Note: Descriptions are shown in the official language in which they were submitted.
~~~~1~~;"~~
BATH AND SHOWER COMPOSITION HAVING VESICLE-FORMING
PROPERTIES AND METHOD FOR THE PRODUCTION AND USE THEREOF
Field of Invention: Bath and shower additives, e.g., bath
ails and the like.
The present invention relates to new oily bath and
shower additives comprising a combination of a fatty oil or
other fatty apolar substance, an oil-soluble surfactant, a
vesicle-forming lipid, and other active ingredients as
desired or required. When poured and/or admixed into water
to produce the bath or shower water, liquid, or liquor,
these compositions spontaneously form dispersed vesicles or
liposomes. They are especially suitable for use as or in
the production of long-acting, depot, or extended-action
additives for full, partial, and Shower baths.
By the term "vesicle", as used herein, is intended a
small bladder or enclosed membrane filled with fluid, for
all intents and purposes being equivalent to a liposome, as
is well understood by one skilled in the art, vesicles or
liposomes being generally globular units consisting of
concentric bi-layers which may be, depending upon the size
and number of possibly superposed bi-layers, unilamellar,
oligolamellar, or multilamellar by nature, and which in the
present case are probably what are commonly known as
"reverse micelles", having exterior bilayers of lipidic or
other apolar material, capable of solubilizing water and
1 MERZ 21/dlk
2~~~~.a'~
any contained cosmetically-active ingredient in the polar
center thereof.
Backcxround of the Invention and Prior Art
For balneological (viz., the therapeutic use of baths)
and/or sanitary or cosmetic purposes, various formulations
containing surfactants are commonly employed. These
contain, for example, surfactants which are miscible with
or dispersible in water and, :if required, perfumes and
additional active ingredients such as essential oils,
herbal extracts, vitamins, and the like. Such preparations
are based essentially on ionic or non-ionic surfactants and
the above-mentioned active ingredients, which - after being
added to water-ensure a uniform dispersion of the compo-
nents. The preparations are either clear or exhibit a more
or less pronounced opalescence. The bath liquor embodying
such preparations is usually clear or slightly turbid.
In addition to such products, oily balneological,
sanitary, and/or cosmetic preparations are known. These
products are distinguished from the foregoing preparations
by the relatively high percentage of fatty oils or other
lipophilic liquids contained therein in addition to the
tenside, i.e., the surface-active agent. In contrast to
essentially oil-free products, these oily preparations
produce turbid bath waters, liquids, or liquors in which
the lipophilic constituents are at first dispersed rela-
tively uniformly. After ten to thirty minutes, there is an
increased flotation to the surface. Extent and rate of this
so-called "creaming" process depend inter alia upon various
factors such as type and quantity of the contained surfac-
tant and/or dispersion agent, type and quantity of the
lipophilic agent, and water temperature.
2 MERZ 21/dlk
~~ i.~_~~rl
In addition to the aforementioned products, there are
also balneological preparations containing only a fatty oil
- if required or desired in addition to other oily compo-
nents - and possibly other acaive ingredients such as
essential oils. Inasmuch as these products, after being
added to the water, develop unsatisfactory dispersibility
of the lipophilic constituents, forming a more or less
uniform layer thereof on the bath liquor surface in the
absence of surfactant, they are relatively unsuited for
balneological applications. To achieve a satisfactory
balneological and/or cosmetic effect, dispersion agents or
surfactants are required for dispersing the oils in the
bath water. This ensures deposit of a uniform dispersion of
the oil phase on the skin surface. Moreover, in addition,
penetration of the active ingredients contained in the
preparation into the deeper skin layers should preferably
be enhanced to achieve a potentiation of their effect.
However, due to an absence of vesicular properties in such
prior art compositions, this has so far not been possible
with known formulations.
OBJECTS OF THE INVENTION
.fin objective of the present invention, therefore, is
to provide a balneological or cosmetic bath additive which
- when used for bathing or showering - provides and
releases vesicles without the necessity of expensive
procedures for their production. In consequence, the
additive of the invention has not only a surface-active
effect, but also sets free the incorporated ingredients and
components in a sustained release form, i.e., in the form
of vesicles, thereby considerably improving the duration of
the balneological or cosmetic effect. Other objects of the
3 MERZ 21/dlk
invention will become apparent hereinafter, and still
others will be obvious to one skilled in the art.
