JP2019189560A - Tablet - Google Patents

Abstract

To provide a tablet that has high formulation stability and excellent disintegration by combining a cationized polymer with a carbon dioxide generator composed of carbonate and acid.SOLUTION: A tablet contains sodium bicarbonate, sodium carbonate, organic acid, and a cationized polymer and has a tablet hardness of 2 kgf or more and a liquid absorption time A of 45 min. or more and 65 min. or less.SELECTED DRAWING: None

Description

  The present invention relates to a tablet containing sodium bicarbonate, sodium carbonate, an organic acid, and a cationized polymer, having a specific tableting hardness and liquid absorption time A, sodium bicarbonate as a raw material thereof, and the sodium bicarbonate. The present invention relates to a method for producing a compressed tablet.

Conventionally, tableting containing sodium bicarbonate has been widely used as a bath agent, detergent, agrochemical formulation, pharmaceutical formulation, confectionery, and the like. As for bathing agents, in recent years it has been common to add bathing agents to bathing baths for the purpose of obtaining a hot bath effect, in addition to refreshing the mood of bathing by adding aroma and color to bathing baths, in addition to improving metabolism and improving cooling properties. It is widespread, and various forms such as bath salts, tablets, and liquids are sold. Among them, bathing agents containing a carbon dioxide generator that combines carbonates and acids expand blood vessels by carbon dioxide generated in the bath water and promote metabolism, recovery of fatigue, etc. Many of them are expected to be distributed in the form of tableted tablets.
A tableting tablet is generally produced by a method in which a powder material is molded by applying a high pressure. In this production method, the tableting hardness is an important point for improving the shape retention of the tablet. If the tableting hardness is low, cracks and cracks are likely to occur, and breakage occurs during production, storage, and transportation.On the other hand, if the tableting hardness is too high, the disintegration property deteriorates and functions as a tablet. This is because there is a problem that it cannot be demonstrated. In order to obtain an appropriate tableting hardness, various approaches have been proposed in the fields of bathing agents, cleaning agents, agricultural chemical formulations, pharmaceutical formulations, confectionery, etc. (for example, Patent Documents 1 to 5). Since the proposal improves the tablet hardness and disintegration of a specific tablet in each field, it has been difficult to apply it to other tablets having different compositions.

JP 2012-092031 A Japanese Patent Laid-Open No. 06-122900 Japanese Patent Laid-Open No. 06-157203 JP 2015-212258 A JP 2011-030437 A

Among bathing agents, bathing agents formulated with cationized polymers are one of the bathing agents that mimic natural hot springs, such as the feeling of bathing in natural hot springs and the moist feeling of the skin after bathing. It has gained popularity as one. In addition, cationized polymers are widely used as a conditioning base in the cosmetics and cosmetics fields, particularly in shampoos. However, the present inventor has known from experiments that the tableting hardness of the tableting is greatly reduced by blending the cationized polymer.
Accordingly, an object of the present invention is to provide a tableting that combines the cationized polymer with a carbon dioxide gas generator composed of a carbonate and an acid and has high formulation stability and good disintegration.

As a result of various studies on tableting containing sodium hydrogen carbonate, sodium carbonate, organic acid, and cationized polymer, the present inventor has surprisingly set the tableting hardness to a specific value or more and is described in detail below. By making the liquid absorption time A to be described within a specific range, it is excellent in shape retention that does not cause breakage during production, storage, and transportation, and further, disintegration occurs when the tableting hardness increases. Despite the technical common sense in the tableting field, the tableting of the present invention is also excellent in tablet disintegration, that is, both shape retention and disintegration can be obtained by specific tableting hardness. As a result, the present invention has been completed.
In addition, the present inventor specifically uses sodium hydrogen carbonate containing a specific crystal and having a specific bulk specific gravity as a raw material for tableting containing the cationized polymer of the present invention. It has also been found that the tablet hardness can be improved.

The gist of the present invention is specifically as follows.
1. A tableting composition comprising sodium bicarbonate, sodium carbonate, an organic acid, a cationized polymer, having a tableting hardness of 2 kgf or more, and a liquid absorption time A of 45 minutes to 65 minutes.
Liquid absorption time A: At an environmental temperature of 25 ° C., a circular shaped tablet with a diameter of 30 mm and a total amount of 15 g in a 90 mm diameter petri dish containing 5 ml of liquid paraffin, and the top and bottom surfaces of the circle with respect to the liquid paraffin liquid level 1. Time from the time when the paraffin is placed vertically until the liquid paraffin reaches the top of the tablet. The ratio of the following a line and the following b line (a line / b line) has an average of 2 or more and 4 or less, and a bulk specific gravity of 1.05 g / mL or less. Sodium bicarbonate as a raw material for tableting as described in 1.
Line a: the opposite end line having the longest straight line connecting the ends of one sodium bicarbonate crystal b line: the opposite end line having the longest straight line orthogonal to the line a The average of the ratio of the following a line and the following b line (a line / b line) is 2 or more and 4 or less, and uses sodium hydrogencarbonate whose bulk specific gravity is 1.05 g / mL or less as a raw material. Features 1. The manufacturing method of the tablet as described in 1 ..
Line a: the opposite end line where the straight line connecting the ends of one sodium hydrogen carbonate crystal is the longest line b: the opposite end line where the straight line orthogonal to the a line is the longest Sodium bicarbonate, sodium carbonate, organic acid, wherein the average of the ratio of the following a line and the following b line (a line / b line) is 2 or more and 4 or less and the bulk specific gravity is 1.05 g / mL or less, Obtained by tableting cationized cellulose; Tablets as described in 1.
Line a: the opposite end line where the straight line connecting the ends of one sodium bicarbonate crystal is the longest line b: The end line where the straight line orthogonal to the line a is the longest

The tableting of the present invention does not cause breakage such as cracks or cracks during production, storage and transportation, and not only exhibits excellent shape retention, but also due to this excellent shape retention, The contact surface can be suppressed to a minimum, so that the storage stability is improved and the formulation stability is extremely excellent.
It is known that when the tableting hardness of the effervescent tablet is improved, the disintegration property of the tablet when introduced into water deteriorates, and the generated carbon dioxide gas cannot be efficiently dissolved in water. Although the tableting tablet has a high tableting hardness, good tablet disintegration can be obtained, and the generated carbon dioxide gas can be efficiently dissolved in water.
That is, the tableted tablet of the present invention is extremely useful because it is compatible with formulation stability and disintegration.

