WO2018158042A1 - Composition antitranspiration - Google Patents

Composition antitranspiration Download PDF

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Publication number
WO2018158042A1
WO2018158042A1 PCT/EP2018/052775 EP2018052775W WO2018158042A1 WO 2018158042 A1 WO2018158042 A1 WO 2018158042A1 EP 2018052775 W EP2018052775 W EP 2018052775W WO 2018158042 A1 WO2018158042 A1 WO 2018158042A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
acid
value
compositions
antiperspirant
Prior art date
Application number
PCT/EP2018/052775
Other languages
English (en)
Inventor
Renjiang LIU
Huanjun ZHOU
Original Assignee
Unilever N.V.
Unilever Plc
Conopco, Inc., D/B/A Unilever
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Unilever N.V., Unilever Plc, Conopco, Inc., D/B/A Unilever filed Critical Unilever N.V.
Publication of WO2018158042A1 publication Critical patent/WO2018158042A1/fr

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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds thereof
    • 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
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • 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
    • A61K8/60—Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q15/00—Anti-perspirants or body deodorants

Definitions

  • the present invention is in the field of compositions comprising antiperspirant actives, particularly cosmetic compositions.
  • the present invention more particularly relates to compositions comprising titanium based antiperspirant actives which are stable before use and effective in ensuring anti perspirancy for a long period of time after the product is applied on to the body by the consumer. Background of the invention
  • the present invention relates to compositions, such as those that contain antiperspirant actives. These actives are added to compositions to reduce perspiration on application to the surface of the body, particularly to the underarm regions of the human body viz. the axilia.
  • Antiperspirant actives are typically astringent metal salts such as those of aluminium or zirconium salts. Antiperspirant actives are usually incorporated in compositions at low pH, in the range of 2 to 7. It has also been proposed in the past that salts of titanium may be used but these have not been commercially exploited so far due to technical difficulties in formulating as well as delivering them to have sufficient sustained efficacy when in use.
  • US3090728 (Carter Products, 1963) discloses an antiperspirant composition
  • an oil-water emulsion vehicle having dissolved therein an antiperspirant agent selected from the group consisting of titanic acid complexes of hydroxy aliphatic carboxylic acids having from 2 to 6 carbon atoms and mixtures thereof, said composition having a pH in the range of about 2.5 to 5.
  • EP0586235 discloses an antiperspirant composition suitable for topical application to the human skin, comprising an effective amount of a titanium salt of a hydroxy aliphatic carboxylic acid having a chain length of from C2 to C10, the composition having a pH in aqueous solution of greater than 5.
  • GB2299506 discloses an antiperspirant composition for topical application to the human skin, comprising effective amount of a titanium salt selected from the group consisting of a straight or branched chain saturated or unsaturated non- hydroxy C2-C20 carboxylic acid, C7-C12 aromatic carboxylic acids, ethanolamine complexes, and C4-C12 aliphatic polyols, in a cosmetically suitable vehicle.
  • a titanium salt selected from the group consisting of a straight or branched chain saturated or unsaturated non- hydroxy C2-C20 carboxylic acid, C7-C12 aromatic carboxylic acids, ethanolamine complexes, and C4-C12 aliphatic polyols, in a cosmetically suitable vehicle.
  • the present inventors have tested the titanium salts proposed in the past for anti- perspirancy benefits and discovered that they suffer either from being unstable when formulated or do not provide the desired benefit for the long period of time after application on the body as desired by the consumer, or both of these problems.
  • the antiperspirant active does not degrade when formulated and stored for periods of time (sometimes up to several months) before they are used by the consumer.
  • the formulated product When the formulated product is applied to the skin it is desired that the antiperspirant active hydrolyses in the aqueous saline media of sweat to form particles of the right size such that it can clog or gel in the sweat pores and inhibit further sweating.
  • This rate of hydrolysis to form the particles should not be too fast, else the efficacy is experienced by the consumer only for a few seconds or minutes. It is desirable that the antiperspirant benefit is experienced over several hours.
