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Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch

A transdermal patch and high-dose technology, which is applied in the field of medicine, can solve the problems of short tolerance time and poor compliance of high-dose capsaicin, and achieve the effects of promoting drug efficacy, reducing irritation, and improving compliance

Active Publication Date: 2011-02-02
南京鼎世医疗器械有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to overcome the shortcomings of the existing capsaicin transdermal preparations, especially the short tolerance time and poor compliance of patients to high-dose capsaicin, the present invention provides a double-controlled release high-dose and low-irritation capsaicin compound transdermal patch

Method used

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  • Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch
  • Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch
  • Double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Prescription (43cm 2 Feeding)

[0041] upper layer:

[0042] Menthol 0.10g

[0043] borneol 0.10g

[0044] Oleic acid (OA) 0.08g

[0045] 1,2-propanediol (PG) 0.20g

[0046] Dibutylphenol 0.01g

[0047] Polyacrylate (87-2852, American Chemical Starch Company) 0.5g

[0048] lower level:

[0049] Capsaicin (natural extract) 27.52mg

[0050] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 0.3g

[0051] Laurocaprazine (Az) 0.10g

[0052] Rohm Eudragit E100 (Rohm Germany) 0.4g

[0053] Preparation method: upper layer: take the prescribed amount of menthol and borneol, add OA, PG, dibutylphenol, polyacrylate and an appropriate amount of ethyl acetate, stir evenly, vacuum degas, and apply the upper layer glue on the anti-adhesive layer Cloth into a uniform thin layer with a certain thickness, and bake at 60°C for 30 minutes. Lower layer: Take the prescribed amount of capsaicin and HP-β-CD, add appropriate amount of ethanol to dissolve, and ultrasonically clathrate; take ano...

Embodiment 2

[0062] Prescription (43cm 2 Feeding)

[0063] upper layer:

[0064] Dexketoprofen 0.02g

[0065] Borneol 0.08g

[0066] Menthol 0.10g

[0067] Oleic acid (OA) 0.12g

[0068] 1,2-propanediol (PG) 0.25g

[0069] Propyl Perylate 0.008g

[0070] Polyacrylate (87-8525, American Chemical Starch Company) 0.9g

[0071] lower level:

[0072] Capsaicin (synthetic) 27.52mg

[0073] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 0.3g

[0074] Oleic acid (OA) 0.12g

[0075] Dimethylformamide 0.15g

[0076] ROHM Eudragit RL100 (Germany ROHM company) 0.5g

[0077] Polyvinylpyrrolidone (PVP K30) 0.1g

[0078] Preparation method: upper layer: take the prescription amount of dexketoprofen, menthol, propyl pyritate and borneol, add OA, PG, polyacrylate and an appropriate amount of ethyl acetate, stir evenly, vacuum degas, and put the upper layer of glue Coat the anti-adhesive layer into a uniform thin layer with a certain thickness, and bake at 60°C for 30 minutes. Lower layer: take the pr...

Embodiment 3

[0084] Prescription (43cm 2 Feeding)

[0085] upper layer:

[0086] Flurbiprofen 0.0185g

[0087] borneol 0.15g

[0088] Oleic acid (OA) 0.10g

[0089] 1,2-propanediol (PG) 0.25g

[0090] Dibutylphenol 0.02

[0091] Polyacrylate (87-2677, American Chemical Starch Company) 1.0g

[0092] lower layer:

[0093] Dihydrocapsaicin 21.5mg

[0094] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 0.25g

[0095] Ethyl oleate 0.06g

[0096] Tween-80 0.10g

[0097] Hydroxypropylmethylcellulose (HPMC) 0.06g

[0098] Eudragit L100 (German Rohm company) 0.35g

[0099] Upper layer: Take the prescribed amount of flurbiprofen and borneol, add OA, PG, polyacrylate, dibutylphenol and an appropriate amount of ethyl acetate, stir evenly, vacuum degas, and coat the upper layer of glue on the anti-adhesive layer Form a uniform thin layer with a certain thickness and bake at 60°C for 30 minutes. Lower layer: take the prescribed amount of dihydrocapsaicin and HP-β-CD, add appropriate amount of etha...

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Abstract

The invention discloses a double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch. The patch is divided into an upper layer and a lower layer; a medicament on the upper layer is one or more of menthol, peppermint oil, borneol and a non-steroidal anti-inflammatory medicine which has synergy with capsaicin and can dispel or alleviate local discomfort reaction to the capsaicin, particularly penetrates into the skin more rapidly than the capsaicin to respond, has synergetic therapeutic effect with the capsaicin, and can dispel or alleviate local discomforts such as burning sensation and the like in the initial usage period of the capsaicin; the capsaicin on the lower layer of the patch exists in the form of a cyclodextrin inclusion compound; the patch fully absorbs water after being used on the skin for 6 to 8 hours; and the capsaicin is slowly released from the inclusion compound and penetrates into the skin. The double-controlled release, high-dosage and low-irritation capsaicin compound transdermal patch overcomes the defects of short tolerance time and poor medication compliance of a patient during the transdermal administration of high-dosage capsaicin, and facilitates achieving the maximum pharmacological effect of a medicament.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a capsaicin compound transdermal patch with double controlled release, high dosage and low irritation for treating painful neuropathy, neuralgia, musculoskeletal pain and other superficial pain syndromes . Background technique [0002] Capsaicin is a kind of natural alkaloid extracted and separated from the mature fruit of pepper of Solanaceae plant. There are many capsaicin analogues in natural extracts, including capsaicin and its analogues dihydrocapsaicin, nordihydrocapsaicin, High dihydrocapsaicin, high capsaicin, etc., among which capsaicin is the most pungent and active ingredient. Due to the high cost of extracting and separating high-purity capsaicin, domestic and foreign artificially synthesized capsaicin has been listed. In addition, artificially synthesized capsaicin analogues have also been reported, and studies on the pharmacological effects of capsaicin and its ...

Claims

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Application Information

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IPC IPC(8): A61K36/534A61K47/40A61P19/08A61K45/00A61P25/00A61K31/045A61K36/81A61P21/00A61P29/00A61K31/165A61K9/70A61K131/00A61K31/23
Inventor 叶金翠陈国神
Owner 南京鼎世医疗器械有限公司
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