Film-coated tablets

Abstract

The purpose of the present invention is to provide film-coated tablets which have excellent tablet lubricity in the oral cavity and do not undergo the delay in disintegrating time of uncoated tablets. The present invention provides: film-coated tablets each comprising a tablet, a first film layer that coats the tablet and comprises an inorganic salt, and a second film layer that coats the tablet coated with the first film layer and comprises a thickening agent; film-coated tablets each comprising a tablet, a first film layer that coats the tablet, and a second film layer that coats a part located on the outer side of the first film layer and comprises a thickening agent, in which the first film layer comprises an inorganic salt and the inorganic salt decreases the viscosity of the thickening agent contained in the second film layer; and others.

Description

[Technical Field]

[0001] The present invention relates to a film-coated tablet, and more particularly to a film-coated tablet for use in the fields of pharmaceuticals and health foods. [Background technology]

[0002] Oral administration of tablets and other tablets is a common method of administration and ingestion of pharmaceutical active ingredients, nutritional active ingredients, food ingredients, and the like. Tablets are easy to handle, easy to take, and portable, making them the most commercially available oral dosage form. However, in the medical field, many or large tablets may be ingested. In addition, in the health food field, tablets are commonly used as dosage forms for nutritional supplements, functional foods, and the like, and multiple tablets may be ingested at once. Furthermore, tablets may be difficult for elderly people, children, and patients with impaired swallowing function to ingest. Thus, ingesting multiple or large tablets is a burden for various patients and consumers. Therefore, tablets that are easy to swallow are desired.

[0003] As an example of an easily swallowable tablet, Patent Document 1 discloses an easily ingestible solid preparation in which a slimy or sticky feeling in the oral cavity is suppressed by incorporating a thickener, a binder, and a sugar alcohol into the coating layer. Patent Document 2 also discloses an easily ingestible solid preparation in the form of a minitablet in which a coating layer contains multiple thickeners and polyvalent metal compounds, so that the tablet surface quickly gels upon ingestion, increasing the viscosity and making the tablet more easily slide over the mucous membrane. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Publication No. 2002-275054 [Patent Document 2] International Publication No. 2011 / 125798 Summary of the Invention [Problem to be solved by the invention]

[0005] Thickeners are components used to improve the slipperiness of tablets. On the other hand, they are also used in sustained-release formulations that inhibit or control the dissolution of active ingredients, such as by delaying the disintegration time of tablets. Therefore, in tablets in which thickeners are incorporated into the film layer to make them easier to swallow, there is concern that the disintegration time in the gastrointestinal tract is delayed, delaying the release of the active ingredient, and preventing the original efficacy and effectiveness from being fully demonstrated. Furthermore, there is a problem in that the dissolution rate of the active ingredient is reduced depending on the composition of the drug contained in the tablet and the film layer. Therefore, a film layer that maintains the slipperiness of the tablet without affecting the disintegration time of the uncoated tablet in the gastrointestinal tract is desired.

[0006] An object of the present invention is to provide a film-coated tablet that has excellent tablet sliding properties in the oral cavity and suppresses delay in the disintegration time of an uncoated tablet. [Means for solving the problem]

[0007] As a result of intensive research into the above-mentioned problems, the present inventors have discovered that a film-coated tablet with excellent swallowability and improved disintegration time can be produced by incorporating an inorganic salt into the tablet and the first film layer coating the tablet, and incorporating a thickener into the second film layer, which is the outer layer. Based on this discovery, the present invention has been made.

[0008] That is, the following [1] to [7] are provided as means for solving the above problems. [1] Tablets and a first film layer coating the tablet and containing an inorganic salt; A film-coated tablet comprising: a second film layer that coats the tablet coated with the first film layer and contains a thickener. [2] Tablets and a first film layer coating the tablet; A tablet comprising a film coating comprising: a second film layer that is coated on the outside of the first film layer and contains a thickener; A film-coated tablet, wherein the first film layer contains an inorganic salt, which reduces the viscosity of the thickener contained in the second film layer. [3] Tablets and a first film layer coating the tablet; A film-coated tablet comprising a second film layer that is coated on the outside of the first film layer and contains a thickener, A film-coated tablet, wherein the first film layer comprises an inorganic salt and a water-soluble film base having a viscosity of 100 mPa·s or less in a 2% by weight aqueous solution at 20°C. [4] The content of the inorganic salt in the first film layer is 20 to 55% by mass, The film-coated tablet according to any one of [1] to [3], wherein the content of the thickener in the second film layer is 20 to 40% by mass. [5] The first film layer is 2 to 6 parts by mass per 100 parts by mass of the uncoated tablet, The film-coated tablet according to any one of [1] to [4], wherein the second film layer is 2 to 4 parts by mass per 100 parts by mass of the uncoated tablet. [6] The film-coated tablet according to any one of [1] to [5], wherein the inorganic salt contained in the first film layer is a water-soluble inorganic salt. [7] The inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and sodium chloride; The film-coated tablet according to any one of [1] to [5], wherein the thickener contained in the second film layer is at least one selected from the group consisting of sodium alginate and xanthan gum. [Effects of the Invention]

[0009] According to the film-coated tablet of the present invention, it is possible to provide a film-coated tablet in which the swallowability of the tablet is improved and the delay in the disintegration time of the tablet in the digestive tract is suppressed. [Brief explanation of the drawings]

[0010] [Figure 1] FIG. 1 is a schematic explanatory diagram showing a cross section of a film-coated tablet. [Figure 2] FIG. 1 is a schematic explanatory diagram showing a method for testing tablet sliding properties. DETAILED DESCRIPTION OF THE INVENTION

[0011] Hereinafter, an embodiment of the film-coated tablet will be described in detail with reference to the drawings. The film-coated tablets described in the embodiments are merely examples used to explain film-coated tablets, and are not intended to be limiting.

[0012] Figure 1 is a schematic explanatory diagram showing a cross section of a film-coated tablet of the present invention. As shown in Figure 1, a film-coated tablet 10 comprises an uncoated tablet 12 containing an active ingredient having a desired efficacy and effect, a first film layer 14 as an inner layer that coats the outside of the uncoated tablet 12, and a second film layer 16 as an outer layer that coats the outside of the tablet coated with the first film layer.

[0013] A first aspect of the present invention is a film-coated tablet comprising: a tablet; a first film layer that coats the tablet and contains an inorganic salt; and a second film layer that coats the tablet coated with the first film layer and contains a thickener.

[0014] According to the film-coated tablet of the first aspect of the present invention, when the second film layer comes into contact with water, the tablet surface exhibits slipperiness, making the tablet easier to swallow. Furthermore, the inorganic salt in the first film layer acts to suppress delay in the disintegration time of the uncoated tablet.

