WO2018124572A1 - 실리콘 수지 조성물, 이의 제조방법 및 이를 포함하는 흉터 치료제 - Google Patents

실리콘 수지 조성물, 이의 제조방법 및 이를 포함하는 흉터 치료제 Download PDF

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WO2018124572A1
WO2018124572A1 PCT/KR2017/014888 KR2017014888W WO2018124572A1 WO 2018124572 A1 WO2018124572 A1 WO 2018124572A1 KR 2017014888 W KR2017014888 W KR 2017014888W WO 2018124572 A1 WO2018124572 A1 WO 2018124572A1
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weight
silicone resin
resin composition
scar
silicone
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PCT/KR2017/014888
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English (en)
French (fr)
Korean (ko)
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박일규
김현정
강휘주
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주식회사 제네웰
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Priority to JP2019554461A priority Critical patent/JP6821054B2/ja
Priority to CN201780081658.1A priority patent/CN110121368A/zh
Publication of WO2018124572A1 publication Critical patent/WO2018124572A1/ko

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L26/00Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form
    • A61L26/0009Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form containing macromolecular materials
    • A61L26/0052Mixtures of macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/88Liliopsida (monocotyledons)
    • A61K36/896Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • A61K36/8962Allium, e.g. garden onion, leek, garlic or chives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7015Drug-containing film-forming compositions, e.g. spray-on
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L26/00Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L26/00Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form
    • A61L26/0009Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form containing macromolecular materials
    • A61L26/0019Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form containing macromolecular materials obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L26/00Chemical aspects of, or use of materials for, wound dressings or bandages in liquid, gel or powder form
    • A61L26/0061Use of materials characterised by their function or physical properties
    • A61L26/0066Medicaments; Biocides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/20Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices containing or releasing organic materials
    • A61L2300/22Lipids, fatty acids, e.g. prostaglandins, oils, fats, waxes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/40Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
    • A61L2300/41Anti-inflammatory agents, e.g. NSAIDs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/40Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
    • A61L2300/428Vitamins, e.g. tocopherol, riboflavin

Definitions

  • the present invention relates to a silicone resin composition, a method for preparing the same, and a scar treatment agent including the same. More particularly, the use of a biocompatible raw material harmless to the human body is safe, smooth, and non-sticky, and is quick and dry. It forms a film to protect scars and creates a moisture environment, and is effective in preventing and improving scar erythema and pigmentation due to UV protection and anti-oxidant effect.
  • the drug and the activator In addition, the absorption of the active ingredient is improved, thereby making the scar softer and flatter than the prior art, thereby producing a synergistic effect on the prevention, treatment, and improvement of the scar. It relates to a scar treatment comprising.
  • Scar tissue usually causes the body's body to initiate an accurate and rapid wound healing response when the skin or dermis is cut or burned, causing damaged tissue to be part of the reconstruction or repair process. However, if the reconstruction or repair process is poorly controlled, even the normal healing process may cause excessive scarring and pain.
  • Scars are different from the surrounding skin in the color, roughness or softness of the skin, causing severe mental stress when they appear in the appearance area, and the scars in the areas where stretching is caused to damage the skin tissue again. This results in treatment time, and consequent shrinkage of surrounding tissues causes great inconvenience in life.
  • the present invention is safe, smooth, and non-sticky with the use of biocompatible raw materials harmless to the human body, and convenient to dry quickly, forming a thin silicone film to form a scar protection and moisture environment
  • it is effective in preventing and improving erythema and pigmentation of scars by sun protection and anti-oxidation effect, and the absorption of drugs and activators, that is, active ingredients, is improved due to high occlusive property and skin softening.
  • the purpose of the present invention is to provide a silicone resin composition having excellent flexibility, waterproofness, and moisturizing property, a method of manufacturing the same, and a scar treating agent including the same, in which a synergistic effect is generated in the prevention, treatment, and improvement of the scar by softening and flattening the contrast scar. do.
