Note: Descriptions are shown in the official language in which they were submitted.
CA 02296625 2000-O1-18
SWEAT RESISTANT SUNBLOCK AND ANTIOXIDANT COMPOSITION
Field Of The Invention
The technical field of this invention is compositions and
methods for treating skin to reduce the risk of skin damage caused
by sunlight or other sources of ultraviolet radiation without
forming a visible mask and is sweat resistant. There is further
provided a means for reducing oxidative damage to the skin and
means for increasing the SPF of sunblocking formulations.
Backcrround Of The Invention
Skin damage such as cancer is a prevalent disease in humans
caused by overexposure to ultraviolet radiation from the sun and
other sources . It is commonly known that people with dark skin, or
skin that easily tans, are less likely to develop skin cancer due
to sunlight exposure. This reduced risk of sunlight-induced cancer
is apparently due to the protective nature of melanin against
ultraviolet light, and the relatively higher concentrations of
melanin in the skin of darker skinned peoples. Current methods for
reducing the risk of skin cancer caused by sunlight usually involve
the control or elimination of sunlight exposure. Examples include
mechanical blocking of the sun's rays, or chemical screening of the
sun's rays, such as by using the ultraviolet sunscreen ingredient
para-amino benzoic acid (PABA) . Although such approaches appear to
reduce the risk of sunlight and other ultraviolet radiation induced
skin cancer, there remains a need for additional methods of
treatment, particularly methods which are effective for treatment
after exposure to the ultraviolet light.
CA 02296625 2000-O1-18
PABA may affect some individuals adversely, particularly those
with photosensitivity who are taking certain drugs. For these
people use of opaque creams, pastes and lotions is advisable.
Ultraviolet radiation and the atmosphere also causes oxidative
damage to the skin as to cause dryness, loss of elasticity and
wrinkles. The use of sunblocking pigments is well known, however,
these pigments such as zinc and iron oxide when used alone have a
drying effect.
These pigments have often been used in compositions in large
particle size and in a form which is a mask and used primarily by
skiers and on beaches. However, such compositions have only found
use on the face and particularly on the nose.
Other pigment formulations do not provide a broad spectrum of
protection when used in a form and an amount where they are not
perceivable on the user.
It is therefore desirable to provide a sunblocking composition
which can achieve maximum full spectrum protection throughout the
entire UVB-UVA range plus visible and infrared which does not cause
damage to the skin but provides an antioxidant effect.
It is further desirable to provide a sunblocking formulation
which can be used by people on the beach and those requiring
environmental protection following a surgical trauma.
Summary Of The Invention
According to the present invention, there is provided a sweat
resistant composition for protection against ultraviolet and
infrared radiation which also reduces acute oxidation damage to the
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skin. The composition comprises:
A. about 1.5 to 10.50 by weight of a plurality of micronized
and ultramicronized titanium dioxide particles having a
variety of particle sizes not more than 10 microns;
B, about 0.5 to 2.5o by weight of a plurality of
dermatologically acceptable iron and zinc oxides having
a particle size not more than 10 microns;
C. about 0.5 to 2.5% by weight of talcum having a particle
size less than 10 microns;
_D. about 4.5 to 10% by weight of antioxidants;
E. about 0.5 to 5% by weight of a water soluble polymer
which blocks ultraviolet radiation;
F. a selenium yeast complex; and
G. at least one aqueous topical vehicle selected from the
group consisting of ointments, suspensions, creams,
lotions and emulsions.
The compositions provide an average SPF of at least about 70.
Advantageously, the composition contains non-para aminobenzoic
acid UV absorbers and a selenium protein complex.
It is therefore an object of the invention to provide a sweat
resistant sunblocking formulation which protects over a large range
of radiation wavelengths.
It is another object of the invention to provide a U.V.
blocking formulation for use by parties suffering a skin trauma.
It is yet another object of the invention to provide a
sunblocking formulation which reduces oxidative damage to the skin.
Description Of The Preferred Embodiments
The sweat resistant sunblocking and antioxidative compositions
of the invention comprise:
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A. about 1.5 to 20.50 by weight of micronized and
ultramicronized titanium dioxide particles having a
variety of the different sizes provides the broader
spectrum of radiation blocking;
B. about 0.5 to 2.5% by weight of a plurality of
dermatologically acceptable iron and zinc oxides having
a particle size from about 0.3 to 10 microns.
Preferably, the metal oxides include different kinds of
iron oxides and zinc oxides;
C. about 0.5 to 2.5% by weight of micronized talcum having
a particle size of about 0.3 to 10 microns;
D. about 4.5 to 10% by weight of antioxidants;
E. about 1.5 to 5% by weight of a water soluble ultraviolet
radiation block polymer;
F. a selenium yeast complex;
G. at least one aqueous topical vehicle selected from the
group consisting of ointments, suspensions, creams,
lotions and emulsions; and
H. a UV absorber selected from the group consisting of octyl
methyoxycinnamate, benzophenone-3 and octocrylene.
