TW202207912A - Effervescent oral tablet packed in sealed container containing carbonate, organic acid or its salt, and cellulose - Google Patents
Effervescent oral tablet packed in sealed container containing carbonate, organic acid or its salt, and cellulose Download PDFInfo
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- TW202207912A TW202207912A TW110117097A TW110117097A TW202207912A TW 202207912 A TW202207912 A TW 202207912A TW 110117097 A TW110117097 A TW 110117097A TW 110117097 A TW110117097 A TW 110117097A TW 202207912 A TW202207912 A TW 202207912A
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- 239000001913 cellulose Substances 0.000 title claims abstract description 66
- 229920002678 cellulose Polymers 0.000 title claims abstract description 51
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 title claims abstract description 21
- 150000007524 organic acids Chemical class 0.000 title claims abstract description 15
- 150000003839 salts Chemical class 0.000 title claims abstract description 15
- 229940051312 effervescent oral tablet Drugs 0.000 title abstract 3
- 239000002245 particle Substances 0.000 claims abstract description 34
- 239000002253 acid Substances 0.000 claims abstract description 33
- 229940096978 oral tablet Drugs 0.000 claims description 52
- 239000007935 oral tablet Substances 0.000 claims description 52
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 25
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- 150000005846 sugar alcohols Chemical class 0.000 claims description 8
- 239000007937 lozenge Substances 0.000 claims description 7
- 229920001542 oligosaccharide Polymers 0.000 claims description 7
- 150000002482 oligosaccharides Chemical class 0.000 claims description 7
- 229940100629 oral lozenge Drugs 0.000 claims description 7
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims description 6
- 239000003826 tablet Substances 0.000 abstract description 20
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- 235000019658 bitter taste Nutrition 0.000 description 21
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- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 239000004088 foaming agent Substances 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- 239000001307 helium Substances 0.000 description 1
- 229910052734 helium Inorganic materials 0.000 description 1
- SWQJXJOGLNCZEY-UHFFFAOYSA-N helium atom Chemical compound [He] SWQJXJOGLNCZEY-UHFFFAOYSA-N 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 229940026239 isoascorbic acid Drugs 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000010299 mechanically pulverizing process Methods 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 230000003472 neutralizing effect Effects 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- OQUKIQWCVTZJAF-UHFFFAOYSA-N phenol;sulfuric acid Chemical compound OS(O)(=O)=O.OC1=CC=CC=C1 OQUKIQWCVTZJAF-UHFFFAOYSA-N 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 description 1
- 239000011736 potassium bicarbonate Substances 0.000 description 1
- 235000015497 potassium bicarbonate Nutrition 0.000 description 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 description 1
- 229940086066 potassium hydrogencarbonate Drugs 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- 238000007670 refining Methods 0.000 description 1
- 238000001448 refractive index detection Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000018341 sodium sesquicarbonate Nutrition 0.000 description 1
- 229910000031 sodium sesquicarbonate Inorganic materials 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 235000019411 steviol glycoside Nutrition 0.000 description 1
- 229930182488 steviol glycoside Natural products 0.000 description 1
- 150000008144 steviol glycosides Chemical class 0.000 description 1
- 235000019202 steviosides Nutrition 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000009475 tablet pressing Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- ODBLHEXUDAPZAU-UHFFFAOYSA-N threo-D-isocitric acid Natural products OC(=O)C(O)C(C(O)=O)CC(O)=O ODBLHEXUDAPZAU-UHFFFAOYSA-N 0.000 description 1
- WCTAGTRAWPDFQO-UHFFFAOYSA-K trisodium;hydrogen carbonate;carbonate Chemical compound [Na+].[Na+].[Na+].OC([O-])=O.[O-]C([O-])=O WCTAGTRAWPDFQO-UHFFFAOYSA-K 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
- A23G3/362—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds containing inorganic compounds
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/36—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds
- A23G3/42—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof characterised by the composition containing organic or inorganic compounds characterised by the carbohydrates used, e.g. polysaccharides
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Landscapes
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Inorganic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- General Preparation And Processing Of Foods (AREA)
Abstract
Description
本發明係關於一種密封容器裝之發泡性經口錠劑。The present invention relates to a foamable oral tablet in a sealed container.
已知藉由二氧化碳之發泡，能夠得到唾液分泌促進效果、作用於喉部之成分之增強效果、服用時在口中發泡所帶來的良好使用感。It is known that by foaming with carbon dioxide, it is possible to obtain the effect of promoting saliva secretion, the effect of enhancing the components acting on the throat, and the good feeling of use brought about by foaming in the mouth when taking it.
例如，在專利文獻1中揭示一種糖果，其含有糖類及作為發泡成分之有機酸與碳酸鹽或碳酸氫鹽之組合，使糖類中之麥芽糖類之含有率為25重量%以下，生產率及保存性良好。此外，在專利文獻2中揭示含有寡糖、發泡劑成分及中和劑成分之口感、穩定性良好之發泡性咀嚼錠形態之寡糖補給製劑。For example, Patent Document 1 discloses a candy containing a combination of saccharides and an organic acid as a foaming component, and carbonate or bicarbonate such that the content rate of maltose in the saccharide is 25% by weight or less, and the productivity and preservation are improved. Sex is good. In addition, Patent Document 2 discloses an oligosaccharide supplement in the form of a foamable chewable tablet containing an oligosaccharide, a foaming agent component, and a neutralizing agent component, which has good texture and stability.
另一方面，結晶纖維素等粒徑大之粉末狀纖維素無味，化學惰性，壓縮成形性及壓錠性優異，因此，適合用作錠劑之賦形劑、黏合劑、崩解劑。On the other hand, powdered cellulose with large particle size, such as crystalline cellulose, is odorless, chemically inert, and has excellent compression moldability and tableting properties. Therefore, it is suitable for use as excipients, binders, and disintegrating agents for tablets.
現有技術文獻： 專利文獻1：日本特開2004-16073號公報 專利文獻2：日本特開2001-8666號公報Prior art literature: Patent Document 1: Japanese Patent Laid-Open No. 2004-16073 Patent Document 2: Japanese Patent Laid-Open No. 2001-8666
本發明提供一種密封容器裝之發泡性經口錠劑，其含有以下之成分(A)、(B)及(C)： (A)碳酸鹽14～30質量%； (B)有機酸或其鹽； (C)平均粒徑30～70 μm之纖維素0.5～50質量%， 成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]為0.25以上且3.0以下，並且成分(A)相對於成分(C)之含量質量比[(A)/(C)]為0.5以上。The present invention provides a foamable oral tablet in a sealed container, which contains the following components (A), (B) and (C): (A) 14-30 mass % of carbonate; (B) an organic acid or its salt; (C) 0.5 to 50 mass % of cellulose with an average particle diameter of 30 to 70 μm, The ratio of the moles (mol) of component (A) to the moles of acid groups (mol) of component (B) [(A) moles (mol)/(B) acid groups moles (mol)] is 0.25 or more and 3.0 or less, and the content mass ratio [(A)/(C)] of the component (A) with respect to the component (C) is 0.5 or more.
然而，在發泡性經口製劑中，在為了提高發泡性而大量含有作為發泡成分之碳酸鹽、有機酸之情況下，會感覺到碳酸鹽之苦味，此外，由於在保存中會發生碳酸鹽與酸之反應，由此，在將發泡性經口製劑封裝至密封容器中之情況下，存在諸如容器發生膨脹之保存穩定性上之問題。然而，至今為止，所涉及之此等問題尚未得到關注。However, when a foamable oral preparation contains a large amount of carbonate or an organic acid as a foaming component in order to improve foamability, a bitter taste of carbonate is felt, and furthermore, it occurs during storage. The reaction of carbonate and acid, and thus, in the case where the foamable oral preparation is packaged in a sealed container, has a problem in preservation stability such as expansion of the container. However, so far, these issues involved have not received attention.
因此，本發明係關於一種在高發泡下服用時具有感覺舒適之發泡感，同時具有良好之風味且在容器封裝時不存在膨脹，亦具有高保存穩定性之密封容器裝之發泡性經口錠劑。Therefore, the present invention relates to a foaming experience in a hermetically sealed container that has a pleasant foaming feeling when taken under high foaming, has a good flavor and does not expand when the container is packaged, and also has high storage stability. Lozenges.
本發明人進行了深入研究，結果發現：即使在使用規定之纖維素、為了提高發泡性而大量含有碳酸鹽之情況下，藉由將纖維素以與碳酸鹽之比率成為一定範圍之方式進行組合，並且製劑中之碳酸鹽之莫耳數與有機酸之酸基之莫耳數設為一定範圍進行製劑，能夠得到在口中具有感覺舒適的高發泡感，並且口感良好、碳酸鹽之苦味少、且亦具有容器不存在膨脹之高保存穩定性之密封容器裝之發泡性經口錠劑。As a result of intensive research, the present inventors found that even when a predetermined amount of cellulose is used and carbonate is contained in a large amount in order to improve foamability, it is found that the ratio of cellulose to carbonate is within a certain range. Combination, and the molar number of carbonate in the formulation and the molar number of the acid group of the organic acid are set to a certain range to prepare the formulation, which can obtain a comfortable high foaming feeling in the mouth, good mouthfeel and less bitterness of carbonate. , and also has a foamable oral lozenge in a sealed container with high storage stability without expansion of the container.
