WO2001010435A1 - Timbre - Google Patents

Timbre Download PDF

Info

Publication number
WO2001010435A1
WO2001010435A1 PCT/JP2000/005269 JP0005269W WO0110435A1 WO 2001010435 A1 WO2001010435 A1 WO 2001010435A1 JP 0005269 W JP0005269 W JP 0005269W WO 0110435 A1 WO0110435 A1 WO 0110435A1
Authority
WO
WIPO (PCT)
Prior art keywords
weight
parts
patch
penilylamide
acid
Prior art date
Application number
PCT/JP2000/005269
Other languages
English (en)
Japanese (ja)
Inventor
Eiichiro Manabe
Takashi Kamakura
Original Assignee
Taisho Pharmaceutical Co., Ltd.
Teikoku Seiyaku Co., Ltd.
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 Taisho Pharmaceutical Co., Ltd., Teikoku Seiyaku Co., Ltd. filed Critical Taisho Pharmaceutical Co., Ltd.
Priority to AU63196/00A priority Critical patent/AU6319600A/en
Publication of WO2001010435A1 publication Critical patent/WO2001010435A1/fr

Links

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide

Definitions

  • the present invention relates to a hypoallergenic warming patch.
  • Conventional technology
  • Patches are an excellent dosage form in that the drug to be incorporated can be continuously transdermally administered.
  • patches also have some problems. The most frequent of these problems is skin irritation occurring at the site where the patch was applied to patients.
  • a warming ingredient represented by pepper extract, nonyl acid phenylylamide, etc. is combined, it may further irritate the skin and cause rashes. .
  • An object of the present invention is to provide a patch having an excellent warming effect and less skin irritation. Disclosure of the invention
  • the present inventor has conducted intensive studies in view of the above-mentioned object, and as a result, when combined with cabsaicinoid and nonyluric acid perilylamide, a sufficient warm stimulus was obtained even at a low dose with little skin irritation. And found that the present invention was completed.
  • the present invention relates to a patch containing a water-soluble polymer base, in which cabsaicinoid and nonyl acid penilylamide are blended, and the amount of capsaicinoid in 100 g of the base is [X] (g).
  • the blending amount of nonyl acid penilylamide is [Y] (g)
  • [X] is 0.002 to 0.05
  • [Y] is 0.0005 to 0.05.
  • a patch characterized in that the patch is 07.
  • the present invention provides a patch containing a water-soluble polymer base, in which cabsaicinoid and nonyl acid penilylamide are blended, and the amount of the capsaicinoid in 100 g of the base is [X] (g).
  • the blending amount of nonyl acid penilylamide is [Y] (g)
  • [Y] is 0.005 to 0.003
  • [X] +0.6 X [Y] Is 0.0000 to 0.0208.
  • the present invention provides a patch containing a water-soluble polymer base, in which cabsaicinoid and nonyl acid penilylamide are compounded, and the amount of capsaicinoid in 100 g of the base is [X] (g).
  • the amount of nonyl acid penilylamide is [Y] (g) Wherein [Y] is 0.0005 to 0.007, and [ ⁇ ] + 0.6 X [ ⁇ ] is 0.0046 to 0.0052. .
  • the present invention is characterized in that cabsaicinide and nonyl acid penilylamide are blended in a water-soluble polymer base, and that the blending amount is set to a low dose.
  • capsaicinoid means capsaicin and homologues thereof, and specific examples include capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homodihydrocapsaicin and the like.
  • the turnip cycinoid is preferably derived from a pepper, and may include pepper shakes, pepper powder, and pepper tincture.
  • [X] is preferably 0.0002 or more from the viewpoint of warming effect and 0.005 or less from the viewpoint of reducing skin irritation.
  • [Y] is preferably 0.0005 or more from the viewpoint of warm feeling effect, and from the viewpoint of reducing skin irritation. It is preferably 0.007 or less. Furthermore, [Y] is preferably 0.0005 to 0.003 in the patch for treating stiff shoulder, and [Y] is preferably 0.0005 to 0.007 in the patch for treating back pain.
  • the composition of the water-soluble polymer base is not particularly limited, and any composition may be used.
  • gelatin polyacrylic acid, polyacrylic acid salts such as sodium polyacrylate, partially neutralized polyacrylic acid, starch polyacrylate, polyvinyl alcohol, polyvinylpyrrolidone, polyacrylic acid copolymer, hydroxypropyl Cellulose, carmellose sodium, methylcellulose
  • examples thereof include a maleic anhydride copolymer, an N-vinyl acetate copolymer, and a methacrylic acid copolymer.
  • the water content of the water-soluble polymer base is preferably 35 to 80% by weight based on the whole base in view of the cooling effect when applied.
  • the present invention is also applicable to the following ingredients: menthol, menthol, heart oil, forceful, maleink mouth feniramine, diphenhydramine hydrochloride, azulene, sodium guaizulene sulfonate, glycyrrhetinic acid Drugs such as glycyrrhizic acid and its salts, tocopherol acetate, and d1-camphor can also be added.
  • base components such as excipients (silicic acid anhydride, kaolin, cyclodextrin, zinc oxide, titanium oxide, aluminum silicate moisturizer, etc.), moisturizers (glycerin, diglycerin, Synthetic high molecular compounds such as triglycerin, propylene glycol, butylene glycol, polyethylene glycol, d_sorbitol, etc., adhesives (Ripoxyvinyl polymer, polyvinyl alcohol) or natural high molecular compounds such as gum arabic and xanthan cancer ), Surfactants (glycerin fatty acid ester, polyoxyethylene castor oil, polyoxyethylene hardened castor oil, sorbin fatty acid ester, polysorbate 80, polysorbate 60, sorbitan sesquioleate, etc.) Can be formulated aluminum hydroxide, aluminum glycinate, dihydroxy aluminum ⁇ amino acetate, such as polyvalent metal compounds such as synthetic hydrotalcite), and the like.
  • excipients sicic acid
  • an absorption promoter if necessary, an absorption promoter, a preservative, an antioxidant, a coloring agent, and the like can be added.
  • the patch of the present invention can be spread on a support, a liner, or the like used for a conventional patch to form a patch by a usual method.
  • the support is a flexible woven fabric, nonwoven fabric, film, or sheet, and particularly preferably a breathable material having elasticity in all directions.
  • Example 2 to 8 were prepared in the same manner as in Example 1 with the following compositions. Components not shown in the table were blended in the same amounts as in Example 1. Table 1 (Unit: parts by weight)
  • Castor oil 1.0 part by weight, polyvinyl alcohol 2.0 parts by weight, starch acrylate 2.5 parts by weight, sodium polyacrylate 6.0 parts by weight, hydroxypyrucel cellulose 0.3 parts by weight, propylene glycol 15 Parts by weight, 3.0 parts by weight of kaolin, 0.6 parts by weight of tartaric acid, 0.5 parts by weight of silicon dioxide, and an appropriate amount of purified water are uniformly dispersed, and one liquid is added and mixed uniformly to obtain a plaster for a patch.
  • Example 1 1 3.0 parts by weight of polyvinyl alcohol, 6.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of hydroxypropyl cellulose, 25 parts by weight of 70% D-sorbitol, 3.0 parts by weight of kaolin, 1.2 parts of tartaric acid Parts by weight, 0.12 parts by weight of sodium edetate, and an appropriate amount of purified water were uniformly dispersed, and one part of the solution was added and uniformly mixed to obtain a plaster for a patch. This was uniformly spread on a nonwoven fabric, and a patch was obtained by an ordinary method.
  • Example 1 1 3.0 parts by weight of polyvinyl alcohol, 6.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of hydroxypropyl cellulose, 25 parts by weight of 70% D-sorbitol, 3.0 parts by weight of kaolin, 1.2 parts of tartaric acid Parts by weight, 0.12 parts by weight of sodium edetate, and an appropriate amount of purified water were uniformly dispersed, and
  • Example 1 The patches of Examples 1 to 4 and Comparative Example were applied to the right and left shoulders of three subjects. Each patch was evaluated for warmth, pleasure, effectiveness, and skin irritation when applied for 6 hours as follows, and the average value is shown in Table 2.
  • Example 5 The patches of Examples 5 to 8 were applied to the lumbar regions of three subjects. Each patch was evaluated for warmth, pleasure, effectiveness, and skin irritation when applied for 6 hours in the same manner as in Test Example 1. The average value is shown in Table 3. Table 3

