WO2010003861A1

WO2010003861A1 - Antiperspirant products

Info

Publication number: WO2010003861A1
Application number: PCT/EP2009/058266
Authority: WO
Inventors: Jean-Philippe Andre Roger Courtois; Clive Roderick Harding; Mark Harker; Iain Andrew Weddell
Original assignee: Unilever Plc; Unilever N.V.; Hindustan Unilever Limited
Priority date: 2008-07-08
Filing date: 2009-07-01
Publication date: 2010-01-14
Also published as: AR072720A1

Abstract

A method of reducing perspiration comprising the application of an antiperspirant agent that is β-Ala-Pro-diaminobutyroylbenzylamide or an analogous material and one or more additional antiperspirant agents selected from the group consisting of: astringent salts of aluminium or zirconium; polypeptides comprising the amino acid sequence: Glu.Glu.Met.Gln.Arg.Arg.; polypeptides comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu.; calcium channel blocking agents and lamellar phase stabilised oil-in-water emulsion or an anti-microbial deodorant agent.

Description

Antiperspirant Products

This invention relates to the field of cosmetic products, in particular antiperspirant products. This invention also relates to cosmetic methods of reducing perspiration upon the surface of the human body.

Cosmetic compositions used for reducing perspiration often comprise an astringent metal salt, such as aluminium or zirconium salt. Such salts reduce perspiration by blocking sweat pores. This is an effective method of reducing perspiration, but not beyond improvement. For example, astringent metal salts can be perceived as harsh or irritating by some consumers.

There is a continuing requirement for effective perspiration reduction. The problem to be solved is the provision of effective or improved sweat control via the use of a cosmetically acceptable composition or compositions.

The present invention utilises certain combinations of antiperspirant agents and/or deodorant agents to achieve cosmetic products having enhanced antiperspirancy and/or deodorancy performance. All of the products according to the invention comprise an antiperspirant agent according to formula I:

R¹-NH-CH(R²)-[CHR⁶]_n-CO. N-CH-CO. NH-CH-[CH₂] ₃-_n-NHR⁴

/ \ \

H₂C-CH₂-CH₂ CO.XR³ Wherein:

X = a bond or NH-CH([CH₂]_3+n-NHR⁵)-CO.; n = 0, 1 or 2;

R¹ R⁴ and R⁵ independently = H, optionally substituted Cβ alkyl, amidino or tetra CrCβ alkylamidinium; R² = H or optionally substituted Cβ alkyl, or R¹ and R² together with the group to which they are bonded form a 5- to 7-membered saturated ring; R³ = Ci-Ci₂ alkoxy,

C1-C12 alkylamino, optionally substituted aryl C1-C6 alkylamino, optionally substituted heteroaryl C1-C6 alkylamino, optionally substituted aryl CrC₆ alkoxy, or optionally substituted heteroaryl CrC₆ alkoxy; and

R⁶ = H or, when n = 1 , amino, or together with R1 and the group to which R6 and R1 are bonded, a 5- to 7-membered saturated ring.

Compounds of formula I are disclosed in WO 06/047900 (Pentapharm AG).

A specific compound of formula I, commercially available from Pentapharm AG as SYN^®-AKE and having the structure: β-Ala-Pro-diaminobutyroylbenzylamide, is disclosed as suitable for topical application against hyperhidrosis in Research Disclosure, Vol. 519, 07 2007, p. 685.

According to a first aspect of the invention, there is provided a method of reducing perspiration comprising the application of an antiperspirant agent according to formula I and one or more additional antiperspirant agents selected from the group consisting of: a. Astringent salts of aluminium or zirconium; b. Polypeptides comprising the amino acid sequence: Glu.Glu.Met.Gln.Arg.Arg.; c. Polypeptides comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu.; d. Calcium channel blocking agents; and e. lamellar phase stabilised oil-in-water emulsion. According to a second aspect of the invention, there is provided a cosmetic method of reducing perspiration and body odour comprising the application of an antiperspirant agent according to formula I and an anti-microbial deodorant agent.