SUMMARY OF THE INVENTION
The invention, then, comprises the following, inter
alia, singly or in combination:
a balneological or cosmetic. composition suitable as an
additive for use in bathing or showering, having vesicle-
forming properties, consisting essentially of a fatty oil
and/or a fatty or waxy apolar substance, one or more oil-
soluble surfactants, an optional cosmetically-active
ingredient, and one or more vesicle-forming lipids; such a
composition containing 20% to 90% fatty oil and/or
apolar substance, 2% to 50% oil-soluble surfactant, and
0.1% to 20% vesicle-forming lipid, all by weight of total
composition; such a
composition wherein the percentage of fatty oil and/or
apolar substance is 50% to 70%, the percentage of oil
soluble surfactant is 5% to 35%, and the percentage of
vesicle-forming lipid is 0.5% to 5%, all by weight of total
composition; such a
composition wherein the percentage of oil-soluble
surfactant is 10% to 20% by weight; such a
composition wherein the fatty oil or apolar substance
is selected from the group consisting of peanut, sesame,
sunflower, wheat germ, soy, jojoba, castor, almond, mink,
and olive oils and mixtures thereof as fatty oil, and
paraffin oil, isopropyl myristate, isopropyl palmitate,
medium-chain triglycerides, isooctyl stearate, capryl/
capric acid triglycerides, cetyl palmitate, and mixtures
thereof as apolar substance; such a
4 MERZ 21/dlk
composition wherein the oil-soluble surfactant is an
oil-soluble, water-dispersible tenside having an HLB
value
of 6 to 13; such a
composition wherein the HL~B value is 7 to 10; such
a
composition wherein the oil-soluble surfactant is
selected from the group consisting of polyoxyethylene
lauryl ether having 1 to 4 EO units, polyoxyethylene(5)-
oleyl ether, pol~oxyethylene(7)glyceryl cocoate, cocoa
fatty acid diethanolamide, ethanolamide, mono or di
or tri
(alkyl tetraglycol ether)-ortho-phosphoric acid esters,
polyoxyethylene glycerol trioleate, polyoxyethylene
sorbitan tristearate, polyoxypropylene(15)-stearyl ether,
and mixtures thereof; such a
composition wherein the vesicle-forming lipid is
selected from the group consisting of a lower polyoxyethy-
lated fatty alcohol having an HLB value between 2 and
6 and
a phospholipid; Such a
composition wherein the fatty alcohol is a higher
polyoxyethylated fatty alcohol having 1 to 4 ethylene
oxide
units, and the phospholipid is lecithin, phosphatidylcho-
line, -serine, or -diethanolamine, or a mixture thereof;
such a . .
composition wherein the polyoxyethylated fatty alcohol
is based upon a C16-C18 alcohol; such a
composition containing up to about 30~ of cosmetical-
ly-active ingredient; such a
composition containing 5 to 15~ active ingredient;
such a
composition wherein the active ingredient is selected
from the group consisting of essential oils, herbal
extracts, and vitamins; such a
composition additionally containing up to about 10~
thickener; such a
5 MERZ 21/dlk
2~~~.~.u'~
composition wherein the thickener is selected from
aerosil and aluminum or magnesium stearate; such a
composition incorporated into a conventional bath or
shower formulation; and such a
composition wherein the oi:1 and/or apolar component
is
selected from the group consisting of soya oil, paraffin
oil, isopropyl myristate, jojoba oil, isopropyl palmitate,
capric acid triglyceride, and mixtures thereof, wherein
the
oil-soluble surfactant is selected from the group consist-
ing of alkyl tetraglycol ethers, polyoxyethylene(7)glycerol
cocoate and coconut oil diethanolamide, and wherein
the
vesicle-forming lipid is lecithin.
