Note: Descriptions are shown in the official language in which they were submitted.
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HYDRATING NASAL GEL AND APPLICATOR
Technical Field
During times of sickness, or when the local environment is low in humidity,
the tissues of
1o the inside of the nose can become dried out. This nasal dryness may cause
discomfort,
soreness, congested breathing, and even bleeding and the associated
possibility of nasal
infections.
The present invention is directed to providing relief of dryness of the nasal
tissues within
the nasal cavity, and particularly to providing such relief over an extended
period of time.
The present invention is able to provide such relief without the need for drug
ingredients.
Disclosure of the Invention
2o The present invention is directed to solving the problems associated with
dry nasal tissues
by slowly releasing moisture or water directly to the internal nasal tissues
and to the
micro-environment of the nasal cavity. The present invention solves these
problems by
providing a nasal gel that is applied to the nasal tissue and remains inside
the nose for a
substantial period of time, and which can release water or moisture to the
nasal tissues
and cavity during this time. By doing so, the user is more comfortable and the
nasal
tissues are healthier, without the need to rely on drug ingredients. As used
herein, the
expression "drug ingredients" refers to ingredients classified as drugs by the
United States
Federal Drug Administration (U.S. FDA), with the ingredients being present at
the levels
at which such ingredients function as drugs as determined by the U.S. FDA.
The present invention solves these problems by providing a hydrating nasal gel
comprising: water in an amount preferably ranging from about 50 wt-% to about
99 wt-%; a controlled-release agent in an amount effective to provide water to
a nasal
tissue at a rate of preferably between about 1 wt-% to 50 wt-% per hour at
about 38°C;
and a gel-forming agent in an amount effective to provide a viscosity to the
hydrating
nasal gel of preferably between about 5,000 centipoise to 300,000 centipoise
at about
25°C.
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The present invention is also directed to a method of applying the hydrating
nasal gel
onto the nasal tissues using a device comprising a dispenser and an
applicator. The
applicator comprises a tip having sidewall openings and which preferably has a
sealed
end opposite a second end, which is in communication with a reservoir of the
dispenser.
1o Brief Description of the Drawings
FIG. 1 is a plot showing the percent weight loss over time of one embodiment
of the nasal
gel of the present invention.
FIG. 2 is a side view of one embodiment of the nasal gel applicator of the
present
invention.
FIG. 3 is another side view of the applicator embodiment shown in FIG. 2.
2o FIG. 3A is a cross-sectional view of the applicator embodiment shown in
FIG. 3, taken
along line A-A.
FIG. 3B is a top view of the applicator embodiment shown in FIG. 3.
FIG. 3C is a bottom view of the applicator embodiment shown in FIG. 3.
FIG. 4 is a perspective view of the applicator embodiment shown in FIG. 2.
FIG. S is a perspective view of an alternative embodiment of the nasal gel
applicator of
3o the present invention.
FIG. 6 is a perspective view of another embodiment of the nasal gel applicator
of the
present invention.
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Best Mode for Carrying Out the Invention
To provide moisture to the nasal tissues over a period of time, it is
necessary to overcome
the natural biological actions, such as sneezing, which function to flush out
or remove
foreign materials from the nasal cavity. It is also necessary to provide
moisture in a way
to that retains the water on the nasal tissue and does not simply drain out of
the nose.
The present invention achieves these goals by providing a gelled product in
the nasal
cavity, which resists both flushing and draining out of the nose, and
therefore remains in
the nasal cavity and in contact with the nasal tissues for a substantial
period of time.
To provide a gelled product, a gelling or gel-forming agent is used in the
present
invention. A wide variety of materials is available which can gel an aqueous
solution.
The gel-forming agent should be safe for use on the nasal tissues, be non-
irritating, and be
able to form a gel that is stable over time. Preferably, the gel-forming agent
should form
a gel that has a viscosity sufficient to remain adhered to the nasal tissues
after application,
but that is not so viscous as to be unpleasant to the user, to be difficult to
dispense and
apply, or to interfere with the release of water to the nasal tissues and
nasal cavity. More
preferably, the gel-forming agent should form a thixotropic gel that is easy
to apply in a
thin layer and regains significant viscosity after application to remain on
the nasal tissues
for a prolonged period of time.
