CA2090137C - Bath and shower composition having vesicle-forming properties and method for the production and use thereof - Google Patents
Bath and shower composition having vesicle-forming properties and method for the production and use thereof Download PDFInfo
- Publication number
- CA2090137C CA2090137C CA002090137A CA2090137A CA2090137C CA 2090137 C CA2090137 C CA 2090137C CA 002090137 A CA002090137 A CA 002090137A CA 2090137 A CA2090137 A CA 2090137A CA 2090137 C CA2090137 C CA 2090137C
- Authority
- CA
- Canada
- Prior art keywords
- oil
- composition
- fatty
- group
- polyoxyethylene
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/10—Washing or bathing preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/30—Characterized by the absence of a particular group of ingredients
- A61K2800/31—Anhydrous
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
Abstract
The invention relates to novel oily bath and shower compositions containing a combination of fatty oil and/or fatty or waxy apolar substance, oil-soluble surfactant, and vesicle-forming lipid and, if desired, a cosmetically- or balneologically-active ingredient. When added to water, these formulations spontaneously generate dispersed vesicles. They exhibit an immediate as well as a prolonged or depot effect, can be used alone or added to or together with existing bath or shower formulations, arid are espe-cially suited for use in connection with or as additives to full, partial, and shower baths.
Description
~~~~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
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
Claims (29)
1. A transparent anhydrous liquid balneological or cosmetic composition suitable as an additive for use in bathing or showering, having vesicle-forming properties, which spontaneously forms liposomes or vesicles immediately upon being admixed with water, and which produces an immediate and delayed effect, consisting essentially of the following anhydrous ingredients:
20 to 90% by weight of the composition of at least one of a fatty oil and a fatty or waxy apolar substance, wherein the fatty oil is selected from the group consisting of peanut, sesame, sunflower, wheat germ, soy, jojoba, castor, almond, mink, and olive oils, and wherein the fatty or waxy apolar substance is selected from the group consisting of paraffin oil, isopropyl myristate, isopropyl palmitate, triglycerides, isocytl stearate, capryl/capric acid triglycerides, cetyl palmitate, and mixtures thereof,
20 to 90% by weight of the composition of at least one of a fatty oil and a fatty or waxy apolar substance, wherein the fatty oil is selected from the group consisting of peanut, sesame, sunflower, wheat germ, soy, jojoba, castor, almond, mink, and olive oils, and wherein the fatty or waxy apolar substance is selected from the group consisting of paraffin oil, isopropyl myristate, isopropyl palmitate, triglycerides, isocytl stearate, capryl/capric acid triglycerides, cetyl palmitate, and mixtures thereof,
2 to 50% by weight of the composition of at least one oil-soluble surfactant which is an oil-soluble water-dispersible tenside having an HLB
value of 7 to 10, and which is selected from the group consisting of an oxyethylated 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polmoxyethylene sorbitan tristearate-polyoxypropylene(15)-stearyl ether, and mixtures thereof, 0.1 to 20% by weight of the composition of at least one vesicle-forming lipid selected from the group consisting of an oxyethylated C16 C18 fatty alcohol having 1 to 4 ethylene oxide units and having a HLB value between 2 and 6 and a phospholipid selected from the group consisting of lecithin, phosphatidylcholine, -serine, or -diethanolamine or a mixture thereof, up to 30% by weight of the composition of a cosmetically-active ingredient selected from the group consisting of essential oils, herbal extracts, and vitamins, and 0 to 10% by weight of the composition of a thickener.
2. A composition of Claim 1, containing 20% to 90% fatty oil or apolar substance, 2% to 50% oil-soluble surfactant, and 0.1 % to 20%
vesicle-forming lipid, all by weight of total composition.
value of 7 to 10, and which is selected from the group consisting of an oxyethylated 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polmoxyethylene sorbitan tristearate-polyoxypropylene(15)-stearyl ether, and mixtures thereof, 0.1 to 20% by weight of the composition of at least one vesicle-forming lipid selected from the group consisting of an oxyethylated C16 C18 fatty alcohol having 1 to 4 ethylene oxide units and having a HLB value between 2 and 6 and a phospholipid selected from the group consisting of lecithin, phosphatidylcholine, -serine, or -diethanolamine or a mixture thereof, up to 30% by weight of the composition of a cosmetically-active ingredient selected from the group consisting of essential oils, herbal extracts, and vitamins, and 0 to 10% by weight of the composition of a thickener.
2. A composition of Claim 1, containing 20% to 90% fatty oil or apolar substance, 2% to 50% oil-soluble surfactant, and 0.1 % to 20%
vesicle-forming lipid, all by weight of total composition.
