Solid pharmaceutical dosage forms in form of a particulate...

A - Human Necessities – 61 – K

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A61K 31/427 (2006.01) A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 47/38 (2006.01)

Patent

CA 2292586

Solid particulate dispersions of pharmaceutical agents in a matrix of a water- soluble polymer exhibiting good aqueous dissolution enhanced bioavailability. The method of the invention utilizes water-soluble polymers such as polyvinylpyrrolidone, hydroxypropyl cellulose or hydroxypropylmethyl cellulose as carriers. The invention provides for mixing or extracting the active ingredients in solid particulate form with the polymeric carrier at a temperature at which the polymer softens, or even melts, but the drug remains solid or crystalline. The drug particules thus become coated and produce a product that is matrix coated, i.e. a particulate dispersion.

L'invention concerne des dispersions particulaires solides d'agents pharmaceutiques dans une matrice de polymère soluble dans l'eau présentant une bonne dissolution dans l'eau et une biodégradabilité améliorée. Selon l'invention, on utilise comme excipients, des polymères solubles dans l'eau, tels que des polyvinylpyrrolidones, de la cellulose d'hydroxypropyle ou de la cellulose d'hydroxypropylméthyle. Selon l'invention, il est prévu de mélanger ou d'extraire les principes actifs sous forme particulaire solide avec l'excipient polymère à une température où le polymère ramollit, voire fond, le médicament demeurant néanmoins à l'état solide ou cristallin. Les particules du médicaments sont ainsi enrobées et fournissent un produit qui est une matrice enrobée, c.-à-d. une dispersion particulaire.

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