  • the present invention is a) 5 to 70% by weight of silicone resin, b) 0 to 40% by weight of wax, c) 1 to 15% by weight of emulsifier, d) 0.01 to 10% by weight of drug, e) 0.01 to 10% by weight of activator, f) 0 to 30% by weight of sunscreen, g) 0 to 5% by weight of antioxidant, h) 0 to 80% by weight of water and i) 0.1 to 5% by weight of preservative
  • a silicone resin composition is provided.
  • the present invention is A) 5 to 70% by weight of the silicone resin, 0 to 40% by weight of the wax, 1 to 15% by weight of the emulsifier and 0 to 30% by weight of the sunscreen under stirring at 60 to 80 °C mixing; And B) 0.01 to 10% by weight of drug, 0.01 to 10% by weight of activator, 0 to 5% by weight of antioxidant, 0 to 80% by weight of water and 0.1 to 5% by weight of preservative, and 45 to It provides a method for producing a silicone resin composition comprising a; mixing by stirring under 70 °C.
  • the present invention provides a scar treatment agent comprising the silicone resin composition.
  • the use of biocompatible raw materials that are harmless to the human body is safe, smooth, and non-sticky, convenient, and quickly dried to form a thin silicon film to protect scars and create a moisture environment, and to protect the scars by UV protection and antioxidant efficacy. It is effective in preventing and improving erythema and pigmentation, and the high occlusive property and skin softening improve the absorption of drugs and activators, i.e. active ingredients, making the scars softer and flatter than the prior art. Synergistic effect is generated in the treatment and improvement, and in addition, there is an effect of providing a silicone resin composition having excellent flexibility, waterproofness, and moisturizing property, a method for preparing the same, and a scar treatment agent including the same.
  • FIG. 2 is applied to the four scars of the test subjects prepared in FIG. 1 for histology analysis, respectively, twice a day for 4 weeks with a silicone resin composition prepared in Example 4 and a commercially available scar drug. Next, Masson's trichrome staining method was used for microscopic examination.
  • the present inventors add drugs and activators to a silicone resin mixture consisting of silicone resins, waxes and emulsifiers of a predetermined composition ratio, and optionally apply a silicone resin composition containing a sunscreen, antioxidant, water, and / or a preservative to the scar. When applied, it rapidly dries to form a thin silicon film (high occlusive property) to provide adequate light pressure while creating scar protection and rehydration, which results in capillary permeability and collagen deposition.
  • the silicone resin composition of the present invention comprises a) 5 to 70% by weight of silicone resin, b) 0 to 40% by weight of wax, c) 1 to 15% by weight of emulsifier, d) 0.01 to 10% by weight of drug, e) 0.01 to activator. 10 weight percent, f) 0-30 weight percent sunscreen, g) 0-5 weight percent antioxidant, h) 0-80 weight percent water and i) 0.1-5 weight percent preservative.
  • the silicone resin composition of the present invention comprises a) 5 to 70 weight percent of silicone resin, b) 1 to 40 weight percent of wax, c) 1 to 15 weight percent of emulsifier, d) 0.01 to 10 weight percent of drug, e A) 0.01 to 10% by weight of activator, f) 0 to 30% by weight of sunscreen, g) 0 to 5% by weight of antioxidant, h) 0 to 80% by weight of water and i) 0.1 to 5% by weight of preservative It is characterized by.
  • the silicone resin composition of the present invention comprises a) 15 to 70 weight percent of silicone resin, b) 1 to 40 weight percent of wax, c) 1 to 15 weight percent of emulsifier, d) 0.1 to 10 weight percent of drug, e A) 0.5 to 10 weight percent activator, f) 0 to 30 weight percent sunscreen, g) 0 to 5 weight percent antioxidant, h) 0 to 80 weight percent water and i) 0.1 to 5 weight percent preservative. It is characterized by.
