US5133974A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Extended release pharmaceutical formulations
Assignee: Kv Pharmaceutical Co
•
Filing: 1990-01-24
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Granted: 1992-07-28
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Expires: 2010-01-24
Abstract
Abstract An extended release pharmaceutical formulation adapted to approach zero order release of drug over a 12 to at least 24 hour period, comprised of a mixture of 0 to aobut 50% of an immediate release particle containing a drug, inert substrate and binder, coated with talc and up to 100% of an extended release particle comprising the immediate release particle coated with a dissolution modifying system containing plasticizers and a film forming agent.
Inventors
- 👤 George N. Paradissis
- 👤 James A. Garegnani
- 👤 Roy S. Whaley
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 17:06
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5084; A61K9/5073; A61K9/5078
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
190 words
An extended release pharmaceutical formulation for oral administration, which comprises: a pharmaceutical formulation which is adapted to approach zero order release of drug over a 12 to at least a 24 hour period, which formulation is comprised of a mixture of a) about 0% to about 50% of an immediate release particle containing a core comprising a therapeutically effective amount of at least one water-soluble or water-insoluble drug, about 15% to about 40% by weight inert spherical substrate particles, and about 0.5% to about 4% by weight binder, coated with about 4% to about 20% by weight talc and having a particle size of -10+60 mesh size, U.S. Standard sieve size, and b) up to 100% of an extended release particle comprising about 65% to about 95% by weight of the immediate release particle of a) additionally coated with about 5.0% to about 35% by weight of a dissolution modifying system comprising a film forming agent and plasticizer, wherein the extended release particle has a particle size of -10+60 mesh size, U.S. Standard sieve mesh size, and wherein all percentages are based on the total weight of the pharmaceutical formulation.
Claim 2
Dependent Claim
190 words
An extended release pharmaceutical formulation for oral administration, which comprises: a pharmaceutical formulation which is adapted to approach zero order release of drug over a 12 to at least a 24 hour period, which formulation is comprised of a mixture of a) about 0% to about 50% of an immediate release particle containing a core comprising a therapeutically effective amount of at least one water-soluble or water-insoluble drug, about 15% to about 40% by weight inert spherical substrate particles, and about 0.5% to about 4% by weight binder, coated with about 4% to about 20% by weight talc and having a particle size of -10+60 mesh size, U.S. Standard sieve size, and b) up to 100% of an extended release particle comprising about 65% to about 95% by weight of the immediate release particle of a) additionally coated with about 5.0% to about 35% by weight of a dissolution modifying system comprising a film forming agent and plasticizer, wherein the extended release particle has a particle size of -10+60 mesh size, U.S. Standard sieve mesh size, and wherein all percentages are based on the total weight of the pharmaceutical formulation.
Claim 3
Dependent Claim
35 words
The extended release pharmaceutical formulation of claim 1, wherein the drug is selected from the group consisting of analgesics, anti-inflammatories, antihistamines, antitussives, expectorants, decongestants, narcotics, antibiotics, bronchodilators, cardiovasculars, central nervous system drugs, and mixtures thereof.
Claim 4
Dependent Claim
29 words
The extended release pharmaceutical formulation of claim 1, wherein the inert spherical substrate particles are selected from the group consisting of sugar spheres and non- toxic plastic resin beads.
Claim 5
Dependent Claim
33 words
The extended release pharmaceutical formulation of claim 1, which additionally contains preblended with the drug a non-toxic carrier selected from the group consisting of sugar, lactose, gelatin, starch, silicon dioxide and mixtures thereof.
Claim 6
Dependent Claim
23 words
The extended release pharmaceutical formulation of claim 1 wherein the binder is soluble in a solvent selected from water and an organic solvent.
Claim 7
Dependent Claim
30 words
The formulation of claim 5, wherein the binder is selected from the group consisting of povidone, pharmaceutical glaze, sugar, hydroxpropylmethylcellulose, hydroxpropylcellulose, ethylcellulose, acrylic and methacrylic acid co-polymers and mixtures thereof.
