JP4634589B2 - Food or pharmaceutical ready-to-use agent - Google Patents
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Description
【０００１】
【発明の属する技術分野】
本発明は、水又は液状物質を添加し混合するだけで、加熱及び冷却処理を必要とせず、速やかにゲル状またはペースト状になり、嚥下機能の低い人でも食品や医薬品を容易に服用することが可能となる易服用化剤に関するものである。
【０００２】
【従来の技術】
近年、医療現場からは、有効性、安定性、品質は勿論、より患者に対する負担の少ない薬剤の提供が求められるようになり、特に高齢化社会に向けての問題点として、食物摂取機能障害（義歯装着、咀嚼力の低下、嚥下障害等）により経口服用薬剤が服用できない或いは食事が摂取できない患者が増加している。
【０００３】
このような医療現場からの要望に対応して、水なしで服用できる錠剤（口腔内速崩錠）、ドライシロップ剤、ゼリー剤、グミ製剤、シート状製剤等が開発され、その一部が発売されている。
【０００４】
また、食物摂取が困難な患者のために、寒天やゼラチンを用いて食物をゼリー化させる素材が既に発売されている。
【０００５】
従って、医療現場においては服用し難い医薬品製剤を小児や老人に投与する為に、粉砕した錠剤や、細粒剤等を清涼飲料水、牛乳、ヨーグルト等嗜好品と混合して液状或いはペースト状にして与える等工夫がなされている。
【０００６】
また医療現場外では、介護を要する寝たきりの患者に、通常の錠剤、細粒剤等を上記手投で服用させるためには、介護人にかなりの手間が必要になるばかりか医薬品に関する専門的知識が要求される。
【０００７】
【発明が解決しようとする課題】
本発明者らは、乳幼児、嚥下機能の低下した高齢者、寝たきりの患者は勿論のこと通常の患者でも固形製剤や液剤が飲めないという人に、食品又は医薬品を経口的に服用させる際、本易服用化剤と混合し、或いは薬剤を予め含んだ易服用化剤はそのまま、適量の液体を加えることにより速やかにゲル化或いはペースト状になり、容易に嚥下可能となる易服用化剤を提供するものである。上記のような患者の中には液体でさえも服用できなくなる人もおり、このような場合、ゼリー状のものが良いと言われている。従来の技術で述べた服用性の改善を目的として既に開発されている医薬品の数は非常に少なく、依然として服用性の改善を要する医薬品が大多数である。本易服用化剤は服用性改善を目的とした医薬品開発に利用されるばかりでなく、種々の既存医薬品又は服用性改善を必要とする既存医薬品と混合しその服用性を改善しうるものである。また、寒天や通常のゼラチンを用いたものは加熱や冷却を必要とするが、本易服用化剤はその必要がないことから介護者の手間を軽減できる。更に本易服用化剤が粉末又は粒状物質であることから、ゼリー剤のような特別な容器は必要なく携帯に便利である。以上のように本易服用化剤は幅広い医薬品や食材に利用でき、患者に対する服用時の負担は勿論、介護者の負担をも軽減し、生活の質の向上を提供するものである。
【０００８】
【課題を解決するための手投】
本発明者らは、これら問題点を解決すべく、本易服用化剤が医薬品と配合されるケースを想定し、特に散剤、細粒剤、顆粒剤、ドライシロップ剤、錠剤の粉砕品等の服用性改善を目的として、医薬品と混合した後、少量の水の添加で容易にゲル化或いはペースト化し、食品ゼリーと遜色のない服用性を持つ易服用化剤の検討を行った。その結果、室温では固体であるが水の添加でゲル化する物質（ゲル化剤）の１種或いは２種以上に、糖アルコール類を混合することにより、瞬時にゲル化する易服用化剤を調製するに至った。
【０００９】
本発明の易服用化剤に使用可能なゲル化剤としては、多糖類、ペプチド類、ゴム、天然樹脂等の天然高分子とその関連誘導体又は合成高分子を用いることができ、特にアルギン酸又はその塩（例えばナトリウム塩）、キサンタンガム、ローカストビーンガム、アラビアゴム、グァーガム、ペクチン、トラガント、ゼラチン、水溶性ゼラチン、寒天、デンプン、デンプングリコール酸ナトリウム、ヒドロキシプロピルセルロース、カルメロースナトリウム、ヒドロキシエチルセルロース、ヒドロキシプロピルメチルセルロース、カルボキシビニルポリマー、アルギン酸プロピレングリコールエーテル、グルコノーδ−ラクトン、コンドロイチン硫酸ナトリウム、ステアリン酸ナトリウム、デキストラン、ポリビニルアルコール部分けん化物、メチルセルロース、ヒドロキシエチルメチルセルロース、ポリアクリル酸ナトリウム、ポリオキシエチレン（１６０）ポリオキシプロピレン（３０）グリコール、ポリビニルピロリドン等が使用できる。これらの１種又は２種以上を組み合わせて用いることができる。中でも、水溶性ゼラチン、ヒドロキシプロピルメチルセルロース、カルボキシビニルポリマーが好ましい。
