USOO5652261A United States Patent 19 11 Patent Number: 5,652,261 Ismail 45 Date of Patent: *Jul. 29, 1997 54 METHOD FOR THE TREATMENT AND 964444 8/1964 United Kingdom. PROTECTION OF THE SKN 1453239 10/1976 United Kingdom. 84-02845 8/1984 WIPO. 76 Inventor: Roshdy Ismail, Siebengebirgealee 2, 5 Köln 4, Germany OTHER PUBLICATIONS Dr. R. A. Eckstein, "Lichtwirkung und Lichtschutz" from * Notice: The term of this patent shall not extend Kosmetologie, Nirnberg 1971, pp. 218-228, Linde Eckstein beyond the expiration date of Pat. No. KG. 5,541,220. A. Ya. Potapenko et al., “Inhibition of 8-Methoxypsoralen Photosensibilized Erythema by O-Tocopherol", May 1980, (21 Appl. No.: 298,612 pp. 560-563, BJull. Eksp. Biol. Med. 89(5). "The Effective Non-Paba UV-B Filter", Parasol, Givaudan 22 Filled: Aug. 31, 1994 (brochure). (1980). "Everyday Skin Protection", Parasol, Givaudan (brochure). Related U.S. Application Data (1980). 63 Continuation of Ser. No. 877,377, Apr. 29, 1992, Pat. No. J. P. Van Braeken, “Vitamins in Cosmetology", pp. 10-12, 5,541.220, which is a continuation of Ser. No. 518,565, May Roche Information Service (brochure). (1983). 3, 1990, abandoned, which is a division of Ser. No. 211,125, "Cosmetic Chemists Hear Vitamin E Endorsement” (bro Jun. 21, 1988, Pat. No. 4,938,960, which is a continuation of chure). (1983). Ser. No. 900,727, Aug. 27, 1986, abandoned, which is a continuation-in-part of Ser. No. 706,723, Feb. 28, 1985, Roger H. Brodkin, M.D. et al., “Sensitivity to Topically abandoned. Applied Vitamin E”, Arch. Derm.92 (1965), pp. 76-77. Machlin, “Vitamin E, A Comprehensive Treatise.” (text 30 Foreign Application Priority Data book), pub. Marcel Dekker, Inc., 1980, pp. 579-584. Mar. 7, 1984 DE Germany .......................... 34 08 258.1 W. Pschyrembel, Klinisches Worterbuch, Gruyter, N.Y., Mar. 23, 1984 DEI Germany .......................... 34 10 641.3 1982, p. 369. Jun. 1, 1984 DEI Germany .......................... 3420 459.8 H.D. Cremer, et al., Biochemie und Physiologie der Ernahr Jul. 25, 1984 DE Germany .......................... 3427 374.3 ung, Verlag, N.Y., 1980, pp. 62-63. Sep. 25, 1984 DEI Germany ... 34 35 098.5 Geza Loranth et al., Chemical Abstracts, 30(21): 7634-3 Nov. 15, 1984 DEI Germany ... 344 T11-T. (Nov. 10, 1936). Feb. 12, 1985 DEI Germany .......................... 35 04. 695.3 A. S. Melkumyan et al., Chemical Abstracts, 90(15): (51 Int. Cl. ........... A61K 31/355 115236g (Apr. 9, 1979). 52 U.S. Cl. .......................... 514/458; 514/52; 514/63; Kanebo Cosmetics, Chemical Abstracts, 95(18): 156366W 514/168; 514/276; 514/331; 514/548; 514/560; (Nov. 2, 1981). 514/887 Rote Liste, 1961, p. 356, "Fissan-Baby-O", Editio Cantor, Aulendorf/Wirt, 58 Field of Search ............................... 514/458, 52, 63, Rote Liste, 1983, No. 31 226, “Akne-Ex H”, No. 31 213, 514/168,276,331, 356,548,560, 887 Magopsor and No. 31 150. Delta Pimafucort, Editio Cantor, 56 References Cited Aulendorf/Wirt, Unlisted Drugs, vol. 24, No. 1, Jan. 1972, p. 10, “Norderm". U.S. PATENT DOCUMENTS Unlisted Drugs, vol. 18, No. 3, Mar. 1966, p. 27, “Robu Sanon'. 3,943,248 3/1976 Shulman .............................. 424/196.1 4,144,325 3/1979 Voyt ........................................ 514/.458 Henry Goldschmiedt, “Vitamin Ein Cosmetics”, Aug. 1972, 4,154,823 5/1979 Schutt .................................. 424/195.1 pp. 41-42, Soap/Cosmetics/Chemical Specialities. 4,248,861 2/1981 Schutt ....................................... 424/92 Primary Examiner-Kevin E. Weddington 4,454,159 6/1984 Musher ................................... 514/458 Attorney, Agent, or Firm-Jacobson, Price, Holman & 4,525,344 6/1985 Tutsky ..................................... 54,458 4,938,960 7/1990 Ismail ...................................... 54,458 Stern, PLLC 4,983,626 1/1991 Ismail ...................................... 514,458 57 ABSTRACT FOREIGN PATENT DOCUMENTS The present invention relates to a method for the treatment 0027987 5/1981 European Pat. Off.. and protection of human and animal skin which contains 0133258 2/1985 European Pat. Off.. vitamin E in a high dose and, in addition, may optionally 2105254 4/1972 France. further contain vitamin C, vitamin A, vitamins of the B 22O1070 4/1974 France 2289178 5/1976 France. series, blood circulation-promoting agents and/or 2492659 4f1982 France. vasodilators, phospholipids, unsaturated fatty acids and/or 67210 6/1969 Germany. emulsifiers. 2240187 2/1974 Germany. 822824. 4/1981 U.S.S.R. 18 Claims, No Drawings 5,652.261 1. 