Claim 8
Dependent Claim
49 words
The extended release pharmaceutical formulation of claim 1 wherein the plasticizers which are used to form the extended release particle are selected from the group consisting of diethyl phthalate, diethyl sebacate, triethyl citrate, crotonic acid, propylene glycol, castor oil, citric acid esters, dibutyl phthalate, dibutyl sebacate and mixtures thereof.
Claim 9
Dependent Claim
30 words
The extended release pharmaceutical formulation of claim 1 wherein the film forming agent is selected from the group consisting of ethylcellulose, methylcellulose, hydroxypropylcellulose, cellulose acetate, hydroxypropylmethylcellulose, hydroxyethylcellulose and mixtures thereof.
Claim 10
Dependent Claim
49 words
The extended release pharmaceutical formulation of claim 1 wherein the immediate release particle contains a core comprising about 15 to about 40% inert spherical substrate particles, about 0.5 to about 4% binder and about 4 to about 85% drug, all percents herein are by weight of the final product.
Claim 11
Dependent Claim
13 words
The extended release pharmaceutical formulation of claim 2 wherein the expectorant is guaifenesin.
Claim 12
Dependent Claim
187 words
The extended release pharmaceutical formulation for oral administration, which comprises: a pharmaceutical formulation which is adapted to release a drug over a 12 to at least a 24 hour period, which formulation is comprised of a mixture of a) about 0% to about 50% of an immediate release particle containing a core comprising a therapeutically effective amount of at least one water-soluble or water-insoluble drug, about 15% to about 40% by weight inert spherical substrate particles, and about 0.5% to about 5% by weight binder, coated with about 4% to about 20% by weight talc and having a particle size of -10+60 mesh size, U.S. Standard sieve size, and b) up to 100% of an extended release particle comprising about 65% to about 95% by weight of the immediate release particle of a) additionally coated with about 5.0% to about 35% by weight of a dissolution modifying system comprising a film forming agent and plasticizer, wherein the extended release particle has a particle size of -10+60 mesh size, U.S. Standard sieve mesh size, and wherein all percentages are based on the total weight of the pharmaceutical formulation.
Claim 13
Dependent Claim
187 words
The extended release pharmaceutical formulation for oral administration, which comprises: a pharmaceutical formulation which is adapted to release a drug over a 12 to at least a 24 hour period, which formulation is comprised of a mixture of a) about 0% to about 50% of an immediate release particle containing a core comprising a therapeutically effective amount of at least one water-soluble or water-insoluble drug, about 15% to about 40% by weight inert spherical substrate particles, and about 0.5% to about 5% by weight binder, coated with about 4% to about 20% by weight talc and having a particle size of -10+60 mesh size, U.S. Standard sieve size, and b) up to 100% of an extended release particle comprising about 65% to about 95% by weight of the immediate release particle of a) additionally coated with about 5.0% to about 35% by weight of a dissolution modifying system comprising a film forming agent and plasticizer, wherein the extended release particle has a particle size of -10+60 mesh size, U.S. Standard sieve mesh size, and wherein all percentages are based on the total weight of the pharmaceutical formulation.
Claim 14
Dependent Claim
40 words
The formulation of claim 1, wherein the coating over the immediate release particle contains about 0.5 to about 25% film forming agent by weight, about 0.01 to about 5% plasticizer by weight, and up to 25% of porosity modifying agents.
Claim 15
Dependent Claim
20 words
The formulation of claim 1, wherein the dissolution modifying system of the immediate release particles contains additional amounts of drugs.
Claim 16
Dependent Claim
23 words
The extended release pharmaceutical formulation of claim 1, wherein the formulation is administered in the form of a tablet, capsule or particle form.
Claim 17
Dependent Claim
26 words
The extended release pharmaceutical formulation of claim 2, wherein the analgesics are selected from the group consisting of acetaminophen, ibuprofen, flurbiprofen, ketoprofen, phenacetin, voltaren and salicylamide.
Claim 18
Dependent Claim
22 words
The extended release pharmaceutical formulation of claim 2, wherein the anti-inflammatory drugs are selected from the group consisting of naproxen and indomethacin.
