JP2018158917A - Tablet and method for producing tablet - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a tablet that is easy to swallow and also has reduced production cost, and a method of producing the same.SOLUTION: A tablet has a naked tablet containing a gelator, and at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch decomposition product. Preferably, the gelator is at least one selected from xanthan gum, locust bean gum, guar gum, mannan, glucomannan, hyaluronan, agar, alginic acid, tamarind gum, psyllium seed gum, tara gum, carrageenan, acacia gum, gum arabic, ghatti gum, tragacanth gum, karaya gum, cassia gum, rhamsan gum, welan gum, macrophomopsis gum, curdlan, pullulan, gellan gum, pectin, and soybean polysaccharide, gelatin, collagen, polyglutamic acid, polylactic acid, polyglutamic acid and the like.SELECTED DRAWING: None

Description

  The present invention relates to a tablet and a method for producing the tablet.

With the recent increase in consumer health orientation and the introduction of the functional labeling food system as a new food labeling system, the market for Japanese health foods and supplements is expected to expand in the future. The Of these supplements, tablets are often used as preparations for oral administration, but taking large tablets or multiple tablets at the same time is especially useful for people who are not good at drinking tablets, especially for children and elderly people with low swallowing function. Often difficult.
In order to make the tablet easy to swallow, it is required to improve the slipperiness of the tablet and the difficulty of being caught on the throat. In view of this point, a plurality of techniques that devise coating of solid agents such as tablets have been reported so far (Patent Documents 1 to 3). However, even though the tablet surface becomes slippery due to the coating and the dosage is improved to some extent, the resistance when passing through the pharynx having a complicated shape is still large, and the effect of improving swallowing is not sufficient.

Japanese Patent Laid-Open No. 11-60472 Special table 2011-502132 gazette Special table 2014-534777 gazette

  An object of the present invention is to provide a tablet that can be easily taken with little resistance even for people who are not good at drinking tablets. In addition, the tablet having a coating that is a conventional technique is easily increased in volume due to the coating layer, and the tablet surface is coated after tableting, which requires labor and manufacturing cost. An object of the present invention is to provide a tablet that prevents the enlargement of the tablet and that is easy to swallow and reduces the manufacturing cost.

The present invention includes a gelling agent,
It is intended to provide a tablet having a core tablet containing at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product.

  The present invention is also a method for producing the tablet, wherein the gelling agent is selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product. The present invention provides a method for producing a tablet having a core tablet, which compresses a raw material powder containing the above.

The tablet having the naked tablet of the present invention is elastic when the naked tablet part comes into contact with saliva or ingested water (hereinafter referred to as a liquid medium such as water). It is characterized in that a slimy sensation is generated on the surface of a tablet having a lip, and is excellent in ease of swallowing. Here, a liquid medium such as water means water, tea, soft drinks, milk and other aqueous liquids used for normal drinking, saliva, or a mixture thereof. In addition, since the entire tablet surface is not covered with the coating layer, the tablet having the bare tablet of the present invention can reduce the manufacturing cost and prevent the tablet from becoming large. Furthermore, the tablet having the bare tablet of the present invention is excellent in ease of disintegration after ingestion.
Moreover, the manufacturing method of the tablet which has a naked tablet of this invention can manufacture the tablet which has a naked tablet of this invention by an industrially advantageous method.

FIG. 1 is a conceptual diagram of a maximum stress measurement method. FIG. 2 is an electromyogram when only water is taken. FIG. 3 is an electromyogram when the tablets produced in Example 1 are taken. FIG. 4 is an electromyogram when the tablet produced in Example 2 is taken.

  Hereinafter, the present invention will be described based on preferred embodiments thereof.

  The tablet of the present invention includes a gelling agent and one or more selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product. Have a bare tablet. In general, a bare tablet (also referred to as an uncoated tablet) refers to a tablet having no coating layer formed on the surface thereof. In the specification of the present application, the “tablet having a core tablet” means a tablet in which there is a part where a coating layer is not formed on the surface of the tablet and the part is in a state of a core tablet (hereinafter referred to as the tablet surface). The part where the coating layer is not formed is called a bare tablet part). In the specification of the present application, the “bare tablet” means a tablet having a coating layer substantially not formed on the surface (a tablet having an area ratio of less than 5% covered by the coating layer in the surface area of the tablet). To do. In the present specification, “naked tablet” is a concept encompassed by “tablet having a bare tablet”.

  The tablet having a core tablet of this embodiment exhibits sliminess (also referred to as slipperiness) when a liquid medium such as water comes into contact with the core tablet portion. It is preferable that the tablet which has a naked tablet of this embodiment has a gelatinizer in the outermost surface part of a naked tablet part. The outermost surface portion refers to a portion located on the surface side in the core tablet portion, and refers to a range of 0 mm or more and 1 mm or less from the surface of the core tablet portion toward the center. The tablet of this embodiment has a gelling agent on the outermost tablet portion, particularly the outermost surface portion of the uncoated tablet portion, so that the surface of the uncoated tablet portion is slimmed when contacted with a liquid medium such as water. As a result, the tablet having the uncoated tablet of this embodiment is easy to swallow without providing a coating layer. The tablet having a core tablet particularly preferably has a gelling agent on the entire outermost surface portion of the core tablet portion. In this specification, if it can confirm that a gelatinizer exists in two or more different places in the outermost surface part of a nude tablet part, it can be said that it has a gelatinizer in the whole outermost surface part of a nude tablet part. Here, the presence of the gelling agent in the surface portion can be confirmed by scraping about 30 mg of an arbitrary portion of the outermost surface portion with a knife or the like, and adding an appropriate amount of a liquid medium such as water for gelation. As will be described later, a tablet having a core tablet having a gelling agent on the entire outermost surface portion of the core tablet part is easily obtained as a tablet mixture of mixed powder containing the gelling agent and a specific excipient. be able to.

  Since the tablet having the core tablet of the present invention exhibits the effect of the gelling agent due to the presence of the core tablet portion, it is preferable that the core tablet portion exists on the outermost surface of the tablet. Specifically, the ratio of the surface area occupied by the bare tablet portion on the outermost surface of the tablet is preferably 70% or more, more preferably 90% or more, and particularly preferably 95% or more. Further, when the tablet having the core tablet of the present invention has a coating layer, the ratio of the tablet surface area covered by the coating layer is preferably less than 30%, particularly preferably less than 10%, substantially Most preferably, there is no coating layer (meaning that the proportion of the area covered by the coating layer to the surface area of the tablet is less than 5%). Moreover, when the tablet which has a naked tablet of this invention has a coating layer, 3 mm or less is preferable toward the center direction from the surface of a naked tablet part, 2 mm or less is more preferable, and 1 mm or less is especially preferable. By making the thickness of the coating layer 1 mm or less, the effect of the gelling agent can be easily exhibited, the manufacturing cost can be reduced, and further the enlargement of the tablet can be prevented. When the coating layer covers only a part of the tablet, the coating layer may be continuously present in a partial manner, or may be dispersed in an island shape or the like. For example, if a coating layer is present on a part of the surface of the tablet by spraying a powdered material other than the gelling agent (such as sugars or other seasonings) on the surface of the naked tablet, It can be tolerated because of the effect of the gelling agent present.

