Solid formulations of liquid biologically active agents

Details Solid formulations of liquid biologically active agents Solid formulations of liquid biologically active agents

A - Human Necessities

61

K

A61K 31/47 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 31/05 (2006.01) A61K 31/08 (2006.01) A61K 47/30 (2006.01)

Patent

CA 2589242

The instant invention relates to a solid product comprising a liquid biologically active agent which is intimately associated to a stabilizing agent; particularly a solid product that can be reconstituted to a clear, stable, stabilized nanodispersion or loaded micelles comprising a polymer as a stabilizing agent and a liquid, preferably water immiscible, biologically active agent. The instant invention is further directed toward a process for the production of the above solid product ; particularly to micelles or nanodispersions produced by hydration of a cake or powder of the solid product, produced via an effective treatment of a stabilized solution comprising for example a polymer as a stabilizing agent, such as an amphiphilic block copolymer or a small molecular weight surfactant, loaded with a liquid biologically active agent, such as propofol, an optional additive, and a suitable solvent.

L'invention concerne un produit solide comprenant un agent liquide biologiquement actif qui est intimement associé à un agent stabilisant, en particulier, un produit solide qui peut être reconstitué de manière à former une nanodispersion limpide, stable, stabilisée ou des micelles chargées comprenant un polymère comme agent stabilisant et un agent liquide biologiquement actif, de préférence non miscible à l'eau. L'invention concerne en outre un procédé de production du produit solide précité ; en particulier, des micelles ou des nanodispersions produites par hydratation d'un gâteau ou d'une poudre du produit solide, obtenues via un traitement efficace d'une solution stabilisée comprenant, par exemple, un polymère comme agent stabilisant, tel qu'un copolymère séquencé amphiphile, ou un agent tensio-actif de faible poids moléculaire, chargé avec l'agent liquide biologiquement actif, tel qu'un propofol, un additif facultatif et un solvant approprié.

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