JP7418679B2 - Delayed gelling composition - Google Patents

Delayed gelling composition Download PDF

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JP7418679B2
JP7418679B2 JP2018198857A JP2018198857A JP7418679B2 JP 7418679 B2 JP7418679 B2 JP 7418679B2 JP 2018198857 A JP2018198857 A JP 2018198857A JP 2018198857 A JP2018198857 A JP 2018198857A JP 7418679 B2 JP7418679 B2 JP 7418679B2
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gelling
adding water
composition
viscosity
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由佳理 垣野
菜月 遠藤
慶裕 菱川
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Ohkura Pharmaceutical Co Ltd
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本発明は、ゲル化組成物の技術分野に属する。本発明は、具体的にはペクチン等のゲル化剤を含むゲル化組成物であって、水を加えて金属イオンの存在下においてゲル化を促しても直ちにはゲル化しない遅延性ゲル化組成物に関するものである。 The present invention belongs to the technical field of gelling compositions. Specifically, the present invention relates to a gelling composition containing a gelling agent such as pectin, which is a delayed gelling composition that does not immediately gel even when water is added to promote gelation in the presence of metal ions. It is about things.

ペクチン等のゲル化剤を含む溶液は、カルシウムイオン等の金属イオンと接するとゲル化を起こし、当該溶液はゾル状態からゲル状態へと転移する。かかる溶液のゲルは通常ゼリー状であり、医薬品の製剤分野や食品分野などで利用されている。例えば、ゼリー状の医薬品(ゼリー剤)は、薬物の持つ苦味や強い甘味をゲル中のマトリックスに包埋し、舌の味蕾細胞との接触を抑えることで味をマスキングするために利用されている。また、ゼリーの持つ流動性から、高齢者や嚥下障害者、あるいは小児に飲み易いものを提供するために利用されている。 A solution containing a gelling agent such as pectin undergoes gelation when it comes into contact with metal ions such as calcium ions, and the solution changes from a sol state to a gel state. The gel of such a solution is usually in the form of a jelly and is used in the pharmaceutical formulation field, food field, etc. For example, jelly-like medicines (jelly preparations) are used to mask the taste of drugs by embedding their bitter or strong sweet taste in a gel matrix and suppressing contact with taste bud cells on the tongue. . In addition, due to the fluidity of jelly, it is used to provide easy-to-drink products to the elderly, people with swallowing disorders, and children.

ゼリー状の医薬品は他にも利点を有する。固形医薬品を服用する場合、通常、水と一緒に摂取するが、慢性腎不全により腎透析を受けている患者などは一日に摂取する水分量に制限がある。このことが服薬コンプライアンスの低下につながっている。しかし、ゼリー状の医薬品の場合、上記の通り、マスキング効果や流動性により、水を摂取することなく、あるいは少量の水で服用することができるため、腎透析を受けている患者など水分摂取量が制限されている患者には有用性が高い。さらに、個包装とすることで、液剤やシロップ剤のように1回服薬量を計量する必要がなく、携帯性にも優れている。 Medicinal products in jelly form have other advantages. When taking solid medicines, they are usually taken with water, but patients undergoing renal dialysis due to chronic renal failure have limits on the amount of water they can ingest each day. This leads to a decline in medication compliance. However, in the case of jelly-like medicines, as mentioned above, due to their masking effect and fluidity, they can be taken without ingesting water or with a small amount of water. It is highly useful for patients with limited mobility. Furthermore, since it is individually packaged, there is no need to measure the amount to be taken each time, unlike liquids and syrups, and it is also highly portable.

一方、一般的なゼリー製剤では、水に弱い薬物には応用しがたいこと、また、加温冷却工程が必要であるため、熱に弱い薬物に対しては応用しがたいという欠点がある。そのような欠点により、ゼリー状の医薬品とすることのできる対象薬物は限られることになる。これらの問題に対しては、例えば、予めゼリーを調製し、凍結乾燥させ、用時加水し復元させるゼリー剤が知られているが、凍結乾燥はコストを要し、また後で薬物とゼリーとを混合することから、薬物の均一化の問題を惹起する。
上記に対し、味のマスキング効果や服用性、携帯性など、ゼリー状の医薬品としての特徴を生かしつつ、使用時に温湯や加熱などの溶解操作を加えず、冷却などの操作も必要とせず、またコストを要する凍結乾燥技術を用いることなく、常温における加水のみで短時間(20~90秒)にゼリー状となる粉末の発明が提案されている(特許文献1)。特許文献1の発明によれば、水に不安定な薬物や熱に不安定な薬物にも応用でき、また後で薬物とゼリーとを混合することもなく、単に粉末に加水するのみでゼリー状の医薬品を短時間に調製することが可能である。
On the other hand, general jelly preparations have the drawback that they are difficult to apply to drugs that are sensitive to water, and because they require a heating and cooling process, they are difficult to apply to drugs that are sensitive to heat. Such drawbacks limit the target drugs that can be made into jelly-like pharmaceuticals. To solve these problems, for example, a jelly preparation is known in which the jelly is prepared in advance, freeze-dried, and then reconstituted by adding water before use. However, freeze-drying is costly, and the drug and jelly are not mixed together afterward. This causes the problem of uniformity of the drug.
In contrast to the above, while taking advantage of the characteristics of a jelly-like drug, such as taste masking effect, ease of administration, and portability, it does not require dissolving operations such as hot water or heating, nor does it require operations such as cooling. An invention has been proposed for a powder that becomes jelly-like in a short time (20 to 90 seconds) simply by adding water at room temperature, without using costly freeze-drying technology (Patent Document 1). According to the invention of Patent Document 1, it can be applied to drugs that are unstable in water or drugs that are unstable to heat, and it is possible to form a jelly by simply adding water to powder without mixing the drug and jelly afterwards. It is possible to prepare several pharmaceutical products in a short time.

