WO2017138710A1 - 경피투여용 자외선 경화형 하이드로젤 수지, 하이드로젤 및 이를 포함하는 카타플라스마제 - Google Patents
경피투여용 자외선 경화형 하이드로젤 수지, 하이드로젤 및 이를 포함하는 카타플라스마제 Download PDFInfo
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- WO2017138710A1 WO2017138710A1 PCT/KR2017/001051 KR2017001051W WO2017138710A1 WO 2017138710 A1 WO2017138710 A1 WO 2017138710A1 KR 2017001051 W KR2017001051 W KR 2017001051W WO 2017138710 A1 WO2017138710 A1 WO 2017138710A1
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- coumarin
- thioxanthone
- diacrylate
- hydrogel
- glycol
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- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/02—Making solutions, dispersions, lattices or gels by other methods than by solution, emulsion or suspension polymerisation techniques
- C08J3/03—Making solutions, dispersions, lattices or gels by other methods than by solution, emulsion or suspension polymerisation techniques in aqueous media
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- 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
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- C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
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Definitions
- the present invention relates to a hydrogel resin for transdermal administration prepared using ultraviolet rays, to a hydrogel cured with ultraviolet rays, and to cataplasma containing the same, specifically, to contain a large amount of water to relieve skin irritation, hydrogel It is easy to control the degree of crosslinking, maintains optimum drug release and transdermal absorption, and shows the same effect as oral administration, maintains excellent adhesion and elasticity, is easy to prepare, and a separate aging process after crosslinking
- the present invention relates to a hydrogel and a cataplasma including the same, which may be easily manufactured after being cut and packaged without a cooling process.
- Polyacrylic acid produced by metal complex ion bonding is an excellent material for biocompatibility and adhesion to the human body, such as US Patent No. 4,320,040 (1982) using acrylic acid or methacrylic acid together with polyvinyl alcohol to create a hydrogel.
- An example of making a hydrogel using acrylic acid and starch is also reported as in US Pat. No. 5,223,569 (1993).
- a hydrogel crosslinked with polyacrylic acid as a method for increasing the water resistance to sweat generated from the human body using a polyacrylic acid is a gelling agent, acrylic acid, etaacrylic acid, ester as in US Pat. No. 4,200,561 (1980).
- Polyacrylic acid cataplasma which is crosslinked by metal complex ion bond can not be immediately released into the product because the crosslinking time for metal complex ion bond is very long, and synthetic polyvinyl alcohol aqueous solution can be crosslinked by formaldehyde, gurutalaldehyde, etc.
- the gel may be formed by repeating freezing and thawing.
- crosslinking by aldehydes is not completely removed and toxicity by remaining aldehydes is a problem
- gels formed by repetition of freezing and thawing have a problem of not high strength, and a long period of time due to repetition of freezing and thawing is a problem.
- the process has a problem of rising product prices.
- polyvinylpyrrolidone In order to prepare hydrogel by chemical crosslinking method using polyvinylpyrrolidone, polyvinylpyrrolidone is dissolved in distilled water, followed by ethylene glycol dimethacrylate, propylene glycol dimethacrylate and detraethylene glycol dimethacrylate. Or polyfunctional monomers, such as a trimetholpropane triacrylate, are added and heated together with a chemical initiator.
- polyfunctional monomers such as a trimetholpropane triacrylate
- hydrogels use metal complex ion crosslinking mainly, but in this case, it takes a long time from 1 to 3 weeks to complete crosslinking, and adjusts adhesion and gel strength. There are a lot of difficulties. In addition, there is a problem that crosslinking does not occur as desired under conditions of pH 7 or higher, and there are many difficulties in adding various drugs to the hydrogel by these various matters.
- the present invention In order to solve the long manufacturing time of the hydrogel used in the patch, etc., the present invention not only greatly shortens the curing time of the hydrogel through ultraviolet curing, but also greatly improves the productivity of the drug contained in the hydrogel.
- the present invention seeks to provide a hydrogel having an optimum composition and composition ratio which can increase adhesion to the skin while providing excellent skin absorption and delivery, and also provides a cataplasmase using the hydrogel.
- the present invention for solving the above problems relates to a UV-curable hydrogel resin for transdermal administration, and includes a hydrophilic polymer, an active ingredient, a humectant, a solvent, a transdermal penetration accelerator, an ultraviolet initiator, and an ultraviolet crosslinking agent.
- the hydrogel resin of the present invention is a hydrophilic polymer 5 to 60% by weight, active ingredient 0.1 to 15% by weight, wetting agent 0.6 to 80% by weight, solvent 13.5 to 90% by weight, transdermal permeation promoter 0.5 25 wt%, 0.01-2.0 wt% of UV initiator, and 0.01-2.0 wt% of UV crosslinking agent.
- the hydrogel resin of the present invention may further include a pH adjusting agent.
- the hydrophilic polymer in the hydrogel resin composition of the present invention is polyvinyl alcohol, polyvinylpyrrolidone, polyvinylpyrrolidone / vinyl acetate copolymer, vinyl ether / maleic anhydride copolymer, Isobutylene / maleic anhydride copolymer, methoxyethylene / maleic anhydride copolymer, methacrylic acid / butyl acrylate copolymer, alginate, hydroxyethyl methacrylate, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose , Ethyl cellulose, methyl cellulose, carboxymethyl cellulose sodium, carboxyvinyl copolymer, polyethylene oxide, polyethylene glycol, polyacrylamide, polyhydroxyethyl methacrylate, polydioxolane, polyacrylic acid, sodium polyacrylate, polyvinyl acrylate , Polyacryl
- the active ingredient in the hydrogel resin composition of the present invention is lidocaine, lidocaine hydrochloride, roxofene, roxofene salt, ketoprofen, flurbiprofen, diclofenac, diclofenac salt , Indomethacin, pyricampam, meloxycamp, naproxen, ibuprofen, felbinac, menthol, salicylic acid glycol, methyl salicylate, pepper extract, nonyl acid vanylamide, vinyl butyl ether, centella asiatica, fusidic acid, It may include one or more selected from the fusidate, acrinol, puraria myripica, heparin, heparin salt and allantoin.
- the wetting agent in the hydrogel resin composition of the present invention is glycerin, 1,3-butylene glycol, propylene glycol, polypropylene glycol, sorbitol, mannitol, ethylene glycol, Diethylene glycol, polyethylene glycol and hyaluronic acid may comprise one or more.
- the transdermal penetration promoter in the hydrogel resin composition of the present invention propylene glycol, dipropylene glycol, polyethylene glycol, polyoxyethylene monooleate, polyglyceryl diisostea Latex, glycerin monooleate, polyoxyethylene sorbitan, N-methyl-2-pyrrolidone, N-caprylyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, laurylpyrroli Money, lauryl alcohol, glycerol lauryl alcohol, oleyl alcohol, isopropyl myristrate, sorbitan monooleate, propylene monolaurate, propylene monooleate, oleyl macrogol glyceride, oleic acid, lauroyl macrogol Glyceride, Linoleoyl Macrogol Glyceride, Propylene Glycol Caprylate, Propylene Glycol Caprate, Sorbitan
- the UV initiator in the hydrogel resin composition of the present invention may include one or more selected from rhodanine-based ultraviolet initiators and other ultraviolet initiators.
- the ketone UV initiator is 1-hydroxy-cyclohexyl-phenyl-ketone, 2-hydroxy-2-methyl-1-phenyl-1-propanone, 2-hydroxy- 1- [4- (2-hydroxyethoxy) phenyl] -2-methyl-1-propanone, 2-benzyl-2- (dimethylamino) -1- [4- (4-morpholinyl) phenyl]- It may contain one or more of 1-butanone, 2-methyl-1- [4- (methylthio) phenyl] -2- (4-morpholinyl) -1-propanone.
- the thioxanthone UV initiator is thioxanthone, 2-isopropyl thioxanthone, 2-chloro thioxanthone, 1-chloro-4-propoxy thioxanthone, 2- Dodecyl thioxanthone, 2,4-diethyl thioxanthone, 2,4-dimethyl thioxanthone, 1-methoxy-carbonyl thioxanthone, 2-ethoxycarbonyl thioxanthone, 3- (2-methoxy Ethoxycarbonyl) -thioxanthone, 4-butoxycarbonylthioxanthone, 3-butoxycarbonyl-7-methylthioxanthone, 1-cyano-3-chlorothioxanthone, 1-ethoxycarbon Yl-3-chlorothioxanthone, 1-ethoxycarbonyl-3-ethoxythioxanthone, 1-ethoxycarbon
- the benzophenone-based UV initiator is benzophenone, 4-phenyl benzophenone, 4-methoxy benzophenone, 4,4'-dimethyl benzophenone, 4,4'-dichlorobenzophenone, 4,4'-bis (dimethylamino) -benzophenone, 4,4'-bis (diethylamino) benzophenone, 4,4'-bis (methylethylamino) benzophenone, 4,4'-bis (p -Isopropylphenoxy) benzophenone, 3,3'-dimethyl-4-methoxy benzophenone, methyl-2-benzoylbendoate, 4- (2-hydroxyethylthio) -benzophenone, 4- (4 -Tolylthio) benzophenone, 1- [4- (4-benzoyl-phenylsulfanyl) -phenyl] -2-methyl-2 (toluene-4-sulfony
- the coumarin-based UV initiator is coumarin 1, coumarin 2, coumarin 6, coumarin 7, coumarin 30, coumarin 102, coumarin 106, coumarin 138, coumarin 152, coumarin 153, coumarin 307, coumarin 314 , Coumarin 314T, coumarin 334, coumarin 337, coumarin 500, 3-benzoyl coumarin, 3-benzoyl-7-methoxycoumarin, 3-benzoyl-5,7-dimethoxycoumarin, 3-benzoyl-5,7-dipro Foxycoumarin, 3-benzoyl-6,8-dichlorocoumarin, 3-benzoyl-6-chloro-coumarin, 3,3'-carbonyl-bis [5,7-di (propoxy) -coumarin], 3,3 '-Carbonyl-bis (7-methoxycoumarin), 3,3'-carbonyl-bis (7-diethylamino-coumarin),
- the thiazolin-based UV initiator is 3- (aroylmethylene) -thiazoline, 3-methyl-2-benzoylmethylene- ⁇ --naphthothiazoline,, 3-methyl-2- One or more of benzoylmethylene-benzothiazoline, 3-ethyl-2-tropionylmethylene- ⁇ -naphtholthiazoline.
