Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
  • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
  • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
  • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/673—Vitamin B group
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P39/00—General protective or antinoxious agents
  • A61P39/02—Antidotes

Definitions

• the invention relates generally to a systemically and / or topically applicable sunscreen and in particular to a systemically acting oral sunscreen which has nicotinamide, folic acid or a combination thereof as active sunscreen substances. It also relates to the use of the substances mentioned above for the production of a systemically and / or topically applicable light stabilizer.
• the effect of sunlight on the human skin organ leads to a physiological, non-pathological reaction to the erythema solar or solaris, ie the reddening of the skin by the sun.
• a pathological reaction dermatitis solaris, ie inflammation of the skin caused by sunlight.
• the transitions from erythema solaris to dermatitis solaris are fluid and individually different. They depend on the one hand on the intensity of the sunlight, on the other hand on the natural skin protection against the sunlight and thus on the individual sensitivity to light, which can be normal or increased and thus pathological.
• the composition of sunlight is largely constant in that UV-A, B, C, visible light and infrared light act on human skin, of which UV-B is responsible for reddening the skin and UV-A is responsible for skin pigmentation become.
• the sun intensities can be variable, which also depends on the angle of incidence of light.
• sun protection is effected (1) by the thickness of the horny layer (so-called Miescher * see light calluses) and (2) by the density of melanin, the body's own skin pigment. The quantitative increase of both factors enables light protection vice versa.
• Sunscreens are sunscreens for protecting human skin against the damaging effects of direct and indirect radiation.
• the ultraviolet radiation of the sun which is responsible for the often desired skin tanning, is divided into UV-C (wavelengths 200 - 280 nm), UV-B (280 - 315 nm) and UV-A (315 - 400 nm).
• the intensity of the effective radiation is dependent on geographic, climatic (snow reflection) and other factors and possibly also on air pollution.
• the short-wave UV-C does not appear on the ground, because this radiation in the atmosphere is absorbed by the ozone (if) present there.
• the pigmentation of normal skin under the influence of solar radiation ie the formation of melanin
• UV-B and UV-A Irradiation with UV-A rays results in the direct darkening of the melanin bodies already present in the epidermis.
• the UV-B causes indirect pigmentation.
• the skin is exposed to the unfiltered radiation, which - depending on the duration of exposure - can lead to the formation of reddened skin (erythema), skin inflammation (sunburn) and even blistering.
• the stress on the organism associated with such skin lesions can cause headaches, weariness, fever and cardiovascular disorders.
• UV absorbers or light filters are benzophenone derivatives, hydroxynaphthoquinones, phenylbenzoxazoles and phenylbenzimidazoles, digalloyl trioleate, aminobenzoic acid esters, salicylic acid esters, alicyclic dienones, cinnamic acid esters and benzalazine.
• Aromatic urea derivatives and certain sulfonamides, coumarin derivatives, phenylglyoxylic acid derivatives and others have been proposed as sunscreens.
• Natural sunscreens are mink, avocado, almond, sesame, peanut, olive, Sanflor, coconut and other oils.
• the commercial sunscreens are offered as sun oil, milk (emulsions), cream, jelly, lotion, spray oil and spray emulsions. Their effectiveness depends on the type of light filter used and its concentration.
• sunscreens are added additional agents such as dihydroxyacetone, carotene or walnut shell extracts, which cause an artificial browning of the horny layer.
• a disadvantage of the previous means is the fact that each area of the body to be protected must be protected more or less strongly from sun exposure by local application to the skin without there being a reliable guarantee that the protection will be fully developed and the person will not suffers from a sunburn.
• Unprotected parts of the body, for example the scalp, which are unintentionally exposed to the sun's rays are mostly particularly affected by sunburn.
• the majority of the topically applied is due to abrasion, washing, bathing and body sweat Sunscreen (oil, cream) removed, so that reapplication is necessary, which is annoying, possibly also unreliable and often also only incomplete, since it is only possible under experimental conditions to apply the light filter in the same layer thickness.
