DE2161551A1 - Two-component antiperspirant - Google Patents

Description

Two-component antiperspirant

Known antiperspirants contain as antiperspirant Substance mostly metal salts, such as chlorides, chlorohydroxides, sulfates, sulfamates or other salts of zinc, aluminum, Zircon or rare earths, the visual whitening effect of these Preparations is limited. It is also known, for example from British patent specification 9 Q ^ Q 279, a Mixture of aluminum salt; as an astringent and benzoylscopolamine to use as an antiperspirant. The effectiveness of such Mixtures is particular because of the not long-lasting Perspiration resistance only low,

The invention has the task of proposing an effective and long-lasting antiperspirant.

To solve this problem, a two-component antiperspirant is proposed, consisting of two separately packed

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BATH ORIGINAL

Solutions, emulsions, suspensions or solid mixtures, one of which is atropine, scopolamine or their derivatives esterified on the hydroxyl group of tropic acid, in particular benzoyl scopolamine or alkoxybenzoylscopolamine with a lower Contains alkoxy group while the other is "an antiperspirant" Contains metal salt. .

The anti-vision effect of this two-component anti-inhalant is very surprising when applied separately much larger and more lasting than spraying or applying of the products known to date, regardless of whether they consist of one or more active ingredients in a mixture b

Benzpylseppolamine is preferably used as the hydrobromide, while as Me | all.salg Aluiainiumehlorid, AliMijiiunieMQP "hydroxide or a mixture of these" used WiPd ₉ The YQP separately packaged solutions, emulsions or guspensioripn, which can also be anhydrous j can be sold in a single outer packaging, on which markings or other aids can also be attached? yes if the application of the two components can be displayed or checked at the appropriate time interval,

Benzoylscopolamine known as the anticholinergic compound In addition to the hydrobromide, it can also be used as a hydrochloride or hydroiodide or in the form of other salts, mostly acid salts, such as those of nitric acid, citric acid, Acetic acid, methosulfuric acid, sulfuric acid, phosphoric acid Tartaric acid, lactic acid, benzoic acid.

In addition to benzoylscopolamine, other anticholinergic compounds can be used, such as atropine, scopolamine and benzoylscopolamine derivatives. Preferred derivatives have the following general formula:

ti

CH-C-O

CH <

N - CH _: -CH

CH _n

-CH '

Il

CH.

-o-.c-TV

OR

in which R is a lower alkyl radical having 1 to 6 and preferably 1 to ^ carbon atoms, in particular 1 to 2 carbon atoms. Such compounds are stable to hydrolysis and show excellent antiperspiran properties.

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In the above formula, the alkoxy radical is in the para position to the Benzoyl radical arranged; the substituent can also be in the ortho-position or meta-position on the carbon next to the Carbonyl radical. The para-substituted compounds are preferred. Further derivatives of such compounds non-interfering substituents can usually be found on a phenyl radical contain, such as chlorine, hydroxy, amino, lower. Alkyl and the like. These derivatives are preferred together with benzoylscopolamine or with the benzoylscopolamine substituted with a lower alkoxy radical or salts thereof used.

Of the aluminum, zirconium, zinc and rare earth salts, aluminum salts are preferred, especially aluminum chloride hydroxide and aluminum chloride. Aluminum sulfate, aluminum sulfate, aluminum sulfocarbonate and alkoxy-substituted aluminum salts can also be used can be used, such as dialkoxy-substituted aluminum chloride, the alkoxy radicals 2 to 18 Contain carbon atoms. The corresponding zirconium, zinc and rare earth salts can also be used, for example Zirconium chloride, zirconium sulfate, zinc sulfocarbonate, zinc chloride, Gadolinium chloride, cerium sulfate and hafnium chloride. Further Lithium chloride, magnesium sulfate, iron (III) chloride, cadmium sulfate or titanium tetrachloride, among others, can also be used.

