Nalluri Buchi N, Chowdary K P R, Murthy K V R, Hayman A R, Becket G
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.
AAPS PharmSciTech. 2003;4(1):E2. doi: 10.1208/pt040102.
The objective of this work is physicochemical characterization of nimesulide-cyclodextrin binary systems both in solution and solid state and to improve the dissolution properties of nimesulide (N) via complexation with alpha-, beta, and gamma-cyclodextrins (CDs). Detection of inclusion complexation was done in solution by means of phase solubility analysis, mass spectrometry, and 1H nuclear magnetic resonance (1H-NMR) spectroscopic studies, and in solid state using differential scanning calorimetry (DSC), powder x-ray diffractometry (X-RD), scanning electron microscopy (SEM), and in vitro dissolution studies. Phase solubility, mass spectrometry and 1H-NMR studies in solution revealed 1:1 M complexation of N with all CDs. A true inclusion of N with beta-CD at 1:2 M in solid state was confirmed by DSC, powder X-RD and SEM studies. Dissolution properties of N-CD binary systems were superior when compared to pure N.
本研究的目的是对尼美舒利 - 环糊精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（CDs）络合来改善尼美舒利（N）的溶解性能。通过相溶解度分析、质谱和1H核磁共振（1H - NMR）光谱研究在溶液中检测包合络合作用，并使用差示扫描量热法（DSC）、粉末X射线衍射法（X - RD）、扫描电子显微镜（SEM）和体外溶出度研究在固态下进行检测。溶液中的相溶解度、质谱和1H - NMR研究表明N与所有CDs形成1:1摩尔比的络合物。DSC、粉末X - RD和SEM研究证实了在固态下N与β - CD以1:2摩尔比形成真正的包合物。与纯N相比，N - CD二元体系的溶解性能更优。
