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Diclofenac epolamine jellies, preparing method and uses thereof

A technology of diclofenac epamide and eporamide gel, which is applied in the direction of drug combination, drug delivery, antipyretics, etc., and can solve the problem of poor solubility and poor bioavailability of diclofenac sodium and diclofenac diethylamine salt Ideal, poor skin permeability and other problems, to achieve the effect of good skin coupling, safe function, and convenient use

Active Publication Date: 2008-07-23
SHANGHAI HUILUN BIOLOGICAL TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of diclofenac sodium and diclofenac diethylamine salt, the skin permeability is relatively poor, and the bioavailability is not ideal

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Prescription Carbomer 1%

[0040] Triethanolamine 1.2% (adjust the pH to about 7.0)

[0041] Diclofenac Eporamide 1.3%

[0042] Propylene Glycol 20%

[0043] Glycerol 5%

[0044] EDTA-2Na 0.02%

[0045] Ethylparaben 0.1%

[0046] Purified water makes up 100%

[0047]Preparation: add carbomer to an appropriate amount of pure water, swell naturally for 24 hours, stir well, adjust the pH to about 7.0 with triethanolamine, add glycerol and stir well, and set aside; add diclofenac eporamide to 300g water, EDTA- Add 2Na and dissolve in 10g water, combine the two aqueous solutions, and set aside; take another 1g of ethyl paraben and add it to 200g propylene glycol to dissolve, slowly add it to the carbomer stock solution, stir evenly, and then slowly add diclofenac epodol dropwise Amine solution, stir evenly; add purified water to 1000g, stir evenly, degas, potting, and pack.

Embodiment 2

[0049] Prescription Carbomer 1%

[0050] Triethanolamine 1.2% (adjust the pH to about 7.0)

[0051] Diclofenac Eporamide 1.3%

[0052] Soy Lecithin 5%

[0053] Macrogol 400 Stearate 2%

[0054] Glycerol 10%

[0055] Isopropanol 10%

[0056] Fragrance 0.1%

[0057] Purified water makes up 100%

[0058] Preparation: add carbomer to an appropriate amount of purified water to swell naturally for 24 hours, stir well, adjust the pH to about 7.0 with triethanolamine, and heat in a water bath at 50°C for later use; add glycerol, soybean lecithin and polyethylene glycol 400 Mix stearate, heat and melt in a water bath at 50°C, mix evenly, add diclofenac eporamide into the liquid and stir to dissolve, and set aside; when the temperature reaches about 45°C, slowly pour the solution containing the drug into Carbomer During the process, stir evenly while adding. After adding completely, continue to stir in the water bath for 10 minutes, take it out, and cool it down; ...

Embodiment 3

[0060] Prescription Carbomer 0.6%

[0061] Triethanolamine 1.2% (pH adjusted to about 7.8)

[0062] Diclofenac Eporamide 1.3%

[0063] Polyoxyethylene glyceride (C 12 -C 18 ) 4%

[0064] Macrogol 300 2%

[0065] Propylene Glycol 10%

[0066] Isopropanol 10%

[0067] Fragrance 0.1%

[0068] Purified water makes up 100%

[0069] Preparation: add 6 g of carbomer to 300 g of purified water to swell naturally for 24 hours, stir well, adjust the pH to about 7.8 with triethanolamine, and heat in a water bath at 50°C for later use; mix propylene glycol, polyoxyethylene glyceride (C 12 -C 18 ) and polyethylene glycol 300, heated and melted in a 50°C water bath, mixed evenly, added diclofenac eporamide into the liquid, stirred and dissolved, and set aside; when the temperature reached about 45°C, slowly poured the solution containing the drug In the carbomer, stir evenly while adding, after adding completely, continue stirring in the w...

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PUM

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Abstract

The invention relates to a non-steroidal anti-inflammatory demulcent drug, which is a diclofenac epolamine gel preparation for relieving moderate pain in muscles, soft tissues and articulations. The gel preparation adopts 0.1-8.0 percent (weight percentage) of diclofenac epolamine as a main activated ingredient, 0-20 percent of grease, 0-5 percent of surfactant, 5-20 percent of cosolvent, a pH regulator, 5-20 percent of bacteriostat, 0.5-2.0 percent of gel substrate, etc. and purified water. PH value of the preparation is 6.0-8.0. The invention also provides a preparation method of the gel. The gel preparation of the invention has the advantages of good stability and good skin coupling effect, and can promote absorption of the skin to the drug and improve bioavailability and curative effect; at the same time, the substrate has stable property and no irritation to the skin, can be easily smeared and washed, has no greasiness, is beneficial to releasing of drug, especially water soluble drug and has good safety and clinical practicability.

Description

Technical field: [0001] The invention relates to a diclofenac eporamide gel preparation, a preparation method and a medicinal use thereof. Background technique: [0002] Diclofenac epamide is a non-steroidal anti-inflammatory analgesic drug, mainly used to relieve moderate pain in muscles, soft tissues and joints. After being prepared into a corresponding external preparation and rubbed, the active ingredients can easily penetrate the skin and resist chronic inflammation. Diclofenac diethylamine gel and diclofenac sodium gel have been listed in China. However, because the water solubility of diclofenac sodium and diethylamine salt of diclofenac is not very ideal, the skin permeability is relatively poor, and the bioavailability is not ideal. Therefore, it is necessary to find a novel topical analgesic with good water solubility and high bioavailability. Invention content: [0003] For overcoming above-mentioned existing technical defect, the object of the present invent...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/196A61P29/00
Inventor 秦继红
Owner SHANGHAI HUILUN BIOLOGICAL TECH CO LTD
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