  • the hydrolysis kinetics should be such as to enable the reaction to occur slowly over a matter of several hours.
  • an antiperspirant composition with a pH in the range of 3 to 7 comprising
  • a, b and c each independently have a value of from 0 to 3; d and e each independently have a value from 0 to 10;
  • m has a value from 1 to 18;
  • n has a value from 0 to 9;
  • a+b+c has a value from 1 to 3;
  • d+e has a value from 4 to 10 and
  • m+n has a value from 1 to 18;
  • the ligands present in the titanium organosalt are selected from triethanolamine, diethanolamine or monoethanolamine, most preferably trioethanol amine.
  • Preferred titanium compounds have the following structures.
  • the pH of the composition is from 4 to 7.
  • a method of reducing perspiration comprising the step of applying a composition as claimed in the first aspect on to the desired skin surface.
  • compositions of the invention are typically “personal care compositions", suitable for cosmetic use as detailed below. Further, use of the compositions of the invention is typically cosmetic, non-therapeutic use.
  • compositions may be used for the therapeutic treatment of hyperhidrosis (extreme sweating).
  • composition is meant to include a composition for topical application to the skin of mammals, especially humans.
  • a composition is preferably of the leave-on type.
  • a leave-on composition is meant a composition that is applied to the desired skin surface and left on for a period of time (say from one minute to 24 hours) after which it may be wiped or rinsed off with water, usually during the regular course of personal washing.
  • the composition may also be formulated into a product which is applied to a human body for improving the appearance, cleansing, odor control or general aesthetics.
  • composition of the present invention can be in the form of a liquid, lotion, cream, foam, scrub, gel or stick form and may be delivered through a roll-on device or using a propellant containing aerosol can. It is especially useful for delivering low pH compositions to the axilla of an individual for anti-perspirancy benefits.
  • "Skin” as used herein is meant to include skin on any part of the body (e.g., neck, chest, back, arms, underarms, hands, legs, buttocks and scalp) especially the underarms.
  • the present invention is directed to delivering a titanium based antiperspirant active on to the topical surface of a human body.
  • the active for inclusion in the composition is a titanium compound chelated by alkanolamine having the chemical formula 1 Ti (N)a (NH)b (NH 2 )c Od (OH) e (CH 2 )m (CHs)n
  • a, b and c each independently have a value of from 0 to 3;
  • d and e each independently have a value from 0 to 10;
  • m has a value from 1 to 18;
  • n has a value from 0 to 9;
  • the titanium organo salt is preferably a titanium alkanolamine complex wherein the ligands is preferably selected from a triethanolamine, a diethanolamine or a monoethanolamine.
  • Titanium 2,2,2 - nitrilotrisethanolate ( CAS number: 15879-01 -3) having the following structure:
  • Titanium 2,2,2 - nitrilotrisethanolate (having CAS number: 15879-01 -3) is the most preferred titanium alkanolamine chelated complex, as per this invention (compound of formula 2). It is usually supplied dispersed in isopropanol as thick light yellowish liquid.
  • One major supplier is Dorf Ketal.
  • the aqueous dilution is alkaline due to the presence of triethanolamine. In the chemical industry, it has normally been used as a crosslinker, a catalyst, or a coating adhesion enhancer.
  • the above titanium compound (of formula 1 ) is preferably included in 0.5 to 30%, more preferably 1 to 15%, further more preferably 3 to 10% by weight of the composition.
  • the composition comprises an acid.
  • the acid may be a mineral acid or an organic acid, preferably a mineral acid.
  • the mineral acid for inclusion in the composition is preferably selected from hydrochloric acid, nitric acid, phosphoric acid or sulphuric acid, more preferably hydrochloric acid or nitric acid.
  • the composition of the invention may alternately comprise an organic acid, preferably a carboxylic acid.
  • Carboxylic acids which may be included are oxalic acid, malonic acid, adipic acid, maleic acid, fumaric acid, glycolic acid, lactic acid, salicylic acid, citric acid, tartaric acid, gluconic acid, or malic acid.
  • Particularly preferred carboxylic acids are tartaric acid, oxalic acid, lactic acid or citric acid.
  • the acid may be included in 0.01 to 10%, preferably in 0.01 to 7%, more preferably from 0.1 to 1.5% by weight of the composition.
  • the composition of the invention comprises a polyhydric alcohol.
  • Polyhydric alcohol is also referred to in short as polyol.
  • a polyhydric alcohol as per the present invention is a compound having two or more hydroxyl groups.
