WO2001021148A1 - No-liberating topically applicable composition as biological agent, production and utilization thereof as dermatological and/or cosmetic product - Google Patents
No-liberating topically applicable composition as biological agent, production and utilization thereof as dermatological and/or cosmetic product Download PDFInfo
- Publication number
- WO2001021148A1 WO2001021148A1 PCT/EP2000/008067 EP0008067W WO0121148A1 WO 2001021148 A1 WO2001021148 A1 WO 2001021148A1 EP 0008067 W EP0008067 W EP 0008067W WO 0121148 A1 WO0121148 A1 WO 0121148A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- releasing compound
- composition
- composition according
- skin
- cosmetic
- Prior art date
Links
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
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
-
- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
Definitions
- NO-releasing topically applicable composition as a biological agent, its production and its use as dermatics and / or cosmetics
- the present invention relates to topically administrable NO-releasing compositions, their preparation and their use as pharmaceuticals and / or cosmetics.
- Nitric oxide which is also known in biochemistry as an endothelium-derived relaxing factor. According to Römpp Lexikon Naturtechnik 1997. p. 616, it has a number of physiological functions in vivo when it affects the human body, because it regulates blood pressure and the inhibition of platelet aggregation. wound healing, neuronal signal transmission, inactivation of bacteria, parasites and tumor cells. On the other hand, toxic concentrations of NO are held responsible for a number of diseases, e.g. septic shock, stroke, arthiritis migraine and chronic inflammation.
- diseases e.g. septic shock, stroke, arthiritis migraine and chronic inflammation.
- inorganic NO-releasing agents for example the salt sodium nitrite in an aqueous medium, are not only sensitive to oxidation and toxic in air,
- WO 99/13137 relates to the administration of L-arginine, its salts and derivatives on certain surfaces of the skin, wherein a substance is first applied to the skin which applies an effective amount of a substance, this amount being a biophysical external environment for the substance generated by which the substance passes from the vehicle into the skin and is absorbed by the skin.
- the administration of the substrate for endogenous NO formation described there serves both to stimulate blood circulation when warming cold tissue, to treat impotence, to promote hair growth, and to heal wounds superficial ulcers and finally pain relief
- WO 96/13164 describes a method for accelerated healing of skin wounds by topical application of a water-insoluble NO polymer adduct, which delivers therapeutic doses of nitrogen monoxide in an aqueous environment to the surface of the wound.
- a water-insoluble NO polymer adduct which delivers therapeutic doses of nitrogen monoxide in an aqueous environment to the surface of the wound.
- the insoluble nitrogen monoxide polymer adduct is an NO-polyethyleneimine cellulose
- CA 2 106 105 A1 relates to a polymer composition, a corresponding pharmaceutical preparation through which NO can be released as a cardiovascular agent
- DE 44 20 523 A1 relates, according to claim 1, to the use of NO-releasing compounds for the prevention and treatment of systemic inflammations. Consequently, the oral, rectal or parenteral application site is not the site of action, but rather is only achieved after absorption. Thus, the inventive topical use of the agent locally at which the The application site is the same as the site of action, neither disclosed nor suggested for cosmetic and special medical treatment options
- WO 93/020806 A1 describes the use of NO-releasing compounds for the systemic treatment of tumor diseases
- US Pat. No. 5,814,666 describes the use of liposome-encapsulated NO-releasing compounds for the systemic treatment of diseases caused by microorganisms. This makes the inventive topical use of the agent locally, where the application site is the same as the site of action, for cosmetic and special medical treatment options for vulgar psonasis and diseases from the similar form of cutaneous hyperpro feration, neither disclosed nor suggested
- the present invention is based on the object of providing an agent for topical administration which acts at the site of administration, and to provide an agent of this type for a prophylactic and therapeutic treatment of the abovementioned diseases and as a cosmetic
- the present invention thus relates to a composition
- a composition comprising at least one NO-releasing compound for use as a topically administrable agent which acts at the site of administration and has a biological action, L-arginine further excluding its salts and derivatives and NO-polyethyleneimine cellulose as the NO-releasing compound are
- This composition contains in particular at least one pharmaceutically contractual NO-releasing compound for use as a topically administered Dispensable agent with pharmaceutical activity
- This pharmaceutical composition contains 1 ⁇ mol to 200 mmol, preferably 10 ⁇ mol to 100 mmol, of the NO-releasing compound, based on 100 g of the total composition
- this composition contains at least one NO-releasing compound for use as a topically administrable agent with a cosmetic effect.
