Coated solid preparation, coating composition, and method for improving ease of ingestion of solid preparation

Abstract

To provide easy-to-take coated solid preparations simply and inexpensively.SOLUTION: In order to solve the above problems, a coated solid preparation is provided in which the surface of the solid preparation is coated with a coating layer, the coating layer containing the following components (A) and (B): (A) one or more thickening polysaccharides selected from pectin, tamarind seed gum, and Tremella fuciformis polysaccharides; and (B) hydroxypropyl methylcellulose or hydroxypropyl cellulose, and the ratio (A / B) of the content of component (A) to the content of component (B) being 1 to 9. This makes it possible to provide a coated solid preparation with improved ease of ingestion in a simple and inexpensive manner.SELECTED DRAWING: Figure 1

Description

Technical Field

[0001] The present invention relates to a coated solid preparation for easy administration, a coating composition for coating the same, and a method for improving the ease of administration of a solid preparation.

Background Art

[0002] Pharmaceuticals and supplements are formulated with various active ingredients to exert their medicinal effects, and the formulations may be devised or contain many functional components so that these active ingredients can obtain appropriate efficacy in the body. However, for the purpose of adding high value, increasing the content of such functional components or devising the formulation may increase the diameter and thickness of the formulation, making it more likely to get stuck in the throat and thus more difficult to swallow. As a result, there has been a problem that it causes a decrease in compliance especially in patients with difficulty in swallowing and middle-aged and elderly consumers with declining swallowing function, and at the same time becomes a factor in reducing the market value as a product.

[0003] In response to such problems, Patent Document 1 discloses a fast-disintegrating gel film comprising an undercoat containing a water-soluble polymer and a gel coat containing a polymer that gels upon contact with moisture. Patent Document 2 discloses an oral preparation in which a liquid binder is coated on the surface of a solid agent, and then a slimy material-containing layer improves swallowability by attaching starch, xanthan gum, and roasted bean gum, which are slimy materials. Patent Document 3 discloses a tablet in which a gelling agent and one or more selected from sugar alcohols, monosaccharides, disaccharides, oligosaccharides, cellulose, cellulose derivatives, starch, starch derivatives, and starch degradation products are added to a naked tablet to improve swallowability.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

Patent Document 3

Summary of the Invention

Problems to be Solved by the Invention

[0005] However, in the methods of Patent Documents 1 and 2 shown above, although improvement in swallowability is observed, formation of a plurality of layer structures and formation of a binder layer as a pretreatment are required. As a result, there are problems such as an increase in the size of the tablets and an increase in cost due to an increase in special equipment and processes. On the other hand, when the configuration is a non-coated tablet without providing a coating layer as in Patent Document 3, as a result, the content of additives increases, and there are problems such as a limitation in the degree of freedom in formulation design in terms of increasing the size of the formulation and imparting added value. An inexpensive and simple method for improving the ease of taking solid preparations has not been established.

[0006] Therefore, an object of the present invention is to provide a coated solid preparation that is easy to take in a simple and inexpensive manner.

Means for Solving the Problems

[0007] As a result of intensive studies on the above problems, the present inventors have found that, as a coating composition for coating a solid preparation, a coating layer is coated on the surface of the solid preparation using a coating composition containing a specific thickening polysaccharide and hydroxypropylmethylcellulose or hydroxypropylcellulose in a specific ratio, thereby obtaining a preparation having appropriate slipperiness, no catching in the throat, and being easy to take. At the same time, since only general additives are added, it is possible to provide a coated solid preparation that is inexpensive, simple, and has improved ease of taking without requiring special facilities, and the present invention has been completed.

