U.S. patent application number 11/657860 was filed with the patent office on 2007-10-25 for compositions and kits useful for treatment of respiratory illness.
This patent application is currently assigned to The Proctor & Gamble Company. Invention is credited to Daren K. Anness, Elaine Rose Costeines, Susan Elaine Criss, Douglas William Gledhill, Thomas Edward Huetter, Radhika R. Iyer, Jayant Eknath Khanolkar, Kelly Lee Martin, Niranjan Ramji.
Application Number | 20070249727 11/657860 |
Document ID | / |
Family ID | 48805455 |
Filed Date | 2007-10-25 |
United States Patent
Application |
20070249727 |
Kind Code |
A1 |
Martin; Kelly Lee ; et
al. |
October 25, 2007 |
Compositions and kits useful for treatment of respiratory
illness
Abstract
The invention relates to a clear device: comprising a
composition contained in a device; wherein said composition
comprising a pharmaceutical active selected from the group
consisting of phenylephrine, its free and addition salt forms, and
mixtures thereof. Also disclosed are kits comprising: a composition
contained in a device; wherein said composition comprising a
pharmaceutical active selected from the group consisting of
phenylephrine, its free and addition salt forms, and mixtures
thereof.
Inventors: |
Martin; Kelly Lee;
(Cincinnati, OH) ; Khanolkar; Jayant Eknath;
(Surbiton, GB) ; Gledhill; Douglas William; (St.
Charles, MO) ; Criss; Susan Elaine; (Maineville,
OH) ; Ramji; Niranjan; (Mason, OH) ;
Costeines; Elaine Rose; (Maineville, OH) ; Huetter;
Thomas Edward; (West Chester, OH) ; Iyer; Radhika
R.; (Mason, OH) ; Anness; Daren K.; (Loveland,
OH) |
Correspondence
Address: |
THE PROCTER & GAMBLE COMPANY;INTELLECTUAL PROPERTY DIVISION - WEST BLDG.
WINTON HILL BUSINESS CENTER - BOX 412, 6250 CENTER HILL AVENUE
CINCINNATI
OH
45224
US
|
Assignee: |
The Proctor & Gamble
Company
Cincinnati
OH
|
Family ID: |
48805455 |
Appl. No.: |
11/657860 |
Filed: |
January 25, 2007 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11408299 |
Apr 21, 2006 |
|
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11657860 |
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Current U.S.
Class: |
514/653 |
Current CPC
Class: |
A61P 37/08 20180101;
A61K 31/55 20130101; A61K 31/495 20130101; A61K 45/06 20130101;
A61J 1/05 20130101; A61P 37/00 20180101; A61K 31/137 20130101; A61K
47/22 20130101; A61P 11/02 20180101; A61K 47/26 20130101; A61P
11/00 20180101; A61K 31/519 20130101; A61K 31/485 20130101; A61K
47/10 20130101; A61K 47/12 20130101; A61K 31/473 20130101; A61P
11/04 20180101; A61K 31/167 20130101; A61K 47/20 20130101; A61K
31/522 20130101; A61P 11/14 20180101; A61K 9/0095 20130101; A61K
9/08 20130101; A61K 31/616 20130101; A61K 31/137 20130101; A61K
2300/00 20130101; A61K 31/473 20130101; A61K 2300/00 20130101; A61K
31/485 20130101; A61K 2300/00 20130101; A61K 31/495 20130101; A61K
2300/00 20130101; A61K 31/519 20130101; A61K 2300/00 20130101; A61K
31/522 20130101; A61K 2300/00 20130101; A61K 31/55 20130101; A61K
2300/00 20130101; A61K 31/616 20130101; A61K 2300/00 20130101 |
Class at
Publication: |
514/653 |
International
Class: |
A61K 31/135 20060101
A61K031/135 |
Claims
1. A clear device: comprising a composition contained in a device;
wherein said composition comprising a pharmaceutical active
selected from the group consisting of phenylephrine, its free and
addition salt forms, and mixtures thereof; and wherein said device
comprises a material selected from the group consisting of
Polyethylene Terephthalate (PET), Glycol-modified Polyethylene
Terephthalate (PETG), Oriented Polypropylene (OPP),
Polyvinylchloride (PVC), Polyvinylidene Chloride (PVDC), Nylon,
Polyethylene Terphthalate Polyester (PETP), Polyphene, and
combinations thereof.
2. The clear device of claim 1, wherein said material is
Polyethylene Terephthalate (PET).
3. The clear device of claim 1, wherein said composition has a pH
of from about 2 to about 6.5.
4. The clear device of claim 1, wherein said composition has a pH
of from about 2 to about 5.
5. The clear device of claim 1, comprising from about 0.0001% to
about 2% pharmaceutical active, by weight of the composition.
6. The clear device of claim 1, wherein said composition further
comprising a sweetener.
