US4853230A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical formulations of acid labile substances for oral use
Assignee: Hassle AB
•
Filing: 1987-04-20
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Granted: 1989-08-01
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Expires: 2007-04-20
Abstract
Abstract Pharmaceutical preparation containing an acid labile compound together with an alkaline reacting compound or an alkaline salt of an acid labile compound 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.
Inventors
- 👤 Kurt I. Lovgren
- 👤 Ake G. Pilbrant
- 👤 Mitsuru Yasumura
- 👤 Satoshi Morigaki
- 👤 Minoru Oda
- 👤 Naohiro Ohishi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 11:29
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K9/00; A61K9/20; A61K9/2004; A61K9/2009; A61K9/28; A61K9/2886; A61K9/48; A61K9/50; A61K9/5073
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
127 words
A pharmaceutical preparation comprising: (a) an alkaline reacting core comprising an acid-labile pharmaceutically active substance and an alkaline reacting compound different from said active substance, an alkaline salt of an acid labile pharmaceutically active substance, or an alkaline salt of an acid labile pharmaceutically active substance and an alkaline reacting compound different from said active substance; (b) an inert subcoating which rapidly dissolves or disintegrates in water disposed on said core region, said subcoating comprising one or more layers comprising materials selected from the group consisting of tablet excipients, film-forming compounds and alkaline compounds; and (c) an enteric coating layer surrounding said subcoating layer, wherein the subcoating layer isolates the alkaline reacting core from the enteric coating layer such that the stability of the preparation is enhanced.
Claim 2
Dependent Claim
127 words
A pharmaceutical preparation comprising: (a) an alkaline reacting core comprising an acid-labile pharmaceutically active substance and an alkaline reacting compound different from said active substance, an alkaline salt of an acid labile pharmaceutically active substance, or an alkaline salt of an acid labile pharmaceutically active substance and an alkaline reacting compound different from said active substance; (b) an inert subcoating which rapidly dissolves or disintegrates in water disposed on said core region, said subcoating comprising one or more layers comprising materials selected from the group consisting of tablet excipients, film-forming compounds and alkaline compounds; and (c) an enteric coating layer surrounding said subcoating layer, wherein the subcoating layer isolates the alkaline reacting core from the enteric coating layer such that the stability of the preparation is enhanced.
Claim 3
Dependent Claim
86 words
A preparation according to claim 1, wherein the acid labile compound has the general formula I, ##STR17## wherein A is an optionally substituted heterocyclic group, R 1 , R 2 , R 3 and R 4 are the same or different and select from among hydrogen, lower alkyl, lower alkoxy, --CF 3 , ##STR18## alkyl or halogen and R 5 is H or a lower alkyl group wherein "lower" denotes 1-6 carbon atoms except the compound omerprazole, 5-methoxy-2[[(4-methoxy-3,5 dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole; or the acid labile compound is 2-[(2-dimethylaminobenzyl)sulfinyl]-benzimidazole.
Claim 4
Dependent Claim
51 words
A preparation according to dlaim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance [Al 2 O 3 .6MgO.CO 2 .12H 2 O or MgO.Al 2 O 3 .2SiO 2 .nH 2 O], wherein n is not an integer and less than two.
Claim 5
Dependent Claim
51 words
A preparation according to dlaim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance [Al 2 O 3 .6MgO.CO 2 .12H 2 O or MgO.Al 2 O 3 .2SiO 2 .nH 2 O], wherein n is not an integer and less than two.
Claim 6
Dependent Claim
14 words
A preparation according to claim 2 wherein the subcoating comprises two or more sub-layers.
Claim 7
Dependent Claim
16 words
A preparation according to claim 4 wherein the subcoafting comprises hyroxypropyl methylcellulose, hyroxypropyl cellulose or polyvinyl-pyrrolidone.
Claim 8
Dependent Claim
35 words
A preparation according to claim 1, wherein an alkaline core comprises the acid labile compound and a pH-buffering alkaline reacting compound which renders to the micro-environment of the acid labile compound a pH of 7-12.
Claim 9
Dependent Claim
65 words
A preparation according to claim 6 wherein the alkaline reacting 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 2 O 3 .6MgO.CO 2 .12H 2 O or MgO.Al 2 O 3 .2SiO 2 .nH 2 O, wherein n is not an integer and less than two.
Claim 10
Dependent Claim
29 words
A preparation according to claim 1, wherein the alkaline core comprises an alkaline salt of the acid labile compound such as the sodium, potassium, magnesium calcium or ammonium salt.
Claim 11
Dependent Claim
25 words
A preparation according to claim 7 wherein the alkaline core comprises an alkaline salt of the acid labile compound mixed with an inert, alkaline compound.
Claim 12
Dependent Claim
31 words
A preparation according to claim 1, wherein the enteric coating comprises hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, co-polymerized methacrylic acid/methacrylic acid methyl ester or polyvinyl acetate phthalate, optionally containing a plasticizer.
Claim 13
Dependent Claim
26 words
A preparation according to claim 1, wherein the water content of the final dosage form containing the acid labile compound does not exceed 1.5% by weight.
Claim 14
Dependent Claim
70 words
Process for the preparation of an oral pharmaceutical formulation containing an acid labile compound in which cores containing the acid labile compound mixed with an alkaline reacting compound or compounds or an alkaline salt of the acid labile compound optionally mixed with an alkaline reacting compound or compounds are coated with one or more inert reacting subcoating layers whereafter the subcoated cores are further coated with an enteric coating layer.
Claim 15
Dependent Claim
70 words
Process for the preparation of an oral pharmaceutical formulation containing an acid labile compound in which cores containing the acid labile compound mixed with an alkaline reacting compound or compounds or an alkaline salt of the acid labile compound optionally mixed with an alkaline reacting compound or compounds are coated with one or more inert reacting subcoating layers whereafter the subcoated cores are further coated with an enteric coating layer.
Claim 16
Dependent Claim
33 words
A method for the treatment of gastrointestinal disease characterized in that a preparation according to claim 1 is administered to a host in the need of such treatment in a therapeutically effective amount.
Claim 17
Dependent Claim
26 words
A preparation according to claim 8, wherein the salt of the acid labile compound is selected from among the sodium, potassium, magnesium, calcium and ammonium salts.
Claim 18
Dependent Claim
15 words
A preparation according to claim 1, wherein the subcoating further comprises an alkaline buffering compound.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-07-31 | 1993-01-30 | 1993-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-31 | 1997-01-30 | 1997-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-31 | 2001-01-30 | 2001-08-01 | $7700.00 | Window Closed / Lapsed |