Both the first and second aspects of the invention, as described briefly above and in more detail below, lead to excellent antiperspirancy and/or deodorancy benefits.

The method of controlling perspiration offered by the invention is particularly useful because the benefit can extend for a considerable period of time, often greater than 24 hours and sometimes even up to 4 days after application or longer. Significant deodorancy benefits may also accrue from the use of the present invention, in particular the use of products according to the second aspect of the invention (vide supra).

The methods of controlling perspiration and/or body odour according to present invention are particularly useful when direct application to the surface of the human body is involved. This is especially true when application to the axillae and/or feet is involved. Application to the axillae is most beneficial because of the high concentration of eccrine sweat glands in these regions of the human body.

The method of controlling perspiration typically involves multiple applications of a cosmetic composition comprising the antiperspirant agent according to formula I. It is thought that multiple applications improve perspiration reduction by some form of build up effect. The composition may be applied as part of one's daily regime, after washing, for example.

In this description, the term "comprising" should be understood to be non- exhaustive, i.e., meaning that other components may also be present. - A -

In this description, the term "polypeptide" should be understood to mean "polypeptide or derivative thereof. "Derivatives thereof are typically esters, amides, or salts. Acetate esters are a particular example. Certain polypeptide derivatives hydrolyse on application to yield the parent polypeptide.

In this description, the term "water soluble" should be understood to refer to materials having a solubility in water at 25°C of 1 g/L or greater. Preferred polypeptides have a water solubility of 5g/L or greater and particularly preferred polypeptides have a water solubility of 10g/L or greater.

Antiperspirant agents according to formula I comprise two amino acid residues, typically β-alanine and proline, with a substituent group attached via an amide linkage to the carboxy residue of the proline residue. The proline residue preferably has S- stereochemistry.

Preferred antiperspirant agents according to formula I are water soluble.

A particularly preferred antiperspirant agent according to formula I is β-Ala-Pro- diaminobutyroylbenzylamide:

NH2-CH2-CH2-CO.N-CH-CO.NH-CH-[CH2]2-NH2

/ \ \

H₂C-CH₂-CH₂ CO-NH-CH₂C₆H₅

This material is available as a diacetate salt (S- stereoisomer) under the tradename SYN^®-AKE from Pentapharm Ltd.

The antiperspirant agent according to formula I is preferably incorporated into a composition in an amount of from 0.0005 to 1 %, particularly from 0.001 to 0.5%, and especially from 0.005 to 0.2% by weight of the composition. The first aspect of the present invention involves enhancing the antiperspirancy performance of an antiperspirant agent according to formula I by use of an additional antiperspirant agent selected from a specified group of materials. The feature that the additional antiperspirant agents have in common is that they all function by a different mechanism of action to that of the antiperspirant agent according to formula I. It has been found that the combination of such an additional antiperspirant agent with an antiperspirant agent according to formula I produces a surprisingly enhanced antiperspirancy performance.

When the antiperspirant agent according to formula I is used in conjunction with a further antiperspirant agent, it is not essential that the two are part of the same composition. Independent application of the two materials may be employed. Such application may be concurrent or consecutive, provided that the treated surface experiences the presence of both materials. When the agents are applied from independent compositions, it is preferred that the product also comprises a means for, and/or instruction for, both of the compositions to be applied to the surface requiring treatment.

In a particular embodiment, an antiperspirant agent according to formula I (vide supra) is applied together with a lamellar phase stabilised oil-in-water emulsion.

When this is done, it is not essential that the two are part of the same composition. Independent application of the two materials may be employed.

Such application may be concurrent or consecutive, provided that the treated surface experiences the presence of both materials. When the actives are applied from independent compositions, it is preferred that the product also comprises a means for, and/or instruction for, both of the compositions to be applied to the surface requiring treatment.

Lamellar phase stabilised oil-in-water emulsions are sometimes known as oleosome dispersions. Typically, they comprise dispersed droplets of oil surrounded by multiple layers of liquid crystalline lamellar phase comprised of one or more surfactants, non-ionic surfactants being preferred.

