COMPOSITION AND METHOD OF ENHANCING SUN TANNING

Abstract: Sun tanning, especially of fair skin, is enhanced by topical application of a pseudocatalase prior to exposure to sunlight or UVB light. The preferred pseudocatalases are transition metal co-ordination complexes, especially manganese (II) bicarbonate.

Description: -2- causing an undesirable increase in hydroxyl ion concentration unless catalase or some other competing mechanism removes peroxide ion. Thus, the presence of a pseudocatalase is believed to allow sufficient UVB exposure for superoxide anion radical formation to promote pigmentation in catalase deficient areas without burning or other cell damage. According to a first aspect of the present invention, there is provided the use of a pseudocatalase in the manufacture of a topical composition for the enhancement of tanning of skin, especially fair skin, on exposure to sunlight or UVB light. In a second aspect, the invention provides a topical sunscreen composition comprising a pseudocatalase, a sunscreen agent and a physiologically acceptable topical vehicle therefor. In a third aspect, the invention provides a pseudocatalase for use in the enhancement of tanning of skin, especially fair skin, on exposure to sunlight or UVB light. In a fourth aspect, the invention provides a method of enhancing tanning of skin, especially fair skin, which comprises applying to the skin an effective amount of a pseudocatalase. In a fifth aspect, the invention provides use of a pseudocatalase to enhance tanning of skin on exposure to sunlight or UVB light. The pseudocatalase can be any physiologically acceptable compound which catalyzes the dis utation of -3- hydrogen peroxide. Some compounds such as Mn(II) bicarbonate are already known to be pseudocatalases and others can be determined by simple screening tests. The presently preferred pseudocatalases are transition metal co-ordination complexes in which the inductive effect of the electron acceptor ligand enhances the redox effect of the metal on hydrogen peroxide dismutation. Usually, the metal will be Cu(I) , Fe(II) or, especially Mn(II) and the ligand will be bicarbonate. It is especially preferred that the pseudocatalase is Mn(II) bicarbonate complex. Said complex readily can be prepared by contacting manganous chloride with excess bicarbonate in aqueous solution. The pseudocatalase is formulated in a topical vehicle for use. Conveniently, the vehicle comprises a hydrophilic cream to which an aqueous solution or suspension of the pseudocatalase is added to form a cream or lotion. Alternatively, the vehicle can be a bath oil although any other compatible topical vehicle can be used to provide a topical composition. Usually, the composition will contain a sunscreen agent, and other components such as emollients, perfumes etc conventionally used in sunscreen preparations. In particular, the composition can contain calcium ions, suitably added as calcium chloride, usually in a concentration of 5 to 20 mmol. Subject to compatibility with the pseudocatalase and superoxide anion, any conventional sunscreen agent, such as Parsol MCX, or other component can be used. The invention is illustrated in the following non- limiting Examples. -4 - Example 1 Manganous chloride (380 mg) was added to a solution of sodium bicarbonate (2.3 g) in purified water (3.0 ml) at ambient temperature. The mixture was allowed to stand until the evolution of gas had ceased. The resultant pinkish brown liquid was mixed with a hydrophilic cream (Neribase) to provide a white cream. Neribase is a cream vehicle containing Macrogol stearate 2000; stearic alcohol; liquid paraffin; white soft paraffin; polyacryiic acid; sodium hydroxide; disodium EDTA (i.e. ethylenediaminetetraacetic acid disodium salt); methyl and propyl Paraben (i.e. 4-hydroxybenzoic acid methyl and propyl esters) ; and water. The cream was applied to test skin areas of healthy volunteers having skin type II or III and, after a period of 20, 45 or 60 minutes, the treated skin exposed to UVB light for 10 to 20 seconds. The UVB source was a Saalmann UV-Test machine and the doses were 0.06, 0.05, 0.04, 0.03, 0.02 mJ/cirr (10 seconds) and 0.18, 0.15, 0.12, 0.09, 0.06 mJ/cirr (30 seconds) . The degree of erythema/tanning of the treated area and untreated area was determined by observation after 24 and 72 hours post-irradiation. The results are set forth in Table I below. Tha erythema increase is indicated on the scale +, ++ and +++ with ++ and +++ presenting a darker tan. -5- TABLE I Sex/ Skin T 24 h treated/ 72 h treated/ aσe type min sec control side control side 20 20 20 20 20 20 20 20 20 + - +++ grade of erythema / tanning T j = time between application and UVB irradiation T = time of UVB irradiation Example 2 The test of Example 1 was repeated using creams tc which calcium chloride had been added to provide 5 mmole or 10 mmole calcium ion content. The results are set forth in Tables II and III below. -6- TABLE II (5 mmol Ca 2+ ) T 2 24 h treated/ 72 h treated/ sec control side control side + - +++ grade of erythema / tanning T } = time between application and UVB irradiation time of UVB irradiation -7- TABLE III + - +++ : grade of erythema / tanning τ i = time between application and UVB irradiation T2 = time of UVB irradiation

Claims: -8- CLAIMS 1. A topical composition comprising a pseudocatalase, a sunscreen agent and a physiologically acceptable topical vehicle therefor. 2. A composition as claimed in Claim 1, which is free of calcium ions. 3. A composition as claimed in Claim 1, which contains 5 to 20 mmol calcium ions. 4. A topical composition as claimed in Claim 1, wherein the pseudocatalase is a transition metal co-ordination complex. 5. A composition as claimed in Claim 4, wherein the pseudocatalase is a Cu(I) , Fe(II) or Mn(II) co-ordination complex. 6. A composition as claimed in Claim 4, wherein the ligand of said co-ordination complex is bicarbonate. 7. A composition as claimed in Claim 6, wherein the pseudocatalase is a Mn(II)-bicarbonate complex. 8. A composition as claimed in Claim 7, wherein the Mn(II)-bicarbonate complex has been obtained by contacting manganous chloride with excess sodium bicarbonate in aqueous solution. 9. A method of enhancing tanning of skin which comprises applying to the skin an effective amount of a pseudocatalase. -9- 10. A pseudocatalase for use in the enhancement of tanning of skin on exposure to sunlight or UVB light. 11. The use of a pseudocatalase in the manufacture of a topical composition for the enhancement of tanning skin on exposure to sunlight or UVB light. 12. Use of a pseudocatalase to enhance tanning of skin on exposure to sunlight or UVB light.

Inventors: SCHALLREUTER KARIN UTA, WOOD JOHN MARTIN, SCHALLREUTER, KARIN, UTA, WOOD, JOHN, MARTIN
Applicants: STIEFEL LABORATORIES, STIEFEL LABORATORIES, INC.
Application year: 1992
Main classification: A61K7
IPC codes: A61K8, A61Q17, A61Q19