- the rhodanine-based UV initiator is 4-dimethylaminobenzalardinine, 4-diethylaminobenzalardanine, 3-ethyl-5- (3-octyl-2-benzothiazolinylidene) It may include one or more of rhodanine.
- the other ultraviolet initiators are phenylacetophenone, hydroxy dimethyl acetophenone, 4,4'-bis (dimethylamino) benzyl, methylbenzoylformate, diphenyl (2,4,6- Trimethylbenzoyl) -phosphine oxide, phenyl bis (2,4,6-trimethyl benzoyl), oxy-phenyl-acetic acid-2- [2-oxo-2-phenyl-acetoxy-ethoxy] -ethyl ester, oxy- Phenyl-acetic acid-2- [2-hydroxy-ethoxy] -ethyl ester, 4-cyclopentadien-1-yl) bis [2,6-difluoro-3- (1-H-pyrrole-1- Yl) phenyl] titanium, 2-acetylnaphthalene, 2-naphthalaldehyde, iodonium salt, monocarboxylic acid derivative, 9.10-an
- the ultraviolet crosslinking agent in the hydrogel resin composition of the present invention benzyl methacrylate, lauryl methacrylate, isodecyl methacrylate, phenoxy methacrylate, 2-hydroxyethyl meth Acrylate, tetrahydro perfuryl methacrylate, cetyl (C16) methacrylate, stearyl methacrylate, methoxypig500 methacrylate, methoxypig600 methacrylate, methoxypig1000 methacrylate, 1 , 6-hexanediol dimethacrylate, butadiene dimethacrylate, neopentyl glycol dimethacrylate, ethylene glycol dimethacrylate, diethylene glycol dimethacrylate, triethylene glycol dimethacrylate, tetraethylene glycol Dimethacrylate, bisphenol A (io) 4 dimethacrylate, bisphenol A (io) 3 dimethacrylate, bisphenol A (io) 4 dime
- the pH adjusting agent in the hydrogel resin composition of the present invention comprises at least one selected from citric acid, acetic acid, malic acid, succinic acid, tartaric acid, lactic acid, triethanolamine, diisopropanolamine and diethanolamine can do.
- the hydrogel resin of the present invention may be pH 3 ⁇ 9.
- Another object of the present invention relates to a cured product obtained by ultraviolet curing the hydrogel resin, that is, a hydrogel.
- the hydrogel of the present invention may be 50 gf ⁇ 120 gf when measuring the peel strength (peel shtrength).
- Another object of the present invention relates to a cataplasmase, comprising: a drug layer including the above-described various types of UV-curable hydrogels for transdermal administration; And drug support layers; It includes.
- the drug support layer may include at least one selected from a polyurethane film, a porous film, a perforated film, a fabric, a nonwoven fabric, and a foam. have.
- the drug layer may have an average thickness of 20 ⁇ m to 2,000 ⁇ m, and the drug support layer may have an average thickness of 7 ⁇ m to 500 ⁇ m.
- the cataplasma agent of the present invention further includes a release layer, and the release layer, the drug layer, and the drug support layer may be sequentially stacked.
- the release layer comprises a polymer film coated with a silicone resin or fluorine resin
- the polymer film is polyester; Polyvinyl chloride; Polyvinylidene chloride; Polyethylene terephthalate; And copolymers thereof; It may include one or more polymer compounds selected from.
- the release layer may be an average thickness of 15 ⁇ m ⁇ 500 ⁇ m.
- the cataplasma agent of the present invention may be an anti-inflammatory, analgesic cataplasmase.
- Another object of the present invention relates to a method for preparing cataplasmase, comprising the steps of preparing a hydrogel resin; Coating the hydrogel resin on a release film; Stacking a support on the coated hydrogel resin; And 4 steps of curing the hydrogel resin by irradiating ultraviolet rays of 2,000 to 8,000 mW / cm 2 intensity for 3 minutes to 10 minutes in the support direction.
- Cataplasmase may be prepared by performing a process including.
- UV curable hydrogel for transdermal administration of the present invention is prepared in a non-toxic solvent, can contain a large amount of water to relieve skin irritation, easy to control the degree of cross-linking by controlling the degree of crosslinking, easy to control the elasticity, crosslinking degree of hydrogel
- By controlling the drug release and transdermal absorption can be controlled it is possible to provide a cataplasmase excellent in skin penetration rate and skin penetration rate.
- cataplasma using the hydrogel of the present invention is easy to manufacture, and compared to cataplasma based on a metal complex ion-bonded hydrogel component, it is easy to secure stability even after long-term storage, and separately aged after hydrogel crosslinking. It can be cut and packaged and shipped immediately without a process or cooling process, thereby providing a cataplasmase having excellent economic and commercial viability.
- Method for producing a cataplasma agent of the present invention comprises the steps of preparing a hydrogel resin; Coating the hydrogel resin on a release film; Stacking a support on the coated hydrogel resin; And curing the hydrogel resin by irradiating ultraviolet rays toward the support body. It includes.
- the hydrogel resin is a mixture of a hydrophilic polymer, an active ingredient, a humectant, a solvent, a transdermal permeation accelerator, a UV initiator and an ultraviolet crosslinking agent at a temperature of 15 ⁇ 35 °C at 5 ⁇ 150 ⁇ 1650rpm speed 5 ⁇ Stirring and crosslinking for 12 hours may be performed to sufficiently dissolve the compositions in a solvent.
- the hydrophilic polymer of the hydrogel resin component of the first step serves to impart viscoelasticity to the hydrogel and to maintain moisture content, 5 to 60% by weight of the total weight of the hydrogel resin, preferably 5 to 40% by weight. %, More preferably 8 to 35% by weight, where the hydrophilic polymer content is less than 5% by weight hydrogel does not maintain the water content and viscoelasticity, there is a problem that the skin permeation of the components difficult If it exceeds 60% by weight, the viscosity is too high, the coating is difficult in the second step, there may be a problem that the crosslinkability is greatly reduced.
- the hydrophilic polymer may be polyvinyl alcohol, polyvinylpyrrolidone, polyvinylpyrrolidone / vinylacetate copolymer, vinyl ether / maleic anhydride copolymer, isobutylene / maleic anhydride copolymer, methoxyethylene / maleic anhydride Copolymer, methacrylic acid / butyl acrylate copolymer, alginate, hydroxyethyl methacrylate, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, ethyl cellulose, methyl cellulose, sodium carboxymethyl cellulose, carboxyvinyl copolymer
- the copolymers polyethylene oxide, polyethylene glycol, polyacrylamide, polyhydroxyethyl methacrylate, polydioxolane, polyacrylic acid, sodium polyacrylate, polyvinyl acrylate, polyacryl acetate, polyvinyl chloride and polyacrylamide
- the hydrophilic polymer is 5 to 100 parts by weight of one or more selected from hydroxypropyl cellulose, sodium polyacrylate, polyacrylic acid, sodium carboxymethylcellulose, and polyacrylamide, based on 100 parts by weight of polyvinylidene. Preferably it can be used by mixing 10 to 50 parts by weight. Specific examples include the above hydrophilic polyvinylpyrrolidone and sodium polyacrylate, polyvinylpyrrolidone and polyacrylic acid, polyvinylpyrrolidone and polyacrylamide, polyvinylpyrrolidone and polyvinyl alcohol, and polyvinylpyrrole.
- It may be used by mixing with sodium sodium ralidone and carboxymethyl cellulose, polyvinylpyrrolidone and hydroxyethyl cellulose, polyvinylpyrrolidone and hydroxypropyl cellulose, polyvinylpyrrolidone and hydroxyethyl methacrylate.
- hydrophilic polymer may include a treatment with a known crosslinking agent or polymer.
- the active ingredient may be an active ingredient used in the art according to the use according to the hydrogel, preferably, the active ingredient is lidocaine, lidocaine hydrochloride, roxofene, Roxoprofen salt, ketoprofen, flurbiprofen, diclofenac, diclofenac salt, indomethacin, pyroxicam, meloxycamp, naproxen, ibuprofen, felbinac, menthol, salicylic acid glycol, methyl salicylate, red pepper
- One or two or more selected from extract, vanylamide, vinyl butyl ether, centella asiatica, fusidic acid, fusidate, acrinol, pueraria myripica, heparin, heparin salt and allantoin can be used.
- one or two or more kinds of lidocaine, lidocaine hydrochloride, roxofene, and roxofene salt can be used.
- the hydrogel resin may comprise 0.1 to 15% by weight, preferably 1 to 10% by weight of the active ingredient in the total weight, if the amount of the active ingredient is less than 0.1% by weight its amount is too small to the active ingredient The effect of use may not be seen, and if it exceeds 15% by weight, excessive active ingredients may interfere with the crosslinking, which may cause a problem in hydrogel production.
