JP2020203841A - Solid formulation gelatinized by adding water immediately before consumption - Google Patents

Abstract

To provide a Chinese medicine formulation that is easy to take and can be taken by people with dysphagia.SOLUTION: Chinese herbal bulk medicines, crude drug extracts, or crude drug powders are added with locust bean gum and xanthan gum to obtain a solid formulation that is gelatinized immediately before intake without heating. A medication supplement is also obtained by blending locust bean gum and xanthan gum without blending active ingredients, the medication supplement being gelatinized by stirring with water added to allow the supplement to be taken after wrapping other solid medicines. In addition, by adding hypromellose to them, the stability of the preparation is increased.SELECTED DRAWING: None

Description

The present invention relates to a solid agent to be gelled by adding water immediately before administration.

From the viewpoint of ingredient stability, pharmaceutical products are often solid preparations such as powders, granules, and tablets. Since the single dose of Chinese herbal medicine is particularly large, there is a problem that the solid preparation is unpleasant to take, such as being stuffy when taking it or getting stuck in the throat. In order to solve such a problem, there is a method of using a jelly agent as in Patent Document 1, but since the jelly agent contains a large amount of water, the stability of the pharmaceutical component is poor and water separation occurs. One of the problems is that it causes the jelly.
As a method for solving such a problem, in Patent Document 2, sodium alginate is blended and water is added immediately before administration to form a jelly. However, since sodium alginate reacts with cations to form a gel, the quality may vary depending on the cations derived from the Kampo drug substance. Another problem is that the sodium alginate remaining in the machine after production gels, making cleaning difficult.
There is Patent Document 3 for a preparation that makes it easy to take by wrapping a solid agent in a gel made by adding water immediately before taking, but there is a problem that it is difficult to take easily because heating and cooling are required. There is.

Patent No. 6339906 Japanese Patent Application Laid-Open No. 11-322624 JP 2001-226293

We provide a formulation that is easy to take and can be taken by people with dysphagia.

It was found that by blending locust bean gum and xanthan gum, water was added to the preparation and the mixture was stirred to form a gel without the need for heating and cooling, and there was no water separation during administration.
Furthermore, by adding hypromellose to this, a more stable quality preparation could be produced.

By adding locust bean gum and xanthan gum to Chinese herbal medicine drug substance, crude drug extract or crude drug powder, gelation was achieved by simply adding water and stirring immediately before administration, resulting in a formulation that is easy to swallow without water separation. ..
In addition, by blending locust bean gum and xanthan gum without blending the active ingredient and formulating, it is possible to gel by simply adding water and stirring immediately before taking, and wrapping other solid medicines and taking. I have a medication supplement that I can do.
In the present invention, when water is added to the preparation and stirred, it can be gelled and taken within 1 to 5 minutes. Further, the water to be added does not have to be hot water, and water at room temperature can be added as it is, so that heating and cooling are not required at the time of preparation.
In the present invention, since the preparation easily absorbs moisture during storage by containing locust bean gum and xanthan gum, moisture absorption can be suppressed by further adding hypromellose.

In the present invention, the blending amount of locust bean gum and xanthan gum is preferably 5% by weight to 30% by weight with respect to 100% by weight of the amount of water added. If the amount is less than this, it will not gel, and if it is more than this, the thickener will not dissolve. The ratio of locust bean gum to xanthan gum is preferably 9: 1 to 2: 8, and more preferably 7: 3 to 5: 5. If it is out of this mixing ratio, it will not gel when water is added and stirred, resulting in a viscous liquid, or it will be fooled and difficult to prepare.
In addition to locust bean gum and xanthan gum, a thickener may be added. Specific examples of the thickener include carrageenan, guar gum, gum arabic, and cellulose derivatives.

In the present invention, hypromellose may be further added. The blending amount of hypromellose to be added is preferably 0.05% to 5% with respect to 100% by weight of the solid preparation.

In the present invention, the temperature of the water to be added is preferably 15 to 30 ° C. without any problem as long as it is between 1 and 40 ° C. The amount of water added in one dose is preferably 10 to 50 mL, more preferably 10 mL to 30 mL.

In the present invention, it is preferable that the properties when gelled by adding water satisfy the permission standard 3 of "Permission Criteria for Labeling Foods for Persons with Stomach Difficulty" of Food Safety No. 022001.

In the present invention, the shape of the preparation may be any form as long as it is a solid preparation, and specific examples thereof include powders, fine granules, granules and tablets.
In the present invention, additives necessary for formulation can be added. Specific examples of excipients include corn starch, dextrin, mannitol, lactose, crystalline cellulose, light anhydrous silicic acid, hydrous silicon dioxide, magnesium aluminometasilicate, magnesium stearate, and sucrose fatty acid ester. At least one selected is used.
In the present invention, sweeteners and flavoring agents can be added to improve the feeling of ingestion. Specific examples of sweeteners and flavoring agents include sucrose, fructose, sclarose, acesulfam potassium, reduced maltose water candy, mannitol, xylitol, sorbitol, erythritol, trehalose, citrate hydrate, and sodium citrate hydrate. , At least one selected from these groups is used.
In the present invention, further fragrances, coloring agents and the like can be added.
In the present invention, the preparation is preferably packaged for each dose, but it may be provided in a large container, and a spoon indicating the dose for each dose may be attached thereto.

