High-throughput formation, identification, and analysis of...

C - Chemistry – Metallurgy – 30 – B

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C30B 7/00 (2006.01) B01J 19/00 (2006.01) C07B 61/00 (2006.01) G01N 33/68 (2006.01) B01L 3/00 (2006.01)

Patent

CA 2396079

The invention concerns arrays of solid-forms of substances, such as compounds and rapid-screening methods therefor to identify solid-forms, particularly of pharmaceuticals, with enhanced properties. Such properties include improved bioavailability, solubility, stability, delivery, and processing and manufacturing characteristics. The invention relates to a practical and cost- effective method to rapidly screen hundreds to thousands of samples in parallel. The invention further provides methods for determining the conditions and/or ranges of conditions required to produce crystals with desired compositions, particle sizes, habits, or polymorphic forms. In a further aspect, the invention provides high-throughput methods to identify sets of conditions and/or combinations of components compatible with particular solid-forms, for example, conditions and/or components that are compatible with advantageous polymorphs of a particular pharmaceutical.

L'invention concerne des matrices de formes solides de substances, telles que des composés, ainsi que des méthodes de criblage rapide de ces substances destinées à identifier des formes solides, en particulier de produits pharmaceutiques, possédant des propriétés améliorées. Ces propriétés améliorées comprennent la biodisponibilité, la solubilité, la stabilité, l'administration, ainsi que des caractéristiques de fabrication et de traitement. L'invention concerne un procédé pratique et efficient destiné à cribler rapidement et en parallèle des centaines à des milliers d'échantillons. Elle concerne, en outre, des procédés destinés à déterminer les conditions et/ou les domaines de conditions convenant à la production de cristaux avec des compositions, des tailles de particules, des aspects ou des formes polymorphes recherchés. Dans une autre réalisation, l'invention concerne des procédés d'identification à productivité élevée destinés à identifier des ensembles de conditions et/ou des combinaisons de composants compatibles avec des formes solides particulières, par exemple, des conditions et/ou des composants qui sont compatibles avec des formes polymorphes avantageuses d'un produit pharmaceutique particulier.

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