Topically applicable Anti-inflammatory o/w emulsions comprising pro-penetrating glycols

a technology of pro-penetrating glycol and o/w emulsion, which is applied in the direction of biocide, dermatological disorders, drug compositions, etc., can solve the problem of thick cream of waxy appearan

Inactive Publication Date: 2010-06-10
GALDERMA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The composition achieves physical and chemical stability, maintaining active agent content and avoiding greasiness, with improved penetration and texture, suitable for topical application.

Problems solved by technology

However, the stabilization of a formulation comprising such a percentage of glycol makes it necessary to include in the emulsion emulsifiers and stabilizers of glyceryl stearate or PEG 100 stearate type or, alternatively, stabilizers or consistency factors of white wax or cetostearyl alcohol type, which lead to the formation of a thick cream of waxy appearance.

Method used

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  • Topically applicable Anti-inflammatory o/w emulsions comprising pro-penetrating glycols

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0077]

Waterqs 100ammonium acryloyldimethyltaurate / 1.00%VP copolymerclobetasol propionate0.05%propylene glycol37.50%dimethyl isosorbide10.00%liquid paraffin20.00%PEG-6 isostearate2.00%sodium hydroxideqs pH 6

[0078]Physical and Chemical Stability of the Composition of Example 1:

T0 = thick white milkT1 monthpH = 7.54Centrifuge: 10 000rpm: no commentsMicro: globule size RTMacroscopicThick white milk, inappearanceaccordance with T0pHpH 7.6MicroscopicGlobule size 2.5 μm,appearancehomogeneous carpetAssay of the active97.9%agent (HPLC)T0: 99% 4° C.MacroscopicThick white milk, inappearanceaccordance with T0MicroscopicGlobule size 2.5 μm,appearancehomogeneous carpetNo recrystallization of theclobetasol40° C.MacroscopicThick white milk, inappearanceaccordance with T0Assay of the active96.3%agent (HPLC)T0: 99%

example 2

[0079]

Waterqs 100ammonium acryloyldimethyltaurate / 1.00%VP copolymerclobetasol propionate0.05%propylene glycol42.50%ethanol5.00%liquid paraffin20.00%PEG-6 isostearate2.00%sodium hydroxideqs pH 6T0 = thick white milkT1 monthpH = 6.7Centrifuge: 10 000rpm: no commentsMicro: globule size RTMacroscopicThick white milk, inappearanceaccordance with T0pHpH 6.7MicroscopicGlobule size from 2.5 μmappearanceand 7.5 μm,heterogeneous carpetAssay of the active98.1%agent (HPLC)T0: 99.7% 4° C.MacroscopicThick white milk, inappearanceaccordance with T0MicroscopicGlobule size from 2.5 μmappearanceand 7.5 μm,heterogeneous carpetNo recrystallization of theclobetasol40° C.MacroscopicThick white milk, inappearanceaccordance with T0Assay of the active97.4%agent (HPLC)T0: 99.7%

example 3

[0080]

Waterqs 100acrylates / steareth-203.50%methacrylate copolymerclobetasol propionate0.05%propylene glycol45.00%diethylene glycol monoethyl ether1.50%propylene glycol laurate1.00%liquid paraffin20.00%polyglyceryl-3 diisostearate2.00%sodium hydroxideqs pH 6T0 = thick white milkT1 monthpH = 6.33Centrifuge: 10 000rpm: slight phase separationMicro: globule size RTMacroscopicThick white milk, inappearanceaccordance with T0pHpH 6.36MicroscopicGlobule size appearancehomogeneous carpetAssay of the active98.3%agent (HPLC)T0: 99.6% 4° C.MacroscopicThick white milk, inappearanceaccordance with T0MicroscopicGlobule size appearancehomogeneous carpetNo recrystallization of theclobetasol40° C.MacroscopicThick white milk, inappearanceaccordance with T0Assay of the active97.6%agent (HPLC)T0: 99.6%

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Abstract

Stable, topically applicable, non-greasy and non-tacky oil-in-water (O / W) anti-inflammatory emulsions, useful, e.g., for the treatment of psoriasis, contain:a. a therapeutically effective amount of at least one steroidal anti-inflammatory agent, notably clobetasol propionate;b. a pro-penetrating system which includes at least one pro-penetrating glycol and at least one other pro-penetrating agent; andc. at least one polymeric emulsifier not sensitive to electrolytes, for example not an acrylate / C10-C30 alkyl acrylate copolymer, formulated into a topically applicable, pharmaceutically acceptable vehicle therefor.

Description

CROSS-REFERENCE TO EARLIER APPLICATIONS[0001]This application is a continuation of earlier copending U.S. patent application Ser. No. 11 / 709,840, filed Feb. 23, 2007, which claims priority under 35 U.S.C. §119 of FR 06 / 02283, filed Mar. 15, 2006, both hereby expressly incorporated by reference and assigned to the assignee hereof.CROSS-REFERENCE TO COMPANION APPLICATION[0002]Copending application Ser. No. 11 / 709,839 filed Feb. 23, 2007 [Attorney Docket No. 1034227-000106], filed concurrently with parent application Ser. No. 11 / 709,840 and also assigned to the assignee hereof.BACKGROUND OF THE INVENTION[0003]1. Technical Field of the Invention[0004]The present invention relates to novel compositions in the form of emulsions of oil-in-water (O / W) type for topical application, comprising a novel combination of pro-penetrating agents including at least one glycol, a suitable emulsifying system and a bioactive agent of the family of steroidal anti-inflammatory agents.[0005]2. Description ...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/57A61P17/06
CPCA61K9/0014A61K31/573A61K47/10A61K47/34A61K47/22A61K47/26A61K47/32A61K47/12A61P17/06
InventorSEGURA-ORSONI, SANDRINEROUMEC, SOPHIE
OwnerGALDERMA SA