JP6631997B2 - Oral preparation, method for producing oral preparation, coating composition for oral solid preparation - Google Patents

Description

  The present invention relates to an oral preparation, a method for producing an oral preparation, and a coating composition for an oral solid preparation.

For oral administration, solid preparations (solid preparations) such as tablets and pills are mainly used. Such solid preparations are often difficult to take for children and elderly people who have little swallowing function.
In order to make the solid preparation easy to swallow, the solid preparation is required to be slippery, difficult to catch on the throat, and the like. A plurality of techniques for devising a coating of a solid agent to facilitate swallowing the solid agent have been reported (Patent Documents 1 to 3).

JP-A-62-132831 JP 2001-521910 A JP-A-2002-275054

However, conventional oral preparations are not sufficient in terms of slipperiness in the throat, difficulty in catching in the throat, and the like.
An object of the present invention is to provide an oral preparation having a solid preparation and a coating for coating the surface of the solid preparation, which is hard to catch on the throat and is easy to swallow.

The present invention is an oral preparation having a solid preparation and a slimming material-containing layer covering the surface of the solid preparation,
The slimming material-containing layer has a slimming material and a binder (excluding pullulan) for fixing the slimming material,
The slimming material-containing layer is a single layer or covers the solid agent surface in a state where a plurality of layers are stacked,
The slimming material provides an oral preparation containing at least one selected from starch, xanthan gum, locust bean gum, and salts and derivatives thereof.

The present invention also relates to a method for producing the oral preparation,
A liquid binder is coated on the surface of the solid agent, and a layer forming step of forming a sliming material-containing layer by attaching a slimming material to the binder after the coating is performed. Provided is a method for producing an oral preparation, wherein a laminated structure in which a plurality of containing layers are laminated is formed on the surface of a solid preparation.

  ADVANTAGE OF THE INVENTION According to the oral preparation of this invention, when it drinks with water, the coating which coats a solid preparation absorbs water and exhibits viscosity, and can drink smoothly without the oral preparation sticking to the throat. Further, according to the method for producing an oral preparation of the present invention, the oral preparation of the present invention can be produced efficiently.

FIG. 1 is a schematic diagram showing an example of a cross section of the oral preparation of the present invention.

  Hereinafter, the present invention will be described based on preferred embodiments. The oral preparation of the present invention has a solid preparation and a coating for covering the surface of the solid preparation, and the coating has a layer structure including a slime material-containing layer containing a binder and a slick material. Specifically, the coating has a layer structure including a slimming material-containing layer obtained by fixing a powdery slimming material with a binder, and the layer structure is a single-layer structure including the slimming material-containing layer or This is a laminated structure in which a plurality of the sliming material-containing layers are laminated.

  As the slimming material, a powdery (particulate) material that exhibits viscosity when containing water is used. The present invention is characterized in that at least one selected from starch or a derivative thereof, xanthan gum, and locust bean gum is used as the slimming material. As a result, the oral preparation of the present invention has an excellent sliding speed when drinking with a liquid, and is less sticky when drinking. In the present invention, as the slimming material, only one of starch or a derivative thereof, xanthan gum, and locust bean gum may be used, or two or more thereof may be used in combination. In addition to improving the sliding speed of the oral preparation, it is preferable to use a combination of two or more of starch or a derivative thereof, xanthan gum, and locust bean gum from the viewpoint of enhancing the cosmetic properties such as uniform appearance and non-dusting. , Starch or a derivative thereof, xanthan gum, and locust bean gum are more preferably used in combination. As starch derivatives, starch decomposed products, modified starch, oxidized starch, enzyme-treated starch, pregelatinized starch, starch phosphate, distarch phosphate, starch acetate, starch octenyl succinate, glycerol distarch, carboxymethyl starch, hydroxypropyl starch, Bridged starch, soluble starch, and grafted starch are included. In the present specification, the slimming material refers to a material contained in the coating, and even if a similar component is contained in the solid agent to be coated, it is not regarded as a slimming material.

  The slimming material selected from three types of starch or a derivative thereof, xanthan gum and locust bean gum, when a plurality of sliming material-containing layers are laminated, one, two, or three of the three types are selected from the group consisting of: What is necessary is just to contain in at least one layer among several layers, More preferably, one, two or three of these three types are contained in the outermost layer of a coating. Most preferably, one, two or three of the three types are contained in each of the slime material-containing layers constituting the coating.

  In the oral preparation of the present invention, the total amount of starch and its derivative, xanthan gum, and locust bean gum is 5% by mass or more in the coating (or in the layer containing the slicky material), which makes the oral preparation slippery. It is preferable from the viewpoint of improving the effect of preventing stickiness. On the other hand, the total amount is preferably 95% by mass or less in the coating (or in the layer containing the slimming material), from the viewpoint of making the size of the oral preparation appropriate and the viewpoint of uniformly coating. From these viewpoints, the total amount is more preferably from 10% by mass to 90% by mass in the coating (or in the layer containing the slimming material), and particularly preferably from 20% by mass to 80% by mass. . Further, from the same viewpoint as above, the total amount of starch and its derivative, xanthan gum, and locust bean gum in the coating (or in the layer containing the slimming material) is 1% by mass to 50% by mass in the oral preparation of the present invention. Is preferably not more than 2% by mass and more preferably not more than 30% by mass. In addition, this total amount is the amount of one of the oral preparations containing one of starch or a derivative thereof, xanthan gum, and locust bean gum in the coating (or in the layer containing the slimming material). When two or more kinds are contained, it is the total amount of them.

