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Long-acting diclofenac transdermal patch and preparation technology thereof

A technology of diclofenac and transdermal patch, which is applied in the field of medicine, and can solve problems such as ready-to-use, lower drug transdermal penetration rate, and pressure-sensitive adhesives that cannot be prepared in advance.

Inactive Publication Date: 2016-06-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, polyisobutylenes (PIBs) are the first and most widely used in the field of medical pressure-sensitive adhesives, such as pain-relieving and anti-inflammatory patches for local use (CN028014111), and patches containing non-steroidal anti-inflammatory and analgesic agents (CN200480007150) and anti-inflammatory and analgesic external patch (CN102791267A) and other related patents, but now it is recognized that it is irritating to the skin, and polyisobutylene pressure-sensitive adhesives cannot be prepared in advance, and often need to be prepared and used immediately, which brings new benefits to the production process of the preparation. Inconvenience factor
The second type of polysiloxane pressure-sensitive adhesive (SiliconesPSA) has good affinity with the skin, such as related patents such as patches with adjustable sealing (CN103826619A), but the matrix is ​​sensitive to organic solvents and water except ethyl acetate. None of them have good compatibility, so a certain amount of organic solvent needs to be used in the preparation process to disperse the drug in the viscose matrix, which limits its scope of use.
The third type of polyacrylate pressure-sensitive adhesive (AcrylicsPSA) has good flexibility, high skin affinity, and has certain tolerance to various organic solvents (such as methanol, ethanol, acetone, etc.). It is most suitable as a kind of medical pressure-sensitive adhesive, but the commonly used acrylate adhesive base usually adds plasticizer to achieve proper adhesion, such as diclofenac sodium patch and its preparation method (CN1215838C) and other related patents, commonly used Plasticizers such as citric acid, citrate, succinic acid, succinate, etc. On the one hand, adding additional plasticizers will bring inconvenience to the production process; on the other hand, plasticizers such as citric acid will not only change the patch The pH of the matrix affects the stability of the formulation and there is a risk of reducing the transdermal penetration of the drug

Method used

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  • Long-acting diclofenac transdermal patch and preparation technology thereof
  • Long-acting diclofenac transdermal patch and preparation technology thereof
  • Long-acting diclofenac transdermal patch and preparation technology thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Preparation of long-acting diclofenac patch, drug content per unit area: 2.00mg / cm 2

[0038]

[0039] Preparation process: Precisely weigh diclofenac and add it to a mixed solution of acetone and water to fully dissolve it, add menthol, macrogol glyceride oleate and propylene glycol, shake and mix well. Pour the above mixture into the pressure sensitive adhesive base and stir well. Mix ultrasonically for 20 min until there are no bubbles. Pour the drug glue mixture into a suitable applicator, pull it slowly at a constant speed on the side of the release film with silicone oil, so that the drug glue mixture is evenly coated on the release film, dry at 70°C for 20 minutes, take it out, and attach the backing lining.

Embodiment 2

[0040] Embodiment 2: Preparation of long-acting diclofenac sodium patch, drug content per unit area: 1.00mg / cm 2

[0041]

[0042] Preparation process: Precisely weigh diclofenac sodium and add it to a mixed solution of acetone and water to fully dissolve it, add peppermint oil, oleic acid and azone, shake and mix well. Pour the above mixture into the pressure sensitive adhesive base and stir well. Mix ultrasonically for 20 min until there are no bubbles. Pour the drug glue mixture into a suitable applicator, pull it slowly at a constant speed on the side of the release film with silicone oil, so that the drug glue mixture is evenly coated on the release film, dry at 70°C for 20 minutes, take it out, and attach the backing lining.

Embodiment 3

[0043] Embodiment 3: Preparation of long-acting diclofenac potassium patch, drug content per unit area: 0.50mg / cm 2

[0044]

[0045] Preparation process: Accurately weigh an appropriate amount of diclofenac potassium and add it to a mixed solution of ethanol and water to fully dissolve it, add menthol, caprylic acid macrogol glyceride and isopropanol, shake and mix well. Pour the above mixture into the pressure sensitive adhesive base and stir well. Mix ultrasonically for 20 min until there are no bubbles. Pour the drug glue mixture into a suitable applicator, pull it slowly at a constant speed on the side of the release film with silicone oil, so that the drug glue mixture is evenly coated on the release film, dry at 70°C for 20 minutes, take it out, and attach the backing lining.

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Abstract

The invention discloses a long-acting diclofenac transdermal patch and a preparation technology thereof and belongs to the technical field of medicine. The preparation is mainly prepared from a diclofenac bulk pharmaceutical chemical, a penetration enhancer, a dispersing solvent and a polyacrylate pressure-sensitive adhesive. The long-acting diclofenac transdermal patch and the preparation technology thereof have the following advantages: (1) the drug can be released from a matrix continuously for 12-48 h, the drug remaining amount is low, the percutaneous absorption is excellent, and the drug delivery times and dosage can be reduced; (2) a product has no skin irritation and has good adhesion and flexibility; (3) the main drug and the additives are stable in a viscose matrix; (4) the preparation technology is simple, convenient and pollution-free.

Description

technical field [0001] The invention relates to a long-acting diclofenac transdermal patch, which can contain diclofenac active ingredients, has a long-acting percutaneous penetration effect, can achieve long-lasting and stable drug release, and belongs to the technical field of medicine. Background technique [0002] Diclofenac and its salt forms (Diclofenac) are an important class of non-steroidal antipyretic analgesic anti-inflammatory drugs (Non-steroidal Anti-inflammatory Drugs, NSAIDs), its pharmacological effect is mainly to inhibit the production of prostaglandin (PG) in the body. Synthesis; PG has a high degree of biological activity and participates in various pathological processes such as fever, pain, and inflammation in the body. Diclofenac covers the active center of the enzyme by combining with cyclooxygenase (Cyclooxygenase, COX), thereby blocking the metabolic process of the enzyme that catalyzes the transformation of arachidonic acid (AA) into PG, analgesic...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/196A61K47/32A61P29/00
CPCA61K9/7053A61K31/196
Inventor 周建平徐铄丁杨姜孟劳韩悦
Owner CHINA PHARM UNIV
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