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The benzoylscopolamine compound or the corresponding derivatives are usually applied in an aqueous solution, while the metal salts are applied after a waiting time of preferably at least a few hours and generally not more than 2k hours, preferably within k to 12 and in particular ¹ to 8 hours as a solution, aqueous solution, as an emulsion or as a suspension from an aerosol can, as a paste or powder »can be applied. .

The perspiration inhibition after application of the first component, namely the scopolamine compound, is usually 40 to 80 %; .A often 50 to 70 #ige reducing the normal perspiration but within range of H to 8 Stunden.nach attachment achieved. However, this effect is lost within 24 hours. A further application of this scopolamine component does not lead to any further increase in the resistance to perspiration. The same applies when using the metal salt, which leads to perspiration inhibition even after successive application over the course of several days; surprisingly, however, when using the two-component antiperspirant and applying the second metal salt component after the waiting time specified above, perspiration inhibition is obtained, which lasts longer or is even stronger, especially if the application of the second component is repeated. Self

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if left with this treatment for 2 to 10 days, there is no reduction in the resistance to perspiration when the use of the second component is resumed. If For example, the first component of the two-component antiperspirant, namely, Benzoylscopolamine Hydrobromxd applies. and then after waiting 6 to 8 hours twice a day Applies aluminum chlorohydroxide or a mixture of aluminum chlorohydroxide and aluminum chloride in aqueous solution, in this way one obtains without further use of the first scopolamine component a good antiperspirant effect, even if the antiperspirant has not been applied for 1 to 10 days. When the aluminum salt is then applied, about the same level of perspiration inhibition as it was originally obtained was achieved by applying the first component. In addition, the first scopolamine component would be applied once after such a rest period of 1 to 10 days, the perspiration inhibition is even more and above the value previously achieved Also improve, with subsequent application of the metal salt component this strong resistance to welding for up to 10 days and is retained longer. Comparative tests with other combinations resulted in a much worse fourth.

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The first component, namely the scopolamine derivative, is found in Amounts of 0.0001 to 0.1 g are used, while the second component, namely the metal salt, is usually used in amounts of 0.01 to 1 g is used, preferably per day 0.02 to 0.5 g, but not more than 3 applications per day.

The first scopolamine component can contain a wide variety of additives, preferably contain wetting agents, such as nonionic surfactants or solvents, such as condensation products of Ethylene oxide and propylene oxide with glycol with molecular weights between 2,000 and 10,000 and a ethylene oxide / propylene oxide ratio from 3: 1 to 1: 3

In general, these nonionic surfactants are used, for example, with benzoylscopolamine hydrobromide in a concentration of 0.1 to 5 and preferably 0.5 to 2 % .

The second component, namely the metal salts, can also contain conventional additives, such as emulsifiers, solvents, thickeners, emollients, dyes, pigments, fragrances, bactericides, lanolin, oils or waxes. These metal salts are usually present in the preparation in a concentration of 0.1 to 35 % and preferably 0.6 to 25%.

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The volume ratio or the weight ratio of each other separately packaged two components is in a range from 1: 5 to 1: 25j, with benzoylscopolamine hydrobromide being preferred in aqueous solution and the second component is packaged as a rollable emulsion. Using of aluminum chloride and aluminum chlorohydroxide, the ratio of these two substances is in a range from 1: 100 to 1: 1 and preferably 1:25 to 1: 2, the aluminum chloride being taken into account as the hexahydrate.

example 1

To prepare the two-component antiperspirant, a solution of benzoylscopolamine hydrobromide with a concentration of 0.025 % in a 1 solution of a nonionic surfactant in distilled water was prepared and acidified with hydrogen bromide. A condensation product of ethylene oxide and propylene oxide with a molecular weight of about 8,000 was used as the surfactant.