  When the oral preparation has a plurality of sliming material-containing layers, the preferable amount in the sliming material-containing layer described in the present specification means the amount in any one of the plurality of sliming material-containing layers (or each layer). ) Or the amount in the entire layer structure composed of a plurality of sliming material-containing layers.

  In the present invention, the preferred proportion of the slimy material in the coating (or in the slicky material-containing layer) is preferably the total amount of starch and its derivative, xanthan gum, and locust bean gum in the coating (or in the slicky material-containing layer). Examples of the ratio include the same ratios as those described above. The preferable ratio of the slimming material in the oral preparation is the same as the above-mentioned ratio as the preferable ratio of the total amount of starch and its derivative, xanthan gum, and locust bean gum in the oral preparation.

  When the slimming material of the oral preparation of the present invention contains starch and / or a derivative thereof and xanthan gum and / or locust bean gum, the ratio of the former to the latter in the oral preparation (or the layer containing the slicking material) is defined as starch and starch. When the amount of xanthan gum and / or locust bean gum is 3 parts by mass or more with respect to 100 parts by mass of the derivative thereof, the sliding speed is more easily improved, and the cosmetics are more easily enhanced. On the other hand, it is preferable that the amount of xanthan gum and / or locust bean gum is 500 parts by mass or less based on 100 parts by mass of starch and / or a derivative thereof, because the oral preparation can be made more slippery and easy to drink. From these viewpoints, when starch and / or a derivative thereof and xanthan gum and / or locust bean gum are contained, the ratio of the former to the latter in the oral preparation (or the layer containing the slick material) is defined as starch and / or a derivative thereof. The amount of xanthan gum and / or locust bean gum is more preferably from 30 parts by mass to 400 parts by mass, particularly preferably from 50 parts by mass to 300 parts by mass, per 100 parts by mass. The mass of starch and / or a derivative thereof as referred to herein is the mass when only one of starch and the starch derivative is contained, and is the total amount when both are contained. The same applies to the mass of xanthan gum and / or locust bean gum.

  When the slimming material of the oral preparation of the present invention contains xanthan gum and locust bean gum, the ratio of the former to the latter in the oral preparation (or in the layer containing the stencil material) is such that locust bean gum is 100 parts by mass of xanthan gum. When the amount is 3 parts by mass or more and 200 parts by mass or less, it is preferable to further improve the sliding speed. From these viewpoints, when the slime material contains xanthan gum and locust bean gum, the ratio of the former to the latter in the oral preparation (or the layer containing the slick material) is such that locust bean gum is 15 parts by mass with respect to 100 parts by mass of xanthan gum. It is still more preferable that the amount is not less than 50 parts by mass and not more than 150 parts by mass, particularly preferably not less than 50 parts by mass and not more than 100 parts by mass.

The slimming material-containing layer may contain other slimming materials in addition to the starch or its derivative, xanthan gum, and locust bean gum.
Examples of such other slimming materials include protein degradation products such as gelatin; polyamino acids such as polyglutamic acid; mannan, glucomannan, hyaluronic acid, alginic acid, tamarind gum, guar gum, carrageenan, acacia gum, pullulan and gellan gum. And at least one selected from salts and derivatives thereof. Examples of the derivative include a hyaluronic acid derivative, an alginic acid derivative, and a polyglutamic acid derivative. Examples of the salt include alginates, hyaluronates, polyglutamates and the like. Examples of the hyaluronic acid derivative include a hyaluronic acid ester and acetylated hyaluronic acid. Alginic acid derivatives include alginic acid esters. Examples of the polyglutamic acid derivative include polyglutamic acid esters and the like. Alginates include sodium alginate, potassium alginate, ammonium alginate, calcium alginate and the like. Examples of the hyaluronate include sodium hyaluronate and potassium hyaluronate. Examples of the polyglutamate include sodium polyglutamate and potassium polyglutamate. One of these slimming materials may be used alone, or two or more thereof may be used in combination.

  In the oral preparation of the present invention, the average particle size of the slicking material is preferably from 1 μm to 300 μm, more preferably from 10 μm to 200 μm, even more preferably from 10 μm to 100 μm. The average particle size of the slicky material can be measured using a laser diffraction / scattering particle size distribution analyzer.