Both the left and right figures are photomicrographs for explaining a line and b line in the present invention.

Hereinafter, the tableting of the present invention will be described in detail.
The tableting of the present invention is a combination of sodium bicarbonate, sodium carbonate, organic acid and cationized polymer, tableting hardness of 2 kgf or more, and liquid absorption time A of 45 minutes or more and 65 minutes or less. However, it is important for achieving both the stability of the preparation and the disintegration property.
In the tableting of the present invention, any sodium hydrogen carbonate, sodium carbonate, organic acid, cationized polymer may be used as long as the tableting hardness is 2 kgf or more and the liquid absorption time A is 45 minutes or more and 65 minutes or less. can do.

<Sodium bicarbonate>
Among them, sodium bicarbonate contains the specific crystals described below and has a specific bulk specific gravity. When sodium bicarbonate is used, the tableting hardness of the tablet of the present invention is 2 kgf or more, and the liquid absorption The time A can be set to 45 minutes or more and 65 minutes or less, which is preferable.
Use of sodium bicarbonate having an average of “ratio between a line and b line (a line / b line)” described below of 2 or more and 4 or less is preferable in terms of improving the hardness of the tableting of the present invention. .
(About a line / b line)
The a line and the b line in the present invention perform image analysis by observing sodium hydrogen carbonate with a microscope and paying attention to one crystal. Describing in more detail with reference to FIG. 1, the a line means the opposite end line having the longest straight line connecting the ends of one sodium hydrogencarbonate crystal, as shown by the solid lines in the left and right views of FIG. , B lines mean the opposite end line where the straight line orthogonal to the a line is the longest, as shown by the dotted lines in the left and right diagrams of FIG.
The ratio of the a line to the b line (a line / b line) is a value calculated by dividing the value of the a line by the value of the b line. This observation and measurement calculation were performed on 15 different crystals by a microscope, and the average value was taken as the average of the ratio of a line to b line (a line / b line) of the present invention.
The average of the ratio of a-line to b-line (a-line / b-line) of sodium hydrogen carbonate is preferably 2 or more and 4 or less, more preferably 2 or more and 3 or less, and more preferably 2 or more and 2.5. It is particularly preferred that
Moreover, the sodium hydrogencarbonate used for the tableting of the present invention contains 30% or more of crystals having a ratio of a line to b line (a line / b line) of 2 to 4 with respect to the total amount of sodium hydrogen carbonate. The content is preferably 40% or more, more preferably 50% or more. The content of the crystal can be determined by analyzing an image obtained by observing sodium bicarbonate with a microscope.

Use of sodium bicarbonate having a “bulk specific gravity” of 1.05 g / mL or less, which will be described below, is preferable in terms of improving the hardness of the tableting of the present invention.
(About bulk specific gravity)
The bulk specific gravity of the present invention is generally referred to as loose bulk specific gravity (density). It can be calculated by filling sodium hydrogencarbonate into a 100 mL capacity container “loosely” without tapping and measuring the weight of the filled sodium hydrogencarbonate.
The upper limit of the bulk specific gravity of sodium hydrogencarbonate is preferably 1.05 g / mL or less, more preferably 1.01 g / mL or less, and particularly preferably 0.95 g / mL or less. The lower limit of the bulk specific gravity is preferably 0.70 g / mL or more, more preferably 0.75 g / mL or more, and particularly preferably 0.80 g / mL or more.

Moreover, it is preferable that the sodium hydrogencarbonate used for the tableting of this invention is a specific compression rate.
The compression rate in the present invention is calculated by the following measurement method and calculation formula.
(1) 15 g of sodium bicarbonate was weighed and filled into a cylindrical mortar having a base area of 7.11 cm ² .
(2) The height of the filled sodium hydrogen carbonate of (1) was calculated by the bulk specific gravity of the present invention described above, and was defined as the thickness before compression.
(3) The thickness of the sodium hydrogen carbonate after being compressed at a pressure of 25 kN was measured with a hydraulic pump tableting machine, and the thickness after compression was determined.
[Calculation formula for compression ratio]
Compression rate (%) = (Thickness before compression−Thickness after compression) ÷ Thickness before compression The sodium bicarbonate used in the tableting of the present invention preferably has a lower limit value of 35% or more. 36% or more, more preferably 37% or more. Further, the upper limit value of the compression rate is preferably 50% or less, more preferably 48% or less, and particularly preferably 45% or less.
Furthermore, the sodium hydrogen carbonate used for the tableting of the present invention preferably has an average particle size larger than 150 μm in terms of improving tableting hardness.