7. The clear device of claim 6, wherein said sweetener comprises an
artificial sweetener.
8. The clear device of claim 7, wherein said artificial sweetener
is selected from the group consisting of: sodium saccharin,
acesulfame potassium, sucralose, aspartame, monoammonium
glycyrrhizinate, neohesperidin dihydrochalcone, thaumatin, neotame,
cyclamates, and mixtures thereof.
9. The clear device of claim 8, comprising from about 0.0001% to
about 1% of said artificial sweetener, by weight of said
composition.
10. The clear device of claim 1, wherein said composition further
comprising at least one additional pharmaceutical active.
11. The clear device of claim 10, wherein said additional
pharmaceutical active is selected from the group consisting of
antitussives, antihistamines, non-sedating antihistamines,
decongestants, expectorants, analgesics, antipyretic
anti-inflammatory agents, local anesthetics, anti-inflammatory
agents, demulcents, herbal remedies, vitamins, supplements,
antioxidants, natural ingredients, minerals, energy boosting
ingredients, sleep aids and immune system boosting ingredients, and
mixtures thereof.
12. The clear device of claim 1, wherein said composition further
comprising a chelating agent.
13. The clear device of claim 12, wherein said chelating agent is
selected from the group consisting of: ethylene diamine tetraacetic
acid (EDTA), tetrasodium EDTA, sodium hexametaphosphate (SHMP),
citric acid, phosphoric acid, di(hydroxyethyl)glycine,
8-hydroxyquinoline, salts thereof and mixtures thereof.
14. The clear device of claim 12, comprising from about 0.0001% to
about 2% of said chelating agent, by weight of said
composition.
15. The clear device of claim 1, wherein said composition further
comprising an additional ingredient selected from the group
consisting of a solvent, a reducing agent. a non-aldehydic
aesthetic agent, a chloride salt, a coolant, a colorant, a
preservative, a fragrance, and combinations thereof.
16. The clear device of claim 1, wherein said device delivers from
about 5 ml to about 50 ml of said composition per dose.
17. The clear device of claim 16, wherein said composition is
administered at least once daily.
18. A kit comprising: a composition contained in a device; wherein
said composition comprising a pharmaceutical active selected from
the group consisting of phenylephrine, its free and addition salt
forms, and mixtures thereof; and wherein said device comprises a
material selected from the group consisting of Polyethylene
Terephthalate (PET), Glycol-modified Polyethylene Terephthalate
(PETG), Oriented Polypropylene (OPP), Polyvinylchloride (PVC),
Polyvinylidene Chloride (PVDC), Nylon, Polyethylene Terphthalate
Polyester (PETP), Polyphene, and combinations thereof.
19. The kit of claim 18, further comprising a set of
instructions.
20. The kit of claim 18, wherein said composition further
comprising at least one additional pharmaceutical active.
21. The kit of claim 18, wherein said kit further comprising at
least one additional pharmaceutical active.
Description
FIELD OF THE INVENTION
[0001] The invention relates to a clear device: comprising a
composition contained in a device; wherein said composition
comprising a pharmaceutical active selected from the group
consisting of phenylephrine, its free and addition salt forms, and
mixtures thereof.
BACKGROUND OF THE INVENTION
[0002] The ability to produce a stable composition can be affected
by the type of container or device in which the composition is
located. The container can be made of materials that have certain
affinities for ingredients contained within the composition for
example pharmaceutical actives such phenylephrine, acetaminophen
and/or dextromethorphan. The interaction, between the material that
the container or device is made of and ingredients comprised within
the composition, can result in precipitation of the ingredients and
prevent appropriate dissolution of the ingredients within the
composition.
[0003] Because these actives have different properties and
stabilities, it is a challenge to formulate overall compositions
containing actives wherein the actives are all stable and effective
in a device for delivering the compositions and at the same time
controlling the levels of ingredients in the composition so as to
prevent adverse side effects such as diarrhea.
[0004] Therefore, the present invention provides suitable ranges of
solvent concentrations and ratios that prevent the precipitation of
actives, reduce aldehyde levels, and form stable compositions that
deliver actives to a consumer in need all within a preferred
device.
SUMMARY OF THE INVENTION
[0005] The present invention is directed to a clear device:
comprising a composition contained in a device; wherein said
composition comprising a pharmaceutical active selected from the
group consisting of phenylephrine, its free and addition salt
forms, and mixtures thereof; and wherein said device comprises a
material selected from the group consisting of Polyethylene
Terephthalate (PET), Glycol-modified Polyethylene Terephthalate
(PETG), Oriented Polypropylene (OPP), Polyvinylchloride (PVC),
Polyvinylidene Chloride (PVDC), Nylon, Polyethylene Terphthalate
Polyester (PETP), Polyphene, and combinations thereof.