  A binder is a substance that dissolves in a liquid medium such as an aqueous liquid and exhibits a binding force. Examples of the binder include protein degradation products, saccharides, polyamino acids, synthetic polymers, glycerin and derivatives thereof. Examples of the protein degradation product include gelatin. Examples of the carbohydrate include sugars (monosaccharide or disaccharide) such as fructose, glucose, sucrose, maltose or lactose; dextrin, hyaluronic acid, tamarind gum, carrageenan, locust bean gum, guar gum, agar, mannan, glucomannan, pectin. , Xanthan gum, gellan gum, alginic acid, starch, cellulose and the like. Examples of the polyamino acid include polyglutamic acid. Examples of the synthetic polymer include a carboxyvinyl polymer and polyvinylpyrrolidone. These salts and derivatives are also included in the binder. Examples of the salts and derivatives that can be used as the binder include the same salts and derivatives as those described above as the salts and derivatives that can be used as the slicking material, and a cellulose derivative. Examples of the cellulose derivative include cellulosic semisynthetic polymers such as methylcellulose, ethylcellulose, carboxymethylcellulose and salts thereof (such as sodium carboxymethylcellulose), hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose. One of these binders may be used alone, or two or more thereof may be used in combination.

  In the present invention, the binder and the slimming material may be the same substance or different substances, but are preferably different substances.

  Examples of the liquid medium in which the binder is dissolved include water, an organic solvent, and a mixture thereof, and the organic solvent is preferably an alcohol. Examples of the alcohol include ethanol.

  Among the binders mentioned above, saccharides (monosaccharides or disaccharides) are preferable because when used in combination with the specific slimming material of the present invention, they are excellent in terms of improving sliding speed, preventing stickiness, and improving cosmetic properties. . Specifically, a binder is preferable from the viewpoint of increasing the sliding effect of liquid sugar. Liquid sugar refers to saccharides that are commercially available in the form of a monosaccharide and / or disaccharide in a liquid state, or powdered sugar that is a monosaccharide and / or a disaccharide in a solution state. Examples of liquid sugar include isomerized liquid sugar, reduced maltose starch syrup, honey, molasses, and the like. Examples of isomerized liquid sugars include those specified in Notification No. 2771 of the Ministry of Agriculture, Forestry and Fisheries. As isomerized liquid sugar, any of `` glucose fructose liquid sugar '', `` fructose glucose liquid sugar '', `` high fructose liquid sugar '', `` sugar mixed isomerized liquid sugar '' specified in the notification of the Ministry of Agriculture, Forestry and Fisheries described above, etc. Although it is good, preferably, when used in combination with a specific slimming material, the content of glucose in the solid content in the binder is 10% by mass from the viewpoint of improving the sliding speed, preventing stickiness, and improving cosmetics. The content is preferably from 90% by mass to 90% by mass, and more preferably from 30% by mass to 70% by mass. From the same viewpoint, the content of fructose in the solid content in the binder is preferably from 10% by mass to 90% by mass, and more preferably from 30% by mass to 70% by mass.

  The solid preparation according to the present invention may be any solid preparation containing an active ingredient and having a predetermined shape, and may be an uncoated tablet such as an uncoated tablet, or a solid preparation according to the present invention. (A coating containing a material and a binder). The active ingredient here may be a drug, a functional ingredient other than the drug, a plant or animal, a processed product derived from a microorganism, or the like. The preparation may contain an excipient, a binder, a disintegrant, a lubricant and the like in addition to the active ingredient. The solid preparation used in the present invention is for oral use, that is, for internal use. Specific examples of the solid preparation include tablets, pills, capsules, pellets, granules, powders and the like. Examples of the solid preparation used in the present invention include those in the range of 0.1 g to 1 g per tablet, 3 mm to 15 mm in diameter, and 2 mm to 8 mm in thickness.

A schematic diagram of the oral preparation of the present invention is shown in FIG.
As shown in FIG. 1, an oral preparation 1 of the present invention has a structure in which a powdery slimming material 4 is adhered to the surface of a solid preparation 3 by a binder 2. Specifically, the oral preparation 1 has a slimming material-containing layer 5 in which a powdery slimming material 4 is fixed by a binder 2, and this constitutes a coating that covers the surface of the solid agent 3. . The state that the slimming material 4 is fixed by the binder 2 means, for example, a state where the slimming material 4 is bound to such an extent that the slimming material 4 does not peel off when the oral preparation 1 is held in a hand. The coating has a layer structure 6 including a slimming material-containing layer 5. As shown in FIG. 1, the layer structure 6 may be a laminated structure in which a plurality of sliming material-containing layers 5 are laminated, or may be a single-layer structure including one sliming material-containing layer 5. In the example shown in FIG. 1, the coating substantially covers the entire surface of the solid agent 3. Here, “substantially covering the entire area” means, for example, covering 90% or more, preferably 95% or more, more preferably 99% or more of the surface area of the solid agent 2. During coating (or in the layer containing the slimming material), the powdery slimming material 4 fixed to the binder 2 exhibits viscosity (sliminess) when water is included. For this reason, when the oral preparation 1 is put into the oral cavity together with water, the slimming material 4 exhibits a viscosity containing water, whereby the surface of the oral preparation 1 is slippery and slippery, and the oral preparation 1 does not catch on the throat. It can be easily swallowed.