[0008] That is, the present invention provides the following [1] to [7]. [1] A coated solid preparation in which a coating layer is coated on the surface of a solid preparation, The coating layer contains the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and chondrus ocellatus polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose A coated solid preparation, characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9. According to the present invention, by coating the surface of a solid preparation with a coating layer using a coating composition containing a specific thickening polysaccharide and hydroxypropylmethylcellulose or hydroxypropylcellulose in a specific ratio, a coated solid preparation with improved ease of administration can be simply and inexpensively provided. [2] The coated solid preparation according to [1], characterized in that the content of the coating layer is 0.5 to 5 parts by mass with respect to 100 parts by mass of the solid preparation. According to this feature, even when the content of the coating layer in the coated solid preparation is small, a coated solid preparation with improved ease of administration of the coated solid preparation can be simply and inexpensively provided. [3] The coated solid preparation according to [1] or [2], characterized in that the coating layer contains 20% by mass or more of component (A) and 10% by mass or more of component (B). According to this feature, by satisfying specific lower limit values for component (A) and component (B) in the coating layer, a solid composition having sufficient ease of administration can be simply and inexpensively provided more reliably as a coated solid preparation. [4] The coated solid preparation is a tablet or a capsule, The size of the tablet is such that the diameter is 7 to 10 mm in the round shape, the major axis is 10 to 25 mm in the caplet shape, or the size of the capsule is such that it is No. 2 to No. 000 in the hard capsule and the major axis is 10 to 15 mm in the soft capsule. The coated solid preparation according to any one of [1] to [3]. According to this feature, by limiting the size of the coated solid preparation, a coated solid preparation with further improved ease of administration can be provided. [5] It contains the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and jellyfish polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose A coating composition, characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9. According to the present invention, by coating the surface of a solid preparation with a coating layer using a coating composition containing a specific thickening polysaccharide and hydroxypropylmethylcellulose or hydroxypropylcellulose in a specific ratio, a coated solid preparation with improved ease of administration can be simply and inexpensively provided. [6] The coating composition according to [5], characterized in that the coating composition contains 20% by mass or more of component (A) and 10% by mass or more of component (B). According to this feature, by satisfying the lower limit values of component (A) and component (B) in the coating layer, a solid composition having sufficient ease of administration can be more reliably provided as a coated solid preparation simply and at low cost. [7] A method for improving the ease of administration of a solid preparation, comprising: providing a coating layer on the surface of the solid preparation, wherein the coating layer contains the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and jellyfish polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose A method for improving the ease of administration of a solid preparation, characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9. According to the present invention, by coating a coating layer on the surface of a solid preparation using a coating composition containing a specific thickening polysaccharide and hydroxypropylmethylcellulose or hydroxypropylcellulose in a specific ratio on the surface of the solid preparation, a method can be provided for easily and inexpensively improving the ease of taking the solid preparation.

Effects of the Invention

[0009] According to the present invention, a coated solid preparation that is easy to take can be provided simply and inexpensively.

Brief Description of the Drawings

[0010]

Figure 1

Modes for Carrying Out the Invention

[0011] Hereinafter, the coated solid preparation, coating composition, solid preparation, coating method of the solid preparation, coated tablet and its manufacturing method, and method for improving the ease of taking of the solid preparation of the present invention will be described.

[0012] [Coated Solid Preparation] The coated solid preparation of the present invention is characterized in that the surface of the solid preparation is coated with the coating composition of the present invention. That is, the coated solid preparation of the present invention comprises a solid preparation and a coating layer of the coating composition of the present invention on its surface. According to this coated solid preparation, a coated solid preparation with improved ease of taking can be provided simply and inexpensively.

[0013] The content of the coating composition (coating layer) relative to the weight of the solid preparation is not particularly limited, and is, for example, 0.02 to 20 parts by mass as the parts by mass of the coating composition relative to 100 parts by mass of the solid preparation. As the lower limit, it is more preferably 0.5 part by mass or more, and even more preferably 1 part by mass or more. On the other hand, as the upper limit, it is more preferably 10 parts by mass or less, even more preferably 5 parts by mass or less, and particularly preferably 3 parts by mass or less. By preparing the content of the coating composition relative to the weight of the solid preparation within the above range, the coated solid preparation can be miniaturized, and at the same time, the effect of improving the ease of administration can be more reliably exerted.

[0014] The content of one or more thickening polysaccharides selected from component (A) pectin, tamarind seed gum, and chondrus ocellatus polysaccharide relative to the weight of the solid preparation is not particularly limited, and is, for example, 0.01 to 18 parts by mass as the parts by mass of component (A) relative to 100 parts by mass of the solid preparation. As the lower limit, it is more preferably 0.1 part by mass or more, and even more preferably 0.2 part by mass or more. On the other hand, as the upper limit, it is preferably 5 parts by mass or less, more preferably 2.5 parts by mass or less, and even more preferably 2 parts by mass or less. By preparing the content of component (A) relative to the weight of the solid preparation within the above range, a coated solid preparation with improved ease of administration can be provided.

[0015] The content of component (B) hydroxypropylmethylcellulose or hydroxypropylcellulose relative to the weight of the solid preparation is not particularly limited, and is, for example, 0.01 part by mass to 15 parts by mass as the parts by mass of component (B) relative to 100 parts by mass of the solid preparation. As the lower limit, it is more preferably 0.1 part by mass or more, and even more preferably 0.2 part by mass or more. On the other hand, as the upper limit, it is preferably 5 parts by mass or less, more preferably 2 parts by mass or less, and even more preferably 1 part by mass or less. By preparing the content of component (B) with respect to the weight of the solid preparation to be within the above range, a coated solid preparation with improved ease of administration can be provided.