  The tablet having a core tablet may have a structure in which the surface portion and the portion on the center side are distinguished from each other, or may not have such a structure. For example, a tablet having a core tablet may have a multilayer structure such as a dry-coated tablet. Especially, when the tablet which has a naked tablet does not have a multilayer structure but is a single layer structure, it is preferable at points, such as ease of manufacture.

1. Gelling agent Tablets with bare tablets have a gelling agent. In the present invention, it is preferable to have a gelling agent on the outermost surface part of the tablet having a bare tablet, but it may have a gelling agent in a place other than the outermost surface part. For example, a tablet having a core tablet may contain a gelling agent in both the outermost surface portion and a portion closer to the center (also referred to as a center portion). An example of a tablet having such a core tablet is a tablet having a single layer structure. In the tablet having a core tablet, the composition of the outermost surface part and the composition of the center part may be the same or different, but the same is preferable from the viewpoint of easy manufacture of the tablet having the core tablet. The presence of a gelling agent in the center of a tablet having a core tablet means that, for example, the tablet having a core tablet is cut in half with a cutter, etc. It is possible to confirm by removing about 30 mg of this part with a scalpel or the like and adding an appropriate amount of a liquid medium such as water to gel. In addition, the component listed as a disintegrating agent mentioned later is not contained in the gelling agent in this application.

As the gelling agent, a substance that is powdery (particulate) and exhibits sliminess when containing a liquid medium such as water is used. Gelling agents include xanthan gum, locust bean gum, guar gum, mannan, glucomannan, hyaluronic acid, agar, alginic acid, tamarind gum, psyllium seed gum, tara gum, carrageenan, acacia gum, gum arabic, gati gum, tragacanth gum, caraya gum, cassia gum Natural polysaccharides such as lambzan gum, welan gum, macrohomopsis gum, curdlan, pullulan, gellan gum (deacylated gellan gum, native gellan rum), pectin, and soy polysaccharide; proteolytic products such as collagen; Examples include amino acids; biopolymers such as polylactic acid and polyglutamic acid, and salts and derivatives thereof. Of these, natural polysaccharides are particularly preferred.
Examples of the derivatives include hyaluronic acid derivatives, alginic acid derivatives and polyglutamic acid derivatives. Examples of the salt include alginates, hyaluronates, polyglutamates, and the like. Examples of hyaluronic acid derivatives include hyaluronic acid esters and acetylated hyaluronic acid. Examples of alginic acid derivatives include alginic acid esters. Examples of polyglutamic acid derivatives include polyglutamic acid esters. Examples of the alginate include sodium alginate, potassium alginate, ammonium alginate and calcium alginate. Examples of hyaluronic acid salts include sodium hyaluronate and potassium hyaluronate. Examples of polyglutamate include sodium polyglutamate and potassium polyglutamate. Only one gelling agent may be used alone, or two or more gelling agents may be used in combination.

  In this embodiment, the gelling agent is locust bean gum, mannan, glucomannan, hyaluronic acid, agar, tamarind gum, psyllium seed gum, tara gum, cassia gum, gum arabic, gati gum, tragacanth gum, karaya gum, cassia gum, lamb zan gum, welan gum, The inclusion of one or more selected from macrohomopsis gum, curdlan, pullulan, gellan gum, polyamino acid, polylactic acid, and salts and derivatives thereof (hereinafter also referred to as a specific gelling agent) disintegrates in the body. It is preferable in terms of easyness, and in particular, it is preferable to contain locust bean gum because it is easy to disintegrate after ingestion and also exhibits both high disintegration and slimming properties.

  It is also preferable to combine two or more gelling agents from the viewpoint of achieving both disintegration and slimming properties, and from the viewpoint of manufacturability, and a specific gelling agent and a gelling agent other than the specific gelling agent are combined. More preferably. Specifically, it is preferable to combine locust bean gum, which is a specific gelling agent, and xanthan gum, guar gum, alginic acid, carrageenan, etc., which are gelling agents other than the specific gelling agent. For example, by combining locust bean gum with xanthan gum or guar gum, the ease of swallowing due to a slimy feeling can be effectively enhanced. Moreover, by combining locust bean gum with guar gum, a tablet excellent in disintegration in the body after ingestion can be obtained.

  In the tablet having a bare tablet, the ratio of the gelling agent is preferably 0.01% by mass or more in order to sufficiently produce a slimy feeling when contacted with a liquid medium such as water. Further, the ratio of the gelling agent in the tablet having a bare tablet is preferably 70% by mass or less from the viewpoint of easiness of elution of the active ingredient. From these points, in the tablet having a core tablet, the ratio of the gelling agent is more preferably 0.1% by mass or more and 60% by mass or less, and further preferably 1% by mass or more and 50% by mass or less. It is still more preferably 3% by mass or more and 30% by mass or less, and most preferably 5% by mass or more and 20% by mass or less. When the tablet having a core tablet of this embodiment contains at least one selected from the specific gelling agent in the tablet having a core tablet, the total mass of the specific gelling agent in the tablet having the core tablet As a preferred range, the same range as the preferred range of the gelling agent is mentioned. Here, the total mass of at least one selected from the specific gelling agent refers to the mass of one type when a tablet having a bare tablet contains only one selected from the specific gelling agent. Yes, if a tablet having a bare tablet contains two or more of these, the total mass is the same.

  When the tablet having the core tablet of the present invention contains a specific gelling agent and another gelling agent, the ratio of the specific gelling agent in the tablet having the core tablet: the other gelling agent is From the viewpoint of both sliminess and disintegration, the former is preferably 10 parts by mass or more and 1000 parts by mass or less, and more preferably 15 parts by mass or more and 900 parts by mass or less, with respect to 100 parts by mass of the latter. The amount is particularly preferably 20 parts by mass or more and 800 parts by mass or less.

  For example, when the tablet having a core tablet of the present invention contains xanthan gum and locust bean gum, the ratio of the former: the latter of the tablet having a core tablet increases the slimeness and the content of the active ingredient. More preferably, the locust bean gum is from 10 parts by weight to 1000 parts by weight, more preferably from 15 parts by weight to 900 parts by weight, and more preferably from 20 parts by weight to 800 parts by weight with respect to parts by weight. Is particularly preferred.

  Further, when the tablet having a bare tablet of the present invention contains guar gum and locust bean gum, the ratio of the former: the latter of the tablet having a bare tablet increases the slimeness and the content of the active ingredient. More preferably, the locust bean gum is 10 parts by weight or more and 1000 parts by weight or less, more preferably 15 parts by weight or more and 900 parts by weight or less, and more preferably 20 parts by weight or more and 800 parts by weight or less. Is particularly preferred.