Sodium bicarbonate used in the tableting of the present invention, in particular, the average of the ratio of a line to b line (a line / b line) is 2 or more and 4 or less, and the bulk specific gravity is 1.05 g / mL or less. Any sodium bicarbonate can be used as long as it satisfies these regulations, including commercially available products. Furthermore, even if it is sodium hydrogencarbonate which does not satisfy | fill a prescription | regulation, it can be set as sodium hydrogencarbonate which satisfy | fills these prescription | regulations, for example by means, such as classification and crushing with a sieve.
The average of the ratio of a line to b line (a line / b line) is 2 or more and 4 or less, and 15 g of sodium bicarbonate having a bulk specific gravity of 1.05 g / mL or less is used. filling the die of the ^second cylindrical, the hardness of the striking tablets obtained by compressing at a pressure of 25kN by a hydraulic pump type tabletting machine was 6.0kgf following range of 4.0 kgf.
In the tableting of the present invention, sodium bicarbonate is preferably in the range of 20% by weight to 75% by weight and more preferably in the range of 40% by weight to 65% by weight with respect to the total weight of the tableting. .

<About sodium carbonate>
In the tableting of the present invention, it is preferable to use an anhydrous sodium carbonate, preferably in the range of 3% by weight to 20% by weight with respect to the total weight of the tableting, and 5% by weight or more and 10% by weight or less. The range of is more preferable.
The sodium carbonate used for the tableting of the present invention preferably has an average particle size larger than 150 μm in terms of improving tableting hardness.
<About organic acids>
In the tablet of the present invention, the organic acid contained is selected from fumaric acid, citric acid, malic acid, tartaric acid, succinic acid, maleic acid, phthalic acid, glutaric acid, adipic acid, benzoic acid, salicylic acid and oxalic acid. 1 type or 2 types or more are mentioned. Among these, fumaric acid and / or succinic acid are more preferable from the viewpoint of formulation stability.
In the tableting of the present invention, the amount of the organic acid is preferably in the range of 10% by weight to 75% by weight and more preferably in the range of 20% by weight to 55% by weight with respect to the total weight of the tableting. Furthermore, it is particularly preferable to contain less than 30% by weight.

<About cationized polymers>
Examples of the cationized polymer that can be used in the tableting of the present invention include those available on the market.
Examples of the cationized cellulose include O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethylcellulose chloride, O- [2-hydroxy-3- (lauryldimethylammonio) propyl] hydroxyethylcellulose chloride, and chloride. Dimethyldiallylammonium / hydroxyethylcellulose copolymer, etc., as cationized guar gum, for example, O- [2-hydroxy-3- (trimethylammonio) propyl] guar gum chloride, as cationized dextran, for example, dextran chloride Hydroxypropyltrimethylammonium ether is a cationized acrylamide copolymer. For example, dimethyldiallylammonium chloride / acrylamide copolymer is a cationized collagen. Eg to chloride N- [2- hydroxy-3- (trimethylammonio) propyl] hydrolyzed collagen, other, cationic starch.
Among these, cationized cellulose, cationized guar gum, or cationized dextran is preferable from the viewpoint of obtaining the feel of a hot spring that simulates a natural hot spring and the solubility in water when used as a bath agent. In particular, the cationized cellulose is preferably one having a molecular weight of 100,000 to 2,000,000 and a degree of cationization (number of moles of cation group added per glucose) of 0.1 to 0.4 from the viewpoint of solubility in water. . In the tableting of the present invention, the amount of the cationized polymer is preferably 0.01 to 3.0% by weight, more preferably 0.1 to 2.0% by weight based on the total weight of the tableting. More preferably, it is 0.5 to 1.0% by weight.

<About tableting>
The tableting of the present invention is produced by mixing the above components and tableting, and a known tableting machine can be used. A known tableting machine is an apparatus in which a powder mixture is filled in a mortar and compressed between a lower punch and an upper punch and molded. A tableting machine is a single-punch tableting machine in which a pair of upper and lower punches move up and down within a single die, and a die is embedded in the outer periphery of a horizontally rotating turntable at equal intervals. There is a rotary tableting machine in which a series of operations of filling, compression, and discharging are continuously performed while rotating. As a known tableting machine, a tableting machine manufactured by Shiga Manufacturing Co., Ltd. can be used as a single tableting machine, and a tableting machine manufactured by Kikusui Manufacturing Co., Ltd. can be used as a rotary tableting machine. In addition, a tablet can be produced by single-punching using a mortar matched to the weight of the tablet to be produced and a hydraulic pump such as RaboNect Co., Ltd., Riken Kikai Co., Ltd., or the like. The tableting method should not be limited, and can be produced by a direct powder tableting method (direct compression method) or a granule tableting method (indirect compression method). Further, the order of mixing the components, the mixing method, and the like are appropriately selected.
The tablet size when using a tableting machine is preferably 80 mm or less, more preferably 60 mm or less, and more preferably 10 mm or less in the case of a cylindrical shape (in the case of a polygon, the length of one side). The above is preferable, and 30 mm or more is more preferable. The thickness of the tablet is preferably 20 mm or less, more preferably 17 mm or less, more preferably 5 mm or more, more preferably 8 mm or more, and even more preferably 10 mm or more. The shape of the tablet is not particularly limited, but is selected from a cylindrical shape, a block shape, a spherical shape, a hemispherical shape, a polygonal shape, and the like, and a cylindrical shape is preferable.

