Method and composition for treating ear inflammation caused by dry ear
United States Patent: 7,879,372
Issued: February 1, 2011
Inventors: Yoshpe; Nina
(Huntington Beach, CA), Willner; Ayal (Newport Beach, CA)
Appl. No.: 12/189,501
Filed: August 11, 2008
Covidien Pharmaceuticals Outsourcing
A method of treating diseases and
conditions associated with dry ear comprising topically applying to the
ear canal of a subject that is suffering therefrom a liquid composition
comprising an anti-irritant agent, a wound healing agent; and an
anti-inflammatory agent dissolved in a polyhydroxy liquid solvent.
Description of the
1. Field of the Invention
This invention relates to the treatment of inflammation of the inner ear
of a mammal, e.g. humans or pets, caused by asteatosis, which treatment
comprises topical application of a liquid composition to the inflamed
2. Related Art
It is well known that a moist environment in the inner ear of a human or a
pet can result in various diseases such as Swimmer's Ear. Swimmer's Ear is
an example of a common affectation of the ear caused by excessive moisture
whereby a swimmer receives contaminated water in the ear or overly
moisturizes the ear causing it to succumb to microbial growth (most often
pseudomonas). Thus, there are many compositions that are disclosed for use
in removing water from and drying the ear canal.
Alcohol is commonly used to clean out the ear, especially of pets, because
it dissolves the natural oils and fats present in the ear, but alcohol is
also irritating, especially if the ear is presented with lesions or is
inflamed. Alcohol evaporates quickly, thereby often over-drying the ear
and leaving it red and irritated.
Hydrogen peroxide is also often used to clean pet ears, but it does not
dissolve the waxes and oils and does not kill infections as well as does
alcohol, although it is usually mild enough such as not to irritate the
Also commonly used to clean pet ears is a mixture of acetic acid and
water, or acetic acid and alcohol. While such mixtures are effective in
killing bacteria and in eliminating yeast infections, they are not pH
balanced and may irritate or actually burn the ear if the pH is too low.
Additionally, the acetic acid/alcohol mixture has a tendency to over-dry
Many people clean their ears and/or the ears of their pets with Q-tips.
This procedure can cause dry ear by stripping the protective coating of
earwax that protects the skin lining of the ear canal. As a result, the
ear canal may suffer from atopic dermatitis or even more serious a skin
infection (otitus external can develop in the ear canal
Asteatosis is a common condition of the external auditory canal where the
skin surface in the canal is dry and lacks cerumen production. This
condition is sometimes associated with aging. Because of the lack of
cerumen which is protective of the canal, there is a change in the ph of
the canal which may make it more prone to external ear infection. The
dryness of the canal skin leads to itching and subsequent scratching and
irritation of the canal. It is at this point that many patients will
insert cotton tip applicators and other foreign bodies in the canal to
alleviate the discomfort. Because there is not cerumen in the canal
pathogenic and nonpathogenic bacteria and fungi may dominate the flora of
the canal, cause overgrowth and actual infection. These infections can
often time be very difficult to clear up requiring multiple office visits,
particularly if these is fungal overgrowth.
Thus, in many instances the ear canal may be over-dry as a result of
aging, cleaning or for other reasons.
The problem with over drying the ear canal is that serious diseases or
conditions, e.g. inflammation, may be the result.
The present invention provides a method and composition for treating ear
inflammation caused by dry ear. The compositions of this invention
utilizes as active ingredients, compounds that are derived from natural as
opposed to synthetic ingredients.
BRIEF SUMMARY OF THE INVENTION
The present invention provides a method and composition for treating ear
inflammation caused by dry ear or asteatosis. Said composition comprises a
mixture of natural products having anti-inflammatory, anti-irritant, and
wound healing properties in a polyhydroxy solvent.
The composition of the present invention has emollient and lubrication
properties and is topically applied as ear drops to the ear of a patient
to treat asteatosis or dry ear or the conditions resulting therefrom or
The novel composition used in the method of the present invention
comprises a natural anti-irritant dissolved in polyhydroxy organic
solvent. For example, said natural anti-irritant may comprise an
avenanthramide, such as an oat (Avena Sativa) Kernel extract.