  • the silicone resin may be at least three kinds selected from the group consisting of silicone elastomers, film formers, silicone fluids and cyclic siloxanes, for example, in this case is a biocompatible raw material that is harmless to the human body and is safe and smooth without stickiness. In addition, it forms a thin silicon film as it dries quickly, thereby protecting scars and creating a moisture environment.
  • the a) silicone resin is, for example, a mixture of 2 to 75 wt% of silicone elastomer, 0.5 to 20 wt% of film former, 0.5 to 45 wt% of silicone fluid, and 0 to 80 wt% of cyclic siloxane, based on 100 wt% of the silicone resin. It can be, within this range is a biocompatible raw material harmless to the human body, safe, smooth and non-sticky, convenient, fast drying thin silicone film to form a scar protection and moisture effect is effective.
  • the a) the silicone resin is 5 to 50% by weight of the silicone elastomer, 2 to 10% by weight of the film former, 2 to 40% by weight of the silicone fluid and 0.1 to 65% by weight of the cyclic siloxane based on 100% by weight of the silicone resin It can be a blend of%, within this range is a biocompatible raw material harmless to the human body, safe, smooth and non-sticky, convenient, fast drying, thin silicone film to form a scar protection and moisture effect.
  • the a) the silicone resin is 10 to 50% by weight of the silicone elastomer, 2 to 10% by weight of the film former, 2 to 40% by weight of the silicone fluid and 5 to 65% by weight of the cyclic siloxane relative to 100% by weight of the silicone resin It can be a blend of%, within this range is a biocompatible raw material harmless to the human body, safe, smooth and non-sticky, convenient, fast drying, thin silicone film to form a scar protection and moisture effect.
  • the silicone elastomer may be, for example, a crosslinked silicone polymer having a weight average molecular weight of 100,000 g / mol or more, or 100,000 to 10,000,000 g / mol.
  • the silicone elastomer may be a crosslinked dimethicone or dimethicone derivative, stearyl methyl-dimethyl siloxane copolymer, polysilicon-11, cetearyl dimethicone-vinyl dimethicone crosspolymer, dimethicone-phenyl vinyl dimethicone It may be at least one selected from the group consisting of a crosspolymer and a dimethicone-vinyl dimethicone crosspolymer.
  • the weight average molecular weight may be measured by gel permeation chromatography.
  • the silicone fluid may be, for example, a nonvolatile silicone fluid, preferably a nonvolatile silicone oil, and specifically using Ubelode (manufactured by Fisher Scientific Co.), a glass capillary viscometer according to ASTM D445, IP71. It may be a volatile silicone oil having a measured viscosity at 25 ° C. of 2 to 105,000 cts, 4 to 95,000 cts, 1,000 to 14,000 cts, or 11,000 to 14,000 cts, and has excellent effects in durability and ease of application within this range.
  • the silicone fluid may be a silicone fluid 1 having a viscosity of 1 to 20 cst or 1 to 10 cst, a silicone fluid 2 of 10,000 to 15,000 cst or 11,000 to 14,000 cst, and 80,000 to 120,000 cst or 90,000 to It may be at least one selected from the group consisting of 110,000 cst of silicone fluid (3), preferably 10,000 to 15,000 cst or 11,000 to 14,000 cst of silicone fluid (2), and 80,000 to 120,000 cst or 90,000 to 110,000 cst of silicone A mixture of the fluid 3, most preferably a mixture of the silicone fluid 1 having a viscosity of 1 to 20 cst or 1 to 10 cst and a silicone fluid 3 of 80,000 to 120,000 cst or 90,000 to 110,000 cst In this case, the touch is good, and there is an effect excellent in durability and ease of application.
  • the weight ratio of the silicone fluid 1 and the silicone fluid 3 may be, for example, 1: 0.1 to 0.9, 1: 0.1 to 0.5, or 1: 0.15 to 0.4, the feel is good within this range, durability and application Ease of excellence has an effect.
