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US4713244A
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Sustained-release formulation containing an amino acid polymer with a lower alkyl (C1 -C4) polar solvent
Assignee: Bausch and Lomb Inc
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Filing: 1985-08-16
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Granted: 1987-12-15
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Expires: 2005-08-16
Abstract
Abstract A sustained-release polymeric hydrogel dosage form useful for topical, systemic or transdermal administration of a medicinal agent comprising a cross-linked, polymerized hydrophilic polymer, an amino acid polymer, a cross-linking agent, and an optional hydrophobic monomer and/or a chain regulator in conjunction with a lower alkyl (C 1 -C 4 ), polar solvent and said medicinal agent in a therapeutically effective amount.
Inventors
- 👤 Rajan Bawa
- 👤 William G. Deichert
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 17:17
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/30; A61K47/32; A61K9/00; A61K9/0012; A61K9/0014; A61K9/0048; A61K9/0051
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
53 words
A sustained-release polymeric hydrogel dosage form useful for topical, systemic or transdermal administration of a medicinal agent comprising a cross-linked, polymerized hydrophilic polymer including an amino acid moiety in the polymer, in conjunction with a lower alkyl (C 1 -C 4 ) polar solvent and said medicinal agent in a therapeutically effective amount.
Claim 2
Dependent Claim
53 words
A sustained-release polymeric hydrogel dosage form useful for topical, systemic or transdermal administration of a medicinal agent comprising a cross-linked, polymerized hydrophilic polymer including an amino acid moiety in the polymer, in conjunction with a lower alkyl (C 1 -C 4 ) polar solvent and said medicinal agent in a therapeutically effective amount.
Claim 3
Dependent Claim
15 words
The sustained-release dosage form of claim 1 wherein the polymer includes therein a hydrophobic component:
Claim 4
Dependent Claim
38 words
The sustained-release dosage form of claim 1 or 2 wherein the amino acid moiety is derived from an aliphatic monocarboxylic acid, an aliphatic dicarboxylic acid, an aromatic dicarboxylic acid, an aromatic tricarboxylic acid or an aromatic tetracarboxylic acid.
Claim 5
Dependent Claim
26 words
The sustained-release dosage form of claim 1 or 2 wherein the amino acid moiety is derived from methacroyl glycine, methacroyl glutamate, methacroyl desmosine or methacroyl isodesmosine.
Claim 6
Dependent Claim
60 words
The sustained-release dosage form of claim 1 or 2 wherein the polar solvent is a lower alkyl (C 1 -C 4 ) alcohol, an unmodified ketone, a modified ketone, a mixture of a lower alkyl (C 1 -C 4 ) alcohol and water in any proportion or a mixture of an unmodified ketone and a modified ketone in any proportion.
Claim 7
Dependent Claim
55 words
The sustained-release dosage form of claim 1 or 2 wherein said medicinal agent is an antibiotic, an antiviral, an anti-inflammatory, a steroid, a peptide, a polypeptide, a cardiotonic, an antihypertensive, an antiallergic, an alpha-adrenergic blocking agent, a beta-adrenergic blocking agent, an anticataract agent, an ophthalmic medicament, an ophthalmic lubricating agent or an ophthalmic anesthetic agent.
Claim 8
Dependent Claim
71 words
The sustained-release dosage form of claim 1 or 2 wherein said medicinal agent is selected from the group consisting of pilocarpine, idoxuridine, carbachol, bethanechol, timolol, tetracycline, epinephrine, phenylephrine, eserine, phospholine, demecarium, cyclopentolate, homatropine, scopolamine, nitroglycerin, chlortetracycline, bacitracin, neomycin, polymyxin, gramicidin, oxytetracycline, chloramphenicol, gentamycin, penicillin, erythromycin, sulfacetamide, polymyxin B, tobramycin, isofluorophate, fluoromethalone, dexamethasone, hydrocortisone, fluorocinolone, medrysone, prednisolone, methyl prednisolone, betamethasone, triamcinolone, interferon, cromolyn, all-trans-retinoic acid and a nontoxic, pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
32 words
The sustained-release dosage form of claim 1 or 2 wherein said medicinal agent is an ophthalmic lubricating agent selected from the group consisting of polyvinyl alcohol, a cellulose polymer and a polylactam.