2. Specific excipients Tablets having uncoated tablets are one or more selected from sugar alcohols, monosaccharides, disaccharides, oligosaccharides, cellulose, cellulose derivatives, starch, starch derivatives and starch degradation products (hereinafter these are specified) (Also referred to as an excipient). By combining the gelling agent and these specific excipients, tablets with excellent sliminess and short disintegration time can be obtained.

  As described above, the tablet having a bare tablet may contain at least one selected from monosaccharides, disaccharides, oligosaccharides, cellulose, cellulose derivatives, starch, starch derivatives, and starch degradation products, but is disintegratable. It is preferable that two or more components belonging to different categories are included in combination in order to achieve both balance and sliminess. Specific examples include a combination of disaccharide and cellulose, a combination of disaccharide and reduced maltose, and a combination of disaccharide and starch. Further, it is more preferable to include a combination of three or more components belonging to different categories. Specifically, for example, a combination of disaccharide, starch and cellulose, a combination of disaccharide, reduced maltose and cellulose and the like can be mentioned.

  Examples of sugar alcohols include monosaccharide alcohols, disaccharide alcohols, and trisaccharide or higher alcohols. Examples of monosaccharide alcohols include tetritol such as erythritol, D-threitol and L-threitol, pentitol such as D-arabinitol and xylitol, D-iditol, galactitol (dulcitol), D-glucitol (sorbitol) and the like. Cyclitols such as hexitol and inositol, mannitol, boremitol, ribitol, perseitol, D-erythro-D-galacto-octitol and the like. Examples of the disaccharide alcohol include reduced maltose (maltitol), lactitol, reduced palatinose (isomalt) and the like. Examples of the trisaccharide or higher alcohol include maltotriitol, isomaltotriitol, panitol and the like. The sugar alcohol is preferably at least one selected from disaccharide alcohols from the viewpoint of manufacturability such as obtaining the hardness of a tablet that has been compressed, and in particular, at least one selected from reduced maltose and reduced palatinose. Preferably it is a seed.

  Examples of monosaccharides include glucose, galactose, fructose, and mannose. Among these, glucose is preferable in terms of easy availability and compatibility between disintegration and sliminess.

  Examples of the disaccharide include sucrose, maltose, lactose (lactose), trehalose, tulanose, and cellobiose. Among these, at least one selected from trehalose, sucrose, and maltose is preferable from the viewpoint of both disintegration and sliminess, and sucrose and maltose are more preferable. Even when lactose is included, the effects of the present invention can be obtained. However, from the viewpoint of achieving both disintegration and sliminess, the disaccharide is more preferably a disaccharide other than lactose.

  Examples of oligosaccharides include trisaccharides to 20 sugars, preferably trisaccharides to 10 sugars, more preferably trisaccharides to 6 sugars, specifically, raffinose, maltotriose, Examples include melezitose, gentianose, acarbose, stachyose, galactooligosaccharide, fructooligosaccharide, mannan oligosaccharide, isomaltoligosaccharide (isomaltotriose, panose), xylooligosaccharide, soybean oligosaccharide, nigerooligosaccharide, and whey oligosaccharide. In particular, it is preferable to use isomaltoligosaccharides or fructooligosaccharides in terms of easy availability and compatibility between disintegration and sliminess.

  A tablet having a bare tablet preferably contains any of monosaccharides, disaccharides and oligosaccharides from the viewpoint of masking the taste and promoting the secretion of saliva. In particular, it is preferable to contain these sugars in the surface portion of a tablet having a core tablet.

  Examples of cellulose include powdered cellulose and crystalline cellulose. Crystalline cellulose is obtained by partially depolymerizing and purifying α-cellulose obtained as a pulp from a fibrous plant with an acid. For example, those corresponding to crystalline cellulose described in the 15th revision Japanese Pharmacopoeia Manual (published by Yodogawa Shoten) can be mentioned. Crystalline cellulose can be classified into crystalline cellulose powder and crystalline cellulose composite, and any of these can be used for the tablet having the bare tablet of the present invention.

  Examples of cellulose derivatives include carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, and methylcellulose. Carboxymethyl cellulose having a degree of etherification of 0.2 mol / C6 to 1.0 mol / C6 is preferred from the viewpoint of easy availability and coexistence of sliminess and disintegration time, and 0.5 mol / C6 to 0. More preferred is 8 mol / C6. The effect of the present invention can be obtained even when croscarmellose sodium or low-substituted hydroxypropylcellulose obtained by internally cross-linking sodium carboxymethylcellulose is obtained, but from the viewpoint of achieving both disintegration and sliminess, a cellulose derivative More preferably, it is a cellulose derivative other than croscarmellose sodium and low-substituted hydroxypropylcellulose.

  Examples of starch include natural starch. Examples of the origin of starch include corn, potato, litter, tapioca, sweet potato, rice, wheat, wheat, barley, yam, and taro. When blending starch, it is particularly preferable to blend in combination with a sugar alcohol from the viewpoint of achieving both disintegration and sliminess.

  As starch derivatives, modified starch, oxidized starch, enzyme-treated starch, pregelatinized starch, phosphate starch, phosphate distarch, acetate starch, octenyl succinate starch, glycerol distarch, carboxymethyl starch, hydroxypropyl starch, crosslinked starch, soluble Starch, grafted starch, and sodium carboxymethyl starch can be mentioned, and pregelatinized starch is preferable in terms of both sliminess and disintegration time. When blending a starch derivative, blending with a sugar alcohol is particularly preferred in terms of achieving both disintegration and sliminess. Although the effect of the present invention can be obtained even when carboxymethyl starch sodium is included, from the viewpoint of achieving both disintegration and sliminess, the starch derivative is a starch derivative other than carboxymethyl starch sodium. It is more preferable.

  As the starch degradation product, dextrin is exemplified, and those having a DE of 8 to 9.5 are preferably exemplified.

  The content of the specific excipient in the tablet having a naked tablet is 10 parts by mass or more with respect to 100 parts by mass of the gelling agent in the tablet having a naked tablet. It is preferable from the point that the effect of using the agent in combination is further enhanced, and the amount of the specific excipient is 3000 parts by mass or less with respect to 100 parts by mass of the gelling agent in the tablet having a core tablet. This is preferable from the viewpoint of increasing the content of the active ingredient. From these points, it is preferable that the amount of the specific excipient in the tablet having a core tablet is 10 parts by mass or more and 3000 parts by mass or less with respect to 100 parts by mass of the gelling agent in the tablet having a core tablet. It is more preferably 20 parts by mass or more and 2500 parts by mass or less, and particularly preferably 30 parts by mass or more and 2000 parts by mass or less.