[0016] The size of the coated solid preparation can be changed depending on the shape of the solid preparation, the purpose of administration, etc., and is not particularly limited. However, in the case of a tablet, for example, in the case of a round shape, the diameter is 3 to 25 mm. As the lower limit value, it is more preferably 5 mm or more, and even more preferably 7 mm or more. On the other hand, as the upper limit value, it is more preferably 20 mm or less, even more preferably 15 mm or less, and particularly preferably 10 mm or less. On the other hand, for example, in the case of a capsule shape, the major axis is 5 to 30 mm. As the lower limit value, it is more preferably 10 mm or more, and even more preferably 13 mm or more. On the other hand, as the upper limit value, it is more preferably 25 mm or less, and even more preferably 20 mm or less.

[0017] The thickness in the case of a tablet is not particularly limited, and is, for example, 1.0 to 10 mm. As the lower limit value, it is more preferably 1.5 mm or more, even more preferably 2.0 mm or more, and particularly preferably 2.5 mm or more. On the other hand, as the upper limit value, it is more preferably 8 mm or less, even more preferably 6 mm or less.

[0018] The size of the capsule preparation is not particularly limited. However, for example, in the case of a hard capsule, it is No. 2 to No. 000. For example, in the case of a soft capsule, the major axis is 5 to 20 mm. As the lower limit value, it is more preferably 10 mm or more. On the other hand, as the upper limit value, it is more preferably 15 mm or less. By setting the size, thickness of the tablet, and size of the capsule preparation within the above range, a coated solid preparation that is easier to administer can be obtained.

[0019] [Coating composition] The coating composition of the present invention is a coating composition for coating solid preparations, which contains at least one thickening polysaccharide selected from pectin, tamarind seed gum, and chondrus ocellatus polysaccharide as component (A) and hydroxypropyl methylcellulose or hydroxypropylcellulose as component (B), and is characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9. First, the components contained in the coating composition used in the present invention will be described in detail.

[0020] <Component (A) Thickening Polysaccharide> The thickening polysaccharide which is component (A) of the present invention is at least one thickening polysaccharide selected from pectin, tamarind seed gum, and chondrus ocellatus polysaccharide. Here, there are no particular limitations on the pectin, tamarind seed gum, and chondrus ocellatus polysaccharide that can be used in the present invention. Hereinafter, these thickening polysaccharides will be described in detail.

[0021] (Pectin) Pectin is generally a polysaccharide extracted from citrus fruits, and is a polygalacturonic acid in which D-galacturonic acid residues are linked by α-1,4 bonds, and refers to a group of polysaccharides in which a part of the carboxyl groups are methyl esterified at various ratios. Pectin is classified into high-methoxyl pectin and low-methoxyl pectin according to the ratio of its degree of methyl esterification. Generally, pectin in which 50% or more of the carboxylic acid groups are esterified with methyl alcohol is called high-methoxyl pectin (hereinafter, also referred to as HM pectin), while pectin in which less than 50% of the carboxylic acid groups are esterified with methyl alcohol is called low-methoxyl pectin (hereinafter, also referred to as LM pectin). In the present invention, either the above-mentioned high-methoxyl pectin or low-methoxyl pectin may be used, and these may be mixed and used in any formulation. Also, its DM value is not particularly limited. These pectins can be commercially available products that are distributed on the market in addition to those manufactured industrially.

[0022] (Tamarind Seed Gum) Tamarind seed gum is a neutral polysaccharide whose main chain is composed of glucose and whose side chains are composed of xylose and galactose, and it has a molecular weight of about 470,000. Generally, it can be obtained by hot water extraction or extraction with an alkaline aqueous solution from the endosperm part of the seeds of the leguminous plant tamarind, followed by powdering. In addition, the tamarind seed gum in the present invention can also be used by mixing two or more kinds having different physical property values and properties in an arbitrary formulation. Note that the tamarind seed gum of the present invention can be industrially manufactured or commercially available products on the market can also be used.

[0023] (White jellyfish polysaccharide) White jellyfish polysaccharide can be obtained by extracting from the fruiting body of the basidiomycete white jellyfish (scientific name: Tremella fuciformis) of the family Tremellaceae with water, ethanol, butylene glycol, or a mixed solution thereof. The structure of this white jellyfish polysaccharide is an acidic complex polysaccharide with a molecular weight of 800,000 to 1,000,000, having a repeating unit structure in which D-fucose, D-xylose, and D-glucuronic acid are bonded to the side chain in a composition ratio of 1:4:3 with respect to the main chain in which 9 mannoses are linked by α-1,3 bonds as a representative structure. In addition, the white jellyfish polysaccharide in the present invention can also be used by mixing two or more kinds having different physical property values and properties in an arbitrary formulation. Note that these white jellyfish polysaccharides can be industrially manufactured or commercially available products on the market can also be used.