  In respect of more reliably achieving the effects of the present invention, the thickness of the layer structure 6 is preferably equal to or greater than 0.01 mm, more preferably equal to or greater than 0.02 mm, still more preferably equal to or greater than 0.05 mm, and particularly preferably equal to or greater than 0.1 mm. . On the other hand, the thickness of the layer structure 6 is preferably 6 mm or less, more preferably 3 mm or less, still more preferably 2 mm or less, from the viewpoint of making the oral preparation of the present invention easy to drink and easy to manufacture. 5 m or less is still more preferable, and 1.0 mm or less is particularly preferable. As the preferable numerical range of the coating thickness, the same range as the above-mentioned range as the preferable numerical range of the thickness of the layer structure 6 can be mentioned. When the coating comprises the layer structure 6, the thickness of the layer structure 6 can be measured by using a measuring instrument such as a caliper, for example, by taking the difference in thickness between the coated tablet and the uncoated tablet. Specifically, after measuring the thickness of the uncoated tablet and measuring the thickness of the coated tablet, the value obtained by subtracting the uncoated tablet thickness from the coated tablet thickness is divided by 2 (the upper coating thickness and the Average the thickness of the lower coating). Here, the thickness of the coated tablet refers to the dimension of the coated tablet in a direction perpendicular to the cut surface having the largest cross-sectional area when cutting the coated tablet.

  The layer structure 6 is preferably a structure in which two or more layers of the sliming material are stacked, more preferably a structure in which three or more layers are stacked, and particularly preferably a structure in which five or more layers are stacked. There may be more than one layer. By laminating to such an extent, it is possible to easily obtain a sufficient thickness and amount of the slimy material for improving the swallowability as a coating. Although it is preferable that the number of layers of the sliming material-containing layer 5 is large, the upper limit of the number of layers that is preferable from the viewpoint of ease of production and the like includes about 100 layers, more preferably 50 layers, and still more preferably 30 layers. Even more preferably 10 layers, particularly preferably 6 layers are raised. In FIG. 1, the sliming material-containing layer 5 is shown as two layers for convenience.

  The amount of the slimming material 4 in each slimming material-containing layer 5 in the layer structure 6 may be the same or different. If different, for example, the layer closer to the surface of the solid preparation 3 (the inner layer) may be configured so that the amount of the slimming material 4 is larger, or the layer closer to the surface of the oral preparation 1 (the outer layer) ) The configuration may be such that the number of the slimming materials 4 is larger, or the layers with a larger number of slimming materials and the layers with a smaller number are alternately stacked. Further, the type of the slicking material 4 in each of the sliming material-containing layers 5 in the layer structure 6 may be the same or different. Similarly, the type of the binder 2 in each of the sliming material-containing layers 5 in the layer structure 6 may be the same or different. The layer structure 6 may have a layer having no slimming material 4 in addition to the slimming material-containing layer 5, but the outermost layer of the layer structure 6 is the slimming material-containing layer 5.

  When the amount of the slimming material 4 with respect to 100 parts by mass of the dry mass of the binder during coating (or in the slimming material-containing layer) is 0.01 parts by mass or more, the swallowing effect of the slimming material 4 is easily obtained. preferable. Further, in order to more reliably obtain the effect of fixing by the binder 2, the amount of the sliming material 4 with respect to 100 parts by mass of the dry mass of the binder 2 is preferably 10,000 parts by mass or less. From these viewpoints, the amount of the sliming material 4 with respect to 100 parts by mass of the dry mass of the binder 2 is more preferably from 0.1 to 10,000 parts by mass, still more preferably from 1 to 5,000 parts by mass, and more preferably 10 parts by mass. The amount is particularly preferably from not less than 3000 parts by mass, particularly preferably not less than 50 parts by mass and not more than 1000 parts by mass, and most preferably not less than 100 parts by mass and not more than 500 parts by mass. The preferable ratio of the total amount of starch and its derivative, xanthan gum, and locust bean gum to 100 parts by mass of the dry mass of the binder 2 during the coating (or in the layer containing the slick material) is also the same as that described above in the coating (or the slick material). The amount is the same as the preferable amount of the sliming material 4 with respect to 100 parts by mass of the dry mass of the binder in the (containing layer).

  Further, it is preferable that the dry mass of the binder in the coating (or in the layer containing the slimming material) be 5% by mass or more, because the effect of the interaction between the binder and the sliming material is easily obtained. In addition, the dry mass of the binder in the coating (or in the layer containing the slimming material) is preferably 50% by mass or less from the viewpoint of further increasing the ease of swallowing with the sliming material. From these viewpoints, the dry mass of the binder in the coating (or in the layer containing the slick material) is more preferably 10% by mass or more and 40% by mass or less, and further preferably 15% by mass or more and 30% by mass or less. preferable. Further, from the same viewpoint, the dry mass of the binder in the oral preparation is preferably 0.5% by mass or more and 20% by mass or less, more preferably 1% by mass or more and 15% by mass or less, and further preferably 2% by mass or less. It is particularly preferable that the content is not less than 12.5% by mass.