<About tableting hardness>
The tableting hardness of the tableting of the present invention is determined by applying a force gauge (for example, digital force gauge: MODEL-RZ-50, manufactured by Aiko Engineering Co., Ltd.) to the longitudinal direction (diameter direction) of the tableting. It means the maximum pressure when cracks and cracks occur.
Specifically, it is measured according to the tableting hardness measurement method for 15 g tableting described below.
<Method for measuring tablet hardness with 15 g tablet>
When cracks and cracks occur when pressure is applied under the following measurement conditions to the side (diameter direction) of a cylindrical tablet that is 30mm in diameter, approximately 15mm in thickness, and tableted at a pressure of 25kN. Measure the maximum pressure.
[Measurement condition]
-Digital force gauge: MODEL-RZ-50 (manufactured by Aiko Engineering Co., Ltd.)
-Motorized stand: MODEL-1308U (manufactured by Aiko Engineering Co., Ltd.)
・ Measurement attachment: 012B (circular, diameter 15 mm)
-Motorized stand speed during measurement: 5 mm / min
The tableting tablet of the present invention has a tableting hardness measured by the above measuring method of 2 kgf or more. Especially, the thing of 2.5 kgf or more is preferable, and the thing of 3 kgf or more is more preferable. The upper limit of the tableting hardness of the tableting of the present invention is preferably 6.5 kgf or less, and more preferably 6.0 kgf or less.

<About liquid absorption time A>
The tableting of the present invention is characterized in that the liquid absorption time A described below is 45 minutes or more and 65 minutes or less.
The liquid absorption time A is a cylindrical tablet formed by pressing with a pressure of 25 kN with a diameter of 30 mm, a thickness of about 15 mm, and a total amount of 15 g. A circular top and bottom flow into a 90 mm diameter petri dish containing 5 ml of liquid paraffin. It means the time from the time when the paraffin is placed so as to be perpendicular to the liquid surface of paraffin to the time when the liquid paraffin reaches the top of the tablet.
The liquid paraffin used to measure the liquid absorption time A may be any liquid paraffin having a kinematic viscosity of 8 to 17 mm ² / s at 37.8 ° C., for example, liquid paraffin No. manufactured by Sanko Chemical Co., Ltd. 70-S can be exemplified.
The liquid absorption time A of the tableting of the present invention is 45 minutes or more and 65 minutes or less, and preferably 45 minutes or more and 60 minutes or less.
<About void area and porosity>
The method for measuring the void area of the tableting of the present invention is not particularly limited, and can be calculated, for example, by image analysis of the cross section. Specifically, although it demonstrates in detail by the specific example mentioned later, the following measuring methods can be used. That is, a cylindrical tablet that was compressed with a pressure of 25 kN, having a diameter of 30 mm, a thickness of about 15 mm, and a total amount of 15 g, was roughly divided into two parts at the diameter part, and the cross-sectional image was divided into two parts, the raw material phase and the cell phase (void part). The bubble phase (void part) area (mm ² ) can be regarded as the void area of the present invention, and the void ratio (%) can also be calculated from this image analysis.
In the tableting of the present invention, the actual void area in the specific examples described later is preferably in the range of 0.15 mm ² or less. Moreover, it is preferable that the porosity in the below-mentioned specific example is the range of 2-15%, and it is more preferable that it is the range of 5-15%.

The tableted tablet of the present invention is used for bathing agents, denture cleaning agents, flushing toilet cleaning agents, foam cleaning agents such as drain outlet cleaning agents, agrochemical preparations such as paddy field jumbo agents, foaming confectionery, head spa use, etc. Can also be used.
When the tableted tablet of the present invention is used as a bath agent, in addition to the above-mentioned sodium hydrogen carbonate, sodium carbonate, organic acid, cationized polymer, various components known in the bath agent field as necessary. (Hereinafter also referred to as “optional component”) may be contained alone or in combination of two or more. Although the arbitrary component which can be contained when using the tableting of this invention as a bath agent below is illustrated, it cannot be overemphasized that it is not limited to the component etc. which were described here.

<Inorganic salts (excluding sodium bicarbonate and sodium carbonate)>
Chloride such as sodium chloride, potassium chloride, ammonium chloride, sodium sesquicarbonate, calcium carbonate, potassium carbonate, magnesium carbonate, heavy magnesium carbonate, carbonate, sodium sulfate, magnesium sulfate, aluminum sulfate, iron sulfate, potassium aluminum sulfate , Sulfates such as sodium thiosulfate, calcium thiosulfate, potassium thiosulfate and sodium hyposulfite, nitrates such as sodium nitrate, potassium nitrate and calcium nitrate, phosphates such as sodium phosphate and calcium hydrogen phosphate, calcium silicate, Magnesium silicate, calcium sulfide, calcium disulfide, potassium sulfide, sodium sulfide, ammonium sulfide, barium sulfide, zinc sulfide, tin sulfide, antimony sulfide, iron sulfide, carbon disulfide, phosphorus sulfide, and other sulfides, sodium hydroxide , Hydroxides such as calcium hydroxide, borax, boric acid, calcium oxide, potassium bromide, and potassium permanganate and the like. Among the inorganic salts, sodium chloride, sodium sulfate, potassium aluminum sulfate, magnesium sulfate, calcium carbonate, and calcium silicate are preferable. In particular, when the tableted tablet of the present invention is used as a bath agent, sodium sulfate, silica It is preferable to contain calcium acid, and these are also suitable as formulation aids.
<Oil components>
Natural fats and oils such as nuka oil, jojoba oil, olive oil and soybean oil; hydrocarbons such as petrolatum, squalane and squalene; alcohols such as stearyl alcohol and cetyl alcohol; fatty acids such as myristic acid, lauric acid and palmitic acid; monoglycerides and triglycerides Synthetic oils and fats; silicone and the like. These can also be contained as a moisturizing component.
<High molecular substances (excluding cationized polymers)>
Carboxymethylcellulose and its salt, hydroxyethyl cellulose and its salt, alginic acid and its salt, polyphosphoric acid and its salt, polyacrylic acid and its salt, pyrophosphoric acid and its salt, crystalline cellulose, gum arabic, xanthan gum, guar gum, locust bean Examples include gum, gelatin, styrene polymer emulsion, dextrin, polyethylene glycol, liquid paraffin, casein, polyoxyethylene polyoxypropylene glycol, and polyethylene glycol monostearate. Among the above polymer substances, when the tablet of the present invention is used as a bath agent, it preferably contains liquid paraffin, dextrin and polyethylene glycol, and these are also suitable as formulation aids.