The polyhydroxy solvent may be a glycol or a glycerine compound, e.g. a
mixture of two or more glycols compounds or glycerines.
The composition of this invention may further comprise a compound having
wound healing activity. For example, Alpha bisbolol, i.e., (+)-epi-bisabolol
the wound healing principle of Peperomia galioides may be included in the
compositions of the present invention. Alpha bisbolol is also known as a
The composition of this invention may further include an emollient, such
as Aloe, which reduces irritation and treats abrasions, minor wounds, and
The compositions of this invention also may include a pain reliever such
as a White Willow Bark extract which also has anti-inflammatory
Furthermore, the present compositions may comprise a humectant, e.g. a
pyrrolidone carboxylic acid.
Finally, a compound having anti-allergy properties may be incorporated in
the compositions of the present invention, e.g. a liquorice root extract
such as dipotasium glycyrrhizate, which has anti-allergic properties, but
also is an anti-inflammatory agent and a surfactant.
DETAILED DESCRIPTION OF THE INVENTION
The present invention preferably comprises a mixture of natural products
having anti-inflammatory, anti-irritant and wound healing properties,
(hereinafter "active ingredients") in a polyhydroxy solvent wherein said
solvent is a mixture of one or more glycol compounds or dihuydric alcohol
compounds and one or more glycerin compounds, or trihydric alcohol
compounds e.g. a diglycerine.
The active ingredients may comprise from about 0.5 to about 10%, by
weight, of said ear drop composition. More preferably, said active
ingredients may comprise from about 0.75 to about 5%, by weight, e.g. from
about 1 to about 3%, by weight, of said ear drop composition.
The glycol compounds may comprise dihydroxyalkyl compounds, such as 1,3
butylenegylcol, ethylene glycol, 1,2 propylene glycol or
hydroxyalkyloxyalkyl compounds such hydroxymethyleneoxyethylene glycol,
etc. Most preferably, said glycol is 1,3 butyleneglycol, which besides
having the necessary solvent properties provides anti-fungal and
The glycerin compound or trihydric alcohol may comprise glycerin from
natural or synthetic sources, preferably from natural sources.
In addition, to functioning as a solvent in the eardrop compositions of
this invention glycerin provides emollient, humectant, and lubrication
properties to the present compositions.
The active ingredients preferably are as follows:
An anti-irritant agent derived from a natural source, e.g. an
wherein m is an integer, e.g. of from 1 to 4, i.e. 1, 2 or 3.
A preferred avenantiramide source is a product sold as Drago-Calm
available from Syrmise of Teterboro, N.J., 00768.
Drago-Calm is reported to be an Oat (Avena Satvia) Kernel Extract having a
guaranteed active constituent concentration of 100 ppm avenanthramides
This product has superior anti-irritant and anti-oxidant properties. The
Avenanthramides include in this product are analogues of Tranilast.TM.,
which is a potent anti-histamine
The anti-irritant agent may comprise from about 0.1 to about 5%, by
weight, preferably from 0.5 to about 1.5%, by weight, of the eardrop
composition of this invention.
The composition of this invention may further comprise one or more
compounds having natural wound healing activity. Preferably, said wound
healing compounds may comprise Aloe and/or alpha-bisbolol.
Aloe is a gel obtained by crushing the mucilaginous cells found in the
inner tissue of the plant leaf. Aloe is a wound healing agent and has
emollient properties. The emollient effect of this gel is largely
attributed to a constituent polysaccharide (glucomannan) similar to guar
gum. The term "aloe" refers to a solid residue obtained by evaporating the
latex derived from the outer layers of the plant leaf Aloe latex also
contains the anthraquinone barbaloin (a glucoside of aloe-emodin).
Topical application of aloe in the compositions of this invention
alleviates irritation, inhibit infection and promote healing of abrasions,
minor wounds, and burns.
The beneficial effects of aloe gel in relieving skin irritation in dry ear
may be due, in part, to its moisturizing activity which reduces drying of
abraded or injured skin. Some clinical studies have demonstrated
acceleration of wound healing from aloe.