The oil of the oleosome dispersions should preferably remain in a liquid state at temperatures as low as 20⁰C or even 15°C. For this reasons, typical oils have melting point from their solid state of less than 20⁰C, preferably less than 15°C, and more preferably less than 10⁰C.

Preferred oils should be relatively fluid, having a kinematic viscosity of less than 100 cSt (mm²/s) and preferably less than 50 cSt (mm²/s) at 20°C.

Suitable oils include hydrocarbon oils and ester oils, particularly triglyceride oils, such as sunflower seed oil. Other particular oils that might be used in the oleosomes are C12-15 alkyl benzoate esters, hydrogenated polybutene, PPG-14 butyl ether, triethyl citrate, isopropyl palmitate, and isopropylmyristate.

The lamellar phase of the oleosome dispersion is typically comprised of two non- ionic surfactants, one having a relatively low HLB (less than 8 and preferably less than 5) and one having a relatively high HLB (more than 12 and preferably more than 15). The ratio high HLB surfactant to low HLB surfactant is chosen so as to give a stable oleosome dispersion, typically ratios being from 1 :1 to 1 :6 by weight, respectively. A blend of steareth-2 and steareth-20 has been found to be suitable, particularly when used in combination with sunflower oil. Steareth-2 and steareth- 20 are best used at a ratio of from 1 :4 to 1 :5 by weight.

The oleosome dispersions have an oil content that typically makes up from 1 to 30%, preferably from 1 to 20%, and more preferably from 1 to 10% by weight of the total composition. The surfactant content typically makes up from 1 to 30%, preferably from 1 to 20%, and more preferably from 1 to 10% by weight of the composition. The ratio of oil to surfactant is typically from 1 :3 to 3:1 and preferably from 1 :2 to 2:1.

Compositions may be applied to the surface of the human body by any means. Application of liquid compositions can be by absorption onto a carrier matrix like paper, fabric, or sponge and application by contacting said carrier matrix with the surface. Solid, semi-solid, or gel compositions can be applied by direct contact or can be dissolved or dispersed in a liquid medium prior to application. Application can also comprise a combination of any two or more of the above techniques.

A further antiperspirant agent may be an astringent salt of aluminium and/or zirconium. When employed, such an astringent salt of aluminium and/or zirconium is preferably incorporated into a composition in an amount of from 0.5- 60%, particularly from 5 to 30% or 40% and especially from 5 or 10% to 30 or 35% of the weight of the composition.

When employed, the ratio of the applied amount of astringent salt of aluminium and/or zirconium to the applied amount of antiperspirant agents according to formula I is preferably from 10:1 to 1000:1 and preferably 100:1 or greater.

Preferred astringent salts of aluminium and/or zirconium are aluminium, zirconium and aluminium/zirconium halides and halohydrate salts, such as chlorohyd rates.

Aluminium halohydrates are usually defined by the general formula AI₂(OH)_xQy-WH₂O in which Q represents chlorine, bromine or iodine, x is variable from 2 to 5 and x + y = 6 while wH₂O represents a variable amount of hydration. Especially effective aluminium halohydrate salts, known as activated aluminium chlorohydrates, are described in EP 006,739 (Unilever PLC and NV). Aluminium halohydrates as described herein are particularly preferred in aerosol compositions. Zirconium actives can usually be represented by the empirical general formula: ZrO(OH)2n-nzBz.wH₂0 in which z is a variable in the range of from 0.9 to 2.0 so that the value 2n-nz is zero or positive, n is the valency of B, and B is selected from the group consisting of chloride, other halide, sulphamate, sulphate and mixtures thereof. Possible hydration to a variable extent is represented by wH₂0. Preferable is that B represents chloride and the variable z lies in the range from 1.5 to 1.87.

The above aluminium and zirconium salts may have coordinated and/or bound water in various quantities and/or may be present as polymeric species, mixtures or complexes. In particular, zirconium hydroxy salts often represent a range of salts having various amounts of the hydroxy group. Zirconium aluminium chlorohydrate may be particularly preferred.

