MEDICATED SKIN CLEANSING PRODUCTS
The present invention relates to a medicated skin cleansing product. More particularly, the present invention relates to soap or soap-free skin cleansing products for treatment or prevention of skin disorders having a pH of about between 3.5 to 6.0 and containing an antimycotic agent .
In British Patent 2342862 there is described and claimed a solid cleansing soap bar containing an anti-fungal agent for treatment of mycotic skin disorders wherein said chemical composition is defined as having a pH between 6-10 and being formed into a solid bar cake that is usable as a cleansing bar.
As the pH of healthy skin is acidic (4.5-5.5), it has been an object of the present invention to develop medicated products containing antimycotics and having a pH within the normal skin range.
In addition, it has now been found however that for vaginal products, a pH of between 3.5 to 6.0, that does not disturb the physiological equilibrium of the natural bacterial flora, has to be targeted since a product with a pH of 6 to 10 will disturb the natural physiological pH, raising the vaginal pH from 3.5-4.5 to higher than 6 for a certain period of time, from minutes to hours, depending on the pH of the product (the higher the worse). During this time the overgrowth of the fungi will be accelerated.
As will be described hereinafter it has now been found that the products of the present invention do not change the skin or the vaginal pH, leaving intact the competitive inhibition between the natural bacterial flora and fungi.
Furthermore, it has now been found that a pH of 3.5 to 6.0 will create the best medium for the antimycotic activity of an antimycotic agent such as terbinafine or ciclopirox or an imidazole such as clotrimazole or miconazole.
"Alkaline metal" soaps have a relatively high pH, being salts of weak acids with a strong base.
Antimycotic agents such as Imidazoles or terbinafine or ciclopirox are not stable in liquid soap environments, and therefore cannot be formulated in the form of liquid soaps with regular (alkaline) soap.
Thus, according to the present invention it has now been surprisingly found that these antifungal agents are stable in soap-free soap bar products. This new finding enables the use of imidazoles or terbinafine or ciclopirox , in the convenient
form of bar soap. In addition, it has now been surprisingly found that antimycotic agents such as imidazoles or terbinafine or ciclopirox are stable also in liquid soap-free soaps, provided that the pH is kept in the range of 3.5-7.0.
Thus, according to the present invention there are now provided medicated skin cleansing products for the treatment or prevention of skin disorders containing an antimycotic agent and having a pH between 3.5-6.0 wherein said antimycotic agent is selected from the group consisting of terbinafine or ciclopirox or an imidazole.
In preferred embodiments of the present invention said products are soap-free however combination products including alkaline soap of animal or vegetable origin are also contemplated for use according to the present invention.
In especially preferred embodiments of the present invention said product is in the form of a cleansing bar while in other embodiments said product is in the form of a liquid soap-free soap.
The medicated soap or soap-free products of the present invention can be used for the treatment or prevention of skin -disorders wherein the skin disorder is selected from the group consisting of mycotic, fungal, itching, rash, dermatitis, tinea crusis, body tinea, eczema, pruritus, dermatophytosis, and the microorganisms comprise dermatophytes (like t chophyton, epidermophyton floccosum, microsporum species), aspergillus moulds, malassezia furfur, corynebacteria minutissimum and gram-positive bacteria like staphylococci, streptoccoci.
Preferably the imidazole used in the product of the present invention is selected from the group consisting of Clotrimazole, miconazole, metronidazole, bifonazole, ketoconazole, terconazole, econazole or mixtures thereof.
In especially preferred embodiments of the present invention said imidazole is Clotrimazole.or Miconazole.
Said imidazole is preferably provided in a concentration of between 0.5 and 2.0%. Additional antimycotic agents are terbinafine and Ciclopirox.
The composition of the basic soap-free cleansing bar is based on a clinically proven, dermatologically tested product containing allergy-screened ingredients.
The cleansing bars according to the present invention have been shown to have better substantivity properties, so that the quantity of the antimycotic agent left on the skin is relatively high.
As stated hereinbefore in the preferred embodiments of the present invention the medicated skin cleansing product is soap-free or is primarily soap-free, e.g., is in the form of a combination bar having up to 10% of a soap product and having at least 90% of a soap-free product containing the antimycotic component.
The novel antifungal solid preparations are advantageously prepared by heating the various ingredients together at an elevated temperature as to obtain an intimate fluid or semi-fluid mixture, cooling down the mixture to a lower temperature so as to remain still in a semi-fluid extrudable state, adding thereto the antimycotic agent , and extruding, casting or shaping by other means a desired shape, such as bar, stick or the like.