【００１０】
本発明の易服用化剤には、上記成分以外にさらに１種或いは２種以上の、甘味剤、矯味剤、香料、色素、苦味マスキング剤、製剤原料、食品素材、医薬品等を加えることができる。
【００１１】
本発明において、ゲル化剤である水溶性ゼラチンのゲル化を促進するためには、水添加時の水溶性ゼラチンのママコの発生を抑制する必要があり、水溶性ゼラチン１重量部に対して糖アルコール１重量部以上を配合することが望ましい。更にゲル化促進を充分に発揮させるためには水溶性ゼラチン１重量部に対して糖アルコール３重量部以上を配合することが好ましい。
【００１２】
本発明で用いられる糖アルコールとしては溶解熱（吸収熱量）が−２０ＫＪ／ｋｇ以下のものであれば特に制限はなく、−１００ＫＪ／ｋｇ以下であればより好ましい。例としては、キシリトール、ソルビトール、マンニトール、エリスリトールなどが挙げられる。水溶性ゼラチンのゲル化促進を充分に発揮させるためには、溶解時の吸収熱量の大きいエリスリトールを用いることが望ましい。これらの糖アルコールは、単独で用いるのみでなく、２種以上を組み合わせることもできる。なお、これら糖アルコール類は水に極めて溶けやすく、甘味があり服用性改善にもつながる。
【００１３】
更に、本発明において、ヒドロキシプロピルメチルセルロース、カルボキシビニルポリマーのいずれか又は両方を添加することにより溶解熱が−２０ＫＪ／ｋｇ以下好ましくは−１００ＫＪ／ｋｇ以下の糖アルコールによる水溶性ゼラチンのゲル化促進を更に向上することができる。
【００１４】
これらゲル化剤と糖アルコールを用いた易服用化剤は、少量の水の添加で速やかにゲル化し、食品又は嗜好品のゼリー菓子と遜色のない食感のものが得られる。また、加える水の量を調節することにより、服用者の好み或いは介護者が患者の健康状態に応じ、ペースト状からハードゼリー状のものまで自在に調製できる。
【００１５】
また、本発明の易服用化剤は、既存の医薬品製剤と混合し、少量の水の添加で速やかにゲル化するため、通常のゼリー剤のように、保存時の安定性への配慮や工程数の多い複雑な製造方法を必要としない。
【００１６】
本発明の易服用化剤を医薬品と予め混合した製剤とする場合、散剤、細粒剤、顆粒剤、ドライシロップ剤などとすることができる。これらの製剤は、上記易服用化剤と薬物を用いて常法により製造することができる。この場合においては、賦形剤（乳糖、コーンスターチ、ショ糖、マンニトール、結晶セルロース、軽質無水ケイ酸、リン酸水素カルシウム等）、結合剤（ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、ゼラチン、ポリビニルピロリドン、部分アルファー化デンプン、メチルセルロース、プルラン、デキストリン、アラビアゴム等）、崩壊剤（カルボキシメチルセルロースカルシウム、低置換度ヒドロキシプロピルセルロース、デンプン類、カルメロースナトリウム）、滑沢剤（ステアリン酸マグネシウム、ステアリン酸カルシウム、硬化ヒマシ油、タルク、ショ糖脂肪酸エステル、ラウリル硫酸ナトリウム等）を添加することができ、これらを２種以上添加してもよい。この他、必要に応じ界面活性剤、溶解補助剤、緩衝剤、保存剤、香料、色素、矯味剤、矯臭剤等を本発明の効果を損なわない範囲で配合することができる。
【００１７】
本発明における易服用性とは、水を服用することなく、低い咀嚼力及び嚥下力でも、服用し易いペースト状或いはゼリー状の形態を容易に提供しうるものである。
【００１８】
【実施例】
以下、本発明を実施例に基づき更に詳細に説明する。尚、本発明の易服用化剤は実施例に記載された処方例に限定されるものではない。
【００１９】
＜実施例１＞
【表１】
易服用化剤のゲル化剤として、室温下で固体で経口投与可能であり、かつ少量の水の添加でゲル化の可能性ある物質を選択した（表１）。ゲル化の評価は以下の方法で行った。
【００２１】
