NZ197164A - Antiperspirant composition containing aluminium chloride and aluminium zirconium hydroxychloride - Google Patents

Description

New Zealand Paient Spedficaiion for Paient Number 1 97164 197164 Prserity Datcfs): ;.§9..

CotnpSete Specification FiSsd: 7-Ciass: . ubHcatior. Date: ...

Pf\Q. Journal, !Mo: No.: Date: NEW ZEALAND PATENTS ACI, 1953 COMPLETE SPECIFICATION ANTIPERSPIRANT COMPOSITION CONTAINING AS ACTIVE ANTIPERSPIRANT AGENTS AN ALUMINUM CHLORIDE AND AN ALUMINUM ZIRCONIUM KYDROXYCHLORIDE Jf/We, BRISTOL-MYERS COMPANY, a State of Delaware corporation having offices at 345 Park Avenue, New York, New York, United States of America, hereby declare the invention for which }£ / we pray that a patent may be granted to me/us, and the method by which it is to be performed, to be particularly described in and by the following statement:- (followed by la) - la - ANTIPERSPIRANT COMPOSITION CONTAINING AS ACTIVE ANTIPERSPIRANT AGENTS AN ALUMINUM CHLORIDE AND AN ALUMINUM ZIRCONIUM HYDROXYCHLORIDS This invention relates to novel antiperspirant compositions. More particularly, it concerns antiperspirant compositions containing as active ingredients a combination of an aluminum chloride and an aluminum zirconium hydroxychloride.

It is known in the prior art to use aluminum chloride or aluminum zirconium hydroxychloride individually as antiperspirant materials. We have now found, however, when these materials are employed together they act synergis-tically giving unexpected high activity and response rate.

It is accordingly an object of the present invention to provide a high performance antiperspirant composition containing a carrier and as active antiperspirant material a combination of an aluminum chloride and an aluminum zirconium hydroxychloride.

Other and more detailed objects of this invention will be apparent from the following description and claims.

Unless otherwise indicated the percentages are given in percent by weight based on the total weight of the composition .

It is known that certain types of people will respond to particular types of antiperspirant salts; it being unusual to find more than 60-70% of an antiperspirant panel responding to any one given material. However, when the combination of active ingredients of this invention was used over 93% of the panel participants responded favorably. Additionally, 197164 surprisingly high activities were recorded; 88% had superior activity. It has always been believed that the activity mechanism for different salts differ. What has been discovered here is a combination product that allows activity 5 responses from more than one mechanism.

Normally speaking, one would have expected this combination to be very irritating, since the pH of this solution is very acidic. We have also found that raising the pH alone is not enough to alleviate the irritation response. 10 However, we have also discovered that the use of divalent oxides or hydroxides in combination with small amounts of glycine solve this problem. The alkali earth metal salts or glycine alone can improve the irritation potential problem somewhat, however, it can be essentially eliminated 15 completely with the combination of the divalent metal oxides or hydroxides and glycine used in line with the instant discovery.

The quantity of the aluminum chloride that may be contained in the compositions of the present invention may 20 vary somewhat. For the most part, they will constitute between substantially 5 and substantially 25% by weight based on the total weight of the composition and preferably 7.5% to about 15% by weight. As used herein, the term "an aluminum chloride" is intended to refer to anhydrous aluminum chloride as well 25 as its hydrated and hydroxide forms e.g. AlCl^ • 6^0 or Al2(OH) CI.

The aluminum zirconium hydroxychlorides that are employed in the present invention are well known in the prior art and be described by the general formula: Al . Z 0 (OH) . . CI x H_0 4 n 14-n n 2 wherein n has the value 0 to 14 and x has the value of from 0 to 20. By way of example, mention may be made of compounds PATENT OFRCf 18 MAR 1983 PECEIVEO i n. 197164 of formulas: Al4 ZrO (OH)X1 Cl3 ; and Al ZrO (OH)Cl^ and their corresponding hydrates.

