WO2010114121A1 - Aqueous gel base and aqueous gel plaster - Google Patents
Aqueous gel base and aqueous gel plaster Download PDFInfo
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- 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
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- aqueous gel
- water
- gel base
- soluble polymer
- lidocaine
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Classifications
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- 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
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- 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
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- 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
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- 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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Abstract
Provided is an aqueous gel base comprising a drug active ingredient, water-soluble polymer, polypropylene glycol having a molecular weight of 1,700 to 2,200, and water. Also provided is an aqueous gel plaster obtained by spreading the aqueous gel base over a sheet-like support.
Description
この発明は、薬効成分を含む水性ゲル基剤に関するものであり、より詳細にはリドカインのような薬効成分、水溶性高分子、分子量１７００～２２００のポリプロピレングリコールおよび水を含んでなる水性ゲル基剤、ならびに該水性ゲル基剤をシート状の支持体上に展延してなる水性ゲル貼付剤に関するものである。
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.
リドカインは、表面麻酔など神経ブロック療法の薬物として繁用されているものであり、これを含有した外用貼付剤は多数知られており、例えばヘルペス神経痛やヘルペス後神経痛に対する疼痛の抑制に好適に用いられている。
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.
例えば、特許第３１１５６２５号公報には、水溶性高分子物質、水および保水剤を必須成分とする粘着性ゲル基剤にリドカインまたはその塩を１～１０重量％配合してなる薬物保持層を支持体上に設けたリドカイン含有外用貼付剤が記載されている。
この特許公報には、保水剤としてポリエチレングリコールが例示されており、さらにポリプロピレングリコールを必要に応じて吸収助剤として使用できる旨、記載されている。 For example, 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.
この特許公報には、保水剤としてポリエチレングリコールが例示されており、さらにポリプロピレングリコールを必要に応じて吸収助剤として使用できる旨、記載されている。 For example, 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.
上記の保水剤としてのポリエチレングリコールや、吸収助剤としてのポリプロピレングリコールについては、それらの分子量が具体的に記載されていないものの、これらが低分子量であると、水との親和性も高くなり、経皮吸収され易くなる。そして、これらの成分が経皮吸収されると、吸収部位での細胞内代謝に悪影響を与えるおそれがある。
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.
一般に、経皮吸収製剤では、目的とする有効成分以外の構成成分の吸収を極力抑制するのが、身体への悪影響を回避するという観点から好ましい。吸収されて問題のない成分であっても、同時に吸収された他の成分とあいまって、人体に悪影響を及ぼすおそれもある。
したがって、目的とする薬効成分以外の経皮吸収を極力抑制することは、外用貼付剤にとって好ましいことである。 In general, in a percutaneous absorption preparation, it is preferable from the viewpoint of avoiding adverse effects on the body to suppress absorption of constituent components other than the intended active ingredient as much as possible. Even a component that is absorbed and has no problem may combine with other components absorbed at the same time to adversely affect the human body.
Therefore, it is preferable for an external patch to suppress transdermal absorption other than the intended medicinal component as much as possible.
したがって、目的とする薬効成分以外の経皮吸収を極力抑制することは、外用貼付剤にとって好ましいことである。 In general, in a percutaneous absorption preparation, it is preferable from the viewpoint of avoiding adverse effects on the body to suppress absorption of constituent components other than the intended active ingredient as much as possible. Even a component that is absorbed and has no problem may combine with other components absorbed at the same time to adversely affect the human body.
Therefore, it is preferable for an external patch to suppress transdermal absorption other than the intended medicinal component as much as possible.
本発明者らは、上記の問題を解決すべく、鋭意検討を重ねた結果、分子量１７００～２２００を有するポリプロピレングリコールが、ゲル基剤の保水性を維持しつつ、薬効成分、特にリドカインの溶解分散性にも優れ、かつその経皮吸収性が極めて低いことを見出し、本発明を完成するに到った。
As a result of intensive studies to solve the above problems, the present inventors have found that 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.
