US4178361A
Expired / Lapsed
US
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Sustained release pharmaceutical composition
Assignee: Iolab Corp
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Filing: 1975-12-01
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Granted: 1979-12-11
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Expires: 1995-12-01
Abstract
Abstract A sustained release pharmaceutical composition which includes a pharmacological material; a biological binding agent for the pharmacological material; and a matrix of a water-insoluble but water-swellable hydrophilic polymer.
Inventors
- 👤 Arthur I. Cohen
- 👤 James S. Y. Sim
- 👤 Maurice H. Van Horn
- 👤 Stanley E. Gordesky
- 👤 Stanley I. Gordon
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:44
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2027
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
129 words
A sustained release pharmaceutical composition comprising: (A) a pharmacological material in an amount at least sufficient for the total dosage during a treatment period; (B) a biological binding agent for said pharmacological material, said biological binding agent containing bonding sites complementary to bonding sites of the pharmacological material in an amount effective to bind the pharmacological materials and to provide for the sustained release of said pharmacological material in the desired dosage amount; (C) a matrix of a water-insoluble but water-swellable hydrophilic polymer, which holds said biological binding agent; (D) the molecular size or weight of the biological binding agent being sufficient to cause retention of said biological binding agent in said matrix and to prevent egress of said biological binding agent from said matrix during the treatment period.
Claim 2
Dependent Claim
129 words
A sustained release pharmaceutical composition comprising: (A) a pharmacological material in an amount at least sufficient for the total dosage during a treatment period; (B) a biological binding agent for said pharmacological material, said biological binding agent containing bonding sites complementary to bonding sites of the pharmacological material in an amount effective to bind the pharmacological materials and to provide for the sustained release of said pharmacological material in the desired dosage amount; (C) a matrix of a water-insoluble but water-swellable hydrophilic polymer, which holds said biological binding agent; (D) the molecular size or weight of the biological binding agent being sufficient to cause retention of said biological binding agent in said matrix and to prevent egress of said biological binding agent from said matrix during the treatment period.
Claim 3
Dependent Claim
44 words
The sustained release pharmaceutical composition of claim 1 wherein said pharmacological material is present in an amount from about 0.1 to about 50% by weight based upon the total weight of the pharmacological material, biological binding agent, and the water-insoluble but water-swellable hydrophilic polymer.
Claim 4
Dependent Claim
45 words
The sustained release pharmaceutical composition of claim 1 wherein said pharmacological material is present in an amount from about 0.5 to about 20% by weight based upon the total weight of the pharmacological material, biological binding agent, and the water-insoluble but water swellable hydrophilic polymer.
Claim 5
Dependent Claim
16 words
The sustained release pharmaceutical composition of claim 1 wherein said biological binding agent is a carbohydrate.
Claim 6
Dependent Claim
31 words
The sustained release pharmaceutical composition of claim 1 wherein the pharmacological material is bound to the biological binding agent by bonds which include ionic bonds, and/or hydrogen bonds, and/or hydrophobic bonds.
Claim 7
Dependent Claim
22 words
The sustained release pharmaceutical composition of claim 1 wherein the biological binding agent has a molecular weight of at least about 300.
Claim 8
Dependent Claim
44 words
The sustained release pharmaceutical composition of claim 1 wherein the biological binding agent is present in an amount from about 1 to about 80% by weight based upon the total weight of the pharmacological material, biological binding agent, and water-insoluble but water-swellable hydrophilic polymer.
Claim 9
Dependent Claim
44 words
The sustained release pharmaceutical composition of claim 1 wherein the biological binding agent is present in an amount from about 20 to about 60% by weight based upon the total weight of the pharmacological material, biological binding agent, and water-insoluble but water-swellable hydrophilic polymer.
Claim 10
Dependent Claim
107 words
The sustained release pharmaceutical composition of claim 1 wherein said water-insoluble but water-swellable polymer is a copolymer of a monomer mixture of: (A) a polymerizable monoester of acrylic and/or methacrylic acid and a polyhydric alcohol; and (B) a crosslinking agent selected from the group consisting of a divinyl benzene, divinyl toluene, a polymerizable diester of acrylic and/or methacrylic acid and a polyhydric alcohol, and mixtures thereof, wherein the monomer mixture contains based upon the total weight of the polymerizable monoester and crosslinking agent from about 80% to about 99.95% by weight of the monoester and from about 0.05 to about 20% by weight of the crosslinking agent.
Claim 11
Dependent Claim
15 words
The sustained release pharmaceutical composition of claim 1 wherein said biological binding agent is heparin.
Claim 12
Dependent Claim
15 words
The sustained release pharmaceutical composition of claim 1 wherein said pharmacological material is methantheline bromide.
Claim 13
Dependent Claim
120 words
A process for preparing the sustained release pharmaceutical composition of claim 1 which comprises: (A) admixing a monomeric composition being polymerizable to form a water-insoluble but water-swellable hydrophilic polymer and a biological binding agent; (B) polymerizing the monomeric mixture to form a maxtrix of a water-insoluble but water-swellable hydrophilic polymer having dispersed therein the biological binding agent; (C) adding to the resultant product a pharmacological material in an amount at least sufficient for the total dosage requirement during a treatment period; the molecular size or weight of the biological binding agent being sufficient to cause retention of said biological binding agent in said matrix and to prevent egress of said biological binding agent from said matrix during the treatment period.
Claim 14
Dependent Claim
113 words
A process for preparing the sustained release pharmaceutical composition of claim 1 which comprises: (A) contacting the pharmacological material and the biological binding agent to bond the pharmacological material to the biological binding agent; (B) admixing the resulting composition with a monomeric composition being polymerizable to a water-insoluble but water-swellable hydrophilic polymer; (C) polymerizing to form a matrix of a water-insoluble but water-swellable hydrophilic polymer having dispersed therein the biological binding agent; and (D) the molecular size or weight of the biological binding agent being sufficient to cause retention of said biological binding agent in said matrix and to prevent egress of said biological binding agent from said matrix during the treatment period.
Claim 15
Dependent Claim
79 words
The sustained release pharmaceutical composition of claim 1 wherein said pharmacological material is methantheline; said binding agent is heparin; and said water-insoluble but water-swellable hydrophilic polymer is a polymer of a monomer mixture of hydroxyethyl methacrylate and divinyl benzene wherein the monomer mixture contains based upon the total weight of the methacrylate and divinyl benzene from about 80% to about 99.95% by weight of the methacrylate and from about 0.05 to about 20% by weight of the divinyl benzene.
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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) | 1982-12-10 | 1983-06-11 | 1983-12-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-12-10 | 1987-06-11 | 1987-12-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-12-10 | 1991-06-11 | 1991-12-11 | $7700.00 | Window Closed / Lapsed |