Aloe also has anti-inflammatory properties.
Alpha bisabolol or (+) epi-Alpha-bisobolol is a terpenoid which is the
wound healing principal of Peperomia galioides and also has
anti-inflammatory properties. Natural Alpha bisabolol is available from
BASF. The wound healing components of the present eardrop compositions,
i.e. aloe and/or alpha bisabolol, may comprise from about 0.01 to about
1%, by weight, preferably from about 0.05 to about 0.15%, by weight.
The compositions of the present invention preferably may comprise further
anti-inflammatory agents, which agents may, in addition, have anti-allergy
and analgesic properties such as salts of glycyrrhic acid, e.g.
dipotassium glycyrrhizate and White Willow Bark extract, respectively.
The dipotassium glycyrrhizate may be extracted from liquorice root.
The bark of the white willow tree is a source of salicin and other
salicylic-compounds which are similar in structure to aspirin (acetyl
salicylic acid) Native Americans are thought to have used ground willow
bark a as a medicinal remedy for everything from pain relief to fevers.
Today, white willow bark is often used as a natural alternative
aspirin--one of the most common uses in dietary supplements is as a
adjunct for weight loss.
Thus, the extract of white willow tree bark is utilized in the present
compositions as a pain reliever (headaches, arthritis, minor injuries) and
an anti-inflammatory agent.
The primary active compound in white willow bark is salicin. In the body
salicin can be converted into salicylic acid, which has powerful effects
as an anti-inflammatory and pain reliever.
The anti-inflammatory agents may comprise from about 0.001 to about 1%, by
weight of the compositions of this invention, e.g. from about 0.002 to
about 0.05%, by weight, of such compositions.
The compositions of the present invention may further comprise additional
humectants in addition to glycerin discussed above.
Preferably, the ear drop composition will comprise a natural humectant
such as pyrrolidone carboxylic acid, such as Ajidew N-50 which is the
sodium salt of said acid and is available from Ajinomoto USA, Inc. of
Paramus, N.J. 07652.
Finally, the compositions of the present invention may include one or more
surfactants to stabilize the compositions.
Preferably, at least one of the surfactants is a cationic surfactant, e.g.
a quatenary amine, such as Stepanquat 50 NF which is a dialkyl
dimethylammonium chloride and is available from Stepan Company.
More preferably, the cationic surfactant stabilized compositions
additionally include a nonionic surfactant such as Tween 20.
The surfactants may comprise from about 0.02 to about 1% by weight of said
compositions, more preferably from about 0.2 to about 0.45% by weight.
The composition below discloses a preferred embodiment of this invention
and the sources of the individual components
-- see Original Patent.
The preferred composition is prepared as disclosed below
-- see Original Patent.
1. DD is a 56 Caucasian female who has had recurrent external ear
infections. She has been treated with various antibacterial and antifungal
preparations. After finally getting the infections cleared, she has had no
cerumen production in the external canal. With the use of the emollient
and lubricating drops, she has successfully remained infection free for
greater than six months while continuing her water activity.
2. AH is a 12 year old asian American female with sensorineural hearing
loss with a history of very dry ear canals and external ear infections.
Despite multiple medications it was difficult to clear her ear canals for
long periods of time so that she could wear her hearing aid. Once the
infections had cleared with the use of the emollient and lubricating
drops, she has been able to successfully wear her hearing aids and follow
up visits only every three months.
Claim 1 of 6 Claims
1. A method of treating inflammation
caused by dry ear or asteatosis in a human which comprises topically
applying to the ear canal of a human that is suffering therefrom a liquid
composition comprising: (a) an anti-irritant agent wherein said
anti-irritant agent is avenanthramide; (b) a wound healing agent wherein
said wound healing agent is aloe; (c) an anti-inflammatory agent wherein
said anti-inflammatory agent is dipotassium glycyrrhizate; (d) dissolved
in a polyhydroxy liquid solvent wherein said composition is stabilized
with a cationic surfactant and a nonionic surfactant.
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