[0015] A second aspect of the present invention is a film-coated tablet comprising a film coating including a tablet, a first film layer covering the tablet, and a second film layer covering the tablet from the outside of the first film layer and containing a thickener, wherein the first film layer contains an inorganic salt, and the inorganic salt reduces the viscosity of the thickener contained in the second film layer.

[0016] According to the film-coated tablet of the second aspect of the present invention, the viscosity of the thickener in the outer layer can be reduced by the action of the inorganic salt contained in the first film layer, thereby promoting the penetration of water into the tablet, thereby exerting an effect of inhibiting the swallowability of the tablet and delaying the disintegration time of the plain tablet.

[0017] A third aspect of the present invention is a film-coated tablet comprising a tablet, a first film layer coating the tablet, and a second film layer coating the tablet from the first film layer and containing a thickener, wherein the first film layer contains an inorganic salt and a water-soluble film base having a viscosity of 100 mPa s or less in a 2% by mass aqueous solution at 20°C.

[0018] According to the film-coated tablet of the third aspect of the present invention, the inorganic salt contained in the first film layer acts to allow water to quickly penetrate into the tablet, thereby shortening the disintegration time of the uncoated tablet. Furthermore, the inclusion of a low-viscosity water-soluble film base in the first film layer promotes dissolution of the first film layer. Furthermore, the low viscosity of the solution in which the first film layer is dissolved can promote water penetration into the tablet.

[0019] In one embodiment of the present invention, a film-coated tablet contains an inorganic salt in the first film layer and a thickener in the second film layer. This allows the film-coated tablet to exhibit the following effect: when ingested, the thickener in the second film layer that comes into contact with water or saliva first imparts lubricity to the tablet surface, and then the inorganic salt in the first film layer acts to inhibit delay in the tablet's disintegration time in the digestive tract. Note that multiple film coating layers may be provided inside the first film layer, between the first and second film layers, and on the outside of the second film layer.

[0020] The shape of the tablet is not particularly limited, and examples thereof include round tablets, oval tablets, flower-shaped tablets, etc. Furthermore, the tablet may be provided with one or two scoring lines for dividing into two or four pieces as needed.

[0021] The size of the tablet is not particularly limited, and for example, in the case of a round tablet, the diameter is preferably 3 mm or more and 20 mm or less. The lower limit is more preferably 5 mm or more, even more preferably 7 mm or more, and particularly preferably 9 mm or more. On the other hand, the upper limit is more preferably 15 mm or less, even more preferably 12 mm or less.

[0022] The thickness of the tablet is not particularly limited, but is preferably, for example, 2.0 mm or more and 10.0 mm or less. The lower limit is more preferably 2.5 mm or more, even more preferably 3.0 mm or more, and particularly preferably 3.5 mm or more. On the other hand, the upper limit is more preferably 9.0 mm or less, even more preferably 8.0 mm or less, and particularly preferably 6.0 mm or less.

[0023] By setting the size and thickness of the tablet within the above ranges, the tablet can be made easy to take.

[0024] The coating amount of the first film layer is not particularly limited, and is preferably, for example, 0.1 to 20.0 parts by mass per 100 parts by mass of the uncoated tablet. The lower limit is more preferably 0.5 parts by mass or more, even more preferably 1.0 parts by mass or more, and particularly preferably 2.0 parts by mass or more. On the other hand, the upper limit is more preferably 15.0 parts by mass or less, even more preferably 10.0 parts by mass or less, even more preferably 8.0 parts by mass or less, and particularly preferably 6.0 parts by mass or less.

[0025] The amount of coating of the second film layer is not particularly limited, and is preferably, for example, 0.1 to 20.0 parts by mass per 100 parts by mass of the uncoated tablet. The lower limit is more preferably 0.5 parts by mass or more, even more preferably 1.0 parts by mass or more, and particularly preferably 2.0 parts by mass or more. On the other hand, the upper limit is more preferably 15.0 parts by mass or less, even more preferably 8.0 parts by mass or less, even more preferably 6.0 parts by mass or less, and particularly preferably 4.0 parts by mass or less.

[0026] In one embodiment of the present invention, a film-coated tablet is preferred in which the first film layer is 2 to 6 parts by mass per 100 parts by mass of the uncoated tablet, and the second film layer is 2 to 4 parts by mass per 100 parts by mass of the uncoated tablet. By controlling the coating amounts of the first and second film layers within the above ranges, the swallowability of the tablet and the effect of suppressing delay in disintegration time of the uncoated tablet can be further improved.

[0027] In one embodiment of the present invention, the mass ratio of the first film layer to the second film layer is preferably 1: 1, more preferably 2: 1, and even more preferably 3: 1. By controlling the mass ratio of the first film layer to the second film layer within the above range, the swallowability of the tablet and the effect of suppressing a delay in the disintegration time of the uncoated tablet can be further improved.

[0028] The thickness of the first film layer and the second film layer is not particularly limited, and is preferably, for example, 1 μm or more and 1000 μm or less. The lower limit is more preferably 3 μm or more, even more preferably 5 μm or more, and particularly preferably 10 μm or more. On the other hand, the upper limit is more preferably 500 μm or less, even more preferably 200 μm or less, and particularly preferably 100 μm or less. The coating layer thickness can be measured based on an image of the fracture surface of the preparation taken using a scanning electron microscope.

[0029] By setting the weight and thickness of the first film layer and the second film layer within the above ranges, it is possible to effectively impart to the tablet good swallowability and the effect of inhibiting delay in disintegration time of the uncoated tablet.

[0030] [First film layer] The first film layer contains an inorganic salt, thereby shortening the disintegration time of the tablet. First, the components in the first film layer will be described in detail.

[0031] (inorganic salts) The inorganic salt contained in the first film layer preferably reduces the viscosity of the thickener contained in the second film layer when the film-coated tablet is taken, thereby shortening the disintegration time of the tablet. That is, the inorganic salt preferably reduces the viscosity of the thickener. In particular, the inorganic salt preferably reduces the viscosity of the thickener contained in the second film layer in the digestive tract after taking the film-coated tablet, thereby shortening the disintegration time of the tablet.

[0032] The characteristic that an inorganic salt reduces the viscosity of a thickener can be identified, for example, by determining whether or not the viscosity of an aqueous solution of a thickener decreases when the inorganic salt is added to the aqueous solution.

[0033] As an example of a method for determining whether an inorganic salt reduces the viscosity of a thickener, when the viscosity (20°C) of a first aqueous solution of thickener having a thickener concentration of 1% by mass is compared with the viscosity (20°C) of a second aqueous solution of thickener having a thickener concentration of 1% by mass and an inorganic salt concentration of 2% by mass, if the viscosity (20°C) of the second aqueous solution of thickener is lower, it can be determined that the inorganic salt reduces the viscosity of the thickener. The viscosity of the first or second aqueous solution of thickener can be measured by a capillary viscometer method described in the 17th Edition of the Japanese Pharmacopoeia, or the like.