本発明は、薬効成分、水溶性高分子、分子量１７００～２２００のポリプロピレングリコールおよび水を含む水性ゲル基剤に関する。
本発明は、前記の薬効成分がリドカインまたはその塩である水性ゲル基剤にも関する。
本発明は、前記の水溶性高分子が、ポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物である水性ゲル基剤にも関する。
本発明は、水溶性高分子としてポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物に加えて、半合成水溶性高分子をさらに含む水性ゲル基剤にも関する。
本発明は、前記の半合成水溶性高分子が、澱粉－アクリル酸グラフト重合体、澱粉－スチレンスルホン酸グラフト重合体、澱粉－ビニルスルホン酸グラフト重合体、ポリビニルアルコール架橋重合体からなる群から選ばれる少なくとも1種である水性ゲル基剤にも関する。
さらに、本発明は、前記の水性ゲル基剤がシート状の支持体上に展延されてなる水性ゲル貼付剤にも関する。 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. .
In the present invention, 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.
本発明は、前記の薬効成分がリドカインまたはその塩である水性ゲル基剤にも関する。
本発明は、前記の水溶性高分子が、ポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物である水性ゲル基剤にも関する。
本発明は、水溶性高分子としてポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物に加えて、半合成水溶性高分子をさらに含む水性ゲル基剤にも関する。
本発明は、前記の半合成水溶性高分子が、澱粉－アクリル酸グラフト重合体、澱粉－スチレンスルホン酸グラフト重合体、澱粉－ビニルスルホン酸グラフト重合体、ポリビニルアルコール架橋重合体からなる群から選ばれる少なくとも1種である水性ゲル基剤にも関する。
さらに、本発明は、前記の水性ゲル基剤がシート状の支持体上に展延されてなる水性ゲル貼付剤にも関する。 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. .
In the present invention, 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.
上記の水溶性高分子としては、天然水溶性高分子、合成水溶性高分子および半合成水溶性高分子のいずれをも用いることができる。
As the water-soluble polymer, any of natural water-soluble polymers, synthetic water-soluble polymers, and semi-synthetic water-soluble polymers can be used.
上記の天然水溶性高分子としては、例えば、カラギーナン、ローカストビーンガム、アラビアガム、トラガントガム、カラヤガム、ゼラチン、デンブン，寒天、マンナン、アルギン酸、デキストリンなどが挙げられる。
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.
上記の合成水溶性高分子としては、例えば、ポリアクリル酸またはその塩、メチルセルロース、カルボキシメチルセルロース、ポリビニルアルコール、ポリビニルピロリドン、メチルビニルエーテル－無水マレイン酸共重合体などが挙げられる。上記のポリアクリル酸の塩としては、例えばナトリウム塩が挙げられる。
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. As a salt of said polyacrylic acid, a sodium salt is mentioned, for example.
上記の半合成水溶性高分子としては、例えば、澱粉－アクリロニトリルグラフト重合体、澱粉－アクリル酸グラフト重合体、澱粉－スチレンスルホン酸グラフト重合体、澱粉－ビニルスルホン酸グラフト重合体、アクリル酸－酢酸ビニルケン化物などが挙げられる。
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.
これらの水溶性高分子は、その金属塩であってもよく、あるいは架橋剤により架橋されたものであってもよい。また、これらの水溶性高分子は、単独で用いてもよく、２種以上を組み合わせて用いてもよい。
水溶性高分子の水性ゲル基剤中の配合割合は、０．５～５０重量％が好ましく、５～２５重量％がより好ましい。 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.
水溶性高分子の水性ゲル基剤中の配合割合は、０．５～５０重量％が好ましく、５～２５重量％がより好ましい。 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.
なお、水溶性高分子として、ポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物に加えて、上記の半合成水溶性高分子を併用すると、ゲル基剤中の水分含量を高めるとともに、保水性を高めることができる。その場合の半合成水溶性高分子の水性ゲル基剤中の配合割合は、０．０１～１０重量％の範囲が好適である。
In addition to polyacrylic acid, polyacrylic acid salt, polyacrylic acid partial neutralized product, or a mixture thereof as a water-soluble polymer, when the above semi-synthetic water-soluble polymer is used in combination, While increasing the water content, water retention can be increased. In this case, 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.
本発明の水性ゲル基剤中に含まれるポリプロピレングリコールは、薬効成分、特にリドカインを水性ゲル基剤中に均一に分散させる作用に優れ、かつそれ自体は経皮吸収され難いという点で、分子量が約１７００～２２００であるものが好ましく、約１９００～２１００であるものがより好ましい。
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.
