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Thermal and spectroscopic analysis of inclusion complex of spironolactone prepared by evaporation and hot melt methods
Authors:G. Patyi  A. Bódis  I. Antal  B. Vajna  Zs. Nagy  Gy. Marosi
Affiliation:1.Technology of Pharmaceutical, Enviromental and Safety Materials Research Group, Department of Organic Chemistry and Technology,Budapest University of Technology and Economics,Budapest,Hungary;2.Pharmaceutical Technology Department,Gedeon Richter Plc,Budapest,Hungary;3.Department of Pharmaceutics,Semmelweis University,Budapest,Hungary
Abstract:Solvent and melt techniques were used to obtain molecular dispersion of the poorly soluble spironolactone (SPIR) model drug enhancing its dissolution rate. DSC study of the interaction between SPIR and hydroxypropyl-β-cyclodextrin confirmed the need for molecular dispersion if their complexation is required. Solvent-free twin-screw extrusion was suitable for forming inclusion complex significantly below the melting temperature of the SPIR. According to DSC, Raman and XRPD results fine dispersion of both components was achieved in a hydrophilic polymer. The molecules of the active ingredient are separated from each other in the polymer and the lack of the lattice energy causes faster dissolution.
Keywords:
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