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|Title:||Pharmaceutical preparation for oral use|
|Abstract:||Pharmaceutical preparation containing omeprazole together with an alkaline reacting compound or an alkaline salt of omeprazole optionally together with an alkaline compound as the core material, one or more subcoating layers comprising inert reacting compounds which are soluble or rapidly disintegrating in water, or polymeric, water soluble filmforming compounds, optionally containing pH-buffering alkaline compounds and an enteric coating as well as a process for the preparation thereof and the use in the treatment of gastrointestinal diseases.|
|Inventor(s):||Lovgren; Kurt I. (Molnlycke, SE), Pilbrant; Ake G. (Kungsbacka, SE), Yasumura; Mitsuru (Hyogo, JP), Morigaki; Satoshi (Hyogo, JP), Oda; Minoru (Ohita, JP), Ohishi; Naohiro (Fukuoka, JP)|
|Assignee:||Aktiebolaget Hassle (SE)|
1. An oral pharmaceutical preparation comprising
(a) a core region comprising an effective amount of a material selected from the group consisting of omeprazole plus an alkaline reacting compound, an alkaline omeprazole salt plus an alkaline reacting compound and an alkaline omeprazole salt alone;
(b) an inert subcoating which is soluble or rapidly disintegrating in water disposed on said core region, said subcoating comprising one or more layers of materials selected from among tablet excipients and polymeric film-forming compounds; and
(c) an outer layer disposed on said subcoating comprising an enteric coating.
2. A preparation according to claim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance [Al.sub.2 O.sub.3.6MgO.CO.sub.2.12H.sub.2 O or MgO.Al.sub.2 O.sub.3.2SiO.sub.2.nH.sub.2 O], wherein n is not an integer and less than 2.
3. A preparation according to claim 1 wherein the subcoating comprises two or more sub-layers.
4. A preparation according to claim 3 wherein the subcoating comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose or polyvinylpyrrolidone.
5. A preparation according to claim 1 wherein the alkaline core comprises omeprazole and pH-buffering alkaline compound rendering to the micro-environment of omeprazole a pH of 7-12.
6. A preparation according to claim 5 wherein the alkaline compound comprises one or more of magnesium oxide, hydroxide or carbonate, aluminium hydroxide, aluminium, calcium, sodium or potassium carbonate, phosphate or citrate, the composite aluminium/magnesium compounds Al.sub.2 O.sub.3.6MgO.CO.sub.2.12H.sub.2 O or MgO.Al.sub.2 O.sub.3.2SiO.sub.2.nH.sub.2 O, where n is not an integer and less than 2.
7. A preparation according to claim 1, wherein the core region comprises a salt of omeprazole selected from along the sodium, potassium, magnesium, calcium and ammonium salts.
8. A preparation according to claim 1 wherein the enteric coating comprises hydroxypropyl methylcellulose pthalate, cellulose acetate phthalate, co-polymerized methacrylic acid/methacrylic acid methyl ester or polyvinyl acetate phthalate, optionally containing a plasticizer.
9. A preparation according to claim 1 wherein the water content of the final dosage form containing omeprazole does not exceed 1.5% by weight.
10. A method for the treatment of gastrointestinal disease comprising administering to a host in need of such treatment a therapeutically effective amount of a preparation according to claim 1.
11. A preparation according to claim 1, wherein the subcoating further comprises an alkaline buffering compound.
12. A preparation according to claim 1, wherein the core comprises omeprazole and disodium hydrogen phosphate, and the subcoating comprises hydroxy propyl methyl cellulose.
13. A preparation according to claim 1, wherein the alkaline core comprises omeprazole and magnesium hydroxide, the subcoating comprises a layer comprising hydroxypropyl cellulose and synthetic hydrotalcite, and the outer layer comprises hydroxypropyl cellulose.
14. A process for the preparation of an oral pharmaceutical preparation containing omeprazole, comprising
(a) preparing a core comprising an effective amount of a material selected from the group consisting of omeprazole plus an alkaline reacting compound, an alkaline omeprazole salt plus an alkaline reacting compound and an alkaline omeprazole salt alone;
(b) coating the core with one or more layers of an inert subcoating material selected from among tablet excipients and polymeric film-forming compounds to form a subcoated core; and
(c) coating the subcoated core with an enteric coating.
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