Diclofenac diethylamine emulgel and preparation method thereof

A technology of diclofenac diethylamine and latex, applied in anti-inflammatory agents, pharmaceutical formulations, aerosol delivery, etc., can solve the problems of slow drug onset, poor skin permeability, slow onset, etc., and achieve transdermal absorption effect Good, the effect of reducing inflammatory swelling and pain relief

Active Publication Date: 2012-07-04
湖北科益药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diclofenac diethylamine gels and emulsions have been marketed in China, but due to the strong hydrophilicity of diclofenac diethylamine, common topical preparations have poor skin penetration, slow drug onset, and unsatisfactory bioavailability
The use of emulsification technology in preparation technology can increase the fat solubility of diclofenac diethylamine to a certain extent. For example, the diclofenac diethylamine emulsion (trade name: Voltaren latex) currently on the market in China uses isopropanol, propylene glycol, carboxylate Perm, cetumago, liquid paraffin, fatty alcohol caprylic acid / capric acid ester, fragrance and water and other auxiliary materials are prepared, but the transdermal efficiency is still not ideal, and the onset of effect is slow, which is difficult to meet the clinical requirements for rapid pain relief

Method used

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  • Diclofenac diethylamine emulgel and preparation method thereof
  • Diclofenac diethylamine emulgel and preparation method thereof
  • Diclofenac diethylamine emulgel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 isopropyl myristate prescription screening test

[0030] Different amounts of isopropyl myristate were selected to prepare diclofenac diethylamine emulsions, and the transdermal absorption test was carried out to measure the cumulative penetration per unit area of ​​diclofenac diethylamine in 1 hour. The specific results are shown in Table 1.

[0031] Table 1 Isopropyl myristate prescription screening results (unit: g / 100g)

[0032]

[0033]

[0034] Test result shows: isopropyl myristate has significant transdermal absorption promoting effect to diclofenac diethylamine, and when its dosage is 10-20%, transdermal absorption effect is the best, but when the consumption of isopropyl myristate When it reaches about 10%, its transdermal absorption promotion effect will reach the peak, and the continuous increase of its dosage will not bring significant impact on the transdermal absorption of diclofenac diethylamine, so its optimum dosage is selected as 10...

Embodiment 2

[0035] Embodiment 2 isopropanol prescription screening test

[0036] Different amounts of isopropanol were selected to make diclofenac diethylamine emulsions, and a transdermal absorption test was carried out to measure the cumulative penetration per unit area of ​​diclofenac diethylamine in 1 hour. The specific results are shown in Table 2.

[0037] Table 2 Isopropanol prescription screening results (unit: g / 100g)

[0038]

[0039] Test result shows: isopropanol has significant transdermal absorption promoting effect to diclofenac diethylamine, and when its consumption is 10-20%, transdermal absorption effect is the best, but when the consumption of isopropanol reaches about 10%, Its transdermal absorption promotion effect reaches the peak, and the increase of its dosage will not increase the transdermal absorption of diclofenac diethylamine, so its optimal dosage is 10%.

Embodiment 3

[0040] Embodiment 3 Emulsifier and oil phase prescription screening test

[0041] Different amounts of emulsifiers and oil phases were selected to make diclofenac diethylamine emulsions, and their appearance and microscopic observation were carried out, and the delamination was observed by centrifugation. The specific results are shown in Table 3.

[0042] Table 3 Screening results of emulsifier and oil phase formulation (unit: g / 100g)

[0043]

[0044] The test results show that if polysorbate 80 and glyceryl monostearate are selected as emulsifiers, and liquid paraffin is selected as the oil phase, a stable and uniform emulsion can be obtained. When the consumption of polysorbate 80 and mono-distearin was 0.5% respectively, and the consumption of oil phase was 2%, the effect was the best.

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Abstract

The invention discloses diclofenac diethylamine emulgel. In the emulgel, isopropyl myristate, isopropyl alcohol and propylene glycol are combined as a penetration enhancer; carbomer 980 is used as a water-based gel substrate matrix; liquid paraffin is used as an oil-phase matrix; and polysorbate 80 and glycerol monostearate/distearate are used as emulsifiers. The diclofenac diethylamine emulgel disclosed by the invention is high in in-vitro penetration absorption speed, takes effect quickly, and is favorable for easing the pain of a patient in time; and moreover, the diclofenac diethylamine emulgel has the characteristics of less skin irritation and high stability.

Description

technical field [0001] The invention relates to a diclofenac diethylamine emulsion and a preparation method thereof. Background technique [0002] Diclofenac diethylamine is a non-steroidal anti-inflammatory analgesic, which has anti-inflammatory and analgesic effects. When applied topically, its active ingredients can penetrate the skin to reach the inflammatory area, relieve acute and chronic inflammatory reactions, and reduce inflammatory swelling , Pain relief. Diclofenac diethylamine gels and emulsions have been marketed in China. However, due to the strong hydrophilicity of diclofenac diethylamine, common topical preparations have poor skin penetration, slow drug onset, and unsatisfactory bioavailability. The use of emulsification technology in preparation technology can increase the fat solubility of diclofenac diethylamine to a certain extent. For example, the diclofenac diethylamine emulsion (trade name: Voltaren latex) currently on the market in China uses isoprop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/205A61K47/14A61K47/10A61K47/32A61K47/44A61K47/26A61P29/00A61K31/196
Inventor 余修祥史自东郭小杰吴迪王菁烨李瑛
Owner 湖北科益药业股份有限公司
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