WO2015025767A1 - Patch adhésif - Google Patents

Patch adhésif Download PDF

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Publication number
WO2015025767A1
WO2015025767A1 PCT/JP2014/071219 JP2014071219W WO2015025767A1 WO 2015025767 A1 WO2015025767 A1 WO 2015025767A1 JP 2014071219 W JP2014071219 W JP 2014071219W WO 2015025767 A1 WO2015025767 A1 WO 2015025767A1
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WO
WIPO (PCT)
Prior art keywords
adhesive
patch
pressure
drug
mass
Prior art date
Application number
PCT/JP2014/071219
Other languages
English (en)
Japanese (ja)
Inventor
藤田　直子
知宏 篠田
Original Assignee
久光製薬株式会社
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 久光製薬株式会社 filed Critical 久光製薬株式会社
Priority to JP2015532825A priority Critical patent/JP6359014B2/ja
Publication of WO2015025767A1 publication Critical patent/WO2015025767A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7069—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics

Definitions

  • the present invention relates to a patch.
  • Pruritus in hemodialysis patients is a disease in which the patient's QOL is greatly impaired due to the fact that it induces strong generalized itching without inflammation and is unable to get enough sleep at night.
  • nalfrafin hydrochloride which is a ⁇ -type opioid receptor agonist compound is known (see, for example, Patent Document 1).
  • Nalfurafine hydrochloride is prescribed as an oral agent for intractable pruritus associated with hemodialysis.
  • an object of the present invention is to provide a nalflaphine-containing preparation that exhibits excellent preparation stability.
  • the present invention is a patch comprising a support and a pressure-sensitive adhesive layer containing a drug and a pressure-sensitive adhesive disposed on at least one side of the support, wherein the drug is a free form of nalfraphine or a salt thereof.
  • the adhesive is at least one selected from a styrene block copolymer adhesive, a polyisobutylene adhesive, and a silicone adhesive.
  • the drug contains, as nalflavine, only the free form of nalflaphine, or the free form of nalflaphine and a salt thereof.
  • the pressure-sensitive adhesive layer containing such a drug can exhibit more excellent formulation stability.
  • the pressure-sensitive adhesive layer may be obtained by mixing a free body of nalfurafine with a pressure-sensitive adhesive, or may be obtained by mixing a salt of nalfrafin with a pressure-sensitive adhesive together with a desalting agent. .
  • the salt of narfrafin with an adhesive together with a desalting agent it exists in the form of a salt that is excellent in handleability until formulation, and it is converted into a free form by a desalting agent in the formulation, so it is more efficient.
  • the formulation can be prepared.
  • the desalting agent is preferably at least one selected from sodium acetate and sodium hydroxide, and more preferably sodium acetate.
  • the content of the desalting agent is preferably 0.3 to 5 mol per 1 mol of the salt of narfrafin.
  • nalflaphine-containing preparation that exhibits excellent preparation stability.
  • the patch according to the present embodiment is a patch comprising a support and a pressure-sensitive adhesive layer containing a drug and a pressure-sensitive adhesive (drug-containing pressure-sensitive adhesive layer) disposed on at least one side of the support.
  • the drug includes a free form of nalflaphine or a salt thereof, and the adhesive is at least one selected from a styrene block copolymer adhesive, a polyisobutylene adhesive, and a silicone adhesive.
  • a stretchable or non-stretchable material that can be usually used for a patch is used.
  • a film or sheet formed of a synthetic resin such as polyethylene terephthalate, polyethylene, polypropylene, polybutadiene, ethylene vinyl acetate polymer, polyvinyl chloride, polyester, nylon, polyurethane, or a laminate thereof, or a porous film A foam, a woven fabric and a non-woven fabric, or a paper material can be suitably used.
  • the drug-containing pressure-sensitive adhesive layer contains at least one selected from a styrene block copolymer pressure-sensitive adhesive, a polyisobutylene pressure-sensitive adhesive, and a silicone pressure-sensitive adhesive. These pressure-sensitive adhesives may be used alone or in combination of two or more. Examples of the pressure-sensitive adhesive used in combination of two or more include an embodiment in which a styrene block copolymer pressure-sensitive adhesive and a polyisobutylene pressure-sensitive adhesive are combined.
