CN110559275A - Application for skin anesthesia and preparation method thereof - Google Patents

Application for skin anesthesia and preparation method thereof Download PDF

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Publication number
CN110559275A
CN110559275A CN201910788397.8A CN201910788397A CN110559275A CN 110559275 A CN110559275 A CN 110559275A CN 201910788397 A CN201910788397 A CN 201910788397A CN 110559275 A CN110559275 A CN 110559275A
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parts
patch
weight
anesthesia
skin anesthesia
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卢敏
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Xi'an Bo He Medical Technology Co Ltd
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Xi'an Bo He Medical Technology Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Anesthesiology (AREA)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention provides a patch for skin anesthesia, which comprises the following components in parts by weight: 2-15 parts of film forming material, 0.5-1 part of thickening agent, 5-10 parts of anesthetic, 17-68 parts of transdermal absorbent, 0.1-0.8 part of bacteriostatic agent and 36-67 parts of water. The patch for skin anesthesia has the advantages of stable dosage, easy operation, short onset time, long drug effect time and strong anesthesia and analgesia depth.

Description

Application for skin anesthesia and preparation method thereof
Technical Field
The invention belongs to the field of preparation and application of medicines, and particularly relates to a patch for skin anesthesia and a preparation method thereof.
Background
With the development of society, people's demand for painless treatment in clinical medical practice is gradually increasing. For many medical cosmetology and treatment operations (laser, freezing, needle roller and the like) in dermatology, a considerable part of the operations are accompanied with certain pain feeling, so that the fear of patients on treatment is caused, and the coordination and the enthusiasm of the treatment are influenced.
At present, the method for solving the problem mainly takes oral analgesic, local injection anesthetic infiltration anesthesia and application of compound lidocaine emulsifiable paste as main materials. The oral analgesic has a first-pass effect and a slow action effect; there is a significant pain associated with injection anesthesia, and some large area treatments are not suitable for injection. The most commonly used lidocaine emulsifiable paste needs to be smeared to a certain thickness, and meanwhile, the lidocaine emulsifiable paste needs to be covered by a film for use, the smearing amount cannot be accurately controlled in the actual operation process, the smearing uniformity degree is related to the personal operation level, the anesthesia effect cannot be achieved due to too little smearing or the size and time of the anesthesia effect are not enough, the risk of causing allergy is easily wasted or increased due to too much smearing, and the workload, time and difficulty of the operation are increased. The existing product can not meet the requirement of people on pain reduction in use convenience and effectiveness, so that the development of the anesthesia application for local skin use, which has short onset time, long drug effect time, strong anesthesia and analgesia depth and convenient and stable operation, has wide clinical application value.
the patent CN100443078C discloses a gel for local anesthesia and analgesia on the surface of a skin and application thereof, wherein tetracaine base or lidocaine is adopted as a local anesthetic drug, the concentration is 2.5 ~ 7.5%, carbomer and CMC are simultaneously used as thickening agents, 2 ~ 8% menthol is used as a penetration enhancer, triethanolamine and NaOH are used as pH regulators, the pH value of the product is 6 ~ 11, the product protected by the technical characteristics described in the patent CN100443078C is the same as a cream product in the using process, the product still needs to be coated to a certain thickness and covered by a covering film for use, the using amount of the product needs to be controlled by anesthesia operators, the anesthesia operation is dependent on personal experience and operation level, the drug effect is uneven and unstable, the operation is complicated, and the experience in the anesthesia process is poor.
Disclosure of Invention
Aiming at the problems in the prior art, the invention aims to provide a patch for skin anesthesia and a preparation method thereof. The patch for skin anesthesia has the advantages of stable dosage, easy operation, short onset time, long drug effect time and strong anesthesia and analgesia depth.
The purpose of the invention is realized by the following technical scheme:
The invention provides a patch for skin anesthesia, which comprises the following components in parts by weight: 2-15 parts of film forming material, 0.5-1 part of thickening agent, 5-10 parts of anesthetic, 17-68 parts of transdermal absorbent, 0.1-0.8 part of bacteriostatic agent and 36-67 parts of water.
Preferably, the components of the patch for skin anesthesia comprise, by weight: 5-12 parts of film forming material, 0.8-1 part of thickening agent, 7-9 parts of anesthetic, 27-48 parts of transdermal absorbent, 0.3-0.6 part of bacteriostatic agent and 46-57 parts of water.
Preferably, the patch for skin anesthesia is in the shape of a sticker.