[0024] The content of component (A) in the coating composition of the present invention is not particularly limited. For example, it is 5 to 90% by mass based on the total amount of the coating composition. The lower limit is not particularly limited, but 10% by mass or more is more preferable, 20% by mass or more is further preferable, 30% by mass or more is particularly preferable, and 40% by mass or more is most preferable. On the other hand, the upper limit is not particularly limited, but 80% by mass or less is more preferable, and 70% by mass or less is further preferable. By setting the content of component (A) in the coating composition within the above range, the effect of improving the ease of taking of the coating solid preparation of the present invention can be more surely achieved, and at the same time, the miniaturization of the coated solid preparation becomes easy.

[0025] <Hydroxypropyl methylcellulose or hydroxypropyl cellulose> The hydroxypropyl methylcellulose (hereinafter also referred to as "HPMC") that can be used in the present invention is not particularly limited. Hydroxypropyl methylcellulose is a non-ionic polymer in which a part of the hydroxyl groups of methylcellulose is etherified and hydroxypropyl groups are bonded. Also, the hydroxypropyl cellulose (hereinafter also referred to as "HPC") that can be used in the present invention is not particularly limited. Hydroxypropyl cellulose is a non-ionic polymer in which a part of the hydroxyl groups of cellulose is etherified and hydroxypropyl groups are bonded.

[0026] In addition, the viscosity, the number of bonded hydroxypropyl groups, and the molecular weight of the hydroxypropyl methylcellulose or hydroxypropyl cellulose used in the present invention are not particularly limited. Furthermore, the hydroxypropyl methylcellulose or hydroxypropyl cellulose of the present invention may be used alone with the same viscosity, number of bonded hydroxypropyl groups, molecular weight, etc., or two or more kinds with different viscosities, numbers of bonded hydroxypropyl groups, molecular weights, etc. may be combined and used in any formulation. These hydroxypropyl methylcellulose or hydroxypropyl cellulose can be industrially manufactured, or commercially available products on the market can also be used.

[0027] The content of hydroxypropyl methylcellulose or hydroxypropyl cellulose in the coating composition is not particularly limited and can be changed according to the content of component (A), the administration target of the preparation, the purpose of use, etc. For example, it is 3 to 50% by mass. As the lower limit value, it is preferably 10% by mass or more, more preferably 15% by mass or more, and still more preferably 20% by mass or more. On the other hand, as the upper limit value, it is preferably 45% by mass or less, more preferably 40% by mass or less. By setting the content of hydroxypropylmethylcellulose or hydroxypropylcellulose in the coating composition within the above range, the effect of improving the ease of administration of the coating solid preparation of the present invention can be more surely achieved, and at the same time, the miniaturization of the coated solid preparation becomes easy.

[0028] Furthermore, it is more preferable that the contents of component (A) and component (B) as described above simultaneously satisfy any lower limit value or upper limit value. For example, as the lower limit value, containing 3% by mass or more of component (A) and 5% by mass or more of component (B), containing 20% by mass or more of component (A) and 10% by mass or more of component (B), etc. can be mentioned. On the other hand, as the upper limit value, for example, containing 90% by mass or less of component (A) and 50% by mass or less of component (B), containing 80% by mass or less of component (A) and 45% by mass or less of component (B), etc. can be mentioned. By satisfying both the lower limit value or upper limit value of component (A) and component (B), the effect of improving the ease of administration of the coated solid preparation of the present invention is more surely exhibited.

[0029] (Ratio of the content of component (A) to the content of component (B)) The coating composition of the present invention is characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9. As the lower limit value, it is more preferably 1.5 or more, and further preferably 2 or more. On the other hand, as the upper limit value, it is more preferably 8 or less, and more preferably 7.5 or less. By setting the ratio (A / B) of the content of component (A) to the content of component (B) in the coating composition within the above range, a coated solid preparation with appropriate smoothness, no catching in the throat, and easy to swallow, with improved ease of administration, can be easily and inexpensively provided. Furthermore, the unique flavor that HPMC has when blended alone is improved to such an extent that it is hardly felt at all.

[0030] <Other components> In addition to component (A) pectin, tamarind seed gum, and jellyfish polysaccharide, and component (B) hydroxypropylmethylcellulose or hydroxypropylcellulose, the coating composition of the present invention may contain other components as necessary within a range that does not affect the effects of the present invention. Specific examples of the components to be added include, for example, zein, plasticizers, flavoring substances, coloring agents, and the like.

