CA1206881A - Anti seborrhoeic composition - Google Patents

Abstract

Abstract A preparation for treating seborrhoea, seborrhoeic dermatitis and seborrhoeic eczema of the scalp containing as an active ingredient 13-cis Vitamin A acid, esters or pharmaceutically acceptable salts thereof to the scalp.

Description

~LZ~6~38~

The compound Swiss Vitamin A acid has been used topically or orally in selected areas of dermatology such as in the treatment of acne. See united Kingdom Patent No. 1,335,867; Peck et at., New Erg. J. Med. 300:329-333 (1959) and Gunny JIMMY. 240:610 (1978). Furthermore, 10 this compound has been used orally in the treatment and prophylaxis of carcinomas of the epithelial cells. Sworn et at. Federation Proceedings, 35, No. 6,1332 (1976). In addition, Swiss Vitamin A acid has been used orally and subcutaneously to suppress the secretion of the setaceous 15 glands. See Gums it 21., J. Invest, Dermatol. 74:392-7 tl980) and Strauss, Abstract No. 29, Into Dermatol. Swamp-slum Oct. 13-15, 1980, Berlin, Germany.

As seen from above, these publications demonstrate 20 that Swiss retinoic acid orally administered has been shown to he effective in the control of various Durham-to logical disorders such as acne, psoriasis and other no-fated disorders. However, many compounds, useful in the control of acne, psoriasis and related disorders, have I little, if any, effect on the control of Siberia, seborrhoeic dermatitis and seborrhoeic eczema, which cause dandruff, loss of hair, and other related disorders. It has long been desired to provide an agent effective in controlling, either through treating or through trophy-30 taxis, Siberia, seborrhoeic dermatitis and seborrhoeiceczema of the scalp.

In accordance with this invention, it has been disk covered that when an agent selected from the group consist 35 tying of Swiss Vitamin A acid, lower alkyd esters thereof :: ;

Gun/ 6 . g . 8 2 `_ : ' . :,_`~ ' .

:

0688~L

and pharmaceutically acceptable salts, as well as mixtures thereon, are applied to the scalp control of Siberia, seborrhoeic dermatitis and seborrhoeic eczema is achieved.
In carrying out this invention, any pharmaceutically accept table salt of Swiss Vitamin A acid can be utilize. Among the preferred salts are included the alkali metal salts such as sodium, potassium and lithium, alkaline earth metal salts such as calcium and ammonium salts. The term "lower alkyd esters" as used in the specification designates any conventional lower alkyd ester where the lower alkyd group contains from 1 to 7 carbon atoms. Among the preferred lower alkyd esters are the methyl, ethyl, n-propyl, isopropyl, n-butyl, and isobutyl esters.

In applying the agent of this invention, any convent tonal inert carrier for topical application to the scalp can be utilized in formulating the compositions containing these agents. The pharmaceutical preparation utilized in accordance with the present invention can be manufactured 20 by mixing the aforementioned agents with one or more pear-mystical acceptable carriers suitable for topical ad-ministration by conventional methods.

In accordance with this invention, it has been found I that the aforementioned agents are effective against Siberia, seborrhoeic dermatitis and seborrhoeic eczema of the scalp particularly dandruff and hair loss. Among the other disorders associated with Siberia of the scalp are included: Siberia wapitis; dermatitis Siberia-hoe; Siberia in M. Parkinson and Parkinsonism.

For topical administration to the scalp, the agent scan be conventionally prepared as ointments, tinctures, creams, gels, solutions, lotions, sprays, suspensions, shampoos, hair soaps, perfumes and the like. In fact, any conventional composition utilized for application to the scalp can be utilized in accordance with this invention.
Among the preferred methods of applying the composition 36~8~L

containing the agents of this invention is in the form ox shampoos, solutions and perfumes. The pharmaceutical pro-parathion for topical administration to the scalp can be prepared by mixing the aforementioned active ingredient with non-toxic, therapeutically inert, solid or liquid carriers customarily used in such preparations. Generally, these preparations should contain from about 0.001% to about 5% by weight, based upon the total weight of the combo-session of the active ingredient with 0.01 to lye by weight 10 being preferred and 0.1% to 0.4% by weight being especially preferred. Generally the concentration of the active inure-dint in shampoos is from about 0.2 to 2% by weight based upon the total weight of the shampoo and in lotions from 0.01 to 0.5 by weight. Generally, it is preferred to apply these preparations once or twice daily to the scalp. These preparations can be applied according to the need of the patient.

In carrying out this invention, the active inure-20 dint can be applied in a solution of an alcohol such as ethyl alcohol which contains from about 0.001% to about 5% by weight of the active ingredient. Generally, it is preferred to use an alcohol solution containing from about 0.01% to about 0.5% by weight, of the active ingredient in the alcohol.

