U.S. patent application number 13/961102 was filed with the patent office on 2014-01-16 for clear, greaseless skin care compositions.
This patent application is currently assigned to Chemsil Silicones, Inc.. The applicant listed for this patent is Chemsil Silicones, Inc.. Invention is credited to James Jefferies Harrison, Nohemi Harrison.
Application Number | 20140018328 13/961102 |
Document ID | / |
Family ID | 49914486 |
Filed Date | 2014-01-16 |
United States Patent
Application |
20140018328 |
Kind Code |
A1 |
Harrison; James Jefferies ;
et al. |
January 16, 2014 |
Clear, Greaseless Skin Care Compositions
Abstract
The present invention relates to compositions including
anhydrous compositions which include a dimethicone crosspolymer
and/or dimethicone elastomer gum and one or more skin care products
which may include retinoic acid, retinoic acid derivatives,
retinal, retinol and/or retinyl esters, and methods of making,
storing, and using such compositions.
Inventors: |
Harrison; James Jefferies;
(West Hills, CA) ; Harrison; Nohemi; (West Hills,
CA) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Chemsil Silicones, Inc. |
Chatsworth |
CA |
US |
|
|
Assignee: |
Chemsil Silicones, Inc.
Chatsworth
CA
|
Family ID: |
49914486 |
Appl. No.: |
13/961102 |
Filed: |
August 7, 2013 |
Related U.S. Patent Documents
|
|
|
|
|
|
Application
Number |
Filing Date |
Patent Number |
|
|
10855934 |
May 26, 2004 |
|
|
|
13961102 |
|
|
|
|
10254418 |
Sep 25, 2002 |
|
|
|
10855934 |
|
|
|
|
Current U.S.
Class: |
514/159 ;
514/627; 514/692; 514/729; 514/772 |
Current CPC
Class: |
A61K 31/07 20130101;
A61K 31/165 20130101; A61K 31/125 20130101; A61K 31/045 20130101;
A61K 31/165 20130101; A61K 31/618 20130101; A61K 31/07 20130101;
A61K 47/34 20130101; A61K 31/045 20130101; A61K 2300/00 20130101;
A61K 2300/00 20130101; A61K 2300/00 20130101; A61K 2300/00
20130101; A61K 9/0014 20130101; A61K 31/125 20130101; A61K 31/618
20130101; A61K 9/06 20130101; A61K 2300/00 20130101 |
Class at
Publication: |
514/159 ;
514/772; 514/692; 514/729; 514/627 |
International
Class: |
A61K 31/618 20060101
A61K031/618; A61K 31/165 20060101 A61K031/165; A61K 31/045 20060101
A61K031/045; A61K 47/34 20060101 A61K047/34; A61K 31/125 20060101
A61K031/125 |
Claims
1. A topical analgesic composition comprising at least one high
molecular weight silicone component having a molecular weight
between about 100,000 Da and 100,000,000 Da, and at least one
analgesic component, wherein the composition is substantially
anhydrous, greaseless, and substantially clear or translucent.
2. The greaseless analgesic composition of claim 1 wherein the high
molecular weight silicone component is selected from the group
consisting of a dimethicone crosspolymer and a dimethicone gum.
3. The greaseless analgesic composition of claim 1 wherein said at
least one analgesic component is selected from the group consisting
of: methyl salicylate, salicylic acid, a salicylic acid derivative,
camphor, menthol, eucalyptus oil, capsaicin, histamine
dihydrochloride, methyl micotinate, wintergreen extract, eucalyptus
extract, turpentine extract, a pharmaceutically acceptable salt of
lidocaine, a pharmaceutically acceptable salt of bupivacaine, a
pharmaceutically acceptable salt of chlorprocaine, a
pharmaceutically acceptable salt of dibucaine, a pharmaceutically
acceptable salt of etidocaine, a pharmaceutically acceptable salt
of mepivacaine, a pharmaceutically acceptable salt of tetracaine, a
pharmaceutically acceptable salt of dyclonine, a pharmaceutically
acceptable salt of hexylcaine, a pharmaceutically acceptable salt
of procaine, a pharmaceutically acceptable salt of cocaine, a
pharmaceutically acceptable salt of ketamine, a pharmaceutically
acceptable salt of pramoxine, a pharmaceutically acceptable salt of
methdilizine, a pharmaceutically acceptable salt of trimeprazine,
phenol and a steroidal or non-steriodal antiimflammatory agent.
4. The greaseless analgesic composition of claim 3 wherein said at
least one analgesic component is selected from the group consisting
of: methyl salicylate, salicylic acid, a salicylic acid derivative,
camphor, menthol, eucalyptus oil, and capsaicin.
5. The greaseless analgesic composition of claim 1 further
comprising at least one low molecular weight silicone having a
measurable vapor pressure at room temperature.
6. The greaseless analgesic composition of claim 5 wherein said low
molecular weight silicone is selected from the group consisting of
a cyclic silicone and a non-cyclic silicone.
7. The greaseless analgesic composition of claim 6 wherein said low
molecular weight silicone comprises a cyclomethicone.
8. The greaseless analgesic composition of claim 7 wherein said low
molecular weight silicone comprises a cyclomethicone selected from
the group consisting of octylmethylcyclotetrasiloxane,
hexamethylcyclotrisiloxane and decamethylcyclopentasiloxane.
9. The greaseless analgesic composition of claim 6 wherein said low
molecular weight silicone comprises a non-cyclic silicone selected
from the group consisting of hexamethyldisiloxane and low molecular
weight dimethicone.
10. The greaseless analgesic composition of claim 1 comprising a
high molecular weight dimethicone component, a volatile low
molecular weight component, and at least one analgesic component
selected from the group consisting of methyl salicylate, salicylic
acid, a salicylic acid derivative, camphor, menthol, eucalyptus oil
and capsaicin.
11. The greaseless analgesic composition of claim 10 comprising at
least two analgesic components selected from the group consisting
of methyl salicylate, salicylic acid, a salicylic acid derivative,
camphor, menthol, eucalyptus oil and capsaicin.
12. The greaseless analgesic composition of claim 1 comprising a
capsaicin component dissolved in a alkyl fluid.
13. The greaseless analgesic composition of claim 12 comprising at
least one low molecular weight silicone component.
14. The greaseless analgesic composition of claim 1, in the form of
a serum having a viscosity of from about 0.1 centistokes to about
3500 centistokes.
15. A method of reducing pain in a mammal, comprising applying to a
skin surface of said mammal a composition comprising the
composition of claim 1, and permitting said applied composition to
dry on said skin surface, wherein said high molecular weight
silicone component forms a substantially clear, water-resistant
barrier on said skin surface after drying.
16. A topical analgesic composition comprising at least one high
molecular weight dimethicone component having a molecular weight
between about 100,000 Da and 100,000,000 Da, and at least one
analgesic component comprising an agent selected from the group
consisting of selected from the group consisting of: methyl
salicylate, salicylic acid, a salicylic acid derivative, camphor,
menthol, eucalyptus oil, and capsaicin, wherein the composition is
substantially anhydrous, greaseless, and substantially clear or
translucent.
17. The composition of claim 16 wherein the composition further
comprises at least one organic solvent.
18. The composition of claim 17 wherein the organic solvent
comprises an isoparaffinic solvent.
19. The composition of claim 16 wherein the composition comprises a
low molecular weight silicone having a measurable vapor pressure at
room temperature.
20. The composition of claim 17 wherein the composition comprises a
low molecular weight silicone having a measurable vapor pressure at
room temperature.
Description
RELATED APPLICATIONS
[0001] Continuation of pending U.S. patent application Ser. No.
10/855,934, filed May 26, 2004, which was a continuation-in-part of
U.S. patent application Ser. No. 10/254,418, filed Sep. 25, 2002.
The disclosures of each of these applications is hereby
incorporated herein in its entirety by reference.
FIELD OF THE INVENTION
[0002] The present invention relates to clear, greaseless
compositions which include a pharmaceutically active component. The
compositions are preferably anhydrous and include silicones, for
example, one or more of dimethicone crosspolymers, dimethicone gum,
hexamethyldisiloxane and low molecular weight dimethicones.
[0003] More particularly, the composition may be a topically
applied composition containing one or more analgesics or one or
more skin care components.
[0004] In a further and more specific aspect, the invention relates
to clear, greaseless compositions including a pharmaceutically
active component such as an analgesic including methyl salicylate,
camphor, menthol and capsaicin or a skin care component selected
from the group consisting of anti-wrinkle components, anti-skin
atrophy components, skin repair components, and mixtures
thereof.
[0005] Advantageously, the pharmaceutically active component is a
skin care component selected from the group consisting of retinoic
acid, retinoic acid derivatives, retinal, retinol, retinyl esters
and mixtures thereof.
BACKGROUND
[0006] Various pharmaceutical products are designed for topical
application, for instance in the form of gels, creams and lotions.
Among such products are compositions including anti-acne actives,
antimicrobial and antifungal actives, anti-wrinkle and anti-skin
atrophy actives, skin barrier repair aids, cosmetic soothing aids,
artificial tanning agents and accelerators, skin lightening
actives, sunscreen actives, skin tightening agents, anti-itch
agents, hair growth inhibitors, desquamating agents, antiglycation
agents, wound healing actives, actives to treat psoriasis, skin
cancer, impetigo, herpes, chickenpox and dermatitis and mixtures
thereof.
[0007] Some of the above compositions include components that are
insoluble or only slightly soluble in water, but are readily
soluble in non-polar substances such as organic solvents and oils.
However, compositions including oils and the like have certain
drawbacks in their use. For example, they may produce a sticky
and/or greasy feel upon application to the skin. The compositions
may also be inconvenient for use by, for example, requiring an
extended drying time after application to the skin and/or staining
the skin and/or clothing. In addition, these compositions do not
necessarily provide for a film layer that will be effective to
retain volatile actives. Further, after application the
compositions typically are easily solubilized by aqueous solutions
such as perspiration which may lead to loss of the composition
and/or the actives. Further, water or oil containing compositions
often include emulsifiers which can cause skin irritation. In
addition, the process of making these compositions typically
involves heating which may lead to the loss of the actives by, for
example, evaporation and/or sublimation.
[0008] Two classes of pharmaceutical compositions particularly
prone to the aforementioned drawbacks are skin-care compositions
and analgesics.
[0009] Of special interest in the category of skin care
compositions are compositions including anti-wrinkle components,
anti-skin atrophy components, skin repair components and mixtures
thereof, and particularly skin care compositions selected from the
group consisting of retinoic acid, retinoic acid derivatives,
retinal, retinol, retinyl esters and mixtures thereof.
[0010] Retinol, perhaps the most well known of these compositions,
is frequently used in anti-aging creams, lotions, and serums.
Because retinol is very unstable to heat, light, and oxygen,
products containing retinol currently must be manufactured under
inert gas conditions and packaged in aluminum tubes to prevent
oxygen or light from degrading the active retinol. These
restrictive manufacturing and packaging conditions increase the
overall cost of the skin-care products, making them unaffordable to
many consumers.
[0011] Also of interest are analgesic compositions, particularly
compositions selected from the group consisting of methyl
salicylate, camphor, menthol and capsaicin. Methyl salicylate is a
2-hydroxybenzoic acid methyl ester which can occur naturally in
wintergreen oil, betula oil, sweet birch oil, teaberry oil and in
the leaves of Gualtheria procumbens L. Ericadeae and in the bark of
Betula lenta L. Betulaceae. It can also be prepared by
etherification of salicylic acid with methanol. Camphor is
1,7,7-trimethylbicyclo[2,2,1]heptan-2-one and occurs in all parts
of the camphor tree, Cinnamomum camphora T. It is also synthesized
from vinyl chloride and cyclopentadiene. Menthol, or
5-methyl-2-[1-methylethyl]-cyclohexanol, can be obtained from mint
oils, for example, peppermint oil. It can also be obtained through
hydrogenation of thymol. Capsaicin, or
N-(4-hydroxy-3-methoxybenzyl)-8-methylnontrans-6-enamide, can be
obtained from the fruits of plants of the Capsicum genus.
[0012] Water and oil containing compositions such as gels, lotions
and creams are useful for application of menthol, camphor, and
capsaicin and methyl salicylate as well as other analgesics. U.S.
Pat. No. 5,124,320 and U.S. Pat. No. 5,013,726 disclose
compositions in which methyl salicylate, menthol and camphor are
dissolved into C12-C15 alkyl benzoate, eucalyptus oil and jojoba
oil.
[0013] There remains a need for topically applied compositions
which may be used to apply skin-care products. and/or analgesics
which are easily and economically prepared, are non-sticky,
greaseless, require less drying time after application to the skin,
do not stain the skin, provide water resistance or waterproofing,
act to efficiently retain actives and are not irritating to the
skin.
[0014] In addition, a need exists for skin-care products,
particularly retinol-containing skin-care products, which can be
economically packaged in opaque containers and which remain stable
when exposed to oxygen and/or higher than normal temperatures.
SUMMARY
[0015] The present invention meets these needs. Compositions of the
invention can be manufactured at relatively low cost under
non-restrictive conditions. Such compositions are preferably
anhydrous with no oily component, and as such have a reduced greasy
feel relative to similar or identical compositions which include
oil and/or water. Advantageously, the compositions will dry in a
reduced period of time relative to similar or identical
compositions which include oil and/or water. In addition, the
compositions may be made at room temperature which decreases the
loss of certain actives during production. Moreover, the applied
composition has increased resistance to being washed off or rubbed
off, and has greater adhesion to the skin relative to aqueous or
oil based compositions. Further, these compositions can provide a
water resistant or water proof film when applied to a surface, for
example, when applied to the skin. This water resistance or water
proofing can prevent an undesired removal of actives upon exposure
to moisture thereby retaining the active component in proximity to
the surface (e. g. skin) to which the composition is applied. The
water resistance or water proofing may be provided, at least in
part, by a silicone component, which may include dimethicone gum
and/or dimethicone crosspolymer; included in a composition.
[0016] In one broad embodiment, the present invention provides for
an effective amount of a pharmaceutically active component to be
included in a silicone component which may include a low molecular
weight silicone (e.g., hexamethyldisiloxane and/or low molecular
weight dimethicone) and a high molecular weight silicone (e.g.,
weight (e.g., dimethicone crosspolymer and/or dimethicone elastomer
gum). The high molecular weight silicone may be present in an
amount effective to produce a composition with a desired
consistency.
[0017] In one embodiment, the present invention provides for an
anhydrous composition which includes a dimethicone crosspolymer
and/or a dimethicone gum and an analgesic component. The
dimethicone crosspolymer may have a molecular weight of between
about 100,000 and about 100,000,000. The dimethicone gum may have a
molecular weight of between about 100,000 and about 100,000,000. In
still another embodiment, a composition includes the dimethicone
crosspolymer and the dimethicone gum. In one embodiment, the
dimethicone crosspolymer and/or dimethicone gum comprises about 10%
to about 99.999% by weight of the composition.
[0018] In a particularly useful embodiment, the compositions
include a low molecular weight silicone. Examples of low molecular
weight silicones that may be included in a composition include,
without limitation, low molecular weight dimethicone, cyclic
silicones, and hexamethyldisiloxane.
[0019] The compositions may include a skin-care component selected
from the group consisting of anti-wrinkle components, anti-skin
atrophy components, skin repair components, and mixtures thereof.
The skin care component is advantageously selected from the group
consisting of retinoic acid, retinoic acid derivatives, retinal,
retinol, retinyl esters and mixtures thereof. The skin care
component may comprise about 0.0001% to about 1% or about 5% or
about 10% by weight of the composition. In a particularly useful
embodiment, the skin care component comprises about 0.0001% or
about 0.01% or about 0.1% to about 0.3% to about 0.4% or 0.5% or
about 1%, by weight of the composition.
[0020] Alternatively, the compositions may include an analgesic
component which includes one or more analgesics. Examples of
analgesics which may be included in the present compositions
include camphor, menthol, capsaicin and methyl salicylate and
mixtures thereof. The analgesic may comprise about 0.001% to about
90% of the composition by weight.
[0021] Each and every feature described herein, and each and every
combination of two or more of such features, is included within the
scope of the present invention provided that the features included
in such a combination are not mutually inconsistent.
[0022] These and other aspects and advantages of the present
invention are apparent in the following detailed description,
examples and claims.
DETAILED DESCRIPTION
[0023] The present invention is based in part upon the discovery of
clear, greaseless silicone-containing compositions which may be
anhydrous and include a pharmaceutically active component. The
present invention also includes methods of making and using such
compositions.
[0024] In one embodiment, the invention relates to compositions
which include one or more of dimethicone crosspolymers, dimethicone
gum, hexamethyldisiloxane and low molecular weight dimethicones.
The active component may include one or more analgesics to treat
pain. Particularly useful analgesics which may be included in a
composition include, without limitation, methyl salicylate,
camphor, menthol and capsaicin.
[0025] Particularly useful embodiments of the present composition
include one or more of methyl salicylate menthol, camphor and
capsaicin. In one embodiment, the active component includes methyl
salicylate, menthol, camphor and capsaicin. In another embodiment,
the active component includes menthol, camphor and capsaicin. In
another embodiment, the active component includes camphor and
capsaicin. In another embodiment, the active component includes
capsaicin. In another embodiment, the active component includes
camphor. In another embodiment, the active component includes
menthol. In another embodiment, the active component includes
methyl salicylate. In another embodiment, the active component
includes methyl salicylate and camphor. In another embodiment, the
active component includes methyl salicylate and menthol. In another
embodiment, the active component includes methyl salicylate,
camphor and capsaicin. In another embodiment, the active component
includes methyl salicylate and capsaicin. In another embodiment,
the active component includes menthol, and capsaicin. In another
embodiment, the active component includes methyl salicylate,
menthol and capsaicin. In another embodiment, the active component
includes methyl salicylate menthol and camphor.
[0026] These and other embodiments of the present invention are
effective to provide relief from pain by topical application to an
animal patient, for example, topical application to a human
patient, for example, application to the skin of a human patient.
Without wishing to limit the invention to any theory or mechanism
of operation, it is believed that these analgesics can relieve pain
in areas of a body including, but not limited to, the skin,
muscles, joints, or viscera distal to the site of application by
stimulating depressing cutaneous sensory receptors. Additional
analgesics which may be included in a composition include, without
limitation, salicylic acid, salicylic acid derivatives such as
triethanolamine salicylate, histamine dihydrochloride, methyl
nicotinate and wintergreen, eucalyptus and turpentine extracts as
well as other counter irritants.