2 METHOD FOR THE TREATMENT AND It has further been known that cholesterol in human and PROTECTION OF THE SKN animal skin is converted by ultraviolet radiation into cholesterol-alpha-oxide, a substance known to be carcino CROSS-REFERENCE TO RELATED genic. Experiments with mice have shown that upon admin APPLICATION istration of vitamins E and Cand of two further antioxidants This application is a continuation of Ser. No. 07/877,377, no cholesterol-alpha-oxide will be formed (Pharm. Indu.36, filed Apr. 29, 1992, now U.S. Pat. No. 5,541.220 which is a Nr. 3 (1974) Anschel, U.S.A.). continuation of Ser. No. 07/518.565, filed May 3, 1990, It has now surprisingly been found that vitamin E and abandoned, which is a divisional of Ser. No. 07/211,125, combinations comprising vitamin E together with other filed Jun. 21, 1988, U.S. Pat. No. 4938,960, which is a 10 active substances, more specifically, are suitable as agents continuation of Ser. No. 06/900,727, filed Aug. 27, 1986, for the treatment of eczema, skin tetter, skin inflammations, abandoned, which is a continuation-in-part of Ser. No. itch, allergies, wrinkles, pigmentations in the skin, and 06/706,723, filed Feb. 28, 1985, abandoned. alopecia as well as wounds. Moreover, the agents according to the invention can be employed as protective agents BACKGROUND OF THE INVENTION 15 against ultraviolet light and for promoting hair growth. The The present invention relates to an agent containing agents according to the invention are further suitable as vitamin E for treating and protecting the skin. skin-protecting agents in cases of exposure to radiation, e.g. Vitamin E is known as an antioxidant and protective of cancer patients. This new range of indications was not vitamin for phospholipids of the cell membrane. It maintains foreseeable from the state of the art and will open a new the permeability and stability of the cell membrane; cf. Lucy, 20 wide field of applications for vitamin E. The use of vitamin Annals N.Y. Academy of Science 203, p. 4 (1972). There has E. at long sight, will result in a stabilization and permanent further been known that vitamin E has a membrane-sealing elimination of the symptoms, so that the probability of a effect; cf. F. Mittelbach and G. Bodechtel, Munchner Mediz relapse is very low. However, the combination preparations inische Wochenschrift 110 (1968) 36: pp. 1988-1993. In containing vitamin E will have to be taken over an extended erythrocytes, the simplest cells of the human body, there has period of time, for about 6 months or longer. been found that vitamin E provides a protective effect for the SUMMARY OF THE INVENTION cell membrane. In tests with animals and humansit has been proven that anemia is a first signal of a deficiency of vitamin Thus, it is the object of the present invention to provide E. The hemolysis of the erythrocytes will normalize upon agents containing vitamin E for use in the treatment and for administration of high doses of vitamin E; cf. William J. 30 the protection of human and animal skin, which agent is Darbey Vitamin Horm., 26 (50) pp. 685–704 (1968) and characterized in that it contains a high dose of vitamin Eas Phelps DLPediatrics 63 (6) pp.933–935 (1979). From these the essential ingredient in addition to conventional carriers references from the literature there is apparent that after the and/or excipients and, optionally, vitamin C, vitamin A, oral administration of from 200 to 800 mg of vitamin Eover vitamins of the B series, blood circulation promoters and/or a period of from 1 to 4 days the hemolysis of the erythro 35 other vasodilators, phospholipids, unsaturated fatty acids cytes is significantly improved as compared to patients and/or emulsifiers. suffering from vitamin E deficiency. DETALED DESCRIPTION OF THE Vitamin E has further been used to treat sickle cell anemia INVENTION over a period of from 6 to 35 weeks; cf. Natt CL. Am. J. Clin. Since vitamin E is liquid at room temperature, the capsule 33, pp. 968–971 (1980); Natt CL. Am. J. Clin. Nutr. 32, pp. offers itself as a form of application in the first place. The 1359–1362 (1979); Gawlik G. M. Fed. Proc. 35 (3), p. 252 other active ingredients are incorporated in vitamin E and, if (1976) and Gorash L. Bieri J. G. et al. Univ. Conn. desired, in a readily liquid neutral oil and a solutizer and Farmington, GT. introduced into the capsules in a perse known manner. Here It has further been known that a daily dose of 750 mg of 45 emulsifiers such as, e.g., Tween, may be used. vitamin E over a period of from 3 to 6 months was In the agents according to the invention, above all, a successfully used to treat thalassemia patients, whereupon a sufficient dosage of vitamin E which should be at least 200 normalization of the hemolysis of the erythrocytes was mg is crucial for the efficacy of vitamin E. Lower dosages of observed; cf. Kahane I. ISR. J. Mad. 12 (1), pp. 11-15 vitamin E are useless, since large parts thereof are destroyed (1976). 50 by the gastric acid and thereby lose their activity; cf.