The amount of the aluminum zirconiiam hydroxychloride that may be contained in the composition of this invention may also vary somewhat. Usually, however, it will comprise between -substantially 2% to substantially 20% by weight based on the total weight of the composition and preferably between about 5% to about 10%.

An important feature of the present compositions is the ratio of the aluminum salt and the and the aluminum zirconium salt that they contain-. Thi"5 ratio■ will—be--in—the range of from substantially 0.5 to substantially 2; the preferred range being from about 1.2 5 to about 1.75.

Another important relationship in the present compositions is the aluminum plus zirconium metal:chloride mole ratio. It is important that this be less than .9 to retain the ionic character of the complex which is related to its antiperspirant activity.

As indicated previously, it is highly advantageous to use a combination of magnesium hydroxide (or oxide) and glycine to adjust the pH of our compositions. This combination will ordinarily be used to adjust the pH in the range of from about 2.5 to about 4.5. The glycine will be employed at a level of from substantially 0.25% to substantially 5% by weight based on the total weight of the composition; whereas, the magnesium hydroxide (or-oxide) will constitute substantially 1% to substantially 9%. The ratio of glycine to magnesium hydroxide (or oxide) is also an important factor. This ratio may be in the range of from.about .025 to about 5 but we prefer to employ a ratio in the range of from about 0.1 to about 1.0.

The novel combination of antiperspirant materials and the pH adjusting agents described above may be incorporated 'v;^A'f£MT omci 18 MAR J983 in any of a variety of dosage forms useful for delivering the antiperspirant material. They may be incorporated in a lotion, in a cream or gel, in a foam system, in an aerosol dispensing system, in a pump spray system, as part of an antiperspirant stick or may be delivered in the form of a solution in a suitable solvent vehicle. The following are illustrations of types of formulas in which the present compositions may be employed as active antiperspirant materials: A. Roll-On (Lotions and Creams) Actives 25% Emollients 2-4% Surface active agents 2-4% Buffering systems 2-7% Water q.s. 100% B. Suspension-Anhydrous can be used in the formulation of Aerosols and Aerosol Foams Actives % Emollients -15% Suspending agents 2-5% Buffering agents 2-4% Water q.s. 100% Aerosol Above 70-85% Propellant 15-30% Sticks Actives % Gelling agent ro 1 Waxes -20% Emollients -20% Buffering agents ro • •£» Of Externalphase q.s. 100% * Anhydrous solvent The following Examples are given to further illustrate the present invention. It is understood, however, that the invention is not limited thereto.

EXAMPLE 1 Roll-On Lotion (Emulsion o/w) % by Wt.

AlCl . 6H20 15.00 Mg(OH)~ 3.75 1 Al/Zr trichlorohydrate 10.00 Brij 72 (Polyoxyethylene 2 Stearyl Ether) 3.00 Brij 78 (Polyoxyethylene Stearyl Ether) 1.00 Glycine 0.50 Disodium EDTA 0.10 Polyoxypropylene 15 Stearyl Ether (Arlamol E) 4.00 H20 62.65 100.00 EXAMPLE 2 Clear Water Solution (Pump Spray) A1C13 . 6H20 15.00 Mg(OH)2 3.75 Glycine 0.50 Al/Zr trichlorohydrate^" 10.00 H20 65.75 Proce.tyl AWS (PPG-5 Cetheth 20) 5.00 100.00 EXAMPLE 3 Aerosol Antiperspirant Al/Complex Powder2 6.00 Al/Zr trichlorohydrate"^ 4.00 Dibutyl phthalate 11.00 Al4ZrO(OH)11Cl3 Product prepared by spray drying A1C1-; M (OH)_ and glycine in the weight ratio of 4:1: .5 ^ EXAMPLE 3 (Cont'd) Cabosil M-5 0.30 Bentone 34 0.10 Isobutane 78.60 100.00 EXAMPLE 4 Stick Antiperspirant Al/Complex Powder 15.00 Al/Zr trichlorohydrate 10.00 Stearyl alcohol 20.00 Dibutyl phthalate 41.00 Procetyl AWS (PPG-5 Cetheth 20) 10.00 Montan wax 4.00 100.00 To demonstrate the fact that the combination of the aluminum chloride and the aluminum zirconiiam hydroxychloride act synergistically as antiperspirants, three compositions were prepared identified as Compositions A, B and C which were the same in all respects excepting the active antiperspirant material. Composition A contained 25% by weight of aluminum zirconium hydroxychloride; Composition B contained 10% by weight of aluminum zirconiiam hydroxychloride and 15% by weight of aluminum chloride; and Composition C contained 25% by weight of aluminum chloride. Each of these compositions were tested for antiperspirant activity on a group of individuals that served as an antiperspirant panel. The procedure employed was as described in Federal Register, Vol. 43, Number 196, October 10, 1978 and is called the Gravemetric Axillary Antiperspirant Test.

