Tri-azole antifungal compositions
OwnerFrank LÖSCHER, Markus BEIER +1inventors
InventorsFrank LÖSCHER, Markus BEIER, Diana STREHL
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Abstract
The present invention relates to a liquid composition comprising an azole antifungal agent and a vehicle comprising a semifluorinated alkane.
Claims17
A water-free liquid composition comprising efinaconazole dissolved in a vehicle comprising a semifluorinated alkane.
The composition according to any of the preceding claims, wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F4H10, F6H6, F6H8, F6H10.
The composition according to any of the preceding claims, wherein the composition does not comprise a further active ingredient, optionally the composition does not comprise a further antifungal agent, preferably the composition does not comprise tavaborole.
The composition according to any preceding claim, wherein the composition comprises a cosolvent is selected from ethanol, 2-propanol, DMF (N,N-dimethylformamide), DMSO (dimethyl sulfoxide), DMAC (N,N-dimethylacetamide), NMP (1-Methyl-2-pyrrolidon).
The composition according to any preceding claim, wherein efinaconazole is present at a concentration of up to 2% (w/v).
The composition according to any preceding claim, wherein the composition comprises efinaconazole and less than about 0.1% (w/v) of efinaconazole-N-oxid.
The composition according to any preceding claim, being free of one or more further components selected from
- i. ethanol
- ii. penetration enhancer selected from transcutol and isopropyl myristate
- iii. chelating agent selected from EDTA, DTPA
- iv. wetting agent or surface tension lowering agent selected from cyclomethicone)
- v. pH adjusting agent
- vi. moisturizer selected from C12-15alkyl lactate)
- vii. emollient selected from diisopropyl adipate)
- viii. water
- ix. preservative
- x. surfactant
- xi. propylene glycol, ethyl acetate or amyl acetate.
The composition according to any preceding claim, comprising or consisting of efinaconazole dissolved in vehicle comprising or consisting of 1-perfluorohexyloctane, and optionally 2-propanol.
The composition according to any preceding claim, comprising or consisting of about 0.5 to 2% (w/v) efinaconazole dissolved in 98 to 99.5% (v/v) of a vehicle comprising or consisting of 1-perfluroohexyloctane and 2-propanol.
The composition according to any preceding claim, consisting of up 2.0% (w/v) efinaconazole, up to 90% (w/v) of 1-perfluorohexyloctane and less than or equal to 10% (w/v) of 2-propanol, preferably consisting of up 2.0% (w/v) efinaconazole, up to 90% (v/v) of 1-perfluorohexyloctane and less than or equal to 10% (v/v) of 2-propanol.
The composition according to any preceding claim, consisting of 1% (w/v) or of 2.0% (w/v) efinaconazole, up to 90% (v/v) of 1-perfluorohexyloctane and less than or equal to 10% (v/v) of 2-propanol.
The composition according to any preceding claim, for use as medicine.
Dependencies are inferred from the claim text.