本発明の水性ゲル基剤中に含まれるポリプロピレングリコールの配合割合は、約１～１５重量％であるのが好ましく、より好ましくは約３～１０重量％の範囲である。
ポリプロピレングリコールの配合割合が１５重量％より多いと、ゲル基剤中でポリプロピレングリコールのブリージングが生じやすくなるので好ましくなく、逆に１重量％より少ないと、薬効成分、特にリドカインの溶解や分散が不十分となりやすいので好ましくない。
なお、ひまし油などを添加すると、上記のブリージングを抑制することができる。 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.
When 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. Conversely, when the blending ratio is less than 1% by weight, 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.
ポリプロピレングリコールの配合割合が１５重量％より多いと、ゲル基剤中でポリプロピレングリコールのブリージングが生じやすくなるので好ましくなく、逆に１重量％より少ないと、薬効成分、特にリドカインの溶解や分散が不十分となりやすいので好ましくない。
なお、ひまし油などを添加すると、上記のブリージングを抑制することができる。 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.
When 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. Conversely, when the blending ratio is less than 1% by weight, 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.
本発明の水性ゲル基剤中に含まれる薬効成分は、外用剤として用いられているものであれば、水溶性であっても、油溶性であってもよい。
具体的には、例えば、リドカインまたはその塩のような局所麻酔剤、インドメタシン、サリチル酸のような解熱消炎鎮痛剤、ヒドロコルチゾン、プレドニゾロンのようなステロイド系抗炎症剤などが挙げられる。リドカインの塩としては、例えば塩酸塩が挙げられる。
これらの薬効成分は、単独で用いられてもよく、２種以上を適宜組み合わせて用いてもよい。 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.
Specific examples include a local anesthetic such as lidocaine or a salt thereof, an antipyretic analgesic such as indomethacin and salicylic acid, and a steroidal anti-inflammatory agent such as hydrocortisone and prednisolone. Examples of the salt of lidocaine include hydrochloride.
These medicinal components may be used alone or in combination of two or more.
具体的には、例えば、リドカインまたはその塩のような局所麻酔剤、インドメタシン、サリチル酸のような解熱消炎鎮痛剤、ヒドロコルチゾン、プレドニゾロンのようなステロイド系抗炎症剤などが挙げられる。リドカインの塩としては、例えば塩酸塩が挙げられる。
これらの薬効成分は、単独で用いられてもよく、２種以上を適宜組み合わせて用いてもよい。 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.
Specific examples include a local anesthetic such as lidocaine or a salt thereof, an antipyretic analgesic such as indomethacin and salicylic acid, and a steroidal anti-inflammatory agent such as hydrocortisone and prednisolone. Examples of the salt of lidocaine include hydrochloride.
These medicinal components may be used alone or in combination of two or more.
薬効成分がリドカインまたはその塩であると、神経痛に対する鎮痛作用や手足のしびれを緩和するリドカインの薬効が充分に発揮されるので、本発明の水性ゲル基剤はリドカインまたはその塩に特に適している。
薬効成分がリドカインまたはその塩である場合、ゲル基剤中のその配合割合は、特に限定されないが、通常、１～１５重量％であり、好ましくは２～１０重量％である。
なお、リドカインまたはその塩を薬効成分として用いる場合、リドカインは難水溶性であるので、例えばメチルピロリドンのような油性の溶解剤に予め溶解し、それを水性ゲル基剤に混和し、分散させるのが好ましい。 When the medicinal component is lidocaine or a salt thereof, the analgesic action against neuralgia and the medicinal effect of lidocaine that relieves numbness of the limbs are sufficiently exerted, so the aqueous gel base of the present invention is particularly suitable for lidocaine or a salt thereof. .
When the medicinal component is 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.
When 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.
薬効成分がリドカインまたはその塩である場合、ゲル基剤中のその配合割合は、特に限定されないが、通常、１～１５重量％であり、好ましくは２～１０重量％である。
なお、リドカインまたはその塩を薬効成分として用いる場合、リドカインは難水溶性であるので、例えばメチルピロリドンのような油性の溶解剤に予め溶解し、それを水性ゲル基剤に混和し、分散させるのが好ましい。 When the medicinal component is lidocaine or a salt thereof, the analgesic action against neuralgia and the medicinal effect of lidocaine that relieves numbness of the limbs are sufficiently exerted, so the aqueous gel base of the present invention is particularly suitable for lidocaine or a salt thereof. .