Moreover, a method for the production of a bath or
shower additive composition, wherein 20o to 90~ fatty
oil
and/or fatty or waxy apolar substance, 0$ to 30o cosmetic-
ally-active ingredient, 2$ to 50~ of one or more oil-
soluble surfactants, and 0.1% to 20~ of one or more
vesicle-forming lipids, are admixed together at a tempera-
ture between about 20C. and 70C; such a
method wherein the amount of fatty oil and/or apolar
component is 50~ t~ 70a, the amount of active ingredient
is
5$ to 15~, the amount of surfactant is 10~ to 20$, and
the
amount~of vesicle-forming lipid is 0.5o to 5%; such
a
method wherein up to about loo by weight of thickener,
based upon the total weight of ingredients, is admixed
together with the other ingredients; such a
method wherein the thickener is selected from aerosil
and aluminum or magnesium stearate; such a
method wherein the fatty oil or apolar substance is
selected from the group consisting of peanut, sesame,
sunflower, wheat germ, soy, jojoba, castor, almond,
mink,
and olive oils and mixtures thereof as fatty oil, and
paraffin oil, isopropyl myristate, isopropyl palmitate,
6 MERZ 21/dlk
~~~~11 ~'~~
medium-chain triglycerides, isooctyl stearate, capryl/cap-
ric acid triglycerides, cetyl palmitate, and mixtures
thereof as apolar substance; such a
method wherein the oil-soluble surfactant is selected
from the group consisting of polyoxyethylene lauryl
ether
having 1 to 4 EO units, polyoxyethylene(5)oleyl ether,
polyoxyethylene(7)glyceryl cocoate, cocoa fatty acid
diethanolamide, ethanolamide, mono or di or tri (alkyl
tetraglycol ether)-artho-phosphoric acid esters, polyoxyet-
hylene glycerol trioleate, polyoxyethylene sorbitan
triste-
arate, polyoxypropylene(15)-stearyl ether, and mixtures
thereof; such a
method wherein the vesicle-forming lipid is selected
from the group consisting of a lower polyoxyethylated
fatty
alcohol having an HLB value between 2 and 6 and a phospho-
lipid; such a
method wherein the fatty alcohol is a higher polyoxy--
ethylated fatty alcohol having 1 to 4 ethylene oxide
units,
and the phospholipid is lecithin, phosphatidylcholine,
-
serine, or -diethanolamine, or a mixture thereof; such
a
method wherein the polyoxyethylated fatty alcohol is
based upon a C16-C18 alcohol; such a
method wherein up to about 30$ of active ingredient,
selected from the group consisting of essential oils,
herbal extracts, and vitamins, is admixed together with
the
other ingredients; and finally such a
method wherein the oil and/or apolar component is
selected from the group consisting of Soya oil, paraffin
oil, isopropyl myristate, jojoba oil, isopropyl palmitate,
capric acid triglyceride, and mixtures thereof, wherein
the
oil-soluble surfactant is selected from the group consist-
ing of alkyl tetraglycol ethers, polyoxyethylene(7)glycerol
7 MERZ 21/dlk
cocoate and coconut oil diethanolamide, and wherein the
vesicle-forming lipid is lecithin.
GENERAL DESCRIPTION OF THE INVENTION
According to the present invention, the problem is
solved by the provision of bath or shower additives
containing a fatty oil and/or other apolar fatty substance
and, if required, an active ingredient and, in addition, a
combination of an oil-soluble surfactant and a vesicle
forming lipid.
Such combinations are unexpectedly characterized in
that, when added to water, they spontaneously form vesi-
cles, although it is known 'that special methods and
equipment are usually required to produce them. Previous
processes are characterized in that lamellar units must
first be produced which - by applying high-energy tech-
niques such as ultrasound, high-pressure jet, or high-speed
agitators - must then be converted into globules having a
small particle size.
It was therefore most surprising ( a ) that the formula
tions according to the invention in or with water form
vesicles, although - as described above - vesicles are
usually formed only by applying high external energy, and
moreover (b) that the vesicle-forming constituents incorpo
rated into the bath water are not dissolved. However, the
vesicles are in fact formed in the bath water and accord-
ingly greatly enhance the value of the compositions of the
present invention as compared to similar prior art prod-
ucts.
