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Topical compositions comprising ascomycins

A kind of technology of ascomycin and composition, applied in the field of topical composition, can solve problems such as difficulty

Inactive Publication Date: 2005-08-10
迈德制药卢森堡有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Particular difficulties arise with topical compositions containing ascomycin for the treatment of lichenified skin conditions such as psoriasis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0117] Prepare an ointment (in g) with the following composition

[0118] Compound A 1

[0119] Urea 10

[0120] Petrolatum 39

[0121] Microcrystalline Wax 10

[0122] liquid paraffin 35

[0123] Isopropyl myristate 5

[0124] total 100

[0125] The composition was prepared as follows: Compound A and urea were suspended in liquid paraffin and isopropyl myristate and heated to about 70°C. The white petrolatum and microcrystalline wax were heated to about 85°C, cooled to about 70°C, and slowly added to the above ascomycin mixture. The composition was then cooled to room temperature. Form into an ointment.

[0126] A total of 20 patients were treated for 3 weeks. The therapeutic effect of the composition on erythema, induration and scaling was evaluated from three clinical signs. In addition, the time to partial disappearance of symptoms was used to evaluate effectiveness. Local tolerability and routine safety parameters of the studied dosing regimens, including hema...

Embodiment 1

[0127] The formulation of Example 1 is effective. Local tolerability of the tested study dosing regimens was good, and no systemic adverse effects were observed.

Embodiment 12

[0129] An ointment having the same composition as the composition of Example 1.1 was prepared. The composition is obtained by heating liquid paraffin, microcrystalline wax, white petrolatum and isopropyl myristate to about 85°C, cooling to about 70°C, and suspending compound A and urea in the obtained mixture. The composition was then cooled to room temperature. Form into an ointment.

[0130] Example 2 3 4 5 6 7

[0131] Compound A 1 0.1 1 2 2 1.5

[0132] Substance that retains moisture in the outer layer of the skin

[0133] Urea 5 0.1 10 7.5 10 2

[0134] Substances that prevent moisture from evaporating from the skin

[0135] Petrolatum 44 99.8 84 85.5 86 73

[0136] Microcrystalline wax 10 - - - - -

[0137] Liquid paraffin 35 - - - - 20

[0138] liquid substance

[0139] Isopropyl myristate 5 - - - - -

[0140] Diisopropyl adipate - - 5 - - -

[0141] Oleyl Erucate - - - - - 3.5

[0142] Oleyl alcohol - - - 5 - -

[0143] Propylene glycol - - - - 2 -

[01...

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PUM

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Abstract

The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin.

Description

technical field [0001] The present invention relates to topical compositions containing ascomycin for the treatment of skin disorders, such as subacute and chronic inflammatory and hyperproliferative skin disorders, such as atopic dermatitis, vitiligo, psoriasis, moss Ringworm-like skin diseases such as lichen planus, lichenified form of atopic dermatitis. Background technique [0002] Ascomycin has several useful pharmacological effects, such as immunosuppression, and it can be administered topically. However, ascomycins pose problems for topical application, especially because of their physicochemical properties, such as high molecular weight and lipophilicity. [0003] Skin diseases, especially lichenification skin diseases such as psoriasis, also have difficulties in treatment. In said disease, the skin is hyperproliferated and the skin barrier function and lipid composition of the skin may be altered. Topical compositions containing ascomycin fo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K9/00A61K31/4353A61K31/436A61K31/445A61K47/00A61K47/02A61K47/06A61K47/10A61K47/12A61K47/14A61K47/16A61K47/32A61K47/44A61P17/00A61P17/06A61P29/00A61P31/00A61P37/00A61P37/06
CPCA61K47/02A61K47/06A61K47/16A61K31/4353A61K31/436A61K47/44A61K47/12A61K9/0014A61K47/10A61K47/14A61P17/00A61P17/06A61P29/00A61P31/00A61P35/00A61P37/00A61P37/06
Inventor K·克里威特D·莱德格伯J·里德尔
Owner 迈德制药卢森堡有限公司
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