[0034] The inorganic salt is preferably a water-soluble inorganic salt that is acceptable for use in pharmaceuticals, foods, etc. and has a solubility of 5 g or more in 100 g of water at 20° C. Examples of inorganic salts include inorganic compounds in which the hydrogen atoms of a water-soluble inorganic acid are substituted with a metal.

[0035] Since the inorganic salt contained in the first film layer is water-soluble, the inorganic salt contained in the first film layer dissolves in water and reacts with the thickener contained in the second film layer to reduce the viscosity of the thickener, thereby further improving the effect of suppressing delay in disintegration time of the uncoated tablet.

[0036] Specific examples of inorganic salts include potassium phosphate (dipotassium phosphate), sodium phosphate (monosodium phosphate), calcium phosphate, potassium hydrogen phosphate (potassium dihydrogen phosphate), sodium hydrogen phosphate, calcium hydrogen phosphate, potassium carbonate, sodium carbonate, calcium carbonate, potassium bicarbonate, sodium bicarbonate, calcium bicarbonate, potassium chloride, sodium chloride, and calcium chloride. Preferred inorganic salts are potassium phosphate, sodium bicarbonate, and sodium chloride, as they are excellent at shortening the disintegration time of tablets. These inorganic salts may be blended alone or in combination of two or more.

[0037] In addition, when a carbonate-based inorganic salt (e.g., potassium carbonate, sodium carbonate, calcium carbonate, potassium bicarbonate, sodium bicarbonate, calcium bicarbonate) is used in the first film layer, it is preferable not to add an organic acid to the first film layer in order to improve stability.

[0038] The content of the inorganic salt in the first film layer is not particularly limited, and is preferably, for example, 10% by mass or more and 60% by mass or less relative to the mass of the first film layer. The lower limit is more preferably 13% by mass or more, even more preferably 15% by mass or more, and particularly preferably 20% by mass or more. On the other hand, the upper limit is more preferably 57% by mass or less, even more preferably 56% by mass or less, and particularly preferably 55% by mass or less. By setting the content of the inorganic salt in the first film layer within the above range, the effect of shortening the disintegration time of the tablet can be significantly improved.

[0039] (Water-soluble film base for the first film layer) The water-soluble film base is a base for forming a film containing an inorganic salt, and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples include cellulose derivatives, synthetic resins, polysaccharides, etc.

[0040] The viscosity of the water-soluble film base is preferably low; for example, the viscosity of a 2% by weight aqueous solution at 20°C is preferably 0.1 mPa·s or more and 100 mPa·s or less. The lower limit is more preferably 1 mPa·s or more, even more preferably 2 mPa·s or more, and particularly preferably 3 mPa·s or more. On the other hand, the upper limit is more preferably 45 mPa·s or less, even more preferably 40 mPa·s or less, and particularly preferably 35 mPa·s or less. The viscosity of the water-soluble film base can be measured by the capillary viscometer method described in the 17th Edition of the Japanese Pharmacopoeia, or the like.

[0041] Specific examples of water-soluble film bases include hydroxypropylmethylcellulose (viscosity of a 2% by weight aqueous solution at 20°C of 15 mPa·s or less), hydroxypropylcellulose (viscosity of a 2% by weight aqueous solution at 20°C of 10 mPa·s or less), polyvinyl alcohol (viscosity of a 4% by weight aqueous solution at 20°C of 6 mPa·s or less), polyvinylpyrrolidone (average molecular weight of 40,000 or less), methylcellulose (viscosity of a 2% by weight aqueous solution at 20°C of 15 mPa·s or less), and pullulan (viscosity of a 10% by weight aqueous solution at 30°C of 15 to 180 mPa·s).

[0042] Preferred water-soluble film bases are hydroxypropyl methylcellulose and hydroxypropyl cellulose, which are readily available and easy to coat. These water-soluble film bases may be used alone or in combination of two or more.

[0043] The content of the water-soluble film base in the first film layer is not particularly limited, and is preferably, for example, 30% by mass or more and 80% by mass or less relative to the mass of the first film layer. The lower limit is more preferably 33% by mass or more, even more preferably 35% by mass or more, and particularly preferably 40% by mass or more. On the other hand, the upper limit is more preferably 77% by mass or less, even more preferably 75% by mass or less, and particularly preferably 74% by mass or less. By setting the content of the water-soluble film base in the first film layer within the above range, a tablet with excellent coatability can be obtained.

[0044] (Other ingredients) The first film layer may contain other components as needed in addition to the inorganic salt and water-soluble film base, such as plasticizers, sweeteners, flavorings, colorants, and light protectants.

[0045] In order to maintain the function of the first film layer in shortening the tablet disintegration time, it is preferable not to incorporate a thickener into the first film layer that reacts with the inorganic salt contained in the first film layer to form a gel. It is also more preferable not to incorporate a thickener into the first film layer. By not incorporating a thickener, the first film layer becomes more easily dissolved, which has the effect of allowing the inorganic salt contained in the first film layer to more easily act on the second film layer. Thickeners will be explained in the section on the second film layer.

[0046] Adding a plasticizer to the first film layer can adjust the flexibility and elasticity of the composition used to coat the uncoated tablet, improving application performance. The plasticizer imparts flexibility and elasticity to the composition and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of plasticizers include polyethers, polyhydric alcohols, esters, organic acids, and vegetable oils.

[0047] Specific examples of plasticizers include polyethylene glycol, polypropylene glycol, glycerin, glycerol, polyol, triethyl citrate, acetyl monoglyceride, butylphthalyl butyl glycolate, dibutyl tartrate, propylene glycol, glycerol monostearate, tripropioin, diacetin, citric acid, medium-chain fatty acid oil, and rapeseed oil.

[0048] The molecular weight of the polyethylene glycol is preferably, for example, from 4,000 to 20,000. Specific examples of polyethylene glycol include PEG 6000 and PEG 8000. These plasticizers may be blended alone or in combination of two or more.

[0049] Adding a sweetener to the first film layer can sweeten the tablet, making it easier to take. The sweetener is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of sweeteners include natural sweeteners and artificial sweeteners.

[0050] Specific examples of sweeteners include erythritol, sorbitol, aspartame, acesulfame potassium, stevia, sucralose, glycyrrhizinic acid, thaumatin, saccharin, saccharin sodium, etc. These sweeteners may be blended alone or in combination of two or more.