  The amount of the slimming material 4 in the coating (or in the slimming material-containing layer) can be measured, for example, using a calculated value from the difference in mass before and after the coating. Further, the amount of the binder 2 in the coating (or in the layer containing the slimming material) can be measured by using a value calculated from the concentration at the time of adjustment and the spray amount.

The coating may consist essentially of the slimming material 4 and the binder 2 only. Substantially consisting only of the slimming material and the binder means that impurities which are unavoidably mixed in the manufacturing process may be contained. For example, the total content of the sliming material and the binder in the dry mass of the coating is 95%. % By mass or more.
However, the coating may also contain other components other than the slime material and the binder.

  The oral preparation preferably contains a sugar alcohol excluding mannitol in the layer containing the slimming material. In this case, the slip speed when drinking the oral preparation using the liquid medium is improved, and the stickiness is reduced, which is preferable. When a plurality of sliming material-containing layers are laminated in the coating, as a specific form containing a sugar alcohol other than mannitol in the slimming material-containing layer, as long as these components are contained in at least one layer. It is preferable, but it is particularly preferable that the outermost layer contains a sugar alcohol other than mannitol, and most preferably, it is contained in each layer. Examples of sugar alcohols other than mannitol include monosaccharide alcohols, disaccharide alcohols, and trisaccharide or higher alcohols. Examples of the monosaccharide alcohol include pentitols such as erythritol, D-threitol and L-threitol, pentitols such as D-arabinitol and xylitol, hexitols such as D-iditol, galactitol (darcitol) and D-glucitol (sorbitol). And cyclitols such as inositol. Examples of the disaccharide alcohol include reduced maltose (maltitol), lactitol, reduced palatinose (isomalto), and the like. Examples of the alcohol having three or more sugars include maltotriitol, isomalttriitol, and panitol. As the sugar alcohol, in combination with the specific slimming material used in the present invention, particularly from the viewpoint of easily improving the sliding speed and easily preventing stickiness, monosaccharide alcohols and disaccharides of either tetritol or pentitol And at least one selected from erythritol, xylitol, reduced maltose and reduced palatinose. In addition, when the oral preparation contains sucralose, aspartame, acesulfame potassium, stevia, licorice, thaumatin, etc. as an artificial sweetener, the same effect as in the case of containing a sugar alcohol other than mannitol is exerted.

  During coating (or in the layer containing the slimming material), the amount ratio of the sugar alcohol excluding mannitol and the total amount of starch and its derivatives, xanthan gum, and locust bean gum is 100 parts by mass of the sugar alcohol, starch and its derivatives, It is preferable that the total amount of xanthan gum and locust bean gum is 10 parts by mass or more from the viewpoint of preventing stickiness. Further, the total amount of starch and its derivative, xanthan gum, and locust bean gum is preferably not more than 1000 parts by mass with respect to 100 parts by mass of the sugar alcohol, from the viewpoint of improving the sliding speed and preventing stickiness easily and easily. From this viewpoint, the total amount of starch and its derivatives, xanthan gum, and locust bean gum is preferably 50 parts by mass or more and 500 parts by mass or less with respect to 100 parts by mass of the sugar alcohol in the coating (or in the layer containing the slick material). More preferably, it is more preferably 100 parts by mass or more and 300 parts by mass or less. In addition, as a preferable ratio of the slimming material to 100 parts by mass of sugar alcohol excluding mannitol during coating (or in the slimming material-containing layer), the ratio of starch and the starch to 100 parts by mass of sugar alcohol in the coating (or in the slimming material-containing layer) is preferable. Preferred proportions of the total amount of the derivative, xanthan gum, and locust bean gum include the amounts listed above.

Other components other than sugar alcohols include water guides, seasonings, thickeners, coloring agents and flavors, plasticizers, various plant extracts, and the like. These other components are most effective when contained in the outermost layer of the coating layer, but may be contained in a layer inside the outermost layer.
By using the water guide agent, moisture can be effectively supplied to the slimming material, and it can be more easily taken. As the water-guiding agent, polysaccharides are preferable, and cellulose and the like can be particularly used. When cellulose is used, 1 part by mass or more and 100 parts by mass of starch and its derivative, xanthan gum, and locust bean gum are used in the coating (or in the layer containing the coloring material) from the viewpoint of maintaining the slimming effect. It is preferably contained in an amount of 5 parts by mass or less, more preferably 5 parts by mass or more and 20 parts by mass or less.