When the medicinal component is 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.
When 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.
本発明の水性ゲル基剤の水分含量は、特に限定されないが、通常、１０～７０重量％が好ましく、より好ましくは２０～５０重量％である。
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.
上記のようにしてなる水性ゲル基剤は、通常、これをシート状の支持体上に展延して得られる、いわゆる粘着性の貼付剤として用いられる。
その際の水性ゲル基剤の展延量は、特に限定されないが、通常、５００～２０００ｇ／ｍ2の範囲が好ましい。 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 .
その際の水性ゲル基剤の展延量は、特に限定されないが、通常、５００～２０００ｇ／ｍ2の範囲が好ましい。 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 .
上記の支持体としては、特に限定されないが、通常、不織布、織布、あるいはこれらに樹脂フィルムをラミネート加工したものなどが挙げられる。
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.
本発明の水性ゲル基剤には、通常の吸収助剤、界面活性剤、防腐剤、酸化防止剤などを、所望により適宜添加してもよい。
上記の吸収助剤としては、例えばサリチル酸、ヒアルロン酸、オレイン酸、ステアリン酸ｎ－ブチル、ベンジルアルコール、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、クロタミトン、ジエチルセバケート、Ｎ－メチルピロリドン、Ｎ－エチルピロリドン、ラウリルアルコールなどが挙げられる。
上記の界面活性剤としては、例えば、ポリオキシエチレンソルビタンモノオレート、ソルビタンモノオレート、ソルビタンモノパルミテートなどが挙げられる。
上記の防腐剤としては、例えば、メチルパラベン、エチルパラベン、プロピルパラベンのようなパラベン類、フェノキシエタノールなどが挙げられ、また酸化防止剤としては、例えば、エデト酸ナトリウム、トコフェロール酢酸エステル、トコフェロール、ビタミンＡ油などが挙げられる。 Ordinary absorption aids, surfactants, preservatives, antioxidants and the like may be appropriately added to the aqueous gel base of the present invention as desired.
Examples of 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.
Examples of 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.
上記の吸収助剤としては、例えばサリチル酸、ヒアルロン酸、オレイン酸、ステアリン酸ｎ－ブチル、ベンジルアルコール、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、クロタミトン、ジエチルセバケート、Ｎ－メチルピロリドン、Ｎ－エチルピロリドン、ラウリルアルコールなどが挙げられる。
上記の界面活性剤としては、例えば、ポリオキシエチレンソルビタンモノオレート、ソルビタンモノオレート、ソルビタンモノパルミテートなどが挙げられる。
上記の防腐剤としては、例えば、メチルパラベン、エチルパラベン、プロピルパラベンのようなパラベン類、フェノキシエタノールなどが挙げられ、また酸化防止剤としては、例えば、エデト酸ナトリウム、トコフェロール酢酸エステル、トコフェロール、ビタミンＡ油などが挙げられる。 Ordinary absorption aids, surfactants, preservatives, antioxidants and the like may be appropriately added to the aqueous gel base of the present invention as desired.
Examples of 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.
Examples of 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.
本発明の水性ゲル基剤によれば、薬効成分を水性ゲル基剤中に均一に分散させることができ、かかる水性ゲル基剤を支持体上に展延してなる水性ゲル貼付剤は、薬効成分を定量的かつ持続的に放出することができるので、これを皮膚に貼付した場合、薬効成分が持続的に安定して経皮吸収される。
また、本発明の水性ゲル基剤によれば、分子量１７００～２２００のポリプロピレングリコールは経皮吸収されないので、人体に対してより安全である。
本発明の水性ゲル貼付剤によれば、他の投与方法に比べて、使用対象者の年齢、健康状態、消化器官の状態、食物の影響などに左右されることなく、薬効成分が安定的に吸収されるので、期待した薬効が確実に発揮され得る。 According to the aqueous gel base of the present invention, 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.
In addition, according to the aqueous gel base of the present invention, polypropylene glycol having a molecular weight of 1700 to 2200 is not absorbed percutaneously, so that it is safer for the human body.
According to the aqueous gel patch of the present invention, 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.
