Active substance for treating alterations of the skin and the mucous membranes.
Abstract
An active substance for topical treatment of changes in the skin and mucous membranes, in particular those due to metabolic and tissue diseases, is a mixture of substances, namely component (a) and component (b). Component (a) consists of at least one aminopolycarboxylic acid and/or its salts and/or its derivatives or of gluconic acid and/or its salts and/or its derivatives. Component (b) consists of at least one salt and/or derivative of a fruit acid. The active substance results in rapid abatement of the symptoms, including those of psoriasis, acne, lichen ruber, neurodermatitis, periodontitis, gingivitis, and herpes. It can be used in pharmaceutical and cosmetic products.
Term
Term ended
Projected expiry passed 9 February 2009, 17.6 years ago.
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12 claims: 9 independent, 3 dependent
- c-de-00011. substance mixture of a) at least one aminopolycarboxylic acid N-carboxymethyl groups and / or their salts and / or its derivatives b) at least one salt and / or derivative of a fruit acid as an active ingredient for Treatment of skin and mucosal changes.
- c-de-00044. substance mixture according to claims 1 to 3, characterized in that b) consists of a salt or derivative of citric acid, preferably their ammonium salt.
- c-de-00055. substance mixture according to claims 1 to 4, characterized in that the mixture of a) and b) is used in an assembly,) are present in a concentration of 0.1 to 50% by weight of a) and b on the total mass of the respective preparation.
- c-de-00066. Subsstanzgemisch from a) at least one salt and / or derivative of gluconic acid and b) at least one salt and / or derivative of a fruit acid as active ingredient in the manufacture of topischenn preparations for the treatment of skin and mucosal lesions.
- c-de-00088. mixture of substances according to claims 6 or 7, characterized in that b) consists of a salt or derivative of citric acid, preferably its ammonium salt, is.
- c-de-00099. substance mixture according to claims 6 to 8, characterized in that the mixture of a) and b) is used in an assembly,) are present in a concentration of 0.1 to 50% by weight of a) and b on the total mass of the respective preparation.
- c-de-001010. A cosmetic preparation, characterized in that the substance mixture according to claims 1 to 5 and / or 6 comprises in addition to customary for formulating additives and optionally further active compounds to 10th
- c-de-001111. Application of the substance mixture according to claims 1 to 5 and / or 6 to 10 in the cosmetic treatment.
- c-de-001212. The use of the substance mixture according to claims 1 to 5 and / or 6 to 10 for the manufacture of pharmaceutical preparations for the treatment of skin and mucosal lesions.
Independent claims9
12 paragraphs, as filed
p0001The invention assumes that occurs as a result of a change in the metabolism of most diseases. These metabolic changes are determine to a large extent differences in the field of trace elements. It is well known that a lack of trace elements causing specific deficiencies. Oversupply also triggers atypical disorders.
p0002For the treatment of metabolic disorders such as exist in Schwermetallintoxikationen or arteriosclerosis and related diseases, have polyamino, particularly ethylenediaminetetraacetic acid (EDTA) proven (BW Halstead "The Scientific Basis of EDTA Chelation Therapy" Golden Quill Publ. Inc., Colton 1979 pages 21 to 27).
p0003The complexing action of polyhydroxycarboxylic and their salts, such as the D-gluconates, one uses in the calcium therapy and for providing bioavailable iron in toning agents from (pharmaceutical substance list, eds. ABDA, Frankfurt / Main "gluconic" P. 84 to 87).
p0004Fruit acids, citric insbesonder previously found application in pharmaceuticals as acidifiers in effervescent tablets, taste modifier, Desinfizienz and stomach acid substitution (pharmaceutical substance list, Edit .: ABDA, Frankfurt / Main "citric" p 86 to 89).
p0005In DE-OS 16 17 607, mixtures of heavy metal salts, input and polybasic Di-nitrilo-R-carboxylic acids and R-oxy-R-carboxylic acids indicated that have physiological effects on rheumatism, viral infections and promote wound healing.
