物对格列齐特的溶出速度远快于纯药物、药物与环糊精的物理混合物、再循环体系,也与文献报道的数据相当。本报告的结果表明,β-环糊精可用于固体格列齐特制剂,因为它可以使药物更快、更均匀地释放。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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