US3856931A

US3856931A - Medicated stick

Info

Publication number: US3856931A
Application number: US00277122A
Authority: US
Inventors: P Fuchs; G Schopflin
Original assignee: Schering AG
Current assignee: Bayer Pharma AG
Priority date: 1972-08-01
Filing date: 1972-08-01
Publication date: 1974-12-24
Anticipated expiration: 1991-12-24

Abstract

Solid cosmetic compositions, in stick shape, comprising a solid wax, a fatty alcohol, a polyol fatty acid ester mixture acid, optionally, a higher saturated hydrocarbon or a fatty acid alkanol amide can readily be applied to the skin, have a lubricating and emolient effect on the skin without imparting a shine thereto, can readily be washed off with water and medicaments can be dissolved therein.

Description

I nited States Patent [191 I uchs et al.

[ MEDICATED STICK [75] Inventors: Peter Fuchs; Gisela Schopflin, both of Berlin, Germany [73] Assignee: Schering Aktiengesellschaft, Berlin and Bergkamen, Germany [22] Filed: Aug. 1, 1972 [21] Appl. No.: 277,122

OTHER PUBLICATIONS Sagarin, Cosmetics Science & Technology, Intersci- Dec. 24, i974 ence, N.Y. (i957) TP983S26C, pages 102, 108, I09, 110, 118, H9, 129, I30, 134, 159, 160, 166, I67, 278, 279, 291, 780, 781, 785.

Primary Examiner-Shep K. Rose Attorney, Agent, or Firm- Millen, Raptes & White [57] ABSTRACT Solid cosmetic compositions, in stick shape, comprising a solid wax, a fatty alcohol, a polyol fatty acid ester mixture acid, optionally, a higher saturated hydrocarbon or a fatty acid alkanol amide can readily be applied to the skin, have a lubricating and emolient effect on the skin without imparting a shine thereto, can readily be washed off with water and medicaments can be dissolved therein.

16 Claims, N0 Drawings MEDICATED STICK BACKGROUND OF THE INVENTION This invention relates to novel medicated sticks for topical application and to a process for the production thereof, and to a stick composition and a process for the preparation thereof.

Medicated sticks for topical application and cosmetic sticks having an antiperspirant and deodorizing effect are conventional. Such sticks can be produced based on alcoholic soap gels or solid hydrogels, using alginates, pectins or carboxyvinyl polymers. In German Unexamined Published Application DOS 1,617,472, stick compositions are described made of polyalkylene glycol ethers of fatty alcohols of 12-22 carbon atoms and polyalkylene glycol esters of waxy acids. For an example of a cosmetic base containing a higher fatty alcohol and a solid wax, see US. Pat. No. 3,211,618. See also U.S. Pat. No. 2,892,732.

Medicated lubricating sticks are also known produced from paraffins and/or cacao butter, partially with the addition of alkaline soaps.

All conventional stick compositions have in common that they are poorly suitable for the production of sufficiently lubricating, cosmetically flawless medicated sticks formed of a formulation which can be washed off. Thus, sticks based on alcoholic soap gels have the disadvantages of insufficient dimensional stability, of being incompatible with various active medical agents and, although these stick compositions can be washed off, they lack any lubricating effect. The desired lubricating effect is present in sticks having a paraffin and- /or cacao butter base, but these stick compositions cannot be readily washed off and are always somewhat tacky, so that they lack sufficient slidability during their application.

It is an object of this invention to provide a composition for a medicated stick, which provides a nonreactive, i.e., inert, vehicle for the effective medical agent, which has a lubricating as well as oil-restoring, emolient effect but does not impart an oily shine to the skin and which can readily be washed off with water.

SUMMARY OF THE INVENTION According to this invention, the above-described objects are achieved by a cosmetic base comprising a solid wax, a fatty alcohol, a polyol fatty acid ester mixture and, optionally, one or both of a higher saturated hydrocarbon and a fatty acid alkanolamide.

DETAILED DISCUSSION The solid waxes and fatty alcohols which are employed are inert from a toxicological viewpoint.