Antiperspirant complexes based on the above-mentioned astringent aluminium and/or zirconium salts can be employed. The complex often employs a compound with a carboxylate group, and advantageously this is an amino acid. Examples of suitable amino acids include dl-tryptophan, dl-phenylalanine, dl- valine, dl-methionine and alanine, and preferably glycine.

Complexes of aluminium halohydrates and zirconium chlorohyd rates together with amino acids such as glycine, which are disclosed in US 3,792,068 (Procter and Gamble Co.) may be employed. Certain of those Al/Zr complexes are commonly called ZAG in the literature. ZAG actives generally contain aluminium, zirconium and chloride with an Al/Zr ratio in a range from 2 to 10, especially 2 to 6, an AI/CI ratio from 2.1 to 0.9 and an amount of glycine.

The proportion of astringent aluminium and/or zirconium salt in a composition normally includes the weight of any water of hydration and any complexing agent that may also be present in the solid active. However, when the active salt is in solution, its weight excludes any water present.

If a composition comprising an astringent salt of aluminium and/or zirconium is in the form of an emulsion the antiperspirant active will be dissolved in the disperse phase. In this case, the antiperspirant active will often provide from 3 to 60% by weight of the aqueous disperse phase, particularly from 10% or 20% up to 55% or 60% of that phase.

Alternatively, a composition comprising an astringent salt of aluminium and/or zirconium may take the form of a suspension in which antiperspirant active in particulate form is suspended in the water-immiscible liquid carrier. Such a composition will generally not have any separate aqueous phase present and may be referred to as "anhydrous" although it should be understood that some water may be present bound to the antiperspirant active. In such compositions, the particle size of the antiperspirant salts often falls within the range of 0.1 to 200 μm with a mean particle size often from 3 to 20 μm.

A further antiperspirant agent may be a polypeptide comprising the amino acid sequence: Glu.Glu.Met.Gln.Arg.Arg.

Other amino acids may also be present in such polypeptides, provided that they do not interrupt the above sequence. It is highly preferred that such polypeptides are water soluble (vide infra), this property enhancing delivery of the polypeptide to its site of action.

Preferred polypeptides of the above type have the specific amino acid sequences:

Glu.Glu.Met.Gln.Arg.Arg.Ala. or

Glu.Glu.Met.Gln.Arg.Arg.Ala.Asp. or

Glu.Glu.Met.Gln.Arg.Arg. A particularly preferred polypeptide of the above type has the amino acid sequence: Glu.Glu.Met.Gln.Arg.Arg. The amino acids in these preferred further antiperspirant agents are typically L-. An example of a polypeptide of this sort, having the N-terminal amino acid acetylated and the C-terminal amino acid amidated, is available under the tradename Argireline^® from Lipotec. It may be represented by the structure Ac-GIu. GIu. Met. Gln.Arg.Arg-NH₂.

A further antiperspirant agent may be a polypeptide comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu. Other amino acids may also be present in such polypeptides, provided that they do not interrupt the above sequence. It is highly preferred that such polypeptides are water soluble (vide infra), this property enhancing delivery of the polypeptide to its site of action.

The stereochemistry of the amino acids of polypeptides comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu. is typically L-, with the exception of the specified alanine amino acid, which is typically D-. Hence, such polypeptides typically comprise the amino acid sequence: L-Tyr.D-Ala.L-Gly.L-Phe.L-Leu.

An especially preferred polypeptide comprising the amino acid sequence:

Tyr.Ala.Gly.Phe.Leu. has the specific amino acid sequence: Tyr.Ala.Gly.Phe.Leu. This pentapeptide is sold by Lipotec as the L-Tyr.D-Ala. L-GIy. L-Phe.L-Leu. stereoisomer under the tradename Leuphasyl.^®

It is preferred that polypeptides comprising the amino acid sequence:

Glu.Glu.Met.Gln.Arg.Arg. or Tyr.Ala.Gly.Phe.Leu. are of 12 amino acid residues or less, more preferably 10 amino acid residues or less, and most preferably 8 amino acid residues or less. It has been found that longer polypeptides have at least the potential for causing undesirable responses on application to the human body. A polypeptide comprising the amino acid sequence: Glu.Glu.Met.GIn.Arg.Arg. or Tyr.Ala.Gly.Phe.Leu., when employed, is preferably incorporated into a composition in an amount of from 0.0005 to 1 %, particularly from 0.001 to 0.5%, and especially from 0.005 to 0.2% by weight of the composition.