本發明之密封容器裝之發泡性經口錠劑具有在口中感覺舒適之高發泡感及口感之良好、良好之風味，且不存在容器封裝時之膨脹，保存穩定性亦為優異的。The foamable oral lozenge in a hermetically sealed container of the present invention has a high foaming feeling comfortable in the mouth and a good mouthfeel and a good flavor, and has no swelling when the container is packaged, and is also excellent in storage stability.
本發明之密封容器裝之發泡性經口錠劑含有碳酸鹽作為成分(A)。作為碳酸鹽，例如可列舉碳酸鈉、碳酸氫鈉、碳酸鉀、碳酸氫鉀、碳酸銨、倍半碳酸鈉等。其可使用1種或組合使用2種以上。其中，自實現在高發泡下服用時感覺舒適之發泡感之觀點出發，成分(A)較佳為選自碳酸鈉、碳酸氫鈉及碳酸鉀中之1種或2種以上，更佳為碳酸氫鈉。The foamable oral tablet in the airtight container of the present invention contains carbonate as the component (A). As carbonate, sodium carbonate, sodium hydrogencarbonate, potassium carbonate, potassium hydrogencarbonate, ammonium carbonate, sodium sesquicarbonate, etc. are mentioned, for example. These can be used alone or in combination of two or more. Among them, from the viewpoint of realizing a comfortable foaming feeling when taken under high foaming, the component (A) is preferably one or more selected from sodium carbonate, sodium bicarbonate and potassium carbonate, more preferably Sodium bicarbonate.
本發明之發泡性經口錠劑中之成分(A)之含量為14～30質量%。藉由以此類特定量含有成分(A)，能夠實現在高發泡下服用時感覺舒適之發泡感，且亦具有不存在容器膨脹之高保存穩定性。 自實現口中感覺舒適之發泡感之觀點出發，本發明之發泡性經口錠劑中之成分(A)之含量為14質量%以上，較佳為15質量%以上，更佳為18質量%以上，此外，自抑制容器之膨脹之觀點出發，為30質量%以下，較佳為26質量%以下，更佳為22質量%以下。而且，本發明之發泡性經口錠劑中之成分(A)之含量為14～30質量%，較佳為15～26質量%，更佳為18～26質量%，進一步較佳為18～22質量%。在本說明書中，成分(A)之含量為碳酸換算值。Content of the component (A) in the foamable oral tablet of this invention is 14-30 mass %. By containing the component (A) in such a specific amount, it is possible to achieve a comfortable foaming feeling when taken with high foaming, and also to have high storage stability without container swelling. From the viewpoint of realizing a comfortable foaming feeling in the mouth, the content of the component (A) in the foamable oral tablet of the present invention is 14 mass % or more, preferably 15 mass % or more, more preferably 18 mass % % or more, and from the viewpoint of suppressing the expansion of the container, it is 30 mass % or less, preferably 26 mass % or less, and more preferably 22 mass % or less. Furthermore, the content of the component (A) in the foamable oral tablet of the present invention is 14 to 30 mass %, preferably 15 to 26 mass %, more preferably 18 to 26 mass %, and further preferably 18 mass % ~22% by mass. In this specification, content of a component (A) is a carbonic acid conversion value.
本發明之發泡性經口錠劑中之成分(A)之莫耳數(mmol/100 g)係指換算為成分(A)中之碳酸根離子或碳酸氫根離子時之莫耳數。 本發明之發泡性經口錠劑中之成分(A)之莫耳數(mmol/100 g)，自在高發泡下服用時實現感覺舒適之發泡感之觀點出發，較佳為160 mmol/100 g以上，更佳為175mmol/100 g以上，進一步較佳為210 mmol/100 g以上，此外，自抑制容器之膨脹之觀點出發，較佳為360 mmol/100 g以下，更佳為300 mmol/100 g以下，進一步較佳為265 mmol/100 g以下。而且，本發明之發泡性經口錠劑中之成分(A)之莫耳數(mmol/100 g)較佳為160～360 mmol/100 g、更佳為175～300 mmol/100 g、進一步較佳為210～300 mmol/100 g、更進一步較佳為210～265 mmol/100 g。The molar number (mmol/100 g) of the component (A) in the foamable oral tablet of the present invention refers to the molar number when converted into carbonate ions or bicarbonate ions in the component (A). The molar number (mmol/100 g) of the component (A) in the foamable oral tablet of the present invention is preferably 160 mmol/ 100 g or more, more preferably 175 mmol/100 g or more, still more preferably 210 mmol/100 g or more, in addition, from the viewpoint of suppressing the expansion of the container, preferably 360 mmol/100 g or less, more preferably 300 mmol /100 g or less, more preferably 265 mmol/100 g or less. Furthermore, the molar number (mmol/100 g) of the component (A) in the foamable oral tablet of the present invention is preferably 160-360 mmol/100 g, more preferably 175-300 mmol/100 g, More preferably, it is 210-300 mmol/100 g, More preferably, it is 210-265 mmol/100 g.
本發明之密封容器裝之發泡性經口錠劑含有有機酸或其鹽作為成分(B)。有機酸或其鹽不存在特定限制，較佳為選自羥基羧酸、二羧酸、抗壞血酸及其等之鹽中之1種或2種以上。 作為羥基羧酸，例如可列舉乳酸、檸檬酸、異檸檬酸、蘋果酸、酒石酸、葡糖酸、奎尼酸等。 作為二羧酸，例如可列舉草酸、丙二酸、琥珀酸、戊二酸、己二酸、富馬酸、馬來酸等。 抗壞血酸中含有作為立體異構體之L-抗壞血酸及異抗壞血酸。 作為鹽，較佳為鹼金屬鹽，進一步較佳選自鈉鹽及鉀鹽中之1種，進一步較佳為鈉鹽。 其中，自在高發泡下服用時實現感覺舒適之發泡感之觀點出發，較佳為選自羥基羧酸、抗壞血酸及其等之鹽中之1種或2種以上，更佳為選自檸檬酸、蘋果酸、酒石酸、抗壞血酸及其等之鹽中之1種或2種以上，進一步較佳為檸檬酸。The foamable oral tablet in the airtight container of the present invention contains an organic acid or a salt thereof as a component (B). The organic acid or its salt is not particularly limited, but is preferably one or two or more selected from the group consisting of hydroxycarboxylic acid, dicarboxylic acid, ascorbic acid, and salts thereof. As a hydroxycarboxylic acid, lactic acid, citric acid, isocitric acid, malic acid, tartaric acid, gluconic acid, quinic acid, etc. are mentioned, for example. As dicarboxylic acid, oxalic acid, malonic acid, succinic acid, glutaric acid, adipic acid, fumaric acid, maleic acid, etc. are mentioned, for example. Ascorbic acid contains L-ascorbic acid and erythorbic acid as stereoisomers. The salt is preferably an alkali metal salt, more preferably one selected from a sodium salt and a potassium salt, and more preferably a sodium salt. Among them, from the viewpoint of realizing a comfortable foaming feeling when taken under high foaming conditions, one or more kinds selected from hydroxycarboxylic acid, ascorbic acid and salts thereof are preferred, and more preferred are selected from citric acid , one or more of salts of malic acid, tartaric acid, ascorbic acid, and the like, and more preferably citric acid.
本發明之發泡性經口錠劑中之成分(B)之含量，自在高發泡下服用時實現感覺舒適之發泡感之觀點出發，較佳為5質量%以上，更佳為10質量%以上，此外，自降低服用時之黏膜不適感之觀點出發，較佳為45質量%以下，更佳為40質量%以下，進一步較佳為25質量%以下。發泡性經口錠劑中之成分(B)之含量較佳為5～45質量%、更佳為5～40質量%、進一步較佳為10～25質量%。在本說明書中，成分(B)之含量為有機酸換算值。The content of the component (B) in the foamable oral tablet of the present invention is preferably 5% by mass or more, more preferably 10% by mass, from the viewpoint of realizing a comfortable foaming feeling when taken under high foaming conditions In addition, from the viewpoint of reducing mucous membrane discomfort during ingestion, the content is preferably 45% by mass or less, more preferably 40% by mass or less, and still more preferably 25% by mass or less. The content of the component (B) in the foamable oral tablet is preferably 5 to 45 mass %, more preferably 5 to 40 mass %, further preferably 10 to 25 mass %. In this specification, content of a component (B) is an organic-acid conversion value.