Solid waxes which can be employed are natural waxy substances. Examples are beeswax, carnauba wax, spermaceti and other waxes having like physical properties.

Fatty alcohols which can be employed are alcohols of 8 30 carbon atoms.

Examples of suitable fatty alcohols are myristyl alcohol, cetyl alcohol, and stearyl alcohol and like higher fatty alcohols.

The polyol fatty acid esters employed in the compositions of this invention are low-polyhydroxylated monoester mixtures of glycerin and carboxylic acids of 8-18 carbon atoms and equivalent esters. The molecular weight of the low-polyhydroxyde is 200 600. Examples are bis-polyethoxylene glyceryl mono stearate and mono myristate.

Medical agents which can be employed in the medicated sticks of this invention include the corticoids, e.g., 11B, 1701,21-trihydroxy-4-pregnene-3,20-dione (hydrocortisone) and the esters thereof; l1B,17a,2ltrihydroxy-l,4-pregnadiene-3,20-dione (prednisolone) and the esters thereof; 6a-fluorol1,8,21-dihydroxy-16a-methyl-l,4-pregnadiene-3,20- dione (fluocortolone) and the esters thereof; 601,9- difluoro-l18,21-dihydroxy-3,20-dioxo-loer-methyl- 1,4-pregnadiene (difluocortolone) and the esters thereof; 6a-fluoro-9,l lB-dichloro- 21-hydroxy-16a-methyl-1,4-pregnadiene-3,20-dione and the esters thereof; 601,1 1B-difluoro-9-chloro-2 1- hydroxy-l6a-methyl-l,4-pregnadiene-3,20-dione and the esters thereof; 9a-chloro-6a-fluoro-l 13,21- dihydroxy-l 6a-methyl-1 ,4-pregnadiene-3 ,20-dione (clocortolone) and the esters thereof; 6-chlorol7a-hydroxy-1a,2or-methylene-4,6-pregnadiene-3,20- dione (cyproterone) and the esters thereof; 9-fluoro- 1 1,6,17,21-trihydroxy- 3,20-dioxo-16a-methyl-1,4-pregnadiene (dexamethasone) and the esters thereof; and/or bactericides, e.g., 5-amino-1,3-bis (ethylhexyl )hexahydro-S- methylpyrimidine (hexetidine), 5,7-dichloro- 8- hydroxyquinaldine (chlorquinaldol) and benzalkonium chloride. -hexadecylpyridinium Also suitable as medicaments are local anesthetics, antiseptics and disinfectants, e.g., ethyl paminobenzoate (Anesthesin), w-diethylamino-2,6- dimethylacetanilide (Xylocaine) and the hydrochloric salt thereof, and a polyoxyethylene ether of dodecyl alcohol (Thesit) or boric acid, 1- hexadecylpyridinium chloride (cetylpyridinium chloride), surfen, anthrasol, Ichthyol or tumenol and/or cignolin or hexachlorophene.

Examples of higher saturated hydrocarbons which can be employed are, in particular, the various types of paraffin, such as, e.g., hard, i.e., solid paraffin, viscous paraffin and liquid paraffin, with a viscosity from about 50 of.

Fatty acid alkanolamides which can be employed are preferably those derived from lower alkanols of 1 5 carbon atoms, e.g., methanol and ethanol, and from higher fatty acids of 8 24 carbon atoms, e.g., myristic acid.

Optionally, other conventional substances with respect to the medicine therein can be present in the stick composition, e.g., perfume oils and coloring agents.

The medicaments employed are suitably incorporated into the cosmetic stick base composition by dissolving the drug directly in the melt of the stick composition. 1f the medicament does not dissolve or only par tially dissolves in this melt, the medicament can be extremely finely triturated with part or all of the amount of the cold, liquid mixture components. The melt of the remaining components of the mixture is then added to this suspension. The method of preparation of the stick composition is not critical, as long as it remains pourable while molten into the molds used to form the sticks.

The still liquid stick composition is suitably poured at once into appropriate screw-type extensible cases with a core as the packaging material (stick casings).