  Further, the amount of the specific excipient is preferably 1 part by weight or more and 90 parts by weight or less, more preferably 2 parts by weight or more and 80 parts by weight or less, and most preferably with respect to 100 parts by weight of the tablet having a core tablet. Is preferably 3 parts by mass or more and 70 parts by mass or less. In particular, from the viewpoint of disintegration, the specific excipient preferably occupies 40% by mass or more, more preferably 50% by mass or more, and 60% by mass or more in the tablet having a core tablet. Is more preferable, and may be 70% by mass or more. Moreover, as an upper limit of the quantity of a specific excipient | filler, it is preferable that it is 95 mass% or less in the tablet which has a naked tablet from the point containing a gelatinizer, and it is more preferable that it is 90 mass% or less.

  The tablet having a core tablet in the present invention contains at least one selected from monosaccharides, disaccharides, oligosaccharides, starch derivatives (particularly pregelatinized starch) and starch degradation products, among specific excipients. Is preferable from the viewpoint of high sliminess, and more preferably contains monosaccharides, disaccharides, oligosaccharides or starch degradation products.

In addition, tablets with bare tablets may contain monosaccharides, disaccharides, oligosaccharides, sugar alcohols, crystalline cellulose or cellulose derivatives (particularly carboxymethylcellulose) as specific excipients, in addition to sliminess. It is preferable from a viewpoint which is excellent in it, and it is further more preferable to contain a monosaccharide, a disaccharide, an oligosaccharide, sugar alcohol, or carboxymethylcellulose.
In addition, the inclusion of sugar alcohols and disaccharides enhances the binding properties of the raw material powder of the tablet, facilitates the formulation such as obtaining the hardness of the tablet, and masks the unpleasant taste of the active ingredient. It is preferable also in the point obtained.

  Monosaccharides, disaccharides, oligosaccharides, sugar alcohols, crystalline cellulose and carboxymethylcellulose are contained as a main component in a specific excipient, specifically, as a component occupying 50% by mass or more in a specific excipient. Most preferably.

  In addition, the tablet having a bare tablet contains a combination of a disaccharide and one or more selected from an oligosaccharide, a sugar alcohol, a cellulose derivative, starch, and a starch degradation product as a specific excipient. From the viewpoint of improving sliminess, a combination of a disaccharide and an oligosaccharide or a cellulose derivative is particularly preferable. When a tablet having a core tablet contains a disaccharide and another specific excipient in combination as a specific excipient, 100 parts by mass of the disaccharide from the viewpoint of both sliminess and disintegration The other specific excipient is more preferably 1 part by mass or more and 1000 parts by mass or less, further preferably 5 parts by mass or more and 300 parts by mass or less, and more preferably 5 parts by mass or more and 100 parts by mass or less. It is particularly preferred that

  Moreover, it is preferable from the point of the improvement of disintegration and slimming that the tablet which has a naked tablet contains sugar alcohol and starch or pregelatinized starch in combination as a specific excipient | filler. When a tablet having a core tablet contains a sugar alcohol and starch or pregelatinized starch as a specific excipient in combination, from the viewpoint of both sliminess and disintegration, 100 parts by weight of the sugar alcohol The starch or pregelatinized starch is more preferably 10 parts by mass or more and 1000 parts by mass or less, further preferably 30 parts by mass or more and 700 parts by mass or less, and more preferably 50 parts by mass or more and 500 parts by mass or less. Particularly preferred.

In this embodiment, starch, starch derivative or starch degradation product is contained, and this can be combined with xanthan gum, locust bean gum and guar gum, and salts and derivatives thereof, particularly locust bean gum, to balance hardness and the degree of gelation. However, it is preferable in that it is easier to obtain a tablet having a bare tablet that is easy to swallow.
In addition, as described later, sugar alcohol, xanthan gum, locust bean gum and guar gum, and salts and derivatives thereof under the condition that the surface does not contain particles containing sugar alcohol and gelling agent coated with a gelling agent. It is also preferable to combine with at least one selected from the viewpoints that it is easier to obtain a tablet that is excellent in hardness, ease of swallowing and slipperiness and easy to swallow. And a gelling agent composed of at least one selected from starch and xanthan gum, locust bean gum or guar gum, and salts and derivatives thereof under the condition that the coating layer of the gelling agent is not contained as described later. A tablet having a bare tablet containing reduced maltose is also preferred.

  The tablet having a core tablet preferably contains a specific excipient at the outermost surface portion of the core tablet part, and further preferably contains a specific excipient also at the center.

3. Other Components It is preferable that a tablet having a bare tablet contains silicon dioxide or the like as a fluidity improver. Examples of silicon dioxide include finely divided silicon dioxide and light anhydrous silicic acid. When silicon dioxide is contained, the amount of silicon dioxide is preferably 0.01 parts by mass or more and 2 parts by mass or less, more preferably 0.1 parts by mass or more and 1. 8 parts by mass or less, more preferably 0.5 parts by mass or more and 1.7 parts by mass or less, and most preferably 1 part by mass or more and 1.5 parts by mass or less.

  The tablet having a bare tablet preferably contains a lubricant from the viewpoint of improvement in manufacturability (preventing wrinkling during tableting). Examples of the lubricant include magnesium stearate and calcium stearate. In the case of containing a lubricant, the ratio is preferably 0.1% by mass or more and 20% by mass or less, more preferably 0.5% by mass or more and 10% by mass or less in the naked tablet of the present invention. preferable.

  The tablet having a core tablet according to this embodiment may contain an active ingredient. The active ingredient here may be a drug, or may be a functional ingredient other than the drug, a plant or animal, a processed product derived from a microorganism, or the like. In addition to the above-mentioned active ingredients, specific excipients, silicon dioxide, disintegrants, lubricants, saccharides, tablets having naked tablets can contain binders, seasonings other than saccharides, emulsifiers, fragrances, and the like. The tablet used in this embodiment is for oral use, that is, for internal use, and is a tablet for swallowing. It goes without saying that the tablet of this embodiment may be used as a supplement, health food, functional nutrition food, functional label food, food for specified health use, and pharmaceutical.

  The tablet having a core tablet of the present embodiment contains a seasoning and / or a fragrance other than a saccharide on the outermost surface part of the core tablet part, so that saliva is secreted when the tablet having the core tablet is included in the oral cavity. And the supply of liquid medium such as water to the tablet can be increased. As the seasoning, sweeteners, acidulants and the like can be used. As the sweetener, sucrose derivatives of sucralose, peptide-based sweeteners such as aspartame, alitame, neotame, glycyrrhizin, stevia, licorice and the like can be used. As the acidulant, an organic acid can be used, and examples thereof include citric acid, malic acid, tartaric acid and the like. In addition to citrus flavors such as grapefruit flavor, lemon flavor, and orange flavor, fruit flavors and the like can be used as perfumes.