Preferably, the shape of the skin anesthetic dressing is a shape that conforms to the contour of the face.
Preferably, the film-forming material is selected from polyvinyl alcohol.
Preferably, the thickener is selected from hydroxymethylcellulose.
Preferably, the anesthetic is a compound of lidocaine hydrochloride and prilocaine hydrochloride, the lidocaine hydrochloride is 2.5-5 parts by weight, and the prilocaine hydrochloride is 2.5-5 parts by weight.
More preferably, the lidocaine hydrochloride is 3-4 parts by weight, and the prilocaine hydrochloride is 3-4 parts by weight.
Preferably, the transdermal absorbent is selected from one or more of propylene glycol, ethanol, menthol, azone, dimethyl isosorbide and inositol.
Preferably, the transdermal absorbent is selected from propylene glycol, ethanol and menthol, wherein the propylene glycol is 10-30 parts by weight, the ethanol is 5-20 parts by weight, and the menthol is 2-15 parts by weight.
Preferably, the bacteriostatic agent is one or two of methyl p-hydroxybenzoate, phenoxyethanol, ethyl hydroxybenzoate, sorbic acid or cymene; the weight parts of the methyl p-hydroxybenzoate, the phenoxyethanol and the ethyl hydroxybenzoate are respectively 0.1-0.3 part, 0.2-0.5 part, 0-0.5 part and 0-0.5 part, respectively, and the weight parts of the sorbic acid and the cymene are respectively 0-0.5 part and 0-0.5 part.
In another aspect of the present invention, a method for preparing the patch for skin anesthesia is provided, which comprises the following steps:
the preparation method comprises the steps of uniformly mixing water and a transdermal absorbent to obtain a solvent phase, dispersing a thickening agent and a film forming material in the solvent phase under the condition of stirring at the rotating speed of 300rpm ~ 1500rpm, uniformly stirring to form a gel matrix, adding an anesthetic and a bacteriostatic agent into the gel matrix under the condition of stirring, uniformly stirring to obtain a gel, pouring the gel into a sticking mold, freezing for 4 hours at rpm ~ 10 to rpm ~ 20 ℃, unfreezing for 4 hours at 20 rpm ~ 25 ℃, and forming the skin anesthesia plaster after 2 rpm ~ 3 rounds of freeze thawing.
Preferably, the transdermal absorbent is selected from propylene glycol, ethanol and menthol, wherein the propylene glycol is 10-30 parts by weight, the ethanol is 5-20 parts by weight, and the menthol is 2-15 parts by weight.
Preferably, the thickening agent is selected from hydroxymethyl cellulose, and the weight part of the hydroxymethyl cellulose is 0.5-1 part.
Preferably, the film forming material is selected from polyvinyl alcohol, and the weight part of the polyvinyl alcohol is 2-15 parts.
Preferably, the anesthetic is a compound of lidocaine hydrochloride and prilocaine hydrochloride, the lidocaine hydrochloride is 2.5-5 parts by weight, and the prilocaine hydrochloride is 2.5-5 parts by weight.
Preferably, the bacteriostatic agent is one or two of methyl p-hydroxybenzoate, phenoxyethanol, ethyl hydroxybenzoate, sorbic acid or cymene; the weight parts of the methyl p-hydroxybenzoate, the ethyl hydroxybenzoate and the sorbic acid are respectively 0.1-0.3, 0.2-0.5, 0-0.5 and 0-0.5, and 0-0.5.
Preferably, the structure of the application mold comprises a base and an application forming cavity arranged on the base, and the application forming cavity is provided with an application forming surface.
Preferably, the applicator shaping surface is contoured to a facial contour curve.
Preferably, the applicator shaping surface is configured to be a flat surface formed by the spread of the facial contour.
Preferably, the application molding cavity is provided with a convex portion including an eye convex portion, a mouth convex portion and a nose convex portion.
Preferably, the cross section of the eye convex part is in an eyebrow shape, the cross section of the mouth convex part is in a straight shape, and the cross section of the nose convex part is in a U shape.
Compared with the prior art, the invention has the beneficial effects that:
The high-molecular film forming material and the patch for skin anesthesia prepared by the freeze thawing process are in a transparent adhesive plaster shape, all parts of the adhesive plaster are tightly connected to form a complete whole, the patch is convenient to use, has certain tensile strength, stable usage amount and consistent skin local uniformity, and can quantitatively and effectively permeate, the product has better sealing property, the product permeation is promoted, and the anesthesia effect is ensured.