[0027] The active component may also include topical anesthetics
such as pharmaceutically-acceptable salts of lidocaine,
bupivacaine, chlorprocaine, dibucaine, etidocaine, mepivacaine,
tetracaine, dyclonine, hexylcaine, procaine, cocaine, ketamine,
pramoxine and phenol. Also included for use in the present
compositions may be antipruritic drugs which include, without
limitation, pharmaceutically-acceptable salts of methdilizine and
trimeprazine.
[0028] Also included in an active component may be nonsteroidal
anti-inflammatory drugs (NSAIDS). The NSAIDS can selected from the
following categories: propionic acid derivatives; acetic acid
derivatives; fenamic acid derivatives; biphenylcarboxylic. acid
derivatives; and oxicams. All of these NSAIDS are described in the
U.S. Pat. No. 4,985,459, which is incorporated in its entirety by
reference herein. Propionic NSAIDS including but not limited to
aspirin, acetaminophen, ibuprofen, naproxen, benoxaprofen,
flurbiprofen, fenoprofen, fenbufen, ketoprofen, indoprofen,
pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen,
tioxaprofen, suprofen, 30 alminoprofen, tiaprofenic acid, fluprofen
and bucloxic acid. Also useful are the steroidal anti-inflammatory
drugs including hydrocortisone and the like.
[0029] Active ingredients useful herein may be categorized by their
therapeutic benefit or their postulated mode of action such as
analgesics, for example, topical analgesics. However, it is to be
understood that the active ingredients 5 useful herein can in some
instances provide more than one therapeutic benefit or operate via
more than one mode of action. Therefore, classifications herein are
made for the sake of convenience and are not intended to limit the
active ingredient to that particular application or applications
listed. Furthermore, pharmaceutically acceptable salts of these
active ingredients are also useful in accordance with the
invention.
[0030] Other classes of active ingredients contemplated for use in
the present compositions include anti-acne actives, antimicrobial
and antifungal actives, anti-wrinkle and anti-skin atrophy actives,
skin barrier repair aids, cosmetic soothing aids, artificial
tanning agents and accelerators, skin lightening actives, sunscreen
actives, skin tightening agents, anti-itch agents, hair growth
inhibitors, desquamating agents, anti-glycation agents, wound
healing actives, actives to treat psoriasis, skin cancer, impetigo,
herpes, chickenpox and dermatitis and mixtures thereof.
Anti-Acne Actives:
[0031] Nonlimiting examples of useful anti-acne actives include the
keratolytics such as salicylic acid (0-hydroxybenzoic acid),
derivatives of salicylic acid such as 5-octanoyl salicylic acid and
4 methoxysalicylic acid, and resorcinol; retinoids such as retinoic
acid and its 30 derivatives (e.g., cis and trans);
sulfur-containing D and L amino acids and their derivatives and
salts, particularly their N-acetyl derivatives, for example,
N-acetyl-Lcysteine; lipoic acid; antibiotics and antimicrobials
such as benzoyl peroxide, octopirox, tetracycline,
2,4,4'trichloro-2'-hydroxy diphenyl ether, 3,4,4'-5
trichlorobanilide, azelaic acid and its derivatives,
phenoxyethanol, phenoxypropanol, phenoxyisopropanol, ethyl acetate,
clindamycin and meclocycline; sebostats such as flavonoids and
bioflavonoids; bile salts such as scymnol sulfate and its
derivatives, deoxycholate, and cholate; abietic acid; adapalene;
allantoin; aloe extracts; arbietic acid and its salts; aryl-2,4
dioxo oxazolidine derivatives; ASEBIOL (available from Laboratories
Serobiologiques, located in Somerville, N.J.); azaleic acid;
barberry extracts; bearberry extracts; belamcanda chinensis;
benzoquinolinones; benzoyl peroxide; berberine; BIODERMINE
(available from Sederma, located in Brooklyn, N.Y.); bioflavinoids;
bisabolol; S-carboxymethyl cysteine; carrot extracts; cassin oil;
clove extracts; citral; citronellal; climazole; Completech MBAC-OS
(available from Lipo); CREMOGEN M82 (available from Dragoco,
located in Totowa, N.J.); cucumber extracts; dehydroacetic acid and
its salts; dehydroeplandersterone salicylate; dichlorophenyl
imidazoldioxolan which is commercially available as COMPLETECH
MBAC-OS (from Lipo, located in Paterson, N.J.); DL valine and its
esters; DMDM hydantoin; Epicutin TT (available from CLR);
erythromycin; escinol; ethyl hexyl monoglyceryl ether; ethyl
2-hydroxy undecanoate; farnesol; farnesol acetate; `geranoil;
glabridin; gluconic acid; gluconolactone; glyceryl monocaprate;
glycolic acid; grapefruit seed extract; gugu lipid; Hederagenin
(available from Maruzen); hesperitin; hinokitol; hops extract;
hydrogenated rosin; 10 hydroxy decanoic acid; ichtyhol; interleukin
1 alpha antagonists: iodo-2-propynyl butyl carbamate: Kapilarine
(available from Greentech): ketoconazole: lactic acid: lemon grass
oil: Lichochalcone LR15 (available from Maruzen): linoleic acid:
LIPACIDE C8CO (available from Seppic, located in Paris, France):
lovastatin: 4 methoxysalicylic acid; metronidazole: minocycline:
mukurossi: neem seed oil: vitamin B3 compounds (such as niacinamide
and nicotinic acid): nisin: 5-octanoly salicylic acid: octopirox:
panthenol: 1-pentadecanol: peonia extract: peppermint extract:
phelladendron extract; 2-phenyl-benzothiophene derivatives;
phloretin; PHLOROGINE (available from Secma); phosphatidyl choline;
proteolytic enzymes: quercetin; red sandalwood extract; resorcinol:
rosemary extract; rutin: sage extract; salicin; salicylic acid:
skull cap extract; siber hegner extract: siberian saxifrage
extract: silicol: sodium lauryl sulfate: sodium sulfoacetamide;
Sophora Extract (available from Maruzen); sorbic acid: tetracyline;
sulfur; sunder vati extract: tea tree oil: tetra hydroabietic acid;
thyme extract; tioxolone: tocopherol; trehalose 6-undecylenoate; 3
tridecene-2-ol; triclosan; tropolone: UNITRIENOL T27 (available
from Unichem, located in Gouda, Netherlands); vitamin D3 and its
analogs: white thyme oil; willow bark extract; wogonin; Ylang
Ylang; zinc glycerolate; zinc linoleate; zinc oxide; zinc
pyrithione: zinc sulfate and mixtures thereof.
Antimicrobial and Antifungal Actives:
[0032] Antimicrobial and antifungal actives can be effective to
prevent the proliferation and growth of bacteria and fungi.
Nonlimiting examples of antimicrobial and antifungal actives
include--lactam drugs, quinolone drugs, ciprofloxacin, norfloxacin,
tetracycline, erythromycin, amikacin,
2,4,4.degree.-trichloro-2.degree.-hydroxy diphenyl ether, 3;
4,4.degree.-trichlorobanilide, phenoxyethanol, phenoxy propanol,
phenoxyisopropanol, doxycycline, chlortetracycline, capreomycin,
chlorhexidine, oxytetracycline, clindamycin, ethambutol, hexamidine
isethionate, metronidazole, pentarnidine, gentamicin, kanamycin,
lineomycin, methacycline, methenamine, minocycline, neomycin,
netilmicin, paromomycin, streptomycin, tobramycin, miconazole,
tetracycline hydrochloride, erythromycin, zinc erythromycin,
erythromycin estolate, erythromycin stearate, amikacin sulfate,
doxycycline hydrochloride, capreomycin sulfate, chlorhexidine
gluconate, chlorhexidine hydrochloride, chlortetracycline
hydrochloride, oxytetracycline hydrochloride, clindamycin
hydrochloride, ethambutol hydrochloride, metronidazole
hydrochloride, pentamidine hydrochloride, gentamicin sulfate,
kanamycin sulfate, lineomycin hydrochloride, methacycline
hydrochloride, methenamine hippurate, methenamine mandelate,
minocycline hydrochloride, neomycin sulfate, netilmicin sulfate,
paromomycin sulfate, streptomycin sulfate, tobramycin sulfate,
miconazole hydrochloride, amanfadine hydrochloride, amanfadine
sulfate, octopirox, parachlorometa xylenol, nystatin, tolnaftate,
zinc pyrithione; clotrimazole; alantolactone; isoalantolactone;
alkanet extract (alaninin); anise; arnica extract (helenalin
acetate and 11,13 dihydrohelenalin); Aspidium extract (phloro,
lucinol containing extract); barberry extract (berberine chloride);
bay sweet extract; bayberry bark extract (myricitrin); benzalkonium
chloride; benzethonium chloride; benzoic acid and its salts;
benzoin; benzyl alcohol; blessed thistle; bletilla tuber;
bloodroot; bois de rose oil; burdock; butyl paraben; cade oil; CAE
(available from Ajinomoto, located in Teaneck, N.J.); cajeput oil;
Cangzhu; capsicum frutescens extract; caraway oil; cascarilla bark
(sold under the tradename ESSENTIAL OIL); cedarleaf oil;
chamomille; chaparral; chlorhexidine gluconate; chlorophenesin;
chlorxylenol; cinnamon oil; citronella oil; clove oil; Crinipan AD
(available from Climbazole); 2,3-dihydro-farnesol; dehydroacetic
acid and its salts; dill seed oil; DOWICIL 200 (available from Dow
Chemical, located in Midland, Mich.); echinacea; elenolic acid;
epimedium; ethyl paraben; Fo-Ti; galbanum; garden burnet; GERMALL
115 and GERMALL II (available from ISP-Sutton Labs, located in
Wayne, N.J.); German chamomille oil; giant knotweed; GLYDANT
(available from Lonza, located in Fairlawn, N.J.); GLYDANT PLUS
(available from Lonza); grapefruit seed oil; 1,6 hexanediol;
hexamidine diisethionate; hinokitiol; honey; honeysuckle flower;
hops; immortelle; iodopropynl butyl carbamide (available from
Lonza); isobutyl paraben; isopropyl paraben; JM ACTICARE (available
from Microbial Systems International, located in Nottingham, NG);
juniper berries; KATHON CG (available from Rohm and Haas, located
in Philadelphia, Pa.); kojic acid; p labdanum: lavender; lemon balm
oil; lemon grass; methyl paraben; mint: mume; mustard; myrrh: neem
seed oil; ortho phenyl phenol; olive leaf extract (available from
Bio Botanica); parsley; patchouly oil; peony root; 1,2 pentandiol;
PHENONIP (available from Nipa Labs, located in Wilmington, Del.);
phenoxyethanol: phytosphingosine; pine needle oil: PLANSERVATIVE
(available from Campo Research); propyl paraben; purslane:
quillaira; rhubarb: rose geranium oil; rosemary:sichuan lovage;
sage: salicylic acid; sassafras; savory; sodium meta bisulfite:
sodium sulfite; SOPHOLIANCE (available from Soliance, located in
Compiegne, France); sorbic acid and its salts; sphingosine; stevia;
storax; sucrose esters; tarmic acid; tea; tea tree oil (cajeput
oil); thyme; triclosan; triclocarban; tropolone; turpentine;
umbelliferone (antifungal); yucca; and mixtures thereof.