  • the styrene block copolymer-based pressure-sensitive adhesive is obtained by adding a tackifier or the like to a styrene block copolymer.
  • the styrene block copolymer adhesive include styrene-isoprene-styrene (SIS) adhesive, styrene-butadiene-styrene (SBS) adhesive, styrene-ethylenebutylene-styrene (SEBS) adhesive, and styrene- And ethylene propylene-styrene (SEPS) pressure sensitive adhesive.
  • SIS styrene-isoprene-styrene
  • SBS styrene-butadiene-styrene
  • SEBS styrene-ethylenebutylene-styrene
  • SEPS styrene- And ethylene propylene-styrene
  • tackifier examples include ester gum (trade name, manufactured by Arakawa Chemical Co., Ltd.), Harrier Star (trade name, manufactured by Harima Kasei Co., Ltd.), pentalin (trade name, manufactured by Eastman Chemical Company), and formal (Eastman Chemical). Rosin resins such as YS resin (Yasuhara Chemical Co., trade name), terpene resins such as picolite (Loose and Dilworth Co., trade name), Alcon (Arakawa Chemical Co., Ltd.
  • tackifiers may be used alone or in combination of two or more.
  • the content of the tackifier can be appropriately set by those skilled in the art in consideration of sufficient adhesive strength of the patch and local irritation at the time of peeling.
  • the upper limit of the content of the tackifier is preferably, for example, 10% by mass or more, more preferably 15% by mass or more, based on the total mass of the adhesive layer, and 20% by mass. % Or more is particularly preferable.
  • the lower limit of the content of the tackifier is preferably, for example, 90% by mass or less, more preferably 70% by mass or less, based on the total mass of the adhesive layer, and 60% by mass or less. It is particularly preferred.
  • the content of the tackifier is preferably 10 to 90% by mass, more preferably 15 to 70% by mass, and particularly preferably 20 to 60% by mass based on the total mass of the adhesive layer. preferable.
  • the polyisobutylene-based pressure-sensitive adhesive is one obtained by adding a plasticizer or the like to polyisobutylene (PIB) to impart adhesiveness.
  • plasticizer examples include petroleum oils such as paraffinic process oil, naphthenic process oil and aromatic process oil, vegetable oils such as olive oil, camellia oil, castor oil, tall oil and peanut oil, dibutyl phthalate and dioctyl.
  • examples thereof include dibasic acid esters such as phthalate, liquid rubbers such as polybutene and liquid isoprene rubber, squalane, squalene, diethylene glycol, polyethylene glycol, propylene glycol and dipropylene glycol. These can be used individually by 1 type or in combination of 2 or more types.
  • liquid paraffin and polybutene are particularly preferable.
  • the content of the plasticizer in the drug-containing pressure-sensitive adhesive layer can be appropriately adjusted by those skilled in the art in consideration of maintaining sufficient adhesive strength as a pressure-sensitive adhesive.
  • the upper limit of the content of the plasticizer is, for example, preferably 1% by mass or more, more preferably 2% by mass or more, based on the total mass of the drug-containing pressure-sensitive adhesive layer. It is particularly preferable that the content is at least mass%.
  • the lower limit of the content of the plasticizer is, for example, preferably 60% by mass or less, more preferably 50% by mass or less, further preferably 40% by mass or less, and 20% by mass or less. It is particularly preferred.
  • the plasticizer content is preferably 1 to 60% by mass, more preferably 2 to 50% by mass, and more preferably 3 to 40% by mass based on the total mass of the drug-containing pressure-sensitive adhesive layer. Further preferred is 3 to 20% by mass.
  • the silicone-based adhesive is an adhesive made of a condensation reaction product of dimethylpolysiloxane and a three-dimensional silicate resin, and examples thereof include Bio-PSA 7-4102 (trade name, manufactured by Dow Corning). Can do.