The patch for skin anesthesia provided by the invention realizes anesthesia by adopting a compound formula of lidocaine hydrochloride and prilocaine hydrochloride, has a strong and lasting local anesthesia effect, helps anesthetic permeation by adding a transdermal absorbent, and has good surface penetrating power.
Drawings
FIG. 1 is a schematic structural view of an application mold according to the present embodiment;
FIG. 2 is a graph showing the results of the anesthesia test performed in this example.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
the following description is given by way of example only with reference to the accompanying drawings and examples and should not be construed as limiting the scope of the invention.
The embodiment of the invention provides a patch for skin anesthesia, which comprises the following components in parts by weight: 2-15 parts of film forming material, 0.5-1 part of thickening agent, 5-10 parts of anesthetic, 17-68 parts of transdermal absorbent, 0.1-0.8 part of bacteriostatic agent and 36-67 parts of water.
In some embodiments, the weight parts of the film-forming material are 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts, or 15 parts.
In some embodiments, the weight fraction of the thickener is 0.5 parts, 0.6 parts, 0.7 parts, 0.8 parts, 0.9 parts, or 1 part.
In some embodiments, the anesthetic is 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, or 10 parts by weight.
In some embodiments, the transdermal absorbent is present in an amount of 17 parts, 18 parts, 19 parts, 20 parts, 21 parts, 22 parts, 23 parts, 24 parts, 25 parts, 26 parts, 27 parts, 28 parts, 29 parts, 30 parts, 31 parts, 32 parts, 33 parts, 34 parts, 35 parts, 36 parts, 37 parts, 38 parts, 39 parts, 40 parts, 41 parts, 42 parts, 43 parts, 44 parts, 45 parts, 46 parts, 47 parts, 48 parts, 49 parts, 50 parts, 51 parts, 52 parts, 53 parts, 54 parts, 55 parts, 56 parts, 57 parts, 58 parts, 59 parts, 60 parts, 61 parts, 62 parts, 63 parts, 64 parts, 65 parts, 66 parts, 67 parts, or 68 parts by weight.
In some embodiments, the bacteriostatic agent is 0.1 part, 0.2 part, 0.3 part, 0.4 part, 0.5 part, 0.6 part, 0.7 part, or 0.8 part by weight.
In some embodiments, the water is present in an amount of 36 parts, 37 parts, 38 parts, 39 parts, 40 parts, 41 parts, 42 parts, 43 parts, 44 parts, 45 parts, 46 parts, 48 parts, 50 parts, 52 parts, 55 parts, 57 parts, 58 parts, 59 parts, 60 parts, 62 parts, 63 parts, 64 parts, 65 parts, 66 parts, or 67 parts by weight.
In this embodiment, the patch for skin anesthesia is in the shape of a sticker, which is rectangular, circular, oval or other desired shape.
In a preferred embodiment of the present invention, the shape of the patch for skin anesthesia is a shape that conforms to the contour of the face.
in this embodiment, the film-forming material is selected from polyvinyl alcohol.
In this embodiment, the thickener is selected from hydroxymethyl cellulose.
In the invention, the anesthetic is a compound of lidocaine hydrochloride and prilocaine hydrochloride. In some embodiments, the lidocaine hydrochloride is present in an amount of 2.5 parts, 2.6 parts, 2.7 parts, 2.8 parts, 2.9 parts, 3 parts, 3.1 parts, 3.2 parts, 3.3 parts, 3.4 parts, 3.5 parts, 3.6 parts, 3.8 parts, 3.9 parts, 4 parts, 4.1 parts, 4.2 parts, 4.3 parts, 4.4 parts, 4.5 parts, 4.6 parts, 4.7 parts, 4.8 parts, 4.9 parts, or 5 parts by weight.
In some embodiments, the prilocaine hydrochloride is in a weight part of 2.5, 2.6, 2.7, 2.8, 2.9, 3, 3.1, 3.2, 3.3, 3.4, 3.5, 3.6, 3.8, 3.9, 4, 4.1, 4.2, 4.3, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9, or 5 parts.
In this embodiment, the transdermal absorbent is selected from one or more of propylene glycol, ethanol, menthol, azone, dimethyl isosorbide, and inositol.
In a preferred embodiment of the present invention, the transdermal absorption agent is selected from the group consisting of propylene glycol, ethanol and menthol. In some embodiments, the propylene glycol is 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 23, 25, 28, or 30 parts by weight, the ethanol is 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20 parts by weight, and the menthol is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or 15 parts by weight.