本發明之發泡性經口錠劑中，自在高發泡下服用時實現感覺舒適之發泡感之觀點出發，成分(B)之酸基之莫耳數(mmol/100 g)較佳為50 mmol/100 g以上，更佳為150 mmol/100 g以上，此外，自降低服用時之黏膜不適感之觀點出發，較佳為600 mmol/100 g以下，更佳為360 mmol/100 g以下。而且，發泡性經口錠劑中之成分(B)之酸基之莫耳數(mmol/100 g)較佳為50～600 mmol/100 g，更佳為150～360 mmol/100 g。需要說明的是，作為成分(B)，在本發明中使用抗壞血酸之情況下，作為具有1個酸基之有機酸，計算上述酸基之莫耳數。In the foamable oral lozenge of the present invention, the molar number (mmol/100 g) of the acid group of the component (B) is preferably 50 from the viewpoint of realizing a comfortable foaming feeling when taken with high foaming. mmol/100 g or more, more preferably 150 mmol/100 g or more, and from the viewpoint of reducing mucosal discomfort when taking it, preferably 600 mmol/100 g or less, more preferably 360 mmol/100 g or less. Furthermore, the molar number (mmol/100 g) of the acid group of the component (B) in the foamable oral tablet is preferably 50-600 mmol/100 g, more preferably 150-360 mmol/100 g. In addition, when ascorbic acid is used in this invention as a component (B), the molar number of the said acid group is calculated as an organic acid which has one acid group.
本發明之發泡性經口錠劑中，成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]為0.25以上且3.0以下。藉由將碳酸鹽之莫耳數與有機酸或其鹽之酸基之莫耳數設為該特定的比，能夠實現在高發泡下服用時感覺舒適之發泡感，此外，能夠降低黏膜之不適感。 關於成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]，自在高發泡下服用時實現感覺舒適之發泡感之觀點、以及使服用時之口感良好之觀點出發，為0.25以上，較佳為0.5以上，更佳為0.8以上，此外，自抑制容器之膨脹之觀點出發，為3.0以下，較佳為1.5以下，更佳為1.0以下。而且，成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]為0.25～3.0，較佳為0.5～1.5，更佳為0.8～1.0。In the foamable oral tablet of the present invention, the ratio of the molar number (mol) of the component (A) to the molar number (mol) of the acid group of the component (B) [(A) molar number (mol) The molar number (mol) of the acid group of )/(B) is 0.25 or more and 3.0 or less. By setting the molar number of the carbonate to the molar number of the acid group of the organic acid or its salt as the specific ratio, it is possible to achieve a comfortable foaming feeling when taken under high foaming conditions, and in addition, it is possible to reduce the mucous membranes. Discomfort. Regarding the ratio of the moles (mol) of the component (A) to the moles (mol) of the acid groups of the component (B) [(A) moles (mol)/(B) acid groups moles (mol)], from the viewpoint of realizing a comfortable foaming feeling when taken with high foaming, and from the viewpoint of making the mouthfeel good when taking it, it is 0.25 or more, preferably 0.5 or more, more preferably 0.8 or more, and in addition , from the viewpoint of suppressing the expansion of the container, is 3.0 or less, preferably 1.5 or less, and more preferably 1.0 or less. Moreover, the ratio of the mole number (mol) of the component (A) to the mole number (mol) of the acid group of the component (B) [(A) mole number (mol)/(B) acid group mole number Ear number (mol)] is 0.25-3.0, Preferably it is 0.5-1.5, More preferably, it is 0.8-1.0.
關於本發明之發泡性經口錠劑，自使成分(A)相對於成分(B)之含量質量比[(A)/(B)]在高發泡下服用時實現感覺舒適之發泡感之觀點、以及使服用時之口感良好之觀點出發，較佳為0.35以上，更佳為0.70以上，進一步較佳為1.1以上，此外，自抑制容器之膨脹之觀點出發，較佳為4.0以下，更佳為2.0以下，進一步較佳為1.4以下。Regarding the foamable oral tablet of the present invention, a comfortable foaming feeling is achieved when the content-mass ratio [(A)/(B)] of the component (A) to the component (B) is taken under high foaming From the viewpoint of and from the viewpoint of improving the mouthfeel at the time of ingestion, it is preferably 0.35 or more, more preferably 0.70 or more, still more preferably 1.1 or more, and from the viewpoint of suppressing the expansion of the container, preferably 4.0 or less, More preferably, it is 2.0 or less, and still more preferably 1.4 or less.
本發明之密封容器裝之發泡性經口錠劑含有平均粒徑為30～70 μm之纖維素作為成分(C)。 除非特別說明，本發明之「纖維素」之用語係基於熟習此項技術者通常接受之定義之纖維素、即具有D-吡喃葡萄糖以β1→4鍵連接之結構之多糖類之總稱，除此之外，亦可用作指後述之結晶纖維素、微細纖維狀纖維素、以及其等之混合物。作為一般可獲得之纖維素，可列舉作為粉末形態之通常的纖維素(以下，稱為「粉末纖維素」)、例如纖維素絮凝物、作為結晶形態之通常的纖維素(以下，稱為「結晶纖維素」)。The foamable oral tablet in the airtight container of the present invention contains cellulose with an average particle diameter of 30 to 70 μm as the component (C). Unless otherwise specified, the term "cellulose" in the present invention is a general term for cellulose based on the definition generally accepted by those skilled in the art, that is, polysaccharides having a structure in which D-glucopyranose is linked by β1→4 bonds, except In addition, it can also be used to refer to a mixture of crystalline cellulose, fine fibrous cellulose, and the like described later. Examples of generally available cellulose include ordinary cellulose in powder form (hereinafter, referred to as "powdered cellulose"), for example, cellulose floes, and ordinary cellulose in crystalline form (hereinafter referred to as "powdered cellulose"). crystalline cellulose").
粉末纖維素係指對自纖維性植物作為紙漿而得到之α-纖維素進行處理後，進行精製、機械粉碎而成的物質。例如，相當於第十五改正版日本藥局方解說書(廣川書店發行)中記載之粉末纖維素。該粉末纖維素之平均聚合度規定為大於440。該值可根據第十五改正版日本藥局方解說書(廣川書店發行)之確認試驗(3)中記載之基於銅乙二胺溶液之還原比黏度法進行測定。作為該粉末纖維素，例如可列舉日本製紙(股)之KC Flock W-100 g等。Powdered cellulose refers to a substance obtained by treating α-cellulose obtained as pulp from a fibrous plant, and then refining and mechanically pulverizing it. For example, it is equivalent to the powdered cellulose described in the 15th revised edition of the Japanese Pharmacopoeia Explanation Book (published by Hirokawa Shoten). The average degree of polymerization of the powdered cellulose is specified to be greater than 440. This value can be measured according to the reduction specific viscosity method based on copper ethylenediamine solution described in the confirmation test (3) of the 15th revised edition of the Japanese Pharmacopoeia Manual (issued by Hirokawa Shoten). As this powdered cellulose, KC Flock W-100 g of Nippon Paper Co., Ltd., etc. are mentioned, for example.
結晶纖維素係指將作為紙漿自纖維性植物中得到之α-纖維素用酸部分解聚、精製而成之物質。例如，相當於第十五改正版日本藥局方解說書(廣川書店發行)中記載之結晶纖維素。結晶纖維素之平均聚合度較佳為350以下。該值可根據第十五改正版日本藥局方解說書(廣川書店發行)之、結晶纖維素之確認試驗(3)中記載之基於銅乙二胺溶液之還原比黏度法進行測定。作為該結晶纖維素，例如可列舉旭化成(股)之Ceolus ST系列等。 需要說明的是，在本發明中，粉末纖維素及結晶纖維素任意種均可使用，也可將2種混合使用。此外，自國別之藥事性之觀點出發，亦可僅使用任一種。Crystalline cellulose refers to a substance obtained by partially depolymerizing and purifying α-cellulose obtained as pulp from fibrous plants with an acid. For example, it corresponds to the crystalline cellulose described in the 15th revised edition of the Japanese Pharmacopoeia Explanation Book (published by Hirokawa Shoten). The average degree of polymerization of crystalline cellulose is preferably 350 or less. This value can be measured according to the reduction specific viscosity method based on copper ethylenediamine solution described in Confirmation Test (3) of Crystalline Cellulose in the 15th Revised Edition of the Japanese Pharmacopoeia Manual (issued by Hirokawa Shoten). As this crystalline cellulose, Ceolus ST series of Asahi Kasei Co., Ltd., etc. are mentioned, for example. In addition, in this invention, either powdered cellulose and crystalline cellulose may be used, and two types may be mixed and used. In addition, from the viewpoint of medicinal properties by country, only any one of them may be used.