Specific examples of Chinese herbal medicines that can be contained in the present invention include Anchu powder, Makyokansekito, Shimbuto, Onsei-drink, Kakkonto, Kakkonto, and Huangren. Detoxification hot water, Otsuji hot water, ▲ Kasho-saiko-san, Kaiho-to, Kakkon-to, Kakkon-to Kagawa ▲ Kyu ▼ ▲ Kyu ▼ Kakkonto, ▲ Kyu ▼ Kakkonto, Kakkonto, Kakkonto, Kakkonto, Kakkonto, Kakkonto, Kakkonto, Kakkonto, Ginju detox, Ginbo detox, Kakkonto, Keishito Kakkonto, Keishikaryukotsuboi-to, Keishi-to, Keishi-ginseng-to, Keishi-Koryo-maru, Keishi-Koryo-maru, ▲ Well ▼ Kakkonto, Genbu-to, Koso-san, Gorei-san, Go Sekisan-to, Goho-san-to, Kure-maki-to, Beef-wheel kidney-kimaru-to, Gomono-detoxifying-to, Shimbuto-to, Saiko-ka-ryuko-to-to, Saiko-keishi-to, Saiko-keishi-to, Saiko-sei-koku-to, San-ho Shimbuto, Shimbuto, Shimbuto, Shosaikoto, Shosaikoto, Shimbuto, Tomi Detoxic Bath, Kakkonto, Makyokansekito, Sanrei Hakuhosan, Juzendaihoto , Akikanso-to, Namakyo-to, Shichimono-dori-to, Sanso-drink, Shimbuto-to, Negotiation-drink, Kiyokami-fufu-to, Zokumei-to, Sho-saiko-to, Daio-botan-kin-to, Inoryo-to, Tsurito-san, Chogokujokito, Tokisekiyaku powder, Tokidoko, Tokakujokito, Tokishikaryukotaku keishito ginger hot water, Ginseng hot water, Hannatsu Koboku hot water, Drainage sanction hot water, Hannatsu Ryoshinto , Mugimon Fuyuyu, Hannatsu Hakusekitenmayu, Shirotora Kajinjinto, Kakkonto, Kakkonto, Hochuekkito, Makyokansekito, Makyokansekito, Makyokansekito , Makyokansekito, ▲ Well ▼ Sho-saiko-to, Kakkonto, Sho-saiko-to, Shimbuto, Ryokanseki-to, Ryokei-sokanto, Rokukimiko-to, Ryuji-ko-to, Rokumi-maru, Takeboiled Examples include shimbuto. One or more kinds of Kampo drug substances can be selected and used from these.

Specific examples of crude drugs that can be contained in the present invention include Asenyaku (Asenyaku), Coptis chinensis (Chengthread), Alpinia officina (Apricot kernel), Uwaurushi, Engosaku (Clove), Clove (Clove), Coptis chinensis (Huang). Hmm ▼), Oubaku (Yellow Kashiwa), Coptis chinensis (Cherry bark), Coptis chinensis (Huangren), Onji (Clove), Gajutsu, Kagosou (Natsubakusa), Kankyo (Dry ginger), Kakkon (Kuzune), Clove, Karonin, Kanokosou , Kanzo (licorice), Coptis chinensis, Kyoko (Kikyou), Kikuka (Kikuhana), Kisage, Kijitsu (Apricot kernel), Kyonin (Apricot kernel), Kyokatsu, Kujin (Bitter), Keigai (Chenpi), Keihi (Chenpi), Gentiana Gennoshoko, Kemponashi (Genpashi), Kouka (Red Flower), Kojin, Kobushi (Kabushi), Koubei, Koboku (Kouboku), Goou, Gositsu (Beef Knee), Goshuyu (Wu 茱萸), Goboushi (Beef Clove), Gomishi (Gomiko), Psycho (Shibahu), Saishin (Spicy), Saffron, Sankirai, Sanshishi (Sanjoko), Sanshuyu (Sanshuyu), Sansho (Sansho), Sanzashi (Yamasuko), Sandscon (Yamatone), Sansounin (Apricot kernel), Sanyaku (Yamayaku), Sanna (Yamana), Jio (Jihuang), Zion, Shakuyaku, Jakou, Shazensou, Juyaku, Shouma (Masuma), Shitsurishi, Shazenshi, Shazensou, Shajin (Sasan), Shuksha (Cross sand), Clove (including Coptis chinensis), Alpinia (Ginger), Jiryu (Giryu), Shini (Spicy), Jikoppi (Chenpi), Shikon, Sexan (Chenpi), Sekko (Gypsum) Senega, Senkotsu (river bone), Zenko (maehu), Senkyu, Senburi, Soujutsu (Aoi), Souhakuhi (Chenpi), Soyo (Suha), Coptis chinensis (Daio), Taisou, Chikujo, Chikusetsu carrot (Takebushi) Ginseng), Chimo (Chomo), Clove (Clove), Chorei (Coptis chinensis), Chinpi (Chenpi), Tennansho (Tennansei), Tougashi (Winter Gourd), Touki (Toki), Tounin (Apricot Kernel), Tokon , Tochu, Nantenjitsu, Carrot (Ginseng), Nindou (Coptis chinensis), Baimo, Bakumondou, Hakka (Light load), Hange (Half-summer), Byakushi, Byakushaku, Byakujutsu (White Clove), Biwayou (Coptis leaf), Binrouji (Chenpi) , Bukuryo (Coptis chinensis), Veradonna, Bowie, Buttonpi (peony skin), Maou (mao), mashinin (apricot kernel), mokutsu, mokko (wooden incense), yutan, yokuinin, ryugannik (dragon eye meat), alpinia (good ginger) ), Examples include Ryukotsu (keel), Ryutan (keel), Rennik (lotus meat), and Forsythia (gentian). One or more kinds of crude drugs can be selected and used from these. As these crude drugs, powdered ones may be used as they are, or extracts extracted with a solvent may be used.