  • these various adhesives may be used individually by 1 type, and may be used in combination of 2 or more type. Further, the content of the pressure-sensitive adhesive can be appropriately set for those skilled in the art in consideration of the formation and adhesion of the drug-containing pressure-sensitive adhesive layer and the tissue permeability of the active ingredient.
  • using a combination of a styrene block copolymer adhesive and a polyisobutylene adhesive not only further improves the formulation stability of narfrafin, but also improves the cohesive strength of the patch. Also, the adhesive strength and the adhesion to the skin tend to be further improved.
  • the ratio of the styrene block copolymer-based pressure-sensitive adhesive and the polyisobutylene-based pressure-sensitive adhesive is preferably in the range of 1:10 to 10: 1 with respect to the styrene block copolymer, preferably from 1: 1 to 9: 1. More preferably, it is in the range of 6: 4 to 8: 1.
  • the content of the tackifier is not particularly limited, but may be, for example, 0.4 times or more based on the content of the plasticizer, It may be 0.5 times or more, 1 time or more, 1.5 times or more, 2 times or more, or 2.5 times or more It may be 3 times or more, or 3.5 times or more.
  • the upper limit of the content of the tackifier is not particularly limited. For example, it may be 100 times or less, 50 times or less, or 10 times or less based on the content of the plasticizer. It may be 5 times or less, or 4 times or less.
  • the upper limit of the content of the adhesive is, for example, preferably 10% by mass or more, more preferably 15% by mass or more, and more preferably 20% by mass or more based on the total mass of the drug-containing adhesive layer. More preferably.
  • the lower limit of the content of the pressure-sensitive adhesive is, for example, preferably 99% by mass or less, more preferably 90% by mass or less, and further preferably 85% by mass or less.
  • the content of the pressure-sensitive adhesive may be 10 to 99% by mass, or 15 to 90% by mass based on the total mass of the drug-containing pressure-sensitive adhesive layer. In particular, the content is preferably 20 to 85% by mass.
  • the drug-containing pressure-sensitive adhesive layer contains a free form of narfrafin or a salt thereof. Furthermore, other drugs may be included as necessary. In particular, it is preferable to include a free form of narfrafin. By including a free form of nalfurafine, the formulation stability of nalfurafine can be further improved.
  • the phrase “containing a free form of nalfurafine” is sufficient if a free form of nalfurafine is present in the drug-containing pressure-sensitive adhesive layer, and a salt of nalfurafine may be present together.
  • nalfurafine In the production of the drug-containing pressure-sensitive adhesive layer, a free form of nalfurafine may be used as a raw material, or a salt of nalfurafine may be used as a raw material together with a desalting agent.
  • a salt of narfrafin When a salt of narfrafin is used as a raw material together with a desalting agent, at least a part of the salt is converted into a free form during or after the manufacture of the patch.
  • the salt of nalfurafine is not particularly limited as long as it is a pharmaceutically acceptable salt, but is preferably an acid addition salt of nalfurafine from the viewpoint of storage stability before producing the patch.
  • acid addition salts include hydrochloride, acetate, maleate, oxalate, citrate, hydroiodide, hydrobromide, mesylate, tartrate, succinate, etc. be able to.
  • the desalting agent used together with the salt of nalfurafine a basic substance is preferable when the acid addition salt of nalfurafine is converted into a free form.
  • a desalting agent include sodium acetate and sodium hydroxide, among which sodium acetate is preferable.
  • the desalting agent is used to convert at least a part of the salt of nalfurafine into a free form in the preparation. It may be converted into a free body as long as stability can be improved. From such a viewpoint, the upper limit of the content of the desalting agent is preferably 0.3 mol or more, more preferably 0.5 mol or more, and more preferably 1 mol or more with respect to 1 mol of the salt of nalfurafine.
  • the lower limit of the content of the desalting agent is preferably 5 mol or less, more preferably 3 mol or less, and even more preferably 2 mol or less.