特開2008-37804号公報Japanese Patent Application Publication No. 2008-37804

特許文献1の発明は、従来言われていたゼリー剤の欠点を多く克服するものであり、また水を加えてから20~90秒といった短時間でゼリー状(ゲル状)となるため有用である。一方、水を加えてから短時間にゲル化してしまうと、却って不都合な場合がある。例えば、加水溶液を2以上に分ける操作を行うことが困難になるおそれがある。また、加水溶液と他の成分とを均一に混合することが困難になるおそれがある。 The invention of Patent Document 1 overcomes many of the drawbacks of conventional jelly preparations, and is useful because it becomes jelly-like (gel-like) in a short period of time, such as 20 to 90 seconds after adding water. . On the other hand, if it gels within a short period of time after adding water, it may be rather inconvenient. For example, it may become difficult to divide the aqueous solution into two or more parts. Moreover, it may become difficult to uniformly mix the hydrous solution and other components.

本発明は、ゲル化組成物に水を加えた溶液に対して、例えば分注操作や他の成分との混合操作を容易にすることができる新たなゲル化組成物を提供することを主な課題とする。
The main purpose of the present invention is to provide a new gelling composition that can facilitate the dispensing operation and mixing operation with other components for a solution obtained by adding water to the gelling composition. Take it as a challenge.

本発明者らは、鋭意検討を重ねた結果、ゲル化組成物に水を加えて調製した溶液の粘度に着目し、ゲル化が進むに従い経時的に上昇する粘度をコントロールすることにより上記課題を解決しうることを見出し、本発明を完成するに至った。 As a result of extensive studies, the present inventors focused on the viscosity of a solution prepared by adding water to a gelling composition, and solved the above problem by controlling the viscosity that increases over time as gelation progresses. We have found a solution to this problem and have completed the present invention.

本発明として、例えば、以下のものを挙げることができる。
[1]ゲル化に金属イオンを必要とし、水を加え加温冷却操作を行うことなく常温でゾル状態からゲル状態に転移させて使用するゲル化組成物であって、
かかるゲル化組成物に水を加えたゾル溶液は、加水後、金属イオンの存在下において少なくとも90秒間ゾル状態を持続し、加水後1時間までに加水後1分の粘度に対して1.2~1.5倍の粘度に達し、加水後6時間までにゲル状態を呈することを特徴とする、遅延性ゲル化組成物。
[2]前記ゲル化剤が、ペクチン;アルギン酸、その塩、もしくはそのエステル;カラギーナン;またはジェランガムのいずれか1種以上である、上記[1]に記載の遅延性ゲル化組成物。
[3]前記金属イオンを生成する金属塩を含む、上記[1]または[2]に記載の遅延性ゲル化組成物。
[4]前記金属イオンが二価の金属イオンである、上記[1]~[3]のいずれか一項に記載の遅延性ゲル化組成物。
[5]さらに甘味剤を含む、上記[1]~[4]のいずれか一項に記載の遅延性ゲル化組成物。
[6]前記ゲル化剤および前記金属イオンもしくは前記金属塩が分離して存在するか、または前記ゲル化剤および前記金属塩の粉末を含む単純混合物、前記ゲル化剤および前記金属塩を含む造粒物、もしくは前記ゲル化剤および前記金属塩を含む打錠成形物である、上記[1]~[5]のいずれか一項に記載の遅延性ゲル化組成物。
Examples of the present invention include the following.
[1] A gelling composition that requires metal ions for gelation and is used by transforming from a sol state to a gel state at room temperature without adding water and performing a heating and cooling operation,
A sol solution obtained by adding water to such a gelling composition maintains a sol state for at least 90 seconds in the presence of metal ions after adding water, and by 1 hour after adding water, the sol solution has a viscosity of 1.2 to 1 minute after adding water. A delayed gelling composition, which is characterized by reaching a viscosity of ~1.5 times and exhibiting a gel state by 6 hours after adding water.
[2] The delayed gelling composition according to [1] above, wherein the gelling agent is any one or more of pectin; alginic acid, a salt thereof, or an ester thereof; carrageenan; or gellan gum.
[3] The delayed gelling composition according to [1] or [2] above, which contains a metal salt that generates the metal ion.
[4] The delayed gelling composition according to any one of [1] to [3] above, wherein the metal ion is a divalent metal ion.
[5] The delayed gelling composition according to any one of [1] to [4] above, further comprising a sweetener.
[6] The gelling agent and the metal ion or the metal salt exist separately, or a simple mixture containing a powder of the gelling agent and the metal salt, or a composition containing the gelling agent and the metal salt. The delayed gelling composition according to any one of [1] to [5] above, which is a granule or a tablet molded product containing the gelling agent and the metal salt.

[7]上記[1]~[6]のいずれか一項に記載の遅延性ゲル化組成物と薬理活性成分とを含む、遅延性ゲル化医薬品。
[8]上記[1]~[6]のいずれか一項に記載の遅延性ゲル化組成物と食品素材とを含む、遅延性ゲル化食品。
[7] A delayed gelling pharmaceutical comprising the delayed gelling composition according to any one of [1] to [6] above and a pharmacologically active ingredient.
[8] A delayed gelling food comprising the delayed gelling composition according to any one of [1] to [6] above and a food material.

[9]薬理活性成分を含むゼリー状医薬品の製造方法であって、上記[1]~[6]のいずれか一項に記載の遅延性ゲル化組成物と水溶液状または水懸濁液状の経口医薬品とを混合し、加温冷却操作を行うことなくゲル化させる工程を含むことを特徴とする、ゼリー状医薬品の製造方法。
[10]食品素材を含むゼリー状食品の製造方法であって、上記[1]~[6]のいずれか一項に記載の遅延性ゲル化組成物と水溶液状または水懸濁液状の食品とを混合し、加温冷却操作を行うことなくゲル化させる工程を含むことを特徴とする、ゼリー状食品の製造方法。
[9] A method for producing a jelly-like pharmaceutical product containing a pharmacologically active ingredient, which comprises administering the delayed gelling composition according to any one of [1] to [6] above and an oral aqueous solution or aqueous suspension. 1. A method for producing a jelly-like drug, comprising a step of mixing the drug with a drug and gelling it without heating and cooling.
[10] A method for producing a jelly-like food containing a food material, comprising: the delayed gelling composition according to any one of [1] to [6] above; and a food in the form of an aqueous solution or suspension. A method for producing a jelly-like food, comprising the step of mixing and gelling without heating and cooling operations.