3. A composition of Claim 2, wherein the percentage of fatty oil 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.
4. A composition of Claim 3, wherein the percentage of oil-soluble surfactant is 10% to 20% by weight.
5. A composition of Claim 2, 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.
6. A composition of Claim 1, wherein the oil-soluble surfactant is an oil-soluble, water-dispersible tenside having an HLB value of 6 to 13.
7. A composition of Claim 6, wherein the HLB value is 7 to 10.
8. A composition of Claim 4, 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polyoxyethylene sorbitan tristearate, polyoxypropylene(15)-stearyl ether, and mixtures thereof.
units, polyoxyethylene(5)oleyl ether, polyoxyethylene(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.
9. A composition of Claim 1, 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 phospholipid.
10. A composition of Claim 9, wherein the fatty alcohol is a higher polyoxyethylated fatty alcohol having 1 to 4 ethylene oxide units, and the phospholipid is lecithin, phosphatidylcholine, -serine, or -diethanolamine, or a mixture thereof.
11. A composition of Claim 9, wherein the polyoxyethylated fatty alcohol is based upon a C18-C18 alcohol.
12. A composition of Claim 1, containing up to 30% of a cosmetically-active ingredient.
13. A composition of Claim 12, containing 5 to 15% active ingredient.
14. A composition of Claim 12, wherein the active ingredient is selected from the group consisting of essential oils, herbal extracts, and vitamins.
15. A composition according to Claim 2, additionally containing up to 10%
thickener.
thickener.
16. A composition of Claim 15, wherein the thickener is selected from aerosil and aluminum or magnesium stearate.
17. A composition of Claim 1, incorporated into a conventional bath or shower formulation.
18. A composition of Claim 2, wherein the oil 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 consisting of alkyl tetraglycol ethers, polyoxyethylene(7)glycerol cocoate and coconut oil diethanolamide, and wherein the vesicle-forming lipid is lecithin.
19. A method for the production of a bath or shower additive composition, which spontaneously forms dispersed liposomes or vesicles immediately upon being admixed with water, and which produces an immediate and delayed effect, which comprises the step of admixing together at a temperature between about 20°C and 70°C the following ingredients:
20 to 90% by weight of the composition of at least one of a fatty oil and a fatty or waxy apolar substance, wherein the fatty oil is selected from the group consisting of peanut, sesame, sunflower, wheat germ, soy, jojoba, castor, almond, mink, and olive oils, and wherein the fatty or waxy apolar substance is selected from the group consisting of paraffin oil, isopropyl myristate, isopropyl palmitate, triglycerides, isocytl stearate, capryl/capric acid triglycerides, cetyl palmitate, and mixtures thereof, 2 to 50% by weight of the composition of at least one oil-soluble surfactant which is an oil-soluble water-dispersible tenside having an HLB
value of 7 to 10, and which is selected from the group consisting of an oxyethylated 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polmoxyethylene sorbitan tristearate-polyoxypropylene(15)-stearyl ether, and mixtures thereof, 0.1 to 20% by weight of the composition of at least one vesicle-forming lipid selected from the group consisting of an oxyethylated C16-C18 fatty alcohol having 1 to 4 ethylene oxide units and having a HLB value between 2 and 6 and a phospholipid selected from the group consisting of lecithin, phosphatidylcholine, -serine, or -diethanolamine or a mixture thereof, up to 30% by weight of the composition of a cosmetically-active ingredient selected from the group consisting of essential oils, herbal extracts, and vitamins, and 0 to 10% by weight of the composition of a thickener.
20. A method of Claim 19, wherein the amount of fatty oil or apolar component is 50% to 70%, 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 0.5% to 5%.
value of 7 to 10, and which is selected from the group consisting of an oxyethylated 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polmoxyethylene sorbitan tristearate-polyoxypropylene(15)-stearyl ether, and mixtures thereof, 0.1 to 20% by weight of the composition of at least one vesicle-forming lipid selected from the group consisting of an oxyethylated C16-C18 fatty alcohol having 1 to 4 ethylene oxide units and having a HLB value between 2 and 6 and a phospholipid selected from the group consisting of lecithin, phosphatidylcholine, -serine, or -diethanolamine or a mixture thereof, up to 30% by weight of the composition of a cosmetically-active ingredient selected from the group consisting of essential oils, herbal extracts, and vitamins, and 0 to 10% by weight of the composition of a thickener.
20. A method of Claim 19, wherein the amount of fatty oil or apolar component is 50% to 70%, 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 0.5% to 5%.
21. A method of Claim 19, wherein up to 10% by weight of thickener, based upon the total weight of ingredients, is admixed together with the other ingredients.
22. A method of Claim 21, wherein the thickener is selected from aerosil and aluminum or magnesium stearate.
23. A method of Claim 19, 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.
24. A method of Claim 23, 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)-ortho-phosphoric acid esters, polyoxyethylene glycerol trioleate, polyoxyethylene sorbitan tristearate, polyoxypropylene(15)-stearyl ether, and mixtures thereof.
units, polyoxyethylene(5)oleyl ether, polyoxyethylene(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.