  • the content of the desalting agent is preferably 0.3 to 5 moles, more preferably 0.5 to 3 moles, and more preferably 0.5 to 2 moles with respect to 1 mole of the salt of narfrafin. Is particularly preferred.
  • the desalting agent may be blended once during the production process, or may be divided into several times.
  • Two or more drug-containing pressure-sensitive adhesive layers may be laminated on the support, and may be laminated not only on one side of the support but also on both sides.
  • the drug-containing pressure-sensitive adhesive layer may contain an absorption accelerator, a filler, an ultraviolet absorber, an antioxidant, a crosslinking agent, a preservative, etc., as necessary. Moreover, you may further contain the tackifier and plasticizer which were mentioned above.
  • aliphatic alcohols such as isostearyl alcohol, fatty acids such as capric acid, fatty acid derivatives such as propylene glycol monolaurate and isopropyl myristate, propylene glycol, polyethylene glycol, diethanolamine laurate and the like can be suitably used.
  • fatty acids such as capric acid
  • fatty acid derivatives such as propylene glycol monolaurate and isopropyl myristate
  • propylene glycol polyethylene glycol, diethanolamine laurate and the like
  • the content of the absorption enhancer can be appropriately set by those skilled in the art in consideration of sufficient permeability of the active ingredient to the tissue as a preparation, local irritation, and the like.
  • the upper limit of the content of the absorption accelerator is, for example, preferably 1% by mass or more, more preferably 3% by mass or more, based on the total mass of the patch.
  • the above is particularly preferable.
  • the lower limit of the content of the absorption accelerator is, for example, preferably 30% by mass or less, more preferably 20% by mass or less, and particularly preferably 15% by mass or less.
  • the content of the absorption accelerator is preferably 1 to 30% by mass, more preferably 3 to 20% by mass, and further preferably 3 to 15% by mass based on the total mass of the patch. It is particularly preferably 5 to 15% by mass.
  • filler examples include silicates such as aluminum silicate and magnesium silicate, aluminum hydroxide, aluminum carbonate, magnesium carbonate, silicic acid, barium sulfate, calcium sulfate, calcium zincate, zinc oxide, titanium oxide and the like. .
  • silicates such as aluminum silicate and magnesium silicate, aluminum hydroxide, aluminum carbonate, magnesium carbonate, silicic acid, barium sulfate, calcium sulfate, calcium zincate, zinc oxide, titanium oxide and the like.
  • ultraviolet absorbers examples include p-aminobenzoic acid derivatives, anthranilic acid derivatives, salicylic acid derivatives, coumarin derivatives, amino acid derivatives, imidazoline derivatives, pyrimidine derivatives, dioxane derivatives and the like.
  • the above fillers, ultraviolet absorbers, antioxidants, crosslinking agents, preservatives are in total, preferably 5% by mass or less, more preferably 3% by mass or less, based on the total mass of the drug-containing pressure-sensitive adhesive layer. Particularly preferably, it is blended in an amount of 1% by mass or less.
  • the method for producing a patch according to the present embodiment includes, for example, a step of obtaining a mixture by dissolving or dispersing a drug and an adhesive in a solvent, and a step of arranging the mixture on at least one side of a support.
  • a pressure-sensitive adhesive solution a free form of nalflavine or a salt thereof, and, if necessary, a desalting agent and other components are dissolved or dispersed in a solvent, That is, a mixture for forming a drug-containing pressure-sensitive adhesive layer is obtained.
  • a solvent e.g., toluene, hexane, ethyl acetate, cyclohexane, heptane, butyl acetate, ethanol, methanol, xylene, isopropanol and the like can be used. These are appropriately selected according to the components to be dissolved or dispersed, and can be used alone or in combination of two or more.
  • Specific embodiments of the step of obtaining the above mixture include an embodiment in which a free body of nalfurafine is mixed with an adhesive, an embodiment in which a salt of nalfurafine is mixed with an adhesive, and a salt of nalfurafine is mixed with an adhesive together with a desalting agent. An aspect etc. are mentioned.