本發明中纖維素之平均粒徑為30～70 μm。若纖維素之平均粒徑小，則成分(A)之苦味降低效果變小，需要用香料等其他成分掩蔽，受到處方之限制，另一方面，若纖維素之平均粒徑為30 μm以上，則處方之自由度提高。 自降低成分(A)之苦味、提高處方之自由度之觀點出發，纖維素之平均粒徑為30 μm以上、較佳為35 μm以上、更佳為40 μm以上，此外，自使服用時之口感良好之觀點、以及在高發泡下服用時實現感覺舒適之發泡感之觀點出發，自降低成分(A)之苦味之觀點出發，纖維素之平均粒徑為70 μm以下、較佳為60 μm以下、更佳為55 μm以下。而且，纖維素之平均粒徑為30～70 μm，較佳為35～60 μm，更佳為40～55 μm。 在此，本發明中之纖維素之平均粒徑係指體積中值粒徑(D50)。本發明中之體積中值粒徑(D50)係指自粒徑小之一方計算以體積分數計算出之累積體積頻率成為50%之粒徑。平均粒徑之測定可使用數字影像分析裝置(MicrotracBEL(股)製CAMSIZER)進行測定。The average particle size of cellulose in the present invention is 30-70 μm. If the average particle size of cellulose is small, the bitterness-reducing effect of the component (A) becomes small, and masking with other ingredients such as fragrance is required, which is restricted by the formulation. On the other hand, if the average particle size of cellulose is 30 μm or more, The degree of freedom of prescription is improved. From the viewpoint of reducing the bitterness of the component (A) and increasing the degree of freedom of formulation, the average particle size of the cellulose is 30 μm or more, preferably 35 μm or more, more preferably 40 μm or more. The average particle size of cellulose is 70 μm or less, preferably 60 μm or less, from the viewpoint of good taste, and from the viewpoint of achieving a comfortable foaming feeling when taken with high foaming, and from the viewpoint of reducing the bitterness of the component (A). μm or less, more preferably 55 μm or less. Moreover, the average particle diameter of cellulose is 30-70 micrometers, Preferably it is 35-60 micrometers, More preferably, it is 40-55 micrometers. Here, the average particle diameter of cellulose in the present invention refers to the volume median diameter (D50). The volume median particle diameter (D50) in the present invention refers to the particle diameter at which the cumulative volume frequency calculated by the volume fraction calculated from the smaller particle diameter becomes 50%. The average particle diameter can be measured using a digital image analyzer (CAMSIZER manufactured by MicrotracBEL Corporation).
在本發明中，自使服用時之口感良好之觀點、在高發泡下服用時實現感覺舒適之發泡感之觀點出發，纖維素之體積密度之值較佳為0.1～0.8 g/cm3 、更佳為0.11～0.3 g/cm3 。作為例子，Ceolus (註冊商標)ST-100 (旭化成(股))之體積密度之值為0.12 g/cm3 。In the present invention, the value of the bulk density of cellulose is preferably 0.1 to 0.8 g/cm 3 , from the viewpoint of improving the mouthfeel when ingested, and from the viewpoint of achieving a comfortable foaming feeling when ingested under high foaming conditions. More preferably, it is 0.11-0.3 g/cm 3 . As an example, the value of the bulk density of Ceolus (registered trademark) ST-100 (Asahi Kasei Co., Ltd.) is 0.12 g/cm 3 .
本發明中之纖維素可為微細之顆粒形狀。纖維素之顆粒形狀可藉由以下記載之L/D來規定。纖維素之L/D係將具有粉末狀、顆粒狀或結晶狀之纖維素之最大直徑設為直徑(L)(長軸之長度)，從而將與直徑(L)垂直之徑中最大徑設為短徑(D)(短軸之長度)時之長徑(L)與短徑(D)之比，藉由使用掃描型電子顯微鏡之顯微鏡觀測，能夠藉由測定長徑(L)及短徑(D)來求出。例如，將作為對象之纖維素以JIS標準篩75 μm進行篩分，對於篩分後之顆粒，使用掃描型電子顯微鏡(日立製作所(股)、FlexSEM)，以加速電壓5KV以放大倍率3000倍進行觀測，根據所得到之影像，測定隨機提取之50個顆粒之長徑(L)及短徑(D)，根據其等之平均值(平均長徑(L)、平均短徑(D))算出L/D。 自降低成分(A)之苦味之觀點出發，纖維素之L/D較佳為2.4以上，更佳為2.7以上，進一步較佳為3.0以上，此外，自使服用時之口感良好之觀點、在高發泡下服用時實現感覺舒適之發泡感之觀點出發，較佳為4.0以下，更佳為3.8以下，進一步較佳為3.6以下。而且，纖維素之L/D較佳為2.4～4.0，更佳為2.7～3.8，進一步較佳為3.0～3.6。The cellulose in the present invention may be in the form of fine particles. The particle shape of cellulose can be specified by L/D described below. The L/D of cellulose is defined as the diameter (L) (the length of the major axis) of the cellulose with the largest diameter in powder, granular or crystalline form, so that the largest diameter among the diameters perpendicular to the diameter (L) is set as the diameter (L). The ratio of the major axis (L) to the minor axis (D) when the minor axis (D) (the length of the minor axis), can be measured by measuring the major axis (L) and the minor axis through microscope observation using a scanning electron microscope. Diameter (D) to find. For example, the target cellulose is sieved with a JIS standard sieve of 75 μm, and the sieved particles are subjected to a scanning electron microscope (Hitachi, Ltd., FlexSEM) at an accelerating voltage of 5KV and a magnification of 3000 times. Observation, according to the obtained image, measure the long diameter (L) and short diameter (D) of 50 randomly extracted particles, and calculate the average value (average long diameter (L), average short diameter (D)) of the same. L/D. From the viewpoint of reducing the bitterness of the component (A), the L/D of the cellulose is preferably 2.4 or more, more preferably 2.7 or more, and further preferably 3.0 or more, and from the viewpoint of making the mouthfeel good when ingested, in From the viewpoint of realizing a comfortable foaming feeling when taken under high foaming, it is preferably 4.0 or less, more preferably 3.8 or less, and still more preferably 3.6 or less. Furthermore, L/D of cellulose is preferably 2.4 to 4.0, more preferably 2.7 to 3.8, and further preferably 3.0 to 3.6.
自降低成分(A)之苦味之觀點出發，本發明之發泡性經口錠劑中之成分(C)之含量為0.5質量%以上，較佳為1.5質量%以上，更佳為2.5質量%以上，進一步較佳為4.0質量%以上，此外，自使服用時之口感良好之觀點以及在高發泡下服用時實現感覺舒適之發泡感之觀點出發，為50質量%以下，較佳為45質量%以下，更佳為25質量%以下，進一步較佳為20質量%以下。而且，本發明之發泡性經口錠劑中之成分(C)之含量為0.5～50質量%，較佳為1.5～45質量%，更佳為2.5～25質量%，進一步較佳為4.0～20質量%。From the viewpoint of reducing the bitterness of the component (A), the content of the component (C) in the foamable oral tablet of the present invention is 0.5 mass % or more, preferably 1.5 mass % or more, more preferably 2.5 mass % More preferably, it is 4.0 mass % or more, and from the viewpoint of improving the mouthfeel at the time of ingestion and realizing a comfortable foaming feeling when ingested with high foaming, it is 50 mass % or less, preferably 45 mass %. mass % or less, more preferably 25 mass % or less, still more preferably 20 mass % or less. Furthermore, the content of the component (C) in the foamable oral tablet of the present invention is 0.5 to 50% by mass, preferably 1.5 to 45% by mass, more preferably 2.5 to 25% by mass, and further preferably 4.0% by mass ~20% by mass.
自使服用時之口感良好之觀點、以及在高發泡下服用時實現感覺舒適之發泡感之觀點出發，本發明之發泡性經口錠劑中之成分(A)相對於成分(C)之含量質量比[(A)/(C)]為0.5以上，較佳為0.8以上，更佳為1.2以上，此外，自降低成分(A)之苦味之觀點以及抑制容器之膨脹之觀點出發，較佳為15以下，更佳為11以下，進一步較佳為4.5以下。而且，本發明之發泡性經口錠劑中之成分(A)相對於成分(C)之含量質量比[(A)/(C)]為0.5以上，較佳為0.5～15，更佳為0.8～11，進一步較佳為1.2～4.5。In the foamable oral tablet of the present invention, the component (A) in the foamable oral tablet of the present invention is relative to the component (C) from the viewpoints of making the mouthfeel good when ingested, and from the viewpoint of realizing a comfortable foaming feeling when ingested with high foaming. The content-to-mass ratio [(A)/(C)] is 0.5 or more, preferably 0.8 or more, more preferably 1.2 or more, and from the viewpoint of reducing the bitterness of the component (A) and suppressing the expansion of the container, Preferably it is 15 or less, More preferably, it is 11 or less, More preferably, it is 4.5 or less. Furthermore, the content-mass ratio [(A)/(C)] of the component (A) to the component (C) in the foamable oral tablet of the present invention is 0.5 or more, preferably 0.5 to 15, more preferably It is 0.8-11, More preferably, it is 1.2-4.5.