- the wetting agent plays a role in maintaining the wet state of the hydrogel, reducing skin irritation, maintaining a sustained cooling ability, and improving the volatilization of water, and a general one used in the art may be used.
- glycerin Preferably selected from glycerin, 1,3-butylene glycol, propylene glycol, polypropylene glycol, sorbitol, mannitol, ethylene glycol, diethylene glycol, polyethylene glycol and hyaluronic acid It may include a species or two or more, preferably one or two or more selected from glycerin, sorbitol and hyaluronic acid, more preferably glycerin and sorbitol in a weight ratio of 1: 0.2 to 0.5 It can be mixed and used.
- the hydrogel resin may include 0.6 to 80% by weight of the wetting agent, preferably 5 to 50% by weight, more preferably 12 to 40% by weight of the total weight, wherein the content of the wetting agent is 0.6 If the weight percentage is less than the hydrogel may not be able to maintain a sufficient wet state, when used in excess of 80% by weight may have a problem that the hydrogel is not cured.
- the solvent of the hydrogel resin component of the first step may be water, such as purified water, distilled water, the content of the solvent is 13.5 to 90% by weight, preferably 18 to 70% by weight, more preferably of the total weight of the hydrogel resin Is 30 to 60% by weight.
- the transdermal permeation accelerator of the hydrogel resin component of the first step is for promoting the absorption of the active ingredient into the percutaneous and sustained action, the content is 0.5 to 25% by weight of the total weight of the hydrogel resin, preferably 0.5 to 23% by weight, more preferably 1 to 20% by weight is good, in this case, if the content of the transdermal permeation accelerator is less than 0.5% by weight, there may be a problem that the transdermal absorption of the active ingredient in the hydrogel is greatly reduced, 25% by weight If used in excess of there may be a problem in the adhesive strength of the hydrogel.
- the active ingredient is sodium roxofene and its salts, propylene glycol, glycerin monooleate, glycerin monooleate, polyoxyethylene sorbitan, N-methyl-2-pyrrolidone and lau It is good to use a mixture of 3 or 4 or more selected from lyrrolidone.
- the UV initiator is a crosslinking reaction initiation component for forming a hydrogel by UV, and includes a ketone UV initiator, a thioxanthone UV initiator, a benzophenone UV initiator, a coumarin UV initiator, and a thia It can be used individually by 1 type or in mixture of 2 or more types selected from a sleepy ultraviolet initiator, a rhodanine ultraviolet initiator, and other ultraviolet initiators.
- the content thereof is 0.01 to 2.0% by weight, preferably 0.025 to 1.5% by weight, more preferably 0.1 to 1.0% by weight of the total weight of the hydrogel resin, when the UV initiator content is less than 0.01% by weight UV irradiation According to the curing time is too long due to the low commerciality, there may be a problem of the lack of viscoelasticity of the cured hydrogel, if the UV initiator content exceeds 2% by weight curing rate is too fast to control the curing rate is difficult and poor adhesion There can be.
- ultraviolet initiators that can be used in the present invention are described as follows.
- the ketone ultraviolet initiators are ⁇ -hydroxy ketones, which include 1-hydroxycyclohexyl-phenyl-ketone, 2-hydroxy-2-methyl-1-phenyl-1-propanone, and 2-hydroxy-1- 2-benzyl-2- (dimethylamino) -1- [4- (4-morpholinyl), which is [4- (2-hydroxyethoxy) phenyl] -2-methyl-1-propanone and ⁇ -aminocatones Phenyl] -1-butanone and 2-methyl-1- [4- (methylthio) phenyl] -2- (4-morpholinyl) -1-propanone, which may be used alone or in combination of two or more thereof. Can be.
- the thioxanthone ultraviolet initiator may be thioxanthone, 2-isopropyl thioxanthone, 2-chloro thioxanthone, 1-chloro-4-propoxy thioxanthone, 2-dodecyl thioxanthone, 2,4- Diethyl thioxanthone, 2,4-dimethyl thioxanthone, 1-methoxy-carbonyl thioxanthone, 2-ethoxycarbonyl thioxanthone, 3- (2-methoxyethoxycarbonyl)-thioxanthone 4-butoxycarbonyl thioxanthone, 3-butoxycarbonyl-7-methyl thioxanthone, 1-cyano-3-chlorothioxanthone, 1-ethoxycarbonyl-3-chlorothioxanthone, 1-ethoxycarbonyl-3-ethoxythioxanthone, 1-ethoxycarbonyl-3-amino
- benzophenone-based ultraviolet initiator benzophenone, 4-phenyl benzophenone, 4-methoxy benzophenone, 4,4'-dimethyl benzophenone, 4,4'-dichlorobenzophenone, 4,4'-bis (dimethyl Amino) -benzophenone, 4,4'-bis (diethylamino) benzophenone, 4,4'-bis (methylethylamino) benzophenone, 4,4'-bis (p-isopropylphenoxy) benzophenone , 3,3'-dimethyl-4-methoxy benzophenone, methyl-2-benzoylbendoate, 4- (2-hydroxyethylthio) -benzophenone, 4- (4-tolylthio) benzophenone, 1 -[4- (4-Benzoyl-phenylsulfanyl) -phenyl] -2-methyl-2 (toluene-4-sulfonyl) -propan-1-
- coumarin-based UV initiator As the coumarin-based UV initiator, coumarin 1, coumarin 2, coumarin 6, coumarin 7, coumarin 30, coumarin 102, coumarin 106, coumarin 138, coumarin 152, coumarin 153, coumarin 307, coumarin 314, coumarin 314T, coumarin 334, coumarin 337, coumarin 500, 3-benzoyl coumarin, 3-benzoyl-7-methoxycoumarin, 3-benzoyl-5,7-dimethoxycoumarin, 3-benzoyl-5,7-dipropoxycoumarin, 3-benzoyl-6 , 8-dichlorocoumarin, 3-benzoyl-6-chloro-coumarin, 3,3'-carbonyl-bis [5,7-di (propoxy) -coumarin], 3,3'-carbonyl-bis (7 -Methoxycoumarin), 3,3'-carbonyl-bis (7-diethylamino-coumarin), 3-is
- the thiazolin based ultraviolet initiators include 3- (aroylmethylene) -thiazoline, 3-methyl-2-benzoylmethylene- ⁇ -naphthothiazoline, 3-methyl-2-benzoylmethylene-benzothiazoline and 3-ethyl It can be used individually by 1 type or in mixture of 2 or more types chosen from the 2-tropionylmethylene- (beta)-naphtholthiazoline.
- rhodanine-based UV initiator one kind selected from 4-dimethylaminobenzallodanine, 4-diethylaminobenzallodanine and 3-ethyl-5- (3-octyl-2-benzothiazolinylidene) -rhodanine alone Or it can mix and use 2 or more types.
- the other ultraviolet initiators are acetophenone, 3-methoxyacetophenone, 4-phenylacetophenone, ⁇ -dimethoxy- ⁇ -phenylacetophenone, hydroxy dimethyl acetophenone, benzyl, 4,4'-bis (dimethyl Amino) benzyl, methylbenzoylformate, diphenyl (2,4,6-trimethylbenzoyl) -phosphine oxide, phenyl bis (2,4,6-trimethyl benzoyl).
- the ultraviolet crosslinking agent in the hydrogel resin component of the first step serves to control the adhesiveness and elasticity of the hydrogel by controlling the degree of crosslinking of the hydrogel, the content is 0.01 to 2% by weight of the total weight of the hydrogel resin, Preferably it is 0.025-2 weight%, More preferably, it is 0.025-1.5 weight%, At this time, if the content of an ultraviolet crosslinking agent is less than 0.01 weight%, there may be a problem that the viscoelasticity of the ultraviolet-cured hydrogel is too low, 2 weight If used in excess of% may have a problem in that the adhesive strength falls.
- the ultraviolet crosslinking agent may be benzyl methacrylate, lauryl methacrylate, isodecyl methacrylate, phenoxy methacrylate, 2-hydroxyethyl methacrylate, tetrahydro perfuryl methacrylate, cetyl (C16).
- methylene bis acrylamide, 2-hydroxyethyl methacrylate, ethylene glycol dimethacrylate, 1,3-butylene glycol dimethacrylate, polyethylene glycol 400 dimethacrylate, tripropylphen glycol diacryl It can be used individually by 1 type or in mixture of 2 or more types chosen from a rate and tetraethylene glycol diacrylate.
- the second step is a process of coating (or applying) the hydrogel resin prepared in step 1 on the release film
- the coating method is a general coating used in the art It can be done by the method.
- the release film is to be separated and removed immediately before use to the skin after the manufacture of the cataplasmase, so that the drug layer of the cataplasma to adhere to the skin
- the release film has an average thickness of 15 ⁇ m ⁇ 500 ⁇ m
- the release film is a polymer film coated with a silicone resin or fluorine resin
- the polymer film is a film polyester; Polyvinyl chloride; Polyvinylidene chloride; Polyethylene terephthalate; And copolymers thereof; It may include one or two or more polymer compounds selected from.
- the third step is a process of laminating a support on a hydrogel resin coated on a release film, the support serves as a drug support layer of the cataplasmase, the support May be used alone or in combination of two or more selected from a polyurethane film, a porous film, a perforated film, a woven fabric, a nonwoven fabric, and a foam.
- the average thickness of the support is preferably 7 ⁇ m to 500 ⁇ m, preferably 50 ⁇ m to 250 ⁇ m, and if the average thickness is less than 7 ⁇ m, the hydrogel is cured because it is too thin to secure sufficient mechanical properties. It may not be able to serve as a support for, and if it exceeds 500 ⁇ m may be too thick to have a problem that the fit to the skin body is poor, it is better to use a support having a thickness within the above range.