In preparing the topical preparations described above additives such as preservatives, thickeners, perfumes and the like conventional in the art of pharmaceutical compounding of topical preparation can be used. In add-lion, conventional antioxidant or mixtures of convent tonal antioxidant can be incorporated into the topical preparations containing the aforementioned active agent Among the conventional antioxidant which can be utilized in these preparations are included ~-methyl-a-tocopherol-amine, tocopherols, butylated hydroxyanisole, bu-tylated hydroxytoluene, ethoxyquin and the like. Cream-base pear-mystical formulations containing the active agent, used .... .

, ZV688~

in accordance with this invention, are composed of aqueous emulsions containing a fatty acid alcohol, semi-solid petroleum hydrocarbon, lo ethyleneglycol and an emulsi-lying agent.

ointment formulations containing the active agent in accordance with this invention comprise admixtures of a semi-solid petroleum hydrocarbon with a solvent dispel-soon of the active material. Cream compositions containing the active ingredient for use in this invention preferably comprise emulsions formed from a water phase of a hummock-lent, a viscosity stabilizer and water, an oil phase of fatty acid alcohol, a semi-solid petroleum hydrocarbon an an emulsifying agent and a phase containing the active 15 agent dispersed in an aqueous stabilizer-buffer solution Stabilizers may be added to the topical preparation. Any conventional stabilizer can be utilized in accordance with this invention. In the oil phase, fatty acid alcohol come pennants function as a stabilizer. These fatty acid alcohol 20 components are derived from the reduction of a long-chain saturated fatty acid from about 14 carbon atoms. Also, conventional perfumes and lotions goner fly utilized in topical preparation for the hair can be utilized in accord dance with this invention. Furthermore, if desired, convent 25 tonal emulsifying agents can be utilized in the topical preparations of this invention.

In accordance with a preferred embodiment of this invention, the Swiss retinoic acid is incorporated into 30 an aqueous shampoo. This shampoo provides a means or treating the scalp and hair for controlling Siberia, seborrhoeic dermatitis and seborrhoeic eczema of the scalp.
In accordance with this preferred embodiment, the concern-traction of the aforementioned agent in the shampoo is from 35 about 0.2 to 2.0%, by weight of the shampoo composition, with amounts of from about 0.5 to 1% by weight being pro-furred. Generally these shampoos can be applied to control said disorders of the scalp according to the needs of the ~206i38~

patient. In general, these shampoos are applied once or twice daily.

The agent of this invention can be incorporated in-to any conventional aqueous shampoo composition. Generally, these shampoos contain water in an amount of from about 40% to 92% by weight. These shampoos also contain surface active agents or detergents in an amulet of from about 5% to 20% by weight of the shampoo composition, with amounts 10 of about lo to 15% by weight being generally preferred. Any conventional surface active agent or detergent for pro-paring shampoo composition can be utilized in accordance with this invention. These detergents or surfactants are preferably either amphoteric or anionic surface active 15 agents. Among the preferred surface active agents or deter-gents are the alkali metal salts of laurel ether sulfates, alkali metals salts of laurel sulfates, as well as the alkali metal salt or ammonium salts of N-beta-hydroxy-ethyl-N-carboxymethyl fatty acid aminoethylamine, fatty 20 alkyldicarboxylic derivatives of imidazolines, alkyd beta-aminoproprionates, sodium polyhydroxy monoether sulk fates, coequal sarcosine, die-thanol/triethanol ammonium laurel sulfate, triethanol amine laurel ether sulfate. Des-creations of various surface active agents and detergents 25 employable in the present shampoos are found in the text Non ionic Surfactants, edited by My Schick and published in l9~7 by Marcel Decker, Inc., and Surface Active Agents and Detergents, Vol. II, by ARM. Schwartz, JAW. Perry and J. Bench, published in 1958 by Intrusions Publishers.
30 Furthermore, shampoos in general contain foaming agents in am amount of from about 2% to 15% by weight of the shampoo with mounts of from 5 to 15% being especially preferred.
Any conventional foaming agent which is generally utilized in shampoos can be utilized in preparing the shampoo come 35 position of this invention. Among the preferred foaming agents are included the coconut fatty acid ethanolamides such as Laurie acid moo or diethanol aside, oleic acid moo or diethanol asides.

6~38~
\

In addition Jo containing the surfactants or deter-gents and foaming agents, the aqueous shampoo composition of this invention may contain, if desired, various other optional adjutants which are generally employed in forum-feting aqueous shampoo compositions. Among these optionaladjuvants are included perfumes and fragrances. Any con-ventional material utilized as perfumes may be incorpo-rated into the shampoo composition of this invention.
Other adjutants which can be incorporated into the aqueous 10 shampoo compositions of this invention include viscosity control agents such as propylene glycol, alcohols such as ethyl alcohols, etc.; conditioning agents such as pro-loin, Panty, D-panthenol, etc.; soaps such as potassium laureate, sodium Stewart, stabilizers and buffers such as 15 sodium phosphate, sodium biphosphate, etc.; pH-adjusters such as citric acids, etc.; pacifiers, etc. Generally, the shampoo composition of this invention contains a pi of from 5.5 to 8.5, with 6.0 to 7.5 being especially pro-furred.
I
The invention is further illustrated by the following examples. In the examples, all percents are percents by weight.