<Perfume ingredients and essential oil ingredients>
Peppermint, eucalyptus, lemon, verbena, citronella, kayapte, salvia, thyme, clove, rosemary, hyssop, jasmine, chamomile, neroli, mugwort, perilla, marjoram, laurel, juniper berry, nutmeg, ginger, onion, garlic, lavender, Bergamot, Clary Sage, Peppermint, Basil, Rose, Petit Glen, Cinnamon, Mace, Citral, Citronellal, Borneol, Linalool, Geraniol, Nerol, Rodinol, Orange, Artemisia, Camphor, Menthol, Cineol, Eugenol, Hydroxycitronellal, Sandalwood, Costas, Labdanum, Amber, Musk, α-Pinene, Limonene, Methyl salicylate, Sowjutsu, Sandalwood, Kanokosou Oil, such as pearl oysters, Japanese cypress, senkyu, spruce, spruce, ginger, peonies, peonies, gongos, sanshin, keihi, carrots, dragonflies, dough cutlet, ginger, ginger, pine bush, peony, jujube, fennel, chimney, chamomile Amyl nitrate, trimethylcyclohexanol, allyl sulfide, nonyl alcohol, decyl alcohol, phenylethyl alcohol, methyl carbonate, ethyl carbonate, phenylacetate, guaiacol, indole, cresol, thiophenol, p-dichlorobenzene, p-methylquinoline, isoquinoline "Perfume and Flavor Materials of Natural Origin", Steffe n Arctander, Allured Pub. Co. (1960), “Encyclopedia of Scents”, edited by Japan Fragrance Association, Asakura Shoten (1989), “Flowers oils and Floral Compounds In Perfumery”, Danute Pajaudis Anonis, Allred Pub. Co. (1993), “Perfume and Flavor Chemicals (aroma chemicals)”, Vols. I and II, Steffen Arctander, Allured Pub. Co. (1994), “Fundamentals of perfumes and fragrances”, edited by Motoki Nakajima, Sangyo Tosho (1995), “Synthetic perfumes Chemistry and product knowledge”, Motokazu Into, Kagaku Kogyo Nipposha (1996), “Encyclopedia of Scents” Examples include fragrance components and essential oil components described in “Encyclopedia”, Mitsatsu Yatakai, Maruzen (2005). These fragrance components and essential oil components can be used alone or in combination of two or more types as a blended fragrance. Furthermore, a solvent, a fragrance | flavor stabilizer, etc. can be mixed suitably and can also be used as a fragrance | flavor composition.

<Herbal medicines>
Examples include chamomile, gailla, campi, fennel, kei-gai, keihi, gyoza, chimpi, senkyu, shobu, tokyo, spruce, dokudami, capsicum, birch, burdock, carrot, garlic, clove, rosemary, yuzu and thyme. These may be contained as an extract. Moreover, it can contain as a fragrance | flavor or a moisturizing component.
<Enzymes>
Examples include trypsin, α-chymotrypsin, bromelain, papain, protease, proctase, seratiothiopeptidase, lysozyme, and pepsin.
<Pigments and minerals>
Titanium oxide, talc, clay, kaolin, bengara, yellow iron oxide, mica, mica, titanium, titanium dioxide, zinc oxide, bentonite, zeolite, silicic anhydride, metasilicic acid, neutral clay, etc. Etc. Among the pigments and minerals, when the tableted tablet of the present invention is used as a bath agent, it is preferable to contain titanium oxide, which is also suitable as a formulation aid.
<Dyes>
Blue No. 1, Blue No. 2, Red No. 102, Red No. 106, Red No. 227, Red No. 230 (1), Yellow No. 4, Yellow No. 5, Yellow No. 202 (1), Green No. 3, Green No. 201 No., legal dyes such as green No. 204 and orange No. 205, and natural dyes such as chlorophyll, riboflavin, annatto and anthocyanin.
<Vitamins and their derivatives>
Vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, vitamin F, vitamin H, pantothenic acid, nicotinic acid or derivatives thereof, vitamin E nicotinate, tocopherol acetate, sodium ascorbate and the like can be mentioned. These can also be contained as a moisturizing component.

<Seaweed extracts>
Anaaaosa, Mill, Usbaaonori, Hitegusa, Susiaoonori, Casanori, Green Algae Plants such as Heraiwata, Hanemomo, Nagarami, etc. Brown algae plants such as Honda walla, Umitorano, Marubaamanori, Asakusanori, Susabinori, Cyprinus, Hirakusa, Macausa, Triashi, Hanafnori, Owl, Nori, Tosekirinsai, Akagiginanso, Nigiri nori, Nigiri norii Extracts obtained from red algae plants and the like. These can also be contained as a moisturizing component.
<Plant extracts>
Examples include aloe extract, green tea extract, loofah water, chamomile extract, licorice extract, comfrey extract, eucalyptus extract, royal jelly extract, lemon extract, rosehip extract, peach leaf extract and the like. There is no particular limitation on the extraction method. These can also be contained as a moisturizing component.
<Cool sensations>
Mentor derivatives such as menthol, camphor and thymol, monocyclic compounds, bicyclic alcohols, tricyclic alcohols, tricyclic amides, mint oil and the like.
<Moisturizing ingredients>
Ceramides such as ceramide, ceramide derivatives and ceramide-like substances; organic acid salts such as sodium lactate, disodium tartrate, sodium pyrrolidonecarboxylate, disodium glutamate; isoprene glycol, propylene glycol, 1,3-butylene glycol, glycerin, Polyhydric alcohols such as xylose, xylitol, sorbitol; water-soluble polymers such as polyvinyl alcohol, sodium alginate, polyvinylpyrrolidone, mucopolysaccharides such as chondroitin sulfate and hyaluronic acid, collagen and derivatives thereof, protein, keratin, fibroin and Hydrolyzate: Fatty acid esters such as isopropyl myristate and isopropyl palmitate, shea butter, squalane, placenta, arbutin, casein, silk, honey, etc. And the like.