[0006] The present invention further relates to a kit comprising: a
composition contained in a device; wherein said composition
comprising a pharmaceutical active selected from the group
consisting of phenylephrine, its free and addition salt forms, and
mixtures thereof; and wherein said device comprises a material
selected from the group consisting of Polyethylene Terephthalate
(PET), Glycol-modified Polyethylene Terephthalate (PETG), Oriented
Polypropylene (OPP), Polyvinylchloride (PVC), Polyvinylidene
Chloride (PVDC), Nylon, Polyethylene Terphthalate Polyester (PETP),
Polyphene, and combinations thereof.
[0007] The invention is further directed to methods of treating
respiratory illness and symptoms thereof comprising orally
administering a composition as described herein.
DETAILED DESCRIPTION OF THE INVENTION
[0008] The present invention comprises a clear device: comprising a
composition contained in a device; wherein said composition
comprising a pharmaceutical active selected from the group
consisting of phenylephrine, its free and addition salt forms, and
mixtures thereof; and wherein said device comprises a material
selected from the group consisting of Polyethylene Terephthalate
(PET), Glycol-modified Polyethylene Terephthalate (PETG), Oriented
Polypropylene (OPP), Polyvinylchloride (PVC), Polyvinylidene
Chloride (PVDC), Nylon, Polyethylene Terphthalate Polyester (PETP),
Polyphene, and combinations thereof.
[0009] These and other limitations of the compositions and methods
of the present invention, as well as many of the optional
ingredients suitable for use herein, are described in detail
hereinafter.
[0010] All weights, measurements and concentrations herein are
measured at 25.degree. C. on the composition in its entirety,
unless otherwise specified.
[0011] All percentages, parts and ratios as used herein are by
weight of the total composition, unless otherwise specified. All
such weights as they pertain to listed ingredients are based on the
active level and, therefore do not include solvents or by-products
that may be included in commercially available materials, unless
otherwise specified.
[0012] The composition and methods of the present invention can
comprise, consist of, or consist essentially of, the essential
elements and limitations of the invention described herein, as well
as any additional or optional ingredients, components, or
limitations described herein or otherwise useful in compositions
intended for companion animal consumption.
Device
[0013] The device of present invention preferably contains a
composition. Nonlimiting examples of the device of the present
invention include a bottle, a canister, a container, and
combinations. Preferably, the device is clear. Clear devices can
include both colorless and colored which permits the user to see
the composition through the device. The device comprises a
material. Nonlimiting examples of a material that can be used in
the present invention include Polyethylene Terephthalate (PET),
Glycol-modified Polyethylene Terephthalate (PETG), Oriented
Polypropylene (OPP), Polyvinylchloride (PVC), Polyvinylidene
Chloride (PVDC), Nylon, Polyethylene Terphthalate Polyester (PETP),
Polyphene, and combinations thereof. Preferably the material of the
present invention is PET.
Composition
[0014] The device of the present invention preferably contains a
composition. The compositions of the present invention are made
stable when placed in devices made of the material described
herein. The compositions of the present invention comprise
phenylephrine; phenylephrine free forms and addition salt forms,
and mixtures thereof. Nonlimiting salts of phenylephrine include
phenylephrine hydrochloride and phenylephrine hydrobromide.
[0015] The compositions of the present invention may comprise an
amount of phenylephrine in the range of about 0.0001 mg to about 60
mg of phenylephrine, from about 0.01 to about 30 mg, from about
0.01 to about 20 mg and from about 5 mg to about 10 mg of
phenylephrine, all per dose of the composition. By way of
non-limiting example, an embodiment of the present invention may
comprise about 10 mg of phenylephrine, per dose. Another embodiment
of the present invention may comprise about 5 mg of phenylephrine,
per dose.
[0016] The compositions of the present invention may comprise an
amount of phenylephrine in the range of from about 0.0001% to about
2%, from about 0.0001% to about 1%, from about 0.001% to about
0.5%, and alternatively from about 0.01% to about 0.25%, all by
weight of the composition.
[0017] The compositions of the present invention may achieve
enhanced stability when the composition has a pH of from about 2 to
about 6.5, from about 2 to about 5, from about 3.5 to about 5, and
from about 4 to about 5. As non-limiting examples, the present
compositions may comprise one or more acidulants in order to reach,
and maintain, the pH. Acidity can be adjusted to and maintained
within the requisite range by known and conventional methods.
Acidulant as used herein means a substance added to a composition
to lower the pH of the composition.
[0018] Organic as well as inorganic edible acids may be used to
adjust the pH of the compositions herein. The acids can be present
in their undissociated form or, alternatively, as their respective
salts, for example, potassium or sodium hydrogen phosphate,
potassium or sodium dihydrogen phosphate salts. Illustrative acids
are edible organic acids which include citric acid, malic acid,
fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric
acid, ascorbic acid, acetic acid, or mixtures thereof.