Some of the preparations were initially heated to about 70-85°C, cooled to about 50-65°C, the antimycotic agent was added and the desired shape of the final product (of the desired shape) was prepared.
The pH of the preparation is advantageously adjusted to a pH in the said range. The pH can be adjusted by the addition of suitable physiologically acceptable acids. Various organic acids are suited for this purpose, such as lactic, citric and phosphoric acid.
In a first set of preferred embodiments of the present invention there is provided a skin cleansing bar composition containing: i. 20-70% of anionic surfactants chosen from a large variety of mild surfactants such as: disodium alkyl sulfosuccinates (Cio-Ciβ), sodium/potassium long chain alkyl sulfate (C10-C20), sodium cocoyl isethionate, sodium alkyl sulfoacetate, acyl taurates, acyl sarcosinates, acyl glutamate, alkyl glyceryl ether sulfonates, and mixtures thereof; ii. 0-10% of amphoteric and cationic surfactants, such as alkylamido propyl betaine, alkyl betaine, alkyl sultaines, alkyl amine oxides and imidazolines and mixtures thereof; iii. 0-10% of nonionic surfactants such as alkyl polyglucosides, polyalkylene glycols, glyceryl monostearate, polyetoxylated fatty alcohols, polyhydroxy fatty acid amides and alkanolamides and mixtures thereof; iv. 2-20% of binders and plasticizers, such as cetostearyl alcohol, paraffin wax, stearic acid, palmitic acid, myristic acid, polyol esters,
polyethylene glycols, fatty acid ethoxylate and mixtures thereof, wherein said plasticizers have a melting point from about 30 to 90 ° C; v. 5-30% of moisturizing agents and emollients, such as: stearic acid, cetostearyl alcohol, mineral oil, vegetable oil, urea, glycerine, propylene glycol, lactic acid, sodium lactate, polyols and mixtures thereof; vi. 10-30% of binding agents and processing aid agents such as maltodextrin, dextrin, starch, talc and mixtures thereof; vii. 0.2%-5% of an antimycotic agent, preferably Clotrimazole/Miconazole
/Terbinafine/Ciclopirox . viii. 0.5%-5% of skin substantivity increasing agents such as quatemized polymers, sodium acrylates copolymer and cationic copolymers and mixtures thereof; and ix. 0.2-5% of pH adjusting acid agents such as lactic acid, phosphoric acid, citric acid, fumaric acid, tartaric acid and mixtures thereof. In further embodiments of the present invention there is provided an antifungal soap-free cleansing bar, comprising:
20-70% anionic surfactants, preferably 30-50% 0-10% amphoteric surfactants, preferably 2-4% 0-10% nonionic surfactants, preferably 1-4%. 10-50% moisturizers, emollients, plasticizers, preferably 15-35% 10-30% binding and processing aid agents, preferably 15-25% 0.2-5% antimycotic agent preferably 0.5-2% 3-10% water, preferably 5-8%.
Preferably said compositions further comprise deionized water in an amount of between 3% and 10% (m/m).
In further embodiments of the present invention there is provided a combination skin cleansing bar composition comprising:
20-60% of anionic surfactants chosen from a large variety of mild surfactants such as: disodium alkyl sulfosuccinates (Cio-Cis), sodium/potassium long chain alkyl sulfate (C10-C20), sodium cocoyl isethionate, sodium alkyl sulfoacetates, acyl taurates, acyl sarcosinates, acyl glutamat, alkyl glyceryl ether sulfonates, and mixtures thereof;
0-10% of amphoteric and cationic surfactants, such as alkylamido propyl betaine, alkyl betaine, imidazolines and mixtures thereof;
0-10% of nonionic surfactants such as glyceryl monostearate, polyalkylene glycols, polyetoxylated fatty alcohos, polyhydroxy fatty acid amides, alkyl polyglucosides, alkanolamides and mixtures thereof;
0-10% of soap, of animal or vegetable origin such as, sodium* tallowate, sodium palmate, sodium cocoate, sodium stearate, sodium palm kemelate, as a processing aid agent and hardener;
2-20% of binders and plasticizers, such as cetostearyl alcohol, paraffin wax, stearic acid, palmitic acid, myristic acid, wherein said plasticizers have a melting point from about 30 to 90°C;
5-30% of moisturizing agents and emollients, such as: stearic acid, cetostearyl alcohol, mineral oil, vegetable oil, urea, glycerine, propylene glycol, lactic acid, sodium lactate, polyols and mixtures thereof;
10-30% of binding agents and processing aid agents such as maltodextrin, dextrin, starch, talc and mixtures thereof;
0.2%-5% of an antimycotic agent, preferably Clotrimazole/Miconazole/ Terbinafine/Ciclopirox
0.5%-5% of skin substantivity increasing agents such as quatemized polymers, sodium acrylate copolymers, cationic copolymers and mixtures thereof; and
0.2-5% of pH adjusting acid agents such as lactic acid, phosphoric acid, citric acid, fumaric acid, tartaric acid and mixtures thereof.
