Note : Les descriptions sont présentées dans la langue officielle dans laquelle elles ont été soumises.
BACXGROUND OF THE INVENTION:
a) field of_the invention
The present invention relates to a topical
composition for th~ protection, care and treatment of the
human skin andfor hairO
b) technical back~round
It is well known that newborn babies have a very
soft and good looking skin. This is usually attributed to
the protective properties of a natural eoating called
~vernix caseosa>~ that covers the ~oetuses during the last
weeks of pregnancy. It is also known from gas chromatograms
made on vernix collected ~rom pre-term (37 weeks) infants
that the natural vernix is made of squalene, cholesterol,
monoesters waxes, cholesteryl esters, tryglyceri~es and few
other unidentified substances. (See S.J. Wysocki et al.
~IPIDS IN FOREHEAD VERNIX FROM NEWBORN INFANTS, Biol.
Nenonate 39: 300-304 (1981)).
SUMM~RY OF THE INVENT~ON:
An object of the present invention is to provide
a topical, synthetic composition for use in protectin~,
curing and/or treating the human skin and/or the human hair,
which composition contains, as active ingredlents~ most of
~he~ major lngreclients Eound in the natural vernix caseosa.
Another obj(-~c~ oE the invention is to provide a
cornposition which, in use, has very good moisturizing pro
perties in addition of being effec~ive agains-t skin diseases
such as eczema, atopic dermatitis, serborrheic dermatitis,
ammoniacal dermatitisl sun erythema, pruritus (especially
old person pruritus), psoriasis and dyshidrosis.
In accordance with the invention, these objects
are achieved with a topical composition for the protection,
care and treatment of h~nan skin or hair, which composition
compriseso
- from 1 to 50% by weight of triacylglycerols
w 1 --
`J~f~5~ 7
wherein the acyl portions are identical or different and
represent a caprylyl radical or a capryl radical;
- from 0.8 to 40% by weight of lanolin alcohol
~preferably solubili~ed in a solvent such as a mineral oil);
- from l to 50% by weight of squalene; and
- from O to 97,2% by weight of one or more
cosmetically or pharmaceutically ~cceptable carrier. To
the above-mentioned basic formulation may ~e added one or
more pharmaceutical or cosmetical additives.
The topical composition according to the invention
may have difEerent formulations depending on its expected
use. By way of example, it ~ay be formulated as a body
moisturizing lotion ~milk), as an oily gel for massage, as
a cream (such as a night cream3, as an ointment, as a l.ip-
stick~ as a hair preparation (such as a hair conditioner)
or as an oil (such as a bath oil, an anti-weals and/or anti-
wrinkle oil). Preferably, however, the topical composition
will be formulated as a cre~m ~r an oil.
When the composition is formulated as an oil, it
preferably contains from l to 50% by weight of triacyl-
ylycerol 5 whexein the acyl portions are identlcal or diff0rent
and repre~ent a caprylyl rad.ical or a capryl radical; from
0.8 to 40% by welght of lanol:Ln alcohol solubillzed in a
tsufficlent amount of an acc~ptable ~olvent; and from 1 to
50% by w~ight of ~.qualene.
When the composition is formulated as a creamr it
preferably contains from 1 to 16~ by weight of triacyl-
glycerols wherein the acyl portions are identical or
different and represent a caprylyl radical or a capryl
radicall from 0.8~ to 12.8~ by weight of lanolin alcohol or
0.8 to 12.8% by weight of lanolin alcohol solubilized in a
mineral oil (advantageousl~ l to 16~ by weight of a mixture
consisting of 80% by weiyht of lanolin alcohol and of 20%
by weight of mineral oil3, and from l to 16% by weight of
sclualene,in admix-ture with a suEEicient cluantity oE a
cosmetical or pharmaceutical carxier. In this par-ticular
case, the total amoun-t o~ txiacylglycerols, oE lanolin
alcohol and oE squalene must be egal -to or lower than 17.8%
by weigh-t of the entire composition -to allow proper emulsion
oE the oily phase wi-th the aqueous phase.
The above n~-rrtioned triacylglycerols IPreferabt.y-those sold
uncter-~e-trade mark ~YRI~OL 318 and commonl~ called caprilic/capric
trig]ycerides)have been specifically selec-ted by t,he Applicants in the
basic formulation of tneir composition because:
- they are esters oE saturated Eatty acids,
thereby avoiding the .risk oE oxidation;
- they are very dermophilic;
- they are very good solvent and are compa-tible
with all the o-ther ingredients of -the composi-
tion; and
- -they have an-ti:Eungal proper-ties, especially
against trichophyton~ and candida strains.