<Solvent>
Purified water, ion-exchanged water, alcohols such as ethanol, propanol and benzyl alcohol, polyhydric alcohols such as ethylene glycol, diethylene glycol, dipropylene glycol, glycerin and 1,3-butanediol, ethylene glycol monomethyl ether, ethylene glycol monoethyl ether , Ethylene glycol monopropyl ether, ethylene glycol monobutyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, diethylene glycol monoisobutyl ether, triethylene glycol monobutyl ether, propylene glycol monomethyl ether, propylene glycol di Chill ether, dipropylene glycol monomethyl ether, tripropylene glycol monomethyl ether, tripropylene glycol monobutyl ether, propylene glycol monopropyl ether, dipropylene glycol monopropyl ether, propylene glycol monobutyl ether, propylene glycol-tert-butyl ether, dipropylene glycol monobutyl ether , Glycol ethers such as dipropylene glycol dimethyl ether, phenyl carbitol, phenyl cellosolve, benzyl carbitol, paraffins such as n-paraffin, esters such as diethyl phthalate, benzyl benzoate, triethyl citrate, isopropyl myristate, etc. 3 -Methyl-4-methoxybutanol N- methylpyrrolidone and propylene carbonate.
<Surfactant>
Nonionic active agents such as polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene fatty acid ester, sorbitan fatty acid ester; fatty acid ester such as soap base, α- Anionic active agents such as sodium olefin sulfonate, sodium lauryl sulfate, sodium polyoxyethylene lauryl sulfate, sodium coconut oil fatty acid methyl taurine; alkyl betaine, alkylamidopropyl betaine, 2-alkyl-N-carboxymethyl-N-hydroxy Examples include amphoteric surfactants such as ethyl imidazolinium betaine; cationic surfactants such as alkylamine salts and quaternary ammonium salts.

<Anti-fading agent>
Examples include amino acids such as glycine, alanine, and glutamic acid; salicylic acid and salts thereof.
<PH adjuster>
Examples thereof include disodium hydrogen phosphate, trisodium phosphate, disodium hydrogen citrate, and trisodium citrate.
<Fungicide>
Examples include isopropylmethylphenol, triclosan, dichloroisocyanuric acid, silver zeolite, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, chlorhexidine chloride, hinokitiol, phenol, glycyrrhizinate and derivatives thereof.
<Others>
Examples thereof include glucose, sucrose, trehalose, phytocollage, isoflavone, paraoxybenzoic acid ester, vegetable or fruit extract (extract), deep sea water and the like.
What is necessary is just to set content of the arbitrary component mentioned above suitably in the range which does not impair the effect of this invention. Moreover, you may cover the tableting of this invention with a well-known water-soluble film etc. as needed and needed.

  EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.

<Reference test>
[Test sample]
A test sample A was a columnar tablet containing sodium bicarbonate, sodium carbonate, succinic acid, cationized cellulose and having a diameter of 50 mm, a thickness of about 15 mm, and a total amount of 45 g and compressed at a pressure of about 98 kN (about 10 t). .
A cylindrical tablet that differs only in that it does not contain test sample A and cationized cellulose was designated as test sample a.
[Test specimen evaluation]
Using a digital force gauge (manufactured by Aiko Engineering Co., Ltd., measurement attachment: pressing part, circle with a diameter of 15 mm) in the side surface (thickness) direction so that pressure is applied to the center of the top surface of the test specimens A and a. On the other hand, pressure was applied, and the maximum pressure when cracks or cracks occurred was defined as tableting hardness. The evaluation test was performed three times, and the average value was defined as each tableting hardness.
The tableting hardness of test specimen a was 5.4 kgf, while the tableting hardness of test specimen A was 2.0 kgf.

From the results of the above “reference test”, it has been clarified that the tableting hardness of the tableting is reduced to about 40% by adding a cationized polymer such as cationized cellulose. When the tableting hardness under the above tableting conditions is about 2.0 kgf, the tableting hardness needs to be improved because damage is expected at the time of manufacture, storage and transportation.
As a result of examining each of sodium hydrogen carbonate, sodium carbonate, succinic acid, and cationized cellulose, we obtained new knowledge that the tableting hardness of the tablet changes by changing sodium bicarbonate, which is the main compounding ingredient. A detailed study was conducted on sodium bicarbonate.

<Detailed study on sodium bicarbonate>
[Preparation of test specimen]
Seven types of sodium bicarbonate were obtained by classifying or crushing commercially available sodium bicarbonate and sieving it with sieves, and these were designated as test samples 1-7. The average particle diameters of the test samples 1 to 7 were all larger than 150 μm.
[Test specimen evaluation]
The tableting hardness was determined by measuring the hardness of a tablet made of only sodium hydrogen carbonate in accordance with the above-mentioned tableting hardness measurement method for 15 g tableting.
Further, according to the measurement method described above, “average ratio of a line to b line (a line / b line)”, “bulk specific gravity”, and “compression ratio” were calculated.
Furthermore, by analyzing the microscope observation image of the test specimen, a crystal having an “ratio of a line to b line (a line / b line)” of 2 or more and 4 or less is included in the total amount of sodium bicarbonate. The ratio of being measured was measured.
The evaluation results are shown in Table 1.