自使服用時之口感良好之觀點、以及在高發泡下服用時實現感覺舒適之發泡感之觀點出發，本發明之發泡性經口錠劑中之成分(B)相對於成分(C)之含量質量比[(B)/(C)]較佳為0.3以上，更佳為0.7以上，進一步較佳為0.9以上，此外，自降低成分(A)之苦味之觀點出發，較佳為10以下，更佳為7以下，進一步較佳為3.5以下。而且，本發明之發泡性經口錠劑中之成分(B)相對於成分(C)之含量質量比[(B)/(C)]較佳為0.3～10，更佳為0.7～7，進一步較佳為0.9～3.5。In the foamable oral tablet of the present invention, the component (B) in the foamable oral tablet of the present invention is relative to the component (C) from the viewpoints of improving the mouthfeel when ingested, and from the viewpoint of achieving a comfortable foaming feeling when ingested with high foaming. The content-to-mass ratio [(B)/(C)] is preferably 0.3 or more, more preferably 0.7 or more, still more preferably 0.9 or more, and from the viewpoint of reducing the bitterness of the component (A), preferably 10 Below, it is more preferable that it is 7 or less, and it is still more preferable that it is 3.5 or less. Furthermore, the content-mass ratio [(B)/(C)] of the component (B) to the component (C) in the foamable oral tablet of the present invention is preferably 0.3 to 10, more preferably 0.7 to 7 , more preferably 0.9 to 3.5.
本發明之發泡性經口錠劑在不損害本發明之效果之範圍內，可含有成分(A)、(B)、(C)以外之添加劑、根據需要而允許之載體。本發明之發泡性經口錠劑中，成分(A)、(B)、(C)以外之成分，自防止錠劑之不需要之吸濕、抑制容器之膨脹之觀點、提高服用時之口感良好之觀點出發，較佳使用吸濕性低之成分。The foamable oral tablet of the present invention may contain additives other than components (A), (B), and (C), and acceptable carriers as necessary, within a range that does not impair the effects of the present invention. In the foamable oral tablet of the present invention, the components other than the components (A), (B) and (C) are from the viewpoint of preventing unnecessary moisture absorption of the tablet, suppressing the expansion of the container, and improving the ingestion of the tablet. From the viewpoint of good texture, it is preferable to use a component with low hygroscopicity.
作為添加劑，不存在特定限定，例如可列舉甜味劑、維生素、礦物質、提取物類、成分(B)以外之酸味劑、香料、著色劑、防腐劑等。添加劑之含量可在不損害本發明目的之範圍內適當設定。The additives are not particularly limited, and examples thereof include sweeteners, vitamins, minerals, extracts, acidulants other than the component (B), flavors, colorants, and preservatives. The content of the additive can be appropriately set within a range that does not impair the purpose of the present invention.
此外，作為載體，例如可列舉賦形劑(蔗糖、乳糖、麥芽糖、海藻糖、帕拉金糖等二糖類、麥芽糖醇、木糖醇、赤蘚糖醇、山梨糖醇、還原帕拉金糖等糖醇)；黏合劑(例如，羥丙基甲基纖維素、羥丙基纖維素、明膠、預膠化澱粉、聚乙烯吡咯啶酮、聚乙烯醇、普魯蘭多糖、甲基纖維素、氫化油等)；崩解劑(例如，羧甲基纖維素、羧甲基纖維素鈣、交聯羧甲基纖維素鈉、交聯聚維酮、玉米澱粉、低取代度羥丙基纖維素等)；潤滑劑(例如，硬脂酸鈣、硬脂酸鎂、蔗糖脂肪酸酯、硬脂富馬酸鈉、滑石、二氧化矽等)；矯味劑(例如甜菊糖苷、薄荷醇、阿斯巴甜等)；瓊脂、輕質無水矽酸、磷酸氫鈣、填充劑、界面活性劑、分散劑、緩衝劑、稀釋劑等載體。載體之含量可在不損害本發明目的之範圍內適當設定。Further, examples of the carrier include excipients (disaccharides such as sucrose, lactose, maltose, trehalose, and palatinose, maltitol, xylitol, erythritol, sorbitol, reduced palatinose, etc.) isosugar alcohols); binders (eg, hydroxypropyl methylcellulose, hydroxypropyl cellulose, gelatin, pregelatinized starch, polyvinylpyrrolidone, polyvinyl alcohol, pullulan, methylcellulose , hydrogenated oil, etc.); disintegrants (for example, carboxymethyl cellulose, calcium carboxymethyl cellulose, croscarmellose sodium, crospovidone, corn starch, low-substituted hydroxypropyl cellulose (such as calcium stearate, magnesium stearate, sucrose fatty acid ester, sodium stearyl fumarate, talc, silicon dioxide, etc.); lubricants (such as steviol glycosides, menthol, Spartame, etc.); agar, light anhydrous silicic acid, calcium hydrogen phosphate, fillers, surfactants, dispersants, buffers, diluents and other carriers. The content of the carrier can be appropriately set within a range that does not impair the purpose of the present invention.
其中，自抑制容器之膨脹之觀點出發，本發明之發泡性經口錠劑較佳含有糖醇。糖醇較佳為麥芽糖醇。糖醇可為無水物、水合物中之任一種。Among them, the foamable oral tablet of the present invention preferably contains a sugar alcohol from the viewpoint of suppressing the expansion of the container. The sugar alcohol is preferably maltitol. The sugar alcohol may be either anhydrous or hydrate.
自抑制容器之膨脹之觀點出發，本發明之發泡性經口錠劑中之糖醇之含量較佳為10質量%以上，更佳為20質量%以上，進一步較佳為30質量%以上，此外，自在高發泡下服用時實現感覺舒適之發泡感之觀點出發，較佳為85質量%以下，更佳為80質量%以下，進一步較佳為65質量%以下。而且，發泡性經口錠劑中之糖醇之含量較佳為10～85質量%，更佳為20～80質量%，進一步較佳為30～65質量%。From the viewpoint of suppressing the expansion of the container, the content of the sugar alcohol in the foamable oral tablet of the present invention is preferably 10% by mass or more, more preferably 20% by mass or more, further preferably 30% by mass or more, In addition, from the viewpoint of realizing a comfortable foaming feeling when taken under high foaming, it is preferably 85% by mass or less, more preferably 80% by mass or less, and still more preferably 65% by mass or less. Furthermore, the content of the sugar alcohol in the foamable oral tablet is preferably 10 to 85% by mass, more preferably 20 to 80% by mass, and still more preferably 30 to 65% by mass.
糖醇之定量可使用HPLC。例如，可使用胺系管柱藉由折射率檢測法進行分析(《食物纖維基礎與應用》，主編：日本食物纖維學會，編輯：日本食物纖維學會編輯委員會等，著：青木誠一郎，出版社：第一出版股份有限公司，發售日：2008年10月)。The sugar alcohol can be quantified using HPLC. For example, it can be analyzed by refractive index detection method using an amine column ("Basics and Applications of Dietary Fiber", Editor-in-Chief: Japan Food Fiber Society, Editor: Editorial Board of Japan Food Fiber Society, etc., Author: Seiichiro Aoki, Publisher: First Publishing Co., Ltd., release date: October 2008).
本發明之發泡性經口錠劑，自防止錠劑之不需要之吸濕、在高發泡下服用時實現感覺舒適之發泡感之觀點、及抑制容器之膨脹之觀點出發，較佳限制寡糖之含有。The foamable oral tablet of the present invention is preferably limited from the viewpoints of preventing unwanted moisture absorption of the tablet, realizing a comfortable foaming feeling when taken under high foaming, and suppressing the expansion of the container. Contains oligosaccharides.
在此，限制寡糖之含有係指寡糖含量在本發明之發泡性經口錠劑中較佳為10質量%以下，更佳為5質量%以下，進一步較佳為1質量%以下，更進一步較佳為實質上不含有。Here, limiting the content of oligosaccharides means that the content of oligosaccharides in the foamable oral tablet of the present invention is preferably 10% by mass or less, more preferably 5% by mass or less, and still more preferably 1% by mass or less, More preferably, it does not contain substantially.
作為本發明中用於封裝發泡性經口錠劑之密封容器，較佳為空氣非透過性之容器，其中較佳為二氧化碳非透過性之容器，可使用在各種塑膠上層壓鋁等金屬之層壓包裝容器、蒸鍍鋁、二氧化矽等之包裝容器、以及利用金屬、玻璃等之容器。在本文中，二氧化碳非透過性係指二氧化碳透過度為50 cc/m2 ･day･atm(ASTD-1434)以下之物質。藉由將使用此類原材料之容器密封等而密閉，能夠以不洩漏二氧化碳之方式進行密封。As the airtight container for packaging the foamable oral tablet in the present invention, an air-impermeable container is preferred, and a carbon dioxide-impermeable container is preferred, and a metal such as aluminum laminated on various plastics can be used. Laminated packaging containers, packaging containers of vapor-deposited aluminum, silicon dioxide, etc., and containers using metal, glass, etc. As used herein, carbon dioxide impermeability refers to substances with a carbon dioxide permeability of 50 cc/m 2 ･day･atm (ASTD-1434) or less. By sealing, etc., a container using such a raw material, it can be sealed so as not to leak carbon dioxide.
