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美洛昔康-环糊精二元体系的物理化学表征及溶解性能

Physicochemical characterization and dissolution properties of meloxicam-cyclodextrin binary systems.

作者信息

Naidu N Buchi, Chowdary K P R, Murthy K V R, Satyanarayana V, Hayman A R, Becket G

机构信息

Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.

出版信息

J Pharm Biomed Anal. 2004 Apr 1;35(1):75-86. doi: 10.1016/j.jpba.2004.01.003.

Abstract

The objective of the work is physicochemical characterization of meloxicam (ME)-cyclodextrin (CD) binary systems both in solution and solid states and to improve the dissolution properties of meloxicam via complexation with alpha-, beta- and gamma-cyclodextrins. Detection of inclusion complexation was done in solution state by means of phase solubility analysis, mass spectrometry and 1H nuclear magnetic resonance (NMR) studies, and in solid state using differential scanning calorimetry (DSC), powder X-ray diffractometry, and in vitro dissolution studies. Phase solubility, mass spectrometry and 1H NMR studies in solution state revealed 1:1M complexation of meloxicam with all CDs. A true inclusion of ME with gamma-CD at 1:1 and 1:2M in solid state was confirmed by DSC, powder XRD and scanning electron microscopy (SEM) studies. Dissolution properties of ME-CDs binary systems were superior when compared to pure ME.

摘要

这项工作的目的是对美洛昔康(ME)-环糊精(CD)二元体系在溶液和固态下进行物理化学表征,并通过与α-、β-和γ-环糊精络合来改善美洛昔康的溶解性能。通过相溶解度分析、质谱和1H核磁共振(NMR)研究在溶液状态下检测包合络合,在固态下使用差示扫描量热法(DSC)、粉末X射线衍射法和体外溶出度研究。溶液状态下的相溶解度、质谱和1H NMR研究表明美洛昔康与所有环糊精形成1:1M的络合物。DSC、粉末XRD和扫描电子显微镜(SEM)研究证实了固态下ME与γ-CD以1:1和1:2M的比例形成真正的包合物。与纯ME相比,ME-CD二元体系的溶解性能更优。

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