p0006these groups of substances have been used so far neither alone nor in combination for the treatment of the consequences of metabolic disorders in the skin, mucous membranes and skin appendages.
p0007It has now surprisingly been found that, as described in the claims, by a combination of salts or derivatives of fruit acids with salts complex-forming organic acids such as of aminopolycarboxylic acids and / or their salts and / or their derivatives or of a salt and / or derivative of gluconic can influence the consequences of metabolic and tissue diseases of skin, mucous membranes and skin appendages positive.
p0008Thus excess supply can be eliminated by complexing salts or can be brought into a form which allows for better or easier distribution at a lower supply.
p0009The claimed formulations showed a surprisingly wide spectrum of action. For all diseases described below occurred in a very short time a relief or cure. As very much must be emphasized that the formulations are not toxic and do not show any side effects.
p0010The active substance of the invention was used in various skin and mucosal changes:<ul><li>1. Presentation by<ul><li>a) <u>bacteria</u> eg folliculitis, boils</li><li>b) <u>viruses</u> for example herpes simplex, varicella, aphthous</li><li>c) <u>microbes</u> eg stomatitis, periodontitis</li><li>d) <u>mushrooms</u> eg intertrigo</li></ul></li><li>2. diseases caused by physical or chemical noxae eg hyperkeratosis, mechanical skin damage (eg scars)</li><li>3. Diseases caused by exogenous or endogenous allergens eg cheilitis, contact dermatitis due to plants, metals or drugs, psoriatic group, eczema, lichen planus</li><li>4. Diseases caused by metabolic disorders (including toxic) eg acne vulgaris, eczema seborroicum, hyperhidrosis</li><li>5. Diseases caused by endocrine disorders eg periodontal disease, fibrosis There is evidence that the agents may also have a cytostatic effect (see FIG. 5)</li><li>7. A cosmetic skin treatment.</li></ul>
application examples
p0011<ul><li>1. With a solution consisting of: 20% ammonium citrate 10% sodium gluconate 5% sodium lactate 65% H₂O Subjects were treated. The solution was applied with cotton swabs.<ul><li>A) <u>Diagnosis:</u> Allergic eczema on both hands Therapy: a) cortisone preparations - no improvement b) solution claimed - skin lesions healed within 6 days</li><li>B) <u>Diagnosis:</u> Psoriasis all over the body (histologically proven in Dermatology) After 15 weeks of inventive treatment lesion healed; Itching removed after 3 days.</li><li>C) <u>Diagnosis:</u> Acne vulgaris (for 7 years) Rouge By treating with an inventive solution after 2 weeks</li></ul></li><li>2. Using a solution consisting of: 20% ammonium citrate 10% (Ethylendinitrilotetraessigasäure disodium) dihydrate 5% sodium lactate 65% H₂O Subjects were treated in the same manner. The healing effect was congruent with the Example 1. In some cases, the substance mixture was applied as a gel, in order to achieve better adherence to the treatment sites. To this end, the solution was placed in ointment consistency with highly disperse silica. It was observed in the treated subjects a strong tightening of the upper parts of the skin, so that it can be assumed that this preparation is to be used as a cosmetic.</li><li>3. solution consisting of 10% by weight citric acid 5 wt% ethylenediaminetetraacetic 85 wt% H₂O pH adjusted to 9 with KOH. With this solution, 6 subjects were treated. <u>Diagnosis:</u> seborrheic dermatitis <u>Therapy:</u> The affected areas were 2 - 3 times a day easily rubbed.. Skin lesions healed after 8 days.