Next, a test example of the present invention will be described, but the present invention is not limited thereto. The physical properties of the gel were measured at a temperature of 20 ± 2 ° C. according to the test method for foods for people with swallowing difficulties described in Food Safety No. 022001.

With the formulations shown in Table 1, granulation was carried out using water as a binder by a fluidized bed granulation method to prepare Examples 1 to 3 and Comparative Examples 1 and 2. 2 g of each of these was taken, 15 mL of water was added, the mixture was stirred for 20 seconds, and then the physical properties were compared when left for 5 minutes.
Examples 1 to 3 were dissolved in water with stirring for 20 seconds and gelled after 1 minute. Comparative Example 1 remained liquid. In Comparative Example 2, lumps remained even after vigorous stirring.
Take 2 g of Example 2, add Kakkonto extract [fine granules] 7 (Matsuura Yakuhin), add 15 mL of water, stir for 20 seconds, and leave for 5 minutes. As a result, a gel that is easy to take in a cohesive manner. Became. Further, when 2 g of Example 2 was taken, 15 mL of water was added, the mixture was stirred for 20 seconds, left for 5 minutes, and then mixed with Kakkonto extract [fine granules] 7 (Matsuura Pharmaceutical Co., Ltd.), this also became a cohesive gel that was easy to take. It was.

Examples 4 to 8 and Comparative Examples 3 to 4 were prepared by granulating with water as a binder by the fluidized bed granulation method with the formulations shown in Table 2. 2 g of each of these was taken, 15 mL of water was added, the mixture was stirred for 20 seconds, and then the physical properties were compared when left for 5 minutes.
Examples 2, 4 to 6 were dissolved in water with stirring for 20 seconds and gelled after 1 minute. Examples 7 to 8 need to be stirred more strongly than Examples 2 and 4 to 6 at the time of dissolution, but like Examples 2 and 4 to 6, they became a gel without lumps. Comparative Example 3 was a viscous liquid, and the hardness was outside the permission standard range of the "permission standard for labeling food for people with swallowing difficulty". In Comparative Example 4, lumps remained even after vigorous stirring. In Examples 2, 4 to 8, no water separation was observed after 1 hour and 2 hours of gelation.

In the formulation shown in Table 3, hypromellose was coated after granulating with water as a binder by a fluidized bed granulation method to obtain Examples 9, 10 and 13. Example 11 was obtained by granulating with water as a binder by a fluidized bed granulation method. Example 12 was obtained by granulating using a cornstarch solution as a binder by a fluidized bed granulation method. Take 2.5 g each of Examples 9 to 11, 1.5 g of Example 12, and 2 g of Example 13, add 15 mL of water to each, stir for 20 seconds, and then leave for 5 minutes to form a gel. The properties were cohesive and easy to take. In Examples 9 to 13, no water separation was observed 1 hour and 2 hours after gelation.

When Example 10 and Example 11 were packaged in 2.5 g each with a multilayer film combining polyethylene, aluminum, and cellophane, and the package was opened after leaving at 60 ° C. for 2 weeks, the appearance of Example 10 changed. Although it was not seen, Example 11 was partially solidified.

According to the present invention, it is possible to provide a Chinese herbal medicine that can be easily taken even by a person who has difficulty swallowing.

Claims (4)

It contains locust bean gum and xanthan gum, and when taken, it becomes a gel when water is added and stirred, and it can be easily taken by mixing with pharmaceuticals. The dosage form is powder, fine granules, granules, tablets. A solid agent that is either. Contains locust bean gum and xanthan gum, and also contains Chinese herbal medicine or crude drug extract, gels when added with water and stirred at the time of administration, and the dosage form is either powder, fine granules, granules, or tablets. Is a solid drug. A solid drug containing locust bean gum and xanthan gum, and further containing crude drug powder, which turns into a gel when added with water and stirred when taken, and whose dosage form is powder, fine granules, granules, or tablets. .. The solid preparation of claims 1 to 3 further containing hypromellose.