NZ200153A - Treating acne and oily skin by topically administering a composition sulphurated lime solution and a mixture of clays - Google Patents

Description

New Zealand Paient Spedficaiion for Paient Number £00153 2 0 01 5 3 Priority Det-wi): Comp!«t« Specification Filed: TV.1?." Cf5«« APR 1985 S| Pubiicaticn Date: P.O. tio: .. ......

Under the provisions of RegO^ latlon 23 (0 the Specification has been ante-dated IJLJ&&4ZC. 19 £L~ SAVINGS NEW ZEALAND PATENTS ACT, J 953 No.. Divided out of No. 198 575 Dale; 7 October^ 19 81 COMPLETE SPECIFICATION 29MAR/9ffif| 11% "METHOD AND COMPOSITION FOR TREATING ACNE" fyWe, RORER INTERNATIONAL (OVERSEAS) INC., a Delaware Corporation, of 110 West Tenth Street, Wilmington, Delaware 19899, U.S.A., hereby declare the invention for which £ / we pray that a patent may be granted to ikk/us, and the method by which it is to be performed, to be particularly described in and by the following statement: - (followed bv paqe la) / 200153 This invention relates to.methods of topically treating acne and oily skin and compositions useful for said treatment. The invention also relates to a method for deodorizing compositions containing sulfurated lime solution which are intended for topical 5 administration, and for preventing stain of skin or fabric as well as discoloration of jewelry by the composition.

This is a divisional of New Zealand Patent Specification 198,575.

It is well established that acne is associated with sebum 10 production and that androgens stimulate sebum production whereas estrogens suppress sebum production; estrogen therapy being indicated as a possible means of treating acne. Several reports indicate that oral contraceptives or the individual active estrogenic components thereof, for example, ethinyl estradiol and 15 derivatives are useful in treating acne in both males and females. r In recent years it has become apparent that estrogenic products currently in use possess certain undesirable side effects which must be set against the undoubted benefits resulting from their use. The use of estrogens for the treatment of acne in women can 20 lead to uterine bleeding and spotting and breast tenderness. In men, estrogen administration can have a feminizing effect and may — I« — result in gynecomastia and impotence [L.F. Goodman and A.

Gilman, The Pharmacological Basis of Therapeutics, 4th ed. , The MacMillan Company, p.1537 (1970)]. Estrogenic therapy has I been reported to give rise' to other deleterious side effects. For example, diethylstilbestrol, a once widely used and well established estrogen has been implicated as possibly being responsible for vaginal cancer and adenosis in the female offspring of pregnant women treated with the compound (Lancet 1975, 1960). Also, ethinyl estradiol and mestranol, which represent estrogenic compounds in current oral contraceptives, are now known to be involved in certain serious side effects associated with oral contraceptives including depression [Nature 243, 58 (1973)], hypertension [Am. J. Obstet. Gynecol. 112, 912, (1972)], carbohydrate and lipid abnormalities (Lancet 1969, p.783), interference with blood .clotting mechanism resulting in thrombosis and stroke [Ann. Intern. Med. 72, 111, (1970)], and jaundice [Am. J. Obstet Gynecol. 119, 1965, (1974)]. Consequently, there is a need, for an improved method of treating acne.

It an cbject of this invention to ao sopo w.?y resting this need or at least to provide the public with a useful choice.

Accordingly the invention may be said broadly to consist, of a method for treating acne and oily skin in a patient in need thereof which comprises topically administering to said patient a composition comprising an effective amount of a sulfurated lime solution in a carrier comprising a pharmaceutically acceptable finely divided inorganic sorbent powder.

In another aspect the invention may be said broadly to consist in a method of treating oily skin in a patient in need thereof which comprises topically administering to said patient a composition comprising 1-10% by weight of a sulfurated lime solution and 5-50% by weight of a pharmaceutically acceptable clay or pigment extender. - 20015,3 In yet another aspect the invention may be said broadly to consist of an anti-acne and anti-seborrheic pharmaceutical composition for topical administration comprising an effective amount of a sulfurated lime solution and 5-50% by weight of a carrier comprising a pharmaceutically acceptable clay, pigment extender or mixtures thereof.

