Oral pharmaceutical extended release dosage form
AssigneeAstraZeneca AB
InventorsPer-Gunnar Karehill, Per Johan Lundberg
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Abstract
An enteric coated pharmaceutical extended release dosage form of a H+, K+-ATPase inhibitor giving an extended plasma concentration profile of a H+, K+-ATPase inhibitor. The extended plasma profile is obtained by a pharmaceutical composition which comprises a core material of a hydrophilic or hydrophobic matrix, and the H+, K+-ATPase inhibitor and optionally pharmaceutically acceptable excipients. The dosage form may be administered once daily.
Claims31
An extended release pharmaceutical dosage form consisting essentially of an active ingredient which is an H+, K+-ATPase inhibitor embedded in a hydrophilic or hydrophobic matrix for the extended release of the active ingredient, optional pharmaceutically acceptable excipients, a water soluble separating layer and an enteric coating layer, and the H+, K+-ATPase inhibitor is a compound of formula I
- wherein
- Hetis
- Het2 is
- X=
- wherein
- N in the berzimidazole moiety means that one of the ring carbon atoms substituted by R6-R9 optionally may be exchanged for a nitrogen atom without any substituents;
- R1, R2 and R3 are the same or different and selected from the group consisting of hydrogen, alkyl, alkoxy, fluorine-substituted alkoxy, alkylthio, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenyl and phenylalkoxy;
- R4 and R5 are the same or different and selected from the group consisting of hydrogen, alkyl and arylalkyl;
- R6′ is selected from the group consisting of hydrogen, halogen, trifluoromethyl, alkyl and alkoxy;
- R6-R9 are the same or different and selected from the group consisting of hydrogen, alkyl, alkoxy, halogen, halo-alkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolinyl, trifluoroalkyl, or adjacent groups R6-R9 form ring structures which may be further substituted;
- R10 is hydrogen or forms an alkylene chain together with R3;
- and R11 and R12 are the same or different and selected from the group consisting of hydrogen, halogen and alkyl.
A process for the manufacture of an extended release dosage form consisting essentially of an active ingredient which is an H+, K+-ATPase inhibitor, optionally pharmaceutically acceptable excipients and a hydrophilic or hydrophobic matrix for the extended release of the active ingredient, wherein the process comprises the following steps:
- a) mixing the H+, K+-ATPase inhibitor, optional pharmaceutically acceptable excipients and the hydrophilic or tie hydrophobic matrix to obtain a core material, and
- b) applying an enteric coating layer onto the core material wherein a water soluble separating layer is applied onto the core material prior to the application of the enteric coating.
Dependencies are inferred from the claim text.