  • Examples of the pressure-sensitive adhesive and desalting agent include the same as those described above, and the content of these is preferably as described above.
  • the obtained mixture for forming a drug-containing pressure-sensitive adhesive layer is directly spread on a support to form a drug-containing pressure-sensitive adhesive layer, or is spread on a release-treated paper or film to form a drug.
  • a containing pressure-sensitive adhesive layer is formed, a support is placed thereon, and the drug-containing pressure-sensitive adhesive layer is pressure-transferred onto the support.
  • the patch according to this embodiment obtained as described above exhibits excellent formulation stability.
  • each patch was packaged with an aluminum wrapping material and sealed. After the sealed patch was stored at 60 ° C. and 75% RH for 2 weeks, the drug content in the preparation was measured by a high performance liquid chromatograph (HPLC) method. The ratio of the drug content after storage to the drug content immediately after sealing was calculated, and the stability was evaluated.
  • HPLC high performance liquid chromatograph
  • Example 1 A mixture obtained by mixing narfraphine free form with methanol in advance is added to SIS, an alicyclic saturated hydrocarbon resin (Arcon P100; manufactured by Arakawa Chemical Co., Ltd., trade name) and a liquid paraffin toluene solution, and mixed. A SIS adhesive solution was obtained. This adhesive solution is coated on a release paper, the solvent is removed by drying, and a drug-containing adhesive layer is formed. Then, a PET film support is placed thereon, and the drug-containing adhesive layer is pressure-transferred. As a result, a patch was obtained. Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 2 A patch was obtained in the same manner as in Example 1 except that as the mixture, a mixture obtained by mixing nalflaphine hydrochloride and sodium acetate as a desalting agent in methanol was used. The content of sodium acetate as a desalting agent was 1.9 mol with respect to 1 mol of nalfurafine hydrochloride. Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 3 A patch was obtained in the same manner as in Example 2 except that an adhesive solution was obtained using SIS and PIB.
  • Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 4 A patch was obtained in the same manner as in Example 2 except that an adhesive solution was obtained using a toluene solution of PIB and liquid paraffin in place of the SIS, alicyclic saturated hydrocarbon resin Alcon P100 and liquid paraffin in toluene.
  • Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 5 A patch was obtained in the same manner as in Example 3 except that sodium hydroxide was used instead of sodium acetate as the desalting agent.
  • the content of sodium hydroxide as a desalting agent was 1.0 mol with respect to 1 mol of nalfurafine hydrochloride.
  • Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 6 A patch was obtained in the same manner as in Example 1 except that a mixture of nalflavine hydrochloride mixed with methanol was used as the mixture. Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 7 A patch was obtained in the same manner as in Example 6 except that an adhesive solution was obtained using SIS and PIB.
  • Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 8 A patch was obtained in the same manner as in Example 6 except that the adhesive solution was obtained using PIB and liquid paraffin instead of SIS, alicyclic saturated hydrocarbon resin Alcon P100 and liquid paraffin in toluene. .
  • Table 1 shows the blending amount of the patch according to this example and the results of stability evaluation.
  • Example 9 A mixture prepared by previously mixing methanol with a free form of narfrafin was added to and mixed with the silicone-based adhesive Bio-PSA 7-4102 to obtain an adhesive solution. This adhesive solution is coated on a release paper, the solvent is removed by drying, and a drug-containing adhesive layer is formed. Then, a PET film support is placed thereon, and the drug-containing adhesive layer is pressure-transferred. As a result, a patch was obtained. Table 2 shows the blending amount of the patch according to this example and the results of the stability evaluation.
  • Example 10 A patch was obtained in the same manner as in Example 9, except that a mixture of nalflaphine hydrochloride and sodium acetate as a desalting agent mixed with methanol was used as the mixture.
  • the content of sodium acetate as a desalting agent was 1.9 mol with respect to 1 mol of nalfurafine hydrochloride.
  • Table 2 shows the blending amount of the patch according to this example and the results of the stability evaluation.
