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US4687662A Expired / Lapsed US ⏱️ 0.0 years remaining

Therapeutic effervescent composition

Assignee: Warner Lambert Co LLC
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Filing: 1986-01-15
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Granted: 1987-08-18
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Expires: 2006-01-15
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Abstract

Abstract Effervescent compositions in the form of tablets or powders comprising a therapeutic agent, a granulating agent, a microparticulate effervescent component and an effervescent system which dissolve rapidly in water to yield an effervescent solution containing a completely dissolved therapeutic agent and a process for their preparation.

Inventors

  • 👤 Alexander M. Schobel

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 21:20
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0002; A61K9/0007

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 199 words
A rapid dissolving therapeutic effervescent composition which comprises: (1) a preblended mixture present in an amount from about 7 to about 57.5% by weight of (A) a granulated therapeutic agent having a particle size of about 100 to about 600 microns, wherein the granulated therapeutic agent comprises a therapeutic agent present in an amount from about 2% to about 27% by weight selected from the group consisting of acetaminophen, aspirin, ibuprofen and mixtures thereof, and a water soluble granulating agent present in an amount from about 0.03 to about 2.5% by weight, being compatible with the therapeutic agent and having a viscosity below 100 cps, 10% by weight, at 25° C. in water, and (B) a component of an effervescent system having a particle size of about 50 to about 600 microns, present in an amount from about 5% to about 30% by weight said component being selected from the group consisting of a carbonate, an acid and mixtures thereof, and (2) an effervescent system present in an amount from about 42.5% to about 90% by weight wherein the effervescent system comprises a carbonate containing material and an acid, all percentages are by weight of the total effervescent composition.
Claim 2
Dependent Claim 199 words
A rapid dissolving therapeutic effervescent composition which comprises: (1) a preblended mixture present in an amount from about 7 to about 57.5% by weight of (A) a granulated therapeutic agent having a particle size of about 100 to about 600 microns, wherein the granulated therapeutic agent comprises a therapeutic agent present in an amount from about 2% to about 27% by weight selected from the group consisting of acetaminophen, aspirin, ibuprofen and mixtures thereof, and a water soluble granulating agent present in an amount from about 0.03 to about 2.5% by weight, being compatible with the therapeutic agent and having a viscosity below 100 cps, 10% by weight, at 25° C. in water, and (B) a component of an effervescent system having a particle size of about 50 to about 600 microns, present in an amount from about 5% to about 30% by weight said component being selected from the group consisting of a carbonate, an acid and mixtures thereof, and (2) an effervescent system present in an amount from about 42.5% to about 90% by weight wherein the effervescent system comprises a carbonate containing material and an acid, all percentages are by weight of the total effervescent composition.
Claim 3
Dependent Claim 25 words
The composition of claim 1 wherein the granulating agent is selected from the group consisting of water, alcohol, polyvinylpyrrolidone. Sucrose, hydroxypropyl cellulose and mixtures thereof.
Claim 4
Dependent Claim 37 words
The composition of claim 1 wherein the analgesic is acetaminophen having a bulk density from about 0.2 to about 0.6 g/ml and the granulated therapeutic agent has a particle size of about 100 to about 400 microns.
Claim 5
Dependent Claim 27 words
The composition of claim 1 wherein the carbonate containing material is present in an amount from about 40 to about 60% by weight of the effervescent composition.
Claim 6
Dependent Claim 40 words
The composition of claim 1 wherein the carbonate containing material is selected from the group consisting of sodium carbonate, sodium bicarbonate, sodium sesquicarbonate, potassium carbonate, potassium bicarbonate, lithium carbonate, lithium bicarbonate, ammonium carbonate, ammonium bicarbonate, ammonium sesquicarbonate and mixtures thereof.
Claim 7
Dependent Claim 28 words
The composition of claim 1 wherein the acid is selected from the group consisting of citric acid, fumaric acid, adipic acid, malic acid, tartaric acid and mixtures thereof.
Claim 8
Dependent Claim 29 words
The composition of claim 1 wherein the component of an effervescent system in the preblended mixture is an acid having a particle size from about 50 to 600 microns.
Claim 9
Dependent Claim 54 words
The composition of claim 1 wherein the acid having a particle size of about 50 to about 600 microns is present in an amount from about 5 to about 30% by weight of the effervescent composition such that the total acid content of the effervescent composition is about 22 to about 46% by weight.
Claim 10
Dependent Claim 11 words
The composition of claim 1 wherein the acid is citric acid.
Claim 11
Dependent Claim 11 words
The composition of claim 1 wherein the granulating agent is polyvinylpyrrolidone.
Claim 12
Independent Claim 173 words
A method for preparing a rapidly dissolving effervescent composition of a therapeutic agent which comprises: (A) forming a granulation by dissolving a granulating agent in a solvent to form a solution containing from about 1 to about 50% by weight granulating agent, and mixing a therapeutic agent with the solution, (B) drying the granulation, (C) sizing the dried granulation by grinding and screening to obtain particles having a size of about 100 to about 600 microns. (D) admixing a component of an effervescent system having a particle size from about 50 to about 600 microns with the sized granulation of step (C) to form a mixture, (E) mixing an effervescent system with the mixture of step (D) to obtain a uniform mixture of granules and recovering the product, wherein said therapeutic agent is selected from the group consisting of acetaminophen, aspirin, ibuoprofen and mixtures thereof, and said granulating agent being compatible with the therapeutic agent, and is water soluble having a viscosity below 100 cps, 10% by weight, at 25° C. in water.
Claim 13
Independent Claim 173 words
A method for preparing a rapidly dissolving effervescent composition of a therapeutic agent which comprises: (A) forming a granulation by dissolving a granulating agent in a solvent to form a solution containing from about 1 to about 50% by weight granulating agent, and mixing a therapeutic agent with the solution, (B) drying the granulation, (C) sizing the dried granulation by grinding and screening to obtain particles having a size of about 100 to about 600 microns. (D) admixing a component of an effervescent system having a particle size from about 50 to about 600 microns with the sized granulation of step (C) to form a mixture, (E) mixing an effervescent system with the mixture of step (D) to obtain a uniform mixture of granules and recovering the product, wherein said therapeutic agent is selected from the group consisting of acetaminophen, aspirin, ibuoprofen and mixtures thereof, and said granulating agent being compatible with the therapeutic agent, and is water soluble having a viscosity below 100 cps, 10% by weight, at 25° C. in water.
Claim 14
Dependent Claim 25 words
The method for preparing a rapid dissolving, effervescent composition of claim 11 wherein the component of an effervescent system in step (D) is an acid.
Claim 15
Dependent Claim 29 words
The method for preparing a rapid dissolving, effervescent composition of claim 12 wherein the therapeutic agent is acetaminophen having a bulk density from about 0.2 to about 0.6 g/ml.
Claim 16
Dependent Claim 24 words
The method for preparing a rapid dissolving, palatable effervescent composition of claim 12 further comprising forming the mixture of step (E) into a tablet.

References Cited (Backward Citations)

US3325357A Cited
US3882228A Cited
GB1328591A Cited
US3773922A Cited
US4093710A Cited
US4309408A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-08-17 1991-02-16 1991-08-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-08-17 1995-02-16 1995-08-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-08-17 1999-02-16 1999-08-18 $7700.00 Window Closed / Lapsed

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