作為本發明之發泡性經口錠劑之形態，自在高發泡下服用時實現感覺舒適之發泡感之觀點、抑制容器之膨脹之觀點出發，較佳為在口中之唾液等之水分之存在下產生二氧化碳之形態，較佳為口含錠。As the form of the foamable oral tablet of the present invention, the presence of moisture such as saliva in the mouth is preferred from the viewpoint of achieving a comfortable foaming feeling when taken with high foaming, and from the viewpoint of suppressing the expansion of the container. The form in which carbon dioxide is generated under the lower temperature is preferably a buccal tablet.
在製造本發明之發泡性經口錠劑時，除了成分(A)～(C)以外，亦可混合根據需要添加之添加劑，將該混合物作為原料粉末直接用壓錠成形機壓縮成形，亦可使用乾式製粒法、濕式製粒法等進行製粒，接著利用壓錠成形機對製粒物進行壓縮成形。作為壓錠成型機，可使用旋轉式壓錠機、單沖式壓錠機等通常使用之壓錠機。自維持成型物之硬度之觀點出發，壓錠時之壓縮成型壓力較佳為約10～30 MPa。為了以更低之壓縮成型壓力製造本發明之發泡性經口錠劑，較佳使用結晶纖維素。此外，錠劑硬度較佳為能夠耐受搬運、保存等之硬度，特定言之，較佳為約10 N～200 N。為了用少量的黏結劑實現上述硬度，較佳使用結晶纖維素。 錠劑之形狀可為圓形或具有橢圓形、長圓形、四邊形等之表面形狀之各種異形錠，自服用性之觀點出發，較佳為圓形。在圓形錠之情況下，自服用性之觀點出發，直徑較佳為3～30 mm，更佳為10～20 mm。此外，對於錠劑而言，自簡便性及有效性之觀點出發，較佳為每一製劑為0.1～6 g、進一步為0.3～3 g之重量。When producing the foamable oral tablet of the present invention, in addition to the components (A) to (C), additives to be added as necessary may be mixed, and the mixture may be directly compressed as a raw material powder with a tablet molding machine. Granulation is performed using a dry granulation method, a wet granulation method, or the like, and then the granulated product is compression-molded with an ingot molding machine. As the ingot press, a generally used ingot press, such as a rotary ingot press and a single-shot ingot press, can be used. From the viewpoint of maintaining the hardness of the molded product, the compression molding pressure during ingot pressing is preferably about 10 to 30 MPa. In order to manufacture the foamable oral tablet of the present invention with a lower compression molding pressure, crystalline cellulose is preferably used. Further, the tablet hardness is preferably a hardness capable of withstanding handling, storage, and the like, and specifically, preferably about 10 N to 200 N. In order to achieve the above-mentioned hardness with a small amount of binder, crystalline cellulose is preferably used. The shape of the lozenge may be round or various special-shaped lozenges having surface shapes such as oval, oval, quadrangle, etc. From the viewpoint of ingestion, it is preferably round. In the case of a round tablet, the diameter is preferably 3 to 30 mm, more preferably 10 to 20 mm, from the viewpoint of ingestion. Moreover, as for a tablet, from a viewpoint of simplicity and effectiveness, it is preferable that it is 0.1-6 g per formulation, and it is 0.3-3 g more preferably.
而且，藉由將由此得到之發泡性經口錠劑封裝至上述密封容器中，能夠得到本發明之密封容器裝之發泡性經口錠劑。And the foamable oral tablet in the airtight container of this invention can be obtained by packing the foamable oral tablet thus obtained in the said airtight container.
關於上述之實施方式，本發明亦揭示以下之實施方式。 ＜1＞一種密封容器裝之發泡性經口錠劑，其含有以下之成分(A)、(B)及(C)： (A)碳酸鹽14～30質量%； (B)有機酸或其鹽； (C)平均粒徑30～70 μm之纖維素0.5～50質量%， 成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]為0.25以上且3.0以下，並且成分(A)相對於成分(C)之含量質量比[(A)/(C)]為0.5以上。Regarding the above-mentioned embodiments, the present invention also discloses the following embodiments. <1> A foamable oral tablet in a sealed container, which contains the following components (A), (B) and (C): (A) 14-30 mass % of carbonate; (B) an organic acid or its salt; (C) 0.5 to 50 mass % of cellulose with an average particle diameter of 30 to 70 μm, The ratio of the moles (mol) of component (A) to the moles of acid groups (mol) of component (B) [(A) moles (mol)/(B) acid groups moles (mol)] is 0.25 or more and 3.0 or less, and the content mass ratio [(A)/(C)] of the component (A) with respect to the component (C) is 0.5 or more.
＜2＞如＜1＞之密封容器裝之發泡性經口錠劑，其中，成分(A)之含量為14質量%以上，較佳為15質量%以上，更佳為18質量%以上，此外，為30質量%以下，較佳為26質量%以下，更佳為22質量%以下，此外，為14～30質量%，較佳為15～26質量%，更佳為18～26質量%，進一步較佳為18～22質量%。 ＜3＞如＜1＞或＜2＞之密封容器裝之發泡性經口錠劑，其中，成分(B)較佳含有選自羥基羧酸、抗壞血酸及其等之鹽中之1種或2種以上，更佳含有選自檸檬酸、蘋果酸、酒石酸、抗壞血酸及其等之鹽中之1種或2種以上，進一步較佳含有檸檬酸。 ＜4＞如＜1＞～＜3＞中任一項之密封容器裝之發泡性經口錠劑，其中，成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比[(A)之莫耳數(mol)/(B)之酸基之莫耳數(mol)]為0.25以上，較佳為0.5以上，更佳為0.8以上，此外，為3.0以下，較佳為1.5以下，更佳為1.0以下，此外，為0.25～3.0，較佳為0.5～1.5，更佳為0.8～1.0。 ＜5＞如＜1＞～＜4＞中任一項之密封容器裝之發泡性經口錠劑，其中，纖維素之平均粒徑為30 μm以上，較佳為35 μm以上，更佳為40 μm以上，此外，為70 μm以下，較佳為60 μm以下，更佳為55 μm以下，此外，為30～70 μm，較佳為35～60 μm，更佳為40～55 μm。 ＜6＞如＜1＞～＜5＞中任一項之密封容器裝之發泡性經口錠劑，其中，纖維素之L/D較佳為2.4以上，更佳為2.7以上，進一步較佳為3.0以上，此外，較佳為4.0以下，更佳為3.8以下，進一步較佳為3.6以下，此外，較佳為2.4～4.0，更佳為2.7～3.8，進一步較佳為3.0～3.6。 ＜7＞如＜1＞～＜6＞中任一項之密封容器裝之發泡性經口錠劑，其中，(C)之含量為0.5質量%以上，較佳為1.5質量%以上，更佳為2.5質量%以上，進一步較佳為4.0質量%以上，此外，為50質量%以下，較佳為45質量%以下，更佳為25質量%以下，進一步較佳為20質量%以下，此外，為0.5～50質量%，較佳為1.5～45質量%，更佳為2.5～25質量%，進一步較佳為4.0～20質量%。 ＜8＞如＜1＞～＜7＞中任一項之密封容器裝之發泡性經口錠劑，其中，成分(A)相對於成分(C)之含量質量比[(A)/(C)]為0.5以上，較佳為0.8以上，更佳為1.2以上，此外，較佳為15以下，更佳為11以下，進一步較佳為4.5以下，此外，較佳為0.5～15，更佳為0.8～11，進一步較佳為1.2～4.5。 ＜9＞如＜1＞～＜8＞中任一項之密封容器裝之發泡性經口錠劑，其中，成分(B)相對於成分(C)之含量質量比[(B)/(C)]較佳為0.3以上，更佳為0.7以上，進一步較佳為0.9以上，此外，較佳為10以下，更佳為7以下，進一步較佳為3.5以下，此外，較佳為0.3～10，更佳為0.7～7，進一步較佳為0.9～3.5。 ＜10＞如＜1＞～＜9＞中任一項之密封容器裝之發泡性經口錠劑，其進一步較佳含有糖醇，更佳含有麥芽糖醇。 ＜11＞如＜1＞～＜10＞中任一項之密封容器裝之發泡性經口錠劑，其中，寡糖之含量較佳為10質量%以下，更佳為5質量%以下，進一步較佳為1質量%以下，更進一步較佳為實質上不含有。 ＜12＞如＜1＞至＜11＞中任一項之密封容器裝之發泡性經口錠劑，其較佳為口含錠。<2> The foamable oral tablet in a sealed container according to <1>, wherein the content of the component (A) is 14% by mass or more, preferably 15% by mass or more, more preferably 18% by mass or more, Moreover, it is 30 mass % or less, Preferably it is 26 mass % or less, More preferably, it is 22 mass % or less, and it is 14-30 mass %, Preferably it is 15-26 mass %, More preferably, it is 18-26 mass % , more preferably 18 to 22 mass %. <3> The foamable oral lozenge in a hermetically sealed container according to <1> or <2>, wherein the component (B) preferably contains one kind selected from the group consisting of hydroxycarboxylic acid, ascorbic acid and salts thereof, or the like. Two or more kinds, more preferably one or two kinds selected from the group consisting of citric acid, malic acid, tartaric acid, ascorbic acid and salts thereof, and more preferably citric acid. <4> The foamable oral tablet in a hermetically sealed container according to any one of <1> to <3>, wherein the molar number (mol) of the component (A) and the acid group of the component (B) are different. The molar number (mol) ratio [(A) molar number (mol)/(B) acid group molar number (mol)] is 0.25 or more, preferably 0.5 or more, more preferably 0.8 or more, Moreover, it is 3.0 or less, Preferably it is 1.5 or less, More preferably, it is 1.0 or less, and it is 0.25-3.0, Preferably it is 0.5-1.5, More