25. A method of Claim 24, 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 phospholipid.
26. A method of Claim 25, wherein the fatty alcohol is a higher polyoxyethylated fatty alcohol having 1 to 4 ethylene oxide units, and the phospholipid is lecithin, phosphatidylcholine, -serine, or -diethanolamine, or a mixture thereof.
27. A method of Claim 26, wherein the polyoxyethylated fatty alcohol is based upon a C16-C18 alcohol.
28. A method of Claim 27, wherein up to 30% of active ingredient, selected from the group consisting of essential oils, herbal extracts, and vitamins, is admixed together with the other ingredients.
29. A method of Claim 19, wherein the oil 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 consisting of alkyl tetraglycol ethers, polyoxyethylene(7)glycerol cocoate and coconut oil diethanolamide, and wherein the vesicle-forming lipid is lecithin.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEP4205548.2 | 1992-02-24 | ||
| DE4205548A DE4205548C3 (en) | 1992-02-24 | 1992-02-24 | Bath and shower additive with vesicle-forming properties, its production and use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2090137A1 CA2090137A1 (en) | 1993-08-25 |
| CA2090137C true CA2090137C (en) | 2002-07-23 |
Family
ID=6452403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002090137A Expired - Lifetime CA2090137C (en) | 1992-02-24 | 1993-02-23 | Bath and shower composition having vesicle-forming properties and method for the production and use thereof |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP0557825B1 (en) |
| AT (1) | ATE165970T1 (en) |
| CA (1) | CA2090137C (en) |
| DE (2) | DE4205548C3 (en) |
| DK (1) | DK0557825T3 (en) |
| ES (1) | ES2117063T3 (en) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9409763D0 (en) * | 1994-05-16 | 1994-07-06 | Phares Pharma Holland | Liposome forming compositions |
| AU3688395A (en) * | 1994-09-27 | 1996-04-19 | Rijksuniversiteit Leiden | Phospholipid- and cholesterol-free aqueous composition for opical application to the skin |
| DE19748921C2 (en) * | 1997-10-30 | 2001-02-22 | Stockhausen Chem Fab Gmbh | Skin-friendly hand cleaners, especially rough hand cleaners |
| DE19757059A1 (en) | 1997-12-20 | 1999-07-01 | Merz & Co Gmbh & Co | Balneological products combining properties of effervescent tablets and liquid or oil bath |
| DE19854827A1 (en) * | 1998-11-27 | 2000-06-08 | Merz & Co Gmbh & Co | Water-based vesicle-forming surfactant-containing cleaning preparations, process for their preparation and their use |
| DE10062610A1 (en) * | 2000-12-15 | 2002-06-27 | Merz & Co Gmbh & Co | Vesicle-forming skin oils from oil-soluble components and W / O emulsifiers with an HLB value of 2-6 and vesicle-forming lipids and optionally one or more customary additives, processes for their preparation and their use |
| US6998372B2 (en) | 2001-08-16 | 2006-02-14 | J&J Consumer Companies, Inc. | Moisturizing detergent compositions |
| JP4757446B2 (en) * | 2004-01-09 | 2011-08-24 | 株式会社 資生堂 | Oily cleansing composition |
| DE102007006778A1 (en) * | 2007-02-08 | 2008-08-14 | Beiersdorf Ag | New shower oil |
| DE102008045280B4 (en) | 2008-09-01 | 2018-12-27 | Merz Pharma Gmbh & Co. Kgaa | Bath pearls forming liposomal structures, their preparation and their use |
| DE102009033109A1 (en) | 2009-07-15 | 2011-02-03 | Merz Pharma Gmbh & Co. Kgaa | Liquid or flowable proteosome-forming bath and shower concentrates, galenic application products thereof and their use |
| GB201017113D0 (en) | 2010-10-11 | 2010-11-24 | Chowdhury Dewan F H | Surfactant vesicles |
| DE102010054461A1 (en) | 2010-12-14 | 2012-06-14 | Merz Pharma Gmbh & Co. Kgaa | Liposome-forming aqueous bath preparations with high active ingredient content and their cosmetic / dermatological / medical application |
| DE102012007734A1 (en) | 2012-04-18 | 2013-10-24 | Merz Pharma Gmbh & Co. Kgaa | Stable solid oil bath salt preparations with application-specific flexibility that are easy to prepare from 2 phases |
| EP2671615A1 (en) | 2012-06-05 | 2013-12-11 | Merz Pharma GmbH & Co. KGaA | Solid bath additive having a retarded olfactory and visual lelease effect profile |