  • Suitable class of polyhydric alcohols that may be included in the composition of the invention are monomeric polyols, polyalkylene glycols or sugars. Preferred monomeric polyols are glycol, propylene glycol, glycerol or xylitol.
  • Suitable polyalkylene glycols are polyethylene glycol or polypropylene glycol.
  • Polyethylene glycol has the structure as given below
  • n is preferably from 4 to 10.
  • Sugars for inclusion in the invention could be monomeric, dimeric, trimeric or of the polymeric form.
  • Preferred sugars include glucose, fructose, mannose, sucrose, threitol, erythritol, sorbitol, mannitol, galactitol, adonitol, dextran, or cyclodextrin.
  • the more preferred sugars are glucose, fructose, sucrose, sorbitol, mannitol, adonitol, dextran, or cyclodextrin.
  • the structure of the above compounds are:
  • the most preferred ones for inclusion in the composition of the invention are glycerol, glucose, sorbitol or xylitol.
  • the polyhydric alcohol is preferably included in 0.01 to 50%, preferably 0.1 to 15% by weight of the composition.
  • the inventors believe that there are two steps necessary to ensure the long lasting benefits afforded by the present invention. It is essential to have the composition formulated and delivered at a low pH in the range of 3 to 7 preferably 4 to 7 further more preferably 5 to 7 in order for the formulation to be stable, effective and safe. This is ensured by including therein an acid so that the desired pH of the composition is quickly attained when the composition is formulated and further when the composition is diluted in the presence of sweat. Once inside the sweat gland, it is believed that the prepared titanium complex crosslinks with mucin, protein or other components inside the gland thereby forming a gel network which clogs the pores of the sweat glands thereby ensuring antiperspirant benefit for a long period of time.
  • the mole ratio of the titanium compound to the polyhydric alcohol is in the range of 1 :0.01 to 1 :15, preferably 1 :0.03 to 1 :1 . It is also particularly preferred that the mole ratio of the titanium compound to the acid is in the range of 1 :0.1 to 1 :15, preferably 1 :1 to 1 :5. If the polyhydric alcohol level is too high, the composition is too stable to be hydrolysed by sweat; if the acid level is too high, the composition has a tendency to destabilise in a shorter period of time.
  • Antiperspirant compositions of the present invention may advantageously comprise an additional, non-titanium, antiperspirant active.
  • this might be a conventional antiperspirant salt comprising Al and/or Zr, such as aluminium chlorohydrate or aluminium-zirconium chlorohydrate optionally complexed with glycine, it is preferred that any additional antiperspirant active is not of this type.
  • compositions of the present invention may also be incorporated in the compositions of the present invention.
  • Such components include skin care agents such emollients, humectants and skin barrier promoters; skin appearance modifiers such as skin lightening agents and skin smoothing agents; antimicrobial agents, in particular organic anti-microbial agents, and preservatives.
  • the anti-perspirant active can be applied cosmetically and topically to the skin, broadly speaking, by one of two methods. Different consumers prefer one method or the other. In one method, sometimes called a contact method, a composition is wiped across the surface of the skin, depositing a fraction of the composition as it passes. In the second method, sometimes called the non-contact method, the composition is sprayed from a dispenser held proximate to the skin, often in an area of about 10 to 20 cm 2 .
  • the spray can be developed by mechanical means of generating pressure on the contents of the dispenser, such as a pump or a squeezable sidewall or by internally generated pressure arising from a fraction of a liquefied propellant volatilising, the dispenser commonly being called an aerosol.
  • the carrier fluid comprises a solvent for the antiperspirant and in a second variation, the antiperspirant remains a particulate solid that is suspended in an oil, usually a blend of oils.
  • gellant for a continuous oil phase
  • materials including waxes, small molecule gelling agents and polymers. They each have their advantages and of them, one of the most popular class of gellant has comprised waxes, partly at least due to their ready availability and ease of processing, including in particular linear fatty alcohol wax gellants.
  • a gelled antiperspirant composition is applied topically to skin by wiping it across and in contact with the skin, thereby depositing on the skin a thin film.
  • the nature of the film depends to a significant extent on the gellant that is employed.