In further preferred embodiments of the present invention there is provided ' an anti-fungal combination cleansing bar comprising:
20-60% anionic surfactants, preferably 30-50%;
0-10% soap preferably 3-6%;
0-10% nonionic surfactants preferably 1 -4%;
0-10% amphoteric surfactants, preferably 2-4%;
10-50%o moisturizers, emollients, plasticizers, preferably 15-35%;
10-30% binding and processing aid agents, preferably 15-25%;
0.2-5% an antimycotic agent preferably 0.5-2%; and
5-13% water, preferably 6-10%.
Preferably said compositions further comprise deionized water in an amount of between 5% and 13% (m/m).
In yet further preferred embodiments of the present invention there is provided a medicated liquid soap composition comprising: i. 5-25% of anionic surfactants chosen from a large variety of surfactants, such as sodium/triethanolamine alkyl sulfates
sodium laureth sulfates, disodium lauryl ethoxy sulfosuccinates (Cto-Ciβ), sodium/ammonium cocoyl isethionate, sodium alkyl sulfoacetate; ii. 0-10% of nonionic surfactants such as alkyl polyglucosides, polymeric quaternary ammonium salt (polyquaternium), glycol distearate, cocamide
DEA, glyceryl esters and various others; iii. 0-10% of amphoteric and cationic surfactants such as of imidazoline type (preferably disodium cocamphodiacetate) and betaine type (preferably alkylamidopropyl betaine, alkyl betaine) and various others; iv. 1-8% of emollients and moisturizing agents, such as mineral oil, vegetal oil, silicone oil derivatives (such as dimethicone copolyol), glycerine, propylene glycol, sodium/ammonium lactate, lactic acid, urea; v. 1 -10% of foam boosters and viscosity improvers, such as cocamides, ethoxylate fatty alcohols, sodium chloride; vi. 0.2-3% of an antimycotic agent, preferably Clotrimazole/Miconazole/
Terbinafine/Ciclopirox vii. 0.2-5% of pH adjusting acid agents such as citric acid, lactic acid, phosphoric acid, fumaric acid, tartaric acid; viii. 0-1% fragrance, dye q.s.; and ix. 70-85% deionized water.
In further preferred embodiments of the present invention there is provided an anti-mycotic liquid soap composition comprising:
5-25% Anionic surfactants, preferably 8-12%;
0-10% Amphoteric and cationic surfactants preferably 1 -4%;
0-10% Nonionic surfactants, preferably 2-6%;
1-8% Moisturizers and emollients preferably 0.5-2%;
0.2-3% an antimycotic agent preferably 0.5-2%; and
70-85%o water preferably 76-82%.
While the invention will now be described in connection with certain preferred embodiments in the following examples so that aspects thereof may be more fully understood and appreciated, it is not intended to limit the invention to these particular embodiments. On the contrary, it is intended to cover all alternatives, modifications and equivalents as may be included within the scope of the invention as defined by the appended claims. Thus, the following examples which include preferred embodiments will serve to illustrate the practice of this invention, it being understood that the particulars shown are by way of example and for purposes of illustrative discussion of preferred embodiments of the present invention only and are presented in the cause of providing what is believed to be the most useful and readily understood description of product procedures as well as of the principles and conceptual aspects of the invention.
Examples of Soap-Free Bars
Exam les of Liquid Soaps
It will be evident to those skilled in the art that the invention is not limited to the details of the foregoing illustrative examples and that the present invention may be embodied in other specific forms without departing from the essential attributes
thereof, and it is therefore desired that the present embodiments and examples be considered in all respects as illustrative and not restrictive, reference being made to the appended claims, rather than to the foregoing description, and all changes which come within the meaning and range of equivalency of the claims are therefore intended to be embraced therein.