The composition is formulated so as to provide an average SPF
of at least about 70. By providing a range of particle sizes from
0.3 to l0 microns of the titanium oxide, iron oxides, zinc oxide
and talc, a wide range of sunblocking is achieved without creating
a noticeable mask. There is achieved a full spectrum of protection
throughout the entire UVB-UVA range plus visible and infrared,
namely, UVB=290nm-32nm; UVA=320nm-380nm; visible - 380/400nm -
650/700nm; infrared - above 650/70onm.
Preferably, different types of iron oxides are utilized,
namely, red, yellow, black, brown and black-brown iron oxide s. The
compositions of the invention can be optimized when eight forms of
milled solids in the micronized and ultramicronized ranges are
utilized.
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Sunblocking protection is further enhanced through the use of
water soluble sunblocking -polymers such as aluminum starch
octenylsuccinate acrylate/octyacrylamide copolymer (Dermacyl LT)
which also helps in dispersion of the oxides.
The addition of up to about 3o by weight of UV protection
boosters such as octyldodecyl neopentanate (tradename ELEFAC-I205k)
enhances the W protection factor and strengthens the atmospheric
skin - shield effectiveness.
The addition of up to about 5o by weight of non-PABA radiation
absorbers such as octyl methoxycinnamate (UVB), benzophenone-3
(UVB-mid UVA) and octocrylene (UVB-mid UVA) are used to assure
continuous uninterrupted coverage.
Addition of at least 0.2 mg/g, preferably 1-5 mg/g, of a
selenium protein complex such as selenium: yeast complexes, sold
under the trademark Biomin SE/P/C, by Brooks Industries, Inc.,
South Plainfield, N.J., have been demonstrated to increase minimal
erythema dose-response while reducing acute skin cell damage due to
UV exposure.
Biomin SE/P/C has a selenium content of about 0.1% and a
polypeptide content of about 700. The Biomins have been found to
increase SPF about 16 to 250.
The antioxidants which may be used in the compositions of the
invention include tocopherol and tocopheryl acetate, ascorbyl
acetate (Vitamin C derived) and beta carotene which are effective
topical cellular protectants. The single most potent antioxidant
is pycnogenol, a bioflavonoid like structure described in U.S.
CA 02296625 2005-09-09
Patent No. 4,698,360.
The composition according to this invention preferably
includes the desired sunblocking ingredients in combination with
one or more suitable topical ointments, creams, lotions or similar
topical vehicles allowing for relatively even and dilute
application of the active ingredient or ingredients to exposed
surfaces of skin. A variety of commercially available topical
vehicles are appropriate for use in this invention. Topical
vehicles suitable for use in this invention can be selected from
water, water-in-oil and oil-in-water emulsions of mineral,
vegetable, animal and synthetic oils; petrolatum; glycerol;
mineral; vegetable, animal and synthetic oils; propylene glycol;
other aliphatic and aromatic alcohols which can be tolerated by the
skin and many other vehicles suitable for topical application to
skin.
The compositions according to this invention can also be
enhanced by including other suitable additives in the topical
mixtures. One preferred class of skin treatment compositions
according to this invention uses a suitable in combination with a
suitable chemical sunscreen, in particular sunscreens which are
effective at reducing the intensity of ultraviolet radiation which
reaches the skin. Sunscreens which may be suitable for use in the
novel skin treatment compositions include in particular nonparamino
benzoic acid sunscreens. Sunscreens are preferably included in the
novel compositions in amounts sufficient to provide concentrations
ranging from none to approximately 100 milligrams of sunscreen per
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millimeter of the topical mixtures. Concentration of the
ultraviolet screening agent in amounts sufficient to provide
sunscreen factors ranging from approximately 1 to approximately 30
are also indicative of the concentration of the ultraviolet
screening agent which may be included. Examples of additional
sunscreens which may be useful include octyl dimethyl PBA, octyl
salicylate, palmitate, oxybenzone, and others. The suitable
ultraviolet screening agent or agents are advantageously included
to provide a sunscreen effect which is particularly effective and
easy to apply in a routine manner prior to or during exposure to
sunlight.
A variety of other additives may also be included in skin
treatment compositions according to this invention for a variety of
purposes. Ingredients for enhancing or providing humectant
properties, spreadability, non-greasiness, fragrance, absorbability
and many other desirable attributes of the novel skin treatment
compositions can also be included.
The novel compositions can also be made by selecting, buying
or manufacturing a suitable cream, lotion, suspension, ointment or
other topical vehicle and then mixing the desired active ingredient
or combination of active ingredients into the vehicle in the
desired proportions. The active ingredients include the desired
micronized particles, anti-oxidants and any suitable ultraviolet
screening agent. Any desired additional such as described above
are also mixed into the topical mixture in the desired
concentrations.
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The invention also includes novel methods for treating skin to
reduce the risk of skin damage induced by sunlight or other source
of ultraviolet radiation. The methods are useful in treatment
mammals, more particularly primates, especially humans, both male
and female. The novel methods include obtaining or preparing a
suitable cream or other composition, such as described hereinabove.