  The tablet having a core tablet according to this embodiment may contain a disintegrant. Examples of disintegrants include sodium bicarbonate (sodium bicarbonate), magnesium carbonate, carmellose calcium, sodium starch glycolate, etc. that can be used as food additives, crospovidone, sodium carboxymethyl starch, croscarmellose sodium, low Substitution degree hydroxypropyl cellulose is mentioned. Even when a disintegrant is included, the effect of the present invention is exhibited, but from the viewpoint of excellent sliminess, it is preferable that the content of the disintegrant is small, specifically, 100 parts by weight of a tablet having a core tablet. On the other hand, the blending amount of the disintegrant is preferably 9.9 parts by weight or less, more preferably 9 parts by weight or less, further preferably 6 parts by weight or less, still more preferably 3 parts by weight or less, and particularly preferably 1 part by weight or less. Preferably, it is not contained.

  Among the disintegrants, one or more disintegrants selected from crospovidone, sodium carboxymethyl starch, croscarmellose sodium or low-substituted hydroxypropylcellulose (hereinafter referred to as specific disintegrations) from the viewpoint of excellent sliminess. The content of (also referred to as an agent) is preferably small. Specifically, the blending amount of the disintegrant is preferably 9.9 parts by weight or less, more preferably 9 parts by weight or less, still more preferably 6 parts by weight or less, based on 100 parts by weight of the tablet having a core tablet. More preferably, it is more preferably 1 part by weight or less, and most preferably 1 part by weight or less. The low-substituted hydroxypropyl cellulose is produced by reacting propylene oxide and alkali cellulose at a high temperature, and those dried at 105 ° C. for 1 hour have a hydroxypropyl group of 5.0 to 16.0%. It means to include.

  The tablet having a core tablet according to this embodiment may contain a sugar alcohol whose surface is coated with a gelling agent and particles containing the gelling agent. The effect of the present invention is exhibited even when the surface includes particles containing a sugar alcohol and a gelling agent coated with a gelling agent, but from the viewpoint of excellent disintegration, the surface is coated with a gelling agent. The content of the particles containing the sugar alcohol and the gelling agent is preferably small, and the composition of the particles containing the sugar alcohol and the gelling agent whose surface is coated with the gelling agent is added to 100 parts by weight of the tablet having a bare tablet. The amount is preferably 10 parts by weight or less, more preferably 5 parts by weight or less, still more preferably 3 parts by weight or less, still more preferably 1 part by weight or less, and most preferably none. The particles containing the sugar alcohol and the gelling agent whose surfaces are coated with the gelling agent are formed by spraying the gelling agent on the particles containing the sugar alcohol. In the present invention, a tablet having a core tablet does not contain sugar alcohol whose surface is coated with a gelling agent and particles containing the gelling agent, and the gelling agent and a specific excipient are uniformly mixed. By making it the state which was made, it becomes easy to make a collapse time shorter.

  The absence of particles containing sugar alcohol and gelling agent coated with gelling agent on the surface, for example, the distribution of gelling agent in tablets with bare tablets is examined by cross-sectional imaging such as TOF-SIMS This can be confirmed. At this time, if the gelling agent is uniformly dispersed in the bare tablet without observing a layer in which the gelling agent is locally concentrated, the surface of the tablet having the bare tablet of the present invention has the surface. It can be said that the particle | grains containing the sugar alcohol coat | covered with the gelatinizer and a gelatinizer are not contained.

4). Physical properties, etc. Considering ease of swallowing, for example, in the case of a tablet having a core tablet, the weight of one tablet is preferably 100 mg or more and 500 mg or less, more preferably 120 mg or more and 450 mg or less, more preferably 150 mg or more 400 mg or less is most preferable. The diameter is preferably 5 mm to 12 mm, more preferably 5.5 mm to 11 mm, and most preferably 6 mm to 10 mm. The thickness is preferably 2 mm or more and 10 mm or less, more preferably 2.5 mm or more and 9 mm or less, and most preferably 3 mm or more and 8 mm or less. The hardness is preferably 3 kgf to 20 kgf, more preferably 4 kgf to 18 kgf, and most preferably 5 kgf to 16 kgf. The diameter, thickness, and hardness can be measured by the methods described later.

Furthermore, the tablet which has the uncoated tablet of this invention can measure the maximum value (maximum stress) of the stress which arises when a tablet moves in a silicone tube by the method described below. Specifically, the tablet is allowed to stand on a plastic substrate, 0.2 μL of water at 25 ° C. is dropped with a dropper per 1 mm ^{2 of the} tablet surface area, and held in that state for 10 to 20 seconds. It can be measured by the procedure. In the tablet having the uncoated tablet of the present invention, the maximum stress is preferably less than 20N, more preferably 15N or less, further preferably 10N or less, and particularly preferably 5N or less.
The maximum stress measurement procedure is as follows. A schematic diagram of the measuring apparatus is shown in FIG. In FIG. 1, reference numeral 1 is a tablet, reference numeral 2 is a slit, and reference numeral 3 is a silicon tube.

<Maximum stress measurement procedure>
A silicon tube arranged along the vertical direction and fixed so as to be movable in the vertical direction, and a pair of slits fixed with the silicon tube sandwiched in the horizontal direction, and under the slit in the silicon tube One tablet is filled on the side, and the maximum stress is measured when the silicon tube is moved 20 mm upward at a speed of 0.5 mm / second along the slit. In addition, as a silicon tube used for the said measurement, the cross-sectional area of a silicon tube is smaller than the cross-sectional area of a tablet, and what is larger than 40% of the cross-sectional area of a tablet is used. The ratio of the cross-sectional area of the tablet to the cross-sectional area of the silicon tube is preferably 40% or more and 60% or less, and more preferably 45% or more and 55% or less.

The vertical direction is a direction orthogonal to a horizontal plane. Moreover, said left-right direction means the direction orthogonal to an up-down direction. The cross-sectional area of the above-mentioned silicon tube refers to the area of the portion surrounded by the inner surface of the silicon tube in a cross section obtained by cutting the silicon tube in a state not filled with the tablet in a direction perpendicular to the longitudinal direction.
Moreover, the cross-sectional area of a tablet refers to the area of the cross section which has the largest area among the cross sections cut | disconnected by the surface orthogonal to the longitudinal direction of a silicon tube of the tablet in the state with which the silicon tube was filled.

  In addition, the tablet having the core tablet of this embodiment has a disintegration time of 60 minutes or less, preferably 40 minutes or less, more preferably 20 minutes or less, using water as a solvent. As a minimum of disintegration time, 1 minute or more is mentioned from the ease of manufacture of a tablet, for example. The disintegration time means the time until the sample in the solvent disintegrates. The procedure for measuring the disintegration time follows the method described in “Disintegration test method” of item “6.09” in the 15th revision Japanese Pharmacopoeia. When using a tablet having a tablet diameter of 3 to 15 mm, a tablet thickness of 4 to 7 mm, and a weight of 150 to 500 mg, it is preferable to use Toyama Sangyo Co., Ltd., model number: NT-400 as a disintegration tester. The tablet of this embodiment preferably has a disintegration time with respect to the tablet thickness of 0.01 min / mm or more and 25 min / mm or less, more preferably 0.05 min / mm or more and 20 min / mm or less, More preferably, it is 0.1 minutes / mm or more and 12 minutes / mm or less, More preferably, it is 0.15 minutes / mm or more and 8 minutes / mm or less, 0.2 minutes / mm or more and 4 minutes / mm or less. Most preferably:

<Measurement procedure of decay time>
One tablet is put into each glass tube of a disintegration tester having six glass tubes. The upper and lower surfaces of each glass tube are open, and a stainless steel mesh with a mesh opening of 1.8 mm to 2.2 mm is attached to the lower surface of the glass tube. The glass tube containing the tablets is placed in 37 ± 2 ° C. water and the disintegration tester is activated. The glass tube in the disintegration tester is observed. When it is confirmed that the tablet is about to disintegrate, the glass tube is pulled up and the state of disintegration of the tablet is observed. This process is repeated and observed until the tablet is completely disintegrated. The time from when the disintegration tester is activated to when all the 6 tablets disintegrate is measured, and the measured time is taken as the disintegration time. It should be noted that the tablet remains disintegrated when it is a soft substance that does not retain the original shape even if it is recognized at all in the glass tube.

5. Production Method Hereinafter, a preferred method for producing a tablet having a core tablet of this embodiment will be further described.
The production method of the present embodiment comprises a gelling agent and at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product (specific excipient) ) Is compressed into a raw material powder.
Examples of the gelling agent, sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative, and starch degradation product include those described above. In addition, the components other than the gelling agent and the specific excipient in the powder containing the gelling agent and the specific excipient include the above-mentioned excipients, disintegrants, binders, lubricants, emulsifiers, effective Ingredients, seasonings, fragrances and the like can be mentioned. Preferred range of mass ratio of gelling agent in raw powder, preferred mass percentage of preferred gelling agent component, preferred mass percentage of specific excipient, preferred mass percentage of excipient, disintegrant, lubricant These are the same as these preferable mass ratios in the above-mentioned core tablet.

  As described above, the core tablet may be nucleated or non-nucleated. In the case of nucleation, a raw material powder containing an arbitrary nucleus is used as the raw material powder. Locked.

The raw material powder containing the gelling agent and the specific excipient may be a mixture of the powdered gelling agent, the powdered specific excipient, and other powdery components contained as necessary. Alternatively, it may be a granulated powder obtained by granulating a mixture of a powdery gelling agent, a powdery specific excipient, and other powdery components contained as necessary.
As the granulation method, a known granulation method used when an oral tablet is produced by the granule tableting method can be used without any particular limitation.

  The method for producing a tablet having a core tablet of the present invention preferably comprises a powder of gelling agent and sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product. And a step of tableting the obtained mixed powder without spraying an aqueous solution in which the gelling agent is dissolved. As described above, this is because the gelling agent is more uniform with the specific excipient than the uncoated tablet obtained by tableting particles containing the sugar alcohol and gelling agent coated with the gelling agent. This is because the uncoated tablet mixed with is superior in disintegrating property and sliminess, particularly disintegrating property.

  As described above, the tablet having the core tablet of the present embodiment is obtained by spraying a mixed powder tablet containing a gelling agent and a specific excipient, in particular, an aqueous solution containing the gelling agent. A tableted product obtained by tableting the mixed powder is preferable because a bare tablet having a gelling agent on the entire surface portion can be easily obtained. Obtaining “mixed powder tablet containing gelling agent and specific excipient” and “mixed powder (including gelling agent and specific excipient) without spraying aqueous solution containing gelling agent Even if the production method is included in the expression “a tableted product obtained by tableting the mixed powder”, the content of the gelling agent and the specific excipient in the bare tablet is described in the present specification. However, it was not realistic to specify in more detail, and there was an impossible situation where such an expression had to be taken.

  As described above, the tablet having a core tablet of this embodiment has a hard property that is not different from a tablet having a core tablet that does not contain a gelling agent during storage because the core tablet contains a gelling agent as described above. When in contact with a liquid medium such as water, the surface gels and has a slimy feeling, flexibility and elasticity, and is easy to swallow. In addition, the shape of the bare tablet portion is maintained when it comes into contact with a liquid medium such as water, and it is possible to prevent the active ingredient and the like present in the bare tablet portion from dissolving in the oral cavity. As described above, the tablet of the present embodiment has a feature that it swells with a liquid medium such as water to cause a slimy feeling on the surface of the bare tablet.

6). Preferred embodiments of the present invention Preferred embodiments of the present invention include, for example, the following.
A gelling agent;
Tablet having a bare tablet containing at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product (sprayed with an aqueous solution in which a gelling agent is dissolved) Except tablets obtained by tableting the granulated particles.

A gelling agent;
Tablets having a naked tablet containing at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product (crospovidone, sodium carboxymethyl starch, cloth Except those containing carmellose sodium or low substituted hydroxypropylcellulose).

A gelling agent;
A tablet having a core tablet containing at least one selected from monosaccharides, disaccharides, oligosaccharides, pregelatinized starch and starch degradation products.

Locust bean gum, mannan, glucomannan, hyaluronic acid, agar, tamarind gum, psyllium seed gum, tara gum, cassia gum, gum arabic, gati gum, tragacanth gum, caraya gum, cassia gum, ramzan gum, welan gum, macrohomopsis gum, curdlan, pullulan, gellan gum One or more selected from polyamino acids, polylactic acids, and salts and derivatives thereof,
A tablet having a plain tablet containing at least one selected from monosaccharides, disaccharides, oligosaccharides, pregelatinized starch, and starch degradation products.

Locust bean gum, mannan, glucomannan, hyaluronic acid, agar, tamarind gum, psyllium seed gum, tara gum, cassia gum, gum arabic, gati gum, tragacanth gum, caraya gum, cassia gum, ramzan gum, welan gum, macrohomopsis gum, curdlan, pullulan, gellan gum One or more selected from polyamino acids, polylactic acids, and salts and derivatives thereof,
One or more selected from xanthan gum, guar gum, alginic acid, carrageenan,
A tablet having a plain tablet containing at least one selected from monosaccharides, disaccharides, oligosaccharides, pregelatinized starch, and starch degradation products.

A gelling agent;
Disaccharides,
A tablet having a core tablet containing at least one selected from oligosaccharides, sugar alcohols, cellulose derivatives, starch, and starch degradation products.

A gelling agent;
Sugar alcohol,
Including at least one selected from starch and pregelatinized starch,
A tablet having a core tablet, which does not contain a coating layer of a gelling agent.

