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An external skin patch containing flupirtine or a pharmaceutically acceptable salt thereof

A technology of medicinal salt and flupirtine, applied in the field of pharmaceutical preparations, can solve the problems of poor bioavailability, low compliance, high blood drug concentration, etc., to improve skin permeability, improve stability, and ensure high effect of concentration

Active Publication Date: 2022-07-15
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, transdermal drug delivery has become a mature technology. This method can be used to transport drugs. However, due to the different properties of drug components, transdermal drug delivery also has limitations. For example, human skin has poor permeability, and most drugs cannot Enter the human body through the skin, poor bioavailability, high blood concentration and low response due to frequent application, and at the same time, transdermal administration may also cause skin irritation, high production cost and unsatisfactory the apparent status quo, etc.

Method used

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  • An external skin patch containing flupirtine or a pharmaceutically acceptable salt thereof
  • An external skin patch containing flupirtine or a pharmaceutically acceptable salt thereof
  • An external skin patch containing flupirtine or a pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Example 1 Self-adhesive matrix layer patch containing acrylate pressure-sensitive adhesive

[0090] Table 1. Formulation of Self-Adhesive Matrix Patches Containing Acrylate Pressure Sensitive Adhesives

[0091]

[0092] Recipe 1: Take the acrylate pressure-sensitive adhesive in the prescribed amount, add 6 parts of flupirtine maleate and 15 parts of solubilizer PVP, mix well, add 18 parts of penetration enhancer azone and 3 parts of antioxidant and sodium metabisulfite, Add an appropriate amount of methanol, mix evenly, add 1 part of sodium bicarbonate, stir evenly to obtain a paste, coat it on the support layer, dry, and after the organic solvent is volatilized, cover the release liner to obtain a transdermal absorption preparation.

[0093] Formulation 2: The difference from Formulation 1 is that each substance was added according to Table 1, and a transdermal absorption preparation was prepared in the same manner as Formulation 1.

[0094] Formulation 3: The diff...

Embodiment 2

[0105] Example 2 Self-adhesive matrix layer patch containing polyisobutylene pressure-sensitive adhesive

[0106] Table 4. Formulation of self-adhesive matrix layer patch containing polyisobutylene pressure-sensitive adhesive

[0107]

[0108] Recipe 5: Take the polyisobutylene pressure-sensitive adhesive in the prescribed amount, add 10 parts of light liquid paraffin, 3 parts of colloidal silicon dioxide, after mixing evenly, add 5 parts of PVP, 5 parts of menthol, 5 parts of azone and an appropriate amount of methanol , stir and mix evenly, add 1 part of flupirtine maleate to the above mixing system, after the drug is completely dissolved, add 0.3 part of sodium bicarbonate, stir evenly, and then get a paste, spread it on the support layer, dry , and after the organic solvent is volatilized, the release liner is covered to obtain a transdermal absorption preparation.

[0109] Formulation 6: The difference from Formulation 4 is that each substance is added according to Ta...

Embodiment 3

[0122] Example 3 A patch containing a self-adhesive matrix layer of silicone pressure-sensitive adhesive

[0123] Table 7. Patch Formulations for Self-Adhesive Matrix Layers Containing Silicone Pressure Sensitive Adhesives

[0124]

[0125]Recipe 9: Take the silicone pressure-sensitive adhesive in the prescribed amount, add 10 parts of light liquid paraffin, 3 parts of colloidal silicon dioxide, mix well, add 15 parts of PVP, 5 parts of menthol, 5 parts of azone and an appropriate amount of methanol , stir and mix evenly, add 6 parts of flupirtine maleate to the above mixing system, after the drug is completely dissolved, add 0.5 part of sodium bicarbonate, stir evenly, and then get a paste, coat it on the support layer, dry , and after the organic solvent is volatilized, the release liner is covered to obtain a transdermal absorption preparation.

[0126] Formulation 10: The difference from Formulation 9 is that each substance is added according to Table 7, the solubilize...

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Abstract

The invention discloses a transdermal absorption preparation containing flupirtine or a pharmaceutically acceptable salt thereof. The preparation contains a support layer that does not interact with matrix components, a self-adhesive matrix layer and a protective foil or film that must be torn off before use. Tablet, wherein the matrix layer contains 0.1-20 mass % of flupirtine or its pharmaceutically acceptable salt, water-insoluble polymer adhesive system and solubilizer as active ingredient, and the selected solubilizer of the present invention can effectively improve flupirtine or The solubility of its medicinal salts, while adding a non-water-soluble polymer adhesive system, based on this, the self-adhesive matrix layer formed can not only effectively improve the solubility of the active pharmaceutical ingredients, but also effectively ensure the stability of the preparation. sex.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an external preparation for skin containing flupirtine or a pharmaceutically acceptable salt thereof. Background technique [0002] Flupirtine is an analgesic drug, which belongs to one of the new non-opioid central drugs. Currently, flupirtine maleate is mainly used in the market, and its dosage form is mainly solid tablets. In addition to the different mechanisms of non-steroidal anti-inflammatory analgesics and opioids commonly used in clinical practice, it also has the effects of analgesia, nerve protection and muscle relaxation. When flupirtine is administered orally, flupirtine is almost completely absorbed from the gastrointestinal tract and biotransformed in the liver, 90% for oral flupirtine from the gastrointestinal tract and 70% for rectal administration, although its Absorption is fast, but its action time is short. Therefore, researchers developed flupirti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K47/32A61K31/44A61P25/04
Inventor 周丽莹刘亚男吴越卢迪
Owner BEIJING TIDE PHARMA
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