Characterization of β-lapachone and methylated β-cyclodextrin solid-state systems
作者： Marcílio S. S. Cunha-Filho , Bruno Dacunha-Marinho , Juan J. Torres-Labandeira , Ramón Martínez-Pacheco , Mariana Landin
DOI: 10.1208/PT0803060
关键词: Dissolution 、 Aqueous solution 、 Solubility 、 Differential scanning calorimetry 、 Fourier transform infrared spectroscopy 、 Dissolution testing 、 Cyclodextrin 、 Chemistry 、 Crystallography 、 Nuclear chemistry 、 Calorimetry
摘要: The purpose of this research was to explore the utility β cyclodextrin (βCD) and derivatives (hydroxypropyl-β-cyclodextrin [HPβCD], sulfobutylether-β-CD [SB\CD], a randomly methylated-β-CD [RMβCD]) form inclusion complexes with antitumoral drug, β-lapachone (βLAP), in order overcome problem its poor water solubility. RMβCD presented highest efficiency for βLAP solubilization selected develop solid-state binary systems. Differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), Fourier transform infrared (FTIR) optical electron microscopy results suggest formation by both freeze-drying kneading techniques dramatic improvement drug dissolution at 20-minute (DE20-minute 67.15% 88.22%, respectively) against 27.11%) or βCD/drug physical mixture 27.22%). However, method gives highly crystalline material that together adequate profile make it best procedure obtaining RMβCD/βLAP convenient different applications βLAP.
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