また、本発明の水性ゲル基剤によれば、分子量１７００～２２００のポリプロピレングリコールは経皮吸収されないので、人体に対してより安全である。
本発明の水性ゲル貼付剤によれば、他の投与方法に比べて、使用対象者の年齢、健康状態、消化器官の状態、食物の影響などに左右されることなく、薬効成分が安定的に吸収されるので、期待した薬効が確実に発揮され得る。 According to the aqueous gel base of the present invention, 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.
In addition, according to the aqueous gel base of the present invention, polypropylene glycol having a molecular weight of 1700 to 2200 is not absorbed percutaneously, so that it is safer for the human body.
According to the aqueous gel patch of the present invention, 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.
以下、試験例および実施例により、本発明をより詳細に説明するが、本発明はこれらの実施例により制限されるものではない。
Hereinafter, the present invention will be described in more detail with reference to test examples and examples, but the present invention is not limited to these examples.
試験例１
本発明者らは、従来から水性ゲル貼付剤の保水剤として用いられているプロピレングリコールと、本発明において薬効成分の分散剤として用いられるポリプロピレングリコールとを、その経皮吸収性について比較試験した。 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.
本発明者らは、従来から水性ゲル貼付剤の保水剤として用いられているプロピレングリコールと、本発明において薬効成分の分散剤として用いられるポリプロピレングリコールとを、その経皮吸収性について比較試験した。 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.
プロピレングリコール（ＰＧ、０．０５ｍｌ）またはポリプロピレングリコール（ＰＰＧ、分子量：２０００、０．０５ｍｌ）を、ラットの皮膚（２ｃｍ2）の一面に直接塗布し、リン酸緩衝生理食塩水１０ｍｌを入れたセルの開口部に、上記ラットの皮膚の裏面（塗布面の反対側）が接触するように載せ、リン酸緩衝生理食塩水中に透過したＰＧまたはＰＰＧの濃度（ｐｐｍ）を、ＨＰＬＣ法により測定した。
その結果を次表に示す。 A cell in which propylene glycol (PG, 0.05 ml) or polypropylene glycol (PPG, molecular weight: 2000, 0.05 ml) was directly applied to one surface of rat skin (2 cm 2 ) and 10 ml of phosphate buffered saline was placed. 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.
その結果を次表に示す。 A cell in which propylene glycol (PG, 0.05 ml) or polypropylene glycol (PPG, molecular weight: 2000, 0.05 ml) was directly applied to one surface of rat skin (2 cm 2 ) and 10 ml of phosphate buffered saline was placed. 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.
上記の試験結果に示されるように、ＰＧの皮膚透過性はかなり大きかったのに対して、ＰＰＧ（分子量：２０００）のそれは、検出限界量（0.003ppm）以下であった。
したがって、ポリプロピレングリコール（分子量：２０００）は、人体に対してより安全性が高いことがわかる。
実施例１
まず、リドカイン（５重量%、水性ゲル基剤に対する重量%、以下同じ）をメチルピロリドン（２．５重量%）に混和して、予め溶解する。
一方、ポリアクリル酸系粘着剤（カルボキシビニルポリマー、ポリアクリル酸、ポリアクリル酸ナトリウム）（９重量%）およびカルボキシメチルセルロースナトリウム４重量%を混和し、これに分子量２０００のポリプロピレングリコール（５重量%）、分散助剤としてのヒマシ油（７重量%）および水（８重量％）を加え、混合して水性粘着剤溶液を調製する。
次に、ポリビニルピロリドン（３重量％）を水（残余）に溶解し、この水溶液にポリソルベート８０（０．２重量%）を加え、これに上記で調製した水性粘着剤溶液を加えてよく混合する。
これに、上記で調製したリドカイン溶解液を加え、よく混合して、リドカイン含有水性ゲル基剤を得た。
このドカイン含有水性ゲル基剤を、不織布上に１０００ｇ／ｍ2の割合で展延して、リドカイン含有水性ゲル貼付剤を得た。
この水性ゲル貼付剤を被験者の上腕に貼付したところ、８時間以上貼付状態が良好に維持され、リドカインの薬効が確認された。 As shown in the above test results, the skin permeability of PG was considerably large, whereas that of PPG (molecular weight: 2000) was below the detection limit (0.003 ppm).