[0019] The compositions of the present invention are preferably
substantially free of aldehydes. As used herein, substantially free
of aldehydes means that the composition comprises less than about
0.1%, alternatively less than about 0.05%, alternatively less than
about 0.01% of total aldehydes, (i.e. compounds containing at least
one aldehydic moiety), all by weight of the composition. As the
inventors have discovered, formulating the compositions of the
present invention to be substantially free of aldehydes upon
manufacture compensates for the potential for formation of some
amount of aldehyde in the composition during storage
conditions.
[0020] Aldehydes are compounds that are well known to the
ordinarily skilled artisan. Flavors are well known for use in
health products for improving consumer acceptance, and many such
flavors are aldehydic in structure. For example, characterizing
compounds for cherry flavors include benzaldehyde and p-tolyl
aldehyde. However, the inventors have found that these same flavors
also often cause degradation of the phenylephrine used herein.
[0021] The present inventors have found that substantial removal of
the aldehydes, as defined herein, greatly stabilizes the resulting
composition.
Additional Pharmaceutical Actives
[0022] The compositions of the present invention can also comprise
at least one additional pharmaceutical active. Pharmaceutical
actives are readily known to the ordinarily skilled artisan and, as
such, the actives are not bound by the descriptions provided
herein. Nonlimiting examples of additional pharmaceutical actives
may include, but are not limited to, antitussives, antihistamines,
non-sedating antihistamines, decongestants, expectorants,
analgesics, antipyretic anti-inflammatory agents, local
anesthetics, anti-inflammatory agents, demulcents, herbal remedies,
vitamins, supplements, antioxidants, natural ingredients, minerals,
energy boosting ingredients, sleep aids and immune system boosting
ingredients, and mixtures thereof.
[0023] Nonlimiting examples of additional pharmaceutical actives
include but are not limited to dextromethorphan, acetaminophen,
ephedrine, pseudoephedrine, phenylpropanolamine, ibuprofen,
aspirin, ketoprofen, guaifenesin, ambroxyl, bromhexine,
diphenhydramine, chlorpheniramine, doxylamine, triprolidine,
clemastine, pyrilamine, promethazine, cetirizine, loratidine,
oxycodone, hydrocodone, naproxen, brompheniramine, carbinoxamine,
caffeine, benzonatate, pheniramine, fentanyl, azatedine,
desloratadine, carbamazepine, buprenorphine, hydromorphone,
indomethacin, oxymorphone, phenol, codeine, mesalamine,
dichlophenac, sulindac, beclomethaxone, meloxicam, fenoproten,
mometasone, menthol, benzocaine, dipyridamole, methscopolamine, the
free and the addition salt forms, chamomile, passion flower,
Vitamin C, Vitamin D, B Vitamins, echinacea, melatonin, green tea,
curcumin, zinc, selenium, calcium, guarana, probiotics and mixtures
thereof.
[0024] Preferably the additional pharmaceutical actives include but
are not limited to dextromethorphan, acetaminophen, doxylamine, and
guaifenesin.
[0025] The compositions of the present invention may comprise an
amount of at least one additional pharmaceutical active in the
range of about zero (0) mg to about 1,000 mg of each of at least
one additional pharmaceutical active, alternatively from about 2.5
mg to about 750 mg, and alternatively from about 5 mg to about 650
mg of each of at least one additional pharmaceutical active, all
per dose of the composition.
[0026] The compositions of the present invention may comprise an
amount of additional pharmaceutical active in the range of about 0%
to about 15%, alternatively 0.0001% to about 10%, alternatively
from about 0.001% to about 7%, and alternatively from about 0.01%
to about 5%, all by weight of the composition.
Sweeteners
[0027] The composition of the present invention may comprise a
sweetener to provide sweetness and aid in the taste masking of a
pharmaceutical active(s) as well as to provide some body and
thickness. When a sweetener is present in the present inventive
composition, the compositions may comprise from about 0.0001% to
about 30% sweetener, from about 0.0001% to about 20% sweetener,
alternatively from about from about 0.0001% to about 10% sweetener,
alternatively from about from about 0.0001% to about 2% sweetener
and alternatively from about 0.05% to about 1.0% sweetener, all by
weight of the composition. The sweeteners of the present invention
can be artificial sweeteners and/or natural sweeteners.
[0028] Non-limiting examples of artificial sweeteners are selected
from the group consisting of sodium saccharine, acesulfame
potassium, sucralose, aspartame, monoammonium glycyrrhizinate,
neohesperidin dihydrochalcone, thaumatin, neotame, cyclamates, and
mixtures thereof. Generally, such artificial sweeteners are solids
when used in sweetening compositions such as those of the present
invention.