[0051] Adding a flavoring substance to the first film layer can make the tablet easier to swallow. The flavoring substance improves the sensory sensation of the tablet in the oral cavity and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of flavoring substances include natural vegetable oils and aldehyde compounds.

[0052] Specific examples of flavoring substances include spearmint oil, peppermint oil, cinnamon oil, fruit essence, benzaldehyde, neral, decanal, tolyl aldehyde, 2-dodenal, aldehyde C-8, aldehyde C-9, aldehyde C-12, 2,6-dimethyloctanal, etc. These flavoring substances may be blended alone or in combination of two or more.

[0053] By adding a colorant to the first film layer, the tablet can be colored, thereby enhancing the palatability and distinguishability of the coated solid preparation. The colorant is not particularly limited as long as it improves the palatability and distinguishability of the tablet and is acceptable for use in pharmaceuticals, foods, etc. Examples of colorants include natural pigments and synthetic pigments.

[0054] Specific examples of coloring agents include cochineal, carmine, curcumin, riboflavin, annatto, titanium oxide, yellow ferric oxide, ferric oxide, talc, calcined silica, magnesium carbonate, and synthetic food colorings such as Food Blue No. 1, Food Blue No. 2, Food Yellow No. 4, Food Yellow No. 5, Food Green No. 3, Food Red No. 2, Food Red No. 3, Food Red No. 102, Food Red No. 104, Food Red No. 105, and Food Red No. 106. These coloring agents may be blended alone or in combination of two or more.

[0055] By adding a light protectant to the first film layer, the ingredients contained in the tablet can be protected from light. The light protectant is not particularly limited as long as it provides light-blocking properties to the tablet and is acceptable for use in pharmaceuticals, foods, etc. Examples of light protectants include oxides and tar-based dyes.

[0056] Specific examples of light protection agents include titanium oxide, yellow ferric oxide, red ferric oxide, food yellow No. 5, and food yellow No. 4. These light protection agents may be blended alone or in combination of two or more.

[0057] (Film coating method) Next, a method for coating the uncoated tablets will be described. The method for film coating the uncoated tablets can be a method for producing a film-coated tablet that is commonly used in the art.

[0058] Examples of methods for film coating uncoated tablets include film coating using a film coating machine. Specifically, uncoated tablets containing active ingredients and additives are loaded into the film coating machine, and the components contained in the first film layer are dissolved and dispersed in an organic solvent such as water, ethanol, hexane, ethyl acetate, or isopropyl alcohol, or a mixture thereof, to prepare a coating solution, which is then sprayed onto the uncoated tablets and dried to coat them.

[0059] With the above-mentioned configuration, the first film layer containing an inorganic salt can exhibit the effect of shortening the disintegration time of the tablet.

[0060] [Second film layer] The second film layer is intended to provide the tablet with slipperiness. The components of the second film layer are not particularly limited as long as they are used in the fields of pharmaceuticals, food, etc. Examples of the components of the second film layer include methacrylic acid polymer compounds, water-insoluble substances, polysaccharides, water-soluble acrylic acid polymers, water-soluble substances such as cellulose derivatives, etc. First, the components of the second film layer will be described in detail.

[0061] (thickener) The thickener has solubility in water and viscosity, and provides lubricity to the tablet surface. There are no particular limitations on the thickener, so long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of thickeners include polysaccharides, water-soluble acrylic acid polymers, and cellulose derivatives. Preferred examples include sodium alginate, xanthan gum, guar gum, carrageenan, gellan gum, pectin, gum arabic, locust bean gum, carboxyvinyl polymer, hydroxypropylmethylcellulose, and hydroxypropylcellulose. More preferred examples include sodium alginate and xanthan gum. These thickeners may be used alone or in combination.

[0062] The inorganic salt contained in the first film layer is preferably at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and potassium chloride, and the thickener contained in the second film layer is preferably at least one selected from the group consisting of alginic acid and xanthan gum. By limiting the inorganic salt contained in the first film layer and the thickener contained in the second film layer to specific compounds, the swallowability of the tablet and the effect of suppressing delay in disintegration time of the uncoated tablet can be further improved.

[0063] Preferred combinations of the inorganic salt contained in the first film layer and the thickener contained in the second film layer include the following (a) and (b). (a) The inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and potassium chloride, and the thickener contained in the second film layer is alginic acid. (b) The inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and potassium chloride, and the thickener contained in the second film layer is xanthan gum.

[0064] Specific examples of the viscosity of the thickener include sodium alginate having a viscosity of 500 mPa·s or more in a 1% by mass aqueous solution at 20°C; xanthan gum having a viscosity of 1000 mPa·s or more in a 1% by mass aqueous solution at 20°C; guar gum having a viscosity of 1000 mPa·s or more in a 1% by mass aqueous solution at 20°C; carrageenan having a viscosity of 100 mPa·s or more in a 1% by mass aqueous solution at 25°C; locust bean gum having a viscosity of 1000 mPa·s or more in a 1% by mass aqueous solution at 25°C; carboxyvinyl polymers having a viscosity of 100 mPa·s or more in a 2% by mass aqueous solution at 20°C; hydroxypropyl methylcellulose having a viscosity of 150 mPa·s or more in a 2% by mass aqueous solution at 20°C; and hydroxypropyl cellulose having a viscosity of 1000 mPa·s or more in a 2% by mass aqueous solution at 20°C.

[0065] Preferred thickeners are sodium alginate and xanthan gum, which improve the lubricity of the tablet surface when in contact with water, making the tablet easier to swallow. These thickeners may be used alone or in combination of two or more.

[0066] The viscosity of the thickener can be measured by the capillary viscometer method described in the 17th edition of the Japanese Pharmacopoeia.

[0067] The content of the thickener in the second film layer is not particularly limited, and is preferably, for example, 10% by mass or more and 50% by mass or less relative to the mass of the second film layer. The lower limit is more preferably 13% by mass or more, even more preferably 15% by mass or more, and particularly preferably 20% by mass or more. On the other hand, the upper limit is more preferably 47% by mass or less, even more preferably 45% by mass or less, and particularly preferably 40% by mass or less. By setting the content of the thickener in the second film layer within the above range, the swallowability of the tablet can be improved.

[0068] In one embodiment of the present invention, a film-coated tablet is preferred in which the content of inorganic salt in the first film layer is 20 to 55% by mass, and the content of thickener in the second film layer is 20 to 40% by mass. By controlling the content of inorganic salt in the first film layer and the content of thickener in the second film layer, the swallowability of the tablet and the effect of suppressing delay in disintegration time of uncoated tablets can be further improved.