Claim 19
Dependent Claim
39 words
The extended release pharmaceutical formulation of claim 2, wherein the antihistamines are selected from the group consisting of chlorpheniramine maleate, phenindamine tartrate, pyrilamine maleate, doxylamine succinate, phenyltoloxamine citrate, diphenhydramine hydrochloride, promethazine, brompheniramine maleate, dexbrompheniramine maleate, clemastine fumerate, and triprolidine.
Claim 20
Dependent Claim
22 words
The extended release pharmaceutical formulation of claim 2, wherein the antitussives are selected from the group consisting of dextromethorphan hydrobromide and guaifenesin.
Claim 21
Dependent Claim
26 words
The extended release pharmaceutical formulation of claim 2, wherein the decongestants are selected from the group consisting of phenylephrine hydrochloride, phenypropanolamine hydrochloride, pseudoephedrine hydrochloride and ephedrine.
Claim 22
Dependent Claim
17 words
The extended release pharmaceutical formulation of claim 1, wherein the drug is phenylpropanolamine hydrochloride and chlorpheniramine maleate.
Claim 23
Dependent Claim
143 words
An extended release pharmaceutical formation for oral administration which comprises: a pharmaceutical formulation which is adapted to approach zero order release of drug over a 12 to at least 24 hour period, which formulation is comprised of a mixture of: a) 0 to about 50% of an immediate release particle containing about 15 to about 40% by weight inert spherical substrate particle about 0.5 to about 4% binder and about 4 to about 85% of at least one drug and a coating comprising about 4 to about 20% talc; and b) up to 100% of an extended release particle comprising an immediate release particle of a) coated with a dissolution modifying system comprising about 0.5 to about 25% film forming agent, about 0.01 to about 5% plasticizer and up to 25% modifying agent, all percents herein are by weight of the final product.
Claim 24
Dependent Claim
143 words
An extended release pharmaceutical formation for oral administration which comprises: a pharmaceutical formulation which is adapted to approach zero order release of drug over a 12 to at least 24 hour period, which formulation is comprised of a mixture of: a) 0 to about 50% of an immediate release particle containing about 15 to about 40% by weight inert spherical substrate particle about 0.5 to about 4% binder and about 4 to about 85% of at least one drug and a coating comprising about 4 to about 20% talc; and b) up to 100% of an extended release particle comprising an immediate release particle of a) coated with a dissolution modifying system comprising about 0.5 to about 25% film forming agent, about 0.01 to about 5% plasticizer and up to 25% modifying agent, all percents herein are by weight of the final product.
Claim 25
Dependent Claim
23 words
The extended release pharmaceutical formulation of claim 2, wherein the narcotics are selected from the group consisting of morphine, codeine and derivatives thereof.
Claim 26
Dependent Claim
24 words
The extended release pharmaceutical formulation of claim 2, wherein the antibiotics are selected from the group consisting of erythromycin, penicillins, cephalosporins and their derivatives.
Claim 27
Dependent Claim
22 words
The extended release pharmaceutical formulation of claim 2, wherein the bronchodilators are selected from the group consisting of theophylline, albuterol and terbutaline.
Claim 28
Dependent Claim
23 words
The extended release pharmaceutical formulation of claim 2, wherein the cardiovasculars are selected from the group consisting of diltiazem, propranolol, nifedepine and clonidine.
Claim 29
Dependent Claim
31 words
The extended release pharmaceutical formulation of claim 2, wherein the central nervous system drugs are selected from the group consisting of meclizine, ergoloid mesylates, thioridazine, diazepam, chlorpromazine, hydroxyzine, carbidopa and levodopa.
Claim 30
Dependent Claim
16 words
The extended release pharmaceutical formulation of claim 1, wherein the drug is pseudoephedrine hydrochloride and triprolidine.
Claim 31
Dependent Claim
14 words
The extended release pharmaceutical formulation of claim 1, wherein the drug is pseudoephedrine hydrochloride.
Claim 32
Dependent Claim
17 words
The extended release pharmaceutical formulation of claim 1, wherein the drug is pseudoephedrine hydrochloride and chlorpheniramine maleate.
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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) | 1995-07-28 | 1996-01-27 | 1996-07-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-07-28 | 2000-01-27 | 2000-07-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-07-28 | 2004-01-27 | 2004-07-28 | $7700.00 | Window Closed / Lapsed |