（各種ゲル化剤のゲル化時間測定法）
各ゲル化剤を丸底共栓遠心沈澱管にとり、約２６℃の水１ｍＬを加え直ちに３０秒間混和した。混和後、静置し３０秒毎に試料を傾斜させ、ゲル化の確認をした。ゲル化時間は試料を倒立させる時、試料が流動せず丸底共栓遠心沈澱管内で形状が保持される時点とした。尚、測定は室温下で行った。
【００２２】
【表２】
選択したゲル化剤のゲル化時間測定結果を表２に示した。測定の結果、選択したゲル化剤のうち、比較的速やかにゲル化したものは、水溶性ゼラチン、ヒドロキシプロピルメチルセルロース、カルボキシビニルポリマーの３品であった。中でも水溶性ゼラチンはゲル化に約４５分要するものの、形成されたゲルはハードゼリー状（弾性体）であり、易服用化剤のゲル化剤として理想的なゲルを形成することが分かった。しかし、ゲル化時間がやや長いためゲル化時間の短縮化を検討することにした。
【００２４】
＜実施例２＞
【表３】
表３に示すように水溶性ゼラチン１重量部に対し、各種糖アルコールを１〜５重量部添加し乳鉢中で混合し、易服用化剤を調製した。調製した易服用化剤について以下に示す方法でゲル化の評価を行った。
【００２６】
（易服用化剤のゲル化時間測定法）
表３に示す採取量だけ丸底共栓遠心沈澱管にとり、約２６℃の水１ｍＬを加え直ちに３０秒間混和した。混和後、静置し３０秒毎に試料を傾斜させ、ゲル化の確認をした。ゲル化時間は試料を倒立させる時、試料が流動せず丸底共栓遠心沈澱管内で形状が保持される時点とした。尚、測定は室温下で行った。
【００２７】
実施例２の結果をもとに水溶性ゼラチンのゲル化時間に対する各種糖アルコール添加量の影響を図表１に示した。
水溶性ゼラチン１重量部に対し、いずれの糖アルコールも１重量部の添加で水溶性ゼラチンのゲル化時間は約３分の１に短縮された。しかし、水溶性ゼラチンのママコは確認されたままであった。更に糖アルコールの配合比率を２〜３重量部に増加させていくと、ママコの消失と共に更にゲル化時間は短縮された。この時点におけるゲル化時間短縮は糖アルコールの添加に伴う水溶性ゼラチンのママコ抑制が大きく関与していると思われた。ママコ消失後は、配合比が増大してもゲル化時間はほぼ一定であった。ママコ消失時における各種糖アルコール類の水溶性ゼラチンのゲル化時間への影響には差が認められた。これより、糖アルコールのゲル化促進作用はママコの抑制以外に他の要因が存在すると考えられた。そこで、ゲル形成時に添加している水に各種糖アルコールが溶解する時生じる溶解熱（吸収熱量）に注目し、ゲル化時間との関係を調べた。
【００２９】
【表４】
表４に検討に用いた糖アルコールの溶解熱を示した。実施例２の中で水溶性ゼラチンのママコの消失が認められた水溶性ゼラチン１重量部に対し、各種糖アルコール類３重量部を添加した組成物のゲル化時間と、表４に示した各種糖アルコール類の溶解熱の関係を図表２に示した。
図表２に示すようにゲル化時間と溶解熱の間には負の相関が認められ、吸収熱量の大きい糖アルコールほど水溶性ゼラチンのゲル化時間を促進した。つまり、水を添加した際、溶解時の吸収熱量の大きい糖アルコールを添加したものほど、系全体の温度が低くなり水溶性ゼラチンのゲル化が促進される。
【００３２】
糖アルコールは水溶性ゼラチンのママコ抑制と糖アルコールが有する溶解熱の相乗効果でゲル化を促進した。中でも、エリスリトールがその作用が最も大きかった。
【００３３】
＜実施例３＞
実施例２の結果から、ゲル化時間が約２分である水溶性ゼラチン１重量部に対し、エリスリトール３重量部の組成である易服用化剤▲１▼に、実施例１でゲル化時間が０分であったヒドロキシプロピルメチルセルロース又はカルボキシビニルポリマーを添加し更にゲル化時間の短縮を試みた。
【００３４】
【表５】
表５に示す組成で易服用化剤▲１▼とヒドロキシプロピルメチルセルロース、カルボキシビニルポリマーを丸底遠心沈澱管に採取し軽く振り混ぜた後、実施例２で示した方法でゲル化の評価を行った。
【００３６】
【表６】
表６に示すように易服用化剤▲１▼のゲル化時間はヒドロキシプロピルメチルセルロースの添加により更に短縮された。一方、カルボキシビニルポリマーは、ハードゼリー状（弾性体）のものが形成されず、逆にゲル化時間が遅延した。
【００３８】
実施例３の結果から、ゲル化時間が大幅に改善された易服用化剤▲１▼８重量部に対し、ヒドロキシプロピルメチルセルロース１重量部を添加した組成物を易服用化剤▲２▼として、既存医薬品及び既存薬物混合時のゲル化時間の変化を調べた。
【００３９】
【表７】
表７に示す組成で易服用化剤と既存医薬品及び薬物を丸底共栓遠心沈澱管に採取し軽く振り混ぜた後、以下に示した方法でゲル化の評価を行った。
【００４１】
（ゲル化時間測定法）
試料を採取した丸底共栓遠心沈澱管に、約２６℃の水３ｍＬを加え直ちに３０秒間混和した。混和後、静置し３０秒毎に試料を傾斜させ、ゲル化の確認を行った。ゲル化時間は試料を倒立させる時、試料が流動せず丸底共栓遠心沈澱管内で形状が保持される時点とした。尚、測定は室温下で行った。
【００４２】
図表３に既存医薬品及び薬物混合時の易服用化剤のゲル化時間を示した。
図表３に示すように既存医薬品及び既存薬物を添加した結果、易服用化剤のゲル化時間が僅かに遅延したものも認められたが、全て１分以内にゲル化した。また、得られたゲルはハードゼリー状であった。
【００４４】
【発明の効果】
本発明はゲル形成高分子（水溶性ゼラチン、ヒドロキシプロピルメチルセルロース）と甘味剤（エリスリトール）を混合した易服用化剤であり、咀嚼及び嚥下機能の低い乳幼児及び高齢者、介護を有する寝たきりの患者等で飲みにくいと思われる既存医薬品と混合し少量の水で速やかにゲル化しゼリー状とすることにより服用性が改善される。また、介護者の調製の手間等の問題も、水を添加して混ぜるだけで、加熱や冷却もなしに僅か１分程度でゲル化することより改善される。また、得られたゼリーの硬さは添加する水の量で調整可能である。更に、本易服用化剤はゼリーを用時調製可能であることより、通常のゼリー剤において問題となる複雑な製造工程が不要、保存時の微生物による汚染或いは物理化学的安定性の確保、携帯が不便等の問題も改善される。[0001]
BACKGROUND OF THE INVENTION
The present invention simply adds water or a liquid substance and mixes it, and does not require heating and cooling treatment, quickly becomes a gel or paste, and even a person with low swallowing function can easily take food and medicine. It relates to an easy-to-use agent that makes it possible.
[0002]
[Prior art]
In recent years, medical sites have been required to provide drugs with less burden on patients as well as efficacy, stability, and quality. Especially, as a problem for an aging society, food intake dysfunction ( Increasing number of patients are unable to take oral medications or eat meals due to dentures, reduced masticatory power, dysphagia, and the like.
[0003]
In response to these demands from the medical field, tablets that can be taken without water (orally disintegrating in the oral cavity), dry syrups, jelly preparations, gummi preparations, sheet preparations, etc. have been developed, and some of them have been released. ing.
[0004]
In addition, for patients who have difficulty in taking food, a material that makes food jelly using agar or gelatin has already been put on the market.
[0005]
Therefore, in order to administer pharmaceutical preparations that are difficult to take in the medical field to children and the elderly, pulverized tablets, fine granules, etc. are mixed with luxury products such as soft drinks, milk, yogurt to make liquid or paste. Have been devised.
[0006]
Outside of the medical field, in order for bedridden patients who need nursing care to take ordinary tablets, fine granules, etc. with the above-mentioned manual throwing, not only caregivers need considerable effort but also expertise in pharmaceuticals. Is required.
[0007]
[Problems to be solved by the invention]
When the present inventors orally administer food or medicine to an infant, an elderly person who has decreased swallowing function, a bedridden patient, or a normal patient who cannot drink solid preparations or liquids, Providing an easy-to-swallow agent that can be easily swallowed by mixing with an easy-to-take agent or by adding an appropriate amount of liquid to the easy-to-take agent that contains the drug in advance. To do. Some of these patients cannot take even liquids, and in such cases, it is said that a jelly-like one is good. The number of drugs already developed for the purpose of improving ingestion as described in the prior art is very small, and the majority of drugs still require improvement in ingestion. This easy-to-use agent is not only used for drug development with the aim of improving dosing, but can be mixed with various existing drugs or existing drugs that need to be improved to improve their dosage. . Moreover, although the thing using an agar and normal gelatin needs heating and cooling, since this easy-to-use agent is not necessary, the caregiver's effort can be reduced. Furthermore, since the ready-to-use agent is a powder or a granular substance, a special container such as a jelly agent is not necessary and is convenient to carry. As described above, this easy-to-use agent can be used for a wide range of medicines and foods, and reduces the burden on caregivers as well as the burden on patients, and provides an improvement in the quality of life.
[0008]
[Hand throws to solve problems]
In order to solve these problems, the present inventors assumed a case where the easy-to-use agent is mixed with a pharmaceutical product, and in particular, taking powders, fine granules, granules, dry syrups, tablet pulverized products, etc. For the purpose of improving the properties, we investigated easy-to-use agents that were easily gelled or pasted by adding a small amount of water after mixing with pharmaceuticals, and that have a dose comparable to food jelly. As a result, an easy-to-use agent that gels instantly by mixing sugar alcohols with one or more substances (gelators) that are solid at room temperature but gel with addition of water. It came to prepare.
[0009]
As the gelling agent that can be used in the easy-to-use agent of the present invention, natural polymers such as polysaccharides, peptides, rubbers, natural resins and related derivatives or synthetic polymers can be used. Salt (for example, sodium salt), xanthan gum, locust bean gum, gum arabic, guar gum, pectin, tragacanth, gelatin, water-soluble gelatin, agar, starch, sodium starch glycolate, hydroxypropyl cellulose, carmellose sodium, hydroxyethyl cellulose, hydroxypropyl Methyl cellulose, carboxyvinyl polymer, propylene glycol alginate, glucono δ-lactone, sodium chondroitin sulfate, sodium stearate, dextran, polyvinyl alcohol partial saponified product, Le cellulose, hydroxyethyl cellulose, sodium polyacrylate, polyoxyethylene (160) polyoxypropylene (30) glycol, polyvinylpyrrolidone and the like can be used. These 1 type (s) or 2 or more types can be used in combination. Of these, water-soluble gelatin, hydroxypropylmethylcellulose, and carboxyvinyl polymer are preferable.
[0010]
In addition to the above components, one or more kinds of sweeteners, flavoring agents, fragrances, pigments, bitterness masking agents, pharmaceutical raw materials, food materials, pharmaceuticals and the like can be added to the easy-to-use agent of the present invention. .
[0011]
In the present invention, in order to promote the gelation of water-soluble gelatin which is a gelling agent, it is necessary to suppress the occurrence of mamako of water-soluble gelatin when water is added. It is desirable to blend at least 1 part by weight of alcohol. Further, in order to sufficiently promote gelation, it is preferable to blend 3 parts by weight or more of sugar alcohol with 1 part by weight of water-soluble gelatin.
[0012]
The sugar alcohol used in the present invention is not particularly limited as long as the heat of dissolution (absorption heat amount) is -20 KJ / kg or less, and more preferably -100 KJ / kg or less. Examples include xylitol, sorbitol, mannitol, erythritol and the like. In order to sufficiently promote the gelation of water-soluble gelatin, it is desirable to use erythritol which has a large heat of absorption at the time of dissolution. These sugar alcohols can be used alone or in combination of two or more. These sugar alcohols are extremely soluble in water, have a sweet taste, and lead to improved dosing.