[0069] In one embodiment of the present invention, the mass ratio of the inorganic salt contained in the first film layer to the thickener contained in the second film layer is preferably 1:1 to 4:1, more preferably 3:1, and even more preferably 4:1. By controlling the mass ratio of the content of the inorganic salt contained in the first film layer to the content of the thickener contained in the second film layer, the swallowability of the tablet and the effect of suppressing delay in disintegration time of the uncoated tablet can be further improved.

[0070] (Water-soluble film base for the second film layer) The water-soluble film base is a base in a composition for coating a plain tablet, and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of water-soluble film bases include cellulose derivatives, synthetic resins, polysaccharides, etc.

[0071] The viscosity of the water-soluble film base is not particularly limited, but a low-viscosity polymer that dissolves quickly in water is preferred. The viscosity of the water-soluble film base, for example, in a 2% by weight aqueous solution at 20°C, is preferably 0.1 mPa·s or more and 50 mPa·s or less. The lower limit is more preferably 1 mPa·s or more, even more preferably 2 mPa·s or more, and particularly preferably 3 mPa·s or more. Meanwhile, the upper limit is more preferably 45 mPa·s or less, even more preferably 40 mPa·s or less, and particularly preferably 35 mPa·s or less. The viscosity of the water-soluble film base can be measured by the capillary viscometer method described in the 17th Edition of the Japanese Pharmacopoeia, or the like.

[0072] Specific examples of water-soluble film bases include hydroxypropyl methylcellulose (viscosity of a 2% by weight aqueous solution at 20°C of 15 mPa·s or less), hydroxypropyl cellulose (viscosity of a 2% by weight aqueous solution at 20°C of 10 mPa·s or less), polyvinyl alcohol (viscosity of a 4% by weight aqueous solution at 20°C of 6 mPa·s or less), polyvinylpyrrolidone (average molecular weight of 40,000 or less), methylcellulose (viscosity of a 2% by weight aqueous solution at 20°C of 15 mPa·s or less), and pullulan (viscosity of a 10% by weight aqueous solution at 30°C of 15 to 180 mPa·s). Hydroxypropyl methylcellulose and hydroxypropyl cellulose are preferred water-soluble film bases due to their ease of availability and ease of coating. These water-soluble film bases may be used alone or in combination.

[0073] The content of the water-soluble film base in the second film layer is not particularly limited, and is preferably, for example, 30% by mass or more and 70% by mass or less relative to the mass of the second film layer. The lower limit is more preferably 33% by mass or more, even more preferably 35% by mass or more, and particularly preferably 40% by mass or more. On the other hand, the upper limit is more preferably 67% by mass or less, even more preferably 65% ​​by mass or less, and particularly preferably 60% by mass or less. By setting the content of the water-soluble film base in the second film layer within the above range, a tablet with excellent coatability can be obtained.

[0074] (Other ingredients) The second film layer may contain other components as needed in addition to the thickener and water-soluble film base, such as plasticizers, sweeteners, flavorings, colorants, and light protectants, as in the first film layer.

[0075] In order to maintain the function of the second film layer, which provides lubricity to the tablet surface and improves swallowability, and to effectively exert the function of the first film layer in the digestive tract, it is preferable not to incorporate inorganic salts such as potassium phosphate, sodium bicarbonate, and sodium chloride, which dissolve in water and react with thickeners, into the second film layer.

[0076] (Film coating method) Next, a method for coating a plain tablet having a first film layer with a second film layer will be described. The film coating method for uncoated tablets having a first film layer can be a method for producing film-coated tablets commonly used in the art. For example, uncoated tablets having a first film layer can be coated by loading the uncoated tablets having a first film layer into a film coating machine, dissolving and dispersing the components contained in the second film layer in an organic solvent such as water, ethanol, hexane, ethyl acetate, or isopropyl alcohol, or a mixture thereof, to prepare a coating liquid, spraying the uncoated tablets with the coating liquid, and drying the uncoated tablets.

[0077] With the above configuration, the second film layer containing a thickener can exert the effect of imparting lubricity to the tablet surface and improving the swallowability of the tablet.

[0078] [Uncoated tablets] The uncoated tablet contains an active ingredient, and the formulation of the uncoated tablet is not particularly limited as long as it does not affect the film layer. First, the components of the uncoated tablet will be described in detail.

[0079] (active ingredient) The active ingredient is not particularly limited as long as it exhibits efficacy and effect and is acceptable for use in pharmaceuticals, foods, etc. Examples of the active ingredient include medicinal ingredients and functional ingredients used in pharmaceuticals, quasi-drugs, over-the-counter drugs, herbal medicines, natural medicines, cosmetics, cosmetic materials, health foods, supplements, etc.

[0080] Specific examples of medicinal ingredients and functional ingredients include lipid regulators, antidiabetic agents, appetite suppressants, antihypertensive agents, vasodilators, β-adrenergic receptor blockers, cardiac ion channel agents, antiarrhythmic agents, anticoagulants, hemostatic agents, anti-inflammatory agents, analgesics, antiallergic agents, immunosuppressants, corticosteroids, steroids, antitumor agents, central nervous system function improving agents, sympathomimetic agents, parasympathomimetic agents, antimuscarinic agonists, dopaminergic agents, antidiarrheal agents, antiemetic agents, sedatives, astringents, tranquilizers, antidepressants, antiepileptics, antianxiety agents, hypnotics, stimulants, bronchodilators, antitussives, diuretics, muscle relaxants, bisphosphonates, antibiotics, antiviral agents, diagnostic agents, imaging diagnostic agents, radiopharmaceuticals, animal-derived substances, plant-derived substances, rapidine, nobiletin, sulforaphane, ampelo Examples of suitable ingredients include pusin, curcumins, resveratrols, geraniol, osajin, isoliquiritigenin, hydroxytyrosol, 25-hydroxycholecalciferol, coenzyme Q-10, S-adenosylmethionine, anthocyanin, ascorbic acid 2-glucoside, proteoglycan, N-acetylglucosamine, collagen, bilberry extract, carrot powder, gokahi, licorice, peony, cinnamon bark, fennel, scutellaria, bifidobacteria, lactic acid bacteria, yeast, vitamins such as vitamin A, vitamin B, and vitamin C, minerals such as calcium, magnesium, and iron, dietary fiber such as polydextrose, fatty acids, polyphenols, proteins, amino acids, oligosaccharides, lecithin, carotenoids, and chlorophyll. These medicinal and functional ingredients may be formulated alone or in combination of two or more.

[0081] (Other ingredients) In addition to the active ingredient, the uncoated tablet may contain additives as needed, such as excipients, binders, disintegrants, lubricants, stabilizers, preservatives, and colorants.

[0082] Adding an excipient to a core tablet can adjust the bulk of the core tablet, making it easier to take the tablet. The excipient adjusts the bulk of the core tablet and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of excipients include sugars, phosphates, sulfates, etc.