preferably, it is 0.8-1.0. <5> The foamable oral tablet in a sealed container according to any one of <1> to <4>, wherein the average particle size of the cellulose is 30 μm or more, preferably 35 μm or more, more preferably It is 40 μm or more, furthermore, 70 μm or less, preferably 60 μm or less, more preferably 55 μm or less, and also 30 to 70 μm, preferably 35 to 60 μm, more preferably 40 to 55 μm. <6> The foamable oral tablet in a sealed container according to any one of <1> to <5>, wherein the L/D of the cellulose is preferably 2.4 or more, more preferably 2.7 or more, and still more It is preferably 3.0 or more, and more preferably 4.0 or less, more preferably 3.8 or less, still more preferably 3.6 or less, and more preferably 2.4 to 4.0, more preferably 2.7 to 3.8, still more preferably 3.0 to 3.6. <7> The foamable oral tablet in a sealed container according to any one of <1> to <6>, wherein the content of (C) is 0.5 mass % or more, preferably 1.5 mass % or more, and more It is preferably 2.5 mass % or more, more preferably 4.0 mass % or more, and further preferably 50 mass % or less, preferably 45 mass % or less, more preferably 25 mass % or less, further preferably 20 mass % or less, and , is 0.5-50 mass %, Preferably it is 1.5-45 mass %, More preferably, it is 2.5-25 mass %, More preferably, it is 4.0-20 mass %. <8> The foamable oral tablet in a sealed container according to any one of <1> to <7>, wherein the content and mass ratio of component (A) to component (C) is [(A)/( C)] is 0.5 or more, preferably 0.8 or more, more preferably 1.2 or more, in addition, preferably 15 or less, more preferably 11 or less, further preferably 4.5 or less, and more preferably 0.5 to 15, more Preferably it is 0.8-11, More preferably, it is 1.2-4.5. <9> The foamable oral tablet in a sealed container according to any one of <1> to <8>, wherein the content and mass ratio of component (B) to component (C) is [(B)/( C)] is preferably 0.3 or more, more preferably 0.7 or more, further preferably 0.9 or more, in addition, preferably 10 or less, more preferably 7 or less, still more preferably 3.5 or less, and more preferably 0.3 to 10, more preferably 0.7 to 7, still more preferably 0.9 to 3.5. <10> The foamable oral lozenge in a hermetically sealed container according to any one of <1> to <9>, further preferably containing a sugar alcohol, more preferably maltitol. <11> The foamable oral tablet in a sealed container according to any one of <1> to <10>, wherein the content of the oligosaccharide is preferably 10% by mass or less, more preferably 5% by mass or less, It is more preferable that it is 1 mass % or less, and it is still more preferable that it does not contain substantially. <12> The foamable oral tablet in a sealed container according to any one of <1> to <11>, which is preferably a buccal tablet.
[實施例] [碳酸鹽之分析] 發泡性經口錠劑中之碳酸鹽的含量之分析方法如下。 採集0.1～0.2 g之發泡性經口錠劑，加入水10 mL及50%磷酸2 mL且密封。進行10分鐘超音波處理後，放置1小時，將頂空氣體進行氣相層析儀測定，求出CO2 量，根據所產生之CO2 量進行計算。 ＜氣相層析操作條件＞ 機種：GC-14B，島津製作所(股) 檢測器：TCD 管柱：Chromosorb 101，80～100 mesh 玻璃管，ϕ3.2 mm×2 m 溫度：管柱50℃，進樣口及檢測器100℃ 單元電流75 mA 氣體壓力：氦(載氣)100 kPa 進樣量：頂空氣體0.2 mL[Examples] [Analysis of Carbonate] The method for analyzing the content of carbonate in the foamable oral tablet is as follows. Collect 0.1-0.2 g of foamable oral lozenges, add 10 mL of water and 2 mL of 50% phosphoric acid, and seal them. After sonicating for 10 minutes, it was left to stand for 1 hour, and the headspace gas was measured by a gas chromatograph, and the amount of CO 2 was obtained, which was calculated based on the amount of generated CO 2 . <Gas chromatography operating conditions> Model: GC-14B, Shimadzu Corporation Detector: TCD Column: Chromosorb 101, 80-100 mesh glass tube, ϕ3.2 mm×2 m Temperature: Column 50°C, Inlet and detector 100°C Unit current 75 mA Gas pressure: Helium (carrier gas) 100 kPa Injection volume: Headspace gas 0.2 mL
[有機酸之分析] 發泡性經口錠劑中之有機酸的含量之分析方法如下。 採集1 g發泡性經口錠劑，加入5%過氯酸20 mL，振盪10分鐘，由此提取。將其用水定容至200 mL，進行10分鐘超音波處理。過濾後供給至高效液相層析(HPLC)。 ＜HPLC操作條件＞ 機種：LC-20AD、島津製作所(股) 檢測器：紫外可見吸光光度計SPD-20AV、島津製作所(股) 管柱：Shim-pack SCR-102H 300×80 (長度×內徑(mm)) 島津製作所(股) 管柱溫度：40℃ 流動相：3 mmol/L過氯酸 反應液：含有0.2 mmol/L溴瑞香草酚藍 15 mmol/L磷酸氫二鈉溶液 流量：流動相1.0 mL/min、反應液1.4 mL/min 測定波長：445 nm[Analysis of Organic Acids] The analysis method of the content of the organic acid in the foamable oral tablet is as follows. Collect 1 g of foaming oral lozenges, add 20 mL of 5% perchloric acid, and shake for 10 minutes to extract. The volume was made up to 200 mL with water and sonicated for 10 minutes. After filtration, it was supplied to high performance liquid chromatography (HPLC). <HPLC operating conditions> Model: LC-20AD, Shimadzu Corporation (stock) Detector: UV-Vis Absorbance Photometer SPD-20AV, Shimadzu Corporation (stock) String: Shim-pack SCR-102H 300×80 (length×inner diameter(mm)) Shimadzu Corporation (stock) Column temperature: 40℃ Mobile phase: 3 mmol/L perchloric acid Reaction solution: containing 0.2 mmol/L bromovanillin blue 15 mmol/L disodium hydrogen phosphate solution Flow rate: mobile phase 1.0 mL/min, reaction solution 1.4 mL/min Measurement wavelength: 445 nm
[纖維素之分析] 在250 mL離心管中採集0.5～10 g之發泡性經口錠劑後，加入0.05%之氯化鈉水溶液85 mL。將混合液在沸騰水浴中進行30分鐘加熱處理，接著迅速冷卻。向冷卻液中添加5 mL胰酶溶液後，在pH 6.5、40℃之環境下培養6小時。將培養液離心分離，使用濾紙(ADVANTEC 101)回收固體物。在回收之殘渣中加入5%硫酸水溶液50 mL，在沸騰水浴中放置2.5小時。接著，使用玻璃過濾器(1G3)對主液進行抽濾後，使用丙酮及二乙醚對殘渣進行清洗。接著，在主清洗後固體物中加入72%硫酸30 mL，在5℃、冰箱中放置24小時以上後，進行抽濾，使用苯酚硫酸法測定濾液中之葡萄糖量，由此對纖維素量進行定量。[Analysis of Cellulose] After collecting 0.5-10 g of foamable oral lozenges in a 250 mL centrifuge tube, add 85 mL of 0.05% sodium chloride aqueous solution. The mixture was heated in a boiling water bath for 30 minutes, followed by rapid cooling. After adding 5 mL of trypsin solution to the cooling solution, the cells were incubated at pH 6.5 and 40°C for 6 hours. The culture broth was centrifuged, and solid matter was recovered using filter paper (ADVANTEC 101). 50 mL of 5% sulfuric acid aqueous solution was added to the recovered residue and placed in a boiling water bath for 2.5 hours. Next, after suction filtration of the main liquid using a glass filter (1G3), the residue was washed with acetone and diethyl ether. Next, 30 mL of 72% sulfuric acid was added to the solids after the main cleaning, and after being placed in a refrigerator at 5°C for more than 24 hours, suction filtration was performed, and the amount of glucose in the filtrate was measured by the phenol-sulfuric acid method to determine the amount of cellulose. Quantitative.
