JPH06183989A - Antiurease cosmetics or dermatologic composition - Google Patents

Abstract

PURPOSE: To provide an antisweating agent or preventive compsn. against diaper dermatitis which contains natural or synthetic substance as an effective component and has good appearance and texture compared to a conventional ointment compsn. CONSTITUTION: This antiurease cosmetic product or dermatologic comspn. contains an effective amt. of condensed tannin and chlorogenic acid deriv. of locust bean or hamamelis in combination with a proper cosmetic base. More particularly, the compsn. is an antisweating agent and a preventive comspn. against diaper dermatitis.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to anti-urease cosmetic or dermatological compositions.

[0002]

BACKGROUND OF THE INVENTION The decomposition of urea by urease to produce ammonia plays an important role in sweating and diaper rash. In the particular case of diaper eruptions, the pH starts to increase, although not directly due to the production of ammonia, which promotes increased stool lipase and protease activity, which in turn leads to skin irritation.

A number of measures have been taken to solve the problem of diaper rash. Disposable diapers have been introduced that guarantee maximum absorption. The utility of over-the-counter drugs and cosmetics is to calm the dermatitis of the buttocks. These products include protective agents (some of which are dangerous to use), disinfectants, anti-inflammatory agents (only available in formulations) or buffer systems (ammonia and acids produced by bacterial degradation). Simple neutralization of) is included.

However, the above-mentioned known solutions are limited in that the effect of the enzyme activity is reduced without attacking the cause of the activity.

Moreover, some anti-urease agents are effective against erythema of the buttocks, for example hydroxamic acid (see, for example, JP-A-57-104276) and hydroxamic acid (for example, JP-A-57-104276). It is known to be active as a deodorant, including S.A. More generally, polyhydroxyphenols and quinones are known for their anti-urease activity (see, eg, HJ Michel, Die.
Pharmazie ", No. 2, February 1
980, page 66, paragraph 6), but there is no literature on its use in the treatment of diaper rash or as an antiperspirant.

[0006]

The problem posed by the present invention is to provide an antiperspirant or antidiaper rash composition whose active ingredient is of natural or synthetic origin, in the latter case, It is a compound found in nature or a compound that is resynthesized. In the case of an anti-diaper rash composition,
The problem is also to provide those which have a more pleasing appearance and feel than the known anti-erythma compositions in the form of pharmaceutical ointments.

[0007]

Accordingly, the present invention relates to an anti-urease cosmetic or dermatological composition containing an effective amount of an anti-urease agent selected from condensed locust methanenin and chlorogenic acid derivatives.

In the present invention, condensed locust bean methanine consists of a more complex form of gallic acid containing a gallic acid ester or depside bond (a bond between two galloyl groups) and glucose. Condensed tannins of witch hazel are composed of gallic acid esters or the more complex forms of gallic acid and hamamelose described above. These tannins may be in the form of somewhat purified plant extracts.

Chlorogenic acid derivatives are cafe oils,
Dicaffeoyl, feruloyl, coumaroyl and caffeoyl feruloyl quinic acid and the corresponding quinides (lactones of quinic acid). These derivatives may be in the form of natural botanical extracts, such as coffee or citrus thistle extract, or in synthetic form. The preferred source of these chlorogenic acids is the decaffeinated residue of an aqueous extract of green coffee, for example by activated carbon adsorption. This residue is obtained by desorbing the adsorbate by elution from the adsorbent and removing caffeine from the eluate by liquid / liquid extraction.

In the present invention, the effective amount of the anti-urease agent is the amount which produces a 50% inhibition rate of urease activity, which is measured by the method described in Example 1 hereinafter.
This inhibition is obtained with an amount of anti-urease agent of 200-2000 μg.

The cosmetic composition according to the invention is optionally an aqueous solution or dispersion, or preferably W / O type or O type.
It may be in the form of a / W emulsion. It is preferably combined with a cosmetic carrier, such as a lotion, cream or emulsion, to provide the anti-urease agent in an amount of 0.
1 to 10% by weight is contained.

In the emulsion, the fatty phase can contain animal, vegetable, mineral or synthetic oils and also waxes, long-chain alcohols, thickeners or gelling agents. 1-2 composition in emulsion form
It is desirable to contain 0% by weight of emulsifier.