In the embodiment, the bacteriostatic agent is one or two of methyl p-hydroxybenzoate, phenoxyethanol, ethyl hydroxybenzoate, sorbic acid or cymene; in some embodiments, the weight parts of methyl paraben is 0.1, 0.2 or 0.3, the weight parts of phenoxyethanol is 0.2, 0.3, 0.4 or 0.5, the weight parts of ethyl hydroxybenzoate is 0, 0.1, 0.2, 0.3, 0.4 or 0.5, the weight parts of sorbic acid is 0, 0.1, 0.2, 0.3, 0.4 or 0.5, and the weight parts of cymene is 0, 0.1, 0.2, 0.3, 0.4 or 0.5.
In another aspect of the present invention, a method for preparing the patch for skin anesthesia is provided, which comprises the following steps:
the preparation method comprises the steps of uniformly mixing water and a transdermal absorbent to obtain a solvent phase, dispersing a thickening agent and a film forming material in the solvent phase under the condition of stirring at the rotating speed of 300rpm ~ 1500rpm, uniformly stirring to form a gel matrix, adding an anesthetic and a bacteriostatic agent into the gel matrix under the condition of stirring, uniformly stirring to obtain a gel, pouring the gel into a sticking mold, freezing for 4 hours at rpm ~ 10 to rpm ~ 20 ℃, unfreezing for 4 hours at 20 rpm ~ 25 ℃, and forming the skin anesthesia plaster after 2 rpm ~ 3 rounds of freeze thawing.
In the above method, the transdermal absorbent is selected from propylene glycol, ethanol and menthol, the propylene glycol is 10 parts, 11 parts, 12 parts, 13 parts, 14 parts, 15 parts, 16 parts, 17 parts, 18 parts, 19 parts, 20 parts, 21 parts, 22 parts, 23 parts, 24 parts, 25 parts, 26 parts, 27 parts, 28 parts, 29 parts or 30 parts by weight, the ethanol is 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts, 15 parts, 16 parts, 17 parts, 18 parts, 19 parts or 20 parts by weight, and the menthol is 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts or 15 parts by weight in some embodiments.
In the method, the thickening agent is selected from hydroxymethyl cellulose, and the weight part of the hydroxymethyl cellulose is 0.5 part, 0.6 part, 0.7 part, 0.8 part, 0.9 part or 1 part.
In the method, the film forming material is selected from polyvinyl alcohol, and the weight parts of the polyvinyl alcohol are 2 parts, 3 parts, 4 parts, 5 parts, 6 parts, 7 parts, 8 parts, 9 parts, 10 parts, 11 parts, 12 parts, 13 parts, 14 parts or 15 parts.
In the method, the anesthetic is a compound of lidocaine hydrochloride and prilocaine hydrochloride, and the lidocaine hydrochloride is 2.5 parts, 2.6 parts, 2.7 parts, 2.8 parts, 2.9 parts, 3 parts, 3.1 parts, 3.2 parts, 3.3 parts, 3.4 parts, 3.5 parts, 3.6 parts, 3.8 parts, 3.9 parts, 4 parts, 4.1 parts, 4.2 parts, 4.3 parts, 4.4 parts, 4.5 parts, 4.6 parts, 4.7 parts, 4.8 parts, 4.9 parts or 5 parts by weight.
In some embodiments, the prilocaine hydrochloride is in a weight part of 2.5, 2.6, 2.7, 2.8, 2.9, 3, 3.1, 3.2, 3.3, 3.4, 3.5, 3.6, 3.8, 3.9, 4, 4.1, 4.2, 4.3, 4.4, 4.5, 4.6, 4.7, 4.8, 4.9, or 5 parts.
In the method, the bacteriostatic agent is one or two of methyl p-hydroxybenzoate, phenoxyethanol, ethyl hydroxybenzoate, sorbic acid and cymene; in some embodiments, the parts by weight of methyl paraben is 0.1, 0.2 or 0.3, the parts by weight of phenoxyethanol is 0.2, 0.3, 0.4 or 0.5, the parts by weight of ethyl hydroxybenzoate is 0, 0.1, 0.2, 0.3, 0.4 or 0.5, the parts by weight of sorbic acid is 0, 0.1, 0.2, 0.3, 0.4 or 0.5, and the parts by weight of cymene is 0, 0.1, 0.2, 0.3, 0.4 or 0.5.
