CA2535401A1 - Emulsive composition containing dapsone - Google Patents
Emulsive composition containing dapsone Download PDFInfo
- Publication number
- CA2535401A1 CA2535401A1 CA002535401A CA2535401A CA2535401A1 CA 2535401 A1 CA2535401 A1 CA 2535401A1 CA 002535401 A CA002535401 A CA 002535401A CA 2535401 A CA2535401 A CA 2535401A CA 2535401 A1 CA2535401 A1 CA 2535401A1
- Authority
- CA
- Canada
- Prior art keywords
- percent
- composition according
- emulsive composition
- dapsone
- emulsive
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Classifications
-
- 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
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/08—Antibacterial agents for leprosy
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- 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
- A61Q17/005—Antimicrobial preparations
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Birds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention relates to a topical, emulsive composition containing Dapsone or its derivative. The inventive composition incorporates emollients and Dapsone or its derivative in a stable emulsion. The stability is achieved through the use of a combination of certain surfactant mixtures and an enhancer providing solubility of the Dapsone.
Claims (33)
1. An emulsive composition comprising the components a) Dapsone or its derivative, b) a solvation medium, c) an emulsifier system and d) an oil phase component.
2. An emulsive composition according to claim 1 further comprising water as component e).
3. An emulsive composition according to claim 2 wherein the water and the solvation medium at least partially dissolve the Dapsone or its derivative.
4. An emulsive composition according to claim 1 wherein the weight percentages of components relative to the total weight of the emulsive composition comprise:
a) Dapsone or its derivative from about 0.005 percent to about 30 percent;
b) solvation medium from about 0.5 percent to about 99 percent;
c) emulsifier system from about 0.1 percent to about 30 percent;
d) oil phase component from about 0.1 weight percent to about 75 percent.
a) Dapsone or its derivative from about 0.005 percent to about 30 percent;
b) solvation medium from about 0.5 percent to about 99 percent;
c) emulsifier system from about 0.1 percent to about 30 percent;
d) oil phase component from about 0.1 weight percent to about 75 percent.
5. An emulsive composition according to claim 2 wherein the water weight percentage ranges up to about 99 percent.
6. An emulsive composition according to claim 4 further including water in a weight percentage range of up to about 99 percent.
7. An emulsive composition according to claim 1 wherein the weight percentages of components relative to the total weight of the emulsive composition comprise:
a) Dapsone or its derivative from about 0.1 percent to about 25 percent;
b) solvation medium from about 0.5 percent to about 50 percent;
c) emulsifier system from about 0.5 percent to about 25 percent;
d) oil phase component from about 0.1 weight percent to about 50 percent.
a) Dapsone or its derivative from about 0.1 percent to about 25 percent;
b) solvation medium from about 0.5 percent to about 50 percent;
c) emulsifier system from about 0.5 percent to about 25 percent;
d) oil phase component from about 0.1 weight percent to about 50 percent.
8. An emulsive composition according to claim 1 further comprising optional water, and wherein the weight percentages of components relative to the total weight of the emulsive composition are selected from among the following ranges such that the total amounts equal 140 percent, and each succeeding range for each component is preferred relative to the preceding range:
a) Dapsone range selections are from about 0.005 percent to about 30 percent: about 0.1 percent to about 25 percent; about 0.1 percent to about 15 percent; about 0.1 percent to about 10 percent; about 0.2 percent to about 8 percent; about 0.5 to about 5 percent by weight of the emulsive composition;
b) the solvation medium range selections are from about 0.5 percent to about 99 percent; about 0.5 percent to about 50 percent; about 5 percent to about 40 percent; about 5 percent to about 35 percent; about 5 percent to about 30 percent;
c) the emulsifier system range selections are from about 0.1 percent to about 30 percent; about 0.5 percent to about 25 percent; about 1 percent to about 25 percent; about 5 percent to about 25 percent; about 5 percent to about 20 percent;
d) the oil phase component range selections are from about 0.1 weight percent to about 75 percent; about 0.1 to about 50 percent; about 1 to about 45 percent; about 2 to about 40 percent; and e) optional water range selections are from 0 percent to about 99 percent; from 0 to about 50 percent; from 0 to about 40 percent; from 0 to about 35 percent.