</li><li>4. solution consisting of: 0.1% by weight citric acid 0.5 wt% (ethylenediaminetetraacetic acid disodium salt) dihydrate 99.4 wt% H₂O pH adjusted to 5.2 with NaOH. With this solution, 3 subjects (infants) were treated. <u>Diagnosis:</u> neurodermatitis <u>Therapy:</u> The affected areas were slightly daily rubbed with the solution 3 times. Relief of typical itching after 8 hours. Healing after 12 days.</li><li>5. solution consisting of: 10% by weight malic acid 5% by weight (ethylenediaminetetraacetic acid disodium salt) dihydrate 85 wt% H₂O pH was adjusted with ammonia to 5.2. With this solution, 10 subjects were treated. <u>Diagnosis:</u> gingivitis simplex <u>Therapy:</u> Brush the affected areas. Already after the first treatment, a decay of the inflammatory symptoms was observed. Healing in 2 times a day. Application after about 7 days.</li><li>6. A solution consisting of: 10% by weight potassium citrate 3% by weight cyclohexylene (1,2) -dinitrilotetraessigsäure (monohydrate) 87 wt% H₂O was placed in ointment consistency means highly disperse silica. This ointment 4 subjects were treated.<u>Diagnosis:</u> Heavily exuding and itchy eczema <u>Therapy:</u> 2 times a day. Applying the ointment. Skin changes depending on the severity after 4 - 9 weeks abgheilt.</li><li>7. A solution consisting of: 20% by weight potassium citrate 5 wt% diethylenetriaminepentaacetic acid, 3-aza-3- (carboxymethyl) pentamethylendinitrilotetraessigsäure 75 wt% H₂O was placed in ointment consistency with highly disperse silica. This ointment subject was enrolled. <u>Diagnosis:</u> Wasp sting with local infection, allergic skin reaction and swelling of the left lower leg lateral. <u>Therapy:</u> 2 times a day. Applying the ointment. Itching after 10 minutes. Decayed. After 3 days the entire allergic skin reaction had subsided and healed the local infection at the injection site. After discontinuation of the ointment no recurrence.</li><li>8. A reading consisting of: 5% by weight potassium citrate 0.1 wt% of bis (aminoethyl) glycol ethers-N, N, N ', N'-tetraacetic acid (3.6 Dioxaoctamethylen-dinitrilo-tetraacetic acid) 94.9 wt% H₂O was brought to salve consistency with talc. This ointment 4 patients were treated. <u>Diagnosis:</u> Strong contact allergy <u>Therapy:</u> 1 -. 2 times daily application of ointment to the affected areas. Skin lesions after 4 - 6 days healed.</li><li>9. Using a solution consisting of: 10% by weight ammonium citrate 5% by weight sodium gluconate 85 wt% H₂O were treated 9 subjects: <u>Diagnosis:</u> tonsillitis <u>Therapy:</u> The initial solution was developed by the subjects themselves with tap water to 1: 1 - 1: 4 diluted and 3 - 4 times a day gargled.. After 2 - 3 days, the subjects were free of symptoms.</li><li>10. With a solution of: 20% by weight ammonium citrate 10% by weight ethylenediaminetetraacetic acid disodium salt - dihydrate 70 wt% W / O emulsion 3 treated subjects. <u>Diagnosis:</u> rosacea <u>Therapy:</u> 2 times daily application of the emulsion. After 4 days there is a clear decline in the lesions. After treatment for 4 weeks and discontinuation of ointment no recurrence.</li><li>11. With a solution consisting of: 20% by weight ammonium citrate 10 wt% (ethylenediaminetetraacetic acid disodium salt) - dihydrate 70 wt% H₂O treated 32 subjects. <u>Diagnosis:</u> Strong periodontitis <u>Therapy:</u> was administered by 2 - 3 times a day applying with cotton swabs.. Healing, after 10 - 14 days depending on the severity of the phenomenon.