Anti-Wrinkle, Anti-Skin Atrophy and Skin Repair Actives:
[0033] Anti-wrinkle, anti-skin atrophy and skin repair actives can
be effective in replenishing or rejuvenating the epidermal layer.
These actives generally provide these desirable skin care benefits
by promoting or maintaining the natural process of desquamation.
Nonlimiting examples of antiwrinkle and anti-skin atrophy actives
include retinoic acid and its derivatives (e.g., cis and trans);
retinal; retinol; retinyl esters such as retinyl acetate, retinyl
palmitate, and retinyl propionate; vitamin B compounds (such as
niacinamide and nicotinic acid), salicylic acid and derivatives
thereof (such as 5-octanoyl salicylic acid, heptyloxy 4 salicylic
acid, and 4-methoxy salicylic acid); sulfur-containing D and L
amino acids and their derivatives and salts, particularly the
N-acetyl derivatives, for example, N-acetyl-L-cysteine; thiols,
e.g. ethane thiol; hydroxy acids, phytic acid, lipoic acid;
lysophosphatidic acid; skin peel agents (e.g., phenol and the
like); Actein 27-Deoxyactein Cimicifugoside (available from
Cirnigoside); adapalene; ademethionine; adenosine; aletris extract;
alkyl glutathione esters; alkoxyalkoxy alkoxyn benzoic and
derivatives; aloe derived lectins; amino propane phosphoric acid;
3-aminopropyl dihydrogen phosphate; Amadorine (available from
Barnet Products); anise extracts; AOSINE (available from Secma);
arginine amino benzoate; ASC III (available from E. Merck, located
in Darmstadt, Germany); ascorbic acid; ascorbyl palmitate; asiatic
acid; asiaticosides; ARLAMOL GEO.TM. (available from IC, located in
Wilmington, Del.); azaleic acid; benzoic acid derivatives;
Bertholletia extracts; betulinic acid; BIOCHANIN A AND BIOPEPTIDE
CL (available from Sederma, located in Brooklyn, N.Y.); BIOPEPTIDE
EL (available from Sederma); biotin; blackberry bark extract;
blackberry lily extracts; black cohosh extract; blue cohesh
extract; butanoyl betulinic acid; carboxymethyl 1,3 beta glucan;
catecholamnines; chalcones; citric acid esters; chaste tree
extract; clover extracts; coumestrol; CPC Peptide (available from
Barnet Products); daidzein; dang gui extract; darutoside; debromo
laurinterol; 1-decanoyl-glycero-phosphonic acid;
dehydrocholesterol; dehydrodicreosol; dehydrodieugenol;
dehydroepiandersterone; DERMOLECTINE (available from Sederma);
dehydroascorbic acid; dehydroepiandersterone sulfate; dianethole;
dihydroxy benzoic acid; 2,4 dihydroxybenzoic acid; diglycol
guanidine succinate; diosgenin; disodium ascorbyl phosphate;
dodecanedioic acid; Ederline (available from Seporga); Enderline
(available from Laboratories Seporga); equal; eriodictyol; estrogen
and its derivatives; ETF (available from Laboratories Seporga);
ethocyn; ELESERYL SH (available from Laboratories Serobiologiques,
located in Somerville, N.J.); ENDONUCLEINE (available from
Laboratories Serobiologiques); ergosterol; eythrobic acid; fennel
extract; fenugreek seed extract; FIBRASTIL (available from
Sederma); FIBROSTlMULINES Sand P (available from Sederma); FIRMOGEN
LS 8445 (available from Laboratories Serobiologiques);
formononetin; forsythia fruit extract; gallic acid esters; gamma
amino butyric acid; GATULINE RC (available from Gattlefosse,
located in Priest, France); genistein; genisteine; genistic acid;
gentisyl alcohol; gingko bilboa extracts; ginseng extracts;
ginsenoside; gluco pyranosyl-L-ascorbate; glutathione and its
esters; glycitein; hesperitin; hexahydro curcumin; HMG-coenzyme A
reductase inhibitors; hops extracts; 11 hydroxy undecanoic acid; 10
hydroxy decanoic acid; 25-hydroxycholesterol; 7-hydroxylated
sterols; hydroxyethyl isostearyloxy isopropanolamine; hydroxy-tetra
methyl piperidinyloxy; 10 hypotaurine; ibukijakou extract;
isoflavone SG 10 (available from Barnet Products); kinetin; kohki
extract; L-2-OXO-thiazolidine-4-carboxylic acid esters; lactate
dehydrogenase inhibitors; 1-lauryl, -lyso-phosphatidyl choline;
lectins; lichochalcone LF15 (available from 15 Maruzen); licorice
extracts; lignan; lumisterol; lupenes; luteolin; lysophosphitidic
acid; magnesium ascorbyl phosphate; margin; melatonin; melibiose;
metalloproteinase inhibitors; methoprene; methoprenic acid;
mevalonic acid; MPC COMPLEX (available from CLR); N methyl serine;
N methyl taurine; N,N.sup.1-bis(lactyl)cysteamine; naringenin;
neotigogenin; o-desmethylangoiensin; oat beta glucan; oleanolic
acid; pantethine; phenylalanine; photoanethone; piperdine;
placental extracts; pratensein; pregnenolone; pregnenolone acetate;
pregnenolone succinate; premarin; quillaic acid; raloxifene; REPAIR
FACTOR 1 and REPAIR FACTOR FCP (both available from Sederna);
retinoates (esters of C2-C20 alcohols); retinyl glucuronate;
retinyl linoleate; S-carboxymethyl cysteine; SEANAMINE FP
(available from Laboratories Serobiologiques); sodium ascorbyl
phosphate; soya extracts; spleen extracts; tachysterol; taurine;
tazarotene; tempol; thymulen; thymus extracts; thyroid hormones;
tigogenin; tocopheryl retinoate; toxifolin; traumatic acid;
tricholine citrate; trifoside; uracil derivatives; ursolic acid;
vitamin D.sub.3 and its analogs; vitamin K; vitex extract; yam
extract; yamogenin; zeatin; and mixtures thereof.
Skin Barrier Repair Actives:
[0034] Skin barrier repair actives are those skin care actives
which can help repair and replenish the natural moisture barrier
function of the epidermis. Nonlimiting examples of skin barrier
repair actives include Alpha Lipid (available from Lucas Meyer);
ascorbic acid; biotin; biotin esters; brassicasterol; caffeine;
campesterol; canola derived sterols; Cennamides (available from
Ennagram); Ceramax (available from Alban Muller); CERAMAX
(available from Quest, located in Ashford, England); CERAMIDE 2 and
CERAMIDE H03.TM. (both available from Sederma); CERAMIDE II
(available from Quest); CERAMIDE III and IIIB (both available from
Cosmoferm, located in Deft, Netherlands); CERAMIDE LS 3773
(available from Laboratories Serobiologiques); CERAMINOL (available
from Inocosm); 20 Cerasol and Cephalip (both available from
Pentapharm); cholesterol; cholesterol hydroxystearate; cholesterol
isostearate; 7 dehydrocholesterol; DERMATEIN BRC and DERMATEIN GSL
(both available from Hormel); ELDEW CL 301 AND ELDEW PS 203 (both
available from Ajinomoto); Fitobroside (available from Pentapharm);
galactocerebrosides; General 122 (available from Henkel); glyceryl
serine amide; hydroxyethyl isostearyl isopropanolamine; lactic
acid; Lactomide (available from Pentapharm); lanolin; lanolin
alcohols; lanosterol; lauric 30 acid N laurylglucamide; lipoic
acid; N-acetyl cysteine; Nacetyl-L-serine; N-methyl-L-Serine; Net
Sterol-ISO (available from Barnet Products); vitamin B3 compounds
(such as niacinamide and nicotinic acid); palmitic acid; panthenol;
panthetine; phosphodiesterase inhibitors; PHYTO/CER (available from
Intergen) phytoglycolipid millet extract (available from Barnet
Products Distributer, located in Englewood, N.J.); PHYTOSPHINGOSINE
(available from Gist Brocades, located in King of Prussia, Pa.);
PSENDOFILAGGRIN (available from Brooks Industries, located in South
Plainfield, N.J.); QUESTAMIDE H (available from Quest); serine;
sigmasterol; sitosterol; soybean derived sterols; sphingosine;
sphingomylinase; S-lactoyl glutathione; stearic acid; Structurine
(available from Silah); SUPER STEROL ESTERS (available from Croda);
thioctic acid; THSC CERAMIDE OIL (available from Campo Research);
trimethyl glycine; tocopheryl nicotinate; vitamin D.sub.3; Y2
(available from Ocean Pharmaceutical); and mixtures thereof.