  • wax fatty alcohols have been employed as gellant for many years, and are effective for the purpose of gelling, the resultant product is rather ineffective at improving the visual appearance of skin, and in particular underarm skin, to which the composition has been applied.
  • This problem has been solved by including ameliorating materials for example, di or polyhydric humectants and/or a triglyceride oil.
  • Liquid compositions that are applicable from a roll-on broadly speaking can be divided into two classes, namely those in which an antiperspirant active is suspended in a hydrophobic carrier, such as a volatile silicone and those in which the antiperspirant active is dissolved in a carrier liquid.
  • a hydrophobic carrier such as a volatile silicone
  • the antiperspirant active is dissolved in a carrier liquid.
  • the latter has proven to be more popular.
  • dissolving carrier liquid namely carriers that are predominantly alcoholic, which is to say the greater part of the dissolving carrier fluid comprises ethanol and the second class in which the carrier liquid is mainly water.
  • the former was very popular because ethanol is a mild bactericide in its own right, but its popularity waned because it stings, especially if the surface onto which the composition has been applied has been damaged or cut, such as can easily arise during shaving or other de-hairing operations.
  • the second class of formulations that is an alternative to alcoholic formulations comprise a dispersion of water-insoluble or very poorly water soluble ingredients in an aqueous solution of the antiperspirant.
  • emulsions Such compositions will be called emulsions.
  • Antiperspirant roll-on emulsions commonly comprise one or more emulsifiers to maintain a distribution of the water-soluble ingredients. Aerosol compositions
  • the antiperspirant composition may be delivered through an aerosol composition which comprises a propellant in addition to the other ingredients described hereinabove.
  • the propellant is employed in a weight ratio to the base formulation of from 95:5 to 5:95.
  • the ratio of propellant to base formulation is normally at least 20:80, generally at least 30:70, particularly at least 40:60, and in many formulations, the weight ratio is from 90:10 to 50:50.
  • a ratio range of from 70:30 to 90:10 is sometimes preferred.
  • Propellants herein generally are one of three classes; i) low boiling point gasses liquifided by compression, ii) volatile ethers and iii) compressed non-oxidising gases.
  • Class i is conveniently a low boiling point material, typically boiling below -5°C, and often below -15°C, and in particular, alkanes and/or halogenated hydrocarbons.
  • This class of propellant is usually liquefied at the pressure in the aerosol canister and evaporates to generate the pressure to expel the composition out of the canister. Examples of suitable alkanes include particularly propane, butane or isobutane.
  • the second class of propellant comprises a very volatile ether of which the most widely employed ether hitherto is dimethyl ether. This propellant can advantageously be employed at relatively low weight ratio of propellant to base formulation, for example to as low as 5:95. It can also be employed in admixture with, for example, compressible/liquefiable alkane gasses.
  • the third class of propellant comprises compressed non-oxidising gasses, and in particular carbon dioxide or nitrogen. Inert gases like neon are a theoretical alternative.
  • the topically acceptable carrier comprises a hydrophobic carrier or an aqueous carrier.
  • the hydrophobic carrier in such cases may comprise a silicone compound, low boiling alcohol or a wax.
  • the composition comprises a propellant it is delivered as an aerosol.
  • composition of the present invention can comprise a wide range of other optional components.
  • CTFA Personal care Ingredient Handbook Second Edition, 1992, which is incorporated by reference herein in its entirety, describes a wide variety of non- limiting personal care and pharmaceutical ingredients commonly used in the skin care industry, which are suitable for use in the compositions of the present invention. Examples include: antioxidants, binders, biological additives, buffering agents, colorants, thickeners, polymers, astringents, fragrance, conditioners, exfoliating agents, pH adjusters, preservatives, natural extracts, essential oils, skin sensates, skin soothing agents, and skin healing agents.
  • the present invention also provides for a method of reducing perspiration comprising the step of applying the composition of the first aspect on to the desired skin surface.
  • the skin surface could be any topical surface which is prone to sweating especially the axilla i.e. the underarm portion of the human body.
  • the method is preferably non-therapeutic.
  • the invention also provides for use of the titanium compound having the chemical formula 1 , for manufacture of a composition as claimed in the present invention, for reduction of sweat.
