Oral-administration forms of a medicament containing pantoprazol

Details Oral-administration forms of a medicament containing pantoprazol Oral-administration forms of a medicament containing pantoprazol

1993-12-17

1999-12-07

Bawa, Raj

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424464, 424468, 424471, 424474, 424484, 424490, A61K 930

Patent

active

059979038

DESCRIPTION:

BRIEF SUMMARY
PRIOR ART

European Patent Application EP-A-244 380 describes oral presentation forms for acid-unstable active compounds from the class of H.sup.+ /K.sup.+ -ATPase inhibitors having a pyridylmethylsulphinyl-1B-benzimidazole structure, which have a core, an intermediate layer, and an outer layer which is resistant to gastric juice. European Patent Application EP-A-247 983 describes and claims the formulations disclosed in EP-A-244 380 in connection with the H.sup.+ /K.sup.+ -ATPase inhibitor omeprazole.
In the case of the presentation forms claimed in European Patent Applications EP-A-244 380 and EP-A-247 983, stabilization of the acid-unstable active compounds is achieved, in particular, by adding bases to the core and thus increasing the pH; to achieve an adequate storage stability, however, certain conditions must be maintained both during preparation and during storage, and these can be reconciled with an optimum pharmaceutical formulation and problem-free stock-holding only with difficulty. EP-A-247 983 thus appropriately states: "It is essential for long-term stability during storage that the water content of the presentation form containing the active compound omeprazole (tablets, capsules and pellets with a coating which is resistant to gastric juice) is kept low and is preferably not more that 1.5 wt. %. Final packs with pellets which have a coating which is resistant to gastric juice and are contained in hard gelatine capsules accordingly are preferably to be provided with drying agents which reduce the water content of the gelatine shells to the extent that the water content in the pellets does not exceed 1.5 wt. %".
The water content, which is to be kept low during preparation of pellet cores for stability reasons, thus means that the mass to be extruded for preparation of the pellet core is no longer sufficiently plastic for the extrudate subsequently to be rounded off into spherical particles. Rather, cylindrical bodies are formed, which, during the subsequent coating step, receive thinner lacquer coatings on the ends and therefore do not have the required resistance to gastric juice at these points, and moreover do not protect the core reliably from the coating which is resistant to gastric juice by a sub-coating, which is essential for the stability.
The stability problems described also arise if attempts are made to formulate the H.sup.+ /K.sup.+ -ATPase inhibitor pantoprazole (prop. INN for the compound 5-(difluoromethoxy)-2-[(3,4-dimethoxy-2-pyridyl)methylsulphinyl]-1H-benzim idazole) as described in European Patent Applications EP-A-244 380 and EP-A-247 983.


DESCRIPTION OF THE INVENTION

It has now been found, surprisingly, that if certain fillers and binders often used as tablet auxiliaries, such as are mentioned for the preparation of the pellet and tablet cores in European Patent Applications EP-A-244 380 and EP-A-247 983, are dispensed with, the stability problems described do not occur. These fillers and binders are, in particular, lactose, microcrystalline cellulose and hydroxypropylcellulose.
The invention thus relates to a medicament in pellet or tablet form which contains the active compound pantoprazole, is to be administered orally, is resistant to gastric juice and consists of a basic pellet core or tablet core, one or more inert, water-soluble intermediate layer(s) and an outer layer which is resistant to gastric juice, and which is characterized in that the core contains, in addition to pantoprazole or in addition to a pantoprazole salt, polyvinylpyrrolidone and/or hydroxypropylmethylcellulose as the binder, and if desired mannitol additionally as an inert filler.
For a basic reaction of the pellet core or tablet core--if the desired increase in pH has not already been achieved by using the active compound salt - an inorganic base is admixed to this. Examples which may be mentioned here are the pharmacologically tolerated alkali metal, alkaline earth metal or earth metal salts of weak acids and the pharmacologically tolerated hydroxides and oxides of alkaline earth and ea

REFERENCES:
Remington's Pharmaceutical Sciences, 17th Ed, 1985, Mack Pub. Co., p. 1633-38.

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