In this embodiment, the structure of the application mold comprises a base and an application molding cavity arranged on the base, wherein the application molding cavity is provided with an application molding surface.
In some embodiments, the applicator shaping surface is contoured to a facial contour curve.
in some embodiments, the applicator shaping surface is configured to be flat after the facial contour is unfolded.
In some embodiments, the application molding cavity is provided with a raised portion including an eye raised portion, a mouth raised portion and a nose raised portion.
In some embodiments, the eye-nose protrusion has a brow-shaped cross-section, the mouth-nose protrusion has a straight-line-shaped cross-section, and the nose-nose protrusion has a U-shaped cross-section.
the technical solution of the present invention will be exemplarily described below with reference to specific embodiments.
Example 1
The embodiment provides a patch for skin anesthesia, which is prepared from the following components in parts by weight: 2 parts of polyvinyl alcohol, 0.6 part of hydroxymethyl cellulose, 3 parts of lidocaine hydrochloride, 3 parts of prilocaine hydrochloride, 7 parts of ethanol, 15 parts of propylene glycol, 10 parts of menthol, 0.5 part of methyl p-hydroxybenzoate, 0.3 part of phenoxyethanol and 36 parts of water.
Example 2
the embodiment provides a patch for skin anesthesia, which is prepared from the following components in parts by weight: 12 parts of polyvinyl alcohol, 0.7 part of hydroxymethyl cellulose, 3.5 parts of lidocaine hydrochloride, 3.5 parts of prilocaine hydrochloride, 15 parts of ethanol, 25 parts of propylene glycol, 15 parts of menthol, 0.7 part of methyl p-hydroxybenzoate, 0.4 part of phenoxyethanol and 67 parts of water.
Example 3
The embodiment provides a patch for skin anesthesia, which is prepared from the following components in parts by weight: 9 parts of polyvinyl alcohol, 1 part of hydroxymethyl cellulose, 4 parts of lidocaine hydrochloride, 2.5 parts of prilocaine hydrochloride, 5 parts of ethanol, 30 parts of propylene glycol, 8 parts of menthol, 0.8 part of methyl p-hydroxybenzoate, 0.2 part of phenoxyethanol and 42 parts of water.
Example 4
The embodiment provides a patch for skin anesthesia, which is prepared from the following components in parts by weight: 15 parts of polyvinyl alcohol, 0.3 part of hydroxymethyl cellulose, 2.5 parts of lidocaine hydrochloride, 4 parts of prilocaine hydrochloride, 20 parts of ethanol, 10 parts of propylene glycol, 2 parts of menthol, 0.3 part of methyl p-hydroxybenzoate, 0.1 part of phenoxyethanol and 44 parts of water.
example 5
The embodiment provides a patch for skin anesthesia, which is prepared from the following components in parts by weight: 5 parts of polyvinyl alcohol, 0.1 part of hydroxymethyl cellulose, 5 parts of lidocaine hydrochloride, 5 parts of prilocaine hydrochloride, 10 parts of ethanol, 20 parts of propylene glycol, 5 parts of menthol, 0.1 part of methyl p-hydroxybenzoate, 0.5 part of phenoxyethanol and 49 parts of water.
Example 6
This example provides the preparation method of the patch for skin anesthesia described in examples 1 to 5, which was prepared according to the following steps, respectively, in accordance with the amounts of the respective components in examples 1 to 5:
Weighing water, ethanol, propylene glycol and menthol, and mixing uniformly to obtain a solvent phase;
dispersing hydroxymethyl cellulose in a solvent under the condition of stirring at the rotating speed of 300-1500 rpm, uniformly stirring to form gel, adding lidocaine hydrochloride, prilocaine hydrochloride, methyl p-hydroxybenzoate and phenoxyethanol into a gel matrix under the condition of stirring, and continuously stirring and uniformly mixing.
pouring the uniformly stirred gel into a sticking mould, freezing for 4h at-10 ~ -20 ℃, thawing for 4h at 20-25 ℃, and performing freeze thawing for 2-3 rounds ~ form the anesthetic sticking product.