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

L'invention concerne un timbre comprenant un polymère soluble dans l'eau en tant que base, qui est caractérisé en ce qu'il contient un capsaicinoide et un N-vanillylnonanamide dans des quantités pour 100g de la base respectivement entre 0,0002 et 0,005g et entre 0,0005 et 0,007g.
PCT/JP2000/005269 1999-08-05 2000-08-04 Timbre WO2001010435A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU63196/00A AU6319600A (en) 1999-08-05 2000-08-04 Patch

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP22261699 1999-08-05
JP11/222616 1999-08-05

Publications (1)

Publication Number Publication Date
WO2001010435A1 true WO2001010435A1 (fr) 2001-02-15

Family

ID=16785257

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2000/005269 WO2001010435A1 (fr) 1999-08-05 2000-08-04 Timbre

Country Status (2)

Country Link
AU (1) AU6319600A (fr)
WO (1) WO2001010435A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004047820A1 (fr) 2002-11-27 2004-06-10 Hisamitsu Pharmaceutical Co., Inc. Cataplasme chaud
WO2007114380A1 (fr) * 2006-03-31 2007-10-11 Kobayashi Pharmaceutical Co., Ltd. Agent pour application cutanée externe
TWI734953B (zh) 2018-01-24 2021-08-01 日商久光製藥股份有限公司 貼附劑

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5391114A (en) * 1977-01-21 1978-08-10 Riido Kemikaru Kk Pappu medicine stimulated by narming
JPH05105628A (ja) * 1991-10-14 1993-04-27 Lion Corp 外用消炎鎮痛剤
JPH10298066A (ja) * 1997-04-24 1998-11-10 Taisho Pharmaceut Co Ltd 温感貼付剤

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5391114A (en) * 1977-01-21 1978-08-10 Riido Kemikaru Kk Pappu medicine stimulated by narming
JPH05105628A (ja) * 1991-10-14 1993-04-27 Lion Corp 外用消炎鎮痛剤
JPH10298066A (ja) * 1997-04-24 1998-11-10 Taisho Pharmaceut Co Ltd 温感貼付剤

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004047820A1 (fr) 2002-11-27 2004-06-10 Hisamitsu Pharmaceutical Co., Inc. Cataplasme chaud
CN100372526C (zh) * 2002-11-27 2008-03-05 久光制药株式会社 温感敷剂
WO2007114380A1 (fr) * 2006-03-31 2007-10-11 Kobayashi Pharmaceutical Co., Ltd. Agent pour application cutanée externe
JP2007269693A (ja) * 2006-03-31 2007-10-18 Kobayashi Pharmaceut Co Ltd 皮膚外用剤
TWI734953B (zh) 2018-01-24 2021-08-01 日商久光製藥股份有限公司 貼附劑

Also Published As

Publication number Publication date
AU6319600A (en) 2001-03-05

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