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聚乙烯吡咯烷酮K30和/或L-精氨酸对依托考昔-羟丙基-β-环糊精包合物稳定常数的影响:依托考昔-羟丙基-β-环糊精二元体系的制备与表征

Effect of PVP K30 and/or L-arginine on stability constant of etoricoxib-HPbetaCD inclusion complex: preparation and characterization of etoricoxib-HPbetaCD binary system.

作者信息

Shah Manali, Karekar Poonam, Sancheti Pankajkumar, Vyas Vikrant, Pore Yogesh

机构信息

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, India.

出版信息

Drug Dev Ind Pharm. 2009 Jan;35(1):118-29. doi: 10.1080/03639040802220292.

DOI:10.1080/03639040802220292
PMID:18979307
Abstract

The effect of polyvinyl pyrrolidone (PVP) K30 and/or L-arginine on etoricoxib-HPbetaCD complex was investigated. The phase solubility profiles were classified as A(L)-type, both in absence or presence of auxiliary substances used. The apparent stability constant (K(c)) of binary complex obtained at room temperature, 371.80 +/- 2.61 M(-1), was decreased with the addition of PVP and arginine indicating no benefit of addition of auxiliary substances to promote higher complexation efficiency. Therefore, solid etoricoxib-HPbetaCD binary systems were prepared and characterized by proton nuclear magnetic resonance spectroscopy (1HNMR), X-ray powder diffractometry, Fourier transformation-infrared spectroscopy, and dissolution studies. Among all binary systems, a lyophilized product showed superior performance in enhancing dissolution of etoricoxib.

摘要

研究了聚乙烯吡咯烷酮(PVP)K30和/或L-精氨酸对依托考昔-HPβCD复合物的影响。无论是否存在所用辅助物质,相溶解度曲线均归类为A(L)型。在室温下获得的二元复合物的表观稳定常数(Kc)为371.80±2.61 M-1,随着PVP和精氨酸的加入而降低,这表明添加辅助物质无助于提高络合效率。因此,制备了固体依托考昔-HPβCD二元体系,并通过质子核磁共振光谱(1HNMR)、X射线粉末衍射、傅里叶变换红外光谱和溶出度研究对其进行了表征。在所有二元体系中,冻干产品在提高依托考昔溶出度方面表现出优异性能。

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