  Hereinafter, the present invention will be described in more detail with reference to examples. However, the scope of the present invention is not limited to such examples. In addition, as the materials described in Table 1-3, commercially available products were used. In particular, isomalt 900P manufactured by Showa Sangyo Co., Ltd. was used as the isomaltoligosaccharide. As crystalline cellulose, KC Flock W-400G manufactured by Nippon Paper Industries Co., Ltd. was used. As carboxymethylcellulose, carboxymethylcellulose calcium having an etherification degree of 0.5 to 0.7 mol / C6 was used. As the starch powder, Perfiller 102 manufactured by Freund Sangyo Co., Ltd. was used. As the pregelatinized starch, NON-GMO corn alpha-Y manufactured by Sanwa Starch Co., Ltd. was used. As the dextrin, Max 1000 manufactured by Matsutani Chemical Industry Co., Ltd. was used.

1. Evaluation of sliminess [Example 1]
As raw material powders, various raw materials (excluding calcium stearate) for 400 grains were mixed in a plastic bag according to the mixing ratio of Table 1, and then passed through a sieve, and further calcium stearate was added and mixed. This mixed powder was directly tableted with a rotary tableting machine (Kikusui Seisakusho) to obtain a disk-shaped uncoated tablet. The hardness of the obtained uncoated tablet was measured with a Schleunigel tablet hardness tester. Further, when the tablet diameter (diameter) and tablet thickness of the obtained plain tablet were measured with a digital caliper (Digimatic Caliper CD-15AX; Mitutoyo), the hardness was 7.4 kgf, the tablet diameter was 10 mm, and the tablet thickness was 3.52 mm. It was. Moreover, it was 270 mg when the weight of one obtained tablet was measured. In addition, hardness, a tablet diameter, a tablet thickness, and a weight are the average values of the measured value of each three tablets.

[Example 2]
A plain tablet was obtained in the same manner as in Example 1 except that the mixing ratio of the raw material powder was changed according to the mixing ratio in Table 1. The obtained bare tablets were measured in the same manner as in Example 1. As a result, the hardness was 7.7 kgf, the tablet diameter was 10 mm, the tablet thickness was 3.50 mm, and the weight was 270 mg.

[Evaluation of Examples 1 and 2]
About the naked tablet obtained in Examples 1 and 2, the throat myoelectric potential measurement at the time of taking and a dosing feeling questionnaire were conducted in a single blind crossover.
In addition, the slope sliding time was measured in order to evaluate the slipperiness of the tablets.

・ Method of taking naked tablets The subjects selected 6 healthy adults who were not good at drinking tablets (ratio 2: 4). As a method of taking, first, the subject four tablets were included in the mouth, then 20 mL of water at 22 ° C. was included in the mouth, and the tablets were taken together with water.

-Myoelectric potential measurement The myoelectric potential measurement used the electromyograph (The wireless myoelectric measurement and analysis system "Lateo" by AM Science Co., Ltd.). Although the measurement method followed the manual attached to the electromyograph, specifically, it was performed as follows. The electromyograph electrode was attached to the throat, and in order to acclimate the throat, the subject was allowed to take 20 mL of water in the same amount as when taking a naked tablet. Next, the myoelectric potential of the throat when 20 mL of water was taken was measured. Then, after containing 4 tablets in the mouth, the myoelectric potential of the throat when taken with 20 mL of water was measured for each test group. The amount of muscle activity was calculated from the integrated value calculated based on the obtained myoelectric potential (unit volts (V)), and the relative value when the amount of muscle activity when taking only water was taken as 100 (%) was obtained. . The value obtained by adding the relative values once per person and dividing by the number of people was defined as the amount of muscle activity (%). 1 to 3, 1Count is 1/200 second.
In addition, the measurement of each test section was performed with a rest time of about 5 minutes, and the order of taking the bare tablets was changed for each subject.

・ Questionnaire The slipperiness is caught when taking tablets, and the minimum rating (-3 points) is that it is difficult to drink without slipping to the extent that it does not advance through the throat. Evaluation was made in 7 stages, with the highest rating (3 points) being slippery and easy to drink.
For stickiness, the lowest evaluation (-3 points) is when the sticky and sticky to the tongue or pharynx is difficult, and the stickiness is not sticky to the tongue or pharynx and is easy to drink without feeling sticky. The evaluation was made on a 7-point scale with a maximum rating (3 points).

Slope sliding time 150 ml of water was supplied from the upper part of the channel to an aluminum channel having a U-shaped cross section fixed at an angle of 30 ° (straight side view, channel length 90 cm, width 1.2 cm). In this state, one core tablet was slid and flowed from a position 10 cm below the upper end of the channel, and the time (seconds) required to slide 80 cm to the lower end was measured. The test was performed 5 times, the average value of 5 times was calculated, and it was set as the slope sliding time (second).

The amount of muscle activity (%) in the throat obtained by the myoelectric potential measurement is shown in Table 1, and representative electromyograms are shown in FIGS.
Table 1 shows the measurement results of the average value and slope sliding time (seconds) of six people for the evaluation points obtained by the questionnaire. In Table 1, the unit of the composition of the core tablet is parts by mass.

As is clear from Table 1 and FIGS. 2 to 4, the uncoated tablets of Examples 1 and 2 were able to suppress the amount of muscle activity in the throat to an increase of about 1.5 times compared to the case of taking only water. It is a bare tablet that does not require any force when taken, is less susceptible to swallowing stress, and is easy to swallow. The questionnaire shows that it is easy to swallow without feeling sticky on the tongue or pharynx while feeling slippery.
In the case of a bare tablet containing crospovidone, sodium carboxymethyl starch, croscarmellose sodium or low-substituted hydroxypropylcellulose, the slipperiness and stickiness are reduced as compared with Example 1 or 2.

In addition, when comparing the slope sliding time, as shown in Table 1, since Examples 1 and 2 slide down in 2 seconds or less, the bare tablets of the Examples become slippery when in contact with water, and thus are easy to swallow. You can see that it is a thing.
In addition, as for the plain tablet which mix | blended crospovidone, sodium carboxymethyl starch, croscarmellose sodium, or the low substituted hydroxypropyl cellulose, compared with Example 1 or 2, slope sliding property falls.

  As described above, in the case of a bare tablet containing a gelling agent and a specific excipient (sugar alcohol, pregelatinized starch), even a person who is not good at drinking a tablet can easily take it with little resistance. It was.

2. Evaluation of disintegration [Examples 3 to 6]
According to the blending ratio in Table 1 below, the hardness is 9 kgf, the tablet diameter is 9 mm, and the tablet thickness is 4.81 to 5.08 mm (Example 3 is 4.81 mm, Examples 4 and 6 are 4.89 mm, Example 5 is 5 0.08 mm), and the weight was changed to 300 mg, and a bare tablet was obtained in the same manner as in Example 1.
The disintegration time of the obtained plain tablet was measured by the following method. The results are shown in Table 2.

-Disintegration time Using the disintegration tester (Toyama Sangyo Co., Ltd., model number: NT-40H) according to the method described in "Disintegration test method" of item "6.09" in the 15th revision Japanese Pharmacopoeia, n = The disintegration time was measured at 6. The solution was water.

  The unit in the composition of Table 2 is part by mass.

