JP2010053056A - Sustained release preparation and method for producing the same - Google Patents

Sustained release preparation and method for producing the same Download PDF

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JP2010053056A
JP2010053056A JP2008218293A JP2008218293A JP2010053056A JP 2010053056 A JP2010053056 A JP 2010053056A JP 2008218293 A JP2008218293 A JP 2008218293A JP 2008218293 A JP2008218293 A JP 2008218293A JP 2010053056 A JP2010053056 A JP 2010053056A
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drug component
release preparation
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temperature volatile
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JP5435911B2 (en
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Takahiko Iida
孝彦 飯田
Kensuke Kawarada
研介 瓦田
Rumi Konuma
ルミ 小沼
Iwao Miyazaki
巌 宮崎
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Tokyo Metropolitan Industrial Technology Research Instititute (TIRI)
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a sustained release preparation which can slowly release an ordinary temperature volatile drug component easy to vaporize in a short period, has a small amount of waste, can easily judge the disappearance of the effect of the drug component, has high safety to the human body, furthermore can incorporate a drug component at high concentration, and is easy to adjust the content of the drug component and a method for producing the same. <P>SOLUTION: The sustained release preparation is obtained by mixing a silane alkoxide hydrolyzate fluid with a drug component volatile at normal temperatures to form a mixed fluid and adding a curing catalyst to this mixed fluid to solidify the resulting mixture. <P>COPYRIGHT: (C)2010,JPO&amp;INPIT

Description

本発明は、徐放性製剤とその製造方法に関するものである。   The present invention relates to a sustained-release preparation and a method for producing the same.

従来、防かび剤、抗菌剤、殺虫・防虫剤、消臭剤、香料などの常温揮発性薬剤成分を徐放させる徐放性製剤が知られている(特許文献1、2参照)。   Conventionally, sustained-release preparations that release room-temperature volatile chemical components such as fungicides, antibacterial agents, insecticides / insecticides, deodorants, and fragrances are known (see Patent Documents 1 and 2).

例えば、徐放性製剤として、常温揮発性薬剤成分をゼオライト、不織布、紙などに含浸させたもの、常温揮発性薬剤成分をゲル化させたものなどが知られている。また、防かび剤等としてアリルイソチオシアネートを用いた場合には、エタノールに溶解して揮発性を調整することや(非特許文献1参照)、担持体としてのシリカゲルをアリルイソチオシアネートに含浸し、シリカゲルの細孔内にアリルイソチオシアネートを担持させることで徐放性製剤とすること(特許文献3参照)が提案されている。
特開平10−158112号公報 特開平3−145404号公報 特開2005−255532号公報 J. Food Hyg. Soc. Japan, 35, 365-370 (1994)
For example, known sustained-release preparations include those obtained by impregnating a normal temperature volatile drug component with zeolite, nonwoven fabric, paper, or the like, and those obtained by gelling a normal temperature volatile drug component. When allyl isothiocyanate is used as a fungicide or the like, it is dissolved in ethanol to adjust volatility (see Non-Patent Document 1), or silica gel as a support is impregnated in allyl isothiocyanate, It has been proposed to make a sustained-release preparation by supporting allyl isothiocyanate in the pores of silica gel (see Patent Document 3).
JP-A-10-158112 JP-A-3-145404 JP 2005-255532 A J. Food Hyg. Soc. Japan, 35, 365-370 (1994)

しかしながら、従来の徐放性製剤は、初期の放出速度が高く、放出速度の調整が困難で経時的に放出量が減少するため、長期に渡って安定して薬剤成分を放出することが難しいという問題点があった。   However, conventional sustained-release preparations have a high initial release rate, it is difficult to adjust the release rate, and the amount of release decreases over time, so it is difficult to stably release drug components over a long period of time. There was a problem.

また、常温揮発性薬剤成分をゲル化させたものは、ゲル化剤は親水性であるのに対し、防かび剤などの薬剤成分の多くは親油性であり、均一に分散させるためには界面活性剤などを用いる必要があった。さらに、これらのゲル化固形物は通常、専用のプラスチック製容器やガラス製容器に詰められて市販されているが、使用後は容器が廃棄物となり、省資源や廃棄物減量化の点で問題があった。   In addition, gelation of room-temperature volatile drug components is that the gelling agent is hydrophilic, whereas many drug components such as fungicides are oleophilic, and in order to disperse uniformly, the interface It was necessary to use an activator or the like. In addition, these gelled solids are usually marketed in dedicated plastic containers or glass containers, but after use, the containers become waste, which is problematic in terms of resource saving and waste reduction. was there.

また、アリルイソチオシアネートをエタノールに溶解した場合、揮発性の調整は可能であるが、有効成分であるアリルイソチオシアネートが変質してしまうことが報告されている(非特許文献1参照)。   Moreover, when allyl isothiocyanate is dissolved in ethanol, volatility can be adjusted, but it has been reported that allyl isothiocyanate, which is an active ingredient, is altered (see Non-Patent Document 1).

また、アリルイソチオシアネートをシリカゲルに含浸して担持させる技術では、シリカゲルの細孔容積に限界があるため含浸量に限界があり、有効成分であるアリルイソチオシアネートを高濃度に含有する製剤の創製が難しいという問題点や、その含有量を自由に調整することが難しいという問題点があった。   In addition, in the technology of impregnating and supporting allyl isothiocyanate on silica gel, the amount of impregnation is limited because the pore volume of silica gel is limited, and the creation of a preparation containing allyl isothiocyanate, which is an active ingredient, at a high concentration is possible. There was a problem that it was difficult and it was difficult to freely adjust its content.

本発明は、以上の通りの事情に鑑みてなされたものであり、短期間で気化し易い常温揮発性薬剤成分を緩やかに放出することができ、廃棄物量が少なく、薬剤成分の効果の消失を容易に判別することができ、人体への安全性も高く、さらに薬剤成分を高濃度に含有させることができ、薬剤成分の含有量の調整が容易な徐放性製剤とその製造方法を提供することを課題としている。   The present invention has been made in view of the circumstances as described above, and can slowly release a room-temperature volatile drug component that is easily vaporized in a short period of time, reducing the amount of waste, and eliminating the effect of the drug component. Provided are a sustained-release preparation that can be easily discriminated, has high safety to the human body, can contain a high concentration of drug components, and can easily adjust the content of drug components, and a method for producing the same. It is an issue.

本発明は、上記の課題を解決するために、以下のことを特徴としている。   The present invention is characterized by the following in order to solve the above problems.

第1:シランアルコキシド加水分解液と、常温揮発性薬剤成分とを混合し、この混合液に硬化触媒を添加して固化したものであることを特徴とする徐放性製剤。   First: A sustained-release preparation characterized in that a silane alkoxide hydrolyzed solution and a room temperature volatile drug component are mixed and a curing catalyst is added to the mixed solution to solidify.

第2:常温揮発性薬剤成分は、防かび剤、抗菌剤、殺虫・防虫剤、消臭剤、および香料から選ばれる少なくとも1種であることを特徴とする上記第1の徐放性製剤。   Second: The first sustained-release preparation as described above, wherein the room temperature volatile drug component is at least one selected from a fungicide, an antibacterial agent, an insecticide / insecticide, a deodorant, and a fragrance.

第3:シランアルコキシド加水分解液と、常温揮発性薬剤成分とを混合して混合液を調製する工程と、この混合液に硬化触媒を添加して加水分解反応を進行させ混合液を固化させる工程とを含むことを特徴とする徐放性製剤の製造方法。   Third: A step of mixing a silane alkoxide hydrolyzed solution and a room temperature volatile chemical component to prepare a mixed solution, and a step of adding a curing catalyst to the mixed solution to advance a hydrolysis reaction to solidify the mixed solution. And a method for producing a sustained-release preparation.

本発明の徐放性製剤によれば、常温揮発性薬剤成分を予めシランアルコキシド加水分解液と混合し、この混合液に硬化触媒を添加して固化して製剤とすることで、短期間で気化し易い常温揮発性薬剤成分を緩やかに放出することができる。   According to the sustained-release preparation of the present invention, a room temperature volatile drug component is mixed with a silane alkoxide hydrolyzed solution in advance, and a curing catalyst is added to the mixed solution to solidify it into a preparation. The room temperature volatile drug component that is easily converted can be released slowly.

また、徐放に伴い容積が減少し、薬剤成分の効果の消失時には容積が大幅に減少しているため、薬剤成分の効果の消失を容易に判別することができ、また廃棄物量を少なくすることができる。さらに、容器や包装体に収容する場合にも選択の幅が広く、省資源化および廃棄物減量化を考慮して適切なものとすることができる。   In addition, the volume decreases with the sustained release, and when the effect of the drug component disappears, the volume greatly decreases. Therefore, the disappearance of the effect of the drug component can be easily identified, and the amount of waste should be reduced. Can do. Furthermore, the range of selection is also wide when accommodated in a container or a package, and it can be made appropriate in consideration of resource saving and waste reduction.

また、基材としてのシリカゲルは安全性が高いものであり、特に天然系の薬剤成分を用いることで人体への安全性を高いものとすることができる。   Further, silica gel as a base material has high safety, and in particular, by using a natural drug component, safety to the human body can be increased.

また、常温揮発性薬剤成分を予めシランアルコキシド加水分解液と混合し、この混合液に硬化触媒を添加して固化して製剤とすることで、常温揮発性薬剤成分をシリカゲルに含浸して担持させる場合に比べて薬剤成分を高濃度に含有させることができ、さらに薬剤成分の含有量の調整も容易である。   In addition, normal temperature volatile drug component is mixed with silane alkoxide hydrolysis solution in advance, and a curing catalyst is added to this mixed solution to solidify it into a preparation, so that normal temperature volatile drug component is impregnated and supported on silica gel. Compared to the case, the drug component can be contained at a high concentration, and the content of the drug component can be easily adjusted.

本発明の徐放性製剤の製造方法によれば、常温揮発性薬剤成分を予めシランアルコキシド加水分解液と混合し、この混合液に硬化触媒を添加して固化して製剤とすることで、短期間で気化し易い常温揮発性薬剤成分を緩やかに放出することができ、廃棄物量が少なく、薬剤成分の効果の消失を容易に判別することができ、人体への安全性も高い徐放性製剤を容易に調製することができる。   According to the method for producing a sustained-release preparation of the present invention, a normal temperature volatile drug component is mixed with a silane alkoxide hydrolyzed solution in advance, and a curing catalyst is added to the mixed solution to solidify it into a preparation. Sustained-release preparations that can slowly release volatile drug components that are easily vaporized between them, have a small amount of waste, can easily determine the disappearance of the effects of drug components, and are highly safe for the human body Can be easily prepared.

また、常温揮発性薬剤成分を予めシランアルコキシド加水分解液と混合し、この混合液に硬化触媒を添加して固化して製剤とすることで、常温揮発性薬剤成分をシリカゲルに含浸して担持させる場合に比べて薬剤成分を高濃度に含有させることができ、さらに薬剤成分の含有量の調整も容易である。   In addition, normal temperature volatile drug component is mixed with silane alkoxide hydrolysis solution in advance, and a curing catalyst is added to this mixed solution to solidify it into a preparation, so that normal temperature volatile drug component is impregnated and supported on silica gel. Compared to the case, the drug component can be contained at a high concentration, and the content of the drug component can be easily adjusted.

以下、本発明を詳細に説明する。   Hereinafter, the present invention will be described in detail.

本発明に用いられるシリコンアルコキシド加水分解液は、シリコンアルコキシド含有液に水を添加し加水分解を進行させて調製したものであり、シリコンアルコキシドの具体例としては、トリメトキシシラン、テトラメトキシシラン、トリエトキシシラン、テトラエトキシシラン、テトラプロポキシシラン、テトラブトキシシラン等の炭素数1〜4の低級アルキル基を有するトリまたはテトラアルコキシシランあるいはそれらのオリゴマーなどが挙げられる。中でも、テトラメトキシシラン、テトラエトキシシラン、およびそれらのオリゴマーが好ましい。   The silicon alkoxide hydrolyzed liquid used in the present invention is prepared by adding water to a silicon alkoxide-containing liquid and allowing hydrolysis to proceed. Specific examples of silicon alkoxide include trimethoxysilane, tetramethoxysilane, Examples thereof include tri- or tetraalkoxysilanes having a lower alkyl group having 1 to 4 carbon atoms such as ethoxysilane, tetraethoxysilane, tetrapropoxysilane, and tetrabutoxysilane, and oligomers thereof. Of these, tetramethoxysilane, tetraethoxysilane, and oligomers thereof are preferable.

シリコンアルコキシド加水分解液を調製するに際し、加水分解時には、必要に応じて水と相溶性のあるアルコール類などの溶媒を添加してもよい。具体的には、炭素数1〜3の低級アルコール類、ジメチルホルムアミド、ジメチルスルホキシド、アセトン、テトラヒドロフラン、メチルエチルケトン、その他の水と任意に混合できる有機溶媒を用いることができる。   In preparing the silicon alkoxide hydrolyzed solution, a solvent such as alcohol having compatibility with water may be added as needed during the hydrolysis. Specifically, lower alcohols having 1 to 3 carbon atoms, dimethylformamide, dimethyl sulfoxide, acetone, tetrahydrofuran, methyl ethyl ketone, and other organic solvents that can be arbitrarily mixed with water can be used.

本発明に用いられるシリコンアルコキシド加水分解液として、エチルシリケートを加水分解させて得られる、アルコール中にシリカ(SiO2)がコロイド状に分散したアルコール性シリカゾルが好適なものとして例示される。なお、エチルシリケート加水分解液がアルコール性シリカゾルであるのは、エチルシリケートと水は互いに溶解しないため、エチルシリケートと水にそれぞれ可溶な溶媒である、アルコール系溶媒を用いて加水分解した試薬を用いているためである。 As the silicon alkoxide hydrolyzate used in the present invention, an alcoholic silica sol obtained by hydrolyzing ethyl silicate in which silica (SiO 2 ) is colloidally dispersed in alcohol is exemplified as a preferable one. The ethyl silicate hydrolyzed solution is an alcoholic silica sol because ethyl silicate and water are insoluble in each other. Therefore, a hydrolyzed reagent using an alcohol solvent, which is a solvent soluble in ethyl silicate and water, respectively. It is because it uses.

本発明に用いられる常温揮発性薬剤成分の種類は特に制限されず、目的とする徐放性製剤の用途に応じて適宜に選択すればよい。常温揮発性薬剤成分の具体例としては、防かび剤、抗菌剤、殺虫・防虫剤、消臭剤、香料などが挙げられる。なお、ここで「常温揮発性」とは、25℃において薬剤として有効な程度の揮発性を示すことを意味する。また、常温揮発性薬剤成分には、有効成分としての薬剤化合物を揮発性有機溶媒などに溶解したものを含む。   The kind of the room-temperature volatile drug component used in the present invention is not particularly limited, and may be appropriately selected depending on the intended use of the sustained-release preparation. Specific examples of the room temperature volatile chemical component include a fungicide, an antibacterial agent, an insecticide / insect repellent, a deodorant, and a fragrance. Here, “normal temperature volatility” means that it exhibits an effective volatility as a drug at 25 ° C. Further, the room temperature volatile drug component includes a drug compound as an active ingredient dissolved in a volatile organic solvent.

防かび剤の具体例としては、天然系または合成系の防かび剤、例えば、アリルイソチオシアネート、それ以外の天然植物から得られる精油などが挙げられる。これらは1種単独で用いてもよく、2種類以上を併用してもよい。   Specific examples of the fungicide include natural or synthetic fungicides, such as allyl isothiocyanate, and other essential oils obtained from natural plants. These may be used alone or in combination of two or more.

抗菌剤の具体例としては、天然系または合成系の抗菌剤、例えば、ヒバオイル、月桃オイル、ペニーロイヤル、レモングラス、レモン、スパイスクラベンダー、ナツメグ、オレガノ、セージ、ジンジャー、セーボリー、タイム、ヒノキチオール、オールスパイス、シダーウッド、シナモンバーク、クローブバッズ、カユブテ、パイン、ティートゥリー、カプサイシン、スクワレン、スクワラン、アーモンドオイル、ノニルフェノールスルホン酸銅、ジネブ、アンゼブ、チウラム、ポリオキシン、シクロヘキシミド、ヒアルロン酸化合物などが挙げられる。これらは1種単独で用いてもよく、2種類以上を併用してもよい。   Specific examples of antibacterial agents include natural or synthetic antibacterial agents such as hiba oil, moon peach oil, penny royal, lemongrass, lemon, spice lavender, nutmeg, oregano, sage, ginger, savory, thyme, hinokitiol. , Allspice, cedarwood, cinnamon bark, clovebuds, cayubute, pine, tea tree, capsaicin, squalene, squalane, almond oil, copper nonylphenol sulfonate, dineb, anzeb, thiuram, polyoxin, cycloheximide, hyaluronic acid compounds, etc. . These may be used alone or in combination of two or more.

殺虫・防虫剤の具体例としては、農薬用殺虫剤としてのサリチオン、マラソン、ジメトエート、ダイアジノン、ジエチルアミド、2−エチルチオメチルフェニルメチルカルバメート、チオリン酸、2−メチル−3−シクロヘキセン−1−カルボン酸;除草剤としてのクロメトキシニル、ニトラリン、3−(3,3−ジメチルウレイド)フェニル−tert−ブチルカルバメート、害虫忌避剤・防虫剤としてのピレスロイド系化合物、パラジクロルベンゼン、ナフタリン、樟脳、N,N−ジエチル−m−トルアミドなどが挙げられる。これらは1種単独で用いてもよく、2種類以上を併用してもよい。   Specific examples of insecticides and insecticides include salicione, marathon, dimethoate, diazinon, diethylamide, 2-ethylthiomethylphenylmethylcarbamate, thiophosphoric acid, 2-methyl-3-cyclohexene-1-carboxylic acid as insecticides for agricultural chemicals Cromethoxynil, nitralin, 3- (3,3-dimethylureido) phenyl-tert-butylcarbamate as herbicides, pyrethroid compounds as insect repellents and insect repellents, paradichlorobenzene, naphthalene, camphor, N, N- Examples include diethyl-m-toluamide. These may be used alone or in combination of two or more.

消臭剤の具体例としては、天然系または合成系の消臭剤、例えば、ヒノキ油、ローズ油、ラベンダー油、アビエス油、ベルガモット油、ビターアーモンド油、カナンガ油、カシア油、シダーリーフ油、シダーウッド油、シナモン油、シトロネラ油、ゲラニウム油、ホー油、ラバンジン油、レモン油、ライム油、ナツメグ油、オークモス油、オリガナム油、ペチグレン油、ペパーミント油、パイン油、スターアニス油、スイートオレンジ油、テレビン油、ベチバー油、メチルメタクリレート、エチルメタクリレート、ラウリルメタクリレート、ステアリルメタクリレート、ピルビン酸エチル、マレイン酸ジメチルなどが挙げられる。これらは1種単独で用いてもよく、2種類以上を併用してもよい。   Specific examples of the deodorant include natural or synthetic deodorants such as cypress oil, rose oil, lavender oil, abies oil, bergamot oil, bitter almond oil, cananga oil, cassia oil, cedar leaf oil, Cedarwood oil, cinnamon oil, citronella oil, geranium oil, ho oil, lavandin oil, lemon oil, lime oil, nutmeg oil, oak moss oil, origanum oil, pettigren oil, peppermint oil, pine oil, star anise oil, sweet orange oil, Examples include turpentine oil, vetiver oil, methyl methacrylate, ethyl methacrylate, lauryl methacrylate, stearyl methacrylate, ethyl pyruvate, and dimethyl maleate. These may be used alone or in combination of two or more.

香料の具体例としては、天然系または合成系の香料、例えば、脂肪族炭化水素、テルペン炭化水素、芳香族炭化水素等の炭化水素類;脂肪族アルコール、テルペンアルコール、芳香族アルコール等のアルコール類;脂肪族エーテル、芳香族エーテル等のエーテル類;脂肪族オキサイド、テルペン類のオキサイド等のオキサイド類;脂肪族アルデヒド、チオアルデヒド、芳香族アルデヒド等のアルデヒド類;脂肪族ケトン、テルペンケトン、水素化芳香族ケトン、脂肪族環状ケトン、非ベンゼン系芳香族ケトン、芳香族ケトン等のケトン類;アセタール類、ケタール類、フェノール類、フェノールエーテル類、脂肪酸、テルペン系カルボン酸、水素化芳香族カルボン酸、芳香族カルボン酸等の酸類;酸アマイド類、脂肪族ラクトン、環状ラクトン、テルペン系ラクトン、水素化芳香族ラクトン、芳香族ラクトン等のラクトン類、脂肪族エステル、フラン系のカルボン酸族エステル;脂肪族環状カルボン酸エステル、芳香族カルボン酸エステル等のエステル類;ニトロムスク類、ニトリル、アミン、ピリジン類、キノリン類、ピロール、インドール等の含窒素化合物などの合成系香料;動物、植物からの天然系香料;天然系香料および/また合成系香料を含む調合香料などが挙げられる。これらは1種単独で用いてもよく、2種類以上を併用してもよい。   Specific examples of the fragrances include natural or synthetic fragrances, for example, hydrocarbons such as aliphatic hydrocarbons, terpene hydrocarbons and aromatic hydrocarbons; alcohols such as aliphatic alcohols, terpene alcohols and aromatic alcohols. Ethers such as aliphatic ethers and aromatic ethers; oxides such as aliphatic oxides and terpene oxides; aldehydes such as aliphatic aldehydes, thioaldehydes and aromatic aldehydes; aliphatic ketones, terpene ketones, hydrogenation Ketones such as aromatic ketones, aliphatic cyclic ketones, non-benzene aromatic ketones, aromatic ketones; acetals, ketals, phenols, phenol ethers, fatty acids, terpene carboxylic acids, hydrogenated aromatic carboxylic acids Acids such as aromatic carboxylic acids; acid amides, aliphatic lactones, cyclic lactates Terpenoid lactones, hydrogenated aromatic lactones, lactones such as aromatic lactones, aliphatic esters, furan carboxylic acid esters; aliphatic cyclic carboxylic acid esters, aromatic carboxylic acid esters, etc .; nitromusks Synthetic fragrances such as nitrogen-containing compounds such as nitriles, amines, pyridines, quinolines, pyrrole and indole; natural fragrances from animals and plants; blended fragrances containing natural fragrances and / or synthetic fragrances It is done. These may be used alone or in combination of two or more.

本発明では、上記した常温揮発性薬剤成分をシランアルコキシド加水分解液と混合して混合液を調製し、次いでこの混合液に炭酸アンモニウム等の塩基性アンモニウム、モルホリン、トリエチルアミン等のアミンなどの硬化触媒を添加して加水分解反応を進行させて固化(ゲル化)させることで徐放性製剤が製造される。固化時において型に入れて成形物を得ることもでき、また、固化物を粉末状に粉砕することも可能である。常温揮発性薬剤成分として防かび剤のアリルイソチオシアネートを用い、エチルシリケート加水分解液と混合して徐放性製剤を製造する場合の例を図1のフローチャートに示す。   In the present invention, the above-mentioned room temperature volatile drug component is mixed with a silane alkoxide hydrolyzed solution to prepare a mixed solution, and then the mixed catalyst is a basic ammonium such as ammonium carbonate, a curing catalyst such as an amine such as morpholine and triethylamine. A sustained-release preparation can be produced by adding hydrogel and allowing the hydrolysis reaction to proceed and solidify (gelate). It is possible to obtain a molded product by putting it in a mold at the time of solidification, and it is also possible to pulverize the solidified product into a powder form. The flow chart of FIG. 1 shows an example of producing a sustained-release preparation by using an antifungal allyl isothiocyanate as a room temperature volatile drug component and mixing with an ethyl silicate hydrolyzate.

本発明の徐放性製剤は、薬剤成分を透過可能な容器または包装体に収容して用いることもできる。例えば、薬剤成分が透過できる空孔を全面または一部に設けた、樹脂、紙、木材、金属、セラミックスなどを基材とする袋状、箱状、筒状などの容器または包装体に本発明の徐放性製剤を収容することができる。また、薄膜、板、フィルムなどの上に本発明の徐放性製剤を展伸したものを何層かに積層したものや、薬剤成分に対して透過性を示す樹脂からなる成形体の中に本発明の徐放性製剤を練り込んで分散させたものとすることができる。   The sustained-release preparation of the present invention can also be used by being contained in a container or package that can permeate the drug component. For example, the present invention can be applied to a bag, box, cylinder, or other container or package having a base material made of resin, paper, wood, metal, ceramics, etc., provided with holes through which a drug component can permeate. The sustained-release preparation can be accommodated. In addition, in a layered product formed by laminating several layers of the sustained-release preparation of the present invention on a thin film, plate, film, etc. The sustained-release preparation of the present invention can be kneaded and dispersed.

以上に説明した本発明の徐放性製剤は、例えば薬剤成分が防かび剤の場合には、各種工業材料・製品、日用品などの保管容器内に入れておくことにより、輸入、輸送、保管期間中において、かびの発生を抑制できる(図2参照)。また、薬剤成分の放出によって徐放性製剤の容積が減少することにより錠剤の薬剤効果の消失が容易に判別できる。   The sustained-release preparation of the present invention described above, for example, when the drug component is an antifungal agent, is placed in a storage container for various industrial materials / products, daily necessities, etc. In the inside, generation | occurrence | production of mold | fungi can be suppressed (refer FIG. 2). Further, the disappearance of the drug effect of the tablet can be easily determined by reducing the volume of the sustained-release preparation due to the release of the drug component.

以下、実施例により本発明をさらに詳しく説明するが、本発明はこれらの実施例に何ら限定されるものではない。
<実施例1>
エチルシリケート加水分解液(コルコート(株)製、HAS−6)に対してアリルイソチオシアネートを10%、20%、30%混合した溶液を調製した。それぞれの混合液に3%炭酸アンモニウム溶液を硬化触媒として滴下し固化させ、十分に固化後、粉砕し、粉末状にした製剤を得た。
EXAMPLES Hereinafter, although an Example demonstrates this invention in more detail, this invention is not limited to these Examples at all.
<Example 1>
A solution in which 10%, 20%, and 30% of allyl isothiocyanate was mixed with ethyl silicate hydrolyzate (manufactured by Colcoat Co., Ltd., HAS-6) was prepared. A 3% ammonium carbonate solution was dropped into each mixed solution as a curing catalyst to solidify, and after sufficiently solidifying, the mixture was pulverized to obtain a powdery formulation.

内径90mmのシャーレに、高圧蒸気滅菌したポテトデキストロース寒天培地を約20mL注入し固化させた。JIS Z 2911:2006かび抵抗性試験に用いる5種類のかびであるAspergillus niger van Tieghem、Penicillium citrinum Thom、Rhizopus oryzae Went et Prinsen-Geerligs、Cladosporium cladosporioides (Fresenius) de Vries およびChaetomium globosum Kunze ex Friesのそれぞれについて、胞子を一定量(5白金耳)とり、湿潤剤添加殺菌水(スルホこはく酸ジオクチルナトリウム50mg/l)10mlに懸濁させ、単一胞子懸濁液とした。   About 20 mL of potato dextrose agar medium sterilized by autoclaving was injected into a petri dish having an inner diameter of 90 mm and solidified. JIS Z 2911: 2006 Five types of fungi used in the mold resistance test, Aspergillus niger van Tieghem, Penicillium citrinum Thom, Rhizopus oryzae Went et Prinsen-Geerligs, Cladosporium cladosporioides (Fresenius) de Vries and Chaetomium globosum Kunze ex Fries, respectively A fixed amount (5 platinum ears) of a spore was taken and suspended in 10 ml of sterilized water with a wetting agent (dioctyl sodium sulfosuccinate 50 mg / l) to obtain a single spore suspension.

単一胞子懸濁液をガラスウールを詰めたロートで濾過し、全量50mlになるように湿潤剤添加殺菌水を加えた。コンラージ棒を濾過後の単一胞子懸濁液に浸し、速やかに上記ポテトデキストロース寒天培地上にコンラージ棒を用いて塗沫した。   The single spore suspension was filtered through a funnel filled with glass wool, and sterilized water with a wetting agent was added to a total volume of 50 ml. The large rod was dipped in the filtered single spore suspension and quickly spread on the potato dextrose agar medium using the large rod.

5種類のかびについて、上記において調製したアリルイソチオシアネートを10%、20%、および30%含有する製剤0.1gを、培地に直接接しないようにアルミ箔を敷き静置した。また、対照試験として、製剤を静置しない培地を用意した。   For 5 types of fungi, 0.1 g of a preparation containing 10%, 20%, and 30% of allyl isothiocyanate prepared above was laid on an aluminum foil so as not to be in direct contact with the medium. As a control test, a medium in which the preparation was not allowed to stand was prepared.

次に、これらの培地を温度28℃、相対湿度90%以上の環境で7日間培養し、かびの生長を観察した。   Next, these media were cultured for 7 days in an environment at a temperature of 28 ° C. and a relative humidity of 90% or more, and the growth of mold was observed.

その結果を表1および図3に示す。   The results are shown in Table 1 and FIG.

製剤を付与しない対照試験では、5種類のかびのそれぞれについてシャーレ全面に旺盛なかびの発生が見られたが、製剤を静置した場合、アリルイソチオシアネートの含有量が10%の場合においても十分にかびの発生が抑制された。
<実施例2>
内径90mmのシャーレに、高圧蒸気滅菌したポテトデキストロース寒天培地を約20mL注入し固化させた。JIS Z 2911:2006かび抵抗性試験に用いる2種類のかびであるAspergillus niger van Tieghem、およびPenicillium citrinum Thom、それぞれについて、胞子を一定量(5白金耳)とり、湿潤剤添加殺菌水(スルホこはく酸ジオクチルナトリウム50mg/l)10mlに懸濁させ、単一胞子懸濁液とした。
In the control test where no preparation was given, vigorous fungi were observed on the entire petri dish for each of the five types of fungi. However, when the preparation was allowed to stand, it was sufficient even when the allyl isothiocyanate content was 10%. The occurrence of mold was suppressed.
<Example 2>
About 20 mL of potato dextrose agar medium sterilized by autoclaving was injected into a petri dish having an inner diameter of 90 mm and solidified. JIS Z 2911: 2006 Aspergillus niger van Tieghem and Penicillium citrinum Thom, which are two types of fungi used in the mold resistance test, take a certain amount of spores (5 platinum ears), add humectant-added sterilized water (sulfosuccinic acid) Dioctyl sodium 50 mg / l) was suspended in 10 ml to form a single spore suspension.

単一胞子懸濁液をガラスウールを詰めたロートで濾過し、全量50mlになるように湿潤剤添加殺菌水を加えた。コンラージ棒を濾過後の単一胞子懸濁液に浸し、速やかに上記ポテトデキストロース寒天培地上にコンラージ棒を用いて塗沫した。   The single spore suspension was filtered through a funnel filled with glass wool, and sterilized water with a wetting agent was added to a total volume of 50 ml. The large rod was dipped in the filtered single spore suspension and quickly spread on the potato dextrose agar medium using the large rod.

一方、実施例1で調製した、アリルイソシアネートを10%含有する製剤を5g入れた別のシャーレを用意した。   On the other hand, another petri dish containing 5 g of a preparation containing 10% of allyl isocyanate prepared in Example 1 was prepared.

次に、2種類のかびを塗沫したシャーレおよび製剤を入れたシャーレを、紙製容器(靴用紙製箱、寸法;幅19cm、長さ31cm、高さ11cm)内に静置し、この容器を温度28℃の環境で1週間培養し、かびの生長を観察した。その結果を表2および図4に示す。   Next, the petri dish coated with two types of fungi and the petri dish containing the preparation are left in a paper container (shoe paper box, dimensions: width 19 cm, length 31 cm, height 11 cm). Was cultured in an environment at a temperature of 28 ° C. for 1 week, and the growth of mold was observed. The results are shown in Table 2 and FIG.

製剤を付与しない対照実験では、2種類のかびのそれぞれについてシャーレ全面に旺盛なかびの発生が見られたが、製剤を静置した場合、かびの発生が抑制された。   In the control experiment in which the preparation was not applied, vigorous fungi were observed on the entire petri dish for each of the two types of fungi, but when the preparation was allowed to stand, the occurrence of fungi was suppressed.

防かび剤のアリルチオイソチオシアネートと、エチルシリケート加水分解液を用いた本発明の徐放性製剤の製造工程の一例を示すフローチャートである。It is a flowchart which shows an example of the manufacturing process of the sustained release formulation of this invention using the antifungal agent allyl thioisothiocyanate and an ethyl silicate hydrolysis liquid. 防かび剤のアリルチオイソチオシアネートと、エチルシリケート加水分解液を用いた本発明の徐放性製剤の工業材料・製品への利用例を示す概念図である。It is a conceptual diagram which shows the example of utilization to the industrial material and product of the sustained release formulation of this invention using the antifungal agent allyl thioisothiocyanate and the ethyl silicate hydrolyzate. 実施例1における試験結果を示した図である。It is the figure which showed the test result in Example 1. 実施例2における試験結果を示した図である。It is the figure which showed the test result in Example 2. FIG.

Claims (3)

シランアルコキシド加水分解液と、常温揮発性薬剤成分とを混合し、この混合液に硬化触媒を添加して固化したものであることを特徴とする徐放性製剤。   A sustained-release preparation characterized in that a silane alkoxide hydrolyzed solution and a room temperature volatile drug component are mixed and a curing catalyst is added to the mixed solution to solidify. 常温揮発性薬剤成分は、防かび剤、抗菌剤、殺虫・防虫剤、消臭剤、および香料から選ばれる少なくとも1種であることを特徴とする請求項1に記載の徐放性製剤。   The sustained-release preparation according to claim 1, wherein the normal temperature volatile drug component is at least one selected from a fungicide, an antibacterial agent, an insecticide / insecticide, a deodorant, and a fragrance. シランアルコキシド加水分解液と、常温揮発性薬剤成分とを混合して混合液を調製する工程と、この混合液に硬化触媒を添加して加水分解反応を進行させ混合液を固化させる工程とを含むことを特徴とする徐放性製剤の製造方法。   It includes a step of preparing a mixed solution by mixing a silane alkoxide hydrolyzed solution and a room temperature volatile chemical component, and a step of adding a curing catalyst to the mixed solution to advance a hydrolysis reaction and solidifying the mixed solution. A method for producing a sustained-release preparation.
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