a) Dapsone range selections are from about 0.005 percent to about 30 percent: about 0.1 percent to about 25 percent; about 0.1 percent to about 15 percent; about 0.1 percent to about 10 percent; about 0.2 percent to about 8 percent; about 0.5 to about 5 percent by weight of the emulsive composition;
b) the solvation medium range selections are from about 0.5 percent to about 99 percent; about 0.5 percent to about 50 percent; about 5 percent to about 40 percent; about 5 percent to about 35 percent; about 5 percent to about 30 percent;
c) the emulsifier system range selections are from about 0.1 percent to about 30 percent; about 0.5 percent to about 25 percent; about 1 percent to about 25 percent; about 5 percent to about 25 percent; about 5 percent to about 20 percent;
d) the oil phase component range selections are from about 0.1 weight percent to about 75 percent; about 0.1 to about 50 percent; about 1 to about 45 percent; about 2 to about 40 percent; and e) optional water range selections are from 0 percent to about 99 percent; from 0 to about 50 percent; from 0 to about 40 percent; from 0 to about 35 percent.
9. An emulsive composition according to claim 1 wherein the emulsifier system comprises a combination of a fatty alcohol and a surfactant.
10. An emulsive composition according to claim 9 wherein the surfactant comprises a nonionic or anionic surfactant or a combination thereof.
11. An emulsive composition according to claim 9 wherein the fatty alcohol comprises a C8 to C30 alcohol optionally substituted by additional hydroxyl groups, alkoxy groups of C1 to C6 carbons, or alkoxycarbonyl groups of 2 to 6 carbons, or alkyl amido groups of 2 to 6 carbons or any combination thereof.
12. An emulsive composition according to claim 1 wherein the solvation medium comprises an organic solvent in which Dapsone or its derivative is soluble.
13. An emulsive composition according to claim 12 wherein the organic solvent comprises a glycol, a polyol, a glycol or polyol ether or any combination thereof.
14. An emulsive composition according to claim 1 wherein the Dapsone is fully or partially dissolved in the solvation medium.
15. An emulsive composition according to claim 1 wherein the Dapsone is fully or partially dissolved in the solvation medium and the oil phase component.
16. An emulsive composition according to claim 1 wherein the emulsifier system comprises a carbomer copolymer.
17. An emulsive composition comprising a) Dapsone, b) a glycol ether, c) an emulsifier system, d) an oil phase component, and e) optional water.
18. An emulsive composition of claim 17 wherein the glycol ether is ethoxydiglycol.
19. An emulsive composition of claim 18 including a carbomer copolymer.
20. An emulsive composition of claim 18 wherein the emulsifier system comprises a fatty alcohol and a surfactant.
21. An emulsive composition of claim 17 wherein the Dapsone is at a concentration from about 2% to about 5% by weight of the composition.
22. An emulsive composition of claim 17 wherein the ratio of the concentration of the Dapsone to the concentration of the glycol ether is such that the Dapsone is soluble in the glycol ether.
23. An emulsive composition according to any of the preceding claims wherein acidic and/or basic components are neutralized or buffered to a pH of from about 4 to 8, preferably 5 to 8, especially preferably 5 to 7.
24. An emulsive composition comprising: Dapsone, wax or petrolatum, C10 to C20 alcohol, C10 to C20 alkyl C10 to C20 alkanoate , C2 to C6 alkyl (C10 to C20) alkanoate, phosphate surfactant, ethoxydiglycol, polyacrylic acid or copolymer thereof, preservative, optional neutralizing agent and optional water.
25. An emulsive composition according to claim 24 having component ranges according to claim 8.
26. An emulsive composition according to claim 24 wherein the ranges are Dapsone - 2 to 5%, wax or petrolatum - 5 to 10%, C10 to C20 alcohol - 0 to 5%, C10 to C20 alkyl (C10 to C20) alkanoate - 0 to 5% , C2 to C6 alkyl (C10 to C20 alkanoate - 5 to 8%, phosphate surfactant - 0 to 5%, ethoxydiglycol - 10 to 30%, polyacrylic acid or copolymer thereof- 0.1 to 0.2%, preservative 0.04 to 0.2%, neutralizing agent and optional water to 100%, the percentages being by weight relative to the total weight of the composition.
27. An emulsive composition according to claim 24 comprising Dapsone, wax or petrolatum, cetostearyl alcohol, cetyl palmitate, isopropyl myristate, trilaureth-4 phosphate, ethoxydiglycol, carbomer copolymer, carbomer 940, preservative, optional neutralizing agent and optional water.
28. An emulsive composition according to claim 26 comprising 5% Dapsone.
29. An emulsive composition according to claim 26 comprising a plurality of preservatives, each of which is present to the extent of 0.04 to 0.2%.