- this cosmetic composition 1 ⁇ mol to 200 mmol, preferably 5 ⁇ mol to 100 mmol, of the NO-releasing compound based on 100 g of the total composition, contain
- the NO-releasing compound contained in the composition is a spontaneously NO-releasing, biochemically or physically NO-releasing compound under physiological conditions
- NO-releasing compounds are e.g. S-nitrosothiols such as S-nitroso-thioglyzene or compounds of the class of the diazenium diolates, representative of a biochemically, for example enzymatically, NO-releasing compound is the sodium nitroprussiate, an example of compounds that are physically NO-releasing by UV rays is, for example, an alkali or alkaline earth nitrite, such as sodium nitrite
- NO-releasing compound used in the compositions according to the invention can be such that it is selected from inorganic and / or organic compounds which are preferably water-soluble or dispersible, the organic compounds being selected from the class of the S-nitrosothiols and the adducts of nitrogen monoxide with a nucleophile, for example from the class of the diazenium diolates
- Inorganic NO-releasing compounds are understood to mean the salts of nitrous acid, for example, the alkali and earth alkali salts in particular lithium nitrite, sodium nitrite, potassium nitrite, magnesium dinite and calcium dinitrite, furthermore also the nitro nitrate is to be classified here
- Organic NO-releasing compounds are understood to be those selected from the class of S-nitrosothiols, the adducts of nitrogen monoxide with a nucleophile (diazenium diolates) and the corresponding pro-drug systems.
- S-nitrosothiols are S-nitrosothiols , D- (S-N ⁇ troso) -3-mercaptomethylprop ⁇ onyl) -L-prol ⁇ n to name where S-nitroso-thioglyzene is preferred.
- the adducts of nitrogen monoxide with a nucleophile for example, the adducts of NO with polysaccharides mentioned in US Pat. No. 5,814,666 which are linked via primary and secondary aliphatic nurse, as well as S-nitroso-N-acetyl-penicillamine, S-nitroso-penicillamine and S-nitrosogluthathione
- compositions can furthermore contain 0.5% by weight to 20% by weight of light stabilizers for UV-A and / or UV-B, based on the total composition, the light stabilizer preferably being selected is from the class consisting of benzylidene camphor derivatives, dibenzoylmethane derivatives, benzotriazolene derivatives, tnazine derivatives, p-aminobenzoic acid derivatives, cinnamon ester derivatives, salicylic acid derivatives, anthranilic acid derivatives, urocanic acid derivatives, benzophenone dimethyl derivatives and / or benzophenone dimethyl derivatives
- compositions can also be artificial skin tanning agents, for example based on Dihydroxyacetone or also pigments or nanopigments with an average P ⁇ markomchen size of between 5 nm and 100 nm, preferably 10 nm to 50 nm, based on metal oxides, for example based on titanium oxide, either amorphous or crystallized in the form of rutile or anatase, pigments of iron , the zinc, the zirconium or the cerium as they are usually added in sunscreens.
- metal oxides as described in EP-A 0 518 772 and EP-A 0 518 773 can also be used as nanopigments
- the aforementioned cosmetic or pharmaceutical compositions can also contain other auxiliaries which are selected from nonionic, anionic, cationic or amphoteric emulators, thickeners, hydration agents, plasticizers, preservatives, dyes, opacifiers, agents for regulating the pH, propellants and perfumes
- compositions according to the invention are in the form of an ointment, a cream, a gel, embedded in liposomes, an oil, a milk, a solid stick or as an aerosol
- the composition can be in the form of a hydrophobic ointment, a water-absorbing ointment or a hydrophilic ointment.
