US4248855A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical base salts
Assignee: Hydrophilics International Inc
•
Filing: 1976-08-27
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Granted: 1981-02-03
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Expires: 1996-08-27
Abstract
Abstract A salt of a polymer, containing acid groups, soluble or dispersible in water or organic solvents, is combined with a salt-forming pharmaceutically effective compound for application, orally, topically, or systemically. A sustained release of the pharmaceutical compound is thus obtained.
Inventors
- 👤 Izhak Blank
- 👤 Joseph Fertig
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:47
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2027; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
125 words
A method of preparing a stable fluid composition for sustained release of a phramaceutical compound comprising the steps of: dissolving a pharmaceutically pure, acid group containing, water-insoluble, synthetic polymer and a salt-forming basic nitrogen containing pharmaceutically effective compound in organic solvent to form a salt of the polymer and the pharmaceutical compound in organic solution, slowly adding water to said salt solution without coagulating the polymer salt, and removing the organic solvent under vacuum to form a stable emulsion consisting of said salt in water; said polymer comprising from 10 to 75% by weight of at least one hydrophilic monomer and from 25 to 90% by weight of at least one hydrophobic monomer; at least 50% of the acid groups of said polymer being neutralized.
Claim 2
Independent Claim
125 words
A method of preparing a stable fluid composition for sustained release of a phramaceutical compound comprising the steps of: dissolving a pharmaceutically pure, acid group containing, water-insoluble, synthetic polymer and a salt-forming basic nitrogen containing pharmaceutically effective compound in organic solvent to form a salt of the polymer and the pharmaceutical compound in organic solution, slowly adding water to said salt solution without coagulating the polymer salt, and removing the organic solvent under vacuum to form a stable emulsion consisting of said salt in water; said polymer comprising from 10 to 75% by weight of at least one hydrophilic monomer and from 25 to 90% by weight of at least one hydrophobic monomer; at least 50% of the acid groups of said polymer being neutralized.
Claim 3
Dependent Claim
123 words
A stable fluid composition for sustained release of a pharmaceutical compound, said composition consisting of a stable emulsion in water of a salt of a pharmaceutically pure, acid group containing, water-insoluble synthetic polymer and a salt-forming basic nitrogen containing, pharmaceutically effective compound; said polymer comprising from 10 to 75% by weight of at least one hydrophilic monomer and from 25 to 90% by weight of at least one hydrophobic monomer; at least 50% of the acid groups of said polymer being neutralized; said emulsion being formed by dissolving purified polymer and pharmaceutical compound in an organic solvent to form the desired salt in organic solution, slowly adding water to the solution without coagulating the polymer salt and removing the organic solvent under vacuum.
Claim 4
Dependent Claim
123 words
A stable fluid composition for sustained release of a pharmaceutical compound, said composition consisting of a stable emulsion in water of a salt of a pharmaceutically pure, acid group containing, water-insoluble synthetic polymer and a salt-forming basic nitrogen containing, pharmaceutically effective compound; said polymer comprising from 10 to 75% by weight of at least one hydrophilic monomer and from 25 to 90% by weight of at least one hydrophobic monomer; at least 50% of the acid groups of said polymer being neutralized; said emulsion being formed by dissolving purified polymer and pharmaceutical compound in an organic solvent to form the desired salt in organic solution, slowly adding water to the solution without coagulating the polymer salt and removing the organic solvent under vacuum.
Claim 5
Dependent Claim
44 words
The composition of claim 2 wherein the hydrophilic groups of the polymer are selected from acrylic acid, vinyl pyrrolidone, methacrylic acid and maleic anhydride and the hydrophobic groups of the polymer are selected from methyl methacrylate, butyl methacrylate, lauryl methacrylate, methylacrylate, 2-ethyl-hexacrylate and styrene.
Claim 6
Dependent Claim
31 words
The composition of claim 1 in which the monomers from which the polymer is made comprise at least one monomer selected from the class consisting of acrylic acid and vinyl pyrrolidone.
Claim 7
Dependent Claim
15 words
The composition of claim 4 in which the monomers include 20 to 55% acrylic acid.
Claim 8
Dependent Claim
14 words
The composition of claim 2 in which the pharmaceutically effective compound is an alkaloid.
Claim 9
Dependent Claim
13 words
The composition of claim 2 in which the pharmaceutically effective compound is pilocarpine.
Claim 10
Dependent Claim
16 words
The composition of claim 2 in which the pharmaceutically effective compound is cocaine, dibucaine or morphine.
Claim 11
Dependent Claim
15 words
The composition of claim 2 in which the pharmaceutically effective compound is a local anaesthetic.
Claim 12
Dependent Claim
14 words
The composition of claim 2 in which the pharmaceutically effective compound is an analgesic.
Claim 13
Dependent Claim
11 words
The composition of claim 10 in which the compound is lidocaine.
Claim 14
Dependent Claim
14 words
The composition of claim 2 in which the pharmaceutically effective compound is a sulphonamide.
Claim 15
Dependent Claim
11 words
The composition of claim 12 in which the compound is sulphadimetoxin.
Claim 16
Dependent Claim
21 words
The composition of claim 2 in the form of an emulsion wherein the carrier is in the form of a liquid.
Claim 17
Dependent Claim
12 words
The composition of claim 14 wherein the pharmaceutically effective compound is pilocarpine.
Claim 18
Dependent Claim
20 words
The composition as recited in claim 2 wherein the water-insoluble polymer is capable of absorbing water to form a gel.
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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) | 1984-02-03 | 1984-08-04 | 1985-02-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-02-03 | 1988-08-04 | 1989-02-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-02-03 | 1992-08-04 | 1993-02-03 | $7700.00 | Window Closed / Lapsed |