  As is apparent from Table 2, it was found that the bare tablet containing the gelling agent and the specific disintegrant (sugar alcohol, cellulose, cellulose derivative, starch) had a short disintegration time. Further, even when a specific disintegrant (crospovidone) was added, the disintegration time was only shortened by about 20% compared to the case where it was not added.

3. Evaluation of sliminess and disintegration time [Examples 7 to 14, 16 to 21, Comparative Example 1]
A plain tablet was obtained in the same manner as in Example 1 according to the mixing ratio of Table 3 below. The obtained uncoated tablets of Examples 7 to 14, 16 to 21 and Comparative Example 1 were similar in hardness, tablet diameter and tablet thickness to those of Examples 3 to 5 and weighed 300 mg.

Example 15
57.1 parts by mass of sorbitol and 30.0 parts by mass of maltose were charged into a fluidized bed granulator (fluidized bed granulation drying / coating machine model: FD-LAB-1 type, POWREC Co., Ltd.), and a suspension of crystalline cellulose After spraying, the xanthan gum was further granulated by spraying a suspension of xanthan gum diluted with hot water to 0.1% (w / v), and a coating layer of xanthan gum was formed on the particle surface consisting of a mixed powder of sorbitol and maltose. A formed particle composition (particles containing a sugar alcohol and a gelling agent having a surface coated with a gelling agent) was obtained.
After mixing 0.5 parts by mass of calcium stearate into the obtained particle composition, the mixture was tableted using a rotary tableting machine (Kikusui Seisakusho), and the hardness, tablet diameter, and tablet thickness were about the same as in Examples 3-5. Thus, a bare tablet weighing 300 mg was obtained. The amounts of crystalline cellulose and xanthan gum in the bare tablets were those shown in Table 1.

  For the plain tablets obtained in Examples 7 to 21 and Comparative Example 1, the disintegration time was measured by the same method as in Examples 3 to 6. The results are shown in Table 3.

  Furthermore, the maximum stress was measured for the plain tablets obtained in Examples 7 to 21 and Comparative Example 1 by the following method.

<Maximum stress measurement procedure>
The bare tablet was allowed to stand on a plastic substrate, and 0.2 μL of water at 25 ° C. was dropped with a dropper per 1 mm ² of the surface area of the bare tablet, and kept in that state for 15 seconds.
A silicon tube with an inner diameter of 9 mm and an outer diameter of 11 mm, which is arranged along the vertical direction so that the longitudinal direction coincides with the vertical direction and is movably fixed in the vertical direction, and fixed with the silicon tube sandwiched in the horizontal direction Using the pair of slits thus formed, a single tablet of the uncoated tablet (tablet diameter 9 mm) was filled under the slit in the silicon tube. The maximum stress when the silicon tube is moved 20 mm upward at a speed of 0.5 mm / second with respect to the bare tablet along the slit is measured using a Yamaden Corporation creep meter (RE2-33005C). did. The cross-sectional area of the silicon tube used for the measurement was 50% of the cross-sectional area of the bare tablet. When the stress exceeded 20, the measurement was finished at that time. As the silicone tube, a clear silicone square tube manufactured by Fuso Rubber Sangyo Co., Ltd. was used. A special cylindrical extrusion jig (AT-43446) manufactured by Yamaden Co., Ltd. was used as the slit, and this was fixed at a position where the mutual minimum distance was 2 mm.
The maximum stress was determined as an average value of triplicate.

The unit in the composition of Table 3 is part by mass.

As can be seen from the comparison between Examples 7 to 21 and Comparative Example 1 in Table 3, the gelling agent and the specific were compared with the naked tablet of Comparative Example 1 containing only the specific excipient and not containing the gelling agent. In the plain tablets of Examples 7 to 21 containing these excipients, the maximum stress is greatly reduced.
Moreover, from the results of Examples 7 to 14, it can be seen that the maximum stress is particularly low in the case of a plain tablet containing monosaccharide, disaccharide, oligosaccharide or starch degradation product among the specific excipients.

  Further, from the comparison between Examples 15 and 16, the sugar alcohol was compared with the gelling agent as compared with the uncoated tablet obtained by tableting particles containing the sugar alcohol and the gelling agent whose surface was coated with the gelling agent. It can be seen that the uncoated tablets mixed and compressed have a shorter disintegration time and a lower maximum stress.

  In addition, compared with a naked tablet obtained by tableting particles containing a sugar alcohol and a gelling agent whose surface is coated with a gelling agent, The tendency for the disintegration time to be shortened and the maximum stress to be lowered is observed not only when sorbitol is used as the sugar alcohol but also for sugar alcohols other than sorbitol (erythritol, mannitol, etc.).

  In addition, from the results of Examples 17 to 21, when locust bean gum is used as a gelling agent, the disintegration time is shortened and the maximum stress is reduced, so that both disintegration and sliminess are achieved. It can be seen that locust bean gum is particularly excellent among gelling agents.

  In the same manner as in Example 1, the following plain tablets (Prescription Examples 1 to 41) were produced. All the uncoated tablets were excellent in sliminess and disintegration. In particular, a plain tablet combining two or more gelling agents, a monosaccharide, a disaccharide, an oligosaccharide, a starch derivative containing one or more selected from starch derivatives and starch degradation products, a specific excipient Of these, uncoated tablets and disaccharides containing two or more components belonging to different categories in combination with one or more selected from oligosaccharides, sugar alcohols, cellulose derivatives, starch and starch degradation products are excellent. Excellent sliminess and disintegration. In addition, sucrose is applied to the bare tablets prepared in Formulation Examples 1 to 41, and the ratio of the surface area of the tablet covered by the coating layer is adjusted to 20% or more and less than 30% (using sucrose using water). The tablet having a core tablet whose coating ratio was adjusted by attaching) was also excellent in sliminess and disintegration. Similarly, the plain tablet prepared so that the ratio of the surface area of the tablet covered by the coating layer was 5% or more and less than 10% was excellent in sliminess and disintegration.

1 Tablet 2 Slit 3 Silicone tube

  Since the tablet having the bare tablet of the present invention is easy to swallow and does not need to be coated on the entire surface, it is possible to avoid an increase in size due to the coating, and the manufacturing cost can be reduced by not performing the coating. it can. In addition, it is excellent in ease of disintegration after ingestion. Therefore, it is obvious that the tablet having the bare tablet of the present invention can be used and produced as a supplement, health food, nutritional functional food, functional labeling food, food for specified health use, pharmaceuticals and the like, and is useful. is there.

Claims (3)

A gelling agent;
A tablet having a core tablet comprising at least one selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product.   The tablet according to claim 1, wherein the bare tablet comprises one or more selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide and starch degradation product.   A raw material powder containing a gelling agent and at least one excipient selected from sugar alcohol, monosaccharide, disaccharide, oligosaccharide, cellulose, cellulose derivative, starch, starch derivative and starch degradation product The method for producing a tablet according to claim 1, wherein tableting is performed without spraying.