- a hydrophobic ointment for their use as surface ointment, paraffin hydrocarbons, such as, for example, paraffins, or also polyalkylsiloxanes, or lipid substances of vegetable or animal origin are used as the ointment base in the hydrophobic ointments such as hydrogenated oils, medium-chain T ⁇ glyze ⁇ de, or partial Glyze ⁇ de, or waxes and low-viscosity esters and finally fatty alcohols and fatty acids into consideration.
- the hydrophilic ointments macrogols ie PEG or POE polymers are considered as the ointment basis.
- the composition can be in the form of a gel in the form of a hydrophobic or hydrophilic gel.
- Hydrophobic gels are based on liquid paraffin and polyethylene or fatty oils with additives
- hydrophilic gels are the hydrogels based on polyacrylates and acrylic acid or based von Cellulosemem We refer to the aforementioned monograph by Schoffhng-Krause S 324 - 327 and by Bauer, S 329 - 330
- the composition according to the invention can be in the form of a colloidally disperse system, with colloids serving as carriers for these compounds.
- colloids serving as carriers for these compounds.
- the composition can be in the form of an oil based on at least one fatty acid ester of a mineral or fatty oil.
- Such substrates are usually referred to as skin oils.
- the composition can be in the form of milk, that is to say as an oil in water emulsion.
- milk that is to say as an oil in water emulsion.
- the composition can be in the form of an aerosol dispersion, that is, either as a pressurized gas aerosol or as a pump aerosol.
- an aerosol dispersion that is, either as a pressurized gas aerosol or as a pump aerosol.
- composition according to the invention which contains at least one pharmacologically contractual NO-releasing compound, can be used for the treatment and prophylaxis of dermatoses or hyperprohferative dermatoses caused by electromagnetic rays of a wavelength of 1 mm to 1 nm, preferably 400 nm - 200 nm and prophylaxis of skin diseases or the skin can be carried out both on humans and on any mammal or bird, preference is given to use in humans and in domestic and farm animals, for example dogs, horses, pigs, cattle, calves, goats, sheep, the use being on People is particularly preferred
- the dermatoses caused by electromagnetic radiation selected from Combustio Erythema solar, light dermatoses eg Phytophotodermatm's photoallergic contact dermatitis, polymorphic light dermatosis or light urticaria and collagenoses such as cutan or systemic lupus erythematosus
- the hyperprohferative dermatoses are psonasis vulgar, seborrheic keratoses, keratoacanthomas, hyperprohferational dermatoses from the same group of forms the NO-releasing compound in such dermatoses has a differentiation-inducing effect on keratinocytes of the skin, this principle of action is to be exploited here
- the object of the present invention is to provide a method for cosmetic treatment for protecting the skin against damage caused by ultraviolet rays and, at the same time, to cause an increase in tanning (pigmentation) during use
- This relates to a method of cosmetic treatment for protecting the skin against damage caused by ultraviolet rays, which is characterized in that before or during the irradiation an effective amount of at least one NO-releasing compound-containing cosmetic composition is contacted with the skin surface
- the present invention is explained below by means of manufacturing and application examples. Parts are always given as weight points.
- the molar NO content in the composition is measured by known methods, for example by extraction of the NO-releasing substances using suitable solvents directly using chromatographic methods such as HPLC capillary electrophoresis or other analytical methods.
- the release of NO can be done, for example, either directly from the cream using a selective NO electrode (e.g. IsoNO World Presision Instruments, Sarasot FL USA), as well as electrochemical methods or electro- tron spin resonance or by means of chemical mescence eg after heating or UV irradiation of the cream can be detected.
