EP0244380A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Pharmaceutical formulations of acid labile substances for oral use
Assignee: Hassle AB
•
Filing: 1987-04-16
•
Granted: —
•
Expires: 2007-04-16
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 Ingmar Lövgren
- 👤 Ake Gunnar Pilbrant
- 👤 Mitsuru Yasumura
- 👤 Satoshi Morigaki
- 👤 Minoru Oda
- 👤 Naohiro Ohishi
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 20:05
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: 27
Claim 1
Independent Claim
95 words
An oral, pharmaceutical preparation containing an acid labile compound as the active ingredient characterized in that it is composed of core material containing the active ingredient together with an alkaline reacting compound, or an alkaline salt of the active ingredient -optionally together with an alkaline reacting compound, and on said core material one or more inert reacting subcoating layers comprising tablet excipients which are soluble or rapidly disintegrating in water, or polymeric, water soluble, filmforming compounds, optionally containing pH-buffering, alkaline compounds between the alkaline reacting core and an outer layer, which is an enteric coating.
Claim 2
Dependent Claim
95 words
An oral, pharmaceutical preparation containing an acid labile compound as the active ingredient characterized in that it is composed of core material containing the active ingredient together with an alkaline reacting compound, or an alkaline salt of the active ingredient -optionally together with an alkaline reacting compound, and on said core material one or more inert reacting subcoating layers comprising tablet excipients which are soluble or rapidly disintegrating in water, or polymeric, water soluble, filmforming compounds, optionally containing pH-buffering, alkaline compounds between the alkaline reacting core and an outer layer, which is an enteric coating.
Claim 3
Dependent Claim
87 words
A preparation according to claim 1, wherein the acid labile compound has the general formula I. wherein A is an optionally substituted heterocyclic group, R 1 , R 2 , R 3 and R 4 are the same or different and preferably hydrogen, lower alkyl, lower alkoxy, -CF 3 , - lower alkyl or halogen and R 5 is H or a lower alkyl group wherein "lower" denotes 1-6 carbon atoms except the compound omeprazole, 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 claim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance [Al 2 O 3.6 Mg0.CO 2 .12H 2 O or MgO.Al 2 O 3 .2SiO 2 .nH 2 O], wherein n not is an integer and less than two.
Claim 5
Dependent Claim
16 words
A preparation according to claim 2 or 3 wherein the subcoating comprises two or more sub-layers.
Claim 6
Dependent Claim
16 words
A preparation according to claim 4 wherein the subcoating comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose or polyvinyl--pyrrolidone.
Claim 7
Dependent Claim
32 words
A preparation according to claim 1 wherein the alkaline core comprises the acid labile compound and pH-buffering alkaline compound rendering to the micro-environment of the acid labile compound a pH of 7-12.
Claim 8
Dependent Claim
58 words
A preparation according to claim 6 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 A1203.6Mg0.C02.12H20 or M g 0.A1 2 0 3 .2Si0 2 .nH 2 0, wherein n not is an integer and less than two.
Claim 9
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 10
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 11
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 12
Dependent Claim
27 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 13
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 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
19 words
Use of the preparation according to claim 1 for the manufacture of a medicament for treatment of gastrointestinal diseases.
Claim 16
Dependent Claim
119 words
CLAIMS FOR THE CONTRACTING STATES AT, ES, GR. 1. A process for the preparation of an oral, pharmaceutical formulation containing an acid labile compound as the active ingredient characterized in that the cores containing the acid labile compound mixed with an alkaline reacting compound, or an alkaline salt of the active ingredient optionally together with an alkaline reacting compound, are coated with one or more inert reacting subcoating layers comprising tablet excipients which are soluble or rapidly disintegrating in water, or polymeric, water soluble, filmforming compounds, optionally containing pH-buffering, alkaline compounds between the alkaline reacting core and an outer layer, which is an enteric coating layer, whereafter the subcoated cores are further coated with said outer enteric coating layer.
Claim 17
Dependent Claim
89 words
A process according to claim 1, wherein the acid labile compound has the general formula I. wherein A is an optionally substituted heterocyclic group, R 1 , R 2 , R 3 and R 4 are the same or different and preferably hydrogen, lower alkyl, lower alkoxy, -CF 3 , - lower alkyl or halogen and R 5 is H or a lower alkyl group wherein "lower" denotes 1-6 carbon atoms except the compound omeprazole, 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 18
Dependent Claim
54 words
A process according to claim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance L A1 2 0 3 .6M g 0.C0 2 .12H 2 0 or MgO.Al 2 O 3 .2SiO 2 .nH 2 O], wherein n not is an integer and less than two.
Claim 19
Dependent Claim
16 words
A process according to claim 2 or 3 wherein the subcoating comprises two or more sub-layers.
Claim 20
Dependent Claim
16 words
A process according to claim 4 wherein the subcoating comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose or polyvinyl--pyrrolidone.
Claim 21
Dependent Claim
32 words
A process according to claim 1 wherein the alkaline core comprises the acid labile compound and pH-buffering alkaline compound rendering to the micro-environment of the acid labile compound a pH of 7-12.
Claim 22
Dependent Claim
66 words
A process according to claim 6 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 2 O 3 .6MgO.CO 2 .12H 2 O or M g O.A1 2 0 3 .2Si0 2 .nH 2 0, wherein n not is an integer and less than two.
Claim 23
Dependent Claim
29 words
A process 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 24
Dependent Claim
25 words
A process according to claim 7 wherein the alkaline core comprises an alkaline salt of the acid labile compound mixed with an inert, alkaline compound.
Claim 25
Dependent Claim
31 words
A process 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 26
Dependent Claim
27 words
A process 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 27
Dependent Claim
20 words
Use of the formulation prepared according to claim 1 for the manufacture of a medicament for treatment of gastrointestinal diseases.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.