[0083] Specific examples of excipients include crystalline cellulose, lactose, sucrose, mannitol, glucose, starch, calcium phosphate, etc. These excipients may be used alone or in combination of two or more.

[0084] Adding a binder to a core tablet imparts binding strength to the powder components, allowing the production of a stable solid formulation. The binder increases the binding strength of the powder components and imparts tablet hardness, and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of binders include cellulose derivatives, synthetic resins, sugars, polyethers, waxes, etc.

[0085] Specific examples of binders include carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid, polymethacrylic acid, glucose, sucrose, lactose, maltose, dextrin, sorbitol, mannitol, polyethylene glycol, paraffin, gum arabic, gelatin, agar, starch, pullulan, etc. These binders may be blended alone or in combination of two or more.

[0086] The addition of a disintegrant can promote disintegration of the tablet and improve absorbability. The disintegrant disintegrates the tablet by increasing water absorption, and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of disintegrants include sugars, cellulose derivatives, synthetic resins, alginates, etc.

[0087] Specific examples of disintegrants include corn starch, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose calcium, crystalline cellulose, croscarmellose sodium, carboxymethyl starch sodium, crospovidone, sodium starch glycolate, etc. These disintegrants may be blended alone or in combination of two or more.

[0088] Addition of a lubricant can prevent tableting problems such as sticking during tablet production. The lubricant reduces the adhesive force of powder components to increase fluidity, and is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, etc. Examples of lubricants include phyllosilicate mineral powder, silicon oxide, saturated fatty acids, esters, waxes, hydrogenated vegetable oils, fats, polyethers, etc.

[0089] Specific examples of lubricants include talc, light anhydrous silicic acid, magnesium stearate, calcium stearate, magnesium carbonate, sodium benzoate, palmitic acid, sodium stearyl fumarate, sucrose fatty acid esters, beeswax, hardened soybean oil, cacao butter, polyethylene glycol, etc. These lubricants may be blended alone or in combination of two or more.

[0090] The addition of a stabilizer can prevent the active ingredient from being deactivated. The stabilizer is not particularly limited as long as it prevents the chemical and physical decomposition of the active ingredient and is acceptable for use in pharmaceuticals, foods, etc. Examples of stabilizers include inorganic compounds, organic acids, organic acid salts, and vitamins.

[0091] Specific examples of stabilizers include sodium hydrogen sulfite, ascorbic acid, sodium edetate, tocopherol, etc. These stabilizers may be used alone or in combination of two or more.

[0092] Addition of a preservative can prevent the tablet from being contaminated by microorganisms. There are no particular limitations on the preservative, as long as it inhibits the growth of microorganisms and is acceptable for use in pharmaceuticals, foods, etc. Examples of preservatives include benzoates and parahydroxybenzoic acid esters.

[0093] Specific examples of preservatives include sodium benzoate, propyl parahydroxybenzoate, methylparaben, propylparaben, etc. These preservatives may be used alone or in combination of two or more.

[0094] The addition of a colorant can color the tablet and enhance the palatability and distinguishability of the coated solid preparation. The colorant is not particularly limited as long as it improves the palatability and distinguishability of the tablet and is acceptable for use in pharmaceuticals, foods, etc. Examples of colorants include natural dyes and synthetic dyes.

[0095] Specific examples of coloring agents include cochineal, carmine, curcumin, riboflavin, annatto, titanium oxide, yellow ferric oxide, ferric oxide, talc, calcined silica, magnesium carbonate, and synthetic food colorings such as Food Blue No. 1, Food Blue No. 2, Food Yellow No. 4, Food Yellow No. 5, Food Green No. 3, Food Red No. 2, Food Red No. 3, Food Red No. 102, Food Red No. 104, Food Red No. 105, and Food Red No. 106. These coloring agents may be blended alone or in combination of two or more.

[0096] Examples of other additives include solubilizers, surfactants, emulsifiers, antioxidants, glossing agents, foaming agents, moisture-proofing agents, preservatives, fluidizing agents, sweeteners, flavoring agents, refreshing agents, flavoring agents, fragrances, aromatics, disintegration aids, etc. These additives may be blended alone or in combination of two or more.

[0097] Next, a method for producing uncoated tablets will be described. A conventional method used in this technical field can be used for producing uncoated tablets. In the production process of uncoated tablets, a mixture of active ingredients and additives may be directly compressed into tablets, or the active ingredients and additives may be granulated and then compressed into tablets.

[0098] The granulation method is not particularly limited, and examples thereof include dry granulation and wet granulation. More specifically, examples thereof include fluidized bed granulation, tumbling granulation, stirring granulation, and spray granulation.

[0099] The mixer used in the mixing step is not particularly limited, and examples thereof include a tumbler mixer, a V-type mixer, a double-cone mixer, an infinite mixer, etc. The tablet press used in the tableting step is not particularly limited, and examples thereof include a single punch tablet press and a rotary tablet press.

[0100] With the above-mentioned configuration, the uncoated tablet can contain various active ingredients, making it possible to provide a film-coated tablet with a wide range of efficacy and effects.

[0101] [Applications of film-coated tablets] The uses of film-coated tablets are described in detail below. The uses of film-coated tablets are not particularly limited, and examples thereof include pharmaceuticals, quasi-drugs, drinkable cosmetics, drinkable cosmetics, health foods (nutritional supplements, functional foods, foods for the sick, foods for specified health uses, foods with functional claims, etc.), supplements, etc.

[0102] Due to the above-mentioned configuration, film-coated tablets can demonstrate high versatility. [Example]

[0103] Hereinafter, examples of the present invention will be described, but the present invention is not limited to these examples, and various modifications are possible within the technical concept of the present invention.

[0104] (Preparation of test samples) [Test Example 1] Uncoated tablets were prepared without a granulation process as follows: 6480 g of lactose (Tablettose 80, Meigle Japan Co., Ltd.), 1040 g of microcrystalline cellulose (Ceolas PH101, Asahi Kasei Corporation), 400 g of hydroxypropyl cellulose (HPC-L, Nippon Soda Co., Ltd.), and 80 g of magnesium stearate (Partec, Merck Ltd.) were mixed in a mixer (TBM-25, Tokuju Kosakusho Co., Ltd.) to form a mixture.

[0105] The mixture was compressed using a rotary tableting machine (HT-AP15, Hata Iron Works Co., Ltd.) under a compression pressure of 880 kg to produce uncoated tablets with a diameter of 8 mm, a thickness of 4.9 mm, and a weight of 260 mg.

[0106] Film-coated tablets were prepared as in Examples 1 to 11 below.