[0029] When an artificial sweetener is present in the present
inventive composition, the compositions may comprise from about
0.0001% to about 5% artificial sweetener, from about 0.0001% to
about 3.5% artificial sweetener, alternatively from about from
about 0.0001% to about 2.0% artificial sweetener, alternatively
from about from about 0.0001% to about 1.0% artificial sweetener
and alternatively from about 0.05% to about 1.0% artificial
sweetener, all by weight of the composition.
[0030] Nonlimiting examples of natural sweeteners include sucrose,
fructose, glucose, glycerin, sorbitol, maltitol, and mannitol and
combinations thereof. Sucrose, or table sugar, often in liquid
form, may be used. However, sucrose can hydrolyze to its
constituent sugars, namely glucose and fructose. Glucose is an
aldehyde, and therefore may be less desirable for use herein.
However, the present inventors discover herein that the effect of a
sweetener on phenylephrine is less than that of traditional
aldehyde-containing flavors and aromas. Nonetheless, improved
stability can be achieved when low levels of sweeteners are used,
in addition to inclusion of a non-aldehydic aesthetic agent if an
aesthetic agent is used, such that the composition remains
substantially free of aldehydes as described herein. Relatively
highly pure grades of sweeteners, having undergone less hydrolysis
to monosaccharides, may assist in lowering levels of aldehydes as
well. High fructose corn syrup can also be used, though is less
desirable because it contains aldehydes.
[0031] The compositions of the present invention can contain
natural sweeteners, such as sucrose. If the natural sweeteners are
present in a liquid solution, then the natural sweeteners are
present in the range of from about 5% to about 30% by weight of the
natural sweeteners solution, and alternatively from about 10% to
about 25% by weight of the natural sweeteners solution, wherein the
natural sweeteners solution can comprise from about 15% to about
20% by weight of the natural sweeteners solution. If the natural
sweeteners are present but not in a liquid solution, then the
natural sweeteners are present in the range of from about 4% to
about 20% by weight composition, and alternatively from about 8% to
about 17% by weight of the composition, wherein the natural
sweeteners solution can comprise from about 10% to about 13% by
weight of the composition.
Additional Ingredients
[0032] Any or all components typically associated with respiratory
illness and symptom treatment products can be used as required or
as additional ingredients herein. Nonlimiting examples of
additional ingredients include solvents, reducing agents, chloride
salt, non-aldehydic aesthetic agent, coolant, colorant,
preservative, fragrance, and combinations thereof.
Solvents
[0033] The composition of the present invention can comprise a
solvent. In one embodiment, the solvent is water-soluble or water
miscible. As used herein, solvent means a substance used to
dissolve phenylephrine and/or other pharmaceutical active(s).
Non-limiting examples of solvents may be selected from water,
propylene glycol, ethanol, glycerol, sorbitol, and mixtures
thereof.
[0034] In one embodiment, the solvent is selected from water,
propylene glycol, ethanol, polyethylene glycol (PEG) and mixtures
thereof. There are also mixtures of the solvents that may be useful
for certain product forms of the present invention. For example,
wherein the product form is an elixir, liquid-filled capsule or
liquid-filled lozenge, the solvent may optionally be a mixture of
propylene glycol, ethanol, and water. Additionally, for example,
when the product form is a liquid filled capsule, or liquid filled
lozenge the solvent may optionally be PEG and water.
[0035] The level of each solvent that makes up the mixture is
dependent on the solubility of the active(s) and the aesthetic
benefits sought by the formulator. For example, for the
compositions of the present invention, the composition may
optionally comprise from about 40% to about 95% total solvents, or
from about 50% to about 90%, or from about 60% to about 85% total
solvents, all by weight of the composition.
Chelating Agent
[0036] The present compositions may optionally comprise a chelating
agent. It has been found that trace amounts of heavy metal ions may
catalyze auto-oxidation reactions that may compromise stability of
the final composition.
[0037] The compositions may therefore optionally include a
chelating agent. Chelating agents are well known to the ordinarily
skilled artisan. Non-limiting examples of chelating agents include
but are not limited to the salts of disodium and calcium salts of
ethylene diamine tetraacetic acid (EDTA), tetrasodium EDTA, sodium
hexametaphosphate (SHMP), citric acid, phosporic acid,
di(hydroxyethyl)glycine, 8-hydroxyquinoline, and mixtures thereof.
Trivalent metal chelating agents such as galactomannans complexed
with iron may also be useful.
[0038] Wherein the compositions herein comprise a chelaing agent,
the compositions may optionally comprise from about 0.0001% to
about 1% of the chelating agent, alternatively from about 0.001% to
about 0.5%, and alternatively from about 0.01% to about 0.3% of the
chelating agent, all by weight of the composition.
Reducing Agents
[0039] The present compositions may also optionally comprise a
reducing agent. The inclusion of a reducing agent may have a
beneficial chemical stabilizing effect on the pharmaceutical
actives used in the present invention. Therefore, the reducing
agents useful in the composition depend on the active selected and
its solubility.