  • the weight ratio of the silicone fluid 2 and the silicone fluid 3 may be, for example, 1: 1 to 5 or 1: 1.5 to 2.5, and a good feel within this range, and excellent durability and ease of application. .
  • the silicone fluid may be a linear silicone polymer, and in particular, at least one selected from the group consisting of a linear dimethicone polymer, a linear polydimethylsiloxane polymer, a polymethylethylsiloxane, and a polymethiphenylsiloxane, in which case It is effective in durability and ease of application.
  • the film forming agent may be, for example, one of various film forming silicone resins known in the art, and may be, for example, an MQ type silicone resin, a T type silicone resin, or a mixture thereof, and specific examples include trimethylsiloxysilicate, Cyclopentasiloxane, propyl silsesquioxane resin, and silsesquioxane may be one or more selected from the group consisting of, in this case, to improve the fluidity and feel of the silicone resin composition, and improve the dispersion of other additives such as drugs It works.
  • the film-forming agent has a viscosity at 25 ° C. measured using Ubelode (manufactured by Fisher Scientific Co., Ltd.) which is a glass capillary viscometer according to ASTM D445, IP71, for example, 200 to 2,000 cst, 300 to 1,500 cst, Or 400 to 1,000 cst, the flowability and feel of the silicone resin composition is good within this range, and there is an effect of improving the dispersion of other additives such as drugs.
  • Ubelode manufactured by Fisher Scientific Co., Ltd.
  • the cyclic siloxane is not particularly limited in the case of cyclic siloxanes commonly used in the art, and may be, for example, a hypermethylated cyclic siloxane, and specific examples include cyclotetrasiloxane, decamethylcyclopentasiloxane, etc., such as octamethylcyclotetrasiloxane. It may be one or more selected from the group consisting of cyclohexasiloxane, such as cyclopentasiloxane and dodecamethylcyclohexasiloxane.
  • the silicone resin may be, for example, 15 to 65% by weight, 20 to 65% by weight, 15 to 40% by weight, 15 to 30% by weight, or 15 to 25% by weight, the living body harmless to the human body within this range It is safe, smooth, and non-sticky as a suitable raw material. It is convenient to dry and forms a thin silicon film that dries quickly, protecting scars and creating a moisture environment.
  • the wax may be, for example, at least one selected from the group consisting of bees wax, paraffin, sorbitan olivate, and silicone wax, in which case it is effective to improve the stability and spreadability of the formulation.
  • the wax may be, for example, 1 to 30% by weight, 1 to 25% by weight, 1 to 15% by weight, 3 to 10% by weight, 4 to 8% by weight, or 5 to 7% by weight, within this range. It has the effect of improving the stability and spreadability of the formulation.
  • the emulsifier may be at least one selected from the group consisting of fatty alcohols having 15 to 26 carbon atoms and silicone emulsifiers, in which case the natural emulsification effect is excellent, but the biocompatible raw materials are harmless to the human body. It is safe, smooth and has no stickiness and has a convenient effect.
  • the emulsifier may be, for example, 1 to 10% by weight, 2 to 8% by weight, 2 to 7% by weight, or 2 to 5% by weight. It is not sticky and has a convenient effect.
  • the fatty alcohols having 15 to 26 carbon atoms may be, for example, fatty alcohols having 15 to 23 carbon atoms, or fatty alcohols having 16 to 20 carbon atoms, and preferably cetyl alcohol.
  • the silicone emulsifier is not particularly limited in the case of a silicone emulsifier commonly used in the art, for example, selected from the group consisting of a PEG-based silicone emulsifier, a branched polyglycerin-based silicone emulsifier and a crosslinked polyglycerol-based silicone emulsifier It can be 1 or more types, and in this case, the effect of keeping a silicone resin composition uniform is large.
  • the silicone emulsifier may have a viscosity of 1,000 to 5,000 cst, 1,500 to 2,500 cst, or 1,600 to 2,000 cst, and has a great effect of keeping the silicone resin composition uniform in this range.
