Stable particle in liquid formulations

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/00 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 38/18 (2006.01) A61K 38/22 (2006.01) A61K 38/45 (2006.01) A61K 38/46 (2006.01) A61K 47/26 (2006.01) C12N 9/96 (2006.01)

Patent

CA 2293682

A stable particle in liquid formulation comprising a discontinuous phase of microparticles is suspended in a continuous phase which is a non-aqueous liquid, preferably biocompatible in which the microparticles are insoluble. The microparticles comprise finely powdered sugar glass selected from the group consisting of trehalose, palatinit, glucopyranosyl sorbitol, glucopyranosyl mannitol, lactitol and monosaccharide alcohols such as mannitol and inositol, holding at least one biomolecular product, the biomolecular product in the sugar glass either being in stable solid solution or being itself in suspension in the sugar glass. A monodisperse single-particle suspension of microparticles can be produced in the non-aqueous continuous liquid phase by inclusion in the continuous phase of at least one surfactant having a low or very low HLB.

L'invention porte sur une particule stable dans une formulation liquide comprenant une phase discontinue de microparticules, cette particule stable étant en suspension dans une phase continue qui est un liquide non aqueux, de préférence biocompatible, dans lequel les microparticules sont insolubles. Ces microparticules comprennent un verre formé par le sucre, se présentant sous forme d'une poudre fine, et sélectionné dans le groupe constitué par tréhalose, palatinit, glucopyranosyle sorbitol, glucopyranosyle mannitol, lactitol et des alcools de monosaccharide tels que mannitol et inositol. Ce verre formé par le sucre retient au moins un produit biomoléculaire soit dans une solution solide stable, soit en suspension. Une suspension de microparticules monodispersée à particules uniques peut être produite dans la phase liquide continue, non aqueuse, par inclusion dans la phase continue d'au moins un tensioactif ayant un rapport hydrophile-lipophile bas ou très bas.

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