[0031] Zein is a type of corn protein and is extracted with alcohol. By adding zein, the strength of the coating layer can be increased. In addition, functions such as the barrier property against moisture, the sustained release property of the active ingredient, and enteric solubility can be improved. By adding a plasticizer, the flexibility of the coating composition can be adjusted and the coating performance can be improved.

[0032] Moreover, the form of applying the coating composition of the present invention is not particularly limited, and may be, for example, a powder, a solution, or a suspension. When in the form of a solution, it is preferably an aqueous ethanol solution dissolved in a mixed solvent of ethanol and water. Note that the description of the content of each component in the coating composition indicates the content as a solid content.

[0033] [Coating Method] The coating method of the present invention is characterized by coating a solid preparation with the coating composition of the present invention. According to this coating method for the solid preparation, a coating method with excellent coating performance can be provided.

[0034] The specific means of the coating method of the present invention is not particularly limited, but includes, for example, the following steps. Step (I): A step of preparing a coating solution in which the coating composition is dissolved or dispersed. Step (II): A step of applying the coating solution to the solid preparation. Step (III): A step of drying the solid preparation.

[0035] Step (I) is a step of preparing a coating solution in which the coating composition of the present invention is dissolved or dispersed. The coating solution is preferably a solution in which the coating composition is dissolved. By using a solution, a dense coating layer can be formed.

[0036] The liquid for dissolving or dispersing the coating composition is not particularly limited as long as spray injection for coating is possible, and examples thereof include water, alcohols such as ethanol, organic solvents such as hexane, ethyl acetate, and isopropyl alcohol, or a mixture thereof. From the viewpoint of easy dissolution of the coating composition, water, ethanol, or an aqueous ethanol solution obtained by mixing water and ethanol can be preferably used.

[0037] The content of the coating composition in the coating solution is not particularly limited, and is, for example, 0.1% by mass or more and 90% by mass or less. As the lower limit value, it is preferably 1% by mass or more, more preferably 3% by mass or more, still more preferably 5% by mass, and particularly preferably 10% by mass or more. On the other hand, as the upper limit value, it is preferably 70% by mass or less, more preferably 50% by mass, still more preferably 40% by mass or less, and particularly preferably 30% by mass or less. By setting the content of the coating composition in the coating solution within the above range, a thin and uniform coating layer can be formed on the surface of the solid preparation.

[0038] Step (II) is a step of applying the coating solution to the solid preparation. The means for application is not particularly limited, and examples thereof include a means of applying by spraying the coating solution onto the surface of the solid preparation using a sprayer or the like, a means of applying by pouring the coating solution over the surface of the solid preparation, a means of applying by immersing the solid preparation in the coating solution, and a means of applying the coating solution onto the surface of the solid preparation using an applicator such as a brush. Since a dense coating layer can be formed with a thin film, a means of applying by spraying the coating solution onto the surface of the solid preparation is preferable.

[0039] Step (III) is a step of drying the solid preparation coated with the coating liquid. The means for drying is not particularly limited, and examples thereof include means for drying by heating, means for drying by dehumidified air, means for drying by natural drying, and the like. From the viewpoint of shortening the drying time, means for drying by heating and means for drying by dehumidified air are more preferable. More preferably, it is means for drying by dehumidified and heated air.

[0040] The coating method of the present invention is not particularly limited, and for example, conventionally known coating means such as a pan coating method, a fluidized coating method, and a rolling coating method can be used. The spraying device attached to a pan coating device, a drum type coating device, etc. used in these coating methods may be an air spray type or an airless spray type or the like.

[0041] [Solid preparation] The solid preparation may be any article as long as it is coated with the coating composition of the present invention, and the size and shape are not limited. For example, tablets, powders, granules, fine granules, pills, troches, capsules, etc. can be mentioned. Regarding capsules, they may be hard capsules, soft capsules, microcapsules, etc. From the viewpoint of easily forming a coating layer, a tablet is preferable.

[0042] The shape of the tablet is not particularly limited, and examples thereof include circular tablets, oval tablets, flower-shaped tablets, etc. Further, the tablet can be provided with one to two lines for dividing it into two or four parts as needed.

[0043] Additives such as active ingredients, excipients, binders, disintegrants, lubricants, stabilizers, preservatives, fluidizing agents, coloring agents, etc. may be blended in the solid preparation as needed. Further, pectin, tamarind seed gum, silkworm polysaccharide, and other thickening polysaccharides other than hydroxypropylmethylcellulose or hydroxypropylcellulose may be blended within the range where the effects of the present invention are exhibited.