- a selective NO electrode e.g. IsoNO World Presision Instruments, Sarasot FL USA
- electrochemical methods or electro- tron spin resonance or by means of chemical mescence eg after heating or UV irradiation of the cream can be detected.
- the activity of the guanylate cyclase can also be measured by increasing the cGMP level after appropriate aqueous extraction in the cell culture (Methods in Nitnc Oxide Research, ed. M Feelish and J Stamler, John Wiley & Sons, Chichester, 1996)
- Production example 1 (basic cream DAC with S-nitroso-thiols)
- a hydrophobic base gel obtained by reacting 5 parts of polyethylene and 95 parts of viscous paraffin, 9 ml of a 1 M stock solution of S-nitroso-thioglyze ⁇ n (SNOTG) in a final concentration of 80 mM at room temperature (20 ° C.) with thorough stirring mixed
- the preparation was carried out in accordance with Preparation Example 2, but 100 g of the hydrophobic gel were added to 2 ml of a 1 M stock solution of sodium nitroprussiate (final concentration 20 mM).
- Production example 1 was repeated and an additional 0.5 g of tocopherol acetate was added as a cosmetically active substance.
- Subject 8 is a patient with cutaneous lupus erythematosus who also benefited significantly.
- Subject 9 is a patient with polymorphic light dermatosis who benefited very impressively from the NO application (papules).
Abstract
Description
Claims
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00958469A EP1216019A1 (en) | 1999-09-22 | 2000-08-18 | No-liberating topically applicable composition as biological agent, production and utilization thereof as dermatological and/or cosmetic product |
AU69972/00A AU6997200A (en) | 1999-09-22 | 2000-08-18 | No-liberating topically applicable composition as biological agent, production and utilization thereof as dermatological and/or cosmetic product |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19945484.1 | 1999-09-22 | ||
DE19945484A DE19945484A1 (en) | 1999-09-22 | 1999-09-22 | NO-releasing topically applicable composition |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2001021148A1 true WO2001021148A1 (en) | 2001-03-29 |
WO2001021148B1 WO2001021148B1 (en) | 2002-06-06 |
Family
ID=7922947
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/EP2000/008067 WO2001021148A1 (en) | 1999-09-22 | 2000-08-18 | No-liberating topically applicable composition as biological agent, production and utilization thereof as dermatological and/or cosmetic product |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP1216019A1 (en) |
AU (1) | AU6997200A (en) |
DE (1) | DE19945484A1 (en) |
WO (1) | WO2001021148A1 (en) |
Cited By (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005003032A1 (en) * | 2003-07-03 | 2005-01-13 | The University Court Of The University Of St Andrews | Zeolites for delivery of nitric oxide |
CN105979969A (en) * | 2013-08-08 | 2016-09-28 | 诺万公司 | Topical compositions and methods of using the same |
US10206947B2 (en) | 2013-08-08 | 2019-02-19 | Novan, Inc. | Topical compositions and methods of using the same |
US10258564B2 (en) | 2013-02-28 | 2019-04-16 | Novan, Inc. | Topical compositions and methods of using the same |
US10265334B2 (en) | 2011-07-05 | 2019-04-23 | Novan, Inc. | Anhydrous compositions |
US10376538B2 (en) | 2009-08-21 | 2019-08-13 | Novan, Inc. | Topical gels and methods of using the same |
US10821203B2 (en) | 2008-11-21 | 2020-11-03 | Pq Silicas Uk Limited | Composition and dressing with nitric oxide |
US10912743B2 (en) | 2016-03-02 | 2021-02-09 | Novan, Inc. | Compositions for treating inflammation and methods of treating the same |
