WO2010114121A1 - Base pour gel aqueux et pansement de gel aqueux - Google Patents

Base pour gel aqueux et pansement de gel aqueux Download PDF

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Publication number
WO2010114121A1
WO2010114121A1 PCT/JP2010/056072 JP2010056072W WO2010114121A1 WO 2010114121 A1 WO2010114121 A1 WO 2010114121A1 JP 2010056072 W JP2010056072 W JP 2010056072W WO 2010114121 A1 WO2010114121 A1 WO 2010114121A1
Authority
WO
WIPO (PCT)
Prior art keywords
aqueous gel
water
gel base
soluble polymer
lidocaine
Prior art date
Application number
PCT/JP2010/056072
Other languages
English (en)
Japanese (ja)
Inventor
克美 井原
眞滋 守金
大蔵 守金
Original Assignee
ダイヤ製薬株式会社
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 ダイヤ製薬株式会社 filed Critical ダイヤ製薬株式会社
Priority to JP2011507307A priority Critical patent/JPWO2010114121A1/ja
Publication of WO2010114121A1 publication Critical patent/WO2010114121A1/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
    • A61K9/7053—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
    • A61K9/7061—Polyacrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • the present invention relates to an aqueous gel base containing a medicinal component, and more specifically, an aqueous gel base comprising a medicinal component such as lidocaine, a water-soluble polymer, polypropylene glycol having a molecular weight of 1700 to 2200, and water. And an aqueous gel patch obtained by spreading the aqueous gel base on a sheet-like support.
  • Lidocaine is frequently used as a drug for nerve block therapy such as surface anesthesia, and many external patches containing it are known. It has been.
  • Japanese Patent No. 3115625 supports a drug retaining layer comprising 1 to 10% by weight of lidocaine or a salt thereof in an adhesive gel base containing water-soluble polymer substance, water and a water retention agent as essential components.
  • a lidocaine-containing external patch provided on the body is described.
  • This patent publication exemplifies polyethylene glycol as a water retention agent, and further describes that polypropylene glycol can be used as an absorption aid if necessary.
  • Polyethylene glycol as the water retention agent and polypropylene glycol as the absorption aid are not specifically described in terms of their molecular weights, but if these are low molecular weights, the affinity with water is also increased. It is easily absorbed through the skin. And when these components are absorbed percutaneously, there is a risk of adversely affecting intracellular metabolism at the site of absorption.
  • polypropylene glycol having a molecular weight of 1700 to 2200 can dissolve and disperse medicinal components, particularly lidocaine, while maintaining the water retention of the gel base.
  • the present invention has been completed by finding that it has excellent properties and its transdermal absorbability is extremely low.
  • the present invention relates to an aqueous gel base comprising a medicinal component, a water-soluble polymer, polypropylene glycol having a molecular weight of 1700 to 2200, and water.
  • the present invention also relates to an aqueous gel base wherein the medicinal component is lidocaine or a salt thereof.
  • the present invention also relates to an aqueous gel base wherein the water-soluble polymer is polyacrylic acid, polyacrylic acid salt, polyacrylic acid partial neutralized product, or a mixture thereof.
  • the present invention also relates to an aqueous gel base further comprising a semisynthetic water-soluble polymer in addition to polyacrylic acid, polyacrylate, partially neutralized polyacrylic acid, or a mixture thereof as the water-soluble polymer.
  • the semi-synthetic water-soluble polymer is selected from the group consisting of starch-acrylic acid graft polymer, starch-styrene sulfonic acid graft polymer, starch-vinyl sulfonic acid graft polymer, and polyvinyl alcohol crosslinked polymer. It also relates to an aqueous gel base which is at least one kind. Furthermore, the present invention also relates to an aqueous gel patch in which the above aqueous gel base is spread on a sheet-like support.
  • water-soluble polymer any of natural water-soluble polymers, synthetic water-soluble polymers, and semi-synthetic water-soluble polymers can be used.
  • Examples of the natural water-soluble polymer include carrageenan, locust bean gum, gum arabic, tragacanth gum, caraya gum, gelatin, denbun, agar, mannan, alginic acid, and dextrin.
  • Examples of the synthetic water-soluble polymer include polyacrylic acid or a salt thereof, methyl cellulose, carboxymethyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone, methyl vinyl ether-maleic anhydride copolymer, and the like.
  • a salt of said polyacrylic acid a sodium salt is mentioned, for example.
  • Examples of the semi-synthetic water-soluble polymer include starch-acrylonitrile graft polymer, starch-acrylic acid graft polymer, starch-styrene sulfonic acid graft polymer, starch-vinyl sulfonic acid graft polymer, acrylic acid-acetic acid. Examples thereof include vinyl saponified products.
  • These water-soluble polymers may be metal salts thereof or those crosslinked with a crosslinking agent. Moreover, these water-soluble polymers may be used alone or in combination of two or more.
  • the blending ratio of the water-soluble polymer in the aqueous gel base is preferably 0.5 to 50% by weight, and more preferably 5 to 25% by weight.
  • the mixing ratio of the semi-synthetic water-soluble polymer in the aqueous gel base is preferably in the range of 0.01 to 10% by weight.
  • the polypropylene glycol contained in the aqueous gel base of the present invention has a molecular weight in that it is excellent in the action of uniformly dispersing medicinal ingredients, particularly lidocaine, in the aqueous gel base and is hardly percutaneously absorbed. What is about 1700-2200 is preferable, and what is about 1900-2100 is more preferable.
  • the proportion of polypropylene glycol contained in the aqueous gel base of the present invention is preferably about 1 to 15% by weight, more preferably about 3 to 10% by weight.