本発明に係る遅延性ゲル化組成物は、加水してからゲル状態を呈するまでの時間が比較的長くコントロールされているから、ゾル状態を比較的長く保つことができ、その結果、加水してからの分注(小分け)操作が容易であり、また加水溶液と他の成分との混合操作が容易である。
Since the delayed gelling composition according to the present invention can maintain a sol state for a relatively long time since the time from when water is added to when it exhibits a gel state is controlled, it is possible to maintain a sol state for a relatively long time. The dispensing (subdivision) operation from the liquid is easy, and the mixing operation of the aqueous solution and other components is easy.

以下、本発明について詳述する。
1 本発明に係る遅延性ゲル化組成物
本発明に係る遅延性ゲル化組成物(以下、「本発明組成物」という。)は、ゲル化に金属イオンを必要とし、水を加え加温冷却操作を行うことなく常温でゾル状態からゲル状態に転移させて使用するゲル化組成物であって、かかるゲル化組成物に水を加えたゾル溶液は、加水後、金属イオンの存在下において少なくとも90秒間ゾル状態を持続し、加水後1時間までに加水後1分の粘度に対して1.2~1.5倍の粘度に達し、加水後6時間までにゲル状態を呈することを特徴とする。
The present invention will be explained in detail below.
1 Delayed gelling composition according to the present invention The delayed gelling composition according to the present invention (hereinafter referred to as the "composition of the present invention") requires metal ions for gelation, and is heated and cooled by adding water. A gelling composition that is used by being transformed from a sol state to a gel state at room temperature without any operation, and a sol solution obtained by adding water to such a gelling composition is a gelatinous composition that is used after being transformed from a sol state to a gel state at room temperature. It is characterized by maintaining a sol state for 90 seconds, reaching a viscosity 1.2 to 1.5 times the viscosity at 1 minute after adding water by 1 hour after adding water, and exhibiting a gel state by 6 hours after adding water. do.

本発明で用いられるゲル化剤としては、常温の水に可溶であり、金属イオンの存在下において常温でゲル化を起こすものであれば特に制限されないが、例えば、ペクチン;アルギン酸やアルギン酸ナトリウム、アルギン酸カリウム、アルギン酸アンモニウム、アルギン酸カルシウムなどのアルギン酸塩やアルギン酸エステル;カラギーナン;ジェランガムを挙げることができる。この中、ペクチンやアルギン酸塩が好ましい。また、ペクチンについては、通常、エステル化度(DE)が50%以下のLMペクチンが用いられる。好ましくはDE値が20~30のLMペクチンである。当該ゲル化剤は、ゼリー状の医薬品や食品に用いられている。
上記ゲル化剤は、一種であっても二種以上の併用であってもよい。
The gelling agent used in the present invention is not particularly limited as long as it is soluble in water at room temperature and causes gelation at room temperature in the presence of metal ions, but examples include pectin; alginic acid, sodium alginate, Examples include alginates and alginate esters such as potassium alginate, ammonium alginate, and calcium alginate; carrageenan; and gellan gum. Among these, pectin and alginate are preferred. Regarding pectin, LM pectin having a degree of esterification (DE) of 50% or less is usually used. Preferably, it is LM pectin with a DE value of 20 to 30. The gelling agent is used in jelly-like pharmaceuticals and foods.
The above gelling agents may be used alone or in combination of two or more.

本発明で用いられる金属イオンとしては、医薬品や食品の分野においてゲル化に用いられるものであれば特に制限されず、また用いるゲル化剤の種類により異なるが、例えば、カリウム、ナトリウムなどの一価のカチオン;バリウムイオン、ストロンチウムイオン、カルシウムイオン、亜鉛イオン、マンガンイオン、マグネシウムイオンなどの二価のカチオン;鉄イオンなどの三価のカチオンを挙げることができる。この中、カルシウムイオン、マグネシウムイオンといった二価のカチオンが好ましく、カルシウムイオンがより好ましい。 The metal ions used in the present invention are not particularly limited as long as they are used for gelation in the pharmaceutical and food fields, and vary depending on the type of gelling agent used, but examples include monovalent metal ions such as potassium and sodium. cations; divalent cations such as barium ions, strontium ions, calcium ions, zinc ions, manganese ions, magnesium ions; and trivalent cations such as iron ions. Among these, divalent cations such as calcium ions and magnesium ions are preferred, and calcium ions are more preferred.

上記金属イオンを生成する化合物、即ち金属塩としては、例えば、第一リン酸カルシウム、第二リン酸カルシウム、第三リン酸カルシウム、塩化カルシウム、硫酸カルシウム、酢酸カルシウム、乳酸カルシウム、ステアリン酸カルシウム、クエン酸カルシウム、グリセロリン酸カルシウム、パントテン酸カルシウム、グルコン酸カルシウム、水酸化カルシウム、炭酸カルシウム、等のカルシウム塩;第一リン酸マグネシウム、第二リン酸マグネシウム、第三リン酸マグネシウム、塩化マグネシウム、硫酸マグネシウム、酢酸マグネシウム、乳酸マグネシウム、ステアリン酸マグネシウム、クエン酸マグネシウム、グルコン酸マグネシウム、水酸化マグネシウム、炭酸マグネシウム、等のマグネシウム塩;塩化バリウム、塩化ストロンチウムを挙げることができる。この中、第二リン酸カルシウム、クエン酸カルシウムが好ましい。
上記金属塩は、一種であっても二種以上の併用であってもよい。
Examples of compounds that generate the metal ions, that is, metal salts include monocalcium phosphate, dibasic calcium phosphate, tribasic calcium phosphate, calcium chloride, calcium sulfate, calcium acetate, calcium lactate, calcium stearate, calcium citrate, calcium glycerophosphate, Calcium salts such as calcium pantothenate, calcium gluconate, calcium hydroxide, calcium carbonate; monomagnesium phosphate, dibasic magnesium phosphate, tribasic magnesium phosphate, magnesium chloride, magnesium sulfate, magnesium acetate, magnesium lactate, Examples include magnesium salts such as magnesium stearate, magnesium citrate, magnesium gluconate, magnesium hydroxide, and magnesium carbonate; barium chloride and strontium chloride. Among these, dibasic calcium phosphate and calcium citrate are preferred.
The above metal salts may be used alone or in combination of two or more.