Example 1 Pyrolyzed hair shampoo Wyeth Swiss Vitamin A acid The following composition was packaged in an alum minim tube with interior protective lacquering:

1000 g contain:
Nope owe 3~,35 g an hydrous citric Acadia g Sactol 2 OX 28 (1)300.00 g Steinapon AM 2 L 70.00 g Panty 1.00 g D-Panthenol 4,00 g Swiss Vitamin A Acadia g Euperlan PI 771 50.00 g Sactilan LDC ( ) 20.00 g Perfume PLY 3072 4.00 g Demineralized whetter g I
( ) Laurel ether sulfate, No salt

(2) N-beta-hydroxyethyl-N-carboxymethyl fatty acid amidoethylamine, No salt I Pyrolyzing concentrate, mixture of deterrents and 26 pyrolyzing agents; manufacturer: Henkel & Co., Dusseldorf, Germany (4) Coconut fatty acid diethanol aside ( ) ~-panthenol ethyl ether.

D `:!

. ,, ``

~206~

Example 2 Hair lotion with 0 05/~ Swiss Vitamin A acid The following aqueous alcoholic solution was packaged in black lacquered plastic bottles:

1000 ml contains:
Rectified ethyl alcohol 94% 600.00 g 10 Glycofurol 75 ( ) 2.00 g Swiss Vitamin A acid 0.50 g Distilled water ad 1000.00 ml Example 3 Active lotion with 0.10% Swiss Vitamin A acid An aqueous isopropanol solution containing the folio-wing composition was packaged in-black-dyed plastic bottles:
I
1000 ml contained:
Isopropanol 550.00 g Glycofurol 75 (1) 20.00 g Swiss Vitamin A acid 1.00 g 25 distilled water ad 1000.00 ml Mixture of equal parts off tetrahyd.rofurfuryloxy-ethanol and 2-(2-tetrahydrofurfuryloxy~-ethoxy-ethanol.
Example 4 Hair lotion with 0.02% Swiss Vitamin A acid An aqueous alcoholic solution containing the folio-wing composition was packaged in black lacquered plastic mottles:

61~

g 1000 ml contain:
Rectified alcohol 94%600.00 g Glycofurol 75 2. 00 g Swiss Vitamin A acid 0.20 g Disk tilled water ad 1000. 00 ml :

Claims (16)

CLAIMS:

1. A topical preparation for controlling disorders due to seborrhoea, seborrhoeic dermatitis or seborrhoeic eczema of the scalp containing an effective amount of an agent selected from the group consisting of 13-cis vitamin A acid, lower alkyl esters, salts and mixture thereof, together with a conventional inert carrier for topical application to the scalp.

2. A preparation of claim 1 wherein said agent is 13-cis vitamin A acid.

3. A preparation of claim 1 which is in the form of a shampoo.

4. A preparation of claim 1 which is in the form of a lotion.

5. A preparation of claim 1 wherein the effective amount of said agent from about .001 to 5% by weight, based upon the weight of the preparation.

6. A preparation of claim 5 wherein said preparation contains .01% to 2% by weight of said agent.

7. A preparation of claim 3 comprising from about:
a) .2% to 2% by weight of 13 cis Vitamin A acid, lower alkyl esters, salts and mixtures thereof:
b) 5% to 20% by weight of a surface active agent;
c) 2% to 15% by weight of a forming agent; and d) 40% to 92% by weight of water.

8. A preparation of claim 7 wherein agent is 13-cis Vitamin A acid.

9. A preparation of claim 8 wherein said acid is pre-sent in an amount of from about 0.5 to 1% by weight of said preparation.

10. A method of preparing a topical preparation for controlling disorders due to seborrhoea, seborrhoeic derma-titis or seborrhoeic eczema of the scalp comprising mixing an effective amount of an agent selected from the group consisting of 13-cis vitamin A acid, lower alkyl esters, salts and mixture thereof, with a conventional inert carrier for topical application to the scalp.

11. A method as in claim 10 wherein said agent is 13-cis vitamin A acid.

12. A method as in claim 10 which is in the form of a shampoo.

13. A method as in claim 10 which is in the form of a lotion.

14. A method as in claim 10 wherein the effective amount of said agent from about .001 to 5% by weight, based upon the weight of the preparation.

15. A method as in claim 10 for preparing a shampoo for controlling disorders due to seborrhoea, seborrhoeic derma-titis or seborrhoeic eczema of the scalp comprising mixing the following ingredients:
a) .2% to 2% by weight of 13-cis Vitamin A acid, lower alkyl esters, salts and mixtures thereof;
b) 5% to 20% by weight of a surface active agent;
c) 2% to 15% by weight of a forming agent; and d) 40% to 92% by weight of water.

16. A method as in claim 15 wherein the agent is 13-cis Vitamin A acid.