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Pharmaceutical composition

A composition and drug technology, applied in the directions of drug combination, drug delivery, antipyretics, etc., can solve the problems of limiting, limiting the bioavailability of compounds, lack of water solubility, etc.

Active Publication Date: 2019-05-21
AVEXXIN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The polyunsaturated long-chain ketones described in these references are amphipathic but predominantly hydrophobic and thus insoluble in water
Lack of aqueous solubility limits the bioavailability of compounds and limits the ability of technicians to administer useful doses of these compounds to patients
In particular, lack of water solubility limits the ability of those skilled in the art to administer the compound topically to patients
[0004] Another problem with the polyunsaturated ketone compounds of the present invention is that they are prone to degradation

Method used

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  • Pharmaceutical composition
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Embodiment Construction

[0032] The present invention relates to pharmaceutical compositions comprising at least one compound of formula (I) and at least one silicone vehicle (preferably two, three, four or more such silicone vehicles). In preferred embodiments, the silicone vehicle includes decamethylcyclopentasiloxane (Cyclomethicone 5, D5), liquid dimethyl silicone, and elastomeric silicone. We have surprisingly found that the use of silicone vehicles leads to an increased penetration of the active ingredients of formula (I) into the skin compared to formulations based on paraffinic vehicles. Our results demonstrate that silicone-based formulations allow better penetration of the active ingredient into pig skin, resulting in tissue concentrations of the active ingredient that may be 2 to 4 times higher than those of paraffin-based formulations.

[0033] It is especially preferred if the composition according to the invention is in the form of an oil-in-oil emulsion. Without wishing to be bound by ...

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Abstract

A pharmaceutical composition comprising polyunsaturated long-chain ketones and a silicone vehicle or a blend of silicone vehicles. The composition has utility in the treatment and prevention of inflammatory conditions including skin disorders.

Description

technical field [0001] The present invention relates to pharmaceutical compositions comprising certain polyunsaturated long chain ketones and a silicone vehicle, particularly a blend of various silicone vehicles. The invention also relates to the use of said pharmaceutical formulation for the treatment or prevention of inflammatory conditions such as certain skin conditions such as dermatitis and psoriasis. Background technique [0002] Numerous prior art references describe the use of certain polyunsaturated long-chain ketones for the treatment of conditions including psoriasis, dermatitis, skin cancer, glomerulonephritis and rheumatoid arthritis (see EP-A-1469859, WO2010 / 139482, WO2012 / 028688, WO2014 / 082960 and WO2015 / 181135). [0003] The polyunsaturated long-chain ketones described in these references are amphiphilic, but predominantly hydrophobic, and thus insoluble in water. Lack of aqueous solubility limits the bioavailability of the compounds and limits the abilit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/121A61K31/765A61P29/00A61P17/06
CPCA61K31/121A61K31/765A61P17/00A61P17/06A61P29/00A61K9/0014A61K9/06A61K47/24A61K9/107A61K9/12A61K47/02A61K47/06A61K47/44
Inventor 夏洛特·赫斯曼比吉塔·斯文森安德斯·林奎斯特
Owner AVEXXIN