A further antiperspirant agent may be a calcium channel blocking agent, as described for example in WO 02/11690 (Unilever, et al).

In order for a substance to be recognised as a calcium channel blocking agent, it should be able to reduce the intracellular calcium concentration or to reduce the binding of calcium to intracellular proteins, such as calmodulin, as described, for example, in Galizzi et al, J. Biol. Chem., 262, 6947, 1987; Okamiya et al, Eur. J. Pharmacol., 205, 49, 1991 ; Wagner et al, J. Neurosci., 8, 3354, 1988; lee et al, Life Sci., 35, 721 , 1984; Schoemaker and Langer, Eur. J. Pharmacol., 111 , 273, 1985; or Reynolds et al, J. Pharmacol. Exp. Ther., 237, 731 , 1986.

When employed, calcium channel blocking agents are preferably incorporated into a composition in an amount of from 0.1 to 250 mmol.kg^"1 the composition.

Preferred calcium channel blocking agents suitable for use as a further antiperspirant agent are magnesium salts, in particular magnesium gluconate. Such agents are typically employed in compositions at a level of from 0.01 to 1 % by weight of the total composition.

The second aspect of the present invention involves the use of an antiperspirant agent according to formula I together with an anti-microbial deodorant agent. Good antiperspirancy and deodorancy benefits may be achieved by such use.

When the antiperspirant agent according to formula I is used in conjunction with an anti-microbial deodorant agent, it is not essential that the two are part of the same composition. Independent application of the two materials may be employed. Such application may be concurrent or consecutive, provided that the treated surface experiences the presence of both materials. When the agents are applied from independent compositions, it is preferred that the product also comprises a means for, and/or instruction for, both of the compositions to be applied to the surface requiring treatment.

Compositions comprising both an antiperspirant agent according to formula I and an anti-microbial deodorant agent represent a preferred aspect of the present invention.

The anti-microbial deodorant agent may be a bacteriocidal agent or a bacteriostatic agent.

A particularly suitable anti-microbial deodorant agent is an astringent salt of aluminium and/or zirconium, as described above. Such anti-microbial deodorant agents are particularly suitable because they may also function as addition antiperspirant agents (vide supra).

Suitable anti-microbial deodorant agents may be organic in nature and such antimicrobial deodorant agents are particularly preferred in compositions that do not comprise an astringent salt of aluminium and/or zirconium.

When employed, the anti-microbial deodorant agent is typically incorporated into a composition at from 0.01 % to 3% and particularly at from 0.03% to 0.5%.

Preferred anti-microbial deodorant agents have a minimum inhibitory concentration (MIC) of 1 mg.ml^"1 or less, particularly 200 μg.ml^"1 or less, and especially 100 μg.ml^"1 or less. The MIC of an anti-microbial agent is the minimum concentration of the agent required to significantly inhibit microbial growth. lnhibition is considered "significant" if an 80% or greater reduction in the growth of an inoculum of Staphylococcus epidermidis is observed, relative to a control medium without an anti-microbial agent, over a period of 16 to 24 hours at 37⁰C. Details of suitable methods for determining MICs can be found in "Antimicrobial Agents and Susceptibility Testing", C.Thornsberry, (in "Manual of Clinical

Microbiology", 5^th Edition, Ed. A. Balows et al, American Society for Microbiology, Washington D. C, 1991 ). A particularly suitable method is the Macrobroth Dilution Method as described in Chapter 110 of above publication (pp. 1101 -1111 ) by D. F. Sahm and J. A. Washington II. MICs of anti-microbials suitable for inclusion in the compositions of the invention are thclosan: 0.01 -10 μg.ml^"1 (J.Regos et al., Dermatologica (1979), 158: 72-79) and farnesol: ca. 25 μg.ml^"1 (K. Sawano, T. Sato, and R. Hattori, Proceedings of the 17^th IFSCC International Conference, Yokahama (1992) p.210-232). By contrast ethanol and similar alkanols have MICs of greater than 1 mg.ml^"1.

