US4803081A
Expired / Lapsed
US
⏱️ 0.0 years remaining
New pharmaceutical preparations with extended release
Assignee: Hassle AB
•
Filing: 1987-04-03
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Granted: 1989-02-07
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Expires: 2007-04-03
Abstract
Abstract An extended release perparation of an active compound with very low solubility containing the active compound dissolved or dispersed in a semi-solid or liquid non-ionic solubilizer and whereby the amount by weight of the solubilizer is at least equal to the amount by weight of the active compound as well as a process for the preparation thereof.
Inventors
- 👤 Karl-Erik L. Falk
- 👤 Sven M. Hugosson
- 👤 Adam Rosinski
- 👤 John A. Sjogren
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 15:55
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/20; A61K9/2004; A61K9/2013; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/14; A61K9/16; A61K9/1605; A61K9/1617; A61K9/2022; A61K9/205; A61K9/2054
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
66 words
A solid preparation providing extended release of an active compound with very low solubility in water copmrising a solution or dispersion of an effective amount of the active compound in a semi-solid or liquid nonionic solubilizer, wherein the amount by weight of the solubilizer is at least equal to the amount by weight of the active compound, and a release controlling system to provide extended release.
Claim 2
Dependent Claim
66 words
A solid preparation providing extended release of an active compound with very low solubility in water copmrising a solution or dispersion of an effective amount of the active compound in a semi-solid or liquid nonionic solubilizer, wherein the amount by weight of the solubilizer is at least equal to the amount by weight of the active compound, and a release controlling system to provide extended release.
Claim 3
Dependent Claim
18 words
A preparation according to claim 1 wherein the non-ionic solubilizer is selected from esters and/or ethers of polyethyleneglycols.
Claim 4
Dependent Claim
22 words
A preparation according to claim 1 wherein the non-ionic solubilizer is selected from polyethoxylated fatty acids, hydroxylated fatty acids or fatty alcohols.
Claim 5
Dependent Claim
36 words
A preparation according to claim 1 wherein the non-ionic solubilizer is selected from polyethoxylated castor oil, polyethoxylated hydrogenated castor oil, a polyethoxylated fatty acid from castor oil or a polyethoxylated fatty acid from hydrogenated castor oil.
Claim 6
Dependent Claim
25 words
A preparation according to claim 4 wherein the non-ionic solubilizer is esters of hydrogenated castor oil fatty acids wit oxyethylated glycerine, especially Cremophor® 40 (BASF).
Claim 7
Dependent Claim
32 words
A preparation according to claim 1 wherein the proportions between the active compound and the solubilizer varies in the range from 1:1 to 1:10, preferably in the range from 1:2 to 1:6.
Claim 8
Dependent Claim
38 words
A preparation according to claim 1 wherein the active compound has a solubility in water of 1:1000 or less by weight and is solubilizable in the non-ionic solubilizer or in a combination of water and the non-ionic solubilizer.
Claim 9
Dependent Claim
16 words
A preparation according to claim 1 wherein the active compound comprises one or more substituted dihydropyridines.
Claim 10
Dependent Claim
12 words
A preparation according to claim 8 wherein the substituted dihydropyridine is nifedipine.
Claim 11
Dependent Claim
12 words
A preparation according to claim 8 wherein the substituted dihydropyridine is felodipine.
Claim 12
Dependent Claim
24 words
A preparation according to claim 1 wherein the release is controlled by an inert porous matrix, a diffusion retarding coating or a disintegrating coating.
Claim 13
Dependent Claim
16 words
A preparation according to claim 1 wherein the release is controlled by a hydrophilic gel system.
Claim 14
Dependent Claim
19 words
A preparation according to claim 12 wherein the hydrophilic gelforming component constitutes between 20-80% by weight of the preparation.
Claim 15
Dependent Claim
14 words
A preparation according to claim 12 wherein the hydrophilic gel system comprises hydroxypropyl methylcellulose.
Claim 16
Dependent Claim
18 words
A preparation according to claim 14 wherein the hydroxypropyl methylcellulose has a hydroxypropyl content of 4-12% by weight.
Claim 17
Dependent Claim
13 words
A preparation according to claim 12 wherein the hydrophilic gel system contains carboxypolymethylene.
Claim 18
Dependent Claim
78 words
A process for making a solid preparation that provides extended release of an active compound with very low solubility in water comprising dissolving or dispersing an effective amount of the active compound in a semi-solid or liquid nonionic solubilizer, the amount by weight of said solubilizer being at least equal to the amount by wight of the active compound, and incorporating the resulting solution or dispersion into a suitable release controlling system to form a pharmaceutical dosage unit.
Claim 19
Dependent Claim
78 words
A process for making a solid preparation that provides extended release of an active compound with very low solubility in water comprising dissolving or dispersing an effective amount of the active compound in a semi-solid or liquid nonionic solubilizer, the amount by weight of said solubilizer being at least equal to the amount by wight of the active compound, and incorporating the resulting solution or dispersion into a suitable release controlling system to form a pharmaceutical dosage unit.
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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) | 1992-02-07 | 1992-08-08 | 1993-02-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-02-07 | 1996-08-08 | 1997-02-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-02-07 | 2000-08-08 | 2001-02-07 | $7700.00 | Window Closed / Lapsed |