As shown in Table 1, the present inventors have surprisingly found a new finding that the tableting hardness of sodium bicarbonate varies greatly depending on its shape and the like.
When examined in detail, sodium hydrogen carbonate whose tableting hardness is greatly improved is that the average of the ratio of a line to b line (a line / b line) is 2 or more and 4 or less and the bulk specific gravity is 1. It was confirmed that the requirement of “05 g / mL or less” was satisfied, and in Table 1, it was also clarified that the sodium hydrogen carbonates of the test samples 1 to 3 corresponded.
On the other hand, although the average of the ratio of a line to b line (a line / b line) is 2.0, sodium bicarbonate of test specimen 4 whose bulk specific gravity is outside the scope of the present invention is The tablet hardness was 2.5 kgf, which was clearly inferior to the tableting hardness of sodium bicarbonate of Test Samples 1 to 3.
Further, although the bulk specific gravity is 1.03 g / mL, the sodium bicarbonate of the test sample 5 whose average of the ratio of the a line and the b line (a line / b line) is 1.7 is the tableting hardness. Was 1.2 kgf, which was also found to be significantly inferior to the tableting hardness of sodium bicarbonate of Test Samples 1 to 3.

<Tablet hardness confirmation test for tablets>
<Examples 1-3, Comparative Examples 1-4, Reference Examples 1 and 2>
[Preparation of test specimen]
Using the sodium bicarbonates of test specimens 1 to 7 in the above-mentioned “detailed examination test on sodium bicarbonate”, the blending amounts shown in Table 2 (the numbers in Table 2 mean weight%). Mixing uniformly gave a powder mixture. This powder mixture was compression-molded at a pressure of 25 kN using a hydraulic pump type tableting machine to produce 15 g of a tablet having a diameter of 30 mm and a thickness of approximately 15 mm. The tableting hardness of the resulting tableting tablet was measured according to the tableting hardness measurement method for the 15-g tableting tablet described above. The average particle size of the sodium carbonate used was 300 μm. Table 2 summarizes the blending amounts of each of Examples 1 to 3, Comparative Examples 1 to 4, and Reference Examples 1 and 2 and the tableting hardness.

From the results of Table 2, in tableting with sodium bicarbonate alone, sodium bicarbonate of Test Samples 1 to 3 in which improvement in tableting hardness was confirmed was blended with tableting containing cationized cellulose. It has been clarified that the tableting hardness as a tableting tablet can be improved.
Tableting hardness containing cationized cellulose (Examples 1 to 3 and Comparative Examples 1 to 4) has lower tableting hardness than tableting tablets not containing cationized cellulose (Reference Examples 1 and 2). However, it can be understood from the comparison between Example 2 and Reference Example 1 and Comparative Example 4 and Reference Example 2 that the tableting hardness of Example 2 is suppressed from decreasing in tableting hardness.
From these results, the tableting hardness containing cationized cellulose can be set to 2 kgf or more, more preferably 2.5 kgf or more, more preferably 3 kgf or more by blending with specific sodium hydrogen carbonate. Was confirmed.

<Verification test of void area and porosity>
[Measurement method of void area (150 times magnification)]
The tableting (Examples 1 to 3 and Comparative Examples 1 to 4) prepared in the above “Tabletting hardness confirmation test of tableting” was used as a test specimen.
Each test specimen was roughly divided into two parts at the diameter, and the cross section was observed with a scanning electron microscope (SEM) at a magnification of 150 times. In the image of the cross section, the solid phase derived from the raw material and the bubble phase (void portion) were binarized, and the bubble phase area was measured by image processing to obtain a void area (150 magnifications).
[Calculation method of actual void area]
The void area measured at a magnification of 150 times (150 magnification) was converted into an actual void area with a magnification of 1 by the following calculation formula.
<Calculation formula>
Actual void area (mm ² ) = void area (150 magnification) ÷ (150 × 150)
[Calculation method of porosity]
The ratio of the void area (150 magnification) was calculated with respect to the total area subjected to image processing.
<Calculation formula>
Void ratio (%) = (Cavity area (150 magnification) ÷ Processed image area) × 100
The “area of the processed image” in the calculation formula means the area of the cross-sectional image in the “method for measuring the void area (150 magnification)”. The processed image was 1280 pixels × 960.05 pixels, and the resolution was 201 dpi (dots per inch). Since 1 inch is 25.4 mm, 1280 pixels corresponds to 161.75 mm (25.4 ÷ 201 × 1280≈161.75), and 960.05 pixels are 121.32 mm (25.4 ÷ 201 × 960. 05≈121.32). That is, the void ratio (%) of each test specimen was calculated assuming that the area of the processed image was 19623.51 mm ² (161.75 × 121.32).
Table 3 shows the void area (150 magnification) (mm ² ), actual void area (mm ² ), and void ratio (%) of the compressed tablets of Examples 1 to 3 and Comparative Examples 1 to 4.

  From the results of Table 3, it was confirmed that the tableting examples of Examples 1 to 3 were greatly reduced in both the void area and the porosity as compared with the tableting of Comparative Examples 1 to 4.

<Tablet absorption time confirmation test>
[Examination details]
The above-described liquid absorption time A measuring method using the tableting (Examples 1 to 3, Comparative Examples 1 to 4, Reference Examples 1 and 2) prepared in the above “Tabletting hardness confirmation test for tablets” as a test specimen In accordance with this, the liquid absorption time A was measured. Moreover, the liquid absorption amount (g) was calculated from the weight difference between the test specimens before and after the measurement. Table 4 shows the liquid absorption time A (minute) and liquid absorption amount (g) of the tableted tablets of Examples 1 to 3, Comparative Examples 1 to 4, and Reference Examples 1 and 2.