The compositions are applied to the skin in amounts sufficient to
create effective application rates. The novel compositions are
most preferably applied to healthy skin not opened by wound,
disease or other affliction. The novel compositions are spread
evenly onto the skin by the user's hands or with the aid of a
suitable applicator, such as a brush, wand or other implement.
Example I
A 1000 mg. batch of a composition of the invention was
prepared by admixing the following ingredients in the following
order:
Ingredient Wt. mg.
TM
Elefac I-205 25.0
~ 30.0
Polysorbate 20
Tocopheryl Acetate 5.0
Sorbitan Laureate 9.0
Covi-ox T50TM 2.5
Ascorby Palmitate 0.5
Emulgade PL- 45 . 0
1
618T" (CTFA)
z 15.0
,M
Dermacyrl LT
~ 70.0
Uvinul N-539 SC~
Parsol MCX'~" 60.0
Liquipar(mixed parabens) 5.0
~
Carotene in oil (30 0.5
%)
Tiosperse TNTM 75.0
Z-Cote HP~' 32.6
Water QS
Caromel 10.0
Polysorbate 20T" 1.5
Foamine 0-80T"' 3.0
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Benzophenone-3 40.0
Disodium EDTA 1.0
Antifoam FG-10~' ~ 1.0
Titanium Dioxide 175.0
Talc (Sugarload USP) 60.0
Cosmetic Red Iron Oxide 2.7
Cosmetic Yellow Iron Oxide 2.3
Cosmetic Brown Iron Oxide 3.8
Nonocat Superfine Iron Oxide 0.4
Propylene Glycol 40.0
Bonidox LT" 3.0
Dry Flo PCT'' 15.0
Pycnogenol'x' 1 .
0
Biomin SE/P/C T'" 1 .
0
1000mg
The composition when applied provides an average SPF of at
least 70.
Comparative Example I
A study of 21 patients was conducted to determine the sweat
resistance of the composition of Example I. The study was
conducted pursuant to the standard test for sunscreen products
according'to the proposed monograph rules the FDA as reported in
the Federal Register Vol. 43, No. 163 of August 25, 1978.
The results are shown in the following Table:
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Table 1
Individual SPF Values
CPTC Skin Type 8o Homoslate Standard
Pre-sweatingPost-sweating
8990 III 6.3 75.0 60.0
13178 II 5.0 75.0 60.0
728 III 5.0 60.0 60.0
1272 II 5.0 75.0 75.0
7624 II 5.0 75.0 75.0
12800 II 5.0 75.0 75.0
8907 II 4.0 75.0 75.0
11720 II 4.9 75.0 ?5.0
5678 II 4.9 75.0 75.0
10583 II 5.0 75.0 75.0
7285 II 4.9 75_0 75.0
13926 II 5.0 75.0 60.0
3760 II 5.0 60.0 60.0
12448 II 5.0 75.0 75.0
3414 II 5.0 60.0 60.0
3026 III 4.9 75.0 75.0
3656 II 4.9 75.0 75.0
2532 II 5.0 60.0 60.0
12278 III 5.0 75.0 75.0
12305 II ** ** **
Average SPF 49.9 72.75 70.50
CPTC# = Consumer Product Panelist Number
**Technical deviation from the protocol
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Example II
To a commercially available suntan lotion sold under the
brand
name COPPERTONE CREAM which has the following listed ingredients:
palmitate and oxybenzyone as sunscreen agents,
sorbitansesquioleate, sorbitol, glycerol stearate SE,
isopropylmyristate, triethanolamine, octadecene/maleic
anhydride
copolymer, benzyl alcohol, lanolin, jajoba oil, cocoa butter, aloe
extract, methyl paraben, propyl paraben, vitamin E acetate
fragrance and water is added to the following:
Ingredient Wt o
Micronized Titanium Dioxides (6 types) 5.0
Micronized Iron Oxides (2 types) 2_0
Talc 1.0
Pycnogenol 3.0
Dermacryl LT z'~' 1 . 5
Biomin SE/P/C'~" 1.0
Example III
A sweat resistant composition for protection against
ultraviolet and infrared radiation can be prepared by admixing the
following:
A. about 1.5 to 10.50 by weight of micronized and
ultramicronized titanium dioxide particles having
particle sizes from about 0.3 to 10 microns;
B. about 0.5 to 2.5% by weight of a plurality of iron oxides
having a particle size of about 0.3 to 10 microns;
C. about 0.5 to 2.5o by weight of talcum having a particle
size of about 0.3 to 10 microns;
D. about 4.5 to 10% by weight of antioxidants selected from
the group consisting of tocopherol, tocopherol acetate,
ascorbic acetate and beta carotene;
E. about 0.5 to 1.5% by weight of aluminum starch
octenylsuccinate acrylate/octyacrylamide copolymer;
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F. about 1.0 mg. of Biomin SE/P/C;Mand
G. an aqueous topical. lotion.
The topical lotion can be a commercially available sunscreen
lotion such as sold under the brand names SEA and SKI, HAWAIIAN
TROPIC and the like.
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