The hydrating nasal gels of the present invention are effective a viscosity
preferably
ranging from between about 5,000 centipoise to about 300,000 centipoise at
room
temperature, or about 25°C. More preferably, the viscosity of the
hydrating nasal gel of
the present invention is between about 100,000 centipoise to about 300,000
centipoise at
about 25°C, and particularly preferred is a hydrating gel having a
viscosity of about
100,000 centipoise at about 25°C. The viscosity ranges described herein
are measured
using a Brookfield viscometer at room temperature. At the lower end of the
viscosity
ranges, the Brookfield viscometer is fitted with a number 4 spindle operating
at 10 rpm,
and at the higher end of the range, the Brookfield viscometer is fitted with a
TE
heliopathic spindle operating at 0.3 rpm.
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In addition, the hydrating nasal gel of the present invention includes a
controlled-release
agent that physically or chemically entrains, retains or entraps water, so
that moisture will
be progressively released over a substantial period of time. If water is
released too
quickly, the product will be ineffective. If the water is released too slowly,
the hydrating
nasal gel will be ineffective in providing moisture to the nasal tissues.
Water should
1o preferably be released from the entraining or water binding agent at such a
rate that it
maintains moisture in the environment of the nasal cavity and/or in the nasal
linings or
tissues for a substantial period of time.
The controlled-release agent used in the present invention should be safe for
use on the
nasal tissues, be non-irritating, and should not substantially interfere with
the gelling
action of the gel-forming agent. Preferably, the controlled-release agent
should be able to
hold large quantities of water and release it at a relatively steady rate over
a substantial
period of time. In general, the nasal gel should release at least 0.1 gram of
water per
hour, for about two to four hours after application to the nasal tissue.
Preferably, the
nasal gel of the present invention releases water at a rate of between about 1
wt-% to
about 50 wt-% per hour at body temperature, or about 3~°C, based on the
total weight of
the gel. More preferably, the nasal gel of the present invention releases
water at a rate of
between about 1 wt-% to 10 wt-% per hour at body temperature.
It was surprisingly discovered that a nasal gel having a viscosity within the
ranges
described above was not substantially flushed out of the nose by natural
biological
functions, and remained in the nose for a substantial period of time without
causing
discomfort or an unpleasant sensation to the user.
3o In a preferred embodiment, the gel-forming function and the controlled-
release function
are provided by a single ingredient or component of the hydrating nasal gel.
The single
component preferably has all the properties described above for each function.
Examples
of materials that may be used to perform both functions in a single component
include,
but axe not limited to: hydrogel-forming agents, such as
hydroxyethylcellulose; silica;
clay; a carbomer; and the like. Any material that produces a gel and then
releases water
over a period of minutes to hours would be effective in the hydrating nasal
gel of the
present invention.
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One preferred component of the nasal gel that can perform both the gel-forming
function
and the controlled-release function is glyceryl polymethacrylate. Useful
formulations of
the hydrating nasal gel of the present invention comprising glyceryl
polymethacrylate are
summarized in Table I:
1o Table I
Ingredient Weight Percent
Water 50%-99%
Glyceryl polymethacrylate1 %-50%
Other ingredients 0%- 25%
One preferred formulation of the present invention comprised about 65 wt-%
water,
25 wt-% glyceryl polyrnethacrylate, and 10 wt-% other ingredients.
Other ingredients or components in the nasal gel may include, but are not
limited to:
humectants; preservatives; buffers; coloring agents; fragrances; solubilizing
agents;
stabilizing agents; gel modifiers; herbal materials; and vitamins. Each of
these
ingredients can be present in any amount that does not substantially interfere
with the gel-
forming and controlled-release functions of the gel, preferably between about
0 wt-% to
10 wt-%. The preservative, if used, can more preferably be present in amounts
ranging
from 0.1 wt-% to 1.0 wt-%, depending on the preservative.
If any non-water soluble ingredients are used in the gel of the present
invention, it may be
useful or necessary to entrain such ingredients in microvesicles such as
liquid crystals,
micelles, liposomes, encapsulates, and the like.
If a fragrance is used, preferably it is one that provides cold symptom relief
itself, such as
camphor, menthol, or eucalyptus.
Example I
A hydrating nasal gel was prepared according to the formula shown in Table II.