  • the polyglycerol-based silicone emulsifier may be a cross-linked polyglycerol modified dimethicone, for example, polyglyceryl-3 disiloxane dimethicone, polyglyceryl-3 polydimethyldisiloxyethyl dimethicone, lauryl polyglycerol Reel-3 Polydimethyldisiloxyethyl Dimethicone, Dimethicone-Polyglycerin-3 Crosspolymer, Lauryl Dimethicone / Polyglycerin-3 Crosspolymer, Polyethyleneglycol-9 Polydimethylsiloxyethyldimethicone, Dimethicone Copolyol It may be at least one selected from the group consisting of, cetyl dimethicone copolyol, PG-10 dimethicone and polyethylene glycol-7 dimethicone.
  • the emulsifier may have a hydrophile-lipophile balance (HLB) of 1 to 14, and preferably 2 to 11, as measured by Griffin's method, and has a great effect of maintaining the silicone resin composition in a uniform state within this range.
  • HLB hydrophile-lipophile balance
  • the drug d) may be at least one selected from the group consisting of, for example, antioxidants, anticancer agents, anti-inflammatory agents, hormones, and calcium channel blockers, and in this case, it is particularly effective for preventing and improving erythema or pigmentation of scars due to antioxidant effects. Its rapid absorption has a synergistic effect on scar prevention, treatment and improvement.
  • the drug may be, for example, 0.1 to 5% by weight, 0.1 to 3% by weight, 0.1 to 2% by weight, 0.5 to 2% by weight, 1 to 2% by weight, or 1.5 to 2% by weight, within this range It is effective in the prevention and improvement of scar erythema and pigmentation due to the antioxidant effect, and has a synergistic effect on the scar prevention, treatment and improvement by rapid absorption.
  • the antioxidant may be, for example, an ascorbic acid derivative, in which case the antioxidant and scar healing effects are excellent.
  • the ascorbic acid derivatives are not particularly limited in the case of ascorbic acid derivatives commonly used in the art or commercially available, but may be, for example, ascorbic acid and ascorbic acid fatty acid esters thereof, acylated with single or multiple fatty acid groups, and salts thereof. Specific examples include ascorbyl laurate, ascorbyl myristate, ascorbyl palmitate, ascorbyl isopalmitate, ascorbyl-6-palmitate, ascorbyl stearate, ascorbyl behenate and their It may be at least one selected from the group consisting of metal salts, preferably ascorbyl tetraisopalmitate.
  • the anticancer agent may be, for example, 5-fluorouracil, bleomycin, or the like.
  • the anti-inflammatory agent may be, for example, dipotassium glytilytinate, allantoin, or a mixture thereof, preferably allantoin, and when used with water, may be used with a chelating agent such as disodium ethane, and in this case, anti-inflammatory Excellent effect and soothing effect.
  • the allantoin and disodium idieti may be, for example, a weight ratio of 1: 0.01 to 1: 0.5, 1: 0.05 to 1: 0.2, or 1: 0.08 to 1: 0.12, and have an anti-inflammatory effect and a soothing effect in this range. Is excellent.
  • the hormonal agent may be, for example, triamcinolone, which is effective in improving and treating scars.
  • the calcium channel blocker may be, for example, verapamil, in which case the scar healing effect is excellent.
  • the e) activator may be at least one selected from the group consisting of vitamin derivatives and onion extracts (Allium Cepa), for example, in this case, the absorption into the scar with the drug is improved, preventing, treating and improving the scars compared to the prior art. A synergy effect occurs.
  • the e) activator is for example 1 to 5% by weight, 1 to 5% by weight. It may be from 2 to 5% by weight, or from 2 to 3% by weight and within this range the absorption into the scar with the drug is improved resulting in a synergistic effect on scar prevention, treatment and improvement over the prior art.
  • Vitamin derivatives and onion extracts herein are not particularly limited in the case of vitamin derivatives that may be used in the art or are commercially available.