- the step 4 is a release film, the hydrogel resin coating layer and the support is laminated, and then irradiated with UV in the direction of the support to cure the hydrogel resin between the release film and the support To form a hydrogel (drug layer).
- the UV irradiation may be carried out by irradiating the ultraviolet light of 2,000 ⁇ 8,000 mW / cm2 intensity for 3 to 10 minutes, preferably 2,500 ⁇ 5,000 mW / cm2 intensity 3 to 10 minutes.
- the average thickness of the hydrogel formed by UV curing is not particularly limited, but is preferably 20 ⁇ m to 2,000 ⁇ m, more preferably 40 ⁇ m to 1,000 ⁇ m.
- the UV-cured hydrogel is measured for skin permeation of the active ingredient under sink conditions and 30 to 33 ° C. using a Franz diffusion cell having an effective area of 0.64 cm 2 and an aqueous phase volume of 5.2 ml.
- the cumulative skin permeation amount may be 40 to 160 ⁇ g / cm 2, preferably 45 to 150 ⁇ g / cm 2, and more preferably 50 to 150 ⁇ g / cm 2, it may have excellent skin permeability.
- the UV-cured hydrogel is a skin permeation of the active ingredient under sink conditions and 30 ° C. to 33 ° C. using a Franz diffusion cell having an effective area of 0.64 cm 2 and an aqueous phase volume of 5.2 ml.
- the skin permeation rate may be 1.0 to 7.5 ⁇ g / cm 2 / hr, preferably 1.0 to 7.0 ⁇ g / cm 2 / hr, more preferably 1.0 to 6.8 ⁇ g / cm 2 / hr. It may have a skin penetration rate.
- the UV-cured hydrogel based on the adhesive test of the adhesive plaster of the Korean Pharmacopoeia, when measuring the peel strength (peel strength), the adhesion is 40 gf ⁇ 150 gf, preferably 50 gf ⁇ 150 gf, more preferably It can be 60 gf ⁇ 150 gf bar, excellent adhesion to the skin.
- Cataplasma of the present invention prepared by such a method is a release layer; Drug layer containing a UV curable hydrogel for transdermal administration; And a drug support layer, wherein the release layer is a release film as described above, and the release layer is used by removing a cataplasmase from the skin.
- the drug support layer corresponds to the support described above.
- the cataplasma agent of the present invention may vary in its specific use depending on the active ingredient in the drug layer, for example, as an active ingredient, anti-inflammatory using lidocaine, lidocaine hydrochloride, roxofene, roxofene salt, etc. It can be used as an analgesic cataplasmase.
- Hydrogel resin 15% by weight of polyvinylpyrrolidone, 0.25% by weight of flurbiprofen, 28.75% by weight of glycerin, 10% by weight of sorbitol, 15% by weight of propylene glycol, 0.01% by weight of 1-hydroxy-cyclohexyl-phenyl-ketone Hydrogel resin was prepared by mixing, stirring and completely dissolving 0.2 wt% of methylene bis acrylamide and 30.79 wt% of purified water.
- a hydrogel resin was prepared in the same manner as in Example 1, but a hydrogel resin was prepared to have a composition and a composition ratio as shown in Tables 1 to 7 below.
- Hydrogel resins were prepared in the same manner as in Example 1, but hydrogel resins having compositions and composition ratios as shown in Table 8 were prepared by varying the active ingredients.
- Hydrogel resins were prepared in the same manner as in Example 1, but hydrogel resins having compositions and composition ratios as shown in Table 9 were prepared by varying the active ingredients.
- the hydrogel preparation prepared in Example 1 was coated on one surface of a silicone film-coated polyester film (thickness 75 ⁇ m) to cover a nonwoven fabric, and then irradiated with ultraviolet rays for 4 minutes to cure the hydrogel resin coating layer.
- a release film), a drug layer (hydrogel), and a drug support layer (nonwoven fabric) were prepared and laminated cataplasmase. Hydrogel with an average thickness of 500 ⁇ m was prepared.
- Cataplasmase was prepared in the same manner as in Example 1, but cataplasmas were prepared using the hydrogel resins of Examples 2 to 74 instead of the hydrogel resin of Example 1, respectively. Was carried out.
- Cataplasmase was prepared in the same manner as in Example 1, but cured by standing at room temperature (25 ° C.-27 ° C.) for 14 days for bonding metal ions instead of UV irradiation. And, whether or not the curing was determined by whether or not it comes out on the hydrogel and whether it is cut out on the nonwoven fabric.
- Cataplasmase was prepared in the same manner as in Example 1, but instead of the hydrogel resin of Example 1, hydrogel resins of Comparative Examples 2 to 8 were used to prepare cataplasmases, respectively. 8 was carried out.
- Comparative Example 2 in which the hydrogel resin using the hydrophilic polymer was used at less than 5% by weight, and Comparative Preparation Example 7 and Comparative Preparation Example 8 in which the hydrogel resin was used without using the UV initiator and the UV crosslinking agent, gel formation was good. It did not support or did not crosslink, and adhesive force measurement was impossible.
- the adhesive strength was low as 37 gf of less than 50 gf, which resulted in reducing the adhesive strength of the hydrogel by preventing the cross-linking of the active ingredient crosslinking Judging by
- Comparative Preparation Example 5 in which the content of the wetting agent was less than 0.6 wt%, the adhesion was very low, which is considered to be the result of the adhesive strength of the ultraviolet-cured hydrogel being too dry.
- the cumulative skin permeation amount was subjected to a skin permeation test under a sink condition using a Franz diffusion cell (effective area: 0.64 cm 2 , volume of an aqueous phase: 5.2 ml). More specifically, first, the aqueous phase of Phosphate buffered saline (PBS) of pH 7.4 was filled in a Franz Diffusion cell, kept at 32 ⁇ 0.5 ° C., and the sample was cut into circles (area 0.64 cm 2 ). The skin was attached to the center of the prepared human cadaver skin epidermis and the sample was attached to the upper portion of the receiving portion of the Franz Diffusion Cell. Then, the donor was covered and clamped, and then a permeation experiment was performed.
- PBS Phosphate buffered saline
- the skin was used by purchasing a human cadaver skin epidermis layer, stored at -70 °C after purchase and thawed at 40 °C when used. And, the active ingredient permeation analysis was performed using HPLC and the measurement results for 24 hours are shown in Table 14 and Table 15 below.
- Comparative Preparation Example 1 which is a conventional cataplasmase prepared through metal complex ion bonding, showed a low cumulative skin penetration rate and skin penetration rate.
- Comparative Preparation Example 3 which used more than 60% by weight of the hydrophilic polymer, the adhesive strength was excellent in Table 12, but compared to the preparation of Table 13, the cumulative skin penetration rate and skin penetration rate was low It is believed that a large amount of the hydrophilic polymer having a crosslinked structure in the hydrogel has rather reduced the skin delivery power of the active ingredient.
- Comparative Preparation Example 4 having an active ingredient content of more than 15 wt% and Comparative Preparation Example 5 having a wetting agent content of less than 0.6 wt% showed excellent cumulative skin penetration rate and skin penetration rate.
- Comparative Production Example 4 and Comparative Production Example 5 as shown in Table 12, there was a problem that the adhesive strength is not good.
- the curing rate of the drug layer (hydrogel) of the cataplasmase prepared using the hydrogel resin of the present invention through the above Examples and Experimental Examples is economical and commercially excellent, yet the skin delivery power and delivery rate of the drug layer was not only very good, but also the adhesion to the skin was also very good. It is expected that the cataplasmase of the present invention can be used to provide various pharmaceutical patches.