[0107] [Example 1] To a mixed liquid consisting of 39.83 parts by mass of absolute ethanol and 48.13 parts by mass of purified water, 0.84 parts by mass of glycerin fatty acid ester (Mybasset 9-45K, Koyo Shokai Co., Ltd.), 6.66 parts by mass of sodium chloride (special grade, Fujifilm Wako Pure Chemical Industries, Ltd.), and 5.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a first coating liquid.

[0108] To a mixture consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol (Sorbitol FP, Bussan Food Science Co., Ltd.), 0.38 parts by mass of acesulfame potassium (Sunet D, MC Food Specialties Co., Ltd.), 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc (Crown Talc Pharmacopoeia PP, Kihara Chemical Co., Ltd.), and 6.00 parts by mass of sodium alginate (Kimica Algin I-8-270, Kimica Co., Ltd.) were added, dissolved, and dispersed to prepare a second coating liquid.

[0109] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0110] [Example 2] As in Example 1, the first coating liquid was coated up to 4 parts by mass in terms of solid content per 100 parts by mass of the uncoated tablets of Test Example 1. Next, the second coating liquid was coated up to 2 parts by mass in terms of solid content per 100 parts by mass of the uncoated tablets.

[0111] [Example 3] As in Example 1, the first coating liquid was coated up to 6 parts by mass in terms of solid content per 100 parts by mass of the uncoated tablets of Test Example 1, and then the second coating liquid was coated up to 2 parts by mass in terms of solid content per 100 parts by mass of the uncoated tablets.

[0112] [Example 4] To a mixed liquid consisting of 39.83 parts by mass of absolute ethanol and 48.13 parts by mass of purified water, 0.84 parts by mass of glycerin fatty acid ester (Mybasset 9-45K, Koyo Shokai Co., Ltd.), 2.50 parts by mass of sodium bicarbonate (special grade, Fujifilm Wako Pure Chemical Industries, Ltd.), and 9.16 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a first coating liquid.

[0113] To a mixture consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol (Sorbitol FP, Bussan Food Science Co., Ltd.), 0.38 parts by mass of acesulfame potassium (Sunet D, MC Food Specialties Co., Ltd.), 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc (Crown Talc Pharmacopoeia PP, Kihara Chemical Co., Ltd.), and 6.00 parts by mass of sodium alginate (Kimica Algin I-8-270, Kimica Co., Ltd.) were added, dissolved, and dispersed to prepare a second coating liquid.

[0114] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0115] [Example 5] To 87.51 parts by mass of purified water, 0.84 parts by mass of polyethylene glycol 6000 (Macrogol 6000R, NOF Corporation), 6.66 parts by mass of sodium bicarbonate (special grade, Fujifilm Wako Pure Chemical Industries, Ltd.), and 5.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a first coating liquid. A second coating liquid was prepared in the same manner as in Example 4.

[0116] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0117] [Example 6] To a mixed liquid consisting of 39.83 parts by mass of absolute ethanol and 48.13 parts by mass of purified water, 0.84 parts by mass of glycerin fatty acid ester (Mybasset 9-45K, Koyo Shokai Co., Ltd.), 6.66 parts by mass of potassium dihydrogen phosphate (special grade, Fujifilm Wako Pure Chemical Industries, Ltd.), and 5.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a first coating liquid.

[0118] To a mixture consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol (Sorbitol FP, Bussan Food Science Co., Ltd.), 0.38 parts by mass of acesulfame potassium (Sunet D, MC Food Specialties Co., Ltd.), 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc (Crown Talc Pharmacopoeia PP, Kihara Chemical Co., Ltd.), and 6.00 parts by mass of sodium alginate (Kimica Algin I-8-270, Kimica Co., Ltd.) were added, dissolved, and dispersed to prepare a second coating liquid.

[0119] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 4 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0120] [Example 7] As in Example 5, the first coating liquid was sprayed to coat 100 parts by mass of the uncoated tablets of Test Example 1 to 4 parts by mass in terms of solid content. Next, 100 parts by mass of the uncoated tablets of Test Example 1 were sprayed to coat 4 parts by mass in terms of solid content.

[0121] [Example 8] To 87.51 parts by mass of purified water, 0.84 parts by mass of polyethylene glycol 6000 (Macrogol 6000R, NOF Corporation), 6.66 parts by mass of sodium bicarbonate (special grade, Fujifilm Wako Pure Chemical Industries, Ltd.), and 5.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a first coating liquid.

[0122] To a mixture consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol (Sorbitol FP, Bussan Food Science Co., Ltd.), 0.38 parts by mass of acesulfame potassium (Sunet D, MC Food Specialties Co., Ltd.), 9.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc (Crown Talc Pharmacopoeia PP, Kihara Chemical Co., Ltd.), and 3.00 parts by mass of sodium alginate (Kimica Algin I-8-270, Kimica Co., Ltd.) were added, dissolved, and dispersed to prepare a second coating liquid.

[0123] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0124] [Example 9] A first coating liquid for Example 5 was prepared. To a mixed liquid consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol (Sorbitol FP, Bussan Food Science Co., Ltd.), 0.38 parts by mass of acesulfame potassium (Sunet D, MC Food Specialties Co., Ltd.), 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc (Crown Talc Pharmacopoeia PP, Kihara Chemical Co., Ltd.), and 6.00 parts by mass of xanthan gum (Glinted Xanthan 200, Danicos Japan Co., Ltd.) were added, dissolved, and dispersed to prepare a second coating liquid.

[0125] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0126] [Comparative Example 1] To a mixture of 39.83 parts by mass of absolute ethanol and 48.13 parts by mass of purified water, 0.84 parts by mass of glycerin fatty acid ester and 11.66 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) were added, dissolved, and dispersed to prepare a coating liquid. 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the coating liquid was spray coated onto the tablets up to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0127] Comparative Example 2 To a mixed liquid consisting of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water, 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol, 0.38 parts by mass of acesulfame potassium, 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.), 0.12 parts by mass of talc, and 6.00 parts by mass of sodium alginate were added, dissolved, and dispersed to prepare a coating liquid.

[0128] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the coating liquid was spray coated onto the tablets up to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0129] Comparative Example 3 A first coating liquid was prepared by dissolving and dispersing 0.84 parts by mass of glycerin fatty acid ester and 11.66 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) in a mixture of 39.83 parts by mass of absolute ethanol and 48.13 parts by mass of purified water. A second coating liquid was prepared by dissolving and dispersing 1.00 parts by mass of glycerin fatty acid ester, 1.50 parts by mass of sorbitol, 0.38 parts by mass of acesulfame potassium, 6.00 parts by mass of hydroxypropyl cellulose (HPC-SSL, Nippon Soda Co., Ltd.) in a mixture of 75.40 parts by mass of absolute ethanol and 9.60 parts by mass of purified water.