  • the proportion of polypropylene glycol contained in the aqueous gel base of the present invention is preferably about 1 to 15% by weight, more preferably about 3 to 10% by weight.
  • the blending ratio of polypropylene glycol is more than 15% by weight, it is not preferable because polypropylene glycol is likely to be breathed in the gel base.
  • dissolution and dispersion of the medicinal component, particularly lidocaine is not preferable. This is not preferable because it tends to be sufficient. Note that the above breathing can be suppressed by adding castor oil or the like.
  • the medicinal component contained in the aqueous gel base of the present invention may be water-soluble or oil-soluble as long as it is used as an external preparation.
  • a local anesthetic such as lidocaine or a salt thereof
  • an antipyretic analgesic such as indomethacin and salicylic acid
  • a steroidal anti-inflammatory agent such as hydrocortisone and prednisolone.
  • the salt of lidocaine include hydrochloride.
  • the aqueous gel base of the present invention is particularly suitable for lidocaine or a salt thereof.
  • the blending ratio in the gel base is not particularly limited, but is usually 1 to 15% by weight, preferably 2 to 10% by weight.
  • lidocaine or a salt thereof is used as a medicinal ingredient
  • lidocaine is poorly water-soluble, so it is dissolved beforehand in an oil-based solubilizing agent such as methylpyrrolidone, mixed with an aqueous gel base, and dispersed. Is preferred.
  • the water content of the aqueous gel base of the present invention is not particularly limited, but is usually preferably 10 to 70% by weight, more preferably 20 to 50% by weight.
  • the aqueous gel base formed as described above is usually used as a so-called adhesive patch obtained by spreading it on a sheet-like support.
  • the spreading amount of the aqueous gel base at that time is not particularly limited, but is usually preferably in the range of 500 to 2000 g / m 2 .
  • the above support is not particularly limited, and usually includes a nonwoven fabric, a woven fabric, or a laminate obtained by laminating a resin film thereon.
  • absorption aids may be appropriately added to the aqueous gel base of the present invention as desired.
  • the absorption aid include salicylic acid, hyaluronic acid, oleic acid, n-butyl stearate, benzyl alcohol, isopropyl myristate, isopropyl palmitate, crotamiton, diethyl sebacate, N-methylpyrrolidone, N-ethylpyrrolidone, Examples include lauryl alcohol.
  • the surfactant include polyoxyethylene sorbitan monooleate, sorbitan monooleate, sorbitan monopalmitate, and the like.
  • Examples of the preservative include parabens such as methyl paraben, ethyl paraben, and propyl paraben, and phenoxyethanol.
  • Examples of the antioxidant include sodium edetate, tocopherol acetate, tocopherol, and vitamin A oil. Etc.
  • the medicinal component can be uniformly dispersed in the aqueous gel base, and the aqueous gel patch obtained by spreading the aqueous gel base on the support has a medicinal effect. Since the component can be released quantitatively and continuously, when it is applied to the skin, the medicinal component is continuously and stably absorbed.
  • polypropylene glycol having a molecular weight of 1700 to 2200 is not absorbed percutaneously, so that it is safer for the human body.
  • the medicinal component can be stably compared with other administration methods without being influenced by the age, health condition, digestive organ condition, food influence, etc. of the user. Since it is absorbed, the expected medicinal effect can be surely exhibited.
  • Test example 1 The inventors of the present invention conducted a comparative test on the transdermal absorbability of propylene glycol, which has been conventionally used as a water retention agent for aqueous gel patches, and polypropylene glycol, which is used as a dispersant for medicinal ingredients in the present invention.
  • the surface of the rat skin was placed in contact with the back surface of the rat (opposite to the coated surface), and the concentration (ppm) of PG or PPG permeated into the phosphate buffered saline was measured by the HPLC method. The results are shown in the following table.
  • a polyacrylic acid-based pressure-sensitive adhesive (carboxyvinyl polymer, polyacrylic acid, sodium polyacrylate) (9% by weight) and 4% by weight of sodium carboxymethylcellulose were mixed, and polypropylene glycol (5% by weight) having a molecular weight of 2000 was mixed therewith. Then, castor oil (7% by weight) and water (8% by weight) as a dispersion aid are added and mixed to prepare an aqueous adhesive solution. Next, polyvinyl pyrrolidone (3% by weight) is dissolved in water (residue), polysorbate 80 (0.2% by weight) is added to this aqueous solution, and the aqueous adhesive solution prepared above is added thereto and mixed well. .
  • the lidocaine solution prepared above was added thereto and mixed well to obtain a lidocaine-containing aqueous gel base.
  • This docaine-containing aqueous gel base was spread on a nonwoven fabric at a rate of 1000 g / m 2 to obtain a lidocaine-containing aqueous gel patch.
  • this aqueous gel patch was affixed to the upper arm of the subject, the affixed state was maintained satisfactorily for 8 hours or more, and the efficacy of lidocaine was confirmed.
  • Example 2 Acrylic acid-starch graft polymer (5% by weight) was added during the preparation of the aqueous pressure-sensitive adhesive solution in Example 1, and the same treatment as in Example 1 was performed to obtain a lidocaine-containing aqueous gel patch.
  • the acrylic acid-starch graft polymer By adding the acrylic acid-starch graft polymer, the adhesiveness of the patch was improved, and the medicinal effect of lidocaine was fully demonstrated.
  • Example 3 When preparing the aqueous pressure-sensitive adhesive solution in Example 1, hyaluronic acid (2% by weight) was added, and the same treatment as in Example 1 was performed to obtain a lidocaine-containing aqueous gel patch. By adding hyaluronic acid, the adhesiveness of the patch was improved, and the medicinal effect of lidocaine was fully demonstrated.