[0013]
Furthermore, in the present invention, by adding either or both of hydroxypropylmethylcellulose and carboxyvinyl polymer, gelation of water-soluble gelatin by sugar alcohol having a heat of dissolution of -20 KJ / kg or less, preferably -100 KJ / kg or less is promoted. Further improvement can be achieved.
[0014]
These easy-to-use agents using a gelling agent and a sugar alcohol rapidly gel with the addition of a small amount of water, and have a texture that is inferior to that of food or luxury jelly sweets. In addition, by adjusting the amount of water to be added, the user's preference or caregiver can freely prepare a paste-like hard jelly-like one according to the patient's health condition.
[0015]
In addition, the easy-to-use agent of the present invention is mixed with an existing pharmaceutical preparation and quickly gelled by the addition of a small amount of water. A large number of complicated manufacturing methods are not required.
[0016]
When the easy-to-use agent of the present invention is a preparation previously mixed with a pharmaceutical product, it can be a powder, a fine granule, a granule, a dry syrup or the like. These preparations can be produced by a conventional method using the above-mentioned easy-to-use agent and drug. In this case, excipients (lactose, corn starch, sucrose, mannitol, crystalline cellulose, light anhydrous silicic acid, calcium hydrogen phosphate, etc.), binders (hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, polyvinylpyrrolidone, partial Alpha-modified starch, methylcellulose, pullulan, dextrin, gum arabic, etc.), disintegrant (carboxymethylcellulose calcium, low-substituted hydroxypropylcellulose, starches, carmellose sodium), lubricant (magnesium stearate, calcium stearate, hardened castor) Oil, talc, sucrose fatty acid ester, sodium lauryl sulfate, etc.) can be added, and two or more of these may be added. In addition, a surfactant, a solubilizing agent, a buffering agent, a preservative, a fragrance, a coloring matter, a corrigent, a corrigent, and the like can be blended as needed without impairing the effects of the present invention.
[0017]
The easy applicability in the present invention can easily provide a paste-like or jelly-like form that is easy to take even with low chewing and swallowing power without taking water.
[0018]
【Example】
Hereinafter, the present invention will be described in more detail based on examples. The easy-to-use agent of the present invention is not limited to the prescription examples described in the examples.
[0019]
<Example 1>
[Table 1]
As a gelling agent for an easy-to-use agent, a substance that can be orally administered in a solid state at room temperature and can be gelled by adding a small amount of water was selected (Table 1). The gelation was evaluated by the following method.
[0021]
(Method for measuring the gelation time of various gelling agents)
Each gelling agent was placed in a round bottom plug centrifuge tube, and 1 mL of water at about 26 ° C. was added and immediately mixed for 30 seconds. After mixing, the mixture was allowed to stand and the sample was tilted every 30 seconds to confirm gelation. The gelation time was set to the time when the sample did not flow when the sample was inverted and the shape was maintained in the round bottom stoppered centrifugal tube. The measurement was performed at room temperature.
[0022]
[Table 2]
The gelation time measurement results of the selected gelling agents are shown in Table 2. As a result of the measurement, among the selected gelling agents, those that gelled relatively quickly were water-soluble gelatin, hydroxypropylmethylcellulose, and carboxyvinyl polymer. Among them, although water-soluble gelatin required about 45 minutes for gelation, it was found that the gel formed was hard jelly (elastic) and formed an ideal gel as a gelling agent for easy-to-use agents. However, since the gelation time is slightly long, it was decided to consider shortening the gelation time.
[0024]
<Example 2>
[Table 3]
As shown in Table 3, 1 to 5 parts by weight of various sugar alcohols were added to 1 part by weight of water-soluble gelatin and mixed in a mortar to prepare an easy-to-use agent. The prepared easy-to-use agent was evaluated for gelation by the following method.
[0026]
(Method for measuring the gelation time of easy-to-use agents)
The collected amount shown in Table 3 was placed in a round bottom stoppered centrifugal tube, and 1 mL of water at about 26 ° C. was added and immediately mixed for 30 seconds. After mixing, the mixture was allowed to stand and the sample was tilted every 30 seconds to confirm gelation. The gelation time was set to the time when the sample did not flow when the sample was inverted and the shape was maintained in the round bottom stoppered centrifugal tube. The measurement was performed at room temperature.
