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Novel formulation for use in pain management

A lotion, topical technology, applied in the application of local anesthesia cream or lotion, in the field of preparation of this pharmaceutical composition, can solve the problems of prolonging time, delaying the release rate of active substances and the like

Inactive Publication Date: 2001-02-21
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantage of the use of thickeners is that the release rate of the active substance is delayed, i.e. the time for the active agent to take effect is prolonged.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 [% by weight]

[0055] (i) Isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine 15

[0056] (ii) Grindsted PGPR90  10

[0057] (iii)H 2 O 74%

[0058] (ⅳ) Sodium chloride 1%

Embodiment 2

[0059] Example 2 [% by weight]

[0060] (i) Isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine 15

[0061] (ii) Rylo PG19  10

[0062] (iii)H 2 O 74

[0063] (ⅳ) Sodium chloride 1%

[0064] Implementation Pour 3 [%wt]

[0065] (i) Isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine 15

[0066] (ii) Rylo PG19  10

[0067] (iii)H 2 O 75

Embodiment 4

[0068] Example 4 [% by weight]

[0069] (i) Isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine 10

[0070] (ii) Rylo PG19  6.7

[0071] (iii)H 2 O 83.3

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PUM

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Abstract

The present invention is directed to a novel topical pharmaceutical water-in-oil composition in form of a cream or lotion, comprising (i) 2-50% of a local anaesthetic in oil form in the final composition, or two or more local anaesthetics forming an oil when mixed together, effective to produce a topical anaesthetic effect upon administration; (ii) 2-50% of a water-in-oil emulsifier, effective to produce an emulsion of the desired viscosity; and (iii) 2-96% water. Optionally the composition may contain up to 20% of pharmaceutically acceptable stabilizers or penetration enhancers. This novel pharmaceutical composition is useful in therapy, in particularly for the treatment of pain.

Description

field of invention [0001] The present invention relates to novel water-in-oil topical pharmaceutical compositions, their use in therapy, especially as local anesthetic creams or lotions, and processes for the preparation of such pharmaceutical compositions. Background technique [0002] The viscosity of oil-in-water emulsions is so low that such compositions cannot be formulated as topical creams or lotions without the addition of a thickening agent. Therefore, in order to obtain a composition having a viscosity suitable for use as a topical cream or lotion, a thickener needs to be added to such an oil-in-water emulsion. However, the use of thickeners has the disadvantage that the release rate of the active substance is delayed, ie the time it takes for the active agent to take effect is prolonged. [0003] It is therefore an object of the present invention to provide a water-in-oil local anesthetic pharmaceutical composition in the form of a cream or lotion, having a suffi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06C07D211/60A61K9/107A61K31/138A61K31/167A61K31/245A61K31/445A61K31/451A61K47/14A61K47/34A61K47/44A61P23/02C07D211/64
CPCA61K47/44A61K9/0014A61K47/34A61P23/02A61K9/107
Inventor B·伯根斯塔尔K·维林-伯格
Owner ASTRAZENECA AB
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