[0040] As used herein, the reducing agent is a substance that has a
lower redox potential than the pharmaceutical active or other
adjuvant that it is intended to protect from oxidation. Thus,
reducing agents are more readily oxidized than the pharmaceutical
active or other adjuvant and are effective in the presence of
oxidizing agents.
[0041] Reducing agents have an "electrode potential value". The
electrode potential value is defined by the Nernst equation and
measured using standard electrochemical reference cells. The
resulting values are therefore called the "Standard Electrode
Potential", or E.sup.0, as measured in volts (V). Comparing
Standard Electrode Potentials for different substances can be used
to assess the effectiveness of different reducing agents.
[0042] The reducing agents useful in the present invention may
optionally have E.sup.0 values greater than about -0.119V, and
alternatively from about -0.119V to +0.250V. Illustrative reducing
agents are selected from the salts of metabisulfite and bisulfite,
including their sodium and potassium salts, dithiothreitol,
thiourea, sodium thiosulphate, thioglycolic acid, tert-butyl
hydroquinone (TBHQ), acetyl cysteine, hydroquinone, salts thereof,
and mixtures thereof.
[0043] Wherein a reducing agent is utilized, the present
compositions may comprise from about 0.001% to 1%, alternatively
from about 0.01% to about 0.5%, and alternatively from about 0.05%
to about 0.1% of a reducing agent, all by weight of the
composition.
Salts
[0044] The present compositions may optionally comprise a salt,
such as a chloride salt, which has been further discovered to
provide potential stability benefits. Non-limiting examples include
sodium chloride, potassium chloride, ammonium chloride, and
mixtures thereof.
[0045] Wherein the composition comprises a salt, the composition
may optionally comprise from about 0.0001% to about 2%,
alternatively from about 0.25% to about 1% of the salt, all by
weight of the composition. Such salts may slow the dissociation of
a pharmaceutical active from the hydrochloride salt of a
pharmaceutical active. For example, having a chloride salt present
slows the dissociation of phenylephrine from phenylephrine
hydrochloride.
Non-Aldehydic Aesthetic Agent
[0046] The present compositions may also optionally comprise a
non-aldehydic aesthetic agent. Given the desire to provide
compositions that are aesthetically acceptable, the present
invention further provides optional alternatives to typical flavors
and aromas containing significant levels of aldehyde. Such
alternatives are herein referenced as non-aldehydic aesthetic
agents.
[0047] The inventors have discovered that typical flavors and
aromas may be substituted with non-aldehydic aesthetic agents such
as flavor components which are selected from the group consisting
of esters, ketones and alcohols, and also sweeteners, and mixtures
thereof, in order to formulate flavors that smell and taste like
cherry or other desired flavors.
[0048] As further examples, the present compositions may comprise a
non-aldehydic aesthetic agent such as an ester selected from the
group consisting of ethyl butyrate, benzyl acetate, benzyl
butyrate, allyl isovalerate, allyl caproate, ethyl-2-methyl
butyrate, ethyl methyl phenyl glycidate, and mixtures thereof. The
compositions of the present invention may optionally contain from
about 0.0001% to about 5%, alternatively from about 0.01% to about
2%, and alternatively from about 0.025% to about 1.5% of
non-aldehydic aesthetic agents, all by weight of the composition.
Utilizing these fruity esters can readily generate flavors similar
to cherry and berry flavors. The body of the flavor may also be
important to make it take on character and endure. The use of
ketones such as ionones are useful for this purpose. To illustrate,
oxanone (4-(p-hydroxyphenyl)-2-butanone, raspberry ketone) along
with trace amounts of ionones can provide this body.
[0049] As a further example, compounds such as cis-3-hexenol and
trans-2-hexenyl acetate may add to the flavor. Furaneol and maltol
may add a candy-like nuance. In addition, the compositions of the
present invention may optionally comprise low-aldehyde juice
concentrates as flavoring agents.
[0050] Methods of the Present Invention
[0051] In a further embodiment, the present invention is directed
to methods of treating a respiratory illness comprising orally
administering a composition as described herein to a mammal in need
of such treatment. As used herein, the term "respiratory illness"
encompasses a broad range of respiratory ailments, including viral
infections such as influenza and common cold, as well as allergy,
sinusitis, rhinitis, and the like. As further used herein,
"treatment" with respect to respiratory illness means that
administration of the referenced composition prevents, alleviates,
ameliorates, inhibits, or mitigates one or more symptoms of the
respiratory illness or the respiratory illness itself, or any like
benefit with respect to the respiratory illness in a mammalian
subject in need thereof, preferably in humans.