The vesicles obtained according to the invention are
globular. units consisting of concentric bi-layers. Depend-
ing on the size and the number of possibly superposed
bi-layers, distinction is made between unilamellar and
S MERZ 21/dlk
multilamellar or oligolamellar vesicles. These surfactant
associates, namely, the vesicles, are characterized by
considerable stability arid anisotropy (viz., determinable
and reproducible regularly-variable properties) and can
frequently be seen under the polarization microscope.
Therefore, the presence of such vesicles, and particularly
the multilamellar vesicles, can be established by use of
apolarization microscope. In contrast to many vesicles
produced previously, the vesicles produced according to the
present invention do not require the 'presence of a stabi-
lizer such as cholesterol.
By employment of the new additives of the present
invention, the balneological and/or cosmetic effect of bath
formulations can be considerably potentiated, because the
active ingredients are thus able to act via the liposomes
or vesicles over an extended period on and in the skin,
inasmuch as the oily component serves as an action vehicle
and depositing system for the active ingredients which are
then set free in a sustained release manner. Therefore, the
effect of the oil baths attained by employment of a
formulation according to the invention goes beyond the
temporary and short-term care so far achievable, as lipo-
somes and vesicles are known to exert a favorable effect on
the epidermis in the sense of a depot effect of lipids and
active ingredients, thereby inter alia positively influenc-
ing the hydration capacity of the skin over an extended
time period.
Oil Component
The oil bath formulations according to the invention
may contain common fatty oil components and preferably an
oil selected from the group consisting of peanut, sesame,
sunflower, soy, jojoba, castor, almond, olive, mink and
wheat germ oils, and mixtures thereof.
9 MERZ 21/dlk
.~ v r~
As apolar substance (by which is meant a non-polar
substance), which may be employed together with or instead
of the fatty oil according to the present invention, may be
mentioned all kinds of non-polar materials of an oily,
fatty, or waxy nature, as set forth in the following.
Thus, other suitable components of the oil phase can
accordingly be fatty or waxy apolar substances such as
paraffin hydrocarbons, esters of higher alcohols and higher
fatty acids (so-called wax esters), and higher fatty alco
hols. Representative preferred components are:
Paraffin oil
Isopropyl myristate
Isopropyl palmitate
Medium-chain length triglycerides
Propylene glycol esters of medium-chain length fatty
acids
2-Octyl dodecanol
Hexyl dodecanoate
Isooctyl stearate
Capryl/capric acid triglyceride
Cetyl palmitate, and the like.
Such substances, which are already used for incorpora
tion into oil bath compositions, can be used individually
or in combination with the above-described oil components
or mixtures thereof.
Especially preferred are soy, paraffin, and jojoba
oils, as well as isopropyl myristate, isopropyl palmitate,
and capric acid triglyceride, and mixtures thereof.
Oil-Soluble Surfactant
The surfactant employed according to the present
invention is a fat- or oil-soluble surfactant or tenside,
such as sorbitan monooleate, docusate sodium, or the like,
10 MERZ 21/dlk
~ ~~ t~ ~. ~'
which is capable of inducing formation of the vesicles or
liposomes which are essential accarding to the present
invention. As oil-soluble tensides for the dispersion of
the oil phase, common surfactants can therefore be used,
These comprise oil-soluble, water-dispersible substances,
especially those having HLB values between about 6 and 13,
and preferably between about 7 and 10. Particularly pre-
ferred are the following surface-active substances:
Polyoxyethylene lauryl ether with 1 to 4 EO units of
medium chain length
Polyoxyethylene (5) oleyl ether
Polyoxyethylene (7) glyceryl cocoate
Coconut acid diethanolamide
Mono-, di-, and tri-(alkyl te~traglycol ether) ortho-
phosphoric acid esters (mixture)
Polyoxyethylene glycerol trioleate
Polyoxyethylene sorbitan tristearate
Polyoxypropylene (15) stearyl ether, and the like.
Especially preferred are polyoxyethylene lauryl ether
with 1 to 4 EO units, polyoxyethylene (7) glycerol cocoate,
coconut acid diethanolamide, and mixtures thereof.
Vesicle-Forminct Lipid
As vesicle-forming lipid, known substances may be
employed, such as polyoxyethylated fatty alcohols with
preferably 1 to 4 EO in an HLB range from about 2 to 6, the
lipophilic group preferably comprising a C16 - C18 fatty
alcohol.