• the invention is based on the object of providing light protection which develops effective systemic and / or topical prophylaxis against the action of light and the pathogenic effect of light, which includes all parts of the body with their skin organs in the light protection and which provides long-term light protection.
• the invention proposes the use of nicotinic acid amide, folic acid or combinations thereof in a systemically and / or topically applicable and in particular in an oral sunscreen.
• a systemically and / or topically applicable and in particular in an oral sunscreen Through topical application, parenteral application or oral intake of nicotinic acid amide and / or folic acid, all parts of a person's skin are effectively protected against the disease-causing effects of light, in particular sunlight, over a period of more than 12 hours.
• the systemic and / or topical prophylaxis which can be achieved according to the invention serves to protect the skin from physiological and pathological light reactions.
• Nicotinamide acts only to a limited extent, although daily amounts in an adult human up to 3,000 mg may be required. The daily amount can be administered in a single dose or staggered. Folic acid alone also has a light protection effect. Daily amounts of 10 to 30 mg folic acid are already effective.
• a combination of nicotinic acid amide and folic acid in a weight ratio of preferably 10: 1 to 60: 1, preferably with a weight ratio of 30: 1 to 50: 1, has a synergetic effect such that the necessary amount of the two Connections within the combination can be less than when using only one of the connections.
• the active substances can be incorporated in the appropriate dosage into the customary oral formulations.
• Common formulations are tablets, capsules, dragees, juices, injections, syrups, inhalation vehicles and the like.
• the vehicles or carriers used for these individual formulations are the same as are generally known from galenics.
• the corresponding preparations of the active substances for the injections should also be provided.
• systemic sunscreen according to the invention can of course also be used as a supplement to the customary topically applicable suntanning oils, creams, lotions and ointments.
• Nicotinamide was compounded and tableted together with conventional tableting compositions.
• the single tablet received 200 mg nicotinamide.
• nicotinic acid amide and folic acid with a weight ratio of 40: 1 were formulated into tablets which had a composition with 200 mg of nicotinic acid amide and 5 mg of folic acid.
• Example 2 The administration of the oral sun protection according to Example 2 led the boy to re-exposure in the southern sun without any skin symptoms in the sense of light dermatosis and that in the following years the primary exposure was also possible without incompatibility with light.
• the patients also stated that they had seen no or only mild reddening of the skin after sun exposure without the tanning effect of the sun exposure being reduced.
• the combination according to the invention was used by the patients with constant success when traveling in Sun lands applied.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Birds (AREA)
• Dermatology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Toxicology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Liquid Crystal (AREA)
• Prostheses (AREA)
• Glass Compositions (AREA)

Priority Applications (4)

Applications Claiming Priority (2)

Publications (1)

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Family Applications (1)

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Cited By (2)

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Citations (3)

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• 1990
  • 1990-06-13 DE DE4018964A patent/DE4018964C1/de not_active Expired - Lifetime
• 1991
  • 1991-05-24 AT AT91909455T patent/ATE108993T1/de active
  • 1991-05-24 AU AU78657/91A patent/AU645092B2/en not_active Ceased
  • 1991-05-24 CA CA002059641A patent/CA2059641A1/en not_active Abandoned
  • 1991-05-24 DE DE59102350T patent/DE59102350D1/de not_active Expired - Fee Related
  • 1991-05-24 WO PCT/DE1991/000433 patent/WO1991019478A1/de not_active Ceased
  • 1991-05-24 ES ES91909455T patent/ES2061248T3/es not_active Expired - Lifetime
  • 1991-05-24 EP EP91909455A patent/EP0486632B1/de not_active Expired - Lifetime
  • 1991-05-24 JP JP3509066A patent/JPH0635387B2/ja not_active Expired - Lifetime

Patent Citations (3)

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