Claim 10
Dependent Claim
18 words
The sustained-release dosage form of claim 1 or 2 wherein said medicinal agent is an ophthalmic anesthetic agent.
Claim 11
Dependent Claim
37 words
The sustained-release dosage form of claim 1 or 2 wherein said dosage form is molded as a contact lens or ocular insert for ophthalmic administration of a systemic medicament, an ophthalmic medicament or an ophthalmic lubricating agent.
Claim 12
Dependent Claim
41 words
The sustained-release dosage form of claim 1 or 2 wherein said dosage form is molded as a contact lens for opthalmic administration of a systemic medicament, an ophthalmic medicament or an ophthalmic lubricating agent and retains the ability to correct vision.
Claim 13
Dependent Claim
86 words
The sustained-release dosage form of claim 2 wherein a polymeric hydrogel is prepared from a polymerizable hydrophilic monomer present in the amount of about 50% to about 90% w/w, an amino acid monomer present in the amount of about 5% to about 27% w/w, a cross-linking agent present in the amount of about 3% to about 30% w/w and a hydrophobic monomer present in the amount of about 8% to about 20% w/w, the weight percent being based on the total weight of the polymeric hydrogel.
Claim 14
Dependent Claim
56 words
A method of administering a therapeutically effective amount of a medicinal agent over an extended period of time to a mammal in need of the medicinal agent for local or systemic effect which comprises contacting a tissue of said mammal with the sustained-release dosage form of claim 1 or 2 for a prolonged period of time.
Claim 15
Dependent Claim
59 words
A method of administering a therapeutically effective amount of an ophthalmic medicament over an extended period of time to a mammal in need of the medicament which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2 for a prolonged period of time, wherein said medicinal agent is the opthalmic medicament.
Claim 16
Dependent Claim
61 words
A method of administering a therapeutically effective amount of an ophthalmic lubricating agent over an extended period of time to a mammal in need of the agent which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2 for a prolonged period of time, wherein said medicinal agent is the ophthalmic lubricating agent.
Claim 17
Dependent Claim
61 words
A method of administering a therapeutically effective amount of an ophthalmic anesthetic agent over an extended period of time to a mammal in need of ophthalmic anesthesia which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2 for a prolonged period of time, wherein said medicinal agent is the ophthalmic anesthetic agent.
Claim 18
Dependent Claim
47 words
A method of treating glaucoma in a mammal suffering from glaucoma which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2, wherein said medicinal agent is an agent for reducing intraocular pressure for a prolonged period of time.
Claim 19
Dependent Claim
50 words
A method of treating glaucoma in a mammal suffering from glaucoma which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2, wherein said medicinal agent is timolol, pilocarpine or a nontoxic, pharmaceutically acceptable salt thereof for a prolonged period of time.
Claim 20
Dependent Claim
51 words
A method of inducing natural lacrimation or creating artificial lacrimation in a mammal suffering from deficient lacrimation which comprises contacting an eye tissue of said mammal with the sustained-release dosage form of claim 1 or 2 for a prolonged period of time, wherein said medicinal agent is an ophthalmic lubricating agent.
Claim 21
Dependent Claim
47 words
A process for the preparation of the sustained-release dosage form of claim 1 which comprises mixing a hydrophilic monomer, an amino acid monomer, a cross-linking agent and a lower alkyl (C 1 -C 4 ), polar solvent, polymerizing at room temperature, adding a medicinal agent and cross-linking.
Claim 22
Dependent Claim
50 words
A process for the preparation of the sustained-release dosage form of claim 2 which comprises mixing a hydrophilic monomer, an amino acid monomer, a cross-linking agent, a hydrophobic monomer and a lower alkyl (C 1 -C 4 ), polar solvent, polymerizing at room temperature, adding a medicinal agent and cross-linking.
Claim 23
Dependent Claim
12 words
The process of claim 20 or 21 wherein a catalyst is used.
Claim 24
Dependent Claim
13 words
The process of claim 20 or 21 wherein a chain regulator is added.
Claim 25
Dependent Claim
18 words
The process of claim 20 or 21 wherein a catalyst is used and a chain regulator is added.
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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) | 1990-12-14 | 1991-06-15 | 1991-12-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-12-14 | 1995-06-15 | 1995-12-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-12-14 | 1999-06-15 | 1999-12-15 | $7700.00 | Window Closed / Lapsed |