Higher analogues of the respective fatty acids and
phospholipids are also suitable, especially such as
lecithin (egg or soy lecithin), phosphatidylcholine,
-serine, or -diethanolamine, and mixtures thereof.
Z1 MERZ 21/dlk
~E~~~.~_~~
Other suitable lipidic components utilizable for the
production of vesicles or mixed vesicles include sphingo
lipids (e. g., sphingosine, ceramides, cerebrosides,
sphingomyelin), cholesterol, quaternary ammonium compounds,
polyglycerol alkyl ethers, glucosyl dialkyl ethers, saccha-
rose diesters, sulfuric acid esters of higher alcohols,
collagen hydrolysate esters, bile acids, and poloxamers.
Such compounds are already known for the production of
liposomes (cf. DE 41 21 945.7). However, in that case the
vesicles were produced and incorporated into the desired
preparations only by expensive procedure and usually
required a stabilizer, neither of which are required
according to the present invention.
Active Ingredient
As described, the formulations according to the
invention can contain 0 to 30%, preferably 5 to 15~, of one
or more active ingredients such as essential oils, herbal
extracts, and/or vitamins in usual amounts. These active
ingredients may representatively comprise Oleum menthae
japonicum, rosemary oil, lavender oil, menthol, as well as
jojoba.oil, linden blossom, calendula, panthenol, Aloe vera
extract, vitamin E, avocado oil, ivy extract, eucalyptus
oil, thyme oil, a phyto lipid, or the like. Depending upon
the effect desired, such as improvement of skin structure,
care of sensitive skin, stimulation of circulation, or
relaxatian, a suitable combination of active ingredients
can be employed. 2f required, traditional auxiliary agents
can be added in usual amounts (e.g., 1-10~) such as
thickening or jellifying agents, 2.g., aerosil, aluminum or
magnesium stearate or analogues thereof, and mixtures
thereof, depending upon the exact type of product desired
and the effect intended to be attained.
12 MERZ 21/dlk
~~~~~a~~
*****
Especially suited for the vesicle-forming compositions
of the present invention are combinations containing
20 to
90~ oil component (fatty oil and/or fatty or waxy apolar
substance), 2 to 50~ of oil-soluble surfactant or mixtures
thereof, 0.5 to 5$ of lipid anct, if desired, 5 to
15~ of
one or more active ingredients.
When introduce3 into water, the formulations according
to the invention produce both an immediate and a depot
effect. Based upon the compos_i.tion of the formulations
according to the invention, this two-phase action in
the
water effects both a considerable increase in and prolonga-
tion of the intended effect, or a liposome-based cosmetic
depot and "caring" effect without the necessity of
addi-
tional effort in either the production or application,
i.e., use, of the preparation.
In addition, the compositions or formulations accord-
ing to the invention ensure a uniform dispersion of
the oil
phase in the bath water. Although vesicle-forming lipids
themselves possess some degree of emulsifying effect,
they
are normally unable to ensure sufficient dispersion
in the
bath water of all of the oil present in the composition.
The formulations according to the invention may therefore
contain less lipophilic surfactants and/or reduced
amounts
thereof, and therefore have a balancing effect in this
regard. It is only due to a resulting uniform distribution
and dispersion that vesicles can be formed. Therefore,
on
the one hand, the formulations according to the invention
are characterized by their high capacity for emulsification
of the oil phase in the bath liquor and, on the other
hand,
by their capacity for spontaneous vesicle formation.
Both
of these aspects and both the tenside and the lipidic
components are essential for the production of the
products
23 MERZ 21/dlk
%'
according to the invention, thereby generally leading to
highly-desirable transparent compositions.
BRIEF DESCRTPTION OF THE DRAWINGS
Referring now to the drawings, FIG. 1. is an enlarged
view of a product according to the present invention as
produced according to Example 1 hereof, showing the vesicu-
lar components thereof in the form of multiple circles as
seen under an elec::ron microscope.
