Pharmaceutical co-crystals of posaconazole for improvement of physicochemical properties

Abstract

Posaconazole exerts an extended spectrum of antifungal activity against various strains of clinically relevant moulds and yeasts. In recent years, antifungal triazole posaconazole has become increasingly important for the prophylaxis and treatment of systemic mycoses. After oral administration of posaconazole, absolute bioavailability has been estimated to range from 8% to 47%. Pharmaceutical co-crystallization is a promising approach for improving dissolution rate or manipulating other physical properties of API. The objective of this study is to improve the dissolution rate of posaconazole by co-crystallization. A 1:1 stoichiometric co-crystals of adipic acid were prepared by solvent assisted grinding method. The prepared co-crystals were subjected to solid-state characterization by FTIR, PXRD and DSC studies. The physicochemical properties of posaconazole and co-crystals were assessed in terms of melting point, flowability and dissolution rate. The results indicated improvement in flow property and dissolution rate. In vitro dissolution profile of co-crystals showed a significant increased dissolution of posaconazole from initial period in 0.1 N hydrochloric acid solution. The dissolution efficiency for posaconazole-adipic acid co-crystal was 61.65 % against posaconazole, 46.58 %. Thus, cocrystallization can be a promising approach to prepare posaconazole-adipic acid co-crystals with improved physicochemical properties.

Development and Optimization of Dipyridamole- and Roflumilast-Loaded Nanoemulsion and Nanoemulgel for Enhanced Skin Permeation: Formulation, Characterization, and In Vitro Assessment

“…This mixture was then crushed onto a transparent disc, and the resulting spectra were recorded. These spectra were analyzed to verify the absence of any interaction between the medicine and the excipients, which might potentially occur throughout the procedure [ 106 ].…”

Amino Acid as Co-Crystal Coformer for Ebastine Solubility Enhancement

“…Two molar ratios of 1:4 and 1:8 (EB:coformer) molar ratios( Asparagine, L-prolin and L-histidin) molar ratio accordingly by grinding with mortar and pestle for 45 minutes with addition of drop of methanol every ten minutes during grinding (21,22) . The substance is then dried at 40 degrees Celsius.…”