The medicated sticks of the present invention have the advantage that they are dimensionally stable and attractive in appearance. They are gentle to the skin, since they contain no tensides. They have a lubricating and an emolient effect, without causing the skin to shine. The stick composition slides well along the skin and can readily be washed off with water.

In the examples described hereinafter, instead of a medicament other additives can be present, so that such stick compositions can also be utilized for the manufacture, e.g., of cosmetics, e.g., lipstick, deodorant, eyeshadow and perfume sticks.

The proportions of the components employed in the cosmetic bases of this invention generally are:

Percent by Weight Medicament or cosmetic agent Especially preferred are sticks containing a medicament or cosmetic agent dissolved in a solid mixture comprising 4-15 percent cetyl or stearyl alcohol -25 percent beeswax and 50-70 percent of the polyol fatty acid ester mixture employed in the examples below, alone or as a mixture with up to equal parts of a paraffin or microcrystalline wax.

1n the examples below, the polyol fatty acid ester mixture employed is CETlOL HE (Henkel & Cie, Duesseldorf).

Without further elaboration, it is believed that one skilled in the art can, using the preceding description, utilize the present invention to its fullest extent. The following preferred specific embodiments are, therefore, to be construed as merely illustrative, and not limitative of the remainder of the disclosure in any way whatsoever.

EXAMPLE 1 5.0 g. of cetyl alcohol, 25.0 g. of beeswax, 20.0 g. of spermaceti, 17.2 g. of paraffin oil, and 32.8 g. ofa mixture of polyol fatty acid esters are melted. The melt is poured into the stick cases.

EXAMPLE 2 10.0 g. of cetyl alcohol, 25.0 g. of beeswax, and 65.0 g. of a mixture of polyol fatty acid esters are melted together. The melt is poured into the stick cases.

EXAMPLE 3 12.50 g. of beeswax, 18.75 g. of coconut fatty acid monoethanolamide, 12.50 g. of stearyl alcohol, 10.50 g. of highly viscous paraffin, and 43.75 g. of a mixture of polyol fatty acid esters are melted together. The melt is poured into the stick cases.

EXAMPLE 4 7.5 g. of cetyl alcohol, 25.0 g. of beeswax, 10.0 g. of a microcrystalline wax made up of branched-chain hydrocarbons, 15.0 g. of highly viscous paraffin, and 42.5 g. ofa mixture of polyol fatty acid esters are melted together. The melt is poured into the stick cases.

EXAMPLE 5 5.0 g. of cetyl alcohol, 25.0 g. of beeswax, 20.0 g. of hard paraffin (m.p.: 51-53 C.), 17.2 g. of highly viscous paraffin, and 32.8 g. of a mixture of polyol fatty acid esters are melted together. The melt is poured into the stick cases.

EXAMPLE 6 0.025 g. of fluocortolone trimethylacetate and 0.05 g. of chlorquinaldol are dissolved in a melt of 3.185 g. of a mixture of polyol fatty acid esters, 0.490 g. of cetyl alcohol, and 1.225 g. of bleached wax, with the addition of 0.025 g. of Crematest perfume oil, and poured into the stick cases.

EXAMPLE 7 0.05 g. of chlorquinaldol is dissolved in a melt of 3.185 g. of a mixture of polyol fatty acid esters, 0.490 g. of cetyl alcohol, and 1.25 g. of beeswax, with the addition of0.025 g. ofCrematest perfume oil, and poured into the stick cases.

The preceding examples can be repeated with similar success by substituting the generically and specifically described reactants and/or operating conditions of this invention for those used in the preceding examples.

From the foregoing description, one skilled in the art can easily ascertain the essential characteristics of this invention, and without departing from the spirit and scope thereof, can make various changes and modifications of the invention to adapt it to various usages and conditions.