[0027]
Based on the results of Example 2, the effect of various sugar alcohol addition amounts on the gelation time of water-soluble gelatin is shown in Table 1.
Addition of 1 part by weight of any sugar alcohol to 1 part by weight of water-soluble gelatin shortened the gelation time of water-soluble gelatin by about one third. However, the water-soluble gelatin Mamako remained confirmed. Furthermore, when the blending ratio of the sugar alcohol was increased to 2 to 3 parts by weight, the gelation time was further shortened with the disappearance of mamako. The shortening of the gelation time at this point seemed to be largely related to the suppression of water soluble gelatin caused by the addition of sugar alcohol. After Mamako disappeared, the gelation time was almost constant even when the blending ratio increased. Differences were observed in the effects of various sugar alcohols on the gelation time of water-soluble gelatin when Mamako disappeared. From this, it was considered that there are other factors other than the suppression of mamako in the gelling promotion effect of sugar alcohol. Therefore, the heat of dissolution (absorption heat) generated when various sugar alcohols are dissolved in the water added during gel formation was examined, and the relationship with the gelation time was investigated.
[0029]
[Table 4]
Table 4 shows the heat of dissolution of the sugar alcohol used in the study. The gelation time of the composition in which 3 parts by weight of various sugar alcohols were added to 1 part by weight of the water-soluble gelatin in which the disappearance of the water-soluble gelatin in Example 2 was observed, and the various types shown in Table 4 The relationship of the heat of dissolution of sugar alcohols is shown in Chart 2.
As shown in Fig. 2, a negative correlation was observed between the gelation time and the heat of dissolution, and the sugar alcohol having a larger amount of heat of absorption promoted the gelation time of water-soluble gelatin. That is, when water is added, the temperature of the entire system is lowered and the gelation of water-soluble gelatin is promoted as the sugar alcohol having a larger amount of heat of absorption at the time of dissolution is added.
[0032]
Sugar alcohol promoted gelation by the synergistic effect of maco-inhibition of water-soluble gelatin and heat of dissolution of sugar alcohol. Among them, erythritol had the largest effect.
[0033]
<Example 3>
From the results of Example 2, the gelling time in Example 1 was changed to the easy-to-use agent (1) having a composition of 3 parts by weight of erythritol for 1 part by weight of water-soluble gelatin having a gelation time of about 2 minutes. Hydroxypropyl methylcellulose or carboxyvinyl polymer which was 0 minutes was added to further reduce the gelation time.
[0034]
[Table 5]
An easy-to-use agent (1), hydroxypropylmethylcellulose, and carboxyvinyl polymer having the composition shown in Table 5 were collected in a round bottom centrifuge tube and lightly mixed, and then the gelation was evaluated by the method shown in Example 2. It was.
[0036]
[Table 6]
As shown in Table 6, the gelation time of the easy-to-use agent (1) was further shortened by the addition of hydroxypropylmethylcellulose. On the other hand, the carboxyvinyl polymer was not formed into a hard jelly-like (elastic body), and on the contrary, the gelation time was delayed.
[0038]
From the results of Example 3, the composition obtained by adding 1 part by weight of hydroxypropylmethylcellulose to 8 parts by weight of the easy-to-use agent with greatly improved gelation time (1) was used as the easy-to-use agent (2). The change of gelation time when mixing existing drugs and existing drugs was investigated.
[0039]
[Table 7]
An easy-to-use agent, an existing drug and a drug having the composition shown in Table 7 were collected in a round-bottom plug centrifuge tube and gently shaken, and then gelation was evaluated by the method described below.
[0041]
(Gelation time measurement method)
3 mL of water at about 26 ° C. was added to the round bottom stoppered centrifugal tube from which the sample was collected, and immediately mixed for 30 seconds. After mixing, the mixture was allowed to stand and the sample was tilted every 30 seconds to confirm gelation. The gelation time was set to the time when the sample did not flow when the sample was inverted and the shape was maintained in the round bottom stoppered centrifugal tube. The measurement was performed at room temperature.
[0042]
Chart 3 shows the gelation time of the ready-to-use agent when mixing existing drugs and drugs.