Suitable organic anti-microbials are bactericides, for example quaternary ammonium compounds, like cetyltrimethylammonium salts; chlorhexidine and salts thereof; and diglycerol monocaprate, diglycerol monolaurate, glycerol monolaurate, and similar materials, as described in "Deodorant Ingredients", S.A.Makin and M.R.Lowry, in "Antiperspirants and Deodorants", Ed. K. Laden (1999, Marcel Dekker, New York). More preferred anti-microbials for use in the compositions of the invention are polyhexamethylene biguanide salts (also known as polyaminopropyl biguanide salts), an example being Cosmocil CQ™ available from Zeneca PLC, preferably used at up to 1 % and more preferably at 0.03% to 0.3% by weight; 2',4,4'-thchloro,2-hydroxy-diphenyl ether (thclosan), preferably used at up to 1 % by weight of the composition and more preferably at 0.05-0.3%; and 3,7,11 -trimethyldodeca-2, 6,10-thenol (farnesol), preferably used at up to 1 % by weight of the composition and more preferably at up to 0.5%. Other suitable organic antimicrobial agents are transition metal chelators, as described in WO01/52805, for example. Transitional metal chelators having a binding coefficient for iron(lll) of greater than 10²⁶, for example diethylenetriaminepentaacetic acid and salts thereof are preferred.

Other components may also be present in compositions used in accordance with the present invention. Often, for example, water may be present in a composition comprising the polypeptide. In such compositions, the water may be considered as a carrier fluid. Other carrier materials may alternative or additionally be employed, provided that they are cosmetically acceptable.

The other components used in compositions suitable for use in accordance with the invention will vary according to the desired mode of application of the composition. For example, a volatile propellant is a typical component in compositions for spray application and a liquid carrier fluid (usually water) is a typical component in compositions for roll-on application.

A liquid carrier fluid is a highly desirable additional component. Such materials act as solvents or carriers for the other components of the composition, facilitating their delivery. Water can be used as a carrier fluid, although it is more preferable to use mixtures of water and an alcohol, especially ethanol. Alcohol/water mixtures are particularly suitable carrier fluids in roll-on and pump spray products. Cyclomethicones and other volatile silicones are another class of carrier fluid that may be employed. Examples of this latter class are Dow Corning silicone fluids 344, 345, 244, 245, 246, 556, and the 200 series; Union Carbide Corp. silicones 2707 and 7158; and General Electric silicone SF1202. Alternatively, non-silicone hydrophobic liquids may be employed, such as mineral oils, hydrogenated polyisobutene, polydecene, paraffins, isoparaffins of at least 10 carbon atoms, and aliphatic and aromatic ester iols. Propylene glycol, butylene glycol, and related glycols may also be used. Other alternative carrier fluids include materials having multiple functions, for example isopropyl myristate, isopropyl palmitate, dipropylene glycol, and glycerol. Mixtures of carrier fluids may also be employed to advantage. Compositions preferably comprise carrier fluid at a level of from 30% to 98% by weight, or more preferably from 60% to 97% by weight, of the non- volatile components of the composition.

Emulsifiers are further additional components of the compositions of the invention that are highly desirable in certain product forms. Emulsifiers are preferably present at from 0.1 % to 10% by weight of the composition. Suitable emulsifiers include steareth-2, steareth-20, steareth-21 , ceteareth-20, glyceryl stearate, cetyl alcohol, cetearyl alcohol, PEG-20 stearate, and dimethicone copolyol.

Further emulsifiers desirable in certain compositions of the invention are perfume solubilisers and wash-off agents. Examples of the former include PEG- hydrogenated castor oil, available from BASF in the Cremaphor RH and CO ranges, preferably present at up to 1.5% by weight, more preferably 0.3 to 0.7% by weight. Examples of the latter include poly(oxyethylene) ethers.

