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US4855143A Expired / Lapsed US ⏱️ 0.0 years remaining

Method of preparing controlled long-acting pharmaceutical formulations in unit dosage form having uniform and comparable bioavailability characteristics

Assignee: Individual
•
Filing: 1988-07-12
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Granted: 1989-08-08
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Expires: 2008-07-12
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Abstract

Abstract A method of preparing a multiplicity of controlled, long-acting release pharmaceutical tablets, each containing a therapeutic agent and a cellulosic ether carrier base material is shown. The method includes the steps of adding a quantity of cellulose ether base material such as hydroxypropyl methylcellulose and an active therapeutic agent to form a mixture, thoroughly and uniformly mixing that mixture, discontinuing the mixing, permitting the uniform mixture to stand for a period of time, typically two to twenty-four hours or longer, sufficient to cause the therapeutic agent to become bonded to the carrier base material and compressing portions of the mixture to form the solid unit dose tablets. The advantage of the method is that the time release of each tablet from a given batch of formulation and the time release characteristics of tablets prepared in different batches, will be substantially more uniform and comparable.

Inventors

  • 👤 Hans Lowey

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 14:22
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2054; A61K9/14; A61K9/141; A61K9/146

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 209 words
A multiplicity of uniform batches of unit doses of a controlled, long-acting release pharmaceutical formulation, in oral tablet form, wherein each of said doses contains active therapeutic agent and a carrier base material, and wherein each of said unit doses has uniform bioavailability from batch to batch, said unit doses being prepared by a method comprising the steps of: (a) adding a quantity of solid, particulate carrier base material consisting essentially of at least one cellulosic ether selected from the group consisting of hydroxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose and ethyl cellulose, to a quantity of a therapeutically active pharmaceutical agent in granular or powder form; (b) mechanically mixing the carrier base material and the therapeutically active agent to form a uniform mixture; (c) discontinuing the mixing and permitting the mixture formed in step (a) to stand for a period of time from 2-27 hours to cause the therapeutically active pharmaceutical agent to become bonded to the carrier base material; and (d) compressing portions of the mixture formed in steps (b) and (c) into solid oral tablet doses, wherein release of said therapeutic agent from a unit dose of a given batch is substantially the same as release of said therapeutic agent from a unit dose of another batch.
Claim 2
Dependent Claim 209 words
A multiplicity of uniform batches of unit doses of a controlled, long-acting release pharmaceutical formulation, in oral tablet form, wherein each of said doses contains active therapeutic agent and a carrier base material, and wherein each of said unit doses has uniform bioavailability from batch to batch, said unit doses being prepared by a method comprising the steps of: (a) adding a quantity of solid, particulate carrier base material consisting essentially of at least one cellulosic ether selected from the group consisting of hydroxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose and ethyl cellulose, to a quantity of a therapeutically active pharmaceutical agent in granular or powder form; (b) mechanically mixing the carrier base material and the therapeutically active agent to form a uniform mixture; (c) discontinuing the mixing and permitting the mixture formed in step (a) to stand for a period of time from 2-27 hours to cause the therapeutically active pharmaceutical agent to become bonded to the carrier base material; and (d) compressing portions of the mixture formed in steps (b) and (c) into solid oral tablet doses, wherein release of said therapeutic agent from a unit dose of a given batch is substantially the same as release of said therapeutic agent from a unit dose of another batch.
Claim 3
Dependent Claim 36 words
A multiplicity of uniform batches of unit doses as recited in claim 1, wherein the mixture formed in step (b) is permitted to stand for at least 2 hours before compression into a unit dosage form.
Claim 4
Dependent Claim 140 words
A unit dosage form of a controlled, long-acting release pharmaceutical formulation wherein each of said unit dosages contains an active therapeutic agent and a carrier base material, and wherein each of said unit dosages has uniform bioavailability from batch to batch, said unit dosages being prepared by a method comprising the steps of: (a) thoroughly mixing a carrier base material comprising at least one cellulosic ether with a therapeutic agent to form a substantially uniform pharmaceutical formulation; (b) discontinuing the mixing step and permitting the mixture formed in step (a) to stand for a period of time sufficient to cause the said therapeutic agent to become bonded to the said cellulosic ether; and (c) compressing the said pharmaceutical formulation into a suitable unit dosage form wherein release, from batch to batch, is not faster, from one unit dosage to another.
Claim 5
Dependent Claim 140 words
A unit dosage form of a controlled, long-acting release pharmaceutical formulation wherein each of said unit dosages contains an active therapeutic agent and a carrier base material, and wherein each of said unit dosages has uniform bioavailability from batch to batch, said unit dosages being prepared by a method comprising the steps of: (a) thoroughly mixing a carrier base material comprising at least one cellulosic ether with a therapeutic agent to form a substantially uniform pharmaceutical formulation; (b) discontinuing the mixing step and permitting the mixture formed in step (a) to stand for a period of time sufficient to cause the said therapeutic agent to become bonded to the said cellulosic ether; and (c) compressing the said pharmaceutical formulation into a suitable unit dosage form wherein release, from batch to batch, is not faster, from one unit dosage to another.
Claim 6
Dependent Claim 24 words
A unit dosage form as recited in claim 3, wherein the carrier comprises one or more hydroxyalkyl cellulose or hydroxyalkyl alkylcellulose or derivatives thereof.
Claim 7
Dependent Claim 31 words
A unit dosage form as recited in claim 3, wherein the carrier comprises one or more of the cellulose ethers, hydroxypropyl methylcellulose, hydroxypropyl cellulose, carboxymethyl cellulose and ethylcellulose or derivatives thereof.
Claim 8
Dependent Claim 32 words
A unit dosage form as recited in claim 3 wherein the mixture formed in step (a) is permitted to stand for at least 2 hours before compression into a unit dosage form.
Claim 9
Dependent Claim 17 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is isosorbide mononitrate.
Claim 10
Dependent Claim 17 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is isosorbide dinitrate.
Claim 11
Dependent Claim 16 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is theophylline.
Claim 12
Dependent Claim 16 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is nitroglycerin.
Claim 13
Dependent Claim 16 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is ibuprofen.
Claim 14
Dependent Claim 16 words
A unit dosage form, as recited in claim 3 wherein the active therapeutic agent is acetaminophe.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-08-07 1993-02-06 1993-08-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-08-07 1997-02-06 1997-08-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-08-07 2001-02-06 2001-08-08 $7700.00 Window Closed / Lapsed

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