| DE202012005506U1 (en) | 2012-06-05 | 2012-08-28 | Merz Pharma Gmbh & Co. Kgaa | Firm bath additive with retarded olfactory and visual release effects profile |
| DE102015215359A1 (en) * | 2015-08-12 | 2017-02-16 | Beiersdorf Ag | Semi-solid cleaning product based on oil containing exfoliating particles |
| DE102015215358A1 (en) * | 2015-08-12 | 2017-02-16 | Beiersdorf Ag | Semi-solid cleaning product based on oil |
| US11622556B2 (en) | 2016-04-12 | 2023-04-11 | Bio-Up Mimetic Technologies, Inc. | Re-oiled and hyper-oiled lecithin carrier vehicles |
| EP3677244A3 (en) * | 2020-02-04 | 2020-11-18 | Clariant International Ltd | Compositions comprising multilamellar vesicles |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LU85829A1 (en) * | 1985-04-01 | 1986-11-05 | Cird | PSORALENE BASED BATH COMPOSITION FOR THE TREATMENT OF PSORIASIS |
| DE3622438A1 (en) * | 1986-07-04 | 1988-01-07 | Henkel Kgaa | COSMETIC DETERGENT RAW MATERIAL |
| DE4021083C2 (en) * | 1990-07-03 | 1995-08-17 | Hans Dr Lautenschlaeger | Phospholipid formulations and their use for the preparation of liposomal medical and cosmetic baths |
-
1992
- 1992-02-24 DE DE4205548A patent/DE4205548C3/en not_active Expired - Lifetime
-
1993
- 1993-02-12 AT AT93102232T patent/ATE165970T1/en active
- 1993-02-12 DE DE59308520T patent/DE59308520D1/en not_active Expired - Lifetime
- 1993-02-12 DK DK93102232T patent/DK0557825T3/en active
- 1993-02-12 EP EP93102232A patent/EP0557825B1/en not_active Expired - Lifetime
- 1993-02-12 ES ES93102232T patent/ES2117063T3/en not_active Expired - Lifetime
- 1993-02-23 CA CA002090137A patent/CA2090137C/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| ATE165970T1 (en) | 1998-05-15 |
| DE4205548C3 (en) | 1998-07-23 |
| EP0557825B1 (en) | 1998-05-13 |
| DE4205548C2 (en) | 1995-04-06 |
| CA2090137A1 (en) | 1993-08-25 |
| EP0557825A3 (en) | 1995-02-01 |
| DK0557825T3 (en) | 1998-10-07 |
| DE59308520D1 (en) | 1998-06-18 |
| DE4205548A1 (en) | 1993-08-26 |
| EP0557825A2 (en) | 1993-09-01 |
| ES2117063T3 (en) | 1998-08-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2090137C (en) | Bath and shower composition having vesicle-forming properties and method for the production and use thereof | |
| US5766628A (en) | Bath and shower composition having vesicle-forming properties and method for the production and use thereof | |
| US5853755A (en) | Biphasic multilamellar lipid vesicles | |
| EP0956853B1 (en) | Use of nanodispersions in pharmaceutical compositions | |
| DE69433386T2 (en) | Propylene glycol stearate vesicles | |
| US5643600A (en) | Lipid vesicles containing avocado oil unsaponifiables | |
| US4508703A (en) | Production of pulverulent mixtures of lipidic and hydrophobic constituents | |
| EP2542207B1 (en) | Foam formulations containing at least one triterpenoid | |
| JPH07505368A (en) | Local and transdermal administration system using ultra-fine oil spheres | |
| EA004662B1 (en) | Vesicle forming skin oil containing w/o emulsifiers with a hydrophilic-lipophilic balance of 2-6, method for the production and use thereof | |
| KR101642054B1 (en) | Composition for transdermal transfer and cosmetics containing the same | |
| US5741515A (en) | Ketoprofen liposomes | |
| JP2001521547A (en) | Aqueous composition containing lipid and lanolin-derived surfactant and use thereof | |
| DE102009033109A1 (en) | Liquid or flowable proteosome-forming bath and shower concentrates, galenic application products thereof and their use | |
| KR20180124278A (en) | Liposome compositions for accelerating percutaneous absorption | |
| EP0629128A1 (en) | Aqueous phospholipid vesicle dispersion, process for its manufacture and use thereof. | |
| JP2001233754A (en) | Emulsion type skin care preparation | |
| EP1053221B1 (en) | Lipid mixtures and their use | |
| JPH05279242A (en) | Bathing solution | |
| JPS61204109A (en) | Emulsion-type composition for external use | |
| PT1364642E (en) | Composition for delivery of dithranol | |
| US7422756B2 (en) | Skin preparation | |
| JPH09510432A (en) | Lipid vesicles containing unsaponifiable avocado oil | |
| JP6984394B2 (en) | Underwater oil type emulsified cosmetic | |
| KR20170094848A (en) | Composition of non-water liquid crystalline phase comprising ceramide and Method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |