JP2007262100A - Method for preventing reduction in content of terpenoid - Google Patents

Method for preventing reduction in content of terpenoid Download PDF

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Publication number
JP2007262100A
JP2007262100A JP2007189146A JP2007189146A JP2007262100A JP 2007262100 A JP2007262100 A JP 2007262100A JP 2007189146 A JP2007189146 A JP 2007189146A JP 2007189146 A JP2007189146 A JP 2007189146A JP 2007262100 A JP2007262100 A JP 2007262100A
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Prior art keywords
terpenoid
resin
content
container
nasal drop
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JP2007189146A
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Japanese (ja)
Inventor
Koji Doi
光司 土井
Hisayuki Nakayama
久幸 中山
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Senju Pharmaceutical Co Ltd
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Senju Pharmaceutical Co Ltd
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Priority to JP2007189146A priority Critical patent/JP2007262100A/en
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Abstract

<P>PROBLEM TO BE SOLVED: To prevent reduction in the content of a terpenoid in a terpenoid-containing nasal drop charged in a spray container. <P>SOLUTION: This method for preventing reduction in the content of a terpenoid is characterized by charging a terpenoid-containing nasal drop in a spray container whose inner wall material in contact with the terpenoid-containing nasal drop on the charging of the drop is an epoxy resin such as an epoxy phenolic resin, a polyamideimide resin, or a fluororesin, such as a vinylidene fluoride resin. According to the present invention, the terpenoid-containing nasal drop charged in the container can be preserved without accompanying the remarkable content reduction of the terpenoid. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

本発明は特定の容器に充填された点鼻用製剤に関する。   The present invention relates to a nasal preparation filled in a specific container.

鼻みず、鼻づまり等の鼻炎症状の緩解のために、従来抗ヒスタミン剤、殺菌剤、血管収縮剤などに加えて、メントール等のテルペノイドを清涼剤として配合した点鼻液が用いられ、それはポリエチレン又はポリプロピレン製の手動加圧式スプレー容器に充填して市販されている。   In order to relieve nasal inflammation such as nasal congestion and nasal congestion, nasal drops containing terpenoids such as menthol as a cooling agent in addition to conventional antihistamines, bactericides, vasoconstrictors, etc. are used. Commercially available manually pressurized spray containers are filled.

本発明者らの研究の結果、テルペノイドを配合した点鼻薬をポリエチレンやポリプロピレン製のスプレー容器に充填するとテルペノイドが保存中に容器材料に吸収浸透、揮散してその含有量を長期間保持できないことが判った。本発明はスプレー容器に充填したテルペノイド含有点鼻用製剤からテルペノイドの吸収浸透及び揮散を抑制して長期間の保存を可能にしようとするものである。   As a result of our research, when nasal drops containing terpenoids are filled in a spray container made of polyethylene or polypropylene, the terpenoids cannot absorb and permeate into the container material during storage and keep its content for a long time. understood. The present invention is intended to enable long-term storage by suppressing terpenoid absorption penetration and volatilization from a terpenoid-containing nasal preparation filled in a spray container.

本発明は、テルペノイド含有点鼻剤を、薬剤充填時に薬剤に接する内壁面の材料がエポキシ樹脂、ポリアミドイミド樹脂又はフッ素樹脂であるスプレー容器に充填してなる点鼻用製剤である。   The present invention is a nasal preparation prepared by filling a terpenoid-containing nasal drop into a spray container in which the material of the inner wall surface that comes into contact with the drug at the time of drug filling is an epoxy resin, a polyamide-imide resin, or a fluororesin.

本発明によれば、スプレー容器に充填されたテルペノイド含有点鼻剤中のテルペノイドの含量が保存中に減少するのを抑制することができる。   ADVANTAGE OF THE INVENTION According to this invention, it can suppress that the content of the terpenoid in the terpenoid containing nasal drop with which the spray container was filled reduces during a preservation | save.