Non-steroidal Cosmetic Soothing Actives:
[0035] Cosmetic soothing actives can be effective in preventing or
treating inflammation of the skin. The soothing active enhances the
skin appearance benefits of the present invention, e.g., such
agents contribute to a more uniform and acceptable skin tone or
color. The exact amount of anti-inflammatory agent to be used in
the compositions will depend on the particular anti-inflammatory
agent utilized since such agents vary widely in potency.
Nonlimiting examples of cosmetic soothing agents include the
following categories: propionic acid derivatives; acetic acid
derivatives; fenamic acid derivatives; biphenylcarboxylic acid
derivatives; and oxicarns. All of these cosmetic soothing actives
are fully described in U.S. Pat. No. 4,985,459 to Sunshine et al.,
issued Jan. 15, 1991, incorporated by reference herein in its
entirety. Nonlimiting examples of useful cosmetic soothing actives
include acetyl salicylic acid, ibuprofen, naproxen, benoxaprofen,
flurbiprofen, fenoprofen, fenbufen, ketoprofen, indoprofen,
pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen,
tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen,
bucloxic acid, absinthium, acacia, aescin, alder buckthorn extract,
allantoin, aloe, APT (available from Centerchem), arnica,
astragalus, astragalus root extract, azulene, Baicalin SR
(available from Barnet Products Dist.), baikal skullcap, baizhu,
balsam canada, bee pollen, BIOPHYTEX (available from Laboratories
Serobiologiques), bisabolol, black cohosh, black cohosh extract
blue cohosh, blue cohosh extract, boneset, borage, borage oil,
bradykinin antagonists, bromelain, calendula, calendula extract,
Canadian Willowbark Extract (available from Fytokem), candelilla
wax, Cangzhu, canola phytosterols, capsicum, carboxypeptidase,
celery seed, celery stem extract, CENTAURIUM (available from
Sederma), centauryextract, chamazulene, chamomile, chamomile
extract, chaparral, chaste tree, chaste tree extract, chickweed,
chicory root, chicory root extract, chirata, chishao, collodial
oatmeal, comfrey, comfrey extract, CROMOIST CM GLUCAN (available
from Croda), darutoside, dehurian angelica, devil's claw, divalent
metals (such as, magnesium, strontium, and manganese), doggrass,
dogwood, Eashave (available from Pentapharm), eleuthero, ELHIBIN
(available from Pentapharm), ENTELINE 2 (available from Secma),
ephedra, epimedium, esculoside; ethacrynic acid, eyebright, evening
primrose, Extract LE-100 (available from Sino Lion), Fangfeng,
feverfew, ficin, forsythia fruit, Fytosterol 85 (available from
Fytokem), ganoderma, gaoben, Gatuline A (available from
Gattefosse), gentian, germanium extract, gingko bilboa extract,
ginkgo, ginseng extract, goldenseal, gorgonian extract, gotu kola,
grape fruit extract, guaiac wood oil, guggal extract, helenalin
esters, henna, honeysuckle flower, horehound extract,
horsechestnut, horsetail, huzhang, hypericum, ichthyol, immortelle,
ipecac, job's tears, jujube, kola extract, LANACHRYS 28 (available
from Lana Tech), lemon oil, lianqiao, licorice root, ligusticum,
ligustrum, lovage root, luffa, mace, magnolia flower, manjistha
extract, margaspidin, matricin, melatonin, MICROAT IRC (available
from Nurture), mints, mistletoe, Modulene (available from Seporga),
mono or diglucosides of glabridin, mono or diglucosides of
gentisin, MTA (5'-deoxy-5'-methythioadenosine), mung bean extract,
musk, N-methyl arginine, oat beta glucan, oat extract, orange,
panthenol, papain, phenoxyacetic acid, peony bark, peony root,
Phytoplenolin (available from Bio Botanica), phytosphingosine,
Preregen (available from Pentapharm), purslane, QUENCH T (available
from Centerchem), quillaia, red sage, rehmannia, rhubarb, rosemary,
rosmarinic acid, royal jelly, rue, rutin, sandlewood, sanqi,
sarsaparilla, saw palmetto, SENSILINE (available from Silab),
SIEGESBECKIA (available from Sederma), stearyl glycyrrhetinate,
Stimutex (available from Pentapharm), storax, strontium nitrate,
sweet birch oil, sweet woodruff, tagetes, tea extract, thyme
extract, tienchi ginseng, tocopherol, tocopheryl acetate,
triclosan, turmeric, urimei, ursolic acid, white pine bark, witch
hazel xinyi, yarrow, yeast extract, yucca, and mixtures
thereof.
Artificial Tanning Actives and Accelerators.
[0036] Artificial tanning actives can help in simulating a natural
suntan by increasing melanin in the skin or by producing the
appearance of increased melanin in the skin. Nonlimiting examples
of artificial tanning agents and accelerators include
dihydroxyacetaone; tyrosine; tyrosine esters such as ethyl
tyrosinate and glucose tyrosinate; acetyl tyrosine; phospho-DOPA;
brazilin; caffeine; coffee extracts; dihydroxyacetone; DNA
fragments; isobutyl methyl xanthine; methyl xanthine; Phototan
(available from Laboratoires Serobiologiques); prostaglandins; tea
extracts; theophylline; tyrosine; UNIPERTAN P2002 and UNIPERTAN P27
(both available from Unichem); and mixtures thereof.
Skin Lightening Actives:
[0037] Skin lightening actives can actually decrease the amount of
melanin in the skin or provide such an effect by other mechanisms.
Skin lightening actives suitable for use herein are described in
copending patent application Ser. No. 08/479,935, filed on Jun. 7,
1995 in the name of Hillebrand, corresponding to PCT Application
No. U.S. Ser. No. 95/07432, filed Jun. 12, 1995; and copending
patent application Ser. No. 08/390,152, filed on Feb. 24, 1995 in
the names of Kalla L. Kvalnes, Mitchell A. DeLong, Barton J.
Bradbury, Curtis B. Motley, and John D. Carter, corresponding to
PCT Application No. U.S. Ser. No. 95/02809, filed Mar. 1, 1995,
published Sep. 8, 1995; all incorporated herein by reference.
Nonlimiting examples of skin lightening actives useful herein
include adapalene, aloe extract, alpha-glycaryl-L-ascorbic acid,
aminotyroxine, ammonium lactate, anethole derivatives, apple
extract, arbutin, areca catechu L. extract, ascorbic acid, ascorbyl
palmitate, azelaic acid, bamboo extract, bearberry extract,
bletilla tuber, bupleurum falcatum extract, burnet extract, Burnet
Power (available from Barnet Products), butyl hydroxy anisole,
butyl hydroxy toluene, butyl resoreinol, Chuanxiong, cola decaballo
extract, Dang-Gui, deoxyarbutin, 1,3 diphenyl propane derivatives,
2,5 dihydroxybenzoic acid and its derivatives,
2-(4-acetoxyphenyl)-I, 3 dithane, 2-(4-hydroxyphenyl)-I, 3 dithane,
ellagic acid, escinol, estragole derivatives, esculoside,
esculetin, FADEOUT (available from Pentapharm), Fangfeng, fennel
extract, gallic acid and its derivatives, ganodenna extract,
gaoben, GATULINE WHITENING (available from Gattlefosse), genistic
acid and its derivatives, gentisyl alcohol, glabridin and its
derivatives, gluco pyranosyl-l-ascorbate, gluconic acid,
glucosamine, glycolic acid, glycyrrhizinic acid, green tea extract,
4-Hydroxy-5-methyl-3[2H)-furanone, hydroquinine, 4 hydroxyanisole
and its derivatives, 4-hydroxy benzoic acid derivatives,
hydroxycaprylic acid, hyptis extract, inositol ascorbate, kojic
acid, kojic dipalnitate, lactic acid, lemon extract, licorice
extract, Licorice P-TH (available from Barnet Products), linoleic
acid, magnesium ascorbyl phosphate, Melfade (available from
Pentapharm), MELAWHITE (available from Pentapharm), Melanostatine
DM (available from Laboratories Seporga), morus alba extract,
mulberry root extract, niacinamide, 5-octanoyl salicylic acid,
parsley extract, phellinus linteus extract, pinon blanco extract,
pinon negro extract, piri-piri extract, pyrogallol derivatives,
retinoic acid, retinol, retinyl esters (acetate, propionate,
palmitate, linoleate), 2,4 resorcinol derivatives, 3,5 resorcinol
derivatives, rose fruit extract, rucinol, salicylic acid, Song-Yi
extract, Sophora Powder (available from Barnet Products),
4-thioresorein, 5 3,4,5 trihydroxybenzyl derivatives, tranexamic
acid, tyros tat (Rumex Extract available from Fytokem), Tyroslat
10,11 (available from Fytokem), vanilla derivatives, vitamin
D.sub.3 and its analogs, and mixtures thereof.