  • the vitamin derivative may be at least one selected from the group consisting of derivatives of vitamins A, C, D and E, for example, in this case, the absorption into the scar with the drug is improved to prevent, treat and improve the scar compared with the prior art. Synergies occur.
  • the onion extract may be, for example, an extract of dried onions containing water, alcohol or water-alcohol, and specifically, dried onions known as dried onion chips obtained from a stock plant onion at 40-90 ° C.
  • the extract solution (leach) is evaporated at an elevated temperature of 30 °C or more under reduced pressure to obtain an onion extract, and subsequently dissolved in water, alcohol or water-alcohol onion extract in liquid form Can be obtained.
  • the liquid onion extract may be, for example, 5 to 60% by weight, 10 to 50% by weight, 10 to 40% by weight, or 10 to 15% by weight of the solvent.
  • the alcohol may be at least one selected from the group consisting of ethanol, isopropanol, propanol, butylene glycol and propylene glycol, for example.
  • the weight of the onion extract is based on solids.
  • the onion extract may be prepared as follows:
  • the dried onion may be extracted with purified water, for example, at a ratio of 1:16 of the drug (dried onion) to the extraction solvent (water).
  • the ratio of dry agent to natural extract corresponds to 1.8: 1 or 1.5-2.2: 1.
  • the dry drug to liquid extract ratio is 0.16: 1.
  • Drugs eg 16 kg onion chips
  • the leachate is evaporated at 55 ° C. or higher under reduced pressure to obtain onion extract (concentrated extract).
  • the heating is performed briefly here (3 seconds at 141 ° C).
  • the resulting onion extract is a concentrated liquid, which is dissolved in water, alcohol or a water-alcohol mixture to obtain a liquid extract of the aforementioned ratio.
  • the extract is admixable with water in any ratio and has a relative density of 1.00 to 1.03 g / ml at 20 ° C. If water / alcohol (particularly ethanol) is used for the processing, approximately 13-20% (v / v) of alcohol (eg ethanol) may be present.
  • the dry residue (after 2 hours at 105 ° C.) is at least 7.0% (m / m). With regard to microbiological purity, the product meets the requirements of category 3 of German Pharmacopeia 10.
  • the f) sunscreen may be, for example, an inorganic sunscreen, an organic sunscreen, and a mixture thereof, and in this case, it is effective in preventing and improving erythema and pigmentation of scars.
  • the f) sunscreen may be, for example, 0.1 to 30% by weight, 0 to 20% by weight, 0.1 to 20% by weight, 0 to 15% by weight, or 0.1 to 15% by weight, within this range the scar erythema or It is effective in preventing and improving pigmentation.
  • the inorganic sunscreen is not particularly limited as long as it is an inorganic sunscreen commonly available in the art, but may preferably be zinc oxide, titanium oxide or a mixture thereof, preferably zinc oxide, in which case of scar It is effective in preventing and improving erythema and pigmentation.
  • the organic sunscreen is not particularly limited in the case of an organic sunscreen commonly used in the art, but preferably at least one selected from the group consisting of octinoate, octysalate, octocrylene and avobenzone, It is preferably octinoate, in which case it is effective in preventing and improving erythema and pigmentation of scars.
  • the sunscreen agent is benzophenones such as dihydroxy benzophenone, melanin, ethyl paraaminobenzoic acid, 2-dimethylhexyl ester of paradimethylaminobenzoic acid, synoxite, 2-ethylhexyl ester of paramethoxy cinnamic acid, 2 -(2-hydroxy-5-methylphenyl) benzotriazole, urokanoic acid, anthranilate, cinnamate, salicylate, derivative of dibenzoylmethane, derivative of camphor, derivative of triazine, derivative of benzophenone, derivatives of ⁇ , ⁇ '-diphenylacrylate, derivatives of benzotriazole, derivatives of benzyl malonate, derivatives of benzimidazole, imidazolines, derivatives of benzoallyl, derivatives of p-aminobenzoic acid, titanium oxide and oxidation It may be at least one selected from the group consist
  • the h) water may be, for example, 0.1 to 80% by weight, 30 to 80% by weight, 45 to 70% by weight, or 50 to 65% by weight, and sufficiently dissolve drugs, activators, antioxidants, etc. within this range. It is easy to apply, smooth and has no stickiness, and helps to form a thin silicone film that dries quickly.