Abstract
Description
구분(중량%) | 실시예 | ||||||||||
1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | 10 | ||
친수성고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 |
솔비톨 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
용매 | 정제수 | 30.79 | 30.7 | 29.8 | 30.79 | 30.7 | 29.8 | 30.3 | 29.8 | 30.3 | 29.8 |
자외선개시제 | 1-히드록시-사이클로헥실-페닐-케톤 | 0.01 | 0.1 | 1 | - | - | - | - | - | - | - |
벤조페논 | - | - | - | 0.01 | 0.1 | 1 | - | - | - | - | |
메틸벤조일포르메이트 | - | - | - | - | - | - | 0.5 | 1 | |||
포스핀옥사이드,페닐 비스(2,4,6-트리메틸벤조일) | - | - | - | - | - | - | - | - | 0.5 | 1 | |
2-히드록시-2-메틸-1-페닐-1-프로판온 | - | - | - | - | - | - | - | - | - | - | |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 |
구분(중량%) | 실시예 | ||||||||||
11 | 12 | 13 | 14 | 15 | 16 | 17 | 18 | 19 | 20 | ||
친수성고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 10 | 20 | 15 | 15 | 15 | 15 |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 28.75 | 38.75 | 78.75 | 28.75 | 28.75 |
솔비톨 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
용매 | 정제수 | 30.3 | 29.8 | 30.6 | 29.8 | 35.6 | 25.6 | 20.6 | 40.6 | 30.5 | 30.7 |
자외선개시제 | 1-히드록시-사이클로헥실-페닐-케톤 | - | - | 0.1 | 0.5 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 |
벤조페논 | - | - | 0.1 | 0.5 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | |
메틸벤조일포르메이트 | - | - | - | - | - | - | - | - | - | - | |
포스핀옥사이드,페닐 비스(2,4,6-트리메틸벤조일) | - | - | - | - | - | - | - | - | - | - | |
2-히드록시-2-메틸-1-페닐-1-프로판온 | 0.5 | 1 | - | - | - | - | - | - | - | - | |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.3 | 0.1 |
구분(중량%) | 실시예 | ||||||||||
21 | 22 | 23 | 24 | 25 | 26 | 27 | 28 | 29 | 30 | ||
친수성고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 |
솔비톨 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
용매 | 정제수 | 30.8 | 30.35 | 29.85 | 28.85 | 30.8 | 29.85 | 28.85 | 30.6 | 30.8 | 29.85 |
자외선개시제 | 벤조페논 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.05 | 0.5 | 1 | 2 | - | - | - | - | - | |
2-히드록시에틸 메타크릴레이트 | - | - | - | - | 0.05 | 1 | 2 | - | - | ||
에틸렌글리콜 디메타크릴레이트 | - | - | - | - | - | - | - | 0.25 | 0.05 | 1 | |
1,3-부틸렌글리콜 디메타크릴레이트 | - | - | - | - | - | - | - | - | - | - | |
폴리에틸렌글리콜 400 디메타크릴레이트 | - | - | - | - | - | - | - | - | - | - | |
트리프로필펜글리콜 디아크릴레이트 | - | - | - | - | - | - | - | - | - | - | |
테트라에틸렌글리콜 디아크릴레이트 | - | - | - | - | - | - | - | - | - | - |
구분(중량%) | 실시예 | |||||||||||
31 | 32 | 33 | 34 | 35 | 36 | 37 | 38 | 39 | 40 | 41 | ||
친수성고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
유효성분 | 리도카인 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 | 25 |
솔비톨 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
용매 | 정제수 | 29.35 | 28.85 | 30.8 | 29.85 | 28.85 | 30.8 | 29.85 | 28.85 | 30.8 | 29.85 | 28.85 |
자외선개시제 | 벤조페논 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | - | - | - | - | - | - | - | - | - | - | - |
2-히드록시에틸 메타크릴레이트 | - | - | - | - | - | - | - | - | - | - | - | |
에틸렌글리콜 디메타크릴레이트 | - | - | - | - | - | - | - | - | - | - | - | |
1,3-부틸렌글리콜 디메타크릴레이트 | 1.5 | 2 | - | - | - | - | - | - | - | - | - | |
폴리에틸렌글리콜 400 디메타크릴레이트 | - | - | 0.05 | 1 | 2 | - | - | - | - | - | - | |
트리프로필펜글리콜 디아크릴레이트 | - | - | - | - | - | 0.05 | 1 | 2 | - | - | - | |
테트라에틸렌글리콜 디아크릴레이트 | - | - | - | - | - | - | - | - | 0.05 | 1 | 2 |
구분(중량%) | 실시예 | ||||||
42 | 43 | 44 | 45 | 46 | 47 | ||
친수성고분자 | 폴리비닐피롤리돈 | 4 | 7 | 10 | 15 | 20 | 25 |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 25 | 25 | 25 | 15 | 10 | 5 |
솔비톨 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 8.75 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 10 | 10 | 10 |
용매 | 정제수 | 41.5 | 38.5 | 35.5 | 45.5 | 45.5 | 50.5 |
자외선개시제 | 벤조페논 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
pH 조절제 | 주석산 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 |
구분(중량%) | 실시예 | |||||||||
48 | 49 | 50 | 51 | 52 | 53 | 54 | 55 | 56 | ||
친수성고분자 | 폴리비닐피롤리돈 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 | 10 |
폴리아크릴릭산 | 1 | 3 | 5 | 0 | 0 | 0 | 0 | 0 | 0 | |
폴리아크릴아마이드 | 0 | 0 | 0 | 1 | 3 | 5 | 0 | 0 | 0 | |
히드록시프로필셀룰로오스 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 3 | 5 | |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 15 | 10 | 10 | 15 | 10 | 10 | 15 | 10 | 10 |
솔비톨 | 13.75 | 13.75 | 8.75 | 13.75 | 13.75 | 8.75 | 13.75 | 13.75 | 8.75 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 10 | 10 | 15 | 10 | 10 | 15 | 10 | 10 |
용매 | 정제수 | 44.6 | 52.6 | 55.6 | 44.6 | 52.6 | 55.6 | 44.6 | 52.6 | 55.6 |
자외선개시제 | 벤조페논 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 |
자외선가교제 | 에틸렌글리콜 디메타크릴레이트 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
구분(중량%) | 실시예 | ||||||
57 | 58 | 59 | 60 | 61 | 62 | ||
친수성고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 15 | 15 |
유효성분 | 플루르비프로펜 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
습윤제 | 글리세린 | 25 | 25 | 25 | 25 | 25 | 25 |
솔비톨 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | 13.75 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 15 | 15 | 15 | 15 | 15 | 15 |