Lanol:Ln alcohol has been selected by the
Appl:icants because o:E i-ts excellent emoll.ient propert~eC;.
~5 :Lanol:ln alco11ol, use can be macle oE tlle substance solcl
1lnder tt~e tr,~ade Irlr-l:rk ~i~EI~CE10t, [~-10 L, wtni.ch substance
CO11;:i.StS oF an o:l:1.y m:i.xture oE 80~ by weight oE lanol.in
a:Lco1lo:i. with 20~. by weight o~ a mlneral oii
Squalene tpreEerably the one sold under the -trade
mark SUPRAENE) has been selected by the Applicants because
lt is a bactericide and it shows a very high aEEinity for
the skin.
Tests conducted by the Applicants have surpris-
i.nyly shown that the above-mentioned combination oE tri-
acylglycerols wi-th lanolin alcohol and squalene, wi-th
even-tually one or more cosmetical or pharmaceu-tical addi-
-tives has subs-tantially -the same hiyh mois-turizing and
protec-tive properties as -the natural vernix caseosa, in
~'~53~V17
addition of having a remarkable efficiency against ~kin
diseases such as eczema, atopic dermatitis, seborrheic
dermatitis, ammoniacal dermatitis, sun erythema, pruritus
(especially old person pruritus), psoriasis and dyshidrosis.
As cosmetical vr pharmaceutical additive or
carrier use can advantageou~ly be made of water or of
mineral oil ~preferably the heavy mineral oil sold under
the trade mark RAMOL 350).
As all of the triacylglycerols, squalene and
mixture of lanolin alcohol and mineral oil are oilsl they
may be mixed together to define an oil composition without
further association with a carrier~
As possible additives to the composition accord-
ing to the invention, use can be made of one or more com-
pounds selected from the following, non restrictive list:
- anti-oxydant agents
- coloring or dying agents
- emulsifying agents ~such as cholesterol,
magnesium aluminum silicate, polyoxyethylene lauryl ether,
polyoxyethylene ~onostearate, polyoxyethylene sorbitan
monolaurate, propylene glycol monostearate, sodium borate
plus fatty acid, ~odium lauryl sulfate~ sorbitan mono-
palm:i.tate or triethanolami.ne plus fatty acid, and more
particwlarly isopropyl myristate or the emulsiying wax
sold under the txade mark POL~WAX NF)
- perfuming agents (such as 4828-D : fleur
arôme)
- preservative agents ~such as cresol, propyl-
paraben, methylparaben or sorbic acid)
- Imiourea U.S.P. (sold under the trade mark
GERMAL 115)
~ stabilizing or thickening agents ~such as
carbomer, cetyl alcohol~ glyceryl monostearate, methyl-
cellulose, spermaceti or stearyl alcohol)
-- 4 --
~ 7
- tensio~active agents ~such as cholesterol).
Depending ~n its proposed used, the composition
invention may also contain other active agents ~uch as:
- sun screen agents (such as octyl dimethyl
p-amino benzoic acid)
- ci.catrizing agents ~uch as a~lantoin)
- anesthe~ic agents (Such as benzocaine)
- antibiotic agents ~such as NEOSPORIN (trade
mark) or neomycin)
- costicosteroid agents (such as hydrocortisone~
- antifungal agents
- antiseptic agent
- keratolytic agents ~such as salicylic acid)
- emollients (such as cholesterol)
- occlusive emollients (such as the heavy mineral
oil sold under the trade mark R~MOL-350).
When use is made o such additives, their amounts
in the composition will be selected so th2t the composition
contain l~ss than 8~ by weight (preferably 2 to 4~ of octyl
dimethyl para amino benzoic acid; frQm 0.1 to 0.2~ by we.ight
of all~ntoin; ox ~buut 0.5~ by weight of hydrocortisone.
Of course, the use o.E one or more of the above-
mentionf~d other act.ive agents makes the composition usefu.l
as sun ~creen, cicatrl~in~, antibiotic, corti.costeroid,
antifungal, antiseptic, anesthesic and/or keratolytic com-
position.
The following non-restrictive examples will
illustrate preferred embodiments of the present invention.
