Gel formulations for the topical use of 1-amino-alkylcyclohexane derivatives

A technology of local application and gelling agent, which is applied in the direction of non-active ingredient medical preparations, anti-inflammatory agents, drug combinations, etc., and can solve problems such as reducing the volume of the emulsifier and skin irritation

Inactive Publication Date: 2013-01-02
MERZ PHARMA GMBH & CO KGAA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Carbomer gel can also reduce the volume of the emulsifier and since most polyacrylates are synthetic it can cause skin irritation which makes its use challenging for formulations for the treatment of skin diseases

Method used

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  • Gel formulations for the topical use of 1-amino-alkylcyclohexane derivatives
  • Gel formulations for the topical use of 1-amino-alkylcyclohexane derivatives
  • Gel formulations for the topical use of 1-amino-alkylcyclohexane derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0211] Evaluation of Compatibility and Storage Properties of Multiple Prototype Formulations

[0212] Various prototype formulations were produced by dissolving different amounts of neramexane mesylate in water and by adding different amounts of various gelling agents. For each mixture was homogenized and the pH was adjusted to a pH of about 5.5 with citric acid, HCl or NaOH. The properties and characteristics of each prototype formulation were evaluated to assess the compatibility of the components.

Embodiment 12

[0218] Example 1.2: Xantural 75:

[0219] Xantural 75 (INCI: Xanthan gum), known for its powerful ability to increase the viscosity of liquids, was also tested as a gelling agent in different ratios to neramexane mesylate (see Table 2).

[0220] Table 2:

[0221]

[0222] Each homogeneous mixture was adjusted to a pH of approximately 5.5 using a 10% citric acid solution and monitored for gel formation. In addition, experimental storage tests for 7 days and 25 days were performed using glass and plastic tubes and different holding temperatures (6°C, room temperature and 40°C). The formulations were tested for eg consistency, odor and color. Test results showed that the gelling agent Xantural 75 was compatible with neramexane mesylate (see Table 3).

[0223] table 3:

[0224]

[0225] * Experiments were performed only once and may exhibit artifacts.

Embodiment 13

[0226] Example 1.3: Klucel MF Pharma:

[0227] Klucel MF Pharma (INCI: Hydroxypropylcellulose), a solution binder, was also tested as a gelling agent in different ratios with neramexane mesylate (see Table 4).

[0228] Table 4:

[0229]

K1[%(w / w)]

K2[%(w / w)]

K3[%(w / w)]

K4[%(w / w)]

water

88

93

95.5

97.5

Klucel MF

2

2

2

2

Neramexane mesylate

10

5

2.5

0.5

total

100

100

100

100

[0230] Each homogeneous mixture was adjusted to pH 5.5 using 10% citric acid solution. In addition, experimental storage tests for 7 days and 25 days were performed using glass and plastic tubes and different holding temperatures (room temperature and 40°C). The resulting gel had a translucent appearance and test results indicated that the gelling agent Klucel MF Pharma showed good compatibility with neramexane mesylate (see Table 5). Up to 30% of n...

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Abstract

This invention provides a pharmaceutical composition for topical application to the skin of a patient in need of, comprising neramexane or a pharmaceutically acceptable salt thereof, and at least one gel forming agent for the treatment or prevention of inflammatory skin diseases such as impetigo contagiosa, acne, rosacea, eczema, atopic dermatitis, contact dermatitis, seborrheic dermatitis, psoriasis, and / or oily skin. The at least one gel forming agent comprises polymers with neutral and / or positively charged polymer backbones.

Description

field of invention [0001] The present invention provides a method for the treatment or prevention of inflammatory skin diseases such as impetigo contagiosa, acne, rosacea, eczema, atopy, for topical application to the skin of a patient in need thereof. A pharmaceutical composition for dermatitis, contact dermatitis, seborrheic dermatitis, psoriasis and / or oily skin, comprising neramexane or a pharmaceutically acceptable salt thereof, and at least one gelling agent. The at least one gelling agent comprises a polymer having a neutral polymer backbone and / or a positively charged polymer backbone. Background of the invention [0002] Neramexane (1-amino-1,3,3,5,5-pentamethylcyclohexane) and other 1-amino-alkylcyclohexane derivatives are used in various diseases, especially neurological diseases, Includes treatments for Alzheimer's disease and neuropathic pain. Neramexane and other 1-amino-alkylcyclohexane derivatives are disclosed in detail in US Patent Nos. 6,034,134 and 6,07...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61P17/00A61K31/13A61K47/36A61K47/38
CPCA61K47/38A61K31/13A61K9/0014A61K9/06A61K47/36A61P17/00A61P17/06A61P17/08A61P17/10A61P25/04A61P29/00A61P37/08
Inventor 佩特拉·谢普勒B·豪普特迈尔哈利·弗兰克·阿布茨亚历山大·林科
Owner MERZ PHARMA GMBH & CO KGAA
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