As used herein the term "acne" is intended to mean any inflammatory disease or condition of the sebaceous gland commonly occurring at puberty resulting in comedones, pustules, papules, inflamed nodules or infected cysts. A solution of sulfurated lime in combination with a finely divided sorbent powder consisting of a mixture of clays, namely, a montmorillonite clay in combination with attapulgite, has been found to be effective in reducing the amount of sebum produced by sebaceous glands.

The composition of the present invention, when administered to a patient having an acne condition or oily skin condition, t*5 3 represents a novel method of treating acne which offers distinct advantages over previously employed methods of treatment, for example, estrogen therapy, in that the compounds employed do not result in certain deleterious side effects resulting with estrogen therapy as will become more apparent hereinafter.

"Sulfurated lime" as used herein is commercially available and may be prepared according to the procedure,disclosed in Mellor, Vol. Ill, p. 740 (1928). Generally, sulfurated lime contains not less than 55% calcium sulfides and polysulfides and the balance being calcium sulfate, sulfides and carbonate, and the "ash" from the carbonaceous material from which it is formed.

It has been surprisingly discovered that the combination of1 a montmorillonite clay and attapulgite removes the odor of the sulfurated solution while releasing any perfume odor which may be present.

The clay which may be utilized in the composition of the I I present invention are the natural and synthetic montmorillonite clays such as the bentonites, kaolin, hectorite, smectites and saponites or mixtures thereof in combination with attapulgite.

Montmorillonite is the name of a group of clays with an expanding lattice which are members of the clay-mineral group. The montmorillonites contain aluminum silicates with some mont-morillonites having some of the aluminum replaced by magnesium.

The sulfurated lime composition of the present invention can be administered in various manners to achieve the desired effect. The amount of sulfurated lime solution in the composition will vary with the severity of the acne or oily skin condition and the mode of administration. Generally, the sulfurated lime solution comprises about 1-20% by weight of the total composition, preferably 2-10% weight of the total composition. The sorbent powders are 10015 3 employed in the amount of about 5-50% by weight of composition. The sorbent powder to be an effective deodorant for the sulfurated lime solution must contain at least about 2-9% by weight of a montmorillonite clay based on the weight of the total composition, and at least about 1.5% by weight of attapulgite based on the weight of the total composition. The topical formulation of the present invention may contain pharmaceutically acceptable surfactants, particularly those having a detergent action for microabrasion of the uppermost layer of the skin, i.e., horny layer, to provide a smooth feeling to the skin, soothing agents such as camphor, cooling agents such as menthol, dispersing agents, penetrants, perfumes, and a conservation agent such as butylated hydroxytoluene.

The addition of calcium carbonate to the composition has been found to be advantageous for maintaining the composition's i ■ alkalinity and color. Also, it is useful in providing a micro abrasive effect so as to remove the horny layer of the skin and leave a smooth feeling.

Talc may be added to the composition to improve the slip qualities of the composition on the skin.

An effective amount of the other acne-treating agents may be incorporated in the composition such as in an amount of up to 6% by weight of the composition. These additional active ingredients include salicylic acid, resorcinol and its derivatives, retinoic acid and its derivatives, sulfur, erythromycin, and the like. Aerosol preparations containing the sulfurated lime solution and the mixture of clays together with extenders in the form of a finely grouped powder may also be employed for topical administration. The aerosols may be packaged in a pressurized . XO 01 53. ♦ aerosol container together with a gaseous or liquified propellant, for example, dichlorodifluoromethane,"dichlorodifluorcthanet carbon dioxide, nitrogen, or propane with the usual adjuvant such as a suspending agent and wetting agents as may be necessary or desirable. Although the present formulation may be applied directly to the site requiring treatment, it is preferably applied in the form of a face' mask so that during its application, the absorbing and adsorbing action of the sorbent powder on the face oils takes place and the sulfurated lime becomes more effective in the desired treatment of the skin condition.

The following examples are illustrative of formulations of compositions according to thisi invention.