  • the h) water may be, for example, purified water or distilled water.
  • the g) antioxidant may be, for example, 0.1 to 5% by weight, 0.5 to 3% by weight or 0.5 to 2% by weight, it is effective in preventing and improving erythema or pigmentation of scars within this range.
  • the antioxidant in the present disclosure is not particularly limited when the antioxidant is commonly used in the art, but may be, for example, one or more selected from the group consisting of butylhydroxyanisole, molded asset, molded asset propyl and erythorbic acid.
  • the preservative is, for example, imidazolidinyl urea (Imidazolidinyl Urea), methylparaben (Methylparaben), salicylic acid (Salicylic acid), methylchloroisothiazolinone (Methylchloroisothiazolinone), methylisodiazolinone (Methylisothiazolinone), ethyl paraben (Ethylparaben), Butylparaben, Propylparaben, Isopropylparaben, Isopropylparaben, Phenoxyethanol, DMDM Hydantoin, 1,2-hexanediol (1,2 Hexanediol), capryloylglycine, glyceryl caprylate, sodium levulinate, zinc gluconate, copper gluconate, zinc pyrrolidone carboxylic acid, copper pyrrolidone carboxylic acid, phytosphingos
  • Method for producing a silicone resin composition of the present invention is A) 5 to 70% by weight of silicone resin, 1 to 40% by weight of wax, 1 to 15% by weight of emulsifier and 0 to 30% by weight of sunscreen under stirring at 60 to 80 °C mixed Doing; And B) 0.01 to 10% by weight of drug, 0.01 to 10% by weight of activator, 0 to 5% by weight of antioxidant, 0 to 80% by weight of water and 0.1 to 5% by weight of preservative, and 45 to Mixing by stirring under 70 °C; characterized in that it comprises a.
  • steps A) and B) include all of the foregoing.
  • Mixing in the step A) may be carried out at 60 to 75 °C, 65 to 70 °C, or 63 to 67 °C.
  • the drug or a part thereof and a mixed solution made by mixing water under 50 to 75 ° C. are first introduced into the mixture made in the step A) and mixed, and then the activator, antioxidant, and Preservatives can be added, in this case, the dispersion is uniform, there is no stickiness while the silicone resin composition is gently applied to the skin is convenient to use and has the effect of improving the absorption of the active ingredient.
  • the mixed solution of step B) may be prepared by mixing the drug or part thereof with water at 60 to 70 ° C., or 63 to 67 ° C., for example.
  • the mixed solution is added to the mixture made in step A), for example, it can be maintained at 50 to 75 °C, the dispersion is uniform within this range, the silicone resin composition prepared is smoothly applied to the skin without stickiness It is convenient to use and has the effect of improving the absorption of the active ingredient.
  • the mixed solution When the mixed solution is added to the mixture in step B), for example, it may be maintained at 60 to 70 °C, or 63 to 67 °C.
  • the activator, antioxidant and preservative may be added to the mixture made in the step A) after the mixture is cooled to 45 to 55 °C, for example, the dispersion becomes uniform within this range, While the silicone resin composition is gently applied to the skin, there is no stickiness, so it is convenient to use and the absorption of the active ingredient is improved.
  • the activator, antioxidant and preservative may be added when the mixed solution is added to the mixture made in step A) and then cooled to 48 to 52 °C.
  • the scar treatment agent of the present invention is characterized in that it comprises the silicone resin composition.
  • the scar treatment agent herein is not limited to its name, and may include any case of a drug for preventing, ameliorating or treating scars, and examples thereof include scar improvers, scar inhibitors, scar drugs, and the like.