[0044] The active ingredient is not particularly limited and is, for example, a pharmaceutical ingredient, a quasi-drug, an OTC drug, a Chinese herbal medicine, a crude drug, a cosmetic, a health food, a supplement, a veterinary drug, etc., such as a pharmaceutical component, a functional component, etc. used in these. Specific examples of the pharmaceutical component and the functional component include, for example, a lipid regulator, an antidiabetic agent, an appetite suppressant, an antihypertensive agent, a vasodilator, a β-adrenergic receptor blocker, a cardiac ion channel agent, an antiarrhythmic agent, an anticoagulant, a hemostatic agent, an anti-inflammatory agent, an analgesic, an anti-allergic agent, an immunosuppressant, a corticosteroid, a steroid, an antitumor agent, a sympathetic nerve stimulant, a parasympathetic nerve stimulant, an anti-muscarinic agonist, a dopamine agonist, an antidiarrheal agent, an antiemetic agent, a sedative, an astringent, a psychotropic agent, an antidepressant, an antiepileptic agent, an antianxiety agent, a hypnotic, a stimulant, a bronchodilator, an antitussive agent, a diuretic, a muscle relaxant, a bisphosphonate, an antibiotic, an antiviral agent, a diagnostic agent, an imaging diagnostic agent, a radiopharmaceutical, etc. Further, these pharmaceutical components and functional components may be formulated alone or in combination of two or more.

[0045] Other additives include solubilizing agents, surfactants, emulsifiers, antioxidants, brightening agents, foaming agents, moisture-proof agents, preservatives, sweeteners, flavoring agents, cooling agents, perfume agents, fragrances, aromatic agents, disintegration aids, etc. Further, these additives may be formulated alone or in combination of two or more.

[0046] [Coating layer] The coating layer is a film portion formed by applying or spraying the coating composition of the present invention on the surface of a solid preparation.

[0047] The film thickness of the coating layer in the coated solid preparation of the present invention is not particularly limited and is, for example, 1 μm to 1000 μm. As the lower limit value, it is more preferably 3 μm or more. On the other hand, as the upper limit value, it is more preferably 500 μm or less. By setting the film thickness of the coating layer within the above range, it is possible to easily miniaturize the coated solid preparation and make it easy to take.

[0048] In addition, for the coated solid preparation of the present invention, another coating layer may be formed on the lower layer or the upper layer of the coating layer. Examples of the another coating layer include sugar coating, gelatin coating, enteric coating, and the like. However, from the viewpoints of simplification and cost reduction of the present invention, it is preferably a single-layer structure. By containing two common types of additives in specific ratios as additives, the coated solid preparation of the present invention can improve the ease of taking even if the coating layer is a single layer, and at the same time, can realize miniaturization of the preparation and inexpensive and simple provision.

[0049] [Method for manufacturing a coated solid preparation] The method for manufacturing the coated solid preparation of the present invention is characterized by coating a solid preparation with the coating composition of the present invention. The method for manufacturing a coated solid preparation includes the same steps as the coating method of the present invention. However, since this step overlaps with the description of the above coating method, the description is omitted here.

[0050] [Method for manufacturing tablets] The method for manufacturing the tablets of the present invention is not particularly limited. The present invention used as a food or a medicine can be manufactured using known additives acceptable as a food or a medicine, and ordinary formulation techniques employed in the field of food or medicine can be applied.

[0051] For example, there are a method of tableting a mixed powder obtained by mixing various raw materials such as an active ingredient, an excipient, a binder, and a lubricant, and a method of granulating various raw materials by a stirring and mixing granulation method or a fluidized bed granulation method, then adding and mixing a lubricant, and tableting. Note that the timing of adding the components of the tablets is not limited to this.

[0052] The device used for tableting may be a general tableting and forming device such as a rotary tableting machine used for manufacturing tablets. In the case of tablets with a diameter of 6 to 10 mm, the tableting pressure during tableting is preferably 500 to 2000 kgf.

[0053] [Method for improving the ease of taking solid preparations] In the present invention, as another embodiment, a method for improving the ease of taking solid preparations can also be provided. For example, by applying or spraying the coating composition of the present invention containing components (A) and (B) with a ratio of the content of component (A) to the content of component (B) (A / B) of 1 to 9 on the surface of a plain tablet or a capsule, etc., a coating layer is provided, thereby improving the ease of taking the solid preparation. Similarly, by adding components (A) and (B) to the coating composition so as to have a predetermined ratio of the present invention, the ease of taking the coated solid preparation coated with the coating composition can be improved.

Examples

[0054] Hereinafter, examples of the present invention will be described, but the present invention is not limited to only these examples, and various modifications are possible within the technical idea of the present invention.