  • Example 11 A patch was obtained in the same manner as in Example 9, except that a mixture obtained by mixing nalflaphine hydrochloride with methanol was used as the mixture.
  • Table 2 shows the blending amount of the patch according to this example and the results of the stability evaluation.
  • Comparative Example 2 A patch was obtained in the same manner as in Comparative Example 1 except that a mixture in which methanol was mixed with nalflaphine hydrochloride and sodium acetate as a desalting agent as a mixture was used. The content of sodium acetate as a desalting agent was 1.9 mol with respect to 1 mol of nalfurafine hydrochloride. Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • Comparative Example 3 A patch was obtained in the same manner as in Comparative Example 2, except that DURO-TAK 87-235A (trade name, manufactured by Henkel) was used instead of DURO-TAK 87-2510 as the acrylic adhesive. Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • Comparative Example 4 A patch was obtained in the same manner as in Comparative Example 2, except that DURO-TAK 87-4098 (trade name, manufactured by Henkel) was used instead of DURO-TAK 87-2510 as the acrylic adhesive.
  • Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • Comparative Example 5 A patch was obtained in the same manner as in Comparative Example 1 except that a mixture of nalflavine hydrochloride mixed with methanol was used as the mixture. Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • Comparative Example 6 A patch was obtained in the same manner as in Comparative Example 5 except that DURO-TAK 87-235A was used instead of DURO-TAK 87-2510 as the acrylic adhesive.
  • Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • Comparative Example 7 A patch was obtained in the same manner as in Comparative Example 5, except that DURO-TAK 87-4098 was used instead of DURO-TAK 87-2510 as the acrylic adhesive.
  • Table 3 shows the blending amount of the patch according to this comparative example and the results of the stability evaluation.
  • the solution formulation was prepared by mixing nalfrafin hydrochloride with physiological saline.
  • the prepared solution formulation was filled into a glass vial and sealed. Immediately after sealing and after storage for 2 weeks at 60 ° C. and 75% RH, the drug content in the preparation was measured by high performance liquid chromatography (HPLC) method to evaluate the stability.
  • Table 5 shows the amount of the solution preparation and the results of the stability evaluation.
  • the ointment is a free form of nalflaphine or hydrochloride (in the case of hydrochloride, including the case of adding or not adding a desalting agent) and liquid paraffin well mixed in a mortar, and then heated white petrolatum It was prepared by mixing with.
  • the prepared ointment was filled in an aluminum tube and sealed. Immediately after sealing and after storage for 2 weeks at 60 ° C. and 75% RH, the drug content in the preparation was measured by high performance liquid chromatography (HPLC) method to evaluate the stability. Table 6 shows the blending amount of the ointment and the results of the stability evaluation.
  • HPLC high performance liquid chromatography
  • nalflaphine-containing preparation that exhibits excellent preparation stability.

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Abstract

　L'invention concerne un patch adhésif qui comporte: une base; une couche adhésive située sur au moins une face de la base et contenant une substance médicamenteuse et un adhésif. La substance médicamenteuse contient une base libre de Nalfurafine ou un sel de celle-ci et l'adhésif est un adhésif d'au moins une sorte choisi parmi un adhésif de type polymère séquencé styrène, un adhésif de type polyisobutylène et un adhésif de type silicone.
PCT/JP2014/071219 2013-08-21 2014-08-11 Patch adhésif WO2015025767A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2015532825A JP6359014B2 (ja) 2013-08-21 2014-08-11 貼付剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013-171383 2013-08-21
JP2013171383 2013-08-21

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WO2015025767A1 true WO2015025767A1 (fr) 2015-02-26

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JP (1) JP6359014B2 (fr)
TW (1) TW201542247A (fr)
WO (1) WO2015025767A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2015025766A1 (ja) * 2013-08-21 2017-03-02 久光製薬株式会社 貼付剤
WO2017094337A1 (fr) 2015-12-04 2017-06-08 ニチバン株式会社 Timbre transdermique
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WO2017094337A1 (fr) 2015-12-04 2017-06-08 ニチバン株式会社 Timbre transdermique
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