FIG. 2 is a view of a conventional bath oil formula-
tion containing the bath oil plus surfactant without
vesicle-forming lipid, as seen under an electron micro-
scope, evidencing the absence of vesicles, only single
circles and no double circles characteristic of bilayer
vesicles being apparent.
k
SPECIFIC DESCRIPTION OF THE INVENTION
Formulations according to the invention are produced
by traditional methods using traditional equipment (stain
less steel vessel with agitator). Into this vessel the
individual components are introduced, mixed, and formulated
into a.finished product. Depending upon the type of product
desired (e. g., fox bath or shower bath), innumerable
suitable and common auxiliary agents can be included
therein. The invention is described in more detail by the
following examples, which are given to illustrate the
composition and method of the present invention but which
are not to be construed as limiting.
Example 1 - Preparation of an oil bath preparation
Introduce soy ail and paraffin oil into a stainless
steel vessel with agitator> Add, under stirring, Laureth-4
and the following components in the order described.
14 MERZ 21/dlk
~~~~~v~
Prepare the product within a temperature range between 20°
and 70°C. Subsequently cool, filter (100 um), portion, arid
package.
Composition 1
Soy oil 50%
Paraffin oil 20%
Laureth-4 (CTFA - ethoxylated lauryl 15%
alcohol-surfactant)
Coconut acid diethanolamide 5%
Lecithin 3%
Eucalyptus oil 4%
Pine oil 2.5%
Tocopherol acetate 0.5%
Example 2
The following bath formulation was preparedin the manner
described in Example 1.
Composition 2
Soy oil 30%
Isopropyl myristate 20%
Octyl dodecanol 20%
Jojoba.oil 5%
Mono/di/tri (alkyltetraglycol ether)/
o/phosphoric acid ester 5%
Polyoxyethylene (7) glycerol cocoate 5%
Lecithin 5%
Ivy extract 5%
Panthenol (H-complex Vitamin) 3%
Perfume oil 2%
Example 3
A shower gel preparation was prepared according to the
foregoing procedure.
15 MERZ 21/dlk
Composition 3
Soy oil 36%
Paraffin oil 20%
Laureth-3 (CTFA - ethoxylated lauryl
alcohol-surfactant) 10%
Polyoxyethylene (7) glyceryl cocoate 10%
Capryl/capric acid triglyceride 10%
Isopropyl palmitate 8%
Sphingosine 1%
Eucalyptus oil 1%
Aerosil (finely-divided SiOz thixotropic
agent) 3%
Perfume oil 1%
Clinical Evaluation
The increased efficacy of the products according to
the present invention was demonstrated in clinical trials.
In these studies, two galenical formulations according to
the present invention were tested on human volunteers.
Test 1
A,product according to the invention containing 70% of
oil/apolar substances, 20% of surfactants, 3% of lecithin,
as well as eucalyptus oil, pine oil and thyme oil as active
ingredients (composition as per Example 1), was tested as
follows:
Obiective
To determine whether and to what extent the micro-
circulation in the skin can be improved by the new two-
phase bath formulation which produces spontaneous formation
of vesicular lipid particles containing active ingredients
in the bath water.
16 MERZ 21/dlk
Ten volunteers with healthy skin were included in the
study. The trial was carried out using a common dosage of
30 grams of bath concentrate per 100 liter of water at a
temperature of 37°C.
For objective comparison, the same measurements were
made using blank water.
The following methods were applied to determine the
cutaneous microcirculation:
- Laser Doppler measurement of erythrocyte flux
- Measurement of partial transcutaneous oxygen pressure
- Measurement of skin temperature
Results
In healthy skin, the product according to the inven-
tion, as compared to blank water, effects an immediate
clear increase of cutaneous oxygen supply by 212. Erythro
cyte flux in the deeper, dermal vessels and in the capil
laries is enhanced by 66~.
The improvement of cutaneous oxygen supply and
circulation lasts for more than one ( 1 ) hour after bathing,
reaching values of 160 and 33~, respectively, at this
time.
This result can be explained by the so-called depot
effect'of the two-phase bath, making possible a sustained
and intensified action of the active ingredients on human
skin. Due to the special galenical formulation of the
product according to the invention, which contains the
lipid-vesicle action complex, the active ingredients can
form a layer on the skin while bathing (immediate effect)
and effect a prolonged or protracted supply of the active
ingredients to the skin for an extended period after
bathing (depot effect). During this process, there is
marked stimulation of cutaneous circulation, especially in
the deeper dermal layers, and marked improvement of
17 MERZ 21/dlk
epidermal oxygen supply, which contributes to a general
activation and mobilization of the body's own resistance.