Therefore, it can be seen that polypropylene glycol (molecular weight: 2000) is safer for the human body.
Example 1
First, lidocaine (5% by weight,% by weight based on an aqueous gel base, the same applies hereinafter) is mixed with methylpyrrolidone (2.5% by weight) and dissolved in advance.
On the other hand, 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.
When 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.
したがって、ポリプロピレングリコール（分子量：２０００）は、人体に対してより安全性が高いことがわかる。
実施例１
まず、リドカイン（５重量%、水性ゲル基剤に対する重量%、以下同じ）をメチルピロリドン（２．５重量%）に混和して、予め溶解する。
一方、ポリアクリル酸系粘着剤（カルボキシビニルポリマー、ポリアクリル酸、ポリアクリル酸ナトリウム）（９重量%）およびカルボキシメチルセルロースナトリウム４重量%を混和し、これに分子量２０００のポリプロピレングリコール（５重量%）、分散助剤としてのヒマシ油（７重量%）および水（８重量％）を加え、混合して水性粘着剤溶液を調製する。
次に、ポリビニルピロリドン（３重量％）を水（残余）に溶解し、この水溶液にポリソルベート８０（０．２重量%）を加え、これに上記で調製した水性粘着剤溶液を加えてよく混合する。
これに、上記で調製したリドカイン溶解液を加え、よく混合して、リドカイン含有水性ゲル基剤を得た。
このドカイン含有水性ゲル基剤を、不織布上に１０００ｇ／ｍ2の割合で展延して、リドカイン含有水性ゲル貼付剤を得た。
この水性ゲル貼付剤を被験者の上腕に貼付したところ、８時間以上貼付状態が良好に維持され、リドカインの薬効が確認された。 As shown in the above test results, the skin permeability of PG was considerably large, whereas that of PPG (molecular weight: 2000) was below the detection limit (0.003 ppm).
Therefore, it can be seen that polypropylene glycol (molecular weight: 2000) is safer for the human body.
Example 1
First, lidocaine (5% by weight,% by weight based on an aqueous gel base, the same applies hereinafter) is mixed with methylpyrrolidone (2.5% by weight) and dissolved in advance.
On the other hand, 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.
When 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.
実施例２
上記の実施例１における水性粘着剤溶液の調製時にアクリル酸－澱粉グラフト重合体（５重量%）を加え、実施例１と同様に処理して、リドカイン含有水性ゲル貼付剤を得た。
アクリル酸－澱粉グラフト重合体の添加により、貼付剤の粘着性が向上し、リドカインの薬効が充分に示された。 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.
By adding the acrylic acid-starch graft polymer, the adhesiveness of the patch was improved, and the medicinal effect of lidocaine was fully demonstrated.
上記の実施例１における水性粘着剤溶液の調製時にアクリル酸－澱粉グラフト重合体（５重量%）を加え、実施例１と同様に処理して、リドカイン含有水性ゲル貼付剤を得た。
アクリル酸－澱粉グラフト重合体の添加により、貼付剤の粘着性が向上し、リドカインの薬効が充分に示された。 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.
By adding the acrylic acid-starch graft polymer, the adhesiveness of the patch was improved, and the medicinal effect of lidocaine was fully demonstrated.
実施例３
上記の実施例１における水性粘着剤溶液の調製時にヒアルロン酸（２重量%）を加え、実施例１と同様に処理して、リドカイン含有水性ゲル貼付剤を得た。
ヒアルロン酸の添加により、貼付剤の粘着性が向上し、リドカインの薬効が充分に示された。 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.
上記の実施例１における水性粘着剤溶液の調製時にヒアルロン酸（２重量%）を加え、実施例１と同様に処理して、リドカイン含有水性ゲル貼付剤を得た。
ヒアルロン酸の添加により、貼付剤の粘着性が向上し、リドカインの薬効が充分に示された。 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.
Claims (6)
- 薬効成分、水溶性高分子、分子量１７００～２２００のポリプロピレングリコールおよび水を含むことを特徴とする水性ゲル基剤。 An aqueous gel base comprising a medicinal component, a water-soluble polymer, polypropylene glycol having a molecular weight of 1700 to 2200, and water.
- 前記の薬効成分がリドカインまたはその塩である、請求項１に記載の水性ゲル基剤。 The aqueous gel base according to claim 1, wherein the medicinal component is lidocaine or a salt thereof.