As shown in Chart 3, as a result of adding existing drugs and existing drugs, some gelling times of the easy-to-use agents were slightly delayed, but all gelled within 1 minute. Moreover, the obtained gel was hard jelly-like.
[0044]
【The invention's effect】
The present invention is an easy-to-use agent in which a gel-forming polymer (water-soluble gelatin, hydroxypropylmethylcellulose) and a sweetener (erythritol) are mixed, and infants and the elderly with low chewing and swallowing functions, bedridden patients with care, etc. Ingestion is improved by mixing with existing medicine that seems to be difficult to drink and gelling quickly with a small amount of water to form a jelly. In addition, problems such as caregivers' preparation time can be improved by adding water and mixing, and gelling in about 1 minute without heating or cooling. Moreover, the hardness of the obtained jelly can be adjusted with the quantity of the water to add. Furthermore, since the ready-to-use agent can be prepared at the time of use, it does not require a complicated manufacturing process, which is a problem with ordinary jelly preparations. It can be contaminated by microorganisms during storage or ensure physicochemical stability. However, problems such as inconvenience are also improved.
Claims (4)
水溶性ゼラチン、ヒドロキシプロピルメチルセルロース、および溶解熱が−１５３KJ/Kg以下である糖アルコールを含有する易服用化剤。 An easy-to-take agent that is powder or granular and that facilitates the swallowing of foods or pharmaceuticals to be mixed,
An easy-to-use agent comprising water-soluble gelatin, hydroxypropylmethylcellulose, and a sugar alcohol having a heat of dissolution of −153 KJ / Kg or less .
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| JP2000291419A JP4634589B2 (en) | 2000-09-26 | 2000-09-26 | Food or pharmaceutical ready-to-use agent |
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| JP2000291419A JP4634589B2 (en) | 2000-09-26 | 2000-09-26 | Food or pharmaceutical ready-to-use agent |
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| JP4634589B2 true JP4634589B2 (en) | 2011-02-16 |
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| CN1964699B (en) | 2004-06-07 | 2010-12-08 | 株式会社吴羽 | Dry-form composition for oral ingestion and gel-form composition for oral ingestion of type prepared at time of use |
| WO2016004952A1 (en) * | 2014-07-08 | 2016-01-14 | Fertin Pharma A/S | Oral delivery system comprising two compartments |
| WO2017038732A1 (en) * | 2015-08-31 | 2017-03-09 | 大蔵製薬株式会社 | Water-containing pharmaceutical formulation of montelukast |
| CN111936168A (en) * | 2018-04-17 | 2020-11-13 | 株式会社大赛璐 | Easily administrable granule and method for producing the same |
| CN116440074B (en) * | 2023-05-26 | 2024-02-20 | 浙江高跖医药科技股份有限公司 | Potassium chloride oral preparation and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993004670A1 (en) * | 1991-08-30 | 1993-03-18 | Showa Yakuhin Kako Co., Ltd. | Dry gel composition |
| JP2000157212A (en) * | 1998-11-25 | 2000-06-13 | Lion Corp | Readily swallowable auxiliary composition and composition for food and composition for medicine using the same |
| JP2000279107A (en) * | 1999-03-30 | 2000-10-10 | Lion Corp | Noncariogenic easy deglutition composition and food composition and medical composition using the same |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3068343B2 (en) * | 1992-08-12 | 2000-07-24 | 昭和薬品化工株式会社 | Composition for diagnosing swallowing function |
| JP4309481B2 (en) * | 1996-01-12 | 2009-08-05 | テイコクメディックス株式会社 | Jelly oral pharmaceutical composition |
| JP3257983B2 (en) * | 1997-07-31 | 2002-02-18 | 株式会社龍角散 | Drug swallowing aid drink |
| JP3524359B2 (en) * | 1997-12-26 | 2004-05-10 | 伊那食品工業株式会社 | Feeding aid paste for people with difficulty in chewing and swallowing |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993004670A1 (en) * | 1991-08-30 | 1993-03-18 | Showa Yakuhin Kako Co., Ltd. | Dry gel composition |
| JP2000157212A (en) * | 1998-11-25 | 2000-06-13 | Lion Corp | Readily swallowable auxiliary composition and composition for food and composition for medicine using the same |
| JP2000279107A (en) * | 1999-03-30 | 2000-10-10 | Lion Corp | Noncariogenic easy deglutition composition and food composition and medical composition using the same |
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