テルペノイドにはモノテルペン、セスキテルペン、ジテルペンが包含され、その例としては、メントール、ボルネオール、カンフル、ゲラニオール、シネオール、アネトール、リモネン、オイゲノール、ユーカリ油、ファルネソール、ネロリドール、フィトール又はセンブレンなどが挙げられる。好ましいのはメントール、ボルネオール、カンフル、ユーカリ油などである。   Terpenoids include monoterpenes, sesquiterpenes, diterpenes, examples of which include menthol, borneol, camphor, geraniol, cineol, anethole, limonene, eugenol, eucalyptus oil, farnesol, nerolidol, phytol or semblene. . Preference is given to menthol, borneol, camphor, eucalyptus oil and the like.

テルペノイドは点鼻剤中に、必要に応じて選択される他の成分、例えば血管収縮剤、抗ヒスタミン剤、殺菌剤、消炎剤、局所麻酔剤、抗アレルギー剤、収斂剤などと共に配合することができる。   Terpenoids can be blended in nasal drops with other components selected as necessary, for example, vasoconstrictors, antihistamines, bactericides, anti-inflammatory agents, local anesthetics, antiallergic agents, astringents and the like.

本発明において、スプレー容器の充填薬剤に接する内壁面を形成する材料であるエポキシ樹脂としては、例えばエポキシフェノール樹脂が挙げられ、フッ素樹脂としては、例えばフッ化ビニリデン樹脂が挙げられる。スプレー容器における充填薬剤に接する内壁面をこれらの樹脂で形成するには薬剤充填部自体をこれらの樹脂で作製してもよく、またこれらの樹脂で内壁面を塗装して樹脂の被膜として形成させてもよい。これらの樹脂面は充填された点鼻剤中のテルペノイドの吸収、揮散を妨げ、その含有量低下を抑制することができる。   In the present invention, examples of the epoxy resin that is a material forming the inner wall surface in contact with the filling agent of the spray container include an epoxy phenol resin, and examples of the fluororesin include a vinylidene fluoride resin. In order to form the inner wall surface in contact with the filling drug in the spray container with these resins, the drug filling part itself may be made of these resins, or the inner wall surface may be painted with these resins to form a resin film. May be. These resin surfaces prevent absorption and volatilization of terpenoids in the filled nasal drops, and can suppress a decrease in the content thereof.

スプレー容器は手動噴射式又は自動噴射式スプレー容器を包含する。自動噴射式の場合はフロンやLPGのような液化ガスの代りに圧縮空気などの圧縮ガスを用いることもできる。
以下に実施例の形で本発明をさらに説明する。
Spray containers include manual or automatic spray containers. In the case of the automatic injection type, a compressed gas such as compressed air can be used instead of a liquefied gas such as Freon or LPG.
The invention is further described below in the form of examples.

試験液(点鼻薬)
〔処方〕
塩酸テトラヒドロゾリン 0.1g
マレイン酸クロルフェニラミン 0.5g
塩化ベンゼトニウム 0.02g
リドカイン 0.5g
L−メントール 0.015g
ユーカリ油 0.005g
塩酸 適量
水酸化ナトリウム 適量
精製水 適量

(pH6.0) 計100ml
Test solution (nasal drops)
[Prescription]
Tetrahydrozoline hydrochloride 0.1g
Chlorpheniramine maleate 0.5g
Benzethonium chloride 0.02g
Lidocaine 0.5g
L-Menthol 0.015g
Eucalyptus oil 0.005g
Hydrochloric acid appropriate amount sodium hydroxide appropriate amount purified water appropriate amount

(PH 6.0) Total 100ml

〔試験方法〕
ポリエチレン製及びポリプロピレン製の各容器(容量5.5ml)にそれぞれ試験液5mlを入れて気密にし、また、内壁面に内面コート剤のエポキシフェノール、ポリアミドイミド又はフッ化ビニリデン樹脂を塗布した各アルミ缶容器(容量15ml)にそれぞれ試験液14mlと圧縮空気(6.5Kg/cm2 )を入れて気密にし、室温で静置、保存した。4週間経過後、各試験液中のl−メントール及びユーカリ油の残存量をガスクロマトグラフィーにより測定した。結果は下表のとおりである。
〔Test method〕
Each aluminum can in which 5 ml of the test solution is put in a polyethylene and polypropylene container (capacity 5.5 ml), respectively, and the inner wall surface is coated with epoxyphenol, polyamideimide or vinylidene fluoride resin as an inner surface coating agent. Each container (capacity: 15 ml) was filled with 14 ml of the test solution and compressed air (6.5 Kg / cm 2 ) to be airtight, allowed to stand at room temperature and stored. After 4 weeks, the residual amounts of l-menthol and eucalyptus oil in each test solution were measured by gas chromatography. The results are shown in the table below.

