Novel chemical drug patch ketoprofen patch and preparation method thereof

A technology of ketoprofen and transdermal patches, applied in the field of ketoprofen patches, which can solve the problems of volatilization, affecting the quality and curative effect of drugs, and large changes

Active Publication Date: 2020-10-20
北京乳凝创智生物技术研发中心(有限合伙)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But in the data such as existing patent document, there is the ketoprofen patch that contains or does not contain L-menthol, all have set forth respectively in relevant patent document and contain or do not contain the advantages and disadvantages of L-menthol, and its advantage is It can keep the drug continuously passing through the human body and maintain the required blood concentration of the drug. The disadvantage is that the smell is unpleasant, and at the same time, L-menthol is easy to volatilize, so that the content of menthol changes greatly during the long-term storage after the product goes on the market. The penetration effect will have a very large impact, which will affect the quality and curative effect of the drug. At the same time, L-menthol will easily react with ketoprofen to generate new compounds, which will affect the content of ketoprofen in the patch, the quality of the drug and the medication. effectiveness
[0004] And in the ketoprofen related patents that do not contain menthol, documents and other materials, it is shown that in order to achieve the same therapeutic effect when the transdermal amount of the drug is not used when L-menthol is not used, liquid paraffin, olive oil, Soybean oil, castor oil, etc. are used as dissolving agents for ketoprofen, and after ketoprofen is completely dissolved, they are added to a type of adhesive containing styrene-isoprene-styrene to prepare a transdermal patch or in this type of adhesive. The adhesive exists in a completely dissolved molecular state, but the test is carried out according to the content described in its patent information. After our experiments, we found that under the effective dosage contained in the patent of ketoprofen transdermal patch, it can be absorbed by ultrasound, stirring Ketoprofen cannot be used in the above oil solvents under conditions such as prolonging the dissolution time and increasing the amount of oil mentioned above (Note: when the cohesive force added to the adhesive is completely destroyed when the amount of oil is increased) Dissolve completely, when above the fusing point of ketoprofen is heated to above oily substance, ketoprofen melts completely, and when temperature is lower than the fusing point of ketoprofen, ketoprofen all separates out in above-mentioned oil, but, when long-term When in the above high temperature state, the damage of the above oils will volatilize seriously, and the stability of product quality cannot be guaranteed.

Method used

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  • Novel chemical drug patch ketoprofen patch and preparation method thereof
  • Novel chemical drug patch ketoprofen patch and preparation method thereof
  • Novel chemical drug patch ketoprofen patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] In this experiment, a styrene-isoprene-styrene block copolymer with a styrene content of 15% was used as a skeleton material, liquid paraffin was used as a softener, and hydrogenated rosin glyceride was used as a thickener to prepare ketoprofen transdermal Matrix adhesives for patches, specifically as follows:

[0036] Adhesive formula used:

[0037] component name Styrene-isoprene-styrene block copolymer Hydrogenated Rosin Glycerides liquid paraffin antioxidant Other functional additives ContentWt / % 29.9 22.4 42.7 0.2 4.8

[0038] Using "styrene-isoprene-styrene block copolymer" as the skeleton material to prepare adhesives for medical transdermal patches, adding tackifiers, softeners, antioxidants, and other special functional additives such as inorganic Fillers, hydrophilic substances, etc. The specific auxiliary raw materials are as follows:

[0039] Tackifier: The tackifier used in this embodiment can also be used in conjunction ...

Embodiment 2

[0048] In this experiment, a combination of styrene-isoprene-styrene block copolymer and styrene-isoprene diblock copolymer with a styrene content of 15% was used as the skeleton material, and low molecular weight polyisobutylene with a molecular weight of 400 As a softener, hydrogenated rosin glyceride and polyisobutylene of different molecular weights were used as tackifiers to prepare drug carrier adhesives for neck pain patches, as follows:

[0049] Adhesive formula used:

[0050] component name Styrene-isoprene-styrene block copolymers and styrene-isoprene diblock copolymers Hydrogenated Rosin Glycerides Medium Molecular Weight Polyisobutylene Polyisobutylene Mn=400 antioxidant Other functional additives ContentWt / % 29.8 13.6 18.1 32.7 0.1 5.7

[0051] Using styrene-isoprene-styrene block copolymer and styrene-isoprene diblock copolymer as skeleton materials to prepare adhesives for medical transdermal patches, adding tackifiers, soften...

Embodiment 3

[0053] Ketoprofen dissolution effect experiment: This experiment investigated and selected a dissolving agent that has a good dissolving effect on ketoprofen, and focused on selecting a ketoprofen dissolving agent that also has penetration-promoting properties. In the experiment, other patents such as ZL The patent No. is 01808284.X and the patent publication number is the dissolution effect of ketoprofen when particularly mentioning in CN101137356A with liquid paraffin, olive oil, soybean oil, castor oil etc. as ketoprofen dissolving agent, concrete result is as follows:

[0054] Table, the dissolution effect of ketoprofen in different solvents

[0055] Solvent type Ketoprofen content / % Dissolving effect at room temperature Dissolution effect at 60°C 85 ℃ high temperature dissolution effect liquid paraffin 20 insoluble insoluble Dissolved, crystallized ketoprofen appeared at room temperature olive oil 20 insoluble insoluble Dissolved, ...

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Abstract

The present invention discloses a novel chemical drug patch ketoprofen paster and a preparation method thereof. The novel chemical drug patch ketoprofen paster comprises a styrene-isoprene-styrene triblock copolymer, a styrene-isoprene diblock copolymer, a tackifier, a softener and an antioxygen; the patch has the characteristics that the stimulation to skins is very slight, an adhesive is free from the stimulation to the skins, the drug stabilization in long-term storage is good, the pasting with the skins is good, the repeatable pasting is realized, pasting is kept when contacted with water, particularly the pasting with knees, elbows and other parts; the adhesive in the patch comprises components in percentage by weight: 10%-55% of the styrene-isoprene-styrene triblock copolymer and the styrene-isoprene diblock copolymer totally, less than 22% of polyisobutene with high molecular weight, less than 30% of polyisobutene with middle molecular weight, less than 25% of polyisobutene with low molecular weight, 10%-60% of the tackifier, and 12%-55% of the softener; the antioxygen accounts for 0.01%-2.5% of the sum amount of framework materials.

Description

technical field [0001] The invention relates to an adhesive and a drug patch, in particular to a medicinal adhesive and a ketoprofen patch prepared therefrom, which are used for treating lumbago and leg pain, muscle pain, joint pain and the like. Background technique [0002] Mix ketoprofen or its solution with an adhesive containing styrene-isoprene-styrene block copolymers evenly, then attach it to the backing cloth, and cover the release paper on the other side of the glue layer It is known to prepare an external transdermal patch with anti-inflammatory and analgesic effects after a release film. [0003] But in the data such as existing patent document, there is the ketoprofen patch that contains or does not contain L-menthol, all have set forth respectively in relevant patent document and contain or do not contain the advantages and disadvantages of L-menthol, and its advantage is It can keep the drug continuously passing through the human body and maintain the require...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/192A61P29/00A61P19/02
CPCA61K9/7053A61K9/7076A61K31/192
Inventor 侯玉庆刘彦宏陶几中马丹徐建梅侯天歌
Owner 北京乳凝创智生物技术研发中心(有限合伙)
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