Topical pharmaceutical compositions comprising bexarotene and corticosteroids

A kind of technology of corticosteroid, topical medicine, is applied in the field of preparing described composition

Inactive Publication Date: 2014-09-17
ALMIRALL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, until now there is no approved combination of tazarotene or any other retinoid with a corticosteroid for the topical treatment of psoriasis

Method used

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  • Topical pharmaceutical compositions comprising bexarotene and corticosteroids
  • Topical pharmaceutical compositions comprising bexarotene and corticosteroids
  • Topical pharmaceutical compositions comprising bexarotene and corticosteroids

Examples

Experimental program
Comparison scheme
Effect test

specific example

[0129] Specific examples include cyclic methylsiloxanes, which have the formula [(CH 3 ) 2 SiO] x , where x is 3-6, or a short-chain linear methylsiloxane having the formula ((CH 3 ) 2 SiO[(CH 3 ) 2 SiO] y Si(CH 3 ) 3 , where y is 0-5.

[0130] Some suitable cyclomethicones are hexamethylcyclotrisiloxane (D3), a boiling point of 134°C and of the formula [(Me 2 )SiO] 3 The solid; octamethylcyclotetrasiloxane (D4), the boiling point is 176 ° C, the viscosity is 2.3mm 2 / s and is the formula [(Me 2 )SiO] 4 ; Decamethylcyclopentasiloxane (D5) (cyclomethicone), with a boiling point of 210°C and a viscosity of 3.87mm 2 / s and is the formula [(Me 2 )SiO] 5 ; and dodecamethylcyclohexasiloxane (D6), with a boiling point of 245°C and a viscosity of 6.62mm 2 / s and is the formula [(Me 2 )SiO] 6 .

[0131] Some suitable short linear methylsiloxanes are hexamethyldisiloxane (MM) with a boiling point of 100°C and a viscosity of 0-65mm 2 / s and is the formula Me 3 SiOMe ...

Embodiment 1-6

[0149] Preparation of compositions of the present invention as shown in Table 1 (% by weight, based on the total weight of the composition)

[0150] Table 1

[0151]

[0152] The composition is prepared in the following manner:

[0153] 1) Add octyldodecanol into a stainless steel container and heat to 80°C with stirring. Bexarotene was added and dissolved while stirring to obtain a clear solution.

[0154] 2) White soft paraffin and propylene glycol monopalmitostearate are added in a stainless steel container. The ingredients were heated to 60°C and melted with stirring. The molten mixture of lipophilic compounds is homogeneous and clear.

[0155] 3) Transfer and suspend (thoroughly disperse) betamethasone dipropionate into the molten mixture of lipophilic compounds while homogenizing.

[0156] 4) Transfer the bexarotene solution to the batch while stirring.

[0157] 5) Dissolve anhydrous citric acid and sodium citrate in purified water and transfer this solution to ...

Embodiment 7-9

[0161] Preparation of compositions of the present invention as shown in Table 2 (% by weight, based on the total weight of the composition)

[0162] Table 2

[0163]

[0164]

[0165] The composition is prepared in the following manner:

[0166] 1) Add liquid paraffin, white soft paraffin and propylene glycol monopalmitostearate into a stainless steel container. The ingredients were heated to 60°C and melted with stirring. The molten mixture of lipophilic compounds is homogeneous and clear.

[0167] 2) Transfer bexarotene and betamethasone dipropionate into the molten mixture of lipophilic compounds and suspend (thoroughly disperse) while homogenizing.

[0168] 3) Dissolve anhydrous citric acid and sodium citrate in purified water and transfer this solution to the batch while homogenizing.

[0169] 4) Cool the batch to 30°C while stirring.

[0170] 5) The batch was then filled directly into glass bottles.

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Abstract

Topical pharmaceutical compositions are described comprising: a) bexarotene, b) a corticosteroid, and c) a carrier or vehicle. Said compositions are useful for the treatment of skin disorders.

Description

technical field [0001] The present invention relates to topical pharmaceutical compositions comprising bexarotene and corticosteroids. The combination of these two active ingredients produced a pronounced antipsoriatic effect and improved tolerability. The provided compositions are stable and can be easily applied to large skin surfaces. The invention also relates to methods of preparing said compositions and methods of treatment by administering said compositions. Background technique [0002] Psoriasis is a disease characterized by epidermal proliferation manifested by premature keratinization, elongation, dilation, and increased permeability of superficial capillaries in the dermis. There is an associated immune activation that is manifested by inflammation. Clinically active lesions are reddened, raised areas with epidermal scales that peel off easily to develop a silvery appearance. Typically, these psoriatic plaques are diffuse and well-defined, and they are surrou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/573A61K9/06A61K47/02A61K9/00A61P17/06
CPCA61K47/14A61K47/44A61K47/38A61K31/192A61K47/02A61K47/26A61K31/573A61K47/10A61K9/0014A61K9/06A61K47/36A61K47/06A61P17/00A61P17/06A61P43/00A61K2300/00
Inventor F·埃夫斯S·菲尔豪尔H·马尔威茨H·特洛莫C·威乐斯
Owner ALMIRALL
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