本発明組成物には、必要に応じて、例えば増粘剤、pH調整剤、懸濁・分散剤、甘味剤、香料といった添加剤を任意に適量含むことができる。また、目的に応じて、賦形剤、着色料、安定化剤、可溶化剤、保存剤などを含むこともできる。 The composition of the present invention may optionally contain appropriate amounts of additives such as thickeners, pH adjusters, suspending/dispersing agents, sweeteners, and fragrances, as necessary. Furthermore, depending on the purpose, excipients, coloring agents, stabilizers, solubilizers, preservatives, etc. may be included.

増粘剤としては、例えば、キサンタンガム、ローカストビーンガム、グアガム、タラガム、タマリンドシードガム、でんぷん類、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、プルラン、カルメロースまたはその塩、グルコマンナン、寒天、スクシノグリカンを挙げることができる。
pH調整剤としては、例えば、グルコノδラクトン、クエン酸またはその塩、アジピン酸、フマル酸、フタル酸、コハク酸、リン酸またはその塩、酒石酸またはその塩、乳酸またはその塩を挙げることができる。
Examples of thickeners include xanthan gum, locust bean gum, guar gum, tara gum, tamarind seed gum, starches, hydroxypropylcellulose, hydroxypropylmethylcellulose, pullulan, carmellose or its salts, glucomannan, agar, and succinoglycan. be able to.
Examples of the pH adjusting agent include glucono-delta-lactone, citric acid or a salt thereof, adipic acid, fumaric acid, phthalic acid, succinic acid, phosphoric acid or a salt thereof, tartaric acid or a salt thereof, lactic acid or a salt thereof. .

緩衝剤としては、例えば、リン酸またはその塩、炭酸塩など、分散剤としては、デンプン類、乳糖など、甘味剤としては、アスパルテーム、アセスルファムカリウム、ソーマチン、スクラロース、サッカリンナトリウム、アドバンテーム、グリチルリチン酸二カリウム、ステビア、糖アルコール類、ショ糖、粉末還元麦芽糖水あめ、デキストリンなど、香料としては、各種粉末状の香料をそれぞれ挙げることができる。
上記各種添加剤は、それぞれ一種であっても二種以上の併用であってもよい。
Buffers include phosphoric acid or its salts, carbonates, etc. Dispersants include starches, lactose, etc. Sweeteners include aspartame, acesulfame potassium, thaumatin, sucralose, sodium saccharin, advantame, di-glycyrrhizinate. Examples of the fragrance include various powdered fragrances such as potassium, stevia, sugar alcohols, sucrose, powdered reduced maltose syrup, and dextrin.
The various additives mentioned above may be used alone or in combination of two or more.

本発明組成物は、水を加えるとゾル状態の溶液となり、かかるゾル状態は加水後、金属イオンの存在下において少なくとも90秒間持続するが、加水後3~5分あるいは10分程度はゾル状態を持続することが適当である。そして、本発明組成物の当該ゾル溶液は、加水後1時間までに加水後1分の粘度に対して1.2~1.5倍の粘度に達し、加温冷却操作を行うとこなく加水後6時間までにゲル状態を呈する。当該ゾル溶液は、加水後1時間までに加水後1分の粘度に対して1.2~1.5倍の粘度に達すればよく、例えば、加水後45分までに当該粘度に達してもよく、加水後30分ないし20分ないしは10分までに当該粘度に達することが好ましい。また、当該ゾル溶液は、加温冷却操作を行うとこなく加水後6時間までにゲル状態を呈すればよいが、上記粘度に達する時間に応じて、例えば、加水後3時間までにゲル状態を呈してもよく、加水後1時間ないし30分ないし20分ないしは15分までにゲル状態を呈することが好ましい。 When water is added to the composition of the present invention, it becomes a solution in a sol state, and the sol state lasts for at least 90 seconds in the presence of metal ions after water is added, but the sol state remains for about 3 to 5 or 10 minutes after water is added. It is appropriate to continue. The sol solution of the composition of the present invention reaches a viscosity 1.2 to 1.5 times the viscosity of 1 minute after adding water by 1 hour after adding water, and after adding water without performing heating and cooling operations. It takes on a gel state by 6 hours. The sol solution may reach a viscosity 1.2 to 1.5 times the viscosity of 1 minute after adding water by 1 hour after adding water, for example, it may reach the viscosity by 45 minutes after adding water. It is preferable that the viscosity is reached within 30 minutes to 20 minutes to 10 minutes after adding water. In addition, the sol solution may exhibit a gel state within 6 hours after adding water without performing heating and cooling operations, but depending on the time it takes to reach the above viscosity, for example, the sol solution may exhibit a gel state within 3 hours after adding water. It is preferable that the gel state be exhibited within 1 hour to 30 minutes to 20 minutes to 15 minutes after adding water.