Certain sensory modifiers are further desirable components. Such materials are preferably used at a level of up to 20% by weight of the composition. Emollients, humectants, volatile oils, non-volatile oils, and particulate solids which impart lubricity are all suitable classes of sensory modifiers. Examples of such materials include cyclomethicone, dimethicone, dimethiconol, isopropyl myristate, isopropyl palmitate, talc, finely-divided silica (eg. Aerosil 200), particulate polyethylene (eg. Acumist B18), polysaccharides, corn starch, C12-C15 alcohol benzoate, PPG-3 myhstyl ether, octyl dodecanol, C7-C14 isoparaffins, di-isopropyl adipate, isosorbide laurate, PPG-14 butyl ether, glycerol, hydrogenated polyisobutene, polydecene, titanium dioxide, phenyl thmethicone, dioctyl adipate, and hexamethyl disiloxane. Fragrance is also a desirable additional component. Suitable materials include conventional perfumes, such as perfume oils and also include so-called deo- perfumes, as described in EP 545,556 and other publications. Levels of incorporation are preferably up to 4% by weight, particularly from 0.1 % to 2% by weight, and especially from 0.7% to 1.7% by weight.

It should be noted that certain components of compositions perform more than one function. Such components are particularly preferred additional ingredients, their use often saving both money and formulation space. Examples of such components include ethanol, isopropyl myristate, and the many components that can act sensory modifiers.

Further additional components that may also be included are colourants and preservatives at a conventional concentration, for example C1-C3 alkyl parabens.

In compositions comprising an antiperspirant agent according to formula I and one or more additional antiperspirant agent selected from the group consisting of: a. Polypeptides comprising the amino acid sequence:

Glu.Glu.Met.Gln.Arg.Arg.; b. Polypeptides comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu.; c. Calcium channel blocking agents; and d. lamellar phase stabilised oil-in-water emulsion; it is highly preferred to also have a preservative agent present. The preservative agent present in such compositions may be selected from phenoxyethanol, typically at from 0.1 to 1 %; 3-iodo-2-propynylbutylcarbamate (IPBC), typically at from 0.0025 to 0.025%; dimethylol-5,5-dimethylhydantoin [1 ,3-bis(hydroxymethyl)- 5,5-dimethyl-imidazolidine-2,4-dione], typically at from 0.05 to 0.4%; or methylisothiazoline, typically at from 0.01 to 0.1 %; all percentages being by weight of the total composition. Mixtures of two or more of the above preservatives may also be employed.

Examples

The compositions indicated in Table 1 were prepared using methods known in the art. For three consecutive days, trained operators applied, in the morning, Composition 1 to a first axilla of panellists and nothing to their other axilla. After a 4 hour gap, Composition 1 was re-applied to the first axilla of the panellists and, after allowing the composition to dry for up to 30 minutes, Composition 2 was applied on top of this. Composition 2, by itself, was also applied in the afternoon to the other axilla of the panellists as a control. Each composition was applied at a level of approximately 0.3g per application. Conventional roll-ball applicators were used for the applications. 24 hours after the last application, panellists were required to sit in a hot room (temperature: 4O⁰C; relative humidity: 40%) for up to one hour and twenty minutes. During the sitting, sweat was collected on absorbent cotton pads held in each axilla.

Table 1

^* "Dab" = diaminobutyroylbenzylamide. The 4% amount refers to the 0.25% w/w solution of SYN-^®AKE in glycerol/water (70/30 by wt.) supplied by

Pentapharm. Hence, the actual amount of β-Ala-Pro-Dab present in the composition was 0.01 % w/w. ** Sunflower seed oil.

Application of Composition 1 in addition to Composition 2 was found to lead to an additional 8.9% sweat weight reduction (SWR) above that of Composition 2 alone, a difference significant at the 95% level. This is a particularly surprising result in light of the high antiperspirant efficacy of compositions like Composition 2. Compositions comprising 15% ACH typically give approximately 40% SWR in tests of the above type, when compared with non-antiperspirant compositions.