- 前記の水溶性高分子が、ポリアクリル酸、ポリアクリル酸塩、ポリアクリル酸部分中和物、またはそれらの混合物である、請求項１または２に記載の水性ゲル基剤。 The aqueous gel base according to claim 1 or 2, wherein the water-soluble polymer is polyacrylic acid, polyacrylic acid salt, partially neutralized polyacrylic acid, or a mixture thereof.
- 前記の水溶性高分子として半合成水溶性高分子をさらに含む、請求項３に記載の水性ゲル基剤。 The aqueous gel base according to claim 3, further comprising a semi-synthetic water-soluble polymer as the water-soluble polymer.
- 前記の半合成水溶性高分子が、澱粉－アクリル酸グラフト重合体、澱粉－スチレンスルホン酸グラフト重合体、澱粉－ビニルスルホン酸グラフト重合体、ポリビニルアルコール架橋重合体からなる群から選ばれる少なくとも1種である、請求項４に記載の水性ゲル基剤。 The semi-synthetic water-soluble polymer is at least one 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. The aqueous gel base according to claim 4, wherein
- 前記の請求項１～５のいずれか１つに記載の水性ゲル基剤がシート状の支持体上に展延されてなる水性ゲル貼付剤。 An aqueous gel patch obtained by spreading the aqueous gel base according to any one of claims 1 to 5 on a sheet-like support.
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| JP2011507307A JPWO2010114121A1 (en) | 2009-04-02 | 2010-04-02 | Aqueous gel base and aqueous gel patch |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2013027840A1 (en) * | 2011-08-25 | 2015-03-23 | ニプロパッチ株式会社 | Water-containing patch |
| WO2016104644A1 (en) * | 2014-12-26 | 2016-06-30 | 花王株式会社 | Hydrogel composition |
| JP2016188187A (en) * | 2015-03-30 | 2016-11-04 | 株式会社池田模範堂 | External pharmaceutical composition |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS61260014A (en) * | 1985-05-15 | 1986-11-18 | Nitto Electric Ind Co Ltd | Base for hydrous patch |
| JPH04305523A (en) * | 1991-03-30 | 1992-10-28 | Teikoku Seiyaku Co Ltd | Ridocaine-containing application agent for external use |
| JPH09315964A (en) * | 1996-05-27 | 1997-12-09 | Chinhin Boku | Cataplasm for stiff shoulder and frozen shoulder syndrome |
| WO2001047559A1 (en) * | 1999-12-27 | 2001-07-05 | Teikoku Seiyaku Co., Ltd | Patches for external use |
| JP2002284705A (en) * | 2001-01-19 | 2002-10-03 | Shiseido Co Ltd | Torpent |
-
2010
- 2010-04-02 WO PCT/JP2010/056072 patent/WO2010114121A1/en active Application Filing
- 2010-04-02 JP JP2011507307A patent/JPWO2010114121A1/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61260014A (en) * | 1985-05-15 | 1986-11-18 | Nitto Electric Ind Co Ltd | Base for hydrous patch |
| JPH04305523A (en) * | 1991-03-30 | 1992-10-28 | Teikoku Seiyaku Co Ltd | Ridocaine-containing application agent for external use |
| JPH09315964A (en) * | 1996-05-27 | 1997-12-09 | Chinhin Boku | Cataplasm for stiff shoulder and frozen shoulder syndrome |
| WO2001047559A1 (en) * | 1999-12-27 | 2001-07-05 | Teikoku Seiyaku Co., Ltd | Patches for external use |
| JP2002284705A (en) * | 2001-01-19 | 2002-10-03 | Shiseido Co Ltd | Torpent |
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| "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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2013027840A1 (en) * | 2011-08-25 | 2015-03-23 | ニプロパッチ株式会社 | Water-containing patch |
| WO2016104644A1 (en) * | 2014-12-26 | 2016-06-30 | 花王株式会社 | Hydrogel composition |
| US10660829B2 (en) | 2014-12-26 | 2020-05-26 | Kao Corporation | Hydrogel composition |
| JP2016188187A (en) * | 2015-03-30 | 2016-11-04 | 株式会社池田模範堂 | External pharmaceutical composition |
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| JPWO2010114121A1 (en) | 2012-10-11 |
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