30. An emulsive composition according to claim 29 comprising the preservatives methylparaben and propylparaben.
31. An emulsive composition according to claim 30 comprising 0.2%
methylparaben and 0.04% propyl paraben.
methylparaben and 0.04% propyl paraben.
32. An emulsive composition according to claim 26 having the following ingredients: Dapsone 5.0%, white petrolatum 8.0%, cetostearyl alcohol 5.0%, isopropyl myristate 5.0%, ethoxydiglycol 23.0%, trilaureth-4 phosphate 1.0%, carbomer copolymer 0.15%, carbomer 940 0.15%, methylparaben 0.2%, propyl paraben 0.04%, sufficient sodium hydroxide to adjust the pH of the composition to about 7, and purified water to 100%.
33
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US49491203P | 2003-08-13 | 2003-08-13 | |
US60/494,912 | 2003-08-13 | ||
PCT/US2004/026447 WO2005016296A1 (en) | 2003-08-13 | 2004-08-13 | Emulsive composition containing dapsone |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2535401A1 true CA2535401A1 (en) | 2005-02-24 |
CA2535401C CA2535401C (en) | 2011-07-26 |
Family
ID=34193253
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2535401A Active CA2535401C (en) | 2003-08-13 | 2004-08-13 | Emulsive composition containing dapsone |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1675563A4 (en) |
JP (1) | JP2007533606A (en) |
AU (1) | AU2004264964A1 (en) |
CA (1) | CA2535401C (en) |
MX (1) | MXPA06001713A (en) |
WO (1) | WO2005016296A1 (en) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009108147A1 (en) * | 2008-02-27 | 2009-09-03 | Qlt Usa, Inc. | Dapsone to treat rosascea |
EP2922528B1 (en) * | 2012-11-20 | 2017-05-31 | Allergan, Inc. | Topical dapsone and dapsone/adapalene compositions and methods for use thereof |
WO2019236374A2 (en) * | 2018-06-04 | 2019-12-12 | Arcutis, Inc. | Method and formulation for improving roflumilast skin penetration lag time |
US20200155524A1 (en) | 2018-11-16 | 2020-05-21 | Arcutis, Inc. | Method for reducing side effects from administration of phosphodiesterase-4 inhibitors |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5721242A (en) * | 1993-06-17 | 1998-02-24 | Hoffmann-La Roche Inc. | Antibiotic combination |
US5863560A (en) * | 1996-09-11 | 1999-01-26 | Virotex Corporation | Compositions and methods for topical application of therapeutic agents |
US20030157036A1 (en) * | 2002-02-20 | 2003-08-21 | Osborne David W. | Topical dapsone for the treatment of acne |
FR2753626B1 (en) * | 1996-09-20 | 1998-11-06 | Centre International De Rech Dermatologiques Galderma Cird Galderma | NOVEL TOPICAL COMPOSITIONS IN THE FORM OF A FLUID O / W EMULSION WITH A HIGH PRO-PENETRATING GLYCOL CONTENT |
US6372234B1 (en) * | 1997-05-27 | 2002-04-16 | Sembiosys Genetics Inc. | Products for topical applications comprising oil bodies |
US6056955A (en) * | 1999-09-14 | 2000-05-02 | Fischetti; Vincent | Topical treatment of streptococcal infections |
-
2004
- 2004-08-13 JP JP2006523427A patent/JP2007533606A/en active Pending
- 2004-08-13 CA CA2535401A patent/CA2535401C/en active Active
- 2004-08-13 EP EP04781175A patent/EP1675563A4/en not_active Withdrawn
- 2004-08-13 MX MXPA06001713A patent/MXPA06001713A/en not_active Application Discontinuation
- 2004-08-13 AU AU2004264964A patent/AU2004264964A1/en not_active Abandoned
- 2004-08-13 WO PCT/US2004/026447 patent/WO2005016296A1/en active Search and Examination
Also Published As
Publication number | Publication date |
---|---|
EP1675563A1 (en) | 2006-07-05 |
WO2005016296A1 (en) | 2005-02-24 |
EP1675563A4 (en) | 2009-07-15 |
CA2535401C (en) | 2011-07-26 |
AU2004264964A1 (en) | 2005-02-24 |
MXPA06001713A (en) | 2007-01-26 |
JP2007533606A (en) | 2007-11-22 |
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Legal Events
Date | Code | Title | Description |
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EEER | Examination request |