From the results in Table 4, the tableting hardness of Examples 1 to 3 having a tableting hardness of 2 kgf or more has a liquid absorption time A in the range of 45 minutes to 65 minutes, and the tableting hardness of Comparative Examples 1 to 2 is less than 2 kgf. The liquid absorption time A of Reference Example 2 is 10 minutes or more longer than the liquid absorption time A of 4 tableting tablets, that is, the liquid absorption speed is slow, and the tableting hardness is comparable. It was revealed that it was shorter than 10 minutes or more, that is, the liquid absorption speed was high.
As shown in Table 3, it was confirmed that the tableting examples of Examples 1 to 3 were considerably smaller in both void area and porosity than the tableting tablets of Comparative Examples 1 to 4, and the tableting hardness was high. Since the bathing agents 1 to 3 have a small internal void and require time for the liquid to penetrate, the liquid absorption time A was estimated to be longer than the tableting of Comparative Examples 1 to 4. As shown in Table 4, it was clarified that the relationship between the tableting hardness of Examples 1 to 3 and Comparative Examples 1 to 4 and the liquid absorption time A was as expected.
On the other hand, the liquid absorption amounts of Examples 1 to 3 and Comparative Examples 1 to 4 are substantially the same as 1.2 to 1.3 although the porosity is greatly different. It was revealed that the liquid absorption amount of No. 2 decreased by about 25%.
Although the tableting hardness of Examples 1 to 3 having high tableting hardness is considered to be reduced in the amount of liquid absorption due to a smaller internal void portion than the tableting tablets of Comparative Examples 1 to 4, As shown in Table 4, it was confirmed that the relationship between the tableting hardness and the liquid absorption amount in Comparative Examples 1 to 4 was a completely unexpected result contrary to expectations.
The inventor paid attention to the fact that the liquid absorption amounts of Examples 1 to 3 and Comparative Examples 1 to 4 were almost the same, and then performed an evaluation test on the disintegration property of the tableting.

<Tablet disintegration confirmation test>
[Examination details]
The tableting (Examples 1 to 3, Comparative Examples 1 to 4, Reference Examples 1 and 2) prepared in the above-mentioned “Tabletting hardness confirmation test of tableting” was used as a test specimen. One tablet of each test specimen was put into 40 ° C./5 L hot water, and the time (seconds) until one tablet disintegrated and completely dissolved was measured.
Table 5 summarizes the disintegration / dissolution times (seconds) of the compressed tablets of Examples 1 to 3, Comparative Examples 1 to 4, and Reference Examples 1 and 2.

From the results shown in Table 5, the tableting tablets of Examples 1 to 3 are completely poured into hot water despite the fact that the tableting hardness is higher than that of Comparative Examples 1 to 4 and the porosity (%) is low. It was clarified that the time until dissolution was approximately the same and the disintegration was excellent.
With regard to tableting, it is known that if the tableting hardness is high, the disintegration property of the tablet when it is put into water deteriorates, and the generated carbon dioxide gas cannot be efficiently dissolved in water. However, surprisingly, the tableting of the present invention can be obtained with a very good tablet disintegrating property while maintaining a good tableting hardness that does not cause breakage during production, storage and transportation. It was confirmed that carbon dioxide gas can be efficiently dissolved in water.

As described above, the tableting of the present invention not only exhibits excellent shape retention without breakage such as cracks and cracks, but also has excellent shape retention so that the contact surface with air is minimized. Therefore, it is extremely excellent in formulation stability, such as improving storage stability. Moreover, although the tableting of the present invention has high tableting hardness, good tablet disintegration can be obtained, and the generated carbon dioxide gas can be efficiently dissolved in water.
That is, the tableted tablet of the present invention is very useful because it has both good formulation stability and disintegration.

Claims (4)

A tableting composition comprising sodium bicarbonate, sodium carbonate, an organic acid, a cationized polymer, having a tableting hardness of 2 kgf or more, and a liquid absorption time A of 45 minutes to 65 minutes.
Liquid absorption time A: At an environmental temperature of 25 ° C., a circular shaped tablet with a diameter of 30 mm and a total amount of 15 g in a 90 mm diameter petri dish containing 5 ml of liquid paraffin, and the top and bottom surfaces of the circle with respect to the liquid paraffin liquid level Time from placing the liquid paraffin vertically until the liquid paraffin reaches the top of the tablet The average of the ratio of the following a line and the following b line (a line / b line) is 2 or more and 4 or less, and the bulk specific gravity is 1.05 g / mL or less. Sodium bicarbonate as a raw material for tableting as described.
Line a: the opposite end line where the straight line connecting the ends of one sodium bicarbonate crystal is the longest line b: The end line where the straight line orthogonal to the line a is the longest The average of the ratio of the following a line and the following b line (a line / b line) is 2 or more and 4 or less, and uses sodium hydrogencarbonate whose bulk specific gravity is 1.05 g / mL or less as a raw material. The manufacturing method of the tableting tablet of Claim 1 characterized by the above-mentioned.
Line a: the opposite end line with the longest straight line connecting the ends of one sodium bicarbonate crystal b line: The end line with the longest straight line orthogonal to the line a Sodium bicarbonate, sodium carbonate, organic acid, wherein the average of the ratio of the following a line and the following b line (a line / b line) is 2 or more and 4 or less and the bulk specific gravity is 1.05 g / mL or less, The tableting of Claim 1 obtained by tableting a cationized cellulose.
Line a: the opposite end line where the straight line connecting the ends of one sodium bicarbonate crystal is the longest line b: The end line where the straight line orthogonal to the line a is the longest