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Bulk, surface properties and water uptake mechanisms of salt/acid amorphous composite systems

Abstract : Developing amorphous pharmaceuticals can be desirable due to advantageous biopharmaceutical properties. Low glass transition temperature (Tg) amorphous drugs can be protected from crystallisation by mixing with high Tg excipients, such as polymers, or with salt forms. However, both polymers and salts can enhance the water uptake. The aim of this study was to formulate physico-chemically stable amorphous materials, by co-processing different proportions of sulfathiazole and its sodium salt to produce an optimum ratio, characterised by the best physical stability and lowest hygroscopicity. Both sulfathiazole and salt amorphised upon spray drying. At room temperature, sulfathiazole crystallised within 1 h at <5% relative humidity while the salt deliquesced when exposed to ambient humidity conditions. In the case of composite systems, FTIR spectroscopy, thermal and surface analysis suggested interactions with an acid:salt stoichiometry of 1:2. Increasing proportions of salt raised the Tg, enhancing the storage stability, however this was opposed by an enhanced hygroscopicity. The water uptake mechanism within the different amorphous systems, analysed by fitting the water sorption isotherms with the Young and Nelson equation, was dependent on the ratio employed, with the salt and the acid facilitating absorption and adsorption, respectively. Tuning the properties of amorphous salt/acid composites by optimising the ratio appears potentially promising to improve the physical stability of amorphous formulations.
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Stefano Bianco, Frederic Tewes, Lidia Tajber, Vincent Caron, Owen I. Corrigan, et al.. Bulk, surface properties and water uptake mechanisms of salt/acid amorphous composite systems. International Journal of Pharmaceutics, Elsevier, 2013, 456 (1), pp.143-152. ⟨10.1016/j.ijpharm.2013.07.076⟩. ⟨inserm-01102838⟩



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