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

Abstract

Cette invention concerne une base pour gel aqueux comprenant un principe actif pharmacologique, un polymère hydrosoluble, un polypropylène glycol ayant un poids moléculaire de 1 700 à 2 200 et de l'eau. L'invention concerne également un pansement de gel aqueux obtenu en étalant la base pour gel aqueux sur une pellicule support.
PCT/JP2010/056072 2009-04-02 2010-04-02 Base pour gel aqueux et pansement de gel aqueux WO2010114121A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2011507307A JPWO2010114121A1 (ja) 2009-04-02 2010-04-02 水性ゲル基剤および水性ゲル貼付剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2009105682 2009-04-02
JP2009-105682 2009-04-02

Publications (1)

Publication Number Publication Date
WO2010114121A1 true WO2010114121A1 (fr) 2010-10-07

Family

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Family Applications (1)

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PCT/JP2010/056072 WO2010114121A1 (fr) 2009-04-02 2010-04-02 Base pour gel aqueux et pansement de gel aqueux

Country Status (2)

Country Link
JP (1) JPWO2010114121A1 (fr)
WO (1) WO2010114121A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2013027840A1 (ja) * 2011-08-25 2015-03-23 ニプロパッチ株式会社 含水貼付剤
WO2016104644A1 (fr) * 2014-12-26 2016-06-30 花王株式会社 Composition d'hydrogel
JP2016188187A (ja) * 2015-03-30 2016-11-04 株式会社池田模範堂 外用医薬組成物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61260014A (ja) * 1985-05-15 1986-11-18 Nitto Electric Ind Co Ltd 含水貼付剤の基剤
JPH04305523A (ja) * 1991-03-30 1992-10-28 Teikoku Seiyaku Co Ltd リドカイン含有外用貼付剤
JPH09315964A (ja) * 1996-05-27 1997-12-09 Chinhin Boku 肩こり・五十肩治療用貼付剤
WO2001047559A1 (fr) * 1999-12-27 2001-07-05 Teikoku Seiyaku Co., Ltd Pastilles a usage externe
JP2002284705A (ja) * 2001-01-19 2002-10-03 Shiseido Co Ltd 刺激緩和剤

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61260014A (ja) * 1985-05-15 1986-11-18 Nitto Electric Ind Co Ltd 含水貼付剤の基剤
JPH04305523A (ja) * 1991-03-30 1992-10-28 Teikoku Seiyaku Co Ltd リドカイン含有外用貼付剤
JPH09315964A (ja) * 1996-05-27 1997-12-09 Chinhin Boku 肩こり・五十肩治療用貼付剤
WO2001047559A1 (fr) * 1999-12-27 2001-07-05 Teikoku Seiyaku Co., Ltd Pastilles a usage externe
JP2002284705A (ja) * 2001-01-19 2002-10-03 Shiseido Co Ltd 刺激緩和剤

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Final Report on the Safety Assessment of Propylene Glycol and Polypropylene Glycols", JOURNAL OF THE AMERICAN COLLEGE OF TOXICOLOGY, vol. 13, no. 6, 1994, pages 437 - 491 *
IYAKUHIN TENKABUTSU JITEN 2007, 25 July 2007 (2007-07-25), pages 276 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2013027840A1 (ja) * 2011-08-25 2015-03-23 ニプロパッチ株式会社 含水貼付剤
WO2016104644A1 (fr) * 2014-12-26 2016-06-30 花王株式会社 Composition d'hydrogel
US10660829B2 (en) 2014-12-26 2020-05-26 Kao Corporation Hydrogel composition
JP2016188187A (ja) * 2015-03-30 2016-11-04 株式会社池田模範堂 外用医薬組成物

Also Published As

Publication number Publication date
JPWO2010114121A1 (ja) 2012-10-11

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