  By using a seasoning, secretion of saliva can be promoted when the tablet is contained in the oral cavity, and supply of water to the tablet can be increased. As a seasoning, a sweetener, an acidifier, a flavor, and the like can be used. As sweeteners, sugars, sucrose derivatives of sucralose, peptide-based sweeteners such as aspartame, alitame, neotame, glycyrrhizin, stevia, licorice and the like can be used. From the viewpoint of adjusting the timing of the manifestation of the sweetening effect and the manifestation of the slimming effect, it is preferable to use a sucrose derivative or a peptide-based sweetener, and it is particularly preferable to contain at least one selected from aspartame and sucralose. For example, aspartame is 0.001 part by mass or more in the coating (or in the layer containing the slimming material) from the viewpoint of promoting salivary secretion, based on 100 parts by mass of the total amount of starch and its derivatives, xanthan gum, and locust bean gum. The content is preferably 10 parts by mass or less, more preferably 0.01 part by mass or more and 3 parts by mass or less. In addition, sucralose is 0.001 to 10 parts by mass based on 100 parts by mass of starch and its derivatives, xanthan gum, and locust bean gum in the coating (or in the layer containing the slick material) from the viewpoint of promoting salivary secretion. It is preferably contained in an amount of not more than 0.01 part by mass, more preferably not less than 0.01 part by mass and not more than 3 parts by mass. The preferred amount of the whole sweetener during the coating (or in the layer containing the slimming material) is the same as the above-mentioned preferred amount of aspartame and sucralose.

  Organic acids can be used as the acidulant, and examples thereof include citric acid, malic acid, and tartaric acid. It is particularly preferable to use citric acid from the viewpoint of promoting salivary secretion. From this viewpoint, in the coating (or in the layer containing the slick material), the acidulant is present in an amount of 0.01 to 30 parts by mass based on 100 parts by mass of starch and its derivative, xanthan gum, and locust bean gum. The content is preferably not more than 0.1 part by mass and more preferably not more than 10 parts by mass.

  As the flavor, citrus flavors such as grapefruit flavor, lemon flavor, orange flavor and the like, as well as fruit flavors and the like can be used. The fragrance is preferably contained in an amount of 0.1 part by mass or more and 10 parts by mass or less with respect to 100 parts by mass of the starch and its derivative, xanthan gum, and locust bean gum in the oral preparation from the viewpoint of enhancing the fragrance. .

  In addition, the preferable ratio of the above water-conducting agent and each seasoning agent to 100 parts by mass of the slimming material is the ratio described above as the preferable ratio to the total amount of 100 parts by mass of starch and derivatives thereof, xanthan gum, and locust bean gum. A similar ratio is given.

The use of the thickener can enhance the slickness of the slimming material. Examples of the thickener include tamarind gum, guar gum, carrageenan, acacia gum, pullulan, gellan gum, mannan, glucomannan, hyaluronic acid, alginic acid, polyglutamic acid, and salts and derivatives thereof. Examples of the salts and derivatives that can be used as the thickener include the same salts and derivatives as those described above as the salts and derivatives that can be used as the slimming material.
The proportion of the other components in the dry mass of the coating is adjusted so as not to impair the effects of the present invention.

Next, a preferred method for producing the oral preparation of the present invention will be described.
In this production method, a solution obtained by dissolving a binder in a liquid medium (hereinafter, also referred to as a binder solution) is coated (coated) on the surface of the solid agent, and a powdery slick material is attached to the coated binder. Thereby, the layer structure including the sliming material-containing layer is formed on the surface of the solid agent by having the layer forming step of forming the slimming material-containing layer. Further, by repeating the above-described layer forming step, a structure in which a plurality of layers of the sliming material are laminated can be formed on the surface of the solid agent.

  As the binder and the liquid medium, those described above can be used. The amount of the binder in the binder solution (also referred to as the amount of solid content) is more preferably 5% by mass or more and 90% by mass or less. In particular, when a saccharide is used as the binder, the amount is preferably from 10% by mass to 85% by mass, and more preferably from 20% by mass to 80% by mass, from the viewpoint that the production time can be reduced by shortening the drying time of the binder. When the binder is a protein hydrolyzate or the like, the amount of the binder in the binder solution is preferably from 0.1% by mass to 10% by mass, more preferably from 1% by mass to 10% by mass. .

  The solid solution is coated with the binder solution prepared as described above, and before drying, a powdery slick material is adhered to the binder in the coating (or in the slick material-containing layer). The coating of the binder solution and the attachment of the slicking material may be performed in the same step or in different steps. The case of performing in the same step includes, for example, a powder coating method of supplying a powdery slick material while spraying a binder solution onto a solid agent. In the case where the solid agent is coated in a separate step, a method of attaching a slimming material after the coating of the solid agent with the binder solution is used. After the application of the slimming material, the coated binder solution is dried to form a sliming material-containing layer 5. This drying can be performed by natural drying or the like. The oral preparation of the present invention in which the layer structure is formed on the surface of the solid preparation by the above layer forming step is obtained. When the layer structure is a laminated structure as described above, this layer forming step is repeated.

  The thus-obtained oral preparation of the present invention easily slips in the throat when taken with water. Therefore, even a person who is not good at swallowing a solid preparation, an elderly person, and a child can drink the oral preparation of the present invention smoothly without being caught on the throat.

  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 embodiments.

