Pharmaceutical and/or cosmetic composition containing an organosiloxane and a phospholipid

• US 20030170194A1
• Filed: 11/19/2002
• Published: 09/11/2003
• Est. Priority Date: 05/19/2000
• Status: Abandoned Application

• Current Assignee: Mika Pharma Gesellschaft Fur Die Entwicklung Und Vermarktung Pharmazeutischer Produkte Mbh
• Original Assignee: Mika Pharma Gesellschaft Fur Die Entwicklung Und Vermarktung Pharmazeutischer Produkte Mbh
• Inventors: Piotrowiak, Ralf, Siegfried, Bernd G
• Application Number:
  US10/276,766
• Publication Number:
  US 20030170194A1
• Time in Patent Office: Days
• US Class Current: 424/70.12
• CPC Class Codes: A61K 8/046 Aerosols; Foams
• CPC Class Codes: A61K 8/553 Phospholipids, e.g. lecithin
• CPC Class Codes: A61K 8/585 Organosilicon compounds
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61K 9/1277 Processes for preparing; Proliposomes
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: A61Q 19/004 Aftersun preparations
• CPC Class Codes: A61Q 7/00 Preparations for affecting hair growth

Abstract

A pharmaceutical and/or cosmetic composition for use in humans, animals or plants is described, comprising at least one pharmaceutical and/or cosmetic active ingredient and at least one organosilicon compound based on oligomeric and/or polymeric diorganosiloxane, whereby the composition also contains at least one phospholipid.

Claims

1. A pharmaceutical and/or cosmetic composition for use on humans, animals or plants, comprising at least one pharmaceutical and/or cosmetic active ingredient, at least one phospholipid and at least one organosilicon compound on the bases of a diorganosiloxane, characterized in that the composition contains hexamethyldisiloxane as organosilicon compound.

2. The composition according to claim 1, characterized in that the composition comprises as the phospholipid such a phospholipid, being isolated from natural starting materials.

3. The composition according to claim 1 or 2, characterized in that the composition comprises as the phospholipid at least one phospholipid having a high phosphatidylcholine content, preferably such a phospholipid having more than 70% by weight phosphatidylcholine.

4. The composition according to claim 3, characterized in that the phospholipid contains at least 80% by weight and preferably more than 90% by weight phosphatidylcholine.

5. The composition according to one of the preceding claims, characterized in that the phospholipid is a hydrogenated phospholipid, preferably a hydrogenated phosphatidylcholine.

6. The composition according to one of the preceding claims, characterized in that the composition comprises the hexamethyldisiloxane in a concentration between 5% by weight and 96% by weight, based on the total weight of the composition, and at least one phospholipid in a concentration between 2% by weight and 30% by weight, based on the total weight of the composition.

7. The composition according to claim 6, characterized in that the composition contains between 20% by weight and 85% by weight of the hexamethyldisiloxane and between 5% by weight and 20% by weight of the at least one phospholipid.

8. The composition according to one of the preceding claims, characterized in that the composition comprises between 0% by weight and 5% by weight water, and the hexamethyldisiloxane and the phospholipid contained in the composition are mixed together so that the composition forms liposomes and/or micelles spontaneously on coming in contact with water.

9. The composition according to claim 8, characterized in that the liposomes and/or micelles formed spontaneously by adding water have an average particle size between 50 nm and 4000 nm, in particular between 250 nm and 1500 nm.

10. The composition according to one of the preceding claims, characterized in that the composition also comprises water, alcohol, antioxidants, non-phospholipid emulsifiers, pharmaceutical active ingredients, cosmetic active ingredients and/or other auxiliary substances, in addition to the at least one organosilicon compound and the at least one phospholipid.

11. The composition according to claim 10, characterized in that the concentration of the at least one pharmaceutical active ingredient and/or the at least one cosmetic active ingredient in the composition varies between 0.001% by weight and 30% by weight, in particular between 0.1% by weight and 15% by weight, based on the ready-to-use composition.

12. The composition according to one of the preceding claims, characterized in that the composition also contains at least one alcohol, where the concentration of the at least one alcohol amounts to a maximum of 14% by weight and preferably varies between 0.1% by weight and 8.5% by weight, each based on the ready-to-use composition.

13. The composition according to one of the preceding claims, characterized in that the composition for use on humans or animals comprises at least one cosmetic and/or pharmaceutical active ingredient which is selected from the group consisting of local anesthetics, antiallergics, dermatologics, active ingredients to combat influenza infections and colds, active ingredients for treatment of neuropathies, active ingredients for treatment of circulation disorders, chemotherapeutics, quinine, antimycotics, antibiotics, thalidomide, analgesics, non-steroidal anti-inflammatory drugs, leukotrienes, leukotriene inhibitors, antiandrogens, corticosteroids, opiate receptor antagonists, blood coagulation inhibitors, platelet aggregation inhibitors, histamine antagonists, regulatory and enzymatic peptides and proteins, nucleic acids and oligopeptides, antidiabetics, prostaglandins, prostaglandin synthesis inhibitors, antiviral or virustatic substances, antimicrobial substances, active ingredients against prions, immunosuppressants, hormones, active ingredients for treatment of wounds and especially chronic wounds, vitamins, plant extracts or extracts of plant extracts, psychopharmaceuticals, active ingredients to influence sleep, analeptics, general anesthetics, muscle relaxants, antiepileptics, antiparkinsonian drugs, antiemetics, substances that act on the ganglia, substances that act on the sympathetic nervous system, substances that act on the parasympathetic nervous system, calcium antagonists, cardiovascular agents, antiasthmatics, antitussives, expectorants, hepatics, diuretics, choleretics, disinfectants, trace elements, anti-infectives, cytostatics, antimetabolites, hormone antagonists and/or immunomodulators.

14. The composition according to one of the claims 1 to 12, characterized in that the composition for use on plants contains as the active ingredient a fungicide, an insecticide, a herbicide and/or a fertilizer absorbable through leaf parts and/or above-ground plant parts.

15. The composition according to one of the preceding claims, characterized in that the composition has a liquid to pasty viscosity for topical application, whereby the viscosity of the composition preferably varies between 0.4 cSt and 10,000 cSt, in particular between 0.6 cSt and 1500 cSt.

16. The composition according to claim 15, characterized in that the composition comprises the hexamethyldisiloxane and the at least one phospholipid in such a coordinated weight ratio that after applying the composition to human or animal skin in a concentration between 0.05 and 0.3 g per 100 cm² skin, no visible residues of the composition remain on the skin within a period of 1 second to 60 seconds, preferably within a period of 3 seconds to 20 seconds.

17. The composition according to one of the preceding claims, characterized in that the composition comprises at least one vitamin as the pharmaceutical and/or cosmetic active ingredient.

18. The composition according to claim 17, characterized in that the vitamin is vitamin C, vitamin E, vitamin A and/or pro-vitamin A.

19. The composition according to one of the preceding claims, characterized in that the composition is in such a form of administration which permits administration of the composition as a capsule, suppository, plaster, spray, mist, gel, powder and/or cream.

20. The composition according to one of the preceding claims, characterized in that it is prepared for topical application of pharmaceutical and/or cosmetic active ingredients, for buccal application of these active ingredients and/or for oral administration of these active ingredients.