[0052] The present invention can also be directed to methods of
prevention including preventing a respiratory illness or its
associated symptoms from occurring in a mammal, for example when
the mammal is predisposed to acquiring the respiratory illness, but
has not yet been diagnosed with the illness; inhibiting the
respiratory illness or its associated symptoms; and/or alleviating,
reversing, or curing the respiratory illness or its associated
symptoms. Insofar as the methods of the present invention are
directed to preventing a respiratory illness, it is understood that
the term "prevent" does not require that the respiratory illness be
completely thwarted. Rather, as used herein, the term "preventing"
or the like refers to the ability of the skilled artisan to
identify susceptibility to respiratory illness (such as, for
example, in humans during winter months), such that administration
of the referenced compositions may occur prior to the onset of the
symptoms associated with the illness.
[0053] The present invention can also be directed to methods of
recovery including compositions that boost the energy of the mammal
and boost the immune system.
[0054] Respiratory illness may present as any of a variety of
symptoms, such as runny nose, nasal or chest congestion, cough,
sneezing, pressure, headache, aches, fever, or sore throat. The
mammal treated may be a human.
[0055] As used herein, the term "orally administering" with respect
to the mammal means that the mammal ingests or is directed to
ingest, or does ingest, one or more of the present compositions.
Wherein the human is directed to ingest the composition, such
direction may be that which instructs and/or informs the human that
use of the composition may and/or will provide the relief from the
respiratory illness (e.g. symptomatic relief, whether temporary or
permanent) for example, relief from congestion. For example, such
direction may be oral direction (e.g., through oral instruction
from, or example, a physician, pharmacists, or other heath
professional), radio or television media (i.e., advertisement), or
written direction (e.g., through written direction from, for
example a physician, pharmacist, or other health professional
(e.g., scripts), sales professional or organization (e.g., through,
for example, marketing brochures, pamphlets, or other instructive
paraphernalia), written media (e.g., internet, electronic mail, or
other computer-related media), and/or packaging associated with the
composition (e.g., a label present on a container holding the
composition). As used herein, "written" means through words,
pictures, symbols, and/or other visible or tactile descriptors,
such as Braille. Such information need not utilize the actual words
used herein, for example, "respiratory", "illness", or "mammal",
but rather use of words, pictures, symbols and the like conveying
the same or similar meaning are contemplated within the scope of
this invention.
[0056] Administration may be on an as-needed or as-desired basis,
for example, once-monthly, once-weekly, or daily, including
multiple times daily, for example, at least once daily, twice
daily, three times daily, or four times daily or more.
[0057] The amount of composition administered may be dependent on a
variety of factors, including the general quality of health of the
mammal, type of mammal, age, gender, or severity of symptoms.
[0058] In one embodiment herein, the device delivers composition
that is administered to the mammal in total dosage volumes, per
dose, of from about 5 mL to about 50 mL of the composition,
alternatively of from about 10 mL to about 30 mL of the
composition.
Kit
[0059] The present invention can also comprise a kit. The kit of
the present invention can comprise: a composition contained in a
device; wherein said composition comprising a pharmaceutical active
selected from the group consisting of phenylephrine, its free and
addition salt forms, and mixtures thereof; and wherein said device
comprises a material selected from the group consisting of
Polyethylene Terephthalate (PET), Glycol-modified Polyethylene
Terephthalate (PETG), Oriented Polypropylene (OPP),
Polyvinylchloride (PVC), Polyvinylidene Chloride (PVDC), Nylon,
Polyethylene Terphthalate Polyester (PETP), Polyphene, and
combinations thereof.
[0060] The kit may further comprise at least one additional
pharmaceutical active. The kit may also comprise an additional
composition of the present invention in a full size, a sample size
or both. The kit may further comprise an additional composition
that coordinates with the composition that is comprised within the
device or attached to the outside of the device. For, example if
the composition contained in the device is a composition for the
relief from congestion, the coordinating composition may be for a
headache. As well, if the composition in the device is a
composition for runny nose, nasal or chest congestion, cough,
sneezing, pressure, headache, aches, fever, or sore throat, the
coordinating composition may be a vitamin. The kit may further
comprise a coupon, rebate, or advertisement. The kit may further
comprise a set of instructions. These instructions may also include
illustrations.
EXAMPLES
[0061] The following examples further describe and demonstrate
embodiments within the scope of the present invention. They are
given for the purpose of illustration and are not to be construed
as limitations of the present invention.
Examples
[0062] Below are illustrated various non-limiting examples of
compositions of the present invention.