[Example 1]
(Layer forming step)
Uncoated tablets were used as solid preparations. The weight, diameter, and thickness of the uncoated tablet were in the ranges described above. Powdered gelatin was used as a binder and dissolved in water to obtain a binder solution having a concentration of 0.3% by mass. Starch was used as a slimming material. When the average particle size of the starch was measured by the method described above, it was 10 μm or more and 100 μm or less.
By repeating the above-described layer forming process using the binder solution and the slick material, a layer structure in which eight slick material-containing layers are laminated is formed on the surface of the solid agent, and the oral solution of Example 1 is used. Agent was obtained. In this oral preparation, the entire surface of the solid preparation is covered with a coating having the above-mentioned layer structure. The thickness of the coating (layer structure) was 200 μm. The amount of the slimming material in the oral preparation was 3% by mass, and the dry mass of the binder in the oral preparation was 0.1% by mass.

[Comparative Example 1]
The uncoated tablet was used as an oral preparation without any treatment.

[Evaluation]
Twenty healthy adults were randomly selected as subjects. These 20 subjects took the oral preparation of Example 1 and the oral preparation of Comparative Example 1 with water, respectively. After that, 20 persons were asked which of the oral preparations of Example 1 and Comparative Example 1 was easier to drink, and all 20 persons answered that the oral preparation of Example 1 was easier to drink.

  From the above results, it is clear that the oral preparation of the present invention having a coating structure including a slick material-containing layer in which a powdery slick material is fixed with a binder can be smoothly swallowed and has high swallowability.

[Example 2-1]
(Layer forming step)
An uncoated tablet consisting of maltose, cellulose, calcium stearate and silicon dioxide was used as a solid preparation. One uncoated tablet weighed 250 mg, a diameter of 8 mm, and a thickness of 5.0 mm. Liquid sugar as a binder ("fructose glucose liquid sugar", solid content 75% by mass, composition in solid content is glucose 37% by mass (based on solid content), fructose 55% by mass (based on solid content), and oligosaccharides as other components Was used in an amount of 6% by mass (based on solid content), and the other components were used in an amount of 2% by mass (based on solid content). Starch was used as a slimming material.
The binder was coated on uncoated tablets using a pan-type coating machine. The slick material was then applied before drying the coating. Thereafter, the coating was dried to form a single layer of the slick material-containing layer. This step was repeated six times, and a layer structure in which six layers of the sliming material were laminated was formed on the surface of the solid agent. Thus, the oral preparation of Example 2-1 was obtained. In this oral preparation, the entire surface of the solid preparation is covered with a coating having the above-mentioned layer structure. The thickness of the coating (layer structure) measured by the above method, the amount of the slimming material in the oral preparation, the dry mass of the binder in the oral preparation, the amount of the slicking material in the coating (layer structure), and the amount of the coating (layer structure) Table 1 also shows the dry mass of the binder and the amount (parts by mass) of the sliming material based on 100 parts by mass of the dry mass of the binder in the coating.

[Examples 2-2 and 2-3]
An oral preparation was obtained in the same manner as in Example 2-1 except that the components shown in Table 1 were used in the amounts shown in Table 1 as slimming materials.

[Examples 2-4 to 2-13, Comparative Examples 2-2 to 2-4]
As the slimming material, the components shown in Table 1 were used in the amounts shown in Table 1. A slimming material-containing raw material was prepared by mixing the slimming material and the components and amounts of sugar alcohols shown in Table 1. An oral preparation was obtained in the same manner as in Example 2-1 except that this raw material containing a slimming material was used instead of a slimming material consisting of starch, which was adhered to a binder coating before drying. However, in Examples 2-10 to 2-13, the number of layers of the sliming material-containing layer was changed as shown in Table 1. In Comparative Examples 2 and 4, a 3% by mass aqueous solution of pullulan was used as a binder instead of liquid sugar.

[Examples 2-14 to 2-17]
As the slimming material, the components shown in Table 1 were used in the amounts shown in Table 1. A slimming material-containing raw material was prepared by mixing the components and amounts of sugar alcohols and additives shown in Table 1 with a slimming material. An oral preparation was obtained in the same manner as in Example 2-1 except that this raw material containing a slimming material was used instead of a slimming material consisting of starch, which was adhered to a binder coating before drying. As an additive, in Example 2-14, 0.0345 parts by mass of the sweetener in Table 1 contained 0.3 parts by mass of aspartame (0 parts by mass with respect to 100 parts by mass of the total amount of starch, xanthan gum, and locust bean gum). .447 parts by mass) and 0.045 parts by mass of sucralose (0.06705 parts by mass with respect to 100 parts by mass of the same total amount). In Example 2-15, citric acid was used as 1.0 part by mass of acidulant in Table 1 (1.5 parts by mass with respect to 100 parts by mass of starch and its derivative, xanthan gum, and locust bean gum). Using. In Example 2-16, grapefruit flavor was used as 3 parts by mass of the fragrance in Table 1 (4.5 parts by mass with respect to 100 parts by mass of the total amount of starch, xanthan gum, and locust bean gum). Further, in Example 2-17, cellulose was used as 10 parts by mass of the water-guiding agent (15 parts by mass with respect to 100 parts by mass of the total amount of starch, xanthan gum, and locust bean gum).

