Polyaphron topical composition with vitamin d and corticosteroid

A technology of corticosteroids and compositions, applied in the field of topical compositions, which can solve the problems of poor diffusion, unacceptable to patients, unfavorable, etc., and achieve the effect of happy application, enhanced skin permeability, and reduced possibility

Inactive Publication Date: 2010-03-17
DRUG DELIVERYSOLUTIONS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is undesirable and may lead to poor patient acceptance
[0015] Another disadvantage of the composition of US-B-6,753,013 is that in order for the composition to provide beneficial results in topical treatments, high levels of vitamin D or vitamin D analogs are required in order to have sufficient vitamin D or vitamin D analogs penetrating into the skin
This is because the composition exhibits poor diffusion through the skin
This is disadvantageous since vitamin D and vitamin D analogs are known skin irritants

Method used

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  • Polyaphron topical composition with vitamin d and corticosteroid
  • Polyaphron topical composition with vitamin d and corticosteroid
  • Polyaphron topical composition with vitamin d and corticosteroid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Three gel polyaphron dispersions with the compositions described below were prepared by the following methods.

[0122] Gel polymicrobubble dispersion 1

oil phase

％

Calcipotriol solution in caprylic / capric triglyceride (Mygliol 812-Condea) *

(0.0695%)

89.10

Laureth-4 (Volpo L4-Croda)

0.90

water box

Poloxamer 188 (Pluronic F68-BASF)

1.00

softened water

9.00

[0123] Gel polymicrobubble dispersion 2

oil phase

％

Betamethasone dipropionate in caprylic / capric triglyceride (Mygliol 812-Condea)

the solution ** (0.3465%)

89.10

Laureth-4 (Volpo L4-Croda)

0.90

water box

Poloxamer 188 (Pluronic F68-BASF)

1.00

softened water

9.00

[0124] Gel polymicrobubble dispersion 3

oil phase

weight%

Squalane (from Olive - A&E Connock)

9.00 ...

Embodiment 2

Propylene Glycol

10.05

water gel

9.88

[0161] * The final calcipotriol level was 55.4 μg / g.

[0162] ** The final BDP level was 645 μg / g, equivalent to 502 μg / g.

[0163] Manufacturing method

[0164] The method used was as described above in Example 1, except that propylene glycol and the neutralized aqueous gel were added to the final mixture of the three gelling polyaphron dispersions 1, 2 and 3, which were then Proceed to Mix: Mix briefly until the product is a homogeneous mixture of microcellular dispersions.

[0165] Neutralized gels were obtained by adding triethanolamine (a base) to a dispersion of polyacrylic acid to form a clear gel with a pH of 7.5 ± 0.2. Methods for neutralizing polyacrylic acid gels are well known to those skilled in the art.

[0166] Stability measurement

[0167] Stability was tested as in Example 1b.

[0168] The inventors observed that the levels of calcipotriol and betamethasone dipropionate were 104% ± ...

Embodiment 3

[0172] Three gel polyaphron dispersions and aqueous gels of the compositions described below were prepared by the following methods.

[0173] Gel polymicrobubble dispersion 1

oil phase

％

Isopropyl myristate (Lexol IPM NF-Inolex) in a weight ratio of 3:2: caprylic / capric

Calcipotriol solution in a blend of triglycerides (Mygliol 812-Condea) * (0.0573%)

89.10

Laureth-4 (Volpo L4-Croda)

0.90

water box

Poloxamer 188 (Pluronic F68-BASF)

1.00

softened water

9.00

[0174] Gel polymicrobubble dispersion 2

oil phase

％

Betamethasone dipropionate dissolved in caprylic / capric triglyceride (Mygliol 812-Condea)

liquid ** (0.3838%)

89.10

Laureth-4 (Volpo L4-Croda)

0.90

water box

Poloxamer 188 (Pluronic F68-BASF)

1.00

softened water

9.00

[0175] Gel polymicrobub...

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PUM

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Abstract

A composition suitable for topical application comprising a continuous phase and at least one discontinuous phase, said composition comprising at least one polyaphron dispersion, at least one vitaminD or vitamin D analogue and at least one corticosteroid.

Description

technical field [0001] The present invention relates to compositions for topical application comprising at least one vitamin D or vitamin D analogue and at least one corticosteroid. Background technique [0002] It is known that compositions comprising vitamin D or vitamin D analogs are useful in the treatment of a variety of skin conditions. [0003] For example, EP-B-474,517 discloses the use of compositions containing one or more 1α-hydroxylated-19-nor-vitamin D compounds having a triple bond in the side chain for the treatment of psoriasis. [0004] US 4,871,723 discloses a method of treating psoriasis by topical application of a composition comprising vitamin D and a wax carrier. Specifically, US 4,871,723 discloses a composition comprising a) a pharmaceutically effective amount of active vitamin D 3 , b) a solvent selected from fatty acid esters, higher alcohols having more than 10 carbons, and propylene carbonate, and c) an oily carrier selected from white petrolatu...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/59A61K45/06A61P17/06
CPCA61K31/59A61K31/573A61K47/44A61K47/06A61K47/10A61K9/0014A61K45/06A61K9/06A61K9/10A61K9/1075A61K31/00A61K31/56A61K47/14A61K47/24A61K47/34A61P17/00A61P17/06A61K2300/00
Inventor 德里克·阿尔佛雷德·惠勒大卫·弗拉泽·斯蒂尔米歇尔·乔治乌斯蒂恩·欣德特-派得森
Owner DRUG DELIVERYSOLUTIONS LTD
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