US11077194B2 (en) | 2012-03-14 | 2021-08-03 | Novan, Inc. | Nitric oxide releasing pharmaceutical compositions |
US11166980B2 (en) | 2016-04-13 | 2021-11-09 | Novan, Inc. | Compositions, systems, kits, and methods for treating an infection |
US11285171B2 (en) | 2018-03-01 | 2022-03-29 | Novan, Inc. | Nitric oxide releasing suppositories and methods of use thereof |
CN115089606A (en) * | 2022-06-30 | 2022-09-23 | 安徽医科大学 | Zinc/cerium composite nano material, preparation method thereof and application thereof in psoriasis treatment |
CN117442598A (en) * | 2023-12-25 | 2024-01-26 | 天津嘉氏堂科技有限公司 | Application of nitrate compound in preparation of sensitive muscle epidermis barrier improving product |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2856592B1 (en) * | 2003-06-27 | 2008-04-25 | Oreal | A COSMETIC COMPOSITION BASED ON A RADICAL THIYL DRYER (S) FOR THE PERMANENT DEFORMATION OF KERATIN FIBERS |
FR2856591B1 (en) * | 2003-06-27 | 2005-10-14 | Oreal | COSMETIC COMPOSITION BASED ON NITROSONIUM SALT (S) FOR THE PERMANENT DEFORMATION OF KERATIN FIBERS. |
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-
1999
- 1999-09-22 DE DE19945484A patent/DE19945484A1/en not_active Ceased
-
2000
- 2000-08-18 EP EP00958469A patent/EP1216019A1/en not_active Withdrawn
- 2000-08-18 AU AU69972/00A patent/AU6997200A/en not_active Abandoned
- 2000-08-18 WO PCT/EP2000/008067 patent/WO2001021148A1/en not_active Application Discontinuation
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JP2007526867A (en) * | 2003-07-03 | 2007-09-20 | ザ ユニヴァーシティー コート オブ ザ ユニヴァーシティー オブ セント アンドリューズ | Zeolite for releasing nitric oxide |
AU2004253749B2 (en) * | 2003-07-03 | 2010-04-01 | The University Court Of The University Of St Andrews | Zeolites for delivery of nitric oxide |
EA014704B1 (en) * | 2003-07-03 | 2011-02-28 | Ти Юниверсити Корт Оф Ти Юниверсити Оф Ст Эндрюс | Fully or partially dehydrated zeolite material for dosing of nitric oxide |
JP4818108B2 (en) * | 2003-07-03 | 2011-11-16 | ザ、ユニバーシティー、コート、オブ、ザ、ユニバーシティー、オブ、セント、アンドルーズ | Zeolite for releasing nitric oxide |
US8722103B2 (en) | 2003-07-03 | 2014-05-13 | University Court Of The University Of St. Andrews | Zeolites for delivery of nitric oxide |
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US10912743B2 (en) | 2016-03-02 | 2021-02-09 | Novan, Inc. | Compositions for treating inflammation and methods of treating the same |
US11166980B2 (en) | 2016-04-13 | 2021-11-09 | Novan, Inc. | Compositions, systems, kits, and methods for treating an infection |
US11285171B2 (en) | 2018-03-01 | 2022-03-29 | Novan, Inc. | Nitric oxide releasing suppositories and methods of use thereof |
CN115089606A (en) * | 2022-06-30 | 2022-09-23 | 安徽医科大学 | Zinc/cerium composite nano material, preparation method thereof and application thereof in psoriasis treatment |
CN115089606B (en) * | 2022-06-30 | 2023-09-26 | 安徽医科大学 | Zinc/cerium composite nano material, preparation method thereof and application thereof in psoriasis treatment |
CN117442598A (en) * | 2023-12-25 | 2024-01-26 | 天津嘉氏堂科技有限公司 | Application of nitrate compound in preparation of sensitive muscle epidermis barrier improving product |
CN117442598B (en) * | 2023-12-25 | 2024-03-12 | 天津嘉氏堂科技有限公司 | Application of nitrate compound in preparation of sensitive muscle epidermis barrier improving product |
Also Published As
Publication number | Publication date |
---|---|
EP1216019A1 (en) | 2002-06-26 |
WO2001021148B1 (en) | 2002-06-06 |
DE19945484A1 (en) | 2001-04-05 |
AU6997200A (en) | 2001-04-24 |
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