按表1～表4中記載之配合組成混合各成分。接著，使用單充式壓錠機(RIKEN)，用孔徑15 mm之環狀衝頭以18 MPa之壓錠壓進行壓錠，得到錠劑重量1 g/1錠、直徑15 mm之圓形之錠劑。 對於錠劑，按照以下之方法對口感良好、來自碳酸鹽之苦味、發泡感、容器之膨脹進行評價。Each component was mixed in accordance with the compounding compositions described in Tables 1 to 4. Next, use a single-charge tablet press (RIKEN), use a ring punch with a hole diameter of 15 mm to perform tablet pressing at a tablet pressure of 18 MPa, to obtain a tablet weight of 1 g/1 tablet and a round tablet with a diameter of 15 mm. Tablets were evaluated for good texture, carbonate-derived bitterness, foamy feeling, and container expansion according to the following methods.
〔口感之良好〕 根據專業評委3名，對將各例中得到之錠劑1錠放入口中時之口感進行了評價。評價基準如下所述，求出專業評委之評分之平均值，將小數點以後之第二位進行四捨五入而決定評分。需要說明的是，將服用時錠劑緩慢地溶解而感覺到口感最佳之實施例3作為評價基準之4，將服用時感覺到口感差之比較例3評價為評價基準之1。 4：口感非常好 3：口感良好 2：口感稍好 1：口感差[Good taste] The mouthfeel when one tablet obtained in each example was put into the mouth was evaluated by three professional panelists. The evaluation criteria are as follows. The average value of the scores of the professional judges is obtained, and the score is determined by rounding off the second decimal place. It should be noted that Example 3 in which the tablet was slowly dissolved during administration and felt the best in mouthfeel was taken as the 4th evaluation standard, and Comparative Example 3 in which the mouthfeel was felt poor when taken was evaluated as the 1st evaluation standard. 4: The taste is very good 3: Good taste 2: The taste is slightly better 1: poor taste
[苦味] 由專業評委3名評價各例中得到之錠劑1錠放入口中時來自碳酸鹽之苦味。評價基準如下所述，求出專業評委之評分之平均值，將小數點以後之第二位進行四捨五入而決定評分。需要說明的是，將專業評委3名評價為服用時完全不感覺到苦味之實施例3作為評價基準之4，將服用時感到強烈苦味之比較例1評價為評價基準之1。 4：完全沒有感覺到苦味 3：稍微感覺到苦味 2：感覺到苦味 1：感覺到強烈的苦味[bitterness] Three professional panelists evaluated the bitterness derived from carbonate when one tablet obtained in each example was put into the mouth. The evaluation criteria are as follows. The average value of the scores of the professional judges is obtained, and the score is determined by rounding off the second decimal place. In addition, Example 3 which had no bitter taste at all when taken by three professional judges was evaluated as the 4th evaluation standard, and Comparative Example 1 which felt a strong bitter taste when ingested was evaluated as the 1st evaluation standard. 4: No bitterness is felt at all 3: Slightly bitter taste 2: Bitterness is felt 1: Strong bitterness is felt
[發泡感] 藉由專業評委3名，對將各例中得到之錠劑1錠放入口中時之發泡感進行了評價。評價結果求出專業評委之評分之平均值，將小數點以後之第二位進行四捨五入而決定評分。需要說明的是，將在高發泡下服用時非常強烈地感覺到舒適之發泡感之實施例2作為評價基準之4，將服用時幾乎感覺不到舒適之發泡感之比較例2評價為1。 4：非常強烈地感覺到舒適之發泡感 3：強烈地感覺到舒適之發泡感 2：稍微感覺到舒適之發泡感 1：幾乎感覺不到舒適之發泡感[foaming] The foaming feeling when one tablet obtained in each example was put into the mouth was evaluated by three professional panelists. As a result of the evaluation, the average of the scores of the professional judges is calculated, and the second place after the decimal point is rounded to determine the score. It should be noted that Example 2 in which a comfortable foaming feeling is very strongly felt when taken with high foaming was taken as the evaluation standard 4, and Comparative Example 2 in which the comfortable foaming feeling was hardly felt when taken was evaluated as 1. 4: Very strong feeling of comfortable foaming 3: Strong feeling of comfortable foaming 2: Slightly feel a comfortable foaming feeling 1: The comfortable foaming feeling is hardly felt
[容器之膨脹] 將各錠劑放入鋁枕(60 mm×60 mm)中進行密封後，在60℃之恆溫槽中保存1週。利用阿基米德法測定保存前後之枕墊之體積，計算保存前後之枕之體積變化量。評價基準如下所述，確定了評分。 4：膨脹體積小於7 mL 3：膨脹體積為7 mL以上且小於9 mL 2：膨脹體積為9 mL以上且小於10 mL 1：膨脹體積為10 mL以上[Expansion of the container] Each tablet was placed in an aluminum pillow (60 mm×60 mm) for sealing, and then stored in a thermostatic bath at 60° C. for 1 week. The volume of the pillow before and after storage was measured by the Archimedes method, and the volume change of the pillow before and after storage was calculated. The evaluation criteria were as follows, and the scores were determined. 4: The expansion volume is less than 7 mL 3: The expansion volume is more than 7 mL and less than 9 mL 2: The expansion volume is more than 9 mL and less than 10 mL 1: The expansion volume is more than 10 mL
[原料] 碳酸氫鈉：小蘇打(食品添加C)(TOSOH CORPORATION) 檸檬酸：扶桑檸檬酸(無水)(扶桑化學工業(股)) 抗壞血酸：維生素C型SS(扶桑化學工業(股)) 蘋果酸：扶桑蘋果酸(扶桑化學工業(股)) 酒石酸：L-酒石酸型SS (扶桑化學工業(股)) 粉末纖維素：KC-Flock W-100 g (日本製紙(股))，平均粒徑37 μm，L/D＝2.8 結晶纖維素：Ceolus ST-100 (旭化成(股))、平均粒徑50 μm、L/D＝3.5 粉末纖維素：KC-Flock W-400G (日本製紙(股))，平均粒徑24 μm，L/D＝2.1 結晶纖維素：Ceolus UF-F702 (旭化成(股))、平均粒徑90 μm、L/D＝4.8 麥芽糖醇：Amalti MR-50 (Mitsubishi Shoji Foodtech Co., Ltd.) 硬脂酸鈣：硬脂酸鈣(太平化學(股)) 二氧化矽：Carplex FPS-500 (EVONIK公司)[raw material] Sodium bicarbonate: Baking soda (food additive C) (TOSOH CORPORATION) Citric acid: Fuso Citric Acid (anhydrous) (Fuso Chemical Industry Co., Ltd.) Ascorbic acid: Vitamin C type SS (Fuso Chemical Industry Co., Ltd.) Malic acid: Fusang malic acid (Fusang Chemical Industry Co., Ltd.) Tartaric acid: L-tartaric acid type SS (Fuso Chemical Industry Co., Ltd.) Powdered cellulose: KC-Flock W-100 g (Nihon Paper Co., Ltd.), average particle size 37 μm, L/D=2.8 Crystalline cellulose: Ceolus ST-100 (Asahi Kasei Co., Ltd.), average particle size 50 μm, L/D=3.5 Powdered cellulose: KC-Flock W-400G (Nihon Paper Co., Ltd.), average particle size 24 μm, L/D=2.1 Crystalline cellulose: Ceolus UF-F702 (Asahi Kasei Co., Ltd.), average particle size 90 μm, L/D=4.8 Maltitol: Amalti MR-50 (Mitsubishi Shoji Foodtech Co., Ltd.) Calcium stearate: calcium stearate (Taiping Chemical Co., Ltd.) Silica: Carplex FPS-500 (EVONIK)
[表1]
[表2]
[表3]
[表4]
由表1～表4可確認，藉由使成分(C)與成分(A)之比率在特定範圍內，且使成分(A)之莫耳數(mol)與成分(B)之酸基之莫耳數(mol)之比在特定範圍內，其在口中具有感覺舒適之高發泡感及口感之良好、良好之風味，且亦能夠抑制容器封裝時之膨脹。From Tables 1 to 4, it can be confirmed that the ratio of the component (C) to the component (A) is within a specific range, and the molar number (mol) of the component (A) and the acid group of the component (B) are adjusted. When the molar ratio is within a specific range, it has a pleasant high foaming feeling in the mouth and a good mouthfeel, a good flavor, and can also suppress swelling at the time of container sealing.
Claims (5)
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| JP2020085964 | 2020-05-15 | ||
| JP2020-085964 | 2020-05-15 |
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| TW110117097A TW202207912A (en) | 2020-05-15 | 2021-05-12 | Effervescent oral tablet packed in sealed container containing carbonate, organic acid or its salt, and cellulose |
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| JP (1) | JP2021181424A (en) |
| CN (1) | CN113662079A (en) |
| TW (1) | TW202207912A (en) |
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- 2021-05-12 TW TW110117097A patent/TW202207912A/en unknown
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| CN113662079A (en) | 2021-11-19 |
| JP2021181424A (en) | 2021-11-25 |
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