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Table II
Brand Weight
Ingredient Function
Tested Percent
Water Medium; provides moisture34.955%
59.00%
Glyceryl 1 Gel-forming agent; [29.5%-36.58%
Lubrajel water
MS
water
polymethacrylate release agent 22.42% -
29.5%
glyceryl
olymethacrylate]
Fragrance oil Fragrance 2.25%
Liposorb
Polysorbate 20 Solubilizer 2
00%
L-202 .
Preservative Germaben Preservative 0.80%
II'
Propylene glycol Humectant 0.50%
Glycerin Humectant 0.50%
-LubrajelC~ MS is a product of International Specialty Products, Wayne, NJ.
zLiposorb~ L-20 is a product of Lipo Chemicals, Inc., Patterson, NJ.
3Germaben~ II is a product of Sutton Laboratories, Inc., Chatham, NJ.
Ten 0.2 gram dosage units of the gel released an average of 0.2 grams of water
per hour
for six hours.
The water release rate of the hydrating nasal gel of the present invention was
measured by
applying 100 grams of the gel as a 2mm thick layer onto a metal surface. The
metal
surface was then subjected to a temperature near body temperature, or about
100°F, or
about 38°C, and the weight loss of the gel was measured over time. FIG.
1 shows the
weight loss rate over time. The weight loss is attributable to the gel
releasing moisture
into the surrounding environment, such as a nasal cavity.
As seen in FIG. l, the weight loss rate during the first two hours was about 1
gram every
10 minutes, or about 0.1% per minute, or approximately 6% per hour. After the
first two
hours, the weight loss rate of the gel of the present invention tapered off,
but still
continued at a slower rate. This non-linear weight loss rate of the hydrating
gel of the
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present invention was unexpected, since in general, water diffusion is a
linear
phenomenon. The advantage of the non-linear weight loss rate is that although
the weight
loss rate becomes slower over time, the gel remains on the surface and
releases moisture
for a longer period of time than it would have had the weight loss rate
remained linear
over time.
Although the primary function of the hydrating nasal gel of the present
invention is to
deliver water to the nasal membranes or tissues over a substantial period of
time, the gel
could also be used to simultaneously release other beneficial materials such
as vitamins,
herbal extracts, pharmaceutical materials, homeopathic materials, and the
like. The gel of
the present invention could also be used to deliver water-insoluble agents to
the nasal
membranes on a time-release basis, in that as the water in the gel evaporates,
any water-
insoluble components may be released into the nasal tissue as well.
The hydrating nasal gel of the present invention is preferably applied in a
manner to
provide a relatively uniform layer of the gel on the inner nasal tissues, and
more
preferably in such a way as to substantially avoid being directly inserted
into the nasal
passage, where the gel cannot function to hydrate the nasal membranes. This
can be
accomplished in a number of ways, such as by using a cotton swab, a finger
tip, or other
type of applicator. Preferably, a squeeze bottle fitted with an applicator tip
of the present
invention is used to apply the gel to the nasal tissues.
FIG. 2 shows one embodiment of the applicator tip 10 of the present invention.
Applicator tip 10 includes base 11, sidewall 12, closed end 14, open end 16 of
base 11,
and sidewall orifice 18.
Applicator tip 10 generally is of a length and diameter that is appropriate
for the geometry
of the nasal cavity, and is preferably tapered to comfortably fit within the
nasal cavity.
Open end 16 is preferably flared to prevent insertion of tip 10 too deeply
into the nasal
cavity. Sidewall orifices 18 are preferably arranged so as to dispense the gel
at an
appropriate depth into the nasal cavity, with the orifices preferably
longitudinally
positioned along the length of the tip to dispense the gel comfortably and
evenly over the
length of the nasal cavity, substantially without dispensing the gel too far
into the nasal
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length of the nasal cavity, substantially without dispensing the gel too far
into the nasal
cavity, where the gel could be dispensed directly into the nasal passages, or
too little into
the nasal cavity, where the gel would not remain in the nasal cavity for a
period of time
sufficient to provide relief from dryness. Sidewall orifices 18 are preferably
radially
positioned to dispense the gel substantially evenly over the perimeter of the
nasal cavity.
1o Orifices 18 also preferably have relatively restricted openings to retard
the flow of gel to
allow for consistent dosage application amounts.
