Stabilized galenic formulations comprising an acid labile benzimidazole compound and its preparation
AssigneeEsteve Quimica, S.A.
InventorsMontserrat Ballester Rodes, Marinus Van Boven
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Abstract
New stable oral pharmaceutical formulations are prepared by covering an inert nucleus with a first layer containing an acid labile benzimidazole compound, a water soluble polymer and non-alkaline reacting pharmaceutical acceptable excipients, a second isolation layer containing a water soluble polymer, pharmaceutical acceptable excipients and a final enteric coating.
Claims14
A stable oral pharmaceutical preparation containing an acid labile benzimidazole compound of formula I:
- ##STR2## wherein R.sub.1 is hydrogen, methoxy or difluoromethoxy;
- R.sub.2 is methyl or methoxy;
- R.sub.3 is methoxy, 2,2,2-trifluoroethoxy or 3-methoxypropoxy and R.sub.4 is hydrogen or methoxy, which comprises:
- (a) a nucleus formed by an inert core, the acid labile benzimidazole compound of formula I, a non-alkaline inert water soluble polymer and non-alkaline reacting pharmaceutical acceptable exicipients;
- (b) an inert non-alkaline coating disposed on said nucleus, formed by a non-alkaline water soluble polymer and non-alkaline pharmaceutical excipients, and
- (c) an outer layer disposed on the previous coating comprising an enteric coating.
A process for the preparation of a stable oral pharmaceutical preparation containing an acid labile benzimidazole compound of formula I as active ingredient ##STR3## wherein R.sub.1 is hydrogen, methoxy or difluoromethoxy;
- R.sub.2 is methyl or methoxy;
- R.sub.3 is methoxy, 2,2,2-trifluoroethoxy or 3-methoxypropoxy;
- and R.sub.4 is hydrogen or methyl, which comprises:
- (a) preparing a nucleus formed by an inert core, the acid labile benzimidazole, compound of formula I, a non-alkaline inert water soluble polymer and non-alkaline reacting pharmaceutical acceptable excipients;
- (b) coating said nucleus with an inert non-alkaline layer formed by a non-alkaline water soluble polymer and non-alkaline pharmaceutical acceptable excipients;
- and
- (c) coating the coating of step (b) with an enteric coating.
A stable oral pharmaceutical preparation containing an acid labile benzimidazole compound of formula I:
- ##STR4## wherein R.sub.1 is hydrogen, methoxy or difluoromethoxy, R.sub.2 is methyl or methoxy, R.sub.3 is methoxy, 2,2,2-trifluoroethoxy or 3-methoxypropoxy;
- and R.sub.4 is hydrogen or methyl, which consists essentially of:
- (a) a nucleus formed by an inert core, the acid labile benzimidazole compound of formula I, a non-alkaline inert water soluble polymer and non-alkaline reacting pharmaceutical acceptable exicipients;
- (b) an inert non-alkaline coating disposed on said nucleus, formed by a non-alkaline water soluble polymer and non-alkaline pharmaceutical excipients, and
- (c) an outer layer disposed on the previous coating comprising an enteric coating.
A stable oral pharmaceutical preparation containing an acid labile benzimidazole compound of formula I:
- ##STR5## wherein R.sub.1 is methoxy, R.sub.2 is methyl, R.sub.3 is methoxy and R.sub.4 is methyl which consists essentially of:
- (a) a nucleus formed by an inert core, the acid labile benzimidazole compound of formula I, hydroxypropyl methylcellulose and talc;
- (b) an inert non-alkaline coating disposed on said nucleus, formed by hydroxypropylmethylcellulose, talc and titanium dioxide and
- (c) an enteric coating disposed on the coating of (b) consisting essentially of methacrylic acid copolymer, triethylcitrate and talc.
A stable oral pharmaceutical preparation containing an acid labile benzimidazole compound of formula I:
- ##STR6## wherein R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is 2,2,2-trifluoroethoxy and R.sub.4 is hydrogen which consists essentially of:
- (a) a nucleus formed by an inert core, the acid labile benzimidazole compound of formula I, hydroxypropyl methylcellulose and talc;
- (b) an inert non-alkaline coating disposed on said nucleus, formed by hydroxypropylmethylcellulose, talc and titanium dioxide and
- (c) an enteric coating disposed on the coating of (b) consisting essentially of methacrylic acid copolymer, triethylcitrate and talc.
Dependencies are inferred from the claim text.