Referring to fig. 1, the structure of the application mold of the present embodiment includes a base 10 and an application molding cavity 20 provided on the base, the application molding cavity 20 having an application molding surface. The application molding surface is structured as a plane formed by the spread of the facial contour. The application molding cavity is provided with bosses including an eye boss 21, a mouth boss 22, and a nose boss 23. The cross-sectional shape of the eye convex part 21 is an eyebrow shape, the cross-sectional shape of the mouth convex part 22 is a line shape, the cross-sectional shape of the nose convex part 23 is a U shape,
Effect verification:
the results of examples 1, 3 and 5 were compared by taking the commercial product corresponding to the technical scheme disclosed in patent CN100443078C as a control example. And (3) scoring by adopting a visual simulation scoring method, specifically adopting a horizontal line segment which is 10cm and ten times, wherein the two ends are respectively 0 and 10,0 is painless, and 10 is severe pain. The corresponding site of pain was subjectively evaluated by the subject, and then the anesthetic effect was evaluated based on the value of pain (cm), less than 5cm being an acceptable anesthetic analgesic effect. Examples 1, 3 and 5 show that the application for skin anesthesia provided by the invention produces an acceptable anesthesia effect at 40min, the duration of the anesthesia effect is 3.3h, while the control group produces an acceptable starvation anesthesia effect at 80min, the duration of the anesthesia effect is 2h, and the effect verification curve is shown in fig. 2. As can be seen from FIG. 2, the anesthetic effect of the embodiment of the present invention is significantly better than that of the control group.
The above examples and embodiments are only for assisting understanding of the technical solutions of the present invention, and should not be taken as a basis for limiting the scope of the present invention. Modifications and substitutions by one skilled in the art without making any creative effort on the basis of the present invention fall into the protection scope of the present invention.

Claims (10)

1. The patch for skin anesthesia is characterized by being prepared from the following components in parts by weight: 2-15 parts of film forming material, 0.5-1 part of thickening agent, 5-10 parts of anesthetic, 17-68 parts of transdermal absorbent, 0.1-0.8 part of bacteriostatic agent and 36-67 parts of water.
2. The patch for skin anesthesia of claim 1, wherein the patch for skin anesthesia is in the shape of a sticker.
3. The patch for skin anesthesia of claim 1, wherein the shape of the patch for skin anesthesia is a shape that conforms to the contour of the face.
4. A patch for skin anesthesia as defined in claim 1, wherein said film-forming material is selected from polyvinyl alcohol.
5. A patch for cutaneous anaesthesia according to claim 1, characterised in that the thickening agent is selected from hydroxymethylcellulose.
6. The patch as claimed in claim 1, wherein the anesthetic is a combination of lidocaine hydrochloride and prilocaine hydrochloride, the lidocaine hydrochloride is 2.5-5 parts by weight, and the prilocaine hydrochloride is 2.5-5 parts by weight.
7. the patch for skin anesthesia of claim 1, wherein the transdermal absorbent is one or more selected from the group consisting of propylene glycol, ethanol, menthol, azone, dimethyl isosorbide, and inositol.
8. The patch according to claim 5, wherein the transdermal absorbent is selected from the group consisting of propylene glycol, ethanol and menthol, wherein the propylene glycol is present in an amount of 10 to 30 parts by weight, the ethanol is present in an amount of 5 to 20 parts by weight, and the menthol is present in an amount of 2 to 15 parts by weight.
9. the patch for skin anesthesia of claim 1, wherein said bacteriostatic agent is selected from one or two of methylparaben, phenoxyethanol, ethylhydroxybenzoate, sorbic acid or cymene; the weight parts of the methyl p-hydroxybenzoate, the phenoxyethanol and the ethyl hydroxybenzoate are respectively 0.1-0.3 part, 0.2-0.5 part, 0-0.5 part and 0-0.5 part, respectively, and the weight parts of the sorbic acid and the cymene are respectively 0-0.5 part and 0-0.5 part.
10. a method of producing a patch for skin anesthesia as set forth in any one of claims 1 to 7, characterized by comprising the steps of:
the preparation method comprises the steps of uniformly mixing water and a transdermal absorbent to obtain a solvent phase, dispersing a thickening agent and a film forming material in the solvent phase under the condition of stirring at the rotating speed of 300rpm ~ 1500rpm, uniformly stirring to form a gel matrix, adding an anesthetic and a bacteriostatic agent into the gel matrix under the condition of stirring, uniformly stirring to obtain a gel, pouring the gel into a sticking mold, freezing for 4 hours at rpm ~ 10 to rpm ~ 20 ℃, thawing for 4 hours at 25 ℃, and performing freeze thawing for 2 rpm ~ 3 times to form the skin anesthesia sticking patch.
CN201910788397.8A 2019-08-26 2019-08-26 Application for skin anesthesia and preparation method thereof Pending CN110559275A (en)

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