Sunscreen Actives:
[0038] Also useful herein are sunscreening actives. A wide variety
of sunscreening agents are described in U.S. Pat. No. 5,087,445, to
Haffey et al.about., issued Feb. 11, 1992; U.S. Pat. No. 5,073,372,
to Turner et al., issued Dec. 17, 1991; U.S. Pat. No. 5,073,371, to
Turner et al. issued Dec. 17, 1991; and Segarin, et al., at Chapter
VIII, pages 189 et seq., of Cosmetics Science and Technology, all
of which are incorporated herein by reference in their entirety.
Nonlimiting examples of sunscreens which are useful in the
compositions of the present invention are those selected from the
group consisting of 2-ethylhexyl pmethoxycinnamate, 2-ethylhexyl
N,N-dimethyl-paminobenzoate, p-aminobenzoic acid,
2-phenylbenzimidazole-5-sulfonic acid, octocrylene, oxybenzone,
homomenthyl salicylate, octyl salicylate,
4,4'-methoxy-t-butyldibenzoylmethane, 4-isopropyl dibenzoylmethane,
3-benzylidene camphor, 3-(4-methylbenzylidene} camphor, titanium
dioxide, zinc oxide, silica, iron oxide, and mixtures thereof.
Still other useful sunscreens are those disclosed in U.S. Pat. No.
4,937,370, to Sabatelli, issued Jun. 26, 1990; and U.S. Pat. No.
4,999,186, to Sabatelli et al., issued Mar. 12, 1991; these two
references are incorporated by reference herein in their entirety.
Still other useful sunscreens include aminobenzoic acid (PABA),
benzylidene camphor, butyl methoxy dibenzoyl methane,
diethanolamine p-methoxycinnamate, dioxybenzonet ethyl
dihydroxypropyl (PABA), glyceryl aminobenzoate, homomenthyl
salicylate, isopropyl dibenzoyl methane, lawsone and
dihydroxyacetone, menthyl anthranilate, methyl anthranilate, methyl
benzylidene camphor, octocrylene, octyl dimethyl (PABA), octyl
methoxycinnamate, oxybenzone, 2-phenylbenzimidazole-5-sulfonic
acid, red petrolatum, sulisobenzone, titanium dioxide,
triethanolamine salicylate, zinc oxide, and mixtures thereof.
Examples of these sunscreens include those selected from the group
consisting of 4-N,N-(2-ethylhexyl)methylaminobenzoic acid ester of
2,4-dihydroxybenzophenone, 4-N,N-(2-ethylhexyl)methylaminobenzoic
acid ester with 4-hydroxydibenzoylmethane,
4-N,N-(2-ethylhexyl)-methylaminobenzoic acid ester
hydroxyethoxy)benzophenone, of
2-hydroxy-4-(2-4-N,N-(2-ethylhexyl)-methylaminobenzoic acid ester
of 4-(2-hydroxyethoxy)dibenzoylmethane, and mixtures thereof.
[0039] Exact amounts of sunscreens which can be employed will vary
depending upon the sunscreen chosen and the desired Sun Protection
Factor (SPF) to be achieved. SPF is a commonly used measure of
photoprotection of a sunscreen against erythema. See Federal
Register, Vol. 43, No. 166, pp. 38206-38269, Aug. 25, 1978, which
is incorporated herein by reference in its entirety.
Skin Tightening Agents:
[0040] Also useful as active ingredients in the present invention
are skin tightening agents. Nonlimiting examples of skin tightening
agents which are useful in the compositions of the present
invention are those selected from the group consisting of Biocare
SA (available from Amerchol); egg albumen; Flexan 130 (available
from National Starch); Gatuline Lifting (available from
Gattefosse); Pentacare HP (available from Pentapharm); Vegeseryl
(available from Laboratories Serobioloques) and mixtures
thereof.
Anti-Itch Ingredients:
[0041] Also useful as active ingredients in the present invention
are anti-itch ingredients. Nonlimiting examples of anti-itch
ingredients which are useful in the compositions of the present
invention are those selected from the group consisting of Stimu-tex
(available from Pentapharm); Takanal (available from
Ikeda-Distributer); Ichthyol (available from International
Sourcing-Distributor); Oxygenated Glyceryl Triesters (available
from Seporgia) and mixtures thereof.
Hair Growth Inhibitors:
[0042] Nonlimiting examples of hair growth inhibitors which are
useful in the compositions of the present invention include 17-beta
estradiol, adamantyguanidines, adamantylamidines, adenylosuccinate
synthase inhibitors, anti angiogenic steroids, aspartate
transcarbamylase inhibitors, betamethasone valerate, bisabolol,
copper ions, curcuma extract, cycloxygenase inhibitors, cysteme
pathway inhibitors, dehydroacetic acid, dehydroepiandrosterone,
diopyros leak extract, epidermal growth factor, epigallocatechin,
essential fatty acids, evening primrose oil, gamma glutamyl
transpeptidase inhibitors, ginger oil, glucose metabolism
inhibitors, glutamine metabolism inhibitors, glutathione, green tea
extracts, heparin, Kapilanne (available from International Sourcing
Distributor), L, 5 diaminopentanoic acid, L-aspargine synthase
inhibitors, linoleic acid, lipoxygenase inhibitors, longa extract,
mimosinamine dihydrochloride, mimosine, nitric oxide synthase
inhibitors, non-steroidal antiinflamatories, ornithine
decarboxylase inhibitors, omthine aminotransferase inhibitors,
panthenol, phorhetur, phosphodiesterase inhibitors, pleione
extract, protein kinase C inhibitors, salpha reductase inhibi tors,
sulfhydral reactive compounds, tioxolone, transforming growth
factor beta 1, urea, zinc ions and mixtures thereof.
Desquamating Enzyme Enhancers:
[0043] Nonlimiting examples of desquamating enzyme enhancers which
are useful in the compositions of the present invention include
alanine, aspastic acid, N methyl serine, serine, trimethyl glycine
and mixtures thereof.
Anti-Glycation Agents:
[0044] A nonlimiting example of an anti-glycation agent which is
useful in the compositions of the present invention would be
Amadorine (available from Barnet Products Distributor).
[0045] Other useful actives include skin bleaching (or lightening)
actives including but not limited to hydroquinone, ascorbic acid,
kojic acid and sodium metabisulfite.
[0046] Other useful actives include antiperspirant actives.
Suitable for use herein are those which comprise any compound,
composition or mixture thereof having antiperspirant activity.
Astringent metallic salts are antiperspirant materials for use
herein, for example, the inorganic and organic salts of aluminum,
zirconium and zinc, as well as mixtures thereof. Non-limiting
examples are the aluminum and zirconium salts, such as aluminum
halides, aluminum hydroxy halides, zirconyl oxide halides, zirconyl
hydroxy halides, and mixtures thereof. Additionally, deodorant
actives in the form of bacteriostats may be incorporated into the
present 10 compositions. Suitable deodorant bacteriostats include
2,2'-methylenebis(3,4,6-trichlorophenol), 2,4,4'-trichloro-2'
-hydroxy (diphenyl ether), zinc phenolsulfonate,
2,2'thiobis(4,6-dichlorophenol), p-chloro-m-xylenol,
dichlorom-xylenol and the like. One example is 2,4,4'-trichloro-15
2'-hydroxy(diphenyl ether), which is generically known as triclosan
and available from the Ciba-Geigy Corporation under the trademark,
Irgasan DP-300 Registered.TM.. When triclosan is utilized it will
be present in a range from about 0.05 to about 0.9%, for example,
from about 0.1 to 20 about 0.5% (weight %) of the composition.
Other types of bacteriostats include sodium N-lauroyl sarcosine,
sodium N palmitoyl sarcosine, lauroyl sarcosine, N-myristoyl
glycine, potassium N-lauroyl sarcosine and aluminum chlorhydroxy
lactate (sold by Reheis Chemical Company under trademark of
Chloracel).
[0047] Based on a weight percentage, the active component may be
present in a composition in a range of about 0.0001% to about
60.0%, for example, about 0.005% to about 50% (weight %). In one
embodiment, methyl salicylate, menthol, camphor and capsaicin are
each present in a composition in a range of about 0.0001% to about
60%. For example, methyl salicylate may be present in a range of
about 0.1% to about 40.0% (weight percentage), for example, about
0.5% to about 30%; menthol may be present in a range of about 0.1%
to about 20%, for example, about 0.5% to about 16%; camphor may be
present in range of about 0.1% to about 20%, for example, about
0.5% to about 6%; and capsaicin may be present in a range of about
0.0001% to about 5.0% weight percentage, for example, about 0.002%
to about 0.01%. Some or all of the substances (e.g., analgesic
active(s)) which may be included in a composition may be dissolved
in a silicone material. In one embodiment, some or all of the
substances (e.g., analgesic active(s)) which are included in a
composition are dissolved in one or more low molecular weight
silicones. In another embodiment, one or more of the substances
(e.g., analgesic active(s) which are included in a composition are
dissolved in an organic solvent and then added to the silicone
material. For example, capsaicin may be dissolved in a C12-C15
alkyl benzoate and then added to the silicone material which
comprises a composition. In weight percent, about 3% to about 15%
(weight % of composition), for example, about 7% to about 15% of
alkyl benzoate can be used to dissolve capsaicin.