本発明組成物は、ゲル化剤と金属イオンないし金属塩とを含むが、それらが分離して存在していてもよい。このように分離して存在する場合、金属イオンないし金属塩は、粉末等の固形状態であっても、水に溶解ないし懸濁した状態であってもよい。
また、本発明組成物は、例えば、ゲル化剤および金属塩の粉末を含む単純混合物や、ゲル化剤および金属塩を含む造粒物、もしくはゲル化剤および金属塩を含む打錠成形物であってもよい。ゲル化剤と金属塩とが分離して存在する場合、それぞれ別々に造粒物や打錠成形物の形態の中にあってもよい。
The composition of the present invention contains a gelling agent and a metal ion or metal salt, but they may exist separately. When present separately, the metal ions or metal salts may be in a solid state such as a powder, or may be dissolved or suspended in water.
Further, the composition of the present invention may be, for example, a simple mixture containing a powder of a gelling agent and a metal salt, a granulated product containing a gelling agent and a metal salt, or a tablet molded product containing a gelling agent and a metal salt. There may be. When the gelling agent and the metal salt are present separately, they may be present separately in the form of granules or tablets.

本発明組成物中のゲル化剤の含有量は、例えば、0.1~99.9重量%の範囲内で所望により適宜選択することができる。本発明組成物中におけるゲル化剤と金属イオンないし金属塩との含有割合は、それらの種類や所望する遅延性やゲルの硬さなどによって異なるが、ゲル化剤1重量部に対して、通常、金属イオンないし金属塩が0.005~2重量部の範囲内であり、0.01~1.8重量部の範囲内が好ましく、0.1~1.5重量部の範囲内がより好ましい。金属イオンないし金属塩が0.005重量部より少ないと、ゲル化しなかったり、ゲル状態を呈するまで非常に長時間を要するおそれがある。金属イオンないし金属塩が2重量部より多いと、ゲル化しなかったり、ゲル状態を維持できなくなるおそれがある。
The content of the gelling agent in the composition of the present invention can be appropriately selected, for example, within the range of 0.1 to 99.9% by weight. The content ratio of the gelling agent and the metal ions or metal salts in the composition of the present invention varies depending on their types, desired retardation properties, gel hardness, etc., but is usually based on 1 part by weight of the gelling agent. , the metal ion or metal salt is within the range of 0.005 to 2 parts by weight, preferably within the range of 0.01 to 1.8 parts by weight, and more preferably within the range of 0.1 to 1.5 parts by weight. . If the amount of metal ions or metal salts is less than 0.005 parts by weight, it may not gel or it may take a very long time to form a gel state. If the amount of metal ions or metal salts is more than 2 parts by weight, there is a risk that gelation may not occur or the gel state may not be maintained.

2 本発明組成物の使用方法、用途
本発明組成物は、水を加え加温冷却操作を行うことなく常温でゾル状態からゲル状態に転移させることにより使用される。本発明組成物に水を加えた溶液は、ゾル状態から徐々にゲル状態になり、加水後6時間以内にはゲル状態を呈する。ここで常温とは、例えば20℃を挙げることができる。
2 Methods and applications of the composition of the present invention The composition of the present invention is used by transforming it from a sol state to a gel state at room temperature without adding water and performing heating and cooling operations. A solution obtained by adding water to the composition of the present invention gradually changes from a sol state to a gel state, and exhibits a gel state within 6 hours after adding water. Here, the normal temperature can be, for example, 20°C.

本発明組成物に加えることができる水は、特に制限されないが、例えば、精製水や蒸留水、水道水などを挙げることができる。また、当該水は、場合により、前記金属イオンが存在する、または前記金属塩や添加剤などが溶解または懸濁した状態であってもよい。また、本発明組成物がゲル化剤と金属イオンないし金属塩とが分離した状態であれば、当該金属イオンないし金属塩は溶解または懸濁した状態であってもよいが、この場合、当該溶液等を水としてゲル化剤を含む固形物に加え、ゲル状態を形成することもできる。 The water that can be added to the composition of the present invention is not particularly limited, and examples thereof include purified water, distilled water, tap water, and the like. Moreover, the water may be in a state in which the metal ions are present, or the metal salts, additives, and the like are dissolved or suspended. Further, as long as the gelling agent and the metal ion or metal salt are in a separated state in the composition of the present invention, the metal ion or metal salt may be in a dissolved or suspended state; A gel state can also be formed by adding water as water to a solid material containing a gelling agent.

本発明組成物に加える水の温度は、室温ないし常温で十分である。
本発明組成物に加える水の量は、所望により適宜選択されるが、ゲル化剤の濃度が0.3~10重量%の範囲内になる量、好ましくは0.5~5重量%の範囲内になる量、より好ましくは1~3重量%の範囲内になる量である。
The temperature of the water added to the composition of the present invention is sufficiently room temperature to room temperature.
The amount of water added to the composition of the present invention is appropriately selected as desired, but is such that the concentration of the gelling agent is in the range of 0.3 to 10% by weight, preferably in the range of 0.5 to 5% by weight. The amount is preferably within the range of 1 to 3% by weight.

本発明組成物は、加水してから比較的長く(加水してから90秒以上)ゾル状態を保つことができるので、その間に例えば分注(小分け)することができ、他の成分と十分に混合することができる。 Since the composition of the present invention can maintain a sol state for a relatively long time after adding water (90 seconds or more after adding water), it can be dispensed (subdivided) during that time, and can be sufficiently mixed with other ingredients. Can be mixed.

本発明組成物は、薬理活性成分を含んでいてもよいが、含まずに用時調製(Ready-to-use)用のゼリーの素として用いることができる。薬理活性成分を含まない本発明組成物の場合、例えば調剤現場などにて、薬理活性成分またはそれを含む医薬品と本発明組成物(ゼリーの素)とを混合し、分包して提供することができる。その分包を受け取った患者は、それに水を加えてゲル化しゼリー状として服用することができる。また、患者側にて、処方された薬理活性成分ないし医薬品と本発明組成物(ゼリーの素)とを混合し、水を加えてゲル化しゼリー状として服用することもできる。
本発明組成物は、上記のような医薬品用に限らず、食品用のゼリーの素としても用いることができる。
Although the composition of the present invention may contain a pharmacologically active ingredient, it can be used as a ready-to-use jelly base without containing it. In the case of a composition of the present invention that does not contain a pharmacologically active ingredient, the pharmacologically active ingredient or a drug containing the same and the composition of the present invention (jelly base) may be mixed and packaged and provided, for example, at a dispensing site. I can do it. Patients who receive the sachets can add water to it to form a gel and take it as a jelly. Alternatively, the patient can mix the prescribed pharmacologically active ingredient or drug with the composition of the present invention (jelly base), add water to form a gel, and take the mixture in the form of a jelly.
The composition of the present invention can be used not only for pharmaceuticals as described above, but also as a base for jelly for food.

3 遅延性ゲル化医薬品・ゲル化食品
本発明として、また、本発明組成物と薬理活性成分とを含む遅延性ゲル化医薬品や、本発明組成物と食品素材とを含む遅延性ゲル化食品を挙げることができる。本発明組成物と当該薬理活性成分ないし当該食品素材とは、例えば分離して存在していてもよく、これらを含む単純混合物や造粒物、打錠成形物であってもよい。分離して存在する場合、当該薬理活性成分ないし当該食品素材は、粉末等の固形状態であっても、水に溶解ないし懸濁した状態であってもよい。
3. Delayed Gelling Drugs/Gel Foods The present invention also provides delayed gelling drugs containing the composition of the present invention and pharmacologically active ingredients, and delayed gelling foods containing the composition of the present invention and food materials. can be mentioned. The composition of the present invention and the pharmacologically active ingredient or the food material may exist separately, for example, or may be a simple mixture, granulated product, or tablet molded product containing them. When present separately, the pharmacologically active ingredient or the food material may be in a solid state such as a powder, or may be dissolved or suspended in water.

本発明に係る遅延性ゲル化医薬品ないし遅延性ゲル化食品中における本発明組成物と当該薬理活性成分ないし当該食品素材との含有比率は、目的などに応じて所望により適宜選択される。
本発明に係る遅延性ゲル化医薬品ないし遅延性ゲル化食品は、水を加え加温冷却操作を行うことなく常温でゾル状態からゲル状態に転移させて用いられる。これら医薬品ないし食品に水を加えたものはゾル状態から徐々にゲル状態となり、一定時間経過後にゲル化医薬品ないしゲル化食品となる。
The content ratio of the composition of the present invention and the pharmacologically active ingredient or food material in the delayed gelling pharmaceutical or delayed gelling food according to the present invention is appropriately selected depending on the purpose and the like.
The delayed gelling drug or delayed gelling food according to the present invention is used by being transformed from a sol state to a gel state at room temperature without adding water and performing a heating and cooling operation. When water is added to these medicines or foods, the sol state gradually changes to a gel state, and after a certain period of time, it becomes a gelled medicine or gelled food.

本発明に係る遅延性ゲル化医薬品ないし遅延性ゲル化食品に加えることができる水は、特に制限されないが、例えば、精製水、蒸留水、水道水などを挙げることができる。また、本発明組成物と当該薬理活性成分ないし当該食品素材とが分離した状態であれば、上記の通り、当該薬理活性成分ないし当該食品素材は溶解または懸濁した状態であってもよいが、この場合、当該溶液等を水として本発明に係る遅延性ゲル化医薬品ないし遅延性ゲル化食品に加え、ゲル状態を形成することもできる。
The water that can be added to the delayed gelling pharmaceutical or delayed gelling food according to the present invention is not particularly limited, and examples thereof include purified water, distilled water, tap water, and the like. Furthermore, as long as the composition of the present invention and the pharmacologically active ingredient or the food material are separated, the pharmacologically active ingredient or the food material may be in a dissolved or suspended state, as described above. In this case, the solution or the like can be added to the delayed gelling pharmaceutical or delayed gelling food according to the present invention in the form of water to form a gel state.

4 ゼリー状医薬品・食品
本発明として、また、薬理活性成分を含むゼリー状医薬品の製造方法であって、本発明組成物と水溶液状または水懸濁液状の経口医薬品とを混合し、加温冷却操作を行うことなくゲル化させる工程を含むことを特徴とするゼリー状医薬品の製造方法や、食品素材を含むゼリー状食品の製造方法であって、本発明組成物と水溶液状または水懸濁液状の食品とを混合し、加温冷却操作を行うことなくゲル化させる工程を含むことを特徴とするゼリー状食品の製造方法を挙げることができる。
4 Jelly-form pharmaceuticals/foods The present invention also provides a method for producing jelly-form pharmaceuticals containing pharmacologically active ingredients, in which the composition of the present invention and an oral pharmaceutical in the form of an aqueous solution or suspension are mixed, heated and cooled. A method for producing a jelly-like pharmaceutical product characterized by including a step of gelling without performing any manipulation, and a method for producing a jelly-like food product containing a food material, the method comprising: the composition of the present invention and an aqueous solution or aqueous suspension; A method for producing a jelly-like food product is characterized in that it includes a step of mixing a jelly-like food product with a food product and gelling it without performing a heating and cooling operation.

本発明組成物と液状の経口医薬品ないし液状の食品との混合は、常法により行うことができる。本発明組成物と液状の経口医薬品ないし液状の食品とを混合することにより、加温冷却操作を行うことなく常温でゾル状態から徐々にゲル状態に転移し、ゼリー状医薬品ないしゼリー状食品を製造することができる。 The composition of the present invention and a liquid oral drug or a liquid food can be mixed by a conventional method. By mixing the composition of the present invention with a liquid oral drug or liquid food, the sol state gradually changes to a gel state at room temperature without heating and cooling operations, producing a jelly-like drug or jelly-like food. can do.

上記液状の経口医薬品としては、例えば、シロップ剤、シロップ用剤、エリキシル剤、懸濁剤、乳剤、リモナーデ剤、エキス剤、龍エキス剤、浸剤、煎剤などの液状の製剤を挙げることができる。当該経口医薬品に前記金属イオンないし前記金属塩が含まれている場合であって、所望のゼリー状医薬品を製造できるのであれば、本発明組成物には必ずしも前記金属イオンないし前記金属塩が含まれていなくてもよい。
Examples of the above-mentioned liquid oral pharmaceuticals include liquid preparations such as syrups, syrup preparations, elixirs, suspensions, emulsions, limonades, extracts, dragon extracts, infusions, and decoctions. If the oral drug contains the metal ion or the metal salt, and the desired jelly-like drug can be produced, the composition of the present invention does not necessarily contain the metal ion or the metal salt. It doesn't have to be.

以下、実施例を掲げて本発明を更に詳しく説明するが、本発明はそれら実施例等に限定されるものではない。 EXAMPLES Hereinafter, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited to these Examples.

<粘度測定方法>
各溶液の粘度は、粘度測定装置RE80U E型(東機産業株式会社製)を用いて、室温にて行った。測定時間は30秒間、回転数は各溶液に応じて適宜調整した。
<Viscosity measurement method>
The viscosity of each solution was measured at room temperature using a viscosity measuring device RE80U E type (manufactured by Toki Sangyo Co., Ltd.). The measurement time was 30 seconds, and the rotation speed was adjusted as appropriate depending on each solution.

[実施例1]
ペクチン1.2g、第二リン酸カルシウム1.6g、および粉末還元麦芽糖水あめ17.2gを秤取し250mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を90g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表1に示す通りである。
[Example 1]
1.2 g of pectin, 1.6 g of dibasic calcium phosphate, and 17.2 g of powdered reduced maltose starch syrup were weighed out, placed in a 250 mL container, and mixed for 1 minute to prepare a composition of the present invention. To this solution, 90 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in approximately 15 g portions to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 1.

Figure 0007418679000001
Figure 0007418679000001

表1から明らかな通り、加水後5分で加水後1分の粘度の1.2倍に達し、加水後30分以内には加水後1分の粘度の1.5倍に達した。 As is clear from Table 1, the viscosity reached 1.2 times the viscosity 1 minute after adding water within 5 minutes after adding water, and reached 1.5 times the viscosity 1 minute after adding water within 30 minutes after adding water.

[実施例2]
ペクチン0.781g、第二リン酸カルシウム0.103g、および粉末還元麦芽糖水あめ22.224gを秤取し250mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を120.005g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表2に示す通りである。
[Example 2]
0.781 g of pectin, 0.103 g of dibasic calcium phosphate, and 22.224 g of powdered reduced maltose starch syrup were weighed out, placed in a 250 mL container, and shaken for 1 minute to prepare a composition of the present invention. To this solution, 120.005 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in an amount of about 15 g to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 2.

Figure 0007418679000002
Figure 0007418679000002

表2から明らかな通り、加水後30分以内には加水後1分の粘度の1.2倍に達し、加水後1時間以内には加水後1分の粘度の1.5倍に達した。 As is clear from Table 2, the viscosity reached 1.2 times the viscosity 1 minute after adding water within 30 minutes after adding water, and reached 1.5 times the viscosity 1 minute after adding water within 1 hour after adding water.

[実施例3]
ペクチン2.4g、クエン酸カルシウム水和物1.761g、および粉末還元麦芽糖水あめ35.864gを秤取し500mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を180g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表3に示す通りである。
[Example 3]
2.4 g of pectin, 1.761 g of calcium citrate hydrate, and 35.864 g of powdered reduced maltose starch syrup were weighed out, placed in a 500 mL container, and shaken for 1 minute to prepare a composition of the present invention. To this solution, 180 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in an amount of about 15 g to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 3.

Figure 0007418679000003
Figure 0007418679000003

表3から明らかな通り、加水後10分以内には加水後1分の粘度の1.5倍に達した。 As is clear from Table 3, within 10 minutes after adding water, the viscosity reached 1.5 times the viscosity 1 minute after adding water.

[実施例4]
アルギン酸ナトリウム3.125g、乳酸カルシウム0.417g、および精製白糖44.792gを秤取し500mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を160g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表4に示す通りである。
[Example 4]
3.125 g of sodium alginate, 0.417 g of calcium lactate, and 44.792 g of refined white sugar were weighed out, placed in a 500 mL container, and mixed for 1 minute to prepare a composition of the present invention. To this solution, 160 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in approximately 15 g portions to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 4.

Figure 0007418679000004
Figure 0007418679000004

表4から明らかな通り、加水後3時間以内には加水後1分の粘度の1.5倍に達した。 As is clear from Table 4, the viscosity reached 1.5 times the viscosity 1 minute after adding water within 3 hours after adding water.

[実施例5]
ペクチン2.548g、水酸化マグネシウム0.051g、グルコノ-δ-ラクトン12.742g、および粉末還元麦芽糖水あめ39.501gを秤取し500mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を200g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表5に示す通りである。
[Example 5]
Weigh out 2.548 g of pectin, 0.051 g of magnesium hydroxide, 12.742 g of glucono-δ-lactone, and 39.501 g of powdered reduced maltose starch syrup, place them in a 500 mL container, and shake for 1 minute to prepare the composition of the present invention. did. To this solution, 200 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in an amount of about 15 g to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 5.

Figure 0007418679000005
Figure 0007418679000005

表5から明らかな通り、加水後40分以内には加水後1分の粘度の1.5倍に達した。 As is clear from Table 5, within 40 minutes after adding water, the viscosity reached 1.5 times the viscosity 1 minute after adding water.

[実施例6]
ペクチン2.471g、塩化ストロンチウム0.133g、および粉末還元麦芽糖水あめ44.474gを秤取し500mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を200g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表6に示す通りである。
[Example 6]
2.471 g of pectin, 0.133 g of strontium chloride, and 44.474 g of powdered reduced maltose starch syrup were weighed out, placed in a 500 mL container, and mixed for 1 minute to prepare a composition of the present invention. To this solution, 200 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in an amount of about 15 g to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 6.