</li><li>12. solution consisting of: 20% by weight ammonium citrate 10 wt% (ethylenediaminetetraacetic acid disodium salt) - dihydrate 70 wt% H₂O This solution was adjusted by means of highly disperse silica in ointment consistency. It dealt herewith 8 subjects. <u>Diagnosis:</u> Lichen Planus <u>Therapy:</u> The parts to be treated, 1 - 2 times daily with the ointment pocketed.. Significant improvement already after the 3rd treatment. Recovery without relapse after about 4 months.</li><li>13 solution consisting of: 3% by weight ammonium tartrate 3% by weight (ethylenediaminetetraacetic acid disodium salt) dihydrate 94 wt% H₂O With this solution, 1 subject was enrolled. <u>Diagnosis:</u> herpes simplex <u>Therapy:</u> was applied 2 - 3 times a day with cotton swabs.. In all cases, healing after 3 - 4 days.</li><li>14 solution consisting of: 0.1% by weight of nitrilotriacetic acid 0.2 wt% of fumaric acid disodium salt 50.0 wt% ethyl alcohol 49.7 wt% H₂O This solution was adjusted by means of highly disperse silica in ointment consistency. were treated 11 subjects. <u>Diagnosis:</u> contact dermatitis <u>Therapy:</u> By rubbing the affected areas decrease in lesions after about 8-12 hrs .; Healing after 3 - 4 days.</li></ul>
Every citation, both ways
| Document | Relation | Office | Category | Cited during |
|---|---|---|---|---|
| WO9744006A1 | Cited by | World Intellectual Property Organization (WIPO) | – | International search |
| US6391325B1 | Cited by | United States of America | – | Applicant |
| ES2110921A1 | Cited by | Spain | – | Search report |
| US1861189A | Cites | United States of America | X | Search report |
| FR2108827A1 | Cites | France | Y | Search report |
| US3452049A | Cites | United States of America | X | Search report |
| US3558769A | Cites | United States of America | X | Search report |
| US3699221A | Cites | United States of America | X | Search report |
4 priority claims, no other members on record
Priority claims4
| Document | Office | Kind | Date |
|---|---|---|---|
| 3804141 | Germany | A | |
| 3804141 | Germany | – | |
| DE19883804141 | – | – | – |
| 3804141 | – | – | – |
6 legal events, as the office reported them to INPADOC
Over the term
Point at a mark for the eventEvents
| Event | Code | |
|---|---|---|
| Application withdrawnWithdrawn18W | 18W | |
| Information on the status of an ep patent application or granted ep patentGrantedSTATUS: THE APPLICATION HAS BEEN WITHDRAWNSTAA | STAA | |
| Designated contracting statesAK | AK | |
| Search report despatchedORIGINAL CODE: 0009013PUAL | PUAL | |
| Designated contracting statesAK | AK | |
| Public reference made under article 153(3) epc to a published international application that has entered the european phaseORIGINAL CODE: 0009012PUAI | PUAI |
Numbers
- Publication
- 0328091
- Publication, DOCDB
- 0328091
- Publication, EPODOC
- EP0328091
- Application
- 89102210
- Application, DOCDB
- 89102210
- Application, EPODOC
- EP19890102210
Titles6
- German
- Wirksubstanz zur Behandlung von Haut- und Schleimhautveränderungen.
- English
- Active substance for treating alterations of the skin and the mucous membranes.
- French
- Substance active pour le traitement des altérations de la peau et des membranes muqueuses.
- German
- Wirksubstanz zur Behandlung von Haut- und Schleimhautveränderungen
- English
- Active substance for treating alterations of the skin and the mucous membranes
- French
- Substance active pour le traitement des altérations de la peau et des membranes muqueuses
Classification
- CPC, 5
- A61Q11/00
- A61K8/362
- A61K8/365
- A61K8/44
- A61Q19/00
- IPC, 7
- A61K8 362
- A61K8 365
- A61K8 44
- A61K31 19
- A61K31 195
- A61Q11 00
- A61Q19 00
Designated states2
- Contracting states, 2
- Spain
- Greece