[0055] (1) Test Example 1 Improvement effect on the ease of taking of coated solid preparations having a coating layer containing pectin and hydroxypropylmethylcellulose or hydroxypropylcellulose A test was conducted on the effect of containing pectin and hydroxypropylmethylcellulose or hydroxypropylcellulose in the coating layer on the ease of taking tablets. More specifically, the coating compositions prepared with the formulations shown in Tables 2 and 3 were coated on plain tablets to produce the coated tablets of Examples 1 to 21, Reference Example, and Comparative Examples 1 to 12, and sensory evaluation was carried out on the subjects from the perspective of the ease of taking the tablets. The raw materials used for the coated tablets according to the examples and comparative examples are shown in Table 1 below.

[0056]

Table 1

[0057] [Manufacture of coated tablets] The coated tablets of Examples 1 to 21, Reference Example, and Comparative Examples 1 to 12 were manufactured by the following procedure.

[0058] <Manufacture of Core Tablets> 31 kg of cellulose (Ceolus UF-F702, manufactured by Asahi Kasei Corporation), 119.35 kg of maltitol (Powdered Maltitol G-3, manufactured by Mitsubishi Corporation Life Sciences Ltd.), 1.55 kg of silicon dioxide (Aerosil 720, manufactured by Fuji Silysia Chemical Ltd.), and 3.1 kg of calcium stearate (Food additive calcium stearate, manufactured by Taihei Chemical Industry Co., Ltd.) were mixed and tableted using a rotary tablet press (AP-15, manufactured by Hata Iron Works Co., Ltd.) with a pestle shape of φ8 mm and R10 and a tableting pressure of 1000 kgf to obtain core tablets in the form of round tablets with a diameter of approximately 8 mm and a granule mass of 270 mg. The core tablets according to Example 13 were manufactured under the same conditions as above, except that the shape of the tablets was a caplet type (major axis: 10 mm).

[0059] <Preparation of Coating Solution> A coating composition mixed in the blending ratios (mass %) of the raw materials shown in Tables 2 and 3 below was dissolved in a solvent adjusted to ethanol:water = 1:5 to obtain coating solutions, respectively. The solid content concentration in the coating solution was appropriately adjusted within the range possible for spray atomization.

[0060] <Coating Process> A coating apparatus DRC-200 (manufactured by Paurec Co., Ltd.) was used. 200 g of the core tablets obtained in the above process were charged into the coating apparatus, and the coating solution was sprayed to obtain coated tablets of Examples 1 to 21, Reference Example, and Comparative Examples 1 to 12.

[0061] [Sensory Evaluation of Ease of Administration] Regarding the manufactured coated tablets, a sensory evaluation was performed by the following method from the viewpoint of the ease of administration of the tablets.

[0062] <Evaluation Criteria for Ease of Administration> Coated tablets with all ○ evaluations in the following three evaluation items were regarded as qualified (Examples). The results are shown in Tables 2 and 3. The coated tablets were evaluated after ingestion together with water.

[0063] (Sliminess) 〇: With sliminess. △: Slightly slimy. ×: No sliminess felt at all.

[0064] (Ease of swallowing) Compared with the shellac-coated tablets (reference example), 〇: Easy to swallow △: Slightly easier to swallow. ×: Equivalent

[0065] (Flavor) Compared with the tablets coated with only HPMC (comparative example 3), 〇: Flavorless. △: Slightly less flavorful. ×: Feeling the same flavor.

[0066]

Table 2

[0067]

Table 3

[0068] <Results> As shown by the results of Examples 1 to 21, the coated solid preparations containing component (A) pectin, tamarind seed gum, or silkworm excrement polysaccharide and component (B) hydroxypropylmethylcellulose or hydroxypropylcellulose with the ratio (A / B) of the content of component (A) to the content of component (B) being 1 to 9 were found to have the highest evaluations in terms of sliminess, ease of swallowing, and flavor, and the ease of taking was significantly improved. Also, as shown in Examples 14 to 18, even when other components, sugar alcohol, reduced indigestible dextrin, dextrin, glycerin, etc. were added, the evaluation was the highest, and the ease of taking was remarkable. Also, as shown in Example 5, Example 9, and Example 10, even when the coating rate (the ratio of the solid content coated on the core tablet) was changed from 2% to 1 - 3%, it was found that the effect of the ease of taking of the coated tablets of the present invention could still be obtained without change. Furthermore, as shown in Examples 11 - 13, even when the diameter, weight, and shape of the tablets were changed, the evaluation of the ease of taking of the coated tablets remained unchanged and was remarkable.

[0069] On the other hand, in Comparative Examples 1 - 4 in which Component (A) or Component (B) was used alone, Comparative Examples 5 - 9 in which other thickening polysaccharides were used, and Comparative Examples 10 - 12 in which the content ratio of Component (A) to Component (B) was outside the scope of the present invention, the sensory evaluation could not meet the criteria of the present invention.