소르비탄모노올레이트 | 1 | - | - | - | - | - | |
이소프로필미리스트레이트 | - | 1 | - | - | - | - | |
폴리옥시에틸렌모노올레이트 | - | - | 1 | - | - | - | |
글리세롤모노올레이트 | - | - | - | 1 | - | - | |
프로필렌글리콜모노라우레이트 | - | - | - | - | 1 | - | |
폴리글리세릴디이소스테아레이트 | - | - | - | - | - | 1 | |
용매 | 정제수 | 29.6 | 29.6 | 29.6 | 29.6 | 29.6 | 29.6 |
자외선개시제 | 벤조페논 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 |
구분(중량%) | 실시예 | ||||||||
63 | 64 | 65 | 66 | 67 | 68 | 69 | 70 | ||
친수성 고분자 | 폴리비닐피롤리돈 | 15 | 15 | 15 | 15 | 15 | 15 | 15 | 15 |
유효성분 | 록소프로펜 나트륨 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 | 1.5 | 2 |
습윤제 | 글리세린 | 28 | 28 | 28 | 28 | 28 | 28 | 28 | 33 |
솔비톨 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 5 | |
경피투과촉진제 | 트리아세틴 | - | - | 2 | - | 2 | 1.5 | - | - |
프로필렌 글라이콜 | 28 | 28 | 28 | 28 | 28 | 28 | 28 | 28.53 | |
글리세린모노올레에이트 | 2 | - | - | - | - | - | 1 | 1 | |
N- 메틸 -2- 피롤리돈 (NMP) | 0.3 | 0.3 | 0.3 | 0.3 | 0.3 | 0.3 | 0.3 | 0.3 | |
폴리옥시에틸렌소르비탄 | 0.4 | 0.4 | 0.4 | 0.4 | 0.4 | 0.4 | 0.4 | 0.2 | |
라우릴피롤리돈 | - | 2 | - | - | 1 | 1.5 | 1 | 1 | |
용매 | 정제수 | 16.78 | 16.78 | 16.78 | 16.78 | 16.78 | 16.78 | 16.78 | 13 |
자외선개시제 | 벤조페논 | 0.11 | 0.11 | 0.11 | 0.11 | 0.11 | 0.11 | 0.11 | 0.1 |
자외선가교제 | 글리콜해마메타크릴래이트 | 0.16 | 0.16 | 0.16 | 0.16 | 0.16 | 0.16 | 0.16 | 0.15 |
pH 조절제 | 주석산 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 |
보존제 | 메틸파라벤 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0.12 |
착향제 | 엘멘톨 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 | 0.5 |
구분(중량%) | 실시예 | ||||
71 | 72 | 73 | 74 | ||
친수성고분자 | 폴리비닐피롤리돈 | 10 | 10 | 10 | 10 |
유효성분 | 플루르비프로펜 | 1 | 1 | 1.2 | 1.2 |
습윤제 | 글리세린 | 30 | 31 | 31 | 30 |
솔비톨 | 10 | 10 | 10 | 10 | |
경피투과 촉진제 | 프로필렌 글라이콜 | 23 | 23 | 23 | 23 |
소르비탄모노올레이트 | 1 | 1 | 1 | 1 | |
라우릴 피롤리돈 | 1 | 1 | 1 | 1 | |
용매 | 정제수 | 22.63 | 21.68 | 21.5 | 22.53 |
자외선개시제 | 벤조페논 | 0.12 | 0.07 | 0.05 | 0.02 |
자외선가교제 | 글리콜헤마메타크릴래이트 | 0.25 | 0.25 | 0.25 | 0.25 |
착향제 | 멘톨 | 1 | 1 | 1 | 1 |
구분(중량%) | 비교예 1 |
플루루비프로팬 | 0.5 |
글리세린 | 19.00 |
솔비톨 | 20.00 |
폴리아크릴레이트 용액 | 10.00 |
폴리아크릴레이트 나트륨 | 5.00 |
카르복시메틸셀룰로오스 나트륨 | 5.00 |
프로필렌 글라이콜 | 5.00 |
우레아 | 3.00 |
주석산 | 1.50 |
디하이드록시 알루미늄 아미노아세테이트 | 0.25 |
정제수 | 30.75 |
구분 | 비교예 | |||||||
2 | 3 | 4 | 5 | 6 | 7 | 8 | ||
친수성고분자 | 폴리비닐피롤리돈 | 3 | 65 | 15 | 20 | 17 | 15 | 15 |
유효성분 | 플루르비프로펜 | 4 | 4 | 17 | 5 | 5 | 4 | 4 |
습윤제 | 글리세린 | 25 | 10 | 25 | 0.2 | 25 | 25 | 25 |
솔비톨 | 10 | 5 | 10 | 0.2 | 10 | 10 | 10 | |
경피투과 촉진제 | 라우릴피롤리돈 | 15 | 10 | 15 | 30 | 0 | 15 | 15 |
용매 | 정제수 | 44.6 | 5.6 | 17.6 | 44.2 | 42.6 | 30.75 | 30.85 |
자외선개시제 | 1-하이드록시-사이클로헥실-페닐-케톤 | 0.15 | 0.15 | 0.15 | 0.15 | 0.15 | 0 | 0.15 |
자외선가교제 | 메틸렌 비스 아크릴아마이드 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0.25 | 0 |
구분 | 점착력(gf) | 구분 | 점착력(gf) | 구분 | 점착력(gf) |
제조예1 | 70 | 제조예26 | 58 | 제조예51 | 56 |
제조예2 | 64 | 제조예27 | 57 | 제조예52 | 57 |
제조예3 | 61 | 제조예28 | 60 | 제조예53 | 55 |
제조예4 | 71 | 제조예29 | 65 | 제조예54 | 58 |
제조예5 | 64 | 제조예30 | 68 | 제조예55 | 57 |
제조예6 | 60 | 제조예31 | 60 | 제조예56 | 61 |
제조예7 | 71 | 제조예32 | 58 | 제조예57 | 63 |
제조예8 | 63 | 제조예33 | 65 | 제조예58 | 64 |
제조예9 | 68 | 제조예34 | 62 | 제조예59 | 63 |
제조예10 | 61 | 제조예35 | 60 | 제조예60 | 61 |
제조예11 | 72 | 제조예36 | 68 | 제조예61 | 60 |
제조예12 | 61 | 제조예37 | 63 | 제조예62 | 63 |
제조예13 | 81 | 제조예38 | 61 | 제조예63 | 70 |
제조예14 | 68 | 제조예39 | 63 | 제조예64 | 71 |
제조예15 | 62 | 제조예40 | 62 | 제조예65 | 73 |
제조예16 | 95 | 제조예41 | 64 | 제조예66 | 71 |
제조예17 | 85 | 제조예42 | 53 | 제조예67 | 72 |
제조예18 | 69 | 제조예43 | 55 | 제조예68 | 68 |
제조예19 | 79 | 제조예44 | 56 | 제조예69 | 67 |
제조예20 | 76 | 제조예45 | 62 | 제조예70 | 70 |
제조예21 | 68 | 제조예46 | 65 | 제조예71 | 65 |
제조예22 | 64 | 제조예47 | 68 | 제조예72 | 67 |
제조예23 | 63 | 제조예48 | 56 | 제조예73 | 69 |
제조예24 | 61 | 제조예49 | 58 | 제조예74 | 68 |
제조예25 | 58 | 제조예50 | 63 | - | - |
구분 | 점착력(gf) | 구분 | 점착력(gf) |
비교제조예1 | 38 | 비교제조예5 | 32 |
비교제조예2 | × | 비교제조예6 | 64 |
비교제조예3 | 58 | 비교제조예7 | × |
비교제조예4 | 37 | 비교제조예8 | × |
구분 | 누적피부투과량 (μg/cm2) | 피부투과속도 (μg/cm2/hr) | 구분 | 누적피부투과량 (μg/cm2) | 피부투과속도 (μg/cm2/hr) | 구분 | 누적피부투과량 (μg/cm2) | 피부투과속도 (μg/cm2/hr) |
제조예1 | 55±5.70 | 2.292 | 제조예26 | 57±7.12 | 2.375 | 제조예51 | 51±2.1 | 2.125 |
제조예2 | 53±5.84 | 2.208 | 제조예27 | 61±2.78 | 2.542 | 제조예 52 | 52±3.45 | 2.167 |
제조예3 | 51±1.51 | 2.125 | 제조예28 | 57±7.3 | 2.208 | 제조예53 | 57±4.12 | 2.208 |
제조예4 | 48±2.81 | 2.000 | 제조예29 | 58±10.1 | 2.417 | 제조예54 | 61±3.78 | 2.542 |
제조예5 | 57±5.1 | 2.375 | 제조예30 | 59±7.2 | 2.458 | 제조예55 | 57±3.1 | 2.375 |
제조예6 | 58±5.07 | 2.417 | 제조예31 | 62±7.99 | 2.583 | 제조예56 | 56±7.12 | 2.333 |
제조예7 | 60±7.09 | 2.500 | 제조예 32 | 55±5.12 | 2.292 | 제조예 57 | 72±6.22 | 3.000 |
제조예8 | 63±3.19 | 2.625 | 제조예33 | 57±6.78 | 2.375 | 제조예58 | 71±5.81 | 2.958 |
제조예9 | 57±5.7 | 2.375 | 제조예34 | 51±2.78 | 2.125 | 제조예59 | 75±7.14 | 3.125 |
제조예10 | 49±5.1 | 2.042 | 제조예35 | 53±7.18 | 2.208 | 제조예60 | 77±7.37 | 3.208 |
제조예11 | 57±4.3 | 2.375 | 제조예36 | 57±2.07 | 2.375 | 제조예61 | 81±8.17 | 3.375 |
제조예12 | 56±9.1 | 2.333 | 제조예 37 | 56±4.27 | 2.333 | 제조예 62 | 77±7.57 | 3.208 |