E _ 1 - OIL coMro~ oN
An oil composition having the following formula-
tion was prepared:
1~ 53~07
Weight
with
Weight in respect
INGREDIENTS gramsto weight
composi-
tion
Heavy mineral oil (RAMOL 350).......... 698.5 gr 69.85 %
Emulsifying agent lisopropyl
myristate)............................. 100 gr 10.0 %
Squalene (SUPRAENE).................... 50 gr 5.0 %
Triacylglycerols ~MYRITOL 318)......... 100 gr 10.0
Lanolin alcohol (~MERCHOL L-101)....... 50 gr 5.0 %
Preservative agent (Propylparaben)..... 1.5 gr 0.15 %
_
1000.0 gr 100.0 %
The above-mentioned oil composition was prepared
by dissolving propylparaben in a part o~ the 698.5 yr oE
RAMOL 350. EleatincJ was ound necessary to d:Lssolv~3 propyl-
paraben :i.n R~MOL 350. rl'he remr~:Lning par-t oE the 698.5 cJr
oE RAMOr, 350 wa,L, subse~uerlt:ly added to the part contalniny
the propyLparaben, together wi.th the SUPRAENE, MYRITOL 318
ancl AME'RCflOL L-:101. These inyredien-ts were mixed and then
isopropyl myris-tate was added to the mixture. The result-
ing mix-ture was well mixed until it appeared limpid.
EXAMPLE 2 - CREAM COMPOSITION
A cream composition having the following formula-
tion was prepared:
* caprilic/capric triglycerides sold under -the -trademark
~o~3~ ~
Weight %
with
INGREDIENTS Weight in respec-t
yrams -to -the
weiyh-t
composi-
tion
Squalene ~SUPRAENE)~ ....50 gr5.0 %
Triacylglycerols (MYRITOL 318)........... 30 gr 3.0 %
Lanolin alcohol IAMERCHOL L-lOlJ......... 30 gr 3.0 %
Emulsifying agent (POLAWAX NF)........... 80 gr 8.0 %
Stabilizing agent (Cetyl alcohol)........ 10 gr 1.0 %
Tensio-active agent (ChoLesterol)........ 1 gr 0.1 %
Preservative agent (Propylparaben)....... 1 gr 0.1 %
Preservative agent (Methylparaben)....... 2 gr 0.2 %
Imiourea U.S.P. (GERMALL 115)............ 4 gr 0.4 %
Glycerin................................. 80 gr 8.0 ~
~828 ~ Perfume (f:Leur arôme)............ :L gr 0.1 ~,
Water~ 711 gr 71.1 ~
1000 gr 100.0 %
~
The above-mentioned cream composition was
prepared by heating a first mixture of 80 gr of POLAWAX NF,
50 gr of SUP~AENE~ 30 gr oE MYRI~OL 318, 10 gr of cetyl
alcohol, 1 gr of cholesterol, 30 gr of AMERCHOL L~101 and
1 gr of propylparaben a-t 75C. Then, a second mixture of
711 gr of wa-ter, 2 gr of me-thylparaben, 4 gr of GERMALL 115
and 80 gr oE glycerin was prepared ancl heated at 75C. The
first mixture was poured in the second one under s-trong
* caprilic/capric triqlycerides sold under the -trademark
-- 7 --
;~2~:i3~
stirring for about 20 minutes. The resulting mixture was
cooled to 55-60~C and 1 gr of 4828-D Perf~me (fleur arome)
was added thereto. The so perfumed mixture was stirred and
cooled to 30C. The cream was set to its final viscosity
after 48 hours~
EXAMPLE 3 - PHARMACOLVGIC~ ~ESULT
Patients suffering of ecæema, atopic dermatitis
and seborrheic dermatitis were treated with the cream
composition of example 2 for several weeks. This composi-
tion was used as unique therapeutic agent, and led to aclear improvement in khe healing of th~ cutaneous
troubles of most of the patients. In particular, this com-
position has substantially xeduc~d the necessity of using
medicine containing steroids for the treatment of the
L5 aforesaid pathologies. The composition has also shown good
moisturizing property.
EXAMPLE 4 - PHARMACOLOGICAL RESULT
Several persons haviny been subjected to a face-
lift some months ear~ier, were requested to use regularly
the cream composition ~f example 2, and then been repetedly
exposed to solar rays. The cream composition avoided
wrinkling o the skin as is usually noted ~n such cases.
Ii'urthcrmore, the cre~m composLtlon of example 2 allowed
fa5tQr heallng of dermabra~ions and provided skin moisturiz-
ing of better quality.