Test 2
Ten volunteers with healthy skin were tested according
to the above method, applying a preparation according to
the invention containing 70~ of fatty oil/apolar substanc-
es, 10~ of oil-scluble surfactants, 5~ of lecithin and
rosemary oil, pine oil, ivy extract and vitamin E as active
ingredients, according to Example 2.
Results
In healthy skin, the product according to the inven
tion, as compared to blank water, effects a temporary,
clear and sustained improvement of capillary and epidermal
oxygen supply by 147 associated with an increase of dermal
circulation by ~1~.
The improvement of cutaneous oxygen supply and
circulation continues for more than one (1) hour after
bathing, reaching values of 123 and 7.30, respectively, at
this point in time. This can be explained by the so-called
depot effect of the two-phase bath which ensures a pro-
tracted and intensified action of the active ingredients on
human skin.
This test also confirms the high efficacy of the
formulations according to the invention through the two-
phase action, involving both immediate and deposit or depot
effect, and the resulting long-lasting improvement of
epidermal oxygen supply. This improves the skin's condi-
tion, its resistance, and its storage capacity fox active
ingredients over an extended period.
* * * * *
Examples 4-g: The following Compositions are prepared
in essentially the manner described in Example 1 and found
18 MER2 21/dlk
2~~.~4~:~.~r
to be highly effective for their intended purpose, as
already fully described for Examples 1-3, including a high
degree of vesicle formation in use as a bath or shower
additive.
Composition 4
Peanut oil 65.0
Isopropylpalmitate 3.0~
Jojoba oil 5.0~
PEG(4)lauryle-cher 13.0
Lecithin 0.5~
Ceramide 2.0g
Rosemary oil 6.0~
Pine oil 5.0~
Tocopherol 0.5~
Composition 5
Sesame oil 50.0
Octyldodecanol 10.0$
Avocado oil 5.0$
PEG(2)laurylether 10.0$
PEG(7)glycerylcocoate 5.0$
Lecithin 2 . O~S
Sphingosine 3.0~
Eucalyptus oil 12.0$
Turpentine oil 2.0~
Tocopherol 1.0~
19 MERZ 21/dlk
~Q~~:~ x''~
Composition 6
Medium-chain Triglycerides 30.0%
Paraffin subliquidum 30.0%
Isopropylmyristate 5.0%
Almond oil 10.0%
Mono-, Di- and Tri-(alkylt etra-
glycolether)-0-phosphoric acid
4.0%
PEG(4)laurylether 8.0%
Cerebroside 3.0%
Lecithin 1.0%
Ivy extract 4.0%
Calendula extract 2.0%
Perfume oil 2.0%
Tocopherol 1.0%
Composition 7
Paraffin subliquidum 21.0%
Soy oil 30.0%
Olive oil 5.0%
Octyldodecanol 9.0%
D~cyloleate 5.0%
PEG(7)glycerylcocoate 3.0%
PEG(2)laurylether 12.0%
Sphingomyelin 1.0%
PEG(2)stearylether 2.0%
Lecithin 0.5%
Eucalyptus oil 5.0%
Thyme oil 1.5%
Rosemary oil ~.0%
Tocopherol 1.0%
20 MERZ 21/dlk
~~ ~~~~3~~
Composition 8 (Shower composition)
Soy oil 40.0
Medium-chain Triglyceride~; 37.5
Aerosil 3.0~
Cocosfattyaciddiethanolami.de 5.0~
PEG(~)laurylether 9.0v
Lecithin 3.0~
Perfume oil 2.5$
Composition 9
Paraffin subliquidum 50.0
Jojoba oil 15.0
Avocado oil 9.0~
Oleyloleate 5.0~
PEG(4)laurylether 12.0
PEG(2)cetylether 2.5~
Lecithin 1.0~
Cholesterol 1.0~
Lavender oil 2.5~
Citric oil 1.5~
Camphor 0.5~
Tfie replacement of lecithin in
the foregoing examples
by other suitable lipids, such as sphingomyelin, produces
similarly good results, especially as to the vesicle-form-
ing properties. Moreover, innumerable
additional prepara-
tions in accord with the present invention, and having
equivalent effectiveness, may be
prepared and will immedi-
ately be apparent to one skilled n the art.