  • the invention also provides for use of a titanium compound according Formula 1 as an antiperspirant active.
  • a titanium compound according Formula 1 as an antiperspirant active.
  • Examples A-B and 1 -6 Stability of compositions at room temperature over one week storage.
  • a The titanium compound used was the compound of formula 2.
  • compositions were tested for stability by using the following procedure: 2 g of the titanium compound was weighed then added into 30 ml of de-ionised water in a beaker and stirred well. Certain amount of polyol (according to the dosage in Table 1 ) were added dropwise with stirring. Afterwards, required dose (according to Table 1 ) of the acid was added dropwise slowly. The rest of the water was added to reach a total of 40 g system. The composition was further stirred for another 10 minutes.
  • Example B is acceptable as far as stability is concerned but is found to be
  • compositions are stable when stored but hydrolyse to form an insoluble complex soon after they come in contact with sweat on the human body. These particulates would then be expected to clog or gel in the sweat pores thereby acting as antiperspirants.
  • Table - 3 indicates that compositions as per the invention 1 to 6 are transparent on application but get cloudy on storage.
  • Examples 1 ,2,4,5 Quantification of cloudiness by measurement of the particles size The cloudiness of select compositions as per the invention was quantified by measuring the increase of particle size with time and the data for the various compositions is given below.
  • Table - 1 lists the various compositions and Table -4 the measured particle size. The particle size was measured using the following procedure:
  • DLS (Dynamic light scattering) Particle size tracking The compositions were diluted four times to give better DLS signaling and 0.09g NaCI was added to 10ml composition system before the test (0.9% wt NaCI). The samples were transferred into disposable sizing cuvette and placed into DLS Nanosizer (Malvern Zetasizer Nano ZS). The mean volume size of the titanium dioxide particles were measured with at least two repeats at each time point at room temperature (25 °C).
  • Example 7 A Roll-on formulation.
  • Natrosol 250HHR is a hydroxyethylcellulose and is included here as a thickener.
  • the above formulation was stored for over four weeks at room temperature and was found to be stable.
  • pH The pH of the compositions was measured with at least two repeats at room temperature (25 °C).
  • compositions according to the invention (Example 2 and 7) have a pH in the range of 3 to 7, as desired for stable, effective and safe application.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
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  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne le domaine des compositions antitranspiration, en particulier des compositions comprenant des agents actifs antitranspiration. La présente invention concerne plus particulièrement des compositions comprenant des agents actifs antitranspiration à base de titane qui sont stables avant utilisation et efficaces pour assurer un effet antitranspiration de longue durée. Ceci est obtenu par la formulation de l'agent actif antitranspiration dans une base topiquement acceptable en présence d'un acide et d'un alcool polyhydrique.
PCT/EP2018/052775 2017-02-28 2018-02-05 Composition antitranspiration WO2018158042A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2017075136 2017-02-28
CNPCT/CN2017/075136 2017-02-28
EP17164909 2017-04-05
EP17164909.8 2017-04-05

Publications (1)

Publication Number Publication Date
WO2018158042A1 true WO2018158042A1 (fr) 2018-09-07

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PCT/EP2018/052775 WO2018158042A1 (fr) 2017-02-28 2018-02-05 Composition antitranspiration

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3090728A (en) 1957-02-20 1963-05-21 Berger Frank Milan Titanic acid complexes of hydroxy aliphatic carboxylic acids antiperspirant compostions
EP0586235A2 (fr) 1992-09-04 1994-03-09 Unilever Plc Antiperspirants contenant des sels de titane et compositions
GB2299506A (en) 1995-04-03 1996-10-09 Unilever Plc Antiperspirant composition comprising titanium

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3090728A (en) 1957-02-20 1963-05-21 Berger Frank Milan Titanic acid complexes of hydroxy aliphatic carboxylic acids antiperspirant compostions
EP0586235A2 (fr) 1992-09-04 1994-03-09 Unilever Plc Antiperspirants contenant des sels de titane et compositions
GB2299506A (en) 1995-04-03 1996-10-09 Unilever Plc Antiperspirant composition comprising titanium

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"The CTFA Personal care Ingredient Handbook", 1992

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