제조예13 | 55±7.5 | 2.208 | 제조예38 | 57±3.93 | 2.208 | 제조예63 | 94.96±15.28 | 3.950 |
제조예14 | 67±5.74 | 2.208 | 제조예39 | 54±5.24 | 2.208 | 제조예64 | 148±9.03 | 6.610 |
제조예15 | 54±2.21 | 2.208 | 제조예40 | 57±7.91 | 2.208 | 제조예65 | 51±7.52 | 2.120 |
제조예16 | 56±2.71 | 2.208 | 제조예41 | 55±5.17 | 2.208 | 제조예66 | 84.97±2.32 | 3.540 |
제조예17 | 57±7.27 | 2.208 | 제조예42 | 61±3.87 | 2.208 | 제조예67 | 84±3.15 | 3.500 |
제조예18 | 55±7.75 | 2.208 | 제조예43 | 57±4.93 | 2.208 | 제조예68 | 93±4.55 | 3.875 |
제조예19 | 48±3.28 | 2.208 | 제조예44 | 51±4.78 | 2.208 | 제조예69 | 81±4.13 | 3.375 |
제조예20 | 57±7.87 | 2.208 | 제조예45 | 49±5.89 | 2.208 | 제조예70 | 97±17.13 | 4.040 |
제조예21 | 67±5.63 | 2.792 | 제조예46 | 58±5.14 | 2.417 | 제조예 71 | 81±11.23 | 3.375 |
제조예22 | 51±3.93 | 2.125 | 제조예47 | 53±7.79 | 2.208 | 제조예 72 | 84±9.12 | 3.500 |
제조예23 | 57±7.51 | 2.375 | 제조예48 | 52±7.12 | 2.167 | 제조예 73 | 86±7.7 | 3.583 |
제조예24 | 54±7.34 | 2.250 | 제조예49 | 51±8.17 | 2.125 | 제조예 74 | 87±3.14 | 3.625 |
제조예25 | 56±4.57 | 2.333 | 제조예50 | 54±5.42 | 2.250 | - | - | - |
구분 | 누적피부투과량 (μg/cm2) | 피부투과속도 (μg/cm2/hr) |
비교제조예1 | 6.28±0.63 | 0.260 |
비교제조예3 | 33±1.52 | 1.181 |
비교제조예4 | 79±0.58 | 2.832 |
비교제조예5 | 81±1.13 | 3.375 |
비교제조예6 | 12±0.94 | 0.519 |
Claims (16)
- 친수성 고분자 5 ~ 60 중량%, 유효성분 0.1 ~ 15 중량%, 습윤제 0.6 ~ 80 중량%, 용매 13.5 ~ 90 중량%, 경피투과촉진제 0.5 ~ 25 중량%, 자외선 개시제 0.01 ~ 2.0 중량% 및 자외선 가교제 0.01 ~ 2.0 중량%로 포함하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항 있어서, 상기 친수성 고분자는 폴리비닐알콜, 폴리비닐피롤리돈, 폴리비닐피롤리돈/비닐아세테이트 공중합체, 비닐에테르/무수말레인산 공중합체, 이소부틸렌/무수말레인산 공중합체, 메톡시에틸렌/무수말레인산 공중합체, 메타아크릴산/아크릴산부틸 공중합체, 알지네이트, 하이드록시에틸메타크릴레이트, 하이드록시에틸셀룰로오스, 하이드록시프로필셀룰로오스, 하이드록시프로필메틸셀룰로오스, 에틸셀룰로오스, 메틸셀룰로오스, 카르복시메틸셀룰로오스나트륨, 카르복시비닐 공중합체, 폴리에틸렌옥사이드, 폴리에틸렌글리콜, 폴리아크릴아마이드, 폴리하이드록시에틸메타크릴레이트, 폴리디옥솔란, 폴리아크릴산, 폴리아크릴산나트륨, 폴리비닐아크릴레이트, 폴리아크릴아세테이트 및 폴리비닐클로라이드 중에서 선택된 1종 이상을 포함하는 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, 상기 유효성분은 리도카인, 리도카인 염산염, 록소프로펜, 록소프로펜염, 케토프로펜, 플루르비프로펜, 디클로페낙, 디클로페낙염, 인도메타신, 피록시캄, 멜록시캄, 나프록센, 이부프로펜, 펠비낙, 멘톨, 살리실산 글리콜, 메틸 살리실레이트, 고추추출물, 노닐산바닐아미드, 비닐 부틸 에테르, 센텔라 아시아티카, 푸시딘산, 푸시딘산염, 아크리놀, 퓨에라리아 미리피카, 헤파린, 헤파린염 및 알란토인 중에서 선택된 1종 이상 포함하는 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, 상기 습윤제는 글리세린, 1,3-부틸렌글라이콜, 프로필렌글라이콜, 폴리프로필렌글라이콜, 솔비톨, 만니톨, 에틸렌글라이콜, 디에틸렌글라이콜, 폴리에틸렌글라이콜 및 히아룰론산 중에서 선택된 1종 이상을 포함하는 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, 상기 경피투과촉진제는 프로필렌글라이콜, 디프로필렌글라이콜, 폴리에틸렌글라이콜, 폴리옥시에틸렌모노올레이트, 폴리글리세릴디이소스테아레이트, 글리세린모노올레에이트, 폴리옥시에틸렌소르비탄, N-메틸-2-피롤리돈, N-카프릴릴-2-피롤리돈, N-도데실-2-피롤리돈, 라우릴피롤리돈, 라우릴알콜, 글리세롤 라우릴알코올, 올레일 알코올, 이소프로필 미리스트레이트, 소르비탄 모노올레이트, 프로필렌 모노라우레이트, 프로필렌 모노올레이트, 올레오일 마크로골 글리세라이드, 올레인산, 라우로일 마크로골 글리세라이드, 리놀레오일 마크로골 글리세라이드, 프로필렌글리콜 카프릴레이트, 프로필렌글리콜 카프레이트, 소르비탄 모노스테아레이트 모노올레이트, 글리세롤 모노라우레이트, 글리세롤 모노올레이트, 프로필렌글리콜 모노라우레이트, 프로필렌글리콜 모노카프릴레이트, 소르비탄 모노라우레이트, 라우릴 락테이트, 카프릴릭 트리글리세라이드, 카프릭 트리글리세라이드, 옥수수유 PEG-8 에스테르, 옥수수유 PEG-6 에스테르 및 트리아세틴 중에서 선택된 1종 이상을 포함하는 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, 상기 자외선 개시제는 케톤계 자외선 개시제, 티오크산톤계 자외선 개시제, 벤조페논계 자외선 개시제, 쿠마린계 자외선 개시제, 티아졸린계 자외선 개시제, 로다닌계 자외선 개시제 및 기타 자외선 개시제 중에서 선택된 1종 이상을 포함하며,상기 케톤계 자외선 개시제는 1-하이드록시-사이클로헥실-페닐-케톤, 2-하이드록시-2-메틸-1-페닐-1-프로판온, 2-하이드록시-1-[4-(2-하이드록시에톡시)페닐]-2-메틸-1-프로판온, 2-벤질-2-(디메틸아미노)-1-[4-(4-모포리닐)페닐]-1-부탄온, 2-메틸-1-[4-(메틸티오)페닐]-2-(4-모포리닐)-1-프로판온 중 1종 이상을 포함하며,상기 티오크산톤계 자외선 개시제는 티오크산톤, 2-이소프로필티오크산톤, 2-클로로티오크산톤, 1-클로로-4-프로폭시티오크산톤, 2-도데실티오크산톤, 2,4-디에틸티오크산톤, 2,4-디메틸티오크산톤, 1-메톡시-카보닐티오크산톤, 2-에톡시카보닐티오크산톤, 3-(2-메톡시에톡시카보닐)-티오크산톤, 4-부톡시카보닐티오크산톤, 3-부톡시카보닐-7-메틸티오크산톤, 1-시아노-3-클로로티오크산톤, 1-에톡시카보닐-3-클로로티오크산톤, 1-에톡시카보닐-3-에톡시티오크산톤, 1-에톡시카보닐-3-아미노티오크산톤, 1-에톡시카보닐-3-페닐설퍼릴티오크산톤, 3,4-디[2-(2-메톡시에톡시)에톡시카보닐]-티오크산톤, 1,3-디메틸-3-하이드록시-9H-티오크산톤-9-온 2-에틸헥실에테르, 1-에톡시카보닐-3-(1-메틸-1-모르폴리노에틸)-티오크산톤, 2-메틸-6-디메톡시메틸-티오크산톤, 2-메틸-6-(1,1-디메톡시벤질)-티오크산톤, 2-모르폴리노메틸티오크산톤, 2-메틸-6-모르폴리노메틸티오크산톤, N-알릴티오크산톤-3,4-디카복사미드, 1-페녹시티오크산톤, 6-에톡시카보닐-2-메톡시티오크산톤, 6-에톡시카보닐-2-메틸티오크산톤, 티오크산톤-2-카복실산 폴리에틸렌글리콜 에테르, 2-하이드록시-3-(3,4-디메틸-9-옥소-9H-티오크산톤-2-2-일옥시)-N,N,N-트리메틸-1-프로판아미늄클로라이드 중 1종 이상을 포함하고,상기 벤조페논계 자외선 개시제는 벤조페논, 4-페닐 벤조페논, 4-메톡시 벤조페논, 4,4'-디메틸 벤조페논, 4,4'-디클로로벤조페논, 4,4'-비스(디메틸아미노)-벤조페논, 4,4'-비스(디에틸아미노)벤조페논, 4,4'-비스(메틸에틸아미노)벤조페논, 4,4'-비스(p-이소프로필페녹시)벤조페논, 3,3'-디메틸-4-메톡시 벤조페논, 메틸-2-벤조일벤도에이트, 4-(2-하이드록시에틸티오)-벤조페논, 4-(4-톨릴티오)벤조페논, 1-[4-(4-벤조일-페닐설파닐)-페닐]-2-메틸-2(톨루엔-4-설포닐)-프로판-1-온, 4-벤조일-N,N,N-트리메틸벤젠메탄아미늄 클로라이드, 2-하이드록시-3-(4-벤조일-페녹시)-N,N,N-트리메틸-1-프로판아미늄 클로라이드 일수화물, 4-(13-아크릴로일-1,4,7,10,13-펜타옥사트리데실)-벤조페논, 4-벤조일-N,N-디메틸-N-[2-(1-옥소-2-프로페닐)옥시]에틸-벤젠메탄아미늄 클로라이드 중 1종 이상을 포함하며,상기 쿠마린계 자외선 개시제는 쿠마린 1, 쿠마린 2, 쿠마린 6, 쿠마린 7, 쿠마린 30, 쿠마린 102, 쿠마린 106, 쿠마린 138, 쿠마린 152, 쿠마린 153, 쿠마린 307, 쿠마린 314, 쿠마린 314T, 쿠마린 334, 쿠마린 337, 쿠마린 500, 3-벤조일 쿠마린, 3-벤조일-7-메톡시쿠마린, 3-벤조일-5,7-디메톡시쿠마린, 3-벤조일-5,7-디프로폭시쿠마린, 3-벤조일-6,8-디클로로쿠마린, 3-벤조일-6-클로로-쿠마린, 3,3'-카보닐-비스[5,7-디(프로폭시)-쿠마린], 3,3'-카보닐-비스(7-메톡시쿠마린), 3,3'-카보닐-비스(7-디에틸아미노-쿠마린), 3-이소부티로일쿠마린, 3-벤조일-5,7-디메톡시-쿠마린, 3-벤조일-5,7-디에톡시-쿠마린, 3-벤조일-5,7-디부톡시쿠마린, 3-벤조일-5,7-디(메톡시에톡시)-쿠마린, 3-벤조일-5,7-디(알릴옥시)쿠마린, 3-벤조일-7-디메틸아미노쿠마린, 3-벤조일-7-디에틸아미노쿠마린, 3-이소부티로일-7-디메틸아미노쿠마린, 3-벤조일-7-디에틸아미노쿠마린, 3-이소부티로일-7-디메틸아미노쿠마린, 5,7-디메톡시-3-(1-나프토일)-쿠마린, 5,7-디에톡시-3-(1-나프토일)-쿠마린, 3-벤조일벤조[f]쿠마린, 7-디에틸아미노- 3-티에노일쿠마린, 3-(4-시아노벤조일)-5,7-디메톡시쿠마린, 3-(4-시아노벤조일)-5,7-디프로폭시쿠마린, 7-디메틸아미노-3-페닐쿠마린, 7-디에틸아미노-3-페닐쿠마린 중 1종 이상을 포함하고,상기 티아졸린계 자외선 개시제는 3-(아로일메틸렌)-티아졸린류인 3-메틸-2-벤조일메틸렌-β-나프토티아졸린, 3-메틸-2-벤조일메틸렌-벤조티아졸린, 3-에틸-2-트로피오닐메틸렌-β-나프톨티아졸린 중 1종 이상을 포함하며,상기 로다닌계 자외선 개시제는 4-디메틸아미노벤즈알로다닌, 4-디에틸아미노벤즈알로다닌, 3-에틸-5-(3-옥틸-2-벤조티아졸리닐덴)-로다닌 중 1종 이상을 포함하고,상기 기타 자외선 개시제는 페닐아세토페논, 하이드록시 디메틸 아세토페논, 4,4'-비스(디메틸아미노)벤질, 메틸벤조일포메이트, 디페닐 (2,4,6-트리메틸벤조일)-포스핀 옥사이드, 페닐 비스(2,4,6-트리메틸 벤조일). 