A novel bioadhesive drug delivery system based on liquid...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 31/13 (2006.01) A61K 31/52 (2006.01) A61K 31/70 (2006.01) A61K 38/21 (2006.01)

Patent

CA 2286052

A drug delivery system containing a liquid crystalline phase such as a cubic, a hexagonal, a reverse hexagonal, a lamellar, a micellar and a reverse micellar liquid crystalline phase. The compositions are unique in that they, as delivery system, contain A) a substance which is capable of generating a liquid crystalline phase and providing suitable biopharmaceutical properties like e.g. suitable release of the active substance and bioadhesive properties, and B) at least another substance which without having any substantially negative effect on the biopharmaceutical properties provided by the substance mentioned above under A) either takes part in the formation of a liquid crystalline phase or dilutes the proportion of liquid crystalline phase in the composition while still maintaining suitable biopharmaceutical properties and a suitable storage stability. Examples of substances A) are fatty acid esters like e.g. glycerylmonooleate and glycerylmonolinoleate and examples of substances B) are e.g. structurants like phospholipids and tocopherols and/or pharmaceutically acceptable excipients.

Système d'administration de médicaments contenant une phase cristalline liquide, telle qu'une phase cristalline liquide cubique, hexagonale, hexagonale inversée, lamellaire, micellaire ou micellaire inversée. Ces compositions présentent un caractère unique, étant donné qu'elles contiennent, en tant que système d'administration: (A) une substance capable de générer une phase cristalline liquide et produisant des effets biopharmaceutiques appropriés, tels que, par exemple, une libération adéquate de la substance active, tout en possédant des propriétés bioadhésives, et (B) au moins une autre substance qui, sans exercer d'effet sensiblement négatif sur les propriétés biopharmaceutiques que possède la substance (A), soit participe à la constitution d'une phase cristalline liquide, soit dilue la proportion de phase cristalline liquide dans la composition, tout en conservant encore des propriétés biopharmaceutiques et une stabilité de conservation appréciables. Des exemples de substances (A) sont représentés par des esters d'acides gras, tels que, par exemple, glycérylmonooléate et glycérylmonolinoléate et des exemples de substances (B) sont représentés, par exemple, par des agents structurants, tels que des phospholipides et des tocophérols ou par des excipients acceptables sur le plan pharmaceutique.

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