[Comparative Example 2-1]
The uncoated tablet used in Example 2-1 was directly used as an oral preparation of Comparative Example 2-1.

<Evaluation>
The oral preparations of Examples 2-1 to 2-17 and Comparative examples 2-1 to 2-4 were evaluated by the following methods. Table 2 shows the results.

● Slope Sliding Speed 150 ml of water was supplied per minute to a U-shaped aluminum channel (linear in side view, channel length 90 cm, width 1 cm) inclined at 30 °. In this state, one oral preparation was slid and flowed from a position 10 cm below the upper end of the channel, and the time required to slide 80 cm to the lower end was measured. The test was performed three times, and the average value of the three times was evaluated according to the following evaluation criteria.
Within 2 seconds: 3 points over 2 seconds to 2.5 seconds: 2 points over 2.5 seconds to 3 seconds: 1 point over 3 seconds to 3.5 seconds: 0 point over 3.5 seconds to 4 seconds Within: -1 point over 4 seconds to within 4.5 seconds: -2 point over 4.5 seconds: -3 points

● Sensory evaluation Three healthy adults (average age 32 years) were randomly selected as subjects. Each of these three subjects was given four oral preparations of each Example and Comparative Example with 50 ml of water. Thereafter, each subject was evaluated for the slipperiness, stickiness, and size of the oral preparation.
・ Evaluation of the ease of slipping is as follows: When the product is swallowed, it is caught when swallowed, and when it is difficult to swallow and it is difficult to swallow, it is rated as the lowest rating (-3 points). The case where it was slippery and easy to drink to the extent that it did not exist was evaluated on a seven-point scale with the highest rating (3 points).
-Stickiness is the lowest rating (-3 points) when it is sticky to the extent that it feels sticking under the tongue and it is difficult to drink, and the highest rating is when it is easy to drink without stickiness and does not stick under the tongue but only to feel slimy ( (3 points).
-Although the size is slimy compared to Comparative Example 2-1, the case where it is large and difficult to drink due to its diameter and thickness is the lowest rating (-3 points), and the case where there is no difference from Comparative Example 2-1 is the highest rating. (3 points).
Table 2 shows the average value of the scores given by the test subjects as evaluation points.

  The evaluation points of the slope sliding speed and the evaluation points related to the sensory evaluation were summed up, and the total evaluation points of the ease of drinking were described in Table 2.

● Production time Regarding the production time, the case where the coating time is as short as the case without the coating is the highest rating (3 points), and the case where the aqueous solution of pullulan is used as the binder (Comparative Example 2-2) requires the same drying time Was evaluated on a 7-point scale with the lowest rating (-3 points).

● Cosmetic The above three subjects visually evaluated the uniformity and dustiness of the surface of the oral preparation.
The lowest rating (-3 points) is when the part where the slimming material is not fixed is visible and the surface is uneven and dusty enough to cause the peeled powder to adhere to the bag surface when placed in the bag. The highest evaluation (3 points) is given when the entire material is uniformly coated with the slicking material and when the bag is put into a bag, it is so uniform that there is no adherence of the peeled powder on the bag surface. It was evaluated on a graded scale. Table 2 shows the average value of the scores given by the test subjects as evaluation points.

  As is clear from the description in Table 2, each of the examples is excellent in the slope sliding speed, and has a high effect of the ease of drinking in terms of sensory evaluation, particularly in terms of slippage and stickiness. In particular, Example 2-4 contains 50 parts by mass of xanthan gum and 50 parts by mass of locust bean gum, based on 100 parts by mass of starch, and further contains 100 parts by mass of reduced maltose in the coating (in the layer containing the components). , With 6 layers of coating, better slope sliding speed than other examples, especially in sensory evaluation, high effect of ease of drinking in terms of slip, stickiness, etc., and the highest overall evaluation ing. Further, in Examples 2-14 to 17, the coating of Example 2-4 in the coating (in the layer containing the slimming component) was coated with six layers containing any of a sweetener, an acidifier, a flavor, and cellulose. Although the slope sliding speed is slightly inferior to that of Example 2-4, the overall evaluation is the highest as in Example 2-4. On the other hand, it can be seen that Comparative Examples 2 to 4 containing no specific sliding material or using pullulan as a binder are strongly sticky, inferior in slipperiness, and inferior in ease of drinking.

Reference Signs List 1 oral preparation 2 binder 3 solid preparation 4 slimming material 5 slicking material containing layer 6 layer structure

Claims (2)

An oral preparation in which powdery xanthan gum and / or locust bean gum is fixed on a surface of a solid preparation with a binder (excluding pullulan) ,
An oral preparation, wherein the binder contains at least one saccharide selected from fructose, glucose, sucrose, maltose and lactose. An oral preparation (thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate) in which powdery xanthan gum and / or locust bean gum is fixed on the surface of a solid preparation with a binder (excluding pullulan). , Polyvalent metal compounds, and oral preparations coated with a coating composition comprising sucralose).