Oral solid solution formulation of a poorly water-soluble...

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/26 (2006.01) A61K 9/48 (2006.01) A61K 47/32 (2006.01) A61K 47/34 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2472744

The present invention relates to an immediate release formulation with enhanced bio-availability comprising a solid homogeneous and thermostable solution of a poorly water-soluble biologically active substance, characterised in that said solid solution comprises: a) the active substance in an amount of between 10 and 50% of the total weight of the formulation, b) a non-ionic hydrophilic surfactant ingredient, which is in the liquid form between 15~ and 30~C, in an amount of between 20% and 70 % of the total weight of the formulation and c) a pharmaceutically acceptable organic polymer or mixture of polymers, which polymer or mixture of polymers is in a liquid form above 60~C and in a solid form below 30~C, in an amount of between 5% and 70% of the total weight of the formulation, and d) optionally comprises a disintegrating agent in an amount of between 1% and 10% of the total weight of the formulation. The invention further relates to active substances formulated into the above form and methods for producing the formulation.

L'invention concerne une formulation à libération immédiate présentant une biodisponibilité augmentée, qui comprend une solution solide homogène et thermostable d'une substance à faible hydrosolubilité, biologiquement active, caractérisée en ce que ladite solution solide comprend: a) ladite substance active en quantité comprise entre 10 et 50 % du poids total de la formulation; b) un tensioactif hydrophile non ionique sous forme liquide entre 15 DEG et 30 DEG C, en quantité comprise entre 20 et 70 % du poids total de ladite formulation; c) un polymère organique pharmaceutiquement acceptable ou un mélange de polymères sous forme liquide à plus de 60 DEG C et sous forme liquide à moins de 30 DEG C, en quantité comprise entre 5 et 70 % du poids total de ladite formulation; et d) éventuellement un agent de désintégration en quantité comprise entre 1 et 10 % du poids total de ladite formulation. L'invention concerne en outre des substances actives formulées précédemment ainsi que des procédés de production de ladite formulation.

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