The composition according to the invention also comprises various additives, in particular colorants, fragrances, preservatives, wetting agents, buffers,
It can contain pearlescent agents and mineral or organic fillers. Conveniently, an antioxidant, preferably 0.
It is contained in an amount of 02 to 0.2% by weight.

The present invention also relates to the use of an extract of witch hazel as an anti-urease agent. In such use, witch hazel extract can be incorporated into a cosmetic or dermatological composition as described above.

The invention is illustrated by the following examples, in which parts and percentages are by weight unless otherwise indicated.

Example 1 The anti-urease activity of the inhibitory compounds that can be used in the present invention was measured at various concentrations.

Method The method of assaying anti-urease activity for inhibition is based on the principle of measuring ammonia. Urea present in a substrate sample containing a mixture of inhibitor, urea and urease is degraded by urease during a fixed incubation of 37 ° C / 15 minutes. The last two reagents are
It is in the following ratio. That is, 7 μg of urea to 25 μg of urease (botanical origin, ie jack bean), or 0.25 units, ie 6 g of 4- (2-hydroxyethyl) -piperazine-1-ethanesulfonic acid in 1 liter of water itself and 0.25 ml of a solution of 25 mg urease dissolved in 25 ml of a buffer solution prepared by dissolving 0.2 g of ethylenediaminetetraacetic acid and then adjusting the pH to 7.5 by adding dilute sodium hydroxide solution. Ammonia derived from enzyme reaction is a reagent sodium hypochlorite,
An indophenol derivative is quantitatively produced by phenol and sodium nitroprusside. 4 ml of a solution prepared by dissolving 10 g of phenol and 50 mg of sodium nitroprusside in 1 liter of water was added to the sample,
It was then made up to 10 ml by addition of sodium hypochlorite solution (prepared by dissolving 5 g of sodium hydroxide and 10 ml of sodium hypochlorite in 1 liter of water). Three
After incubation for 20 minutes at 7 ° C., the adsorption was measured spectrophotometrically by comparison with a sample which had the same but without the mixture of reagents, and the indophenol derivative obtained was
Its intensity is proportional to the amount of liberated ammonia, 10 mm
The characterization was carried out by coloring, which can be measured at 634 mm in the cell. The% ammonia released was expressed by the following relationship: optical density of sample with inhibitor / optical density of sample without inhibitor x 100.

Results The anti-urease activity was 4 to 4 for each inhibitor tested.
It is expressed as the amount of inhibitor (μg) required to obtain 50% inhibition expressed by the average of 5 measurements. The results are shown in Table 1 below.

[0019]

[Table 1] Table 1 Inhibitor activity (μg) Usnic acid 250 (Usnaea barbata glycolic extract containing 7.5% of usnate) Chlorogenic acid 200 (Artichoke extract containing 46.7% of chlorogenic acid) Witch Hazel 200 (15% tannin) 500 Fractions retained on activated carbon 500 decaffeinated residue of green coffee eluted Green carob extract 500 (saccharified with hot water) green tea extract 1000 5-CQA 250 1 1 CQA 250 3,4-Di-CQA 250 3-CoQA 350 3-FQA 1000 3,3,4-di-CoQA 1000 3,4-di-FQA 1000 3,4-di-CFQA 1000 Ligand CQA = Caffeoylquinic acid FQA = Feruloylquinic acid CoQA = Bear Irukina acid CFQA = cafe oil feruloyl quinic acid

The above quinic acid derivative was prepared according to the applicant's patent application, which was filed on the same day.

Example 2 An in vitro test was carried out on the protective cosmetic cream,
Its anti-urease activity was evaluated by calorimetry of liberated ammonia as described in Example 1 and its pH was measured directly on the reaction mixture using a glass electrode. The first hypothesis is that an infant weighing 6 kg on average changed diapers every 4 hours. During these 4 hours, the infant had an average of 40 ml urine equivalent to 300 mg urea and 3
Stool 30 containing an amount of urease varying from ~ 30U
give g. Therefore, the amount of cream applied to the sensitive area contains 400 mg witch hazel extract as an inhibitor.
It is evaluated as 0 g.