[0048] Organic compounds useful in the present composition include,
without limitation, inert aromatic hydrocarbons, aliphatic
hydrocarbons, alcohols, aldehydes, ketones, esters, ethers,
glycols, glycol ethers, alkyl halides, or aromatic halides.
Representative of some common organic solvents are alcohols such as
methanol, ethanol, 1-propanol, cyclohexanol, benzyl alcohol,
2-octanol, ethylene glycol, propylene glycol, and glycerol;
aliphatic hydrocarbons such as pentane, cyclohexane, heptane,
VM&P solvent, isoparaffinic solvents and mineral spirits; alkyl
halides such as perchloroethylene, chloroform, carbon ethylchloride
and tetrachloride, chlorobenzene; aromatic hydrocarbons such as
benzene, toluene, ethybenzene and xylene; esters such as ethyl
acetate, isopropyl acetate, ethyl acetoacetate, amyl acetate,
isobutyl isobutyrate, and benzyl acetate; ethers such as ethyl
ether, n-butyl ether, tetrahydrofuran, and 1,4-dioxane; glycol
ethers such as ethylene glycol monomethyl ether, ethylene glycol
monomethyl ether acetate, diethylene glycol monobutyl ether and
propylene glycol monophenyl ether; ketones such as acetone, methyl
ethyl ketone, cyclohexanone, diacetone alcohol, methyl amyl ketone,
and diisobutyl ketone. Low molecular weight silicones useful in the
present invention include volatile silicones. By volatile silicone
it is meant a silicone material that has a measurable vapor
pressure at ambient temperature, for example, silicones with a
boiling point of about 250 degrees C. or less at about atmospheric
pressure and with viscosities generally less than about 10
centistokes (CS) measured at twenty-five degrees C., for example,
0.65 to 5.0 centistokes.
[0049] Low molecular weight cyclic silicones such as
cyclomethicones, for example, octylmethylcyclotetrasiloxane,
hexamethylcyclotrisiloxane and decamethylcyclopentasiloxane and the
like are contemplated for use in the present compositions. Low
molecular weight linear silicones may also be useful, for example,
polydimethylsiloxanes. Particularly useful low molecular weight
silicones include hexamethyldisiloxane and low molecular weight
dimethicone. Mixtures of these and other low molecular weight
silicones are also within the scope of the invention. The
compositions may include low molecular weight silicone in a range
of about 5% to about 95% (weight %), for example, about 30% to
about 80%. In one embodiment, the compositions include about 35% to
about 75% hexamethyldisiloxane and/or low molecular weight
dimethicones. Low molecular weight silicones including
hexamethyldisiloxane and low molecular weight dimethicones are
clear fluids, and are essentially odorless, nontoxic, nongreasy and
nonstinging. These fluids are nonirritating to skin, and exhibit
enhanced spreadability and ease of application to the skin.
[0050] Without wishing to limit the invention to any theory or
mechanism of operation it is believed that after application of a
present composition, the low molecular weight silicones
substantially evaporate leaving behind some or all of the remainder
of the composition which may include a high molecular weight
silicone material. This high molecular weight silicone may have an
average molecular weight in excess of 100,000 (e.g., between about
500,000 and about 5,000,000) and/or be non-volatile. Examples of
silicone polymers contemplated for use in the present compositions
include, without limitation, copolymers such as stearyl
methyl-dimethyl siloxane copolymer (Gransil SR-CYC, available from
Grant Industries, Elmwood Park, N.J.); Polysilicone-11 (i.e., a
crosslinked silicone rubber formed by the reaction of vinyl
terminated silicone and methylhydrodimethyl siloxane in the
presence of cyclomethicone), cetearyl dimethicone/vinyl dimethicone
crosspolymer (i. e., a copolymer of cetearyl dimethicone
crosslinked with vinyl dimethyl polysiloxane), dimethicone/phenyl
vinyl dimethicone crosspolymer (i.e., copolymer of
dimethylpolysiloxane crosslinked with phenyl vinyl
dimethylsiloxane), and dimethicone/vinyl dimethicone crosspolymer
(i.e., copolymer of dimethylpolysiloxane crosslinked with vinyl
dimethylsiloxane>. Particularly useful high molecular weight
silicones include crosslinked siloxane, for example dimethicone
crosspolymers or dimethicone derivative crosspolymers and silicone
gums, for example, dimethicone elastomer gum.
[0051] In one particularly useful aspect of the present invention,
the consistency of a composition is controlled by adding certain
amounts of high molecular weight silicone polymers to the low
molecular weight silicones. The viscosity range of the final
compositions may be adjusted to about 0.1 CS to about 50,000 CS or
about 10,000,000, for example, about 0.1 CS to about 3500 CS or
about 0.5 CS to about 50 CS. One useful viscosity range for the
present compositions may be about 0.65 CS to about 10 CS.
[0052] In one particularly useful embodiment, a dimethicone
crosspolymer is employed in a composition and is effective to
control the consistency of compositions. In another particularly
useful embodiment, dimethicone gum is employed in a composition and
is effective to control the consistency of compositions. In another
particularly useful embodiment, dimethicone crosspolymers and/or
dimethicone gum are employed in a composition and are effective to
control the consistency of compositions. The viscosity of the
crosspolymer employed may be about 1,000,000 or higher.
[0053] Advantageously, dimethicone crosspolymers and dimethicone
gum do not have a greasy feel. In addition, these compositions can
provide a water resistant or water proof film when applied to a
surface, for example, when applied to the skin. This water
resistance or water proofing can prevent an undesired removal of
actives upon exposure to moisture. The film can also provide for
moisture retention. The moisture retention may be effective to
retain actives, for example, volatile actives, in proximity to the
surface to which the composition is applied, for example, the
skin.
[0054] The range of molecular weight of high molecular weight
silicones, for example, dimethicone crosspolymers and dimethicone
gum may be from about 100,000 to about 100,000,000, for example,
about 500,000 to about 50,000,000 or about 1,000,000 to about
10,000,000.
[0055] The high molecular weight silicones, for example,
dimethicone crosspolymers and dimethicone gum may be capped. Caps
may be any suitable group including methyl groups, phenyl groups,
hydroxy groups, vinyls and/or amino groups or mixtures or
combinations thereof.
[0056] The compositions may include high molecular weight silicone
in a range of about 5% to about 95% (weight %), for example, about
3% to about 30%. For example, a composition may include dimethicone
crosspolymer and or dimethicone gum in a range of about 5% to about
25%.
[0057] A silicone component includes the silicone material which
comprises a composition of the invention. In one broad embodiment,
a composition of the invention includes a silicone component, which
includes low molecular weight silicones and high molecular weight
silicones present at a concentration in a range of between about
30% to about 99.999% (weight %), for example, about 40-99.9%.
[0058] In one embodiment, one or more of substances (e.g.,
analgesic active (s>> which are included in a composition of
the invention are dissolved into the silicone component.
[0059] In certain embodiments, the present compositions can include
additional substances including, without limitation, moisturizers,
emollients, fragrances preservatives and sugars.
[0060] The compositions of the present invention can include one or
more moisturizing materials. These materials include, but are not
limited to, urea; guanidine; glycolic acid and glycolate salts (e.
g. ammonium and quaternary alkyl ammonium); lactic acid and lactate
salts (e. g. ammonium and quaternary alkyl ammonium); aloe vera in
any of its variety of forms (e.g., aloe vera gel); polyhydroxy
alcohols such as sorbitol, glycerol, hexanetriol, propylene glycol,
butylene glycol, hexylene glycol and the like; polyethylene
glycols; sugars and starches; sugar and starch derivatives (e.g.,
alkoxylated glucose); hyaluronic acid; lactamide monoethanolamine;
acetamide monoethanolamine: and mixtures thereof.
[0061] The compositions useful the present invention may also
include one or more emollients. Examples of suitable emollients
which may be useful in the present compositions include, but are
not limited to, highly branched hydrocarbons, and non-polar
carboxylic acid and alcohol esters, and mixtures thereof. Some
emollients that may be useful in the present compositions are
further described in U.S. Pat. No. 4,919,934, which is incorporated
herein by reference in its entirety.
[0062] Examples of fragrances which may be useful in the present
compositions include, without limitation, peppermint, rose oil,
rose water, aloe vera, clove oil, eucalyptus oil, and other plant
extracts. Certain fragrances may require a solubilizer, e.g.,
PPG-5-ceteareth-20. To eliminate certain odors from compositions,
masking agents may be used. An example of a masking agent includes
ethylene brassylate. Other fragrances and masking agents are listed
on pages 1639-40 of the ICT Handbook.
[0063] Preservatives can be used to protect the compositions from
degradation. Examples of preservatives which may be useful in the
present compositions include, without limitation, liquipar oil,
phenoxyethanol, methyl paraben, propyl paraben, butyl paraben,
isopropyl paraben, isobutyl paraben, dieizolidinyl urea,
imidazolidinyl urea, diazolindyl urea, benzalkonium chloride,
benzethonium chloride, phenol, and mixtures thereof (e. g.,
liquipar oil). Other preservatives are listed on pages 1654-55 of
the ICT Handbook.
[0064] Examples of sugars which may be useful in the present
compositions include, without limitation, monosaccharides,
disaccharides, and polysccharides such as glucose, xylose,
fructose, reose, ribose, pentose, arabinose, allose, tallose,
altrose, mannqse, galactose, lactose, sucrose, erythrose, or any
combination thereof.