[0130] 150 g of the uncoated tablets obtained in Test Example 1 were placed in a drum tablet coating machine (DRC-200 model, Powrex Corporation), and the first coating liquid was spray-coated to 4 parts by mass in solid content per 100 parts by mass of the uncoated tablets. Next, the second coating liquid was spray-coated to 2 parts by mass in solid content per 100 parts by mass of the uncoated tablets.

[0131] (Disintegration test) The disintegration test was carried out on the test sample in accordance with the disintegration test method described in the 17th edition of the Japanese Pharmacopoeia (water, 37±2°C, with an auxiliary plate). The disintegration time of the tablet is preferably as small as possible compared to that of the uncoated tablet, for example, within 20 minutes, more preferably within 10 minutes.

[0132] (Tablet slipperiness test) A schematic diagram of the tablet slippage test method is shown in Figure 2. As shown in Figure 2, the tablet slippage test involves placing a tablet 22 in a silicone tube 20, fixing it in place, then pouring 50 μL of water into the tube and leaving it to stand for 2 minutes. Then, using a small benchtop testing machine (EZ-SX type 50N, manufactured by Shimadzu Corporation) between fixing pins 24 placed at 4 mm intervals, the pulling stress in the direction indicated by the arrow on the silicone tube 20 (SKSQ-0828, manufactured by Fuso Rubber Industries Co., Ltd.) is measured.

[0133] The lower the pulling stress of a tablet is, the more preferable the slipperiness of the tablet is, compared with a tablet of the same shape that does not have slipperiness imparted thereto.

[0134] (result) Next, the results of the disintegration test and tablet sliding property test for each test example, each example, and each comparative example are shown in Tables 1 to 4. The unit of each component amount in the tables is mg. Each value is rounded to two decimal places and expressed to one decimal place.

[0135] [Table 1]

[0136] Table 1 shows the results for the test sample in which the first film layer did not contain an inorganic salt. As shown in Table 1, a comparison of Comparative Examples 1 and 3 revealed that the incorporation of sodium alginate in the film layer, which is the outer layer, improved the slipperiness of the tablet. Furthermore, a comparison of Comparative Examples 2 and 3 revealed that when a film layer containing sodium alginate was provided, a clear delay in disintegration time was observed compared to that of the plain tablet (Test Example 1) in Comparative Example 2, which did not have a film layer, which was the inner layer, and Comparative Example 3, which did not contain an inorganic salt in the first film layer.

[0137] [Table 2]

[0138] Table 2 shows the results for test samples containing an inorganic salt in the first film layer and a thickener in the second film layer. As shown in Table 2, when Examples 1 to 5 are compared with Comparative Examples 1 to 3 in Table 1, in film-coated tablets containing sodium alginate as a thickener in the second film layer, the addition of sodium chloride or sodium bicarbonate as an inorganic salt in the first film layer significantly reduced the delay in disintegration time. Furthermore, it was found that the slipperiness of the film-coated tablets of Examples 1 to 5 was significantly improved.

[0139] [Table 3]

[0140] Table 3 shows the results for test samples containing an inorganic salt in the first film layer and a thickener in the second film layer. As shown in Table 3, when Examples 6 to 9 are compared with Comparative Examples 1 to 3 in Table 1, in film-coated tablets containing sodium alginate and xanthan gum as thickeners in the second film layer, the addition of potassium phosphate and sodium bicarbonate as inorganic salts in the first film layer significantly reduced the delay in disintegration time. Furthermore, the film-coated tablets of Examples 6 to 9 were found to have significantly improved slipperiness.

[0141] From the above, it became clear that by incorporating an inorganic salt in the first film layer (the inner layer) and a thickener in the second film layer (the outer layer) of a film-coated tablet, the delay in disintegration time can be significantly suppressed and the slipperiness of the tablet can also be greatly improved.

[0142] Although the present invention has been described in detail and with reference to specific embodiments, it will be apparent to those skilled in the art that various modifications and variations can be made without departing from the spirit and scope of the present invention. This application is based on a Japanese patent application (Patent Application No. 2020-120267) filed on July 13, 2020, the entire contents of which are incorporated by reference. [Industrial Applicability]

[0143] The present invention provides film-coated tablets with improved disintegration time that can be used for pharmaceuticals, quasi-drugs, drinkable cosmetics, drinkable cosmetics, health foods (nutritional supplements, functional nutritional foods, foods for the sick, foods for specified health uses, foods with functional claims, etc.), and supplements.

Claims

1. Tablets and a first film layer coating the tablet and containing an inorganic salt; a second film layer that coats the tablet coated with the first film layer and contains a thickener; the inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and sodium chloride; the thickener contained in the second film layer is at least one selected from the group consisting of sodium alginate and xanthan gum; the content of the inorganic salt in the first film layer is 20 to 55 mass %, the content of the thickener in the second film layer is 20 to 40% by mass, The first film layer is 2 to 6 parts by mass per 100 parts by mass of the uncoated tablet, and the second film layer is 2 to 4 parts by mass per 100 parts by mass of the uncoated tablet.

2. Tablets and a first film layer covering the tablet; A film-coated tablet comprising: a second film layer that is coated on the outside of the first film layer and contains a thickener; the first film layer contains an inorganic salt, and the inorganic salt reduces the viscosity of the thickener contained in the second film layer; the inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and sodium chloride; the thickener contained in the second film layer is at least one selected from the group consisting of sodium alginate and xanthan gum; the content of the inorganic salt in the first film layer is 20 to 55 mass %, the content of the thickener in the second film layer is 20 to 40% by mass, The first film layer is 2 to 6 parts by mass per 100 parts by mass of the uncoated tablet, The film-coated tablet, wherein the second film layer is 2 to 4 parts by mass per 100 parts by mass of the plain tablet.

3. Tablets and a first film layer covering the tablet; A film-coated tablet comprising: a second film layer that is coated on the outside of the first film layer and contains a thickener; the first film layer contains an inorganic salt and a water-soluble film base having a viscosity of 100 mPa·s or less in a 2% by mass aqueous solution at 20°C; the inorganic salt contained in the first film layer is at least one selected from the group consisting of potassium phosphate, sodium bicarbonate, and sodium chloride; the thickener contained in the second film layer is at least one selected from the group consisting of sodium alginate and xanthan gum; the content of the inorganic salt in the first film layer is 20 to 55 mass %, the content of the thickener in the second film layer is 20 to 40% by mass, The first film layer is 2 to 6 parts by mass per 100 parts by mass of the uncoated tablet, The film-coated tablet, wherein the second film layer is 2 to 4 parts by mass per 100 parts by mass of the plain tablet.

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