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Flurbiprofen paracetamol ester external use slow release transdermal patch and preparation method thereof

A technology of acetaminophen and flurbiprofen, applied in the field of medicine

Active Publication Date: 2013-07-24
WUXI ERYUN TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Flurbiprofen acetaminophen has the characteristics of good fat solubility and high membrane permeability, so it has good transdermal drug properties. If it is developed as a transdermal patch, it can be absorbed by the carboxylate distributed in the skin. The enzyme and the esterase in the blood plasma are slowly hydrolyzed, so as to maintain the effective drug concentration in the affected tissue for a long time, and exert local long-acting anti-inflammatory and analgesic effects; at the same time, there are no obvious side effects of gastrointestinal tract, liver and kidney toxicity, but the existing There is no related report about flurbiprofen acetaminophen transdermal patch in the technology

Method used

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  • Flurbiprofen paracetamol ester external use slow release transdermal patch and preparation method thereof
  • Flurbiprofen paracetamol ester external use slow release transdermal patch and preparation method thereof
  • Flurbiprofen paracetamol ester external use slow release transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Prepare flurbiprofen acetaminophen external sustained-release transdermal patch as follows:

[0072] (1) Add 34g of high-molecular-weight polyisobutene with a molecular weight above 10,000, 15g of low-molecular-weight polyisobutene with a molecular weight of 300-3500, and 12g of liquid paraffin into 100ml of butane for swelling. as matrix solution;

[0073] (2) Dissolve 2 g of flurbiprofen acetaminophen, 5 g of laurocapram, and 1 g of 2,6-di-tert-butyl-p-cresol in 15 ml of absolute ethanol at a temperature of 60° C. to make fluorine Biprofen paracetamol ester concentration is the mixed solution of 13.3wt%;

[0074] (3) adding the mixed solution obtained in step (2) to the substrate solution obtained in step (1), stirring evenly, and ultrasonically removing air bubbles to obtain a drug-containing reservoir layer;

[0075] (4) coating the drug-containing reservoir layer obtained in step (3) on a polyester film whose surface has been treated with silicone oil anti-adhesi...

Embodiment 2

[0079]Prepare flurbiprofen acetaminophen external sustained-release transdermal patch as follows:

[0080] (1) Add 40g of polyacrylate pressure-sensitive adhesive, 26g of liquid paraffin, and 8g of tackifying resin into 100ml of pentane for swelling, and use it as a matrix solution when it is in a uniform and viscous semi-solid fluid state;

[0081] (2) Dissolve 2 g of flurbiprofen acetaminophen together with 5 g of lecithin and 2 g of vitamin E in 10 ml of absolute ethanol at a temperature of 50° C. to make flurbiprofen acetaminophen at a concentration of 20 wt % mixed solution;

[0082] (3) adding the mixed solution obtained in step (2) to the substrate solution obtained in step (1), stirring evenly, and ultrasonically removing air bubbles to obtain a drug-containing reservoir layer;

[0083] (4) coating the drug-containing reservoir layer obtained in step (3) on a polyester film whose surface has been treated with silicone oil anti-adhesive treatment, and drying at a tempe...

Embodiment 3

[0086] Prepare flurbiprofen acetaminophen external sustained-release transdermal patch as follows:

[0087] (1) Add 48g of silicone pressure-sensitive adhesive and 26g of liquid paraffin into 100ml of toluene for swelling, and use it as a matrix solution when it is in a uniform and viscous semi-solid fluid state;

[0088] (2) Flurbiprofen acetaminophen 2g, propylene glycol 5g, and poloxamer 1882g are dissolved in 7ml of absolute ethanol at a temperature of 30°C to make flurbiprofen acetaminophen at a concentration of 28.6wt% mixed solution;

[0089] (3) adding the mixed solution obtained in step (2) to the substrate solution obtained in step (1), stirring evenly, and ultrasonically removing air bubbles to obtain a drug-containing reservoir layer;

[0090] (4) coating the drug-containing reservoir layer obtained in step (3) on a polyester film whose surface has been treated with silicone oil anti-adhesive treatment, and drying at a temperature of 30° C.;

[0091] (5) The surf...

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Abstract

The invention relates to a flurbiprofen paracetamol ester external use slow release transdermal patch and a preparation method thereof. The transdermal patch comprises a backing membrane layer, a drug-containing storage layer and an antistick layer, wherein, the drug-containing storage layer comprises 1-40 wt.% flurbiprofen paracetamol ester and 20-50 wt.% pressure-sensitive adhesive and 10-30 wt.% penetration promoter, as well as 0-20 wt.% additive optionally. The invention provides flurbiprofen paracetamol ester external use slow release transdermal patch has good percutaneous permeability and slow releasing effect, and can maintain effective plasma concentration of the affected part for 24 hours, and performs long-acting anti inflammatory and analgesic effect of the partial part with suitable viscosity, extreme low skin excitant and without obvious toxic and side effect. The patch is especially suitable for treatment of bone arthritis, rheumatoid arthritis, ankylosing spondylitis and other inflammations as well as symptomatic treatment of sprain, muscle strain and other soft tissue aches and postoperative aches.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to non-steroidal anti-inflammatory drugs, in particular to a flurbiprofen acetaminophen external slow-release transdermal patch and a preparation method thereof. Background technique [0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most commonly prescribed drugs in the world, and their antipyretic, analgesic, anti-inflammatory and anti-rheumatic effects have been verified in clinical practice for many years. Flurbiprofen is one of the excellent varieties of non-steroidal anti-inflammatory analgesics, belonging to aryl propionic acid non-steroidal anti-inflammatory analgesics, mainly used for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spine Inflammation, traumatic pain and other pains, etc., show strong anti-inflammatory and analgesic effects among similar drugs, but flurbiprofen also has the common defects of non-steroidal drugs, such as lo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/216A61P29/00
Inventor 葛广波杨凌洪沫宁静邹超张辉
Owner WUXI ERYUN TECH CO LTD
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