Improved formulations and methods for lyophilization and...

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/64 (2006.01) A61K 9/19 (2006.01)

Patent

CA 2707484

The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pll values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) frecze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.

L'invention concerne des compositions, des procédés pour lyophiliser des composés et préparer des compositions pharmaceutiques, et des kits fournissant des solutions et de formulations lyophilisées de composés. Les compositions, procédés et nécessaires sont particulièrement utiles dans des applications pharmaceutiques impliquant des agents thérapeutiques qui ont une faible solubilité à de faibles valeurs de pH et des valeurs de pH moyennes. Certains modes de réalisation proposent des procédés de lyophilisation de composés dans des solutions liquides, qui comprennent les étapes consistant à : a) préparer des solutions aqueuses d'un composé d'intérêt en l'absence d'un tampon ; b) ajuster le pH à des valeurs élevées afin d'augmenter la solubilité du composé d'intérêt ; et c) sécher par congélation la solution pour former une composition solide lyophilisée. Des solutions aqueuses comprenant un tampon sont également révélées. Des formulations lyophilisées, y compris des poudres micronisées et non micronisées, sont proposées.

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