Composition 1 from Table 1 was also evaluated using an amended version of the above protocol. Trained operators applied the composition to a first axilla of panellists once each day for four consecutive days in week one and then for three consecutive days in week two (ca. 0.3g per axilla). A control composition was applied to the panellists' second axilla. The panellists self-applied at home at the weekend in between the two test weeks. A conventional roll-ball applicator was used for the applications. At intervals during the test, panellists were required to sit in a hot room (temperature: 4O⁰C; relative humidity: 40%) for up to one hour and twenty minutes. During the sittings, sweat was collected on absorbent cotton pads held in each axilla and the amount produced was recorded.

Hot room sittings were done after the periods indicated in Table 2. The final sitting was done 96 hours after the final applications, the panellists being allowed to wash as normal during the intervening period. Table 2 indicates the "Sweat Weight Reduction (SWR)" achieved by Composition 1 relative to the control composition (which was a simple ethanolic deodorant, lacking any antiperspirant active).

Table 2

Time after initial application. Hot room sittings done before application on days 4 and 7.

All of the indicated SWRs were statistically significant. Particularly surprising was the benefit after the 4 day "wash out" period.

Claims

1. A method of reducing perspiration comprising the application of an antiperspirant agent according to formula I: R¹-NH-CH(R²)-[CHR⁶]_n-CO. N-CH-CO. NH-CH-[CH₂]₃-_n-NHR⁴

/ \ \

H₂C-CH₂-CH₂ CO.XR³ wherein:

X = a bond or NH-CH([CH₂]_3+n-NHR⁵)-CO.; n = 0, 1 or 2;

R¹ R⁴ and R⁵ independently = H, optionally substituted Cβ alkyl, amidino or tetra CrCβ alkylamidinium;

R² = H or optionally substituted Cβ alkyl, or R¹ and R² together with the group to which they are bonded form a 5- to 7-membered saturated ring; R³ = Ci-Ci₂ alkoxy, CrCi₂ alkylamino, optionally substituted aryl CrC₆ alkylamino, optionally substituted heteroaryl C1-C6 alkylamino, optionally substituted aryl CrC₆ alkoxy, or optionally substituted heteroaryl CrC₆ alkoxy; and

R⁶ = H or, when n = 1 , amino, or together with R1 and the group to which R6 and R1 are bonded, a 5- to 7-membered saturated ring and one or more additional antiperspirant agent selected from the group consisting of: a. astringent salts of aluminium or zirconium; b. polypeptides comprising the amino acid sequence: Glu.Glu.Met.Gln.Arg.Arg.; c. polypeptides comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu.; d. calcium channel blocking agents; and e. lamellar phase stabilised oil-in-water emulsion.

2. A method of reducing perspiration according to claim 1 , comprising the application of an astringent salts of aluminium or zirconium.

3. A method of reducing perspiration according to claim 1 , comprising the application of a polypeptide comprising the amino acid sequence:

Glu.Glu.Met.Gln.Arg.Arg.

4. A method of reducing perspiration according to claim 1 , comprising the application of a polypeptide comprising the amino acid sequence: Tyr.Ala.Gly.Phe.Leu.

5. A method of reducing perspiration according to claim 1 , comprising the application of a calcium channel blocking agent.

6. A method according to any of the preceding claims comprising the application of β-Ala-Pro-diaminobutyroylbenzylamide.

7. A method according to any of the preceding claims comprising the application of lamellar phase stabilised oil-in-water emulsion.

8. A method of reducing perspiration and body odour comprising the application of an antiperspirant agent according to formula I and an antimicrobial deodorant agent.

9. A method according to claim 8, comprising the application of an organic anti-microbial deodorant agent.

10. A deodorant antiperspirant composition comprising an antiperspirant agent according to formula I, an anti-microbial deodorant agent and a cosmetically acceptable carrier material.

11. A deodorant antiperspirant composition according to claim 10, comprising water as a carrier fluid.