The cream is an O / W type emulsion,
Its composition is shown in Table 2 below (the scientific terms used for the ingredients are "Cosmetic, Toiletry an
dFragrance Association, In
c. , Washington DC ”.

[0023]

[Table 2] Table 2 Composition% Phase A Glycerol stearate 10 Cetoaryl octanoate 3 Palm olein (containing C _12-14 fatty acid) 3 Sunflower oil 4 Wheat germ oil 0.3 phase B Glycerol 5 Water qsf100 phase C Cyclomethicone 3 DL-alpha-tocopherol acetate 0.2 Preservative 0.2 Witch hazel extract 4

To prepare the cream, phases A and B are heated separately to 80 ° C. and then phase B is poured into phase A with vigorous stirring. The mixture was then allowed to cool to 40 ° C. with continuous stirring, phase C was mixed in with vigorous stirring and the whole was allowed to cool to ambient temperature with continuous stirring. The activity of the cream containing inhibitor was measured at 0.75 U and 7.5 U enzyme concentration compared to cream without inhibitor. The results related to the amount of liberated ammonia are shown in Table 3 below, while the results related to pH are shown in Table 4.
Shown in.

[0025]

[Table 3] Table 3 Composition Amount of enzyme Free ammonia (mg) (U) (h) 1/4 3 7 20 24 Inhibitor-free 0.75 0.47 0.89 0.97 0.97 0.92 Witch Hazel extract 7.5 after incubation time X 1.13 1.04 1.27 --0.87 Contains 4% 0.75 1.38 2.18 1.74 2.26 2.61 Cream 7.5 5.92 9.66 9.66 --9.38

[0026]

[Table 4] Table 4 Composition Amount of enzyme pH (U) 0 24 after time X (hour) 0.75 5.79 5.84 0.75 5.94 6.53 whamsaku extract 0.75 5.94 6.53 Cream 7.5 5.94 7.73

The results obtained show that the cream containing witch hazel extract can completely inhibit urease at two concentrations of 3 and 30 U.

Example 3 A protective cream was prepared in the form of a W / O emulsion, the composition of which is shown in Table 5 below.

[Table 5] Table 5 Component% Phase A Microcrystalline wax, 9 Pentaerythritol cocoate, Stearyl citrate, Glycerol oleate, Aluminum stearate and propylene glycol Decyl oleate 3 Palm olein (C _12-12 fatty acid 10 Sunflower oil 12 Ozocelite 0.5 wheat germ oil 0.3 phase B glycerol 5 water qsf100 phase C DL-alpha-tocopheryl acetate 0.2 cyclomethicone 3 preservative 0.2 witch hazel extract 4 O / W type cream Was prepared as described above for the cream of Example 2.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁵ Identification code Internal reference number FI Technical indication location A61K 7/32 7252-4C 7/48 9051-4C (72) Inventor Georges Filipocian Lausanne, Switzerland Avenue de Valmont 18 (72) Inventor Ann Van Strasser Paris, France Lubaroll 98

Claims (8)

[Claims] 1. An anti-urease cosmetic or dermatological composition containing tannin, which comprises an effective amount of an anti-urease agent selected from condensed locust methanenin and chlorogenic acid derivatives. 2. The antiperspirant and antidiaper rash composition according to claim 1. 3. A composition according to claim 1, which comprises as anti-urease agent the decaffeinated residue of an aqueous green coffee extract rich in chlorogenic acid. 4. The composition according to claim 1, which contains 0.1 to 10% by weight of an anti-urease agent. 5. A composition according to claim 4, formulated as a cream based on a W / O or O / W emulsion. 6. A fatty phase containing an emulsifier and an aqueous phase are heated separately, the two phases thus heated are mixed with vigorous stirring, the mixture is allowed to cool to an intermediate temperature with stirring, the additives and A process for the preparation of a composition according to claim 5, characterized in that the anti-urease agent is mixed and then the mixture is cooled to ambient temperature with continuous stirring. 7. Use of witch hazel extract as an anti-urease agent. 8. Use according to claim 7 as an anti-diaper rash agent.