TABLE-US-00001 % w/w % w/w Raw Materials Ex. 1 Ex. 2 Propylene
Glycol 40 30 Doxylamine Succinate 0.08 0.08 Dextromethorphan HBr
0.13 0.13 Acetaminophen 4.43 4.43 Alcohol 8.52 8.52 Anethole 0.01
0.01 (Flavoring Agent) Glycerin 10 10 Green Shade 0.005 0.005
Sodium Citrate 0.17 0.17 anhydrous Citric Acid 0.36 0.36
(Anhydrous) Phenylephrine HCl 0.07 0.07 Sodium Saccharin 0.07 0.07
Sucrose Sweetner 31.11 21.16 solution Disodium EDTA 0.05 Sorbitol
Liquid 70% 20 Beta Carotene Water to 100% QS QS pH 4.16 4.10 Green
Shade available from Sensient Pharmaceuticals Tech, St. Louis, MO,
USA
Examples 1 and 2 can be made by first, add propylene glycol,
alcohol and glycerin to a clean vessel. The additional
pharmaceutical active(s), including, for example, acetaminophen,
dextromethorphan, and doxylamine, then flavor is added and stirred
until dissolved. In a separate vessel, water is added to dissolve
phenylephrine, color, buffering agents, sweeteners, and EDTA. The
aqueous solution is added to the propylene glycol solution. The
resulting composition is mixed with sweetener solution and
additional water and the composition is mixed until homogeneous and
then placed in a device comprising the material PET.
TABLE-US-00002 % w/w % w/w RAW MATERIAL Ex. 3 Ex. 4 Water QS QS
Sodium Carboxymethylcellulose 0.10 0.089 Sucrose sweetener solution
17 17.825 Phenylephrine HCl 0.07 0.06 Propylene Glycol 40 35.6
Sorbitol 20 17.8 Glycerin 5 4.45 Dextromethorphan HBr 0.13 0.11
Alcohol 4.25 3.79 Coolant 0.02 .01 Flavor 0.33 0.30 Sodium Benzoate
0.1 0.089 Citric Acid 0.14 0.12 Sodium Chloride 0.50 0.44 Sodium
Saccharin 0.09 0.08 Coloring Agent 0.003 0.026 pH 4.5 4.7 Coolant
available from Takasago International Corp., Tokyo, Japan flavor
available from IFF, Dayton, NJ, USA Coloring Agent available from
Sensient Pharmaceuticals Tech, St. Louis, MO, USA
Examples 3 and 4 can be made by first, add propylene glycol, and
alcohol to a clean vessel. The additional pharmaceutical active(s),
including, for example, acetaminophen and dextromethorphan, then
flavor is added and stirred until dissolved. In a separate vessel,
water is added to dissolve phenylephrine, color, buffering agents,
and sweeteners. The aqueous solution is added to the propylene
glycol solution. The resulting composition is mixed with sucrose
sweetener solution and additional water and the composition is
mixed until homogeneous and then placed in a device comprising the
material PET.
TABLE-US-00003 Ex. 5 Ex. 6 Raw Material wt/wt wt/wt PROPYLENE
GLYCOL USP 23.0202 22.7066 SORBITOL SOLUTION 13.1544 12.9752
GLYCERIN 8 8 Sucrose Sweetener solution 0 5 DEXTROMETHORPHAN 0.0614
0.0606 HYDROBROMIDE, USP Acetaminophen, USP 1.9951 1.9679
PHENYLEPHRINE HYDROCHLORIDE 0.0319 0.0315 Di sodium EDTA 0.05 0.05
Coolants 0.03 0.03 SODIUM BENZOATE NF, FCC 0.1 0.1 CITRIC ACID USP
ANHYDROUS 0.2208 0.2245 Sodium Citrate, Dihydrate, USP 0.2035
0.2065 SODIUM CHLORIDE USP 0.5 0.5 SACCHARIN SODIUM USP 0.1 0.1
Sucralose 0.07 0.07 FD&C Yellow #6 0.067 0.067 SODIUM CMC TYPE
7HOF USP 0.33 0.33 Flavorant 0.234 0.234 Water QS QS pH 4.5 4.5
Examples 5 and 6 can be made by first, add propylene glycol, and
water to a clean vessel. The additional pharmaceutical active(s),
including, for example, acetaminophen and/or dextromethorphan, then
flavor is added and stirred until dissolved. In a separate vessel,
water is added to hydrate sodium CMC and dissolve phenylephrine,
color, buffering agents, sweeteners, preservatives, sodium chloride
and EDTA. The aqueous solution is added to the propylene glycol
solution. The resulting composition is mixed with sucrose sweetener
solution, sorbitol, glycerin and additional water and the
composition is mixed until homogeneous and then placed in a device
comprising the material PET.
[0063] All documents cited in the Detailed Description of the
Invention are, in relevant part, incorporated herein by reference;
the citation of any document is not to be construed as an admission
that it is prior art with respect to the present invention. To the
extent that any meaning or definition of a term in this written
document conflicts with any meaning or definition of the term in a
document incorporated by reference, the meaning or definition
assigned to the term in this written document shall govern.
[0064] While particular embodiments of the present invention have
been illustrated and described, it would be obvious to those
skilled in the art that various other changes and modifications can
be made without departing from the spirit and scope of the
invention. It is therefore intended to cover in the appended claims
all such changes and modifications that are within the scope of
this invention.
* * * * *