i
* * * *
As will be seen from the foregoing Examples, in which
compositions according to the present invention are pre-
pared, and the foregoing clinical evaluations employing the
same, the formulations or compositions of the present
21 MERZ 21/d1k
~~r{)~~ ~_r7~j
i.nvc:rrt:i.arn cnrv,: ttr,crt.'ui. pFc__ :fit: ~r:~ hot:h oi.l ra:r~
shcrwc~~r crnmpo:a:L-
t:iorr,~, whetan.r c;onrplcto oz.° L~tnr°tLa:l., anti wire-then
fao-t batat,
laetn~i l:7ath, or. >=o-r shetmpoo:i_rrg, e:lther. di_rEC:tLy i.ntr~ the
pa:rticrl or c:cnntt.7_ca;e k:>~:U:hr, :~t7o4lc;T, or sharnpao, oz tacJcaher
w.Lth or as an ~rcicl.i.t;:l.vc: :J:oc .Lntr.~crclcrc,tlan :Lrata
aorrvernt:Lona:l.
bath, shower, ac. shearnyao fa:i~rm.r:l.at:Lons, whether a>' oa:l., cle:l,
ac iraarn type, .for. the prov_Ls:.LOn al" ves:La:l_e-~F.orrning compa-
rrernts their.°e:Ln and to irnprave t:he e:f fec~t:1_verml~et and
Er~ptr-
c;:La:Lly tire ;rus t;aanetl ac t.ian thc~reaE .
LO Lt is arcarding:ly seen from the ~a:regainJ ttwut the
p.rer~~3rot :Lnven t.:Lan p rovacir~s nove:L ba t:h air shaw~a;e~ adcl:Ltive
compos:Lta.ons ac :fa:rmr.r:l.at:ions camp:risanJ a :fatty a:L:L and/o:r
a .fa-tt:y air waxy apc~:lar mint~r:i.ai, a vesara.Le-:fa:rm:Lng 7.ipid,
ar1(i err o.L:L--sa.luble surfactarut;, together w:Lth aru topically-.
acta.ve rasmdt:Lc .ingredlerat, i.:f desi red, wh:Lch forrnulat:Lori,
upon :Lwt.roductian ar~to the bath water ac l:i.y.rid, farms a
highly-ef:f active and long-acting two-ptlauE3 bath i:armu:la-
t:ion, involving the immediate e:f:fect a~ providing a layer
a~ ttte .~arrnul.at:Lan and any active lr~gred:lemt thernaE upon
the sic:Ln s'iurang the course of bathing ac showez~3.ng, as wall
as pa~aviding a prolonged or p:r.atrac~ted stapply of the
fo:rmul:~t:ion and any active ingrt~d:tawt cantalnod the:reln
ai=ter campletton of bathand, thereby providing a valuable
depot e:f:fert upon the sk:Lra .fo:r an ax-tandod period after
bathing anc7 invalvir~g a definite .increase a:f au~tanoous
aacygen supp~.y as ws~ll as erythroayta flux in ttxe deeper
dermal vessels arid :Lrt tire capi~.:Laries, improving the skin
aond:ition, its resistance, and its storage oaparaty far
active :Lngredie~mts aver an extended parioc~ acrd oamtributing
:30 to a general act:ivatian and mabi:Lization oil the body' s own
res:Lstanc~:, as tael_L as a method ~o.r the preparation or
fax~rnulai:tan a.f such compositions,
22 MER;L 21/dlk
It is to be understood that the present invention is
not to be limited to the exact details of operation, or to
the exact compounds, compositions, methods, procedures, or
embodiments shown and described, as various modifications
and equivalents will be apparent to one skilled in the art,
wherefore the present invention is to be limited only by
the full scope which can be legally accorded to the append-
ed claims.
23 MERZ 21/dlk