EXAMPLE I A composition for use as a face mask containing the following composition: Sulfurated lime, solution (Vleminckx*s solution) Colloidal aluminum magnesium silicate (Veegum®) (a montmorillonite type clay) Attapulgite Sodium lauryl sulfate Butylated hydroxytoluene Purified water was prepared as follows: Into a beaker containing 5 ml of sulfurated lime solution, 150 mg of sodium lauryl sulfate, 15 mg of butylated hydroxytoluene and 10 ml of purifed water was stirred in 750 mg of colloidal aluminum magenesium silicate and 250 mg of attapulgite until a uniform paste was formed. The composition contained essentially no sulfur odor and was suitable for forming a face mask in the treatment of acne. ml 75 0 mg 250 mg 150 mg 15 mg q. s. 00153 EXAMPLE II A composition for the treatment of acne and seborrheic conditions having the following: Sulfurated lime solution 20 ml Hectorite clay 1.5 g Attapulgite 0.75 g t Polyethylene glycol monostearate 0.50 g Purified water q.s. was prepared as follows: Into a beaker containing 20 ml of sulfurated lime solution was added 1.5 g of Laponite®, a commercially available hectorite clay and 0.75 g of attapulgite. Purified water was then heated and mixed with polyethylene glycol monostearate until uniform. Then mixed and cooled to room temperature. This was then 15 added until a thick paste was formed that was spreadable by use of an applicator stick. V EXAMPLE III ' A paste for a face mask for use in the treatment of severe acne and having an anti-seborrheic effect comprising: Sulfurated lime solution 20 ml Retinoic acid 12 mg Sodium lauryl sulfate 0.5 g Bentonite 2 g Attapulgite 1 g Purified water q.s. was prepared as follows: X0015 3 Into a beaker containing 20 mg of sulfurated lime solution was added with stirring 0.5 g of sodium lauryl sulfate, 12 mg of ■ retinoic acid* 1 g of attapulgite and 2 g of pulverized bentonite clay. Purified water was then added to the mixture until a paste 5 of a desired consistency was obtained. The resulting paste may then be applied directly to the site requiring treatment. A current of warm air may then be blown on the face until the mixture dries. The composition is maintained on the face for about 20 to about 30 minutes and then removed by washing with water. The treatment is 10 administered either every other day or daily until the condition treated is alleviated. i EXAMPLE IV Ingredients % Vleminckx's solution 6.00 Partially acetylated polyoxyethylene 2.00 lanolin ether (Laneth-10 acetate Decyl oleate 0.60 Alcohol 7.00 Titanium dioxide 3.00 • Kaolin 15.00 Calcium Carbonate 2.30.

Attapulgite 3.50 Calcium silicate 2.00 Silica 0.225 EDTA 0.10 .

Paraben 0.20 Dioctyl sodium sulfosuccinate 0.16 Fragrance 0.10 Fatty alkanolamide 5.00 Sodium sulfate of an et-hoxylated fatty alcohol 5.00 Purified water q.s. 2 00153 The formulation was effective for the treatment of acne and oily skin conditions. Removal of the paste after drying by water washing gave a smooth feeling to the skin.

Comparison Experiment A A sulfur-containing lotion was prepared utilizing a convention al formulation with the following ingredients: \ Ingredients % Sulfur (U.S.P.) i 5.00 Cellulose gum 0.45 Propylene glycol 3.00 Attapulgite 2.00 Iron oxide 1.20 Alcohol 20.00 Fragrance • 0.10 Fatty alkanolamide 2.00 Methyl paraben 0.15 Talc 7.00 Zinc oxide 7.00 Deionized water q.s.

Titanium Dioxide 4.00 Comparison Experiment B A lotion was prepared utilizing the formula of Experiment A except that a sulfurated lime solution (Vleminckx's solution) was utilized in lieu of sulfur.