The second component was made up as a rollable emulsion and had the following composition:

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Aluminum chlorhydroxide (50 % active) aluminum chloride hexahydrate ethanol (95 %)
distilled water

nonionic surfactant (alkylphenyl polyoxyethylene ethanol)

Thickener (methy! Cellulose) Lanolin derivative

glycerin

Wisteria

other additives, such as fragrances

44 Parts by weight 1.0 If 22.0 It 25.3 ti 1.0 Il 0.7 It 1.0 It 3.0 It 1.5 dd 0.5 dd

These separately packaged active ingredients of the two-component antiperspirant were examined for their effect. The first component was administered in an amount of 1 ml to five test subjects with profuse sweating in the armpit area. After 3 hours, perspiration was determined by placing a cellulose pad in the armpit area and weighing it periodically. It was found that the perspiration was reduced on average to about 65 % compared to the normal behavior of the test persons * After 24 hours the perspiration had again reached the original starting value. Similar results were obtained when the pH of the solution was changed from 4.5 to 3.0 and to 6.5.

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24 hours after application of the first component, the second component was applied in amounts of 2 to 3 ml, whereupon this process was repeated after a waiting time of 8 hours. The sweat inhibition measured after 1 hour was 65 %. This value was maintained in the test subjects when the second component was applied once or twice a day. After 3 days, the application was interrupted for a further 3 days, whereupon, after a single application of the second component, a 65 / Sige resistance to perspiration was measured again after 1 hour. If the first component was then applied after a period of 12 hours, the perspiration resistance could be improved by more than 60% and this value could also be maintained through regular use of the first component.

Similar results were obtained with para-methoxybenzoylscopolamine and Obtain zinc phenol sulfonate or aluminum sulfamate or zirconium chloride.

In the two-component antiperspirant according to the invention preferably the scopolamine component is packaged in a spray bottle or an aerosol container, while the metal salt component is usually packaged as a paste with a ball applicator in a plastic container. The first component can do the same

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- ii -

as an emulsion with a ball applicator in a plastic container be packaged and the second component applied as a solution or powder or as a cream or paste will.

Example 2

For comparison, the first component according to Example 1 was applied in the same amount and in the same way to 4 test persons and this application was repeated after 24 hours, it being found that the perspiration resistance decreased from about 63% to about 20 % after 24 hours and 1 hour after the second application only took a fourth of 56 % . In a further comparative experiment, the same amounts of the second component were applied to 4 test persons and the anti-swelling was measured after 1, 3>5> 7 »9 and 11 applications over the course of 5 1/2 days, with two applications per day in an interval of 12 hours. The original antiperspirant was about 20 % and gradually increased to about 50 % after 51/2 days.

Example 3

The procedure was analogous to Example 1, but now the scopolamine component was para-OC-methylbenzoylscopolamine hydrochloride

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or the corresponding scopolamine base was used in a concentration of 0.02 % in Vfasser in an amount of 1.5 ml of solution. As a second component a 5% aqueous solution of aluminum chloride, zinc chloride or zirconium sulfate or an aerosol mixture having 10 wt.% Aluminum chlorhydroxide was used, with about 1 g metal salt was used. The results obtained here corresponded to those of Example 1.

It was particularly advantageous when using the two-component antiperspirant, that you achieve a much stronger antiperspirant with much less active ingredient and that you can apply it Interrupt for several days if necessary, in order to avoid inflammation in the case of sensitive skin.

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Claims (4)

Claims -. 1, two-component antiperspirant consisting of two of each other separately packaged solutions, emulsions, suspensions or mixtures of pesticides, one of which. Atropine, scopolamine or their derivatives esterified on the hydroxyl group of tropic acid, in particular benzoylscopolamine or alkoxybenzoylscopolamine with a lower alkoxy group while the other contains an antiperspirant Contains metal salt. 2. Two-component antiperspirant according to claim 1, characterized characterized in that the first component contains benzoylscopolamine hydrobromide. 3. Two-component antiperspirant according to claim 1 and 2, characterized in that the second component is a zinc salt, aluminum salt, zirconium salt or a rare salt Contains earth. 4. Two-component antiperspirant according to claim 1 to 3j characterized in that the first component in aqueous 209828/1089 Solution with a content of 0.001 to 0.05 g is present, while the second component preferably after a waiting time of at least 2 hours in an amount of 0.01 to 1.0 g is applied. 209828/1089