[0065] The compositions of the present invention are used in
conventional ways to provide a desired benefit. The present
compositions can be used to provide, for example, pain relief
(analgesic) by, for example, topical application to the skin.
Methods of use depend upon the type of composition employed but, in
one broad embodiment, involve application of an effective amount of
the product to the skin which may then be allowed to remain on the
skin. By "effective amount" is meant an amount sufficient to
provide a benefit desired. For example, an effective amount of a
composition is applied to and rubbed onto the skin.
[0066] Compositions of the invention may be substantially anhydrous
allowing for application to the skin with no greasy feel. The
compositions dry rapidly leaving behind a silicone polymer film
with no oily residue that prevents evaporation or washing away of
actives thereby retaining the active component in proximity to the
surface of the skin to which the composition is applied.
[0067] The following non-limiting examples illustrate certain
aspects of the present invention.
EXAMPLES
[0068] Percentages presented in the examples are weight
percentages. A weight percentage is a percentage expressed as the
percentage of the total composition based on weight.
Example 1
TABLE-US-00001 [0069] Methyl salicylate 30.0% Menthol 10.0% Camphor
4.0% Low molecular weight dimethicone 45.0% Dimethicone
crosspolymer 11.0%
[0070] The methyl salicylate, menthol and camphor are dissolved in
the low molecular weight dimethicone producing an admixture and the
dimethicone crosspolymer is blended into the admixture.
Example 2
TABLE-US-00002 [0071] Methyl salicylate 15.0% Menthol 7.5% Camphor
2.5% Hexamethyldisiloxane 61.0% Dimethicone crosspolymer 14.0%
[0072] The methyl salicylate, camphor and/or menthol are dissolved
in the hexamethyldisiloxane producing an admixture and the
dimethicone crosspolymer is blended into the admixture.
Example 3
TABLE-US-00003 [0073] Methyl salicylate 5.0% Menthol 1.0% Camphor
2.0% Capsaicin 0.075% C12-C15 alkyl benzoate 16.925%
Hexamethyldisiloxane 61.0% Dimethicone crosspolymer 14.0%
[0074] The capsaicin is dissolved in the alkyl benzoate and the
methyl salicylate, menthol and camphor are dissolved in the
hexamethyldisiloxane to which the capsaicin/alkyl benzoate solution
is added producing an admixture. The dimethicone crosspolymer is
blended into the admixture.
Example 4
TABLE-US-00004 [0075] Capsaican 0.1% C12-C15 alkyl benzoate 15.9%
Low molecular weight dimethicone 70.0% Dimethicone crosspolymer
14.0%
[0076] The capsaicin is dissolved in the alkyl benzoate. The
capsaicin/alkyl benzoate solution and the methyl salicylate,
menthol and camphor are added to the low molecular weight
dimethicone producing an admixture and the dimethicone crosspolymer
is blended into the admixture.
Example 5
TABLE-US-00005 [0077] Methyl salicylate 30.0% Menthol 10.0% Camphor
4.0% Low molecular weight dimethicone 45.0% Dimethicone elastomer
gum 11.0%
[0078] The methyl salicylate, menthol and camphor are dissolved in
the low molecular weight dimethicone producing an admixture and the
dimethicone elastomer gum is blended into the admixture.
Example 6
TABLE-US-00006 [0079] Methyl salicylate 15.0% Menthol 7.5% Camphor
2.5% Hexamethyldisiloxane 61.0% Dimethicone elastomer gum 14.0%
[0080] The methyl salicylate, menthol and camphor are dissolved in
the hexamethyldisiloxane producing an admixture and the dimethicone
elastomer gum is blended into the admixture.
Example 7
TABLE-US-00007 [0081] Methyl salicylate 5.0% Menthol 1.0% Camphor
2.0% Capsaicin 0.075% C12-C15 alkyl benzoate 16.925%
Hexamethyldisiloxane 61.0% Dimethicone elastomer gum 14.0%
[0082] The capsaicin is dissolved in the alkyl benzoate and the
methyl salicylate, menthol and camphor are dissolved in the
hexamethyldisiloxane to which the capsaicin/alkyl benzoate solution
is added producing an admixture. The dimethicone elastomer gum is
blended into the admixture.
Example 8
TABLE-US-00008 [0083] Capsaican 0.1% C12-C15 alkyl benzoate 15.9%
Low molecular weight dimethicone 70.0% Dimethicone elastomer gum
14.0%
[0084] The capsaicin is dissolved in the alkyl benzoate which is
then added to the low molecular weight dimethicone producing an
admixture. The dimethicone elastomer gum is blended into the
admixture.
Example 9
TABLE-US-00009 [0085] Methyl salicylate 30.0% Menthol 10.0% Camphor
4.0% Low molecular weight dimethicone 45.0% Dimethicone
crosspolymer 6.0% Dimethicone elastomer gum 5.0%
[0086] The methyl salicylate, menthol and camphor are dissolved in
the low molecular weight dimethicone producing an admixture and the
dimethicone elastomer gum and dimethicone crosspolymer are blended
into the admixture.
Example 10
TABLE-US-00010 [0087] Methyl salicylate 15.0% Menthol 7.5% Camphor
2.5% Hexamethyldisiloxane 61.0% Dimethicone crosspolymer 7.0%
Dimethicone elastomer gum 7.0%
[0088] The methyl salicylate, menthol and camphor are dissolved in
the hexamethyldisiloxane producing an admixture and the dimethicone
elastomer gum and dimethicone crosspolymer are blended into the
admixture.
Example 11
TABLE-US-00011 [0089] Methyl salicylate 5.0% Menthol 1.0% Camphor
2.0% Capsaicin 0.075% C12-C15 alkyl benzoate 16.925%
Hexamethyldisiloxane 61.0% Dimethicone crosspolymer 7.0%
Dimethicone elastomer gum 7.0%
[0090] The capsaicin is dissolved in the alkyl benzoate and the
methyl salicylate, menthol and camphor are dissolved in the
hexamethyldisiloxane to which the capsaicin/alkyl benzoate solution
is added producing an admixture. The Dimethicone crosspolymer and
dimethicone elastomer gum are blended into the admixture.
Example 12
TABLE-US-00012 [0091] Capsaican 0.1% C12-C15 alkyl benzoate 15.9%
Low molecular weight dimethicone 70.0% Dimethicone crosspolymer
7.0% Dimethicone elastomer gum 7.0%
[0092] The capsaicin is dissolved in the alkyl benzoate and is
added to the low molecular weight dimethicone producing an
admixture. The dimethicone crosspolymer and dimethicone elastomer
gum are blended into the admixture.
Example 13
TABLE-US-00013 [0093] Retinol-15D (a 15% solution of all 0.3% trans
retinol in caprylic/capric triglyceride, stabilized with 1% BHT)
Low molecular weight dimethicone 80.0% Dimethicone crosspolymer
19.7%
[0094] The Retinol-15D is dissolved in the low molecular weight
dimethicone, producing an admixture, and the dimethicone
crosspolymer is blended into the admixture using the cold mix
process. The resulting composition is packaged in opaque high
density polyethylene (HDPE) containers during the production
processing and packaging. No inert gas is used. The compositions in
these containers are tested and found to have no retinol
degradation.
[0095] The containers are resealed and are then exposed to sunlight
and probable higher than normal (room) temperatures, and retested
after three months. After three months of such exposure, the
compositions in the opaque containers are found to be optically
clear, and to contain active retinol.
[0096] Similar tests are conducted except that the compositions are
placed in clear polyethylene terephthalate (PET) containers and
clear glass containers. Again, no inert gas is used during
packaging. Upon retesting, after three months of exposure to
sunlight and higher than normal temperatures, the compositions in
the PET and glass containers are hazy and contain no active
retinol.
Example 14
TABLE-US-00014 [0097] Retinol 15D (a 15% solution of all trans 0.3%
retinol in caprylic/capric triglyceride, stabilized with 1% BHT)
Low molecular weight dimethicone 80.0% Dimethicone gum 19.7%
[0098] The Retinol-15D is dissolved in the low molecular weight
dimethicone, producing an admixture, and the dimethicone gum is
blended into the admixture using the cold mix process. The
resulting composition is packaged in opaque high density
polyethylene (HDPE) containers under the same conditions as Example
13. After testing, the compositions in these containers are found
to have no retinol degradation.
[0099] The containers are resealed and are then exposed to sunlight
and probable higher than normal (room) temperatures, and retested
after three months. After three months of such exposure, the
compositions in the opaque containers are found to be optically
clear, and to contain active retinol.
[0100] Similar tests are conducted except that the compositions are
placed in clear polyethylene terephthalate (PET) containers and
clear glass containers. Again, no inert gas is used during
packaging. Upon retesting, after three months of exposure to
sunlight and higher than normal temperatures, the compositions in
the PET and glass containers are hazy and contain no active
retinol.
[0101] These tests, as set forth in Exhibits 13 and 14, show that
the present compositions, prepared by the cold mix process without
the use of inert gases, are stable when exposed to oxygen and
higher than normal temperatures, but unstable when exposed to
light. Accordingly, such compositions preferably are to be packaged
in opaque containers.
[0102] A number of publications, patents, and patent applications
have been cited hereinabove. Each of the cited publications,
patents, and patent applications are hereby incorporated by
reference in their entireties.
[0103] While this invention has been described with respect to
various specific examples and embodiments, it is to be understood
that the invention is not limited thereto and that it can be
variously practiced with the scope of the following claims.
* * * * *