Figure 0007418679000006
Figure 0007418679000006

表6から明らかな通り、加水後40分以内には加水後1分の粘度の1.2倍に達した。 As is clear from Table 6, within 40 minutes after adding water, the viscosity reached 1.2 times the viscosity 1 minute after adding water.

[実施例7]
ペクチン2.473g、塩化バリウム二水和物0.308g、および粉末還元麦芽糖水あめ44.513gを秤取し500mLの容器に入れ、1分間振り混ぜ、本発明組成物を調製した。これに常温で水を200g加え十分に振り混ぜた溶液を、速やかにプラスチックカップに約15gずつデカンテーションにより充填し、粘度測定用サンプルとした。
加水後の一定時間経過後の各サンプルの粘度等は、表7に示す通りである。
[Example 7]
2.473 g of pectin, 0.308 g of barium chloride dihydrate, and 44.513 g of powdered reduced maltose starch syrup were weighed out, placed in a 500 mL container, and mixed for 1 minute to prepare a composition of the present invention. To this solution, 200 g of water was added at room temperature and thoroughly shaken, and the solution was immediately filled into a plastic cup by decantation in an amount of about 15 g to prepare a sample for viscosity measurement.
The viscosity of each sample after a certain period of time after adding water is as shown in Table 7.

Figure 0007418679000007
Figure 0007418679000007

表7から明らかな通り、加水後15分以内には加水後1分の粘度の1.5倍に達した。
As is clear from Table 7, the viscosity reached 1.5 times the viscosity 1 minute after adding water within 15 minutes after adding water.

本発明組成物は、加水してからゲル状態を呈するまでの時間が比較的長くコントロールされており、医薬品や食品におけるゼリーの素として有用である。 The composition of the present invention has a relatively long controlled time period from when water is added until it exhibits a gel state, and is useful as a base for jelly in pharmaceuticals and foods.

Claims (4)

ゲル化剤としてペクチン;またはアルギン酸、もしくはその塩を含み、水を加え加温冷却操作を行うことなく常温でゾル状態からゲル状態に転移させて使用するゲル化組成物と、薬理活性成分とを含む、加水されていない非ゾル状態かつ非ゲル状態の遅延性ゲル化医薬品(但し、アジピン酸、クエン酸、またはクエン酸ナトリウムを含むものを除く。)であって、
かかるゲル化医薬品に水を加えたゾル溶液は、加水後、当該ゲル化剤1重量部に対して0.1~1.8重量部の範囲内における、カルシウムイオンまたはカルシウム塩;マグネシウムイオンまたはマグネシウム塩;ストロンチウムイオンまたはストロンチウム塩;およびバリウムイオンまたはバリウム塩からなる群から選択される1種以上の金属イオンまたは金属塩の存在下において少なくとも90秒間ゾル状態を持続し、加水後1時間までに加水後1分の粘度に対して1.2~1.5倍の粘度に達し、加水後10分以降かつ加水後6時間までにゲル状態を呈することを特徴とする、遅延性ゲル化医薬品。
A gelling composition that contains pectin or alginic acid or a salt thereof as a gelling agent and is used by being transformed from a sol state to a gel state at room temperature without adding water and performing a heating and cooling operation , and a pharmacologically active ingredient. Non-hydrated, non-sol and non-gel delayed gelling pharmaceuticals containing adipic acid, citric acid, or sodium citrate, including:
A sol solution obtained by adding water to such a gelling drug contains calcium ions or calcium salts; magnesium ions or magnesium in a range of 0.1 to 1.8 parts by weight per 1 part by weight of the gelling agent after adding water. Maintaining a sol state for at least 90 seconds in the presence of one or more metal ions or metal salts selected from the group consisting of salt; strontium ion or strontium salt; and barium ion or barium salt, and adding water within 1 hour after adding water. A delayed gelling drug, which is characterized by reaching a viscosity 1.2 to 1.5 times the viscosity after 1 minute and exhibiting a gel state after 10 minutes and by 6 hours after adding water.
らに甘味剤を含む、請求項1に記載の遅延性ゲル化医薬品。 The delayed gelling pharmaceutical according to claim 1, further comprising a sweetening agent. 記金属イオン前記金属塩も含まない態様であるか、または前記ゲル化剤および前記金属塩の粉末を含む単純混合物の態様、前記ゲル化剤および前記金属塩を含む造粒物の態様、もしくは前記ゲル化剤および前記金属塩を含む打錠成形物の態様である、請求項1または2に記載の遅延性ゲル化医薬品。 An embodiment containing neither the metal ion nor the metal salt, or an embodiment of a simple mixture containing the gelling agent and a powder of the metal salt, an embodiment of a granulated product containing the gelling agent and the metal salt, The delayed gelling pharmaceutical according to claim 1 or 2, which is in the form of a tablet molded product containing the gelling agent and the metal salt. 薬理活性成分を含むゼリー状医薬品(但し、アジピン酸、クエン酸、またはクエン酸ナトリウムを含むものを除く。)の製造方法であって、請求項1に記載のゲル化組成物と水溶液状または水懸濁液状の経口医薬品とを混合して請求項1に記載のゾル溶液とし、加温冷却操作を行うことなく当該ゾル溶液をゲル化させる工程を含むことを特徴とする、ゼリー状医薬品の製造方法。 A method for producing a jelly-like pharmaceutical containing a pharmacologically active ingredient (excluding those containing adipic acid, citric acid, or sodium citrate) , comprising: the gel composition according to claim 1 and an aqueous solution or aqueous solution; Production of a jelly-like pharmaceutical product, which comprises the step of mixing an oral pharmaceutical agent in the form of a suspension to form the sol solution according to claim 1 , and gelling the sol solution without performing a heating and cooling operation. Method.
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