  • the scar treatment agent may be, for example, a sheet type, a cream type or a gel type, preferably a cream type or a gel type, and in this case, it is easy to apply smoothly and is non-sticky, and thus, the treatment area can be arbitrarily adjusted. Simple and economical effect is excellent.
  • the scar treatment agent may have a sun protection index (SPE) according to ISO 24444 standard, for example, 25 or more, 30 or more, or 30 to 50, without adversely affecting other physical properties of the silicone resin composition within this range. It is effective in preventing and improving erythema and pigmentation of scars by UV protection.
  • SPE sun protection index
  • the scar treatment agent may be, for example, at least 40%, at least 45%, at least 50%, or at least 50% of an antioxidant effect by the DPPH method, and if it does not adversely affect other physical properties of the silicone resin composition within this range. It is also effective in preventing and improving erythema and pigmentation of scars due to the antioxidant effect.
  • the components included in the silicone resin mixture are manufactured by Dow corning Co., Ltd. as follows.
  • TI-1050 (Various viscosity range, 95,000 ⁇ 105,000 cst product used for viscosity control)
  • 0.5 g of allantoin, 0.05 g of disodium ethane and 64.45 g of purified water were added to another reactor, and the mixture was heated and stirred to 65 ° C. Slowly pour the contents of the reactor containing purified water into the reactor containing the silicone resin at 65 and stir. When the phases are thoroughly mixed, stop heating and add 50 g of onion extract, 1 g of tocopheryl acetate, and 1 g of 1,2-hexanediol as preservative. Continue to stir until cooled.
  • 0.5 g of allantoin, 0.05 g of disodium ethane, and 51.45 g of purified water were added to another reactor, and the mixture was heated to 65 and stirred.
  • silicone emulsifier Density 1800 mm 2 / s
  • sorbitan oleate 0.1 g of verapamil, 0.5 g of allantoin, 0.05 g of disodium ethane, and 64.35 g of purified water were added thereto, and the mixture was heated and stirred to 65 ° C.
  • 0.1 g of verapamil, 0.5 g of allantoin, 0.05 g of disodium ethane, and 64.35 g of purified water were added thereto, and the mixture was heated and stirred to 65 ° C.
  • silicone emulsifier Density 1100-3500 cps or cst
  • Into another reactor 0.5 g of allantoin, 0.05 g of disodium ethane and 55.45 g of purified water were added, and the mixture was heated to 60 and stirred. After cooling the reactor containing the purified water completely, slowly pour the contents into the reactor containing the silicone resin and stir. When the phases are completely mixed, use a homogenizer to perform high speed agitation.
  • Kelo-cote Topical Gel manufactured by Formulated Solution LLC
  • Kelo-cote Solaire manufactured by Formulated Solutions LLC
  • Dermatix Ultra gel manufactured by Toshiki International Singapore Pte Ltd.
  • Bentlax gel Teguk Pharm
  • Antioxidant effect Measured by DPPH method, the higher the value, the better the antioxidant effect.
  • UV protection performance measured by human patch test according to ISO 2444.
  • Stickiness degree The sample was measured based on the touch when applied to the skin, and if there is no stickiness, +++, the normal case ++, it is marked as + if very sticky.
  • the silicone resin compositions (Examples 4 and 5) of the present invention are excellent in anti-oxidation and UV blocking performance, and smoothly applied while being sticky compared to Comparative Examples 1 to 4 corresponding to the prior art. None could be confirmed.
  • the silicone resin composition (Example 4) of the present invention significantly reduces the abnormal collagen (disorganized collagen) compared to the comparative examples 3 and 4 of the prior art, the normal collagen (normal pattern collagen) is increased maybe confirm.

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KR102285696B1 (ko) 2019-06-13 2021-08-04 신신제약 주식회사 흉터 예방 또는 치료를 위한 국소용 약학적 조성물
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