Stabilized hme composition with small drug particles

Details Stabilized hme composition with small drug particles Stabilized hme composition with small drug particles

A - Human Necessities

61

K

A61K 9/14 (2006.01)

Patent

CA 2598204

A hot-melt extruded composition having finely divided drug-containing particles dispersed within a polymeric and/or lipophyllic carrier matrix is provided. The carrier softens or melts during hot-melt extrusion but it does not dissolve the drug-containing particles during extrusion. As a result, a majority or at least 90 % wt. of the drug-containing particles in the extrudate are deaggregated during extrusion into essentially primary crystalline and/or amorphous particles. PEO is a suitable carrier material for drugs insoluble in the solid state in this carrier. Various functional excipients can be included in the carrier system to stabilize the particle size and physical state of the drug substance in either a crystalline and/or amorphous state. The carrier system is comprised of at least one thermal binder, and may also contain various functional excipients, such as: super- disintegrants, antioxidants, surfactants, wetting agents, stabilizing agents, retardant, or similar functional excipients. A hydrophilic polymer, such as hydroxypropyl methylcellulose (HPMC E15), polyvinyl alcohol (PVA), or poloxamer, and/or a surfactant, such as sodium lauryl sulfate (SLS), can be included in the composition. A process for preparing the extrudate is conducted at a temperature approximating or above the softening or melting temperature of the matrix and below the point of solubilization of drug- containing particles in the carrier system, and below the recrystallization point in the case of amorphous fine drug particles.

L'invention concerne une composition extrudée à chaud qui contient des particules finement broyées dispersées dans une matrice de support polymère et/ou lipophile. Le support se ramollit ou fond par extrusion à chaud mais ne dissout pas les particules médicamenteuses lors de l'extrusion. Ainsi, au cours de l'extrusion, la majeur partie ou au moins 90 % en poids des particules médicamenteuses de l'extrudat se désagrègent principalement en particules de cristallisation primaire et/ou en particules amorphes. L'oxyde de polyéthylène (PEO) peut servir de matériau de support pour les médicaments insolubles à l'état solide dans ce support. Divers excipients fonctionnels peuvent être inclus dans le système de support pour stabiliser à la fois la taille des particules et l'état physique de la substance médicamenteuse dans l'état cristallin et/ou amorphe. Le système de support comprend au moins un agglutinant thermique, et peut éventuellement comprendre divers excipients fonctionnels, tels que: super-délitants, antioxydants, surfactants, agents mouillants, agents stabilisants, retardants, ou excipients fonctionnels similaires. Un polymère hydrophile, tel que l'hydroxypropylméthyl cellulose (HPMC E15), l'alcool polyvinylique (PVA) ou le poloxamère, et/ou un surfactant, tel que le laurylsulfate de sodium (SLS), peuvent être ajoutés à la composition. Le procédé de préparation de l'extrudat de l'invention est appliqué à une température proche ou supérieure à la température de ramollissement ou de fusion de la matrice et inférieure au point de solubilisation des particules médicamenteuses dans le système de support, et inférieure au point de recristallisation dans le cas de particules médicamenteuses fines et amorphes.

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