옥시-페닐-아세트산-2-[2-옥소-2-페닐-아세톡시-에톡시]-에틸 에스테르, 옥시-페닐-아세트산-2-[2-하이드록시-에톡시]-에틸 에스테르, 4-사이클로펜타디엔-1-일) 비스[2,6-디플루오로-3-(1-H-피롤-1-일)페닐] 티타니움, 2-아세틸나프탈렌, 2-나프탈알데하이드, 이오도니움염, 9.10-안트라퀴논, 안트라센, 피렌, 아미노피렌, 퍼릴렌, 펜안트렌, 펜안트렌퀴논, 9-플루오렌온, 디벤조수베론, 커쿠민, 크산톤, 티오미클러 케톤, 2,5-비스(4-디에틸아미노벤질리덴)사이클로펜타논, 2-(4-디메틸아미노-벤질리덴)-인단-1-온, 3-(4-디메틸아미노-페닐)-1-인단-5-일-프로페논과 같은 α-(4-디메틸아미노벤질리덴)케톤, 3-페닐티오프탈이미드, N-메틸-3,5-디(에틸티오)-프탈이미드, N-메틸-3,5-디(에틸티오)-프탈이미드, 페노티아진, 메틸페노티아진, N-페닐글리신, 트리에탄올아민, N-메틸디에탄올아민과 같은 아민, 에틸-p-디메틸아미노벤조에이트, 2-(디메틸아미노)에틸벤조에이트, 2-에틸헥실-p-디메틸아미노벤조에이트, 옥틸-파라-N,N-디메틸아미노벤조에이트, N-(2-하이드록시에틸)-N-메틸-파라-톨루이딘, 부톡시에틸 4-디메틸아미노벤조에이트, 4-디메틸아미노아세토페논, 트리에탄올아민, 메틸디에탄올아민, 디메틸아미노에탄올, 2-(디메틸아미노)에틸 벤조에이트, 폴리(프로필렌글리콜)-4-(디메틸아미노)벤조에이트 및 미클러케톤 중에서 선택된 1종 이상을 포함하는 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, 상기 자외선 가교제는 벤질 메타크릴레이트, 라우릴 메타크릴레이트, 이소데실 메타크릴레이트, 페녹시 메타크릴레이트, 2-하이드록시에틸 메타크릴레이트, 테트라하이드로 퍼퓨릴 메타크릴레이트, 세틸(C16) 메타크릴레이트, 스테아릴 메타크릴레이트, 메톡시피이지500 메타크릴레이트, 메톡시피이지600 메타크릴레이트, 메톡시피이지1000 메타크릴레이트, 1,6-헥산디올 디메타크릴레이트, 부타디엔 디메타크릴레이트, 네오펜틸글리콜 디메타크릴레이트, 에틸렌글리콜 디메타크릴레이트, 디에틸렌글리콜 디메타크릴레이트, 트리에틸렌글리콜 디메타크릴레이트, 테트라에틸렌글리콜 디메타크릴레이트, 비스페놀 A(이오)4 디메타크릴레이트, 비스페놀 A(이오)3 디메타크릴레이트, 비스페놀 A(이오)10 디메타크릴레이트, 비스페놀 A(이오)30 디메타크릴레이트, 1,3-부틸렌글리콜 디메타크릴레이트, 폴리에틸렌 글리콜 400 디메타크릴레이트, 폴리에틸렌 글리콜 200 디메타크릴레이트, 피피지1000(이오)15 디메타크릴레이트, 피피지1000(이오)3 디메타크릴레이트, 트리메틸올프로판 트리메타크릴레이트, 벤질 아크릴레이트, 라우릴 아크릴레이트, 이소데실 아크릴레이트, 페놀(이오) 아크릴레이트, 페놀(이오)2 아크릴레이트, 페놀(이오)4 아크릴레이트, 페놀(이오)6 아크릴레이트, 테트라하이드로 퍼퓨릴 아크릴레이트, 노닐 페놀(이오)4 아크릴레이트, 노닐 페놀(이오)8 아크릴레이트, 노닐 페놀(이오)2 아크릴레이트, 에톡시에톡시 에틸 아크릴레이트, 스테아릴 아크릴레이트, 1,6-헥산디올 이아크릴레이트, 1,6-헥산디올(이오) 디아크릴레이트, 부탄디올 디아크릴레이트, 하이드록시 피바릭 산 네오펜틸 글리콜 디아크릴레이트, 트리프로필렌글릴콜 디아크릴레이트, 디프로필렌 글리콜 디아크릴레이트, 비스페놀 A(이오)4 디아크릴레이트, 비스페놀 A(이오)3 디아크릴레이트, 트리사이클로데칸 디메탄올 디아크릴레이트, 데트라에틸렌 글리콜 디아크릴레이트, 폴리에틸렌 글리콜 400 디아크릴레이트, 폴리에틸렌 글리콜 200 디아크릴레이트, 폴리에틸렌 글리콜 300 디아크릴레이트, 폴리에틸렌 글리콜 600 디아크릴레이트, 폴리프로필렌 글리콜 400 디아크릴레이트, 폴리프로필렌 글리콜 750 디아크릴레이트, 비스페놀 A(이오)10 디아크릴레이트, 비스페놀 A(이오)30 디아크릴레이트, 트리스(2-하이드록시 에틸)이소시아누레이트 디아크릴레이트, 트리메틸올프로판 트리아크릴레이트, 트리메틸올프로판(이오)3 트리아크릴레이트, 트리메틸올프로판(이오)6 트리아크릴레이트, 트리메틸올프로판(이오)9 트리아크릴레이트, 트리메틸올프로판(이오)15 트리아크릴레이트, 글리세린 프로폭시레이티드 트리아크릴레이트, 펜타에리스리톨 트리아크릴레이트, 트리메틸올프로판(피오)3 트리아크릴레이트, 트리스(2-하이드록시 에틸)이소시아누레이트 트리아크릴레이트, 펜타에리스리톨 N-이오 테트라아크릴레이트, 펜타에리스리톨 테트라아크릴레이트, 디펜타에리스리톨 펜타아크릴레이트, 디펜타에리스리톨 헥사아크릴레이트, 카프로락톤 아크릴레이트, O-페닐페놀 이오 아크릴레이트, 메틸렌 비스 아크릴아마이드 중에서 선택된 1종 이상을 포함하는 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항에 있어서, pH 3 ~ 9인 것을 특징으로 하는 경피투여용 자외선 경화형 하이드로젤 수지.
- 제1항 내지 제8항 중 어느 한 항의 하이드로젤 수지의 자외선 경화물이며,대한민국약전 반창고항의 점착력시험에 의거하여 박리강도 측정시, 점착력이 50 ~ 120 gf인 것을 특징으로 경피투여용 자외선 경화형 하이드로젤.
- 제9항의 경피투여용 자외선 경화형 하이드로젤을 포함하는 약물층; 및폴리우레탄 필름, 다공성 필름, 천공 필름, 직물, 부직포 및 폼(foam) 중에서 선택된 1종 이상을 포함하는 약물 지지층;을 포함하는 카타플라스마제.
- 제10항에 있어서, 상기 약물층은 평균두께 20 ~ 2,000㎛이고, 상기 약물 지지층은 평균두께 7 ~ 500㎛인 것을 특징으로 하는 카타플라스마제.
- 제10항에 있어서, 박리층을 더 포함하며,박리층, 약물층 및 약물 지지층이 순차적으로 적층된 것을 특징으로 하는 카타플라스마제.
- 제12항에 있어서, 상기 박리층은 평균두께 15㎛ ~ 500㎛이며,상기 박리층은 실리콘 수지 또는 불소 수지가 코팅된 고분자 필름을 포함하고,상기 고분자 필름은 폴리에스테르; 폴리비닐클로라이드; 폴리비닐리덴클로라이드; 폴리에틸렌테레프탈레이트; 및 이들의 공중합체; 중에서 선택된 1종 이상의 고분자 화합물을 포함하는 것을 특징으로 하는 카타플라스마제.
- 제10항에 있어서, 상기 카타플라스마제는 소염, 진통용 카타플라스마제인 것을 특징으로 하는 카타플라스마제.
- 친수성 고분자, 유효성분, 습윤제, 용매, 경피투과촉진제, 자외선 개시제 및 자외선 가교제를 혼합 및 교반하여 하이드로젤 수지를 제조하는 1단계;상기 하이드로젤 수지를 박리필름 상에 코팅시키는 2단계;코팅된 하이드로젤 수지 상에 지지체를 적층시키는 3단계;지지체 방향으로 2,000 ~ 8,000mW/㎠ 세기의 자외선을 3 ~ 10 분간 조사시켜서 하이드로젤 수지를 경화시키는 4단계;를 포함하는 것을 특징으로 하는 카타플라스마제의 제조방법.
- 제15항에 있어서, 상기 하이드로겔 수지는 친수성 고분자 5 ~ 60 중량%, 유효성분 0.1 ~ 15 중량%, 습윤제 0.6 ~ 80 중량%, 용매 13.5 ~ 90 중량%, 경피투과촉진제 0.5 ~ 25 중량%, 자외선 개시제 0.01 ~ 2.0 중량% 및 자외선 가교제 0.01 ~ 2.0 중량%로 포함하는 카타플라스마제의 제조방법.
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Cited By (2)
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CN112584889A (zh) * | 2018-05-30 | 2021-03-30 | 王子元 | 非侵入性转运方法 |
CN115444837A (zh) * | 2022-10-13 | 2022-12-09 | 湖南九典制药股份有限公司 | 一种洛索洛芬经皮给药系统及其制备方法 |
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CN108697657A (zh) | 2018-10-23 |
JP2019507142A (ja) | 2019-03-14 |
CN114129544A (zh) | 2022-03-04 |
KR101717699B1 (ko) | 2017-03-17 |
JP2020158514A (ja) | 2020-10-01 |
US11382868B2 (en) | 2022-07-12 |
US20190046463A1 (en) | 2019-02-14 |
JP6909520B2 (ja) | 2021-07-28 |
JP6755957B2 (ja) | 2020-09-16 |
EP3415141A4 (en) | 2019-10-09 |
EP3415141A1 (en) | 2018-12-19 |
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