What is claimed is:

l. A solid cosmetic base composition in the shape of cosmetic stick characterized by having a lubricating and emolient effect on the skin without imparting a shine thereto and capable of being readily washed off with water, said composition consisting essentially of, in percent by weight based on the total composition,

10-70 percent solid wax;

4-35 percent fatty alcohols of 8-30 carbon atoms;

and

15-70 percent polyol fatty acid ester mixture consisting essentially of a low-polyhydroxylated monoester mixture of glycerin and carboxylic acids of 8-18 carbon atoms wherein the molecular weight of the low-polyhydroxide is 200-600.

2. a composition according to claim 1, wherein the solid wax is selected from the group consisting of beeswax, carnauba wax and spermateci wax.

3. A composition according to claim 2, wherein the solid wax is beeswax.

4. A composition according to claim 3, containing l025 percent beeswax.

5. A composition according to claim 1, wherein the fatty alcohol is selected from the group consisting of myristyl alcohol, cetyl alcohol and stearyl alcohol.

6. A composition according to claim 5, wherein said fatty alcohol is cetyl alcohol or stearyl alcohol.

7. A composition according to claim 6, containing 4-15 percent of said alcohol.

8. A composition according to claim 1 wherein the solid wax is beeswax and the fatty alcohol is cetyl alcohol or stearyl alcohol.

9. A composition according to claim 8, containing l025 percent beeswax and 4-15 percent of said alcohol.

10. A composition according to claim 1, containing 50-70 percent of said polyol fatty acid ester mixture.

11. A composition according to claim 10, wherein said polyol fatty acid ester is selected from the group consisting of bis-polyethoxylene-glyceryl monostearate and bis-polyethoxylene-glyceryl monomyristate.

112. A composition according to claim 10, wherein the solid wax is beeswax and the fatty alcohol is cetyl alcohol or stearyl alcohol.

13. A composition according to claim 1, containing -25 percent beeswax, 4-15 percent cetyl alcohol or stearyl alcohol and 50-70 percent bis-polyethoxylene glyceryl monostearate or bis-polyethoxylene-glyceryl monomyristate.

14. A composition according to claim 1, further coma higher fatty acid of 8-24 carbon atoms.

Claims

1. A SOLID COSMETIC BASE COMPOSITION IN THE SHAPE OF COSMETIC STICK CHARACTERIZED BY HAVING A LUBRICATING AND EMOLIENT EFFECT ON THE SKIN WITHOUT IMPARTING A SHINE THERETO AND CAPABLE OF BEING READILY WASHED OFF WITH WATER, SAID COMPOSITION CONSISTING ESSENTIALLY OF, IN PERCENT BY WEIGHT BASED ON THE TOTAL COMPOSITION, 10-70 PERCENT SOLID WAX; ; AND 15-70 PERCENT POLYL FATTY ACID ESTER MIXTURE CONSISTING ESSENTIALLY OF A LOW-POLYHYDROXYLATED MINOESTER MIXTURE OF GLYCERIN AND CARBOXYLIC ACIDS OF 8-18 CARBON ATOMS WHEREIN THE MOLECULAR WEIGHT OF THE LOW-POLYHYDROXIDE IS 200-600.

3. A composition according to claim 2, wherein the solid wax is beeswax.

4. A composition according to claim 3, containing 10-25 percent beeswax.

7. A composition according to claim 6, containing 4-15 percent of said alcohol.

9. A composition according to claim 8, containing 10-25 percent beeswax and 4-15 percent of said alcohol.

12. A composition according to claim 10, wherein the solid wax is beeswax and the fatty alcohol is cetyl alcohol or stearyl alcohol.

13. A composition according to claim 1, containing 10-25 percent beeswax, 4-15 percent cetyl alcohol or stearyl alcohol and 50-70 percent bis-polyethoxylene glyceryl monostearate or bis-polyethoxylene-glyceryl monomyristate.

14. A composition according to claim 1, further comprising 0.005 - 20 percent of a medicament or cosmetic agent.

15. A composition according to claim 1, further comprising up to 25 percent of a paraffin having a viscosity of at least 50 centipoises.

16. A composition according to claim 1, further comprising up to 40 percent of a fatty acid alkanol amide derived from a lower alkanol of 1-5 carbon atoms and a higher fatty acid of 8-24 carbon atoms.