TABLE I 200153 Sample 1. Vleminckx's solution 2. Elemental sulfur 3. Paste of Experiment 4 4• Lotion of Experiment A . Lotion of Experiment B Odor Cosmetic Effect Poor (not suitable for use) Objectionable Slightly pungent Poor (could be used) Pleasant Pleasant Slightly Objectionable Good Good Fair (not suitable for use) It was noted that elemental sulfur by itself or in a conventional carrier could be utilized by patients without any ob- I jectionable odor being present. Use of a sulfurated lime solution by itself or in a conventional carrier such as those containing elemental sulfur still produced an objectionable odor which would prevent use on the face area. A formulation prepared according to Example 4 had a pleasant odor and could be utilized for skin care.

EXPERIMENT C A. Mixutes of 6% sulfurated lime solution and the following clays were prepared with sufficient water to give paste-like consistencies: 1. 2. 3. 4.

Clay Bentonite Kaolin Attapulgite TABLE I Test A (parts by wt.) 10 10 Calcium silicate Odor Pungent Pungent Pungent Pungent Test B (parts by wt.) . " 20 Odor Pungent Pungent Pungent Pungent

Claims (4)

2001 53. The pungent "rotten egg" odor of the sulfurated lime solution was evident although somewhat diminished in each of the formulations. Each mixture caused a light yellow stain when applied to fabric. Contact with silver jewelry resulted in tarnishing. B. Mixtures were prepared according to the procedure of Part A. fc TABLE II Clay Test . A (parts Odor by wt.) Test B (parts by wt.) Odor 10 1. Bentonite Kaolin 10 10 Slight Pungent 20 10 : Slight Pungent 2. Bentonite Attapulgite 10 10 None 20 ' 10 None 15 3. Bentonite Calcium Silicate 10 10 Slight Pungent 20 10 Slight Pungent 4. Kaolin Attapulgite 10 10 None 20 10 None 5. Kaolin Calcium Silicate 10 10 Slight Pungent 20 10 Slight Pungent 20 6. Calcium Silicate Attapulgite 10 10 TABLE Slight Pungent III 20 10 Slight Pungent Clay Parts by wt. Odor 25 1. Bentonite Attapulgite 9.0 0.5 Slight Pungent 2. Bentonite Attapulgite 9.0 1.5 None 3. Kaolin Attapulgite 9.0 0.5 Slight Pungent 30 4. Kaolin Attapulgite 9.0 1.5 None 35 The use of 1.5 parts of attapulgite yielded a mixture which was virtually free of sulfurated lime solution odor. Mixtures (2) and (4) caused no staining of fabrics. Contact with silver, gold and chrome plated jewelry caused no tarnishing, even after 10 hours of contact. -11- WHAT WE 'CLAIM IS : 2ooiS3

1. A method for deodorizing cosmetic and therapeutic compositions having an objectionable odoriferous sulfur-containing compound which comprises incorporating in said composition an effective deodorizing amount of a pharmaceutically acceptable finely divided inorganic sorbent powder.

2. The method of Claim 1 wherein the composition comprises 5-50% by weight of said sorbent powder.

3. The method of Claim 1 or Claim 2 wherein said sorbent powder is a clay, pigment extender or mixtures thereof.

4. The method of any one of Claims 1 to 3 wherein said sorbent powder is a clay selected from the group consisting of bentonite, hectorite, smectite, attapulgite, fuller's earth and montmorillonite clays. said sorbent powder is colloidal aluminum magnesium silicate, kaolin, talc or calcium carbonate. ion comprising an effective amount of a sulfurated lime solution and 5-50% by weight of a carrier comprising a pharmaceutically acceptable clay, pigment extender or mixtures thereof.

7. The composition of Claim 6 wherein said sulfurated lime solution comprises 1-10% by weight of said composition.

8. The composition of Claim 6 or 7 including a compound selected from the group consisting of salicylic acid, resorcinol, retinoic acid and derivatives thereof.

5. The method of any one of Claims 1 to 3 wherein

6. A therapeutic composition for topical administratis. The method of any one of Claims 1 to 5 substantially as herein described.

10. The composition of any one of Claims 6 to 8 substantially as herein described. BjM^te/Their Authorised Agents, 12 A. j. PARK & SON