The results of this test are summarized in Table I below which gives the formulas of Compositions A, B and C O c77 ^ ^ £■' I \. as well as the antiperspirant activity measured for each composition.

TABLE I B Aluminum Zirconium hydroxide Complex 25 10 — Aluminum Chloride — 15 25 Emollient 2-4 2-4 2-4 Surface Active Agents 2-4 2-4 2-4 q.s. buffer to pH 3.2 + .3 q.s. water to 100% pH at time of test 3.5 3.2 3.4 Activity 50% 62% 53% As will be seen from the above Table, a 20-25% enhancement of antiperspirant activity is obtained with a combination of aluminum chloride and aluminum zirconium hydroxychloride as compared with the use of aluminum chloride or aluminum zirconium hydroxychloride.

Although the invention has been described with reference to specific forms thereof, it will be understood that many changes and modifications may be made without departing from the spirit of this invention. 197164

Claims (11)

WHAT WE CLAIM IS:

1. An antiperspirant composition comprising a carrier and as active antiperspirant material a combination of an aluminum chloride and an aluminum zirconium hydroxychloride, said composition comprising, based on the total weight of the composition, from substantially 5% to substantially 25% by weight of an aluminum chloride and from substantially 2% to substantially 20% by weight of an aluminum zirconium hydroxychloride; the ratio of aluminum salt to aluminum zirconium salt in said composition being in the range of from substantially 0.5 to substantially 2 and the mole ratio of aluminium plus zirconium metal to chloride being less than .9.

2. A composition according to Claim 1 including as a pH adjusting agent a combination of magnesium hydroxide or oxide and glycine, said magnesium hydroxide or oxide constituting from substantially 1% to substantially 9% by weight of said composition and said glycine constituting from substantially 0.25% to substantially 5% by weight of said composition.

3. A composition according to Claim 1 or Claim 2 in the form of a lotion.

4. A composition according to Claim 1 or Claim 2 in the form of a solution.

5. A composition according to Claim 1 or Claim 2 in the form of a stick.

6. A composition according to Claim 1 or Claim 2 in the form of an aerosol < composition.

7. A composition according to Claim 1 or Claim 2 in the form of a pump spray composition.

8. A composition according' to Claim 1 or Claim 2 in the form of a cream or a gel. 9 . A composition according to Claim 1 or Claim 2 in the form of a foam. 'i.Z P'ATcOT OFFICB 18 MAR 1983 I

9 - 197164

10. A composition according to Claim 2, whenever formulated in accordance with the formula A, B or C hereinbefore described.

11. A composition according to Claim 1 or Claim 2, substantially as hereinbefore described with particular reference to any one of the foregoing Examples. DATED THIS DAY OF 19-PZ/ A. J. PARK & SON PE.l $ ~S- AGENTS FOR THE APPLICANTS