〔試験結果〕
残存率(単位:%)

Figure 2007262100
〔Test results〕
Residual rate (unit:%)
Figure 2007262100

表から明らかなように、ポリエチレン製の容器では、l−メントール及びユーカリ油が残存せず、ポリプロピレン製容器では残存率がそれぞれ僅かに15.6%及び16.5%である。一方、エポキシフェノール、ポリアミドイミド又はフッ化ビニリデン樹脂を内壁面に塗布した容器では残存率がそれぞれ65.2〜67.1%及び76.3〜78.9%を示した。この結果からエポキシフェノール、ポリアミドイミド、及びフッ化ビニリデン樹脂で内壁面が形成された容器には充填された薬剤中のテルペノイド含量の減少を顕著に抑制することが判る。   As is apparent from the table, in the polyethylene container, l-menthol and eucalyptus oil do not remain, and in the polypropylene container, the residual ratios are only 15.6% and 16.5%, respectively. On the other hand, in the container in which epoxyphenol, polyamideimide or vinylidene fluoride resin was applied to the inner wall surface, the residual ratios were 65.2 to 67.1% and 76.3 to 78.9%, respectively. From this result, it can be seen that the decrease in the terpenoid content in the drug filled in the container having the inner wall surface formed of epoxyphenol, polyamideimide, and vinylidene fluoride resin is markedly suppressed.

本発明によれば、スプレー容器に充填されたテルペノイド含有点鼻剤中のテルペノイドの含量が保存中に減少するのを抑制することができるので、保存中のテルぺノイドの含有量低下を顧慮することなく点鼻剤を製造することができる。   According to the present invention, since the terpenoid content in the terpenoid-containing nasal drops filled in the spray container can be suppressed during the storage, the terpenoid content during the storage is reduced. The nasal drops can be produced without any problems.

Claims (3)

充填される薬剤が容器に接する内壁面をエポキシ樹脂、ポリアミドイミド樹脂又はフッ素樹脂で形成したスプレー容器にテルペノイドを含有する鼻炎用点鼻剤を充填することを特徴とするスプレー剤保存中のテルペノイドの含量低下抑制方法。   A terpenoid during storage of a spray, characterized in that a nasal drop containing terpenoid is filled in a spray container in which an inner wall surface in contact with the container is made of epoxy resin, polyamideimide resin or fluororesin. Content reduction control method. 内壁面がエポキシ樹脂、ポリアミドイミド樹脂又はフッ素樹脂である請求項1記載の抑制方法。   The suppression method according to claim 1, wherein the inner wall surface is an epoxy resin, a polyamideimide resin, or a fluororesin. エポキシ樹脂がエポキシフェノール樹脂であり、フッ素樹脂がフッ化ビニリデン樹脂である請求項1記載の抑制方法。   The suppression method according to claim 1, wherein the epoxy resin is an epoxy phenol resin and the fluororesin is a vinylidene fluoride resin.
JP2007189146A 2007-07-20 2007-07-20 Method for preventing reduction in content of terpenoid Withdrawn JP2007262100A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
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Application Number Priority Date Filing Date Title
JP2007189146A JP2007262100A (en) 2007-07-20 2007-07-20 Method for preventing reduction in content of terpenoid

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
JP36219197A Division JP4498480B2 (en) 1997-12-10 1997-12-10 Nasal formulation

Publications (1)

Publication Number Publication Date
JP2007262100A true JP2007262100A (en) 2007-10-11

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Country Status (1)

Country Link
JP (1) JP2007262100A (en)

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