Long-acting viscose dispersing type transdermal patch and preparing process thereof

Abstract

The invention discloses a long-acting viscose dispersing type transdermal patch and a preparing process thereof and belongs to the medical technical field. The transdermal patch is mainly prepared from bulk pharmaceutical chemicals (such as non-steroid anti-inflammatory drug ibuprofen and salt form thereof, naproxen and salt form thereof, ketoprofen, indometacin and salt form thereof), a penetration enhancer (menthol, oleic acid, medium chain triglyceride, propylene glycol monolaurate, azone, propylene glycol and the like), a dispersing solvent (water, acetone, ethanol, carbinol, ethyl acetate and the like), a polyacrylate pressure-sensitive adhesive (crylic acid, butyl acrylate, crylic acid 2-ethylhexyl ester and the like), a backing layer and a release liner. The long-acting viscose dispersing type transdermal patch and the preparing process thereof have the advantages that drugs can be released from a matrix continuously for 12-48 h, the number of drug residues is low, transdermic absorption property is excellent, and dosing frequency and dosing amount can be reduced; skin irritation is avoided, and adhesion and compliance are high; main drugs and additives are stable in a viscose mechanism; preparing technology is simple, and pollution is avoided.

Description

technical field [0001] The invention relates to a long-acting viscose-dispersed transdermal patch, which can contain various types of active ingredients, has high-efficiency transdermal absorption effect, and can achieve stable and long-lasting drug release when used locally, and belongs to the technical field of medicine. Background technique [0002] Ibuprofen and its sodium salt, naproxen and its sodium salt, and ketoprofen are all NSAIDs. Non-steroidal anti-inflammatory drugs are mainly used clinically to treat rheumatism and rheumatoid arthritis, neuritis, lupus erythematosus, pain after surgery, and fever caused by various reasons. Its mechanism of action is to inhibit cyclooxygenase, reduce the biosynthesis of prostaglandins and platelet production, and inhibit lipoxygenase to reduce the production of leukotrienes. However, it has obvious gastrointestinal irritation and short half-life. Common routes of administration of NSAIDs include oral administration, injection...

AI Technical Summary

Problems solved by technology

Among them, polyisobutylene (PIBsPSA) is the earliest and most widely used as medical pressure-sensitive adhesive, such as a kind of ibuprofen transdermal release patch and its preparation method (CN200910079489), a patch containing non-steroidal anti-inflammatory drugs (CN201280059679) and aryl propionic acid non-steroidal anti-inflammatory drug transdermal patch (CN02112132), etc., but now it is recognized that it is irritating to the skin, and the isobutylene pressure-sensitive adhesive cannot be prepared in advance, and it often needs to be prepared and used now. The production process of the preparation brings inconvenience

The second type of polysiloxane pressure-sensitive adhesive (SiliconesPSA) has good affinity with the skin, but it has no good tolerance to organic solvents and water except ethyl acetate, while the viscose skeleton dispersed patch is During the preparation process, a certain amount of organic solvent is used to disperse the drug into the viscose matrix, so the low tolerance to organic solvents and water limits its application range

[0004] But now commonly used acrylate adhesive matrix usually adds vinyl acetate as a modified monomer to improve its creep resistance, such as the topical patch (CN99808428) and patch of non-steroidal antirheumatic drugs with acidic groups (CN03820678) and other related patents, this type of pressure-sensitive adhesive is usually called ethylene acrylate pressure-sensitive adhesive, which has poor aging resistance compared with pure acrylic pressure-sensitive adhesive, and due to the low reaction rate of vinyl acetate, ethylene Acrylic pressure-sensitive adhesives will have a high residual amount of vinyl acetate monomer. On the one hand, it will cause vinyl acetate monomer and organic weakly acidic drugs (such as: ibuprofen, naproxen, ketoprofen, etc.) Under the conditions of the dispersion solvent, the drug cannot be released from the matrix. On the other hand, during the volatilization of the dispersion solvent, the low molecular weight vinyl acetate migrates to the surface of the viscose matrix, making the drug unstable in the matrix. after a while

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