Pharmaceutical preparation with a hydrophobic active...

Details Pharmaceutical preparation with a hydrophobic active... Pharmaceutical preparation with a hydrophobic active...

A - Human Necessities

61

K

A61K 31/445 (2006.01) A61K 9/16 (2006.01) A61K 9/46 (2006.01) A61K 31/4468 (2006.01) A61K 31/4545 (2006.01)

Patent

CA 2191302

The invention concerns pharmaceutical effervescent tablets with at least one hydrophobic active substance, such as for example loratadine or cisapride, and a surfactant. These effervescent tablets advantageously contain at least two different surfactants or emulsifiers, in particular from the group comprising sugar esters, polysorbates and phospholipids. At least one of the emulsifiers can be present in the mixture in the form of granules separately from the effervescent system and/or active substance granules. Preferably, the active substance is also precipitated in the form of separate active substance granules - for example by means of a binder, such as for example polyvinylpyrrolidone - on the surface of a suspended substance or anti- adhesive substance, such as for example Aerosil or Avicel. The active substance can, moreover, contain at least one of the effervescent components and/or a filler which preferably comprises at least one of the following compounds: higher alcohols, e.g. mannitol, sorbitol or lactose; hydrocolloids, such as maltodextrin or dextrin; and starch.

L'invention concerne des comprimés effervescents pharmaceutiques comportant au moins un principe actif hydrophobe, tel que par ex. de la loratadine ou du cisapride, et un tensioactif. Ces comprimés effervescents contiennent au moins deux différents tensioactifs ou émulsifiants, sélectionnés notamment dans le groupe des esters de saccharose, des polysorbates et des phospholipides. Au moins un des émulsifiants peut se trouver présent dans le mélange, sous forme de granulés qui lui sont propres, séparément du système effervescent. Le principe actif est lui aussi précipité, de préférence sous forme de granulés, par exemple à l'aide d'un liant, tel que de la polyvinylpyrrolidone, sur la surface d'une substance en suspension ou d'une substance anti-adhésive, telle que l'Aérosil? ou l'Avicel?. Le principe actif peut contenir en outre au moins un des constituants effervescents et/ou une charge qui comprend de préférence au moins un des composés suivants: alcools supérieurs, par ex. mannitol, sorbitol ou lactose; des hydrocolloïdes comme la maltodextrine ou la dextrine; de l'amidon.

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