Preferably, applicator tip 10 has a length ranging from about 0.5 inch to 1.5
inches. In
one particularly preferred embodiment, applicator tip 10 has a length of
between about
0.75 inch and 0.85 inch.
Open end 16 of base 11 is preferably in communication with a reservoir, not
shown,
containing the hydrating nasal gel of the present invention. Applicator tip 10
and the
reservoir together comprise the dispenser for dispensing the hydrating nasal
gel. Sidewall
12 includes at least one orifice 18, and preferably includes a plurality of
such orifices to
facilitate dispensing the gel from the sidewall orifices onto the nasal
tissues. FIGS. 3A,
3B, and 3C show a cross-sectional view, a top view, and a bottom view,
respectively, of
the applicator tip embodiment shown in FIG. 3. As can be seen in FIG. 3B, the
sidewall
orifices 18 can be positioned generally uniformly around sidewall 12 to
provide relatively
uniform application of the gel within the nasal cavity onto the nasal tissues.
In the
preferred embodiment shown in FIG. 3B, sidewall orifices 18 are positioned
120° apart
from each other. Other positions of the sidewall orifices 18 may be used to
suitably
dispense the gel within the nasal cavity.
3o FIG. 3A is a cross-sectional view of the applicator tip embodiment shown in
FIG. 3, taken
along line A-A of FIG. 3. In this preferred embodiment, the applicator tip 10
has a total
length of about 0.8 inches, a sidewall 12 length of about 0.54 inches, and a
base 11 width
of about 0.37 inches. As stated previously, the dimensions of applicator tip
10 are
selected to comfortably fit within the nasal cavity to apply the nasal gel of
the present
invention.
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FIG. 4 is a perspective view of the applicator tip embodiment shown in FIG. 1.
Other
embodiments of the applicator tip of the present invention are shown in FIGS.
5 and 6.
As can be seen, the number and dimensions of orifice 18 can be varied
depending on the
viscosity of the gel being applied and the amount of gel to be dispensed per
application.
FIG. 6 shows an embodiment in which sidewall orifice 18 has different
dimensions
to depending on the location of each orifice 18 along the sidewall 12.
Applicator tip 10 can be made of any material suitable for use with the
hydrating nasal gel
of the present invention. Such materials must be compatible with the hydrating
nasal gel,
must be safe for the intended use, and should be suitable for use in
conjunction with a
dispenser containing the nasal gel, such as a tube, bottle, sprayer, and the
like. Such
materials include, but axe not limited to, polyethylene, polypropylene,
polyurethane, ABS,
and the like. Preferably, injection molded polyethylene is used to make
applicator tip 10
of the present invention.
2o The applicator tip of the present invention is suitable for dispensing gels
having a
viscosity ranging from between about 5,000 cps to 300,000 cps at room
temperature using
a Brookfield viscometer. Particularly preferred for use with the applicator
tip of the
present invention are gels that are thixotropic and have a significant yield
point, although
flowable gels can be dispensed through this applicator tip as well.
Although the applicator tip has been described for use in the nasal cavity, it
can be used to
apply a gel to any cavity that has a geometry and requirements similar to
those of the
nasal cavity. Also, although the applicator tip has been described for
dispensing a gel
product, a similar applicator can be used to dispense a solid or liquid
product.
Industrial Applicability
Exam lp a II
A study was conducted using the hydrating nasal gel prepared according to the
formula
shown in Table II. The gel was placed in a dispensing tube to which the
applicator tip
shown in FIGS. 2-4 was attached. 115 study participants were asked to use the
gel over a
3 to S day period. The results are shown below.
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Satisfaction with time for gel to take effect:
Extremely satisfied 17%
Very satisfied 42%
Somewhat satisfied 29%
Not very satisfied 5%
io Not at ALL satisfied 7%
Did the product soothe/relieve?
Yes 91
No 9%
is
Duration of soothing effect (in those who said it was soothin
Less than one hour 11
One to two hours 22%
Two to three hours 15%
2o More than three hours 44%
Mean duration of soothing
effect: 3.6 hours
As can be seen, the hydrating nasal gel of the present invention, applied with
the
applicator of the present invention, provided significant relief to subjects
suffering from
25 nasal discomfort without the need for drug ingredients.
Although the foregoing is intended to describe the present invention, it is
not meant to
limit the full scope of the invention, which is set forth in the following
claims.