[0070] (2) Test Example 2 Consideration in the Comparative Clinical Trial of the Effect of Improving the Ease of Taking of Coated Solid Preparations A clinical trial was conducted to compare the coated tablets of the formulation of Example 1 with the tablets coated with HPMC3 (Comparative Example 3), which is one of the common coatings, by the following method. The coating rate used was 2% as the solid content based on the core tablets.

[0071] [Sensory Evaluation of Ease of Taking] A sensory test was conducted on 175 healthy subjects who met the following selection criteria according to the evaluation criteria shown below. The size of the core tablets was 8Φ, 10R, thickness 5.16 mm, and 290 mg / granule.

[0072] [Selection Criteria] 1) Japanese men and women 2) 30 years old or older and less than 80 years old 3) Those who ingest tablet - type supplements at least 2 days a week 4) Those who swallow 2 - 6 tablets of tablet - type supplements at the same time when ingesting

[0073] [Exclusion Criteria] 1) Those with a history that affects swallowing function 2) Pregnant or lactating women 3) In addition, those who the trustee has determined to be unqualified as subjects

[0074] <Evaluation method> As a paired comparison method, Comparative Example 3 and Example 1 were each ingested, and the subjects were asked to answer from the following options, considering the one that was easier to ingest as better. Note that the subjects were divided into two groups (Group A: 88 people, Group B: 87 people) so as not to be affected by the order effect due to the order of ingestion, and Group A evaluated in the order of Comparative Example → Example 1, while Group B evaluated in the order of Example 1 → Comparative Example 1.

[0075] -3: Comparative Example 3 is much better -2: Comparative Example 3 is better -1: Comparative Example 3 is slightly better 1: Example 1 is slightly better 2: Example 1 is better 3: Example 1 is much better

[0076] (Analysis method) Analysis was performed by regression analysis using the statistical analysis software JMP.

[0077] As a result of the regression analysis, it was found that there was a significant difference between Comparative Example 3 and Example 1 (p-value 0.0004), and Example 1 was easier to take. Also, when the ease of taking for each was set as -3, -2, -1, 1, 2, 3 (the above answer group), the difference in the ease of taking between Comparative Example 3 and Example 1 was 0.33. Therefore, the ease of taking of Example 1 when the ease of taking of Comparative Example 3 was set as 1 is shown in Figure 1.

[0078] (3) Test Example 3 Examination of the effect in an uncoated solid preparation containing pectin and hydroxypropylmethylcellulose without a coating layer Referring to the above Patent Document 3, the effect of improving the ease of taking was examined in a solid preparation containing pectin and hydroxypropylmethylcellulose and having no coating layer according to the formulation shown in Table 4.

[0079]

Table 4

[0080] As a result, in the configuration where the tablet does not have a coating layer on its surface, even when components (A) and (B) are contained in the tablet body at the ratios within the specific range of the present invention, it was found that the stickiness of the tablet and the ease of swallowing when taken did not meet the criteria and the effects required by the present invention were not achieved.

[0081] [Production Example] Using the formulations of Examples 2 and 3, production tests were conducted with a tablet charge of 60 kg each using a high coater - FZ (HC - FZ - 130 (manufactured by Freund Industry Co., Ltd.)). The coating rate was sprayed so that the solid content was 2% for each tablet. As a result, it was confirmed that production could be carried out without problems even when the production scale was increased.

[0082] As a result of the above - mentioned tests, it was found that by containing components (A) and (B) in a specific ratio in the coating layer of the coated solid preparation coated on the surface of the solid preparation, the ease of taking the solid preparation was significantly improved.

Industrial Applicability

[0083] According to the present invention, in a solid preparation, by containing one or more thickening polysaccharides selected from pectin, tamarind seed gum, and chondrus ocellatus polysaccharide, which are common additives, and hydroxypropylmethylcellulose or hydroxypropylcellulose in the coating layer, a coated solid preparation with improved ease of taking can be easily and inexpensively provided. The present invention can be effectively utilized according to the purpose of use in the design of the composition of solid preparations in various fields such as pharmaceuticals, quasi - drugs, veterinary products, foods, and supplements.

Claims

1. A coated solid preparation in which a coating layer is coated on the surface of a solid preparation, wherein the coating layer contains the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and jellyfish polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The coated solid preparation is characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9.

2. The coated solid preparation according to claim 1, wherein the coating layer contains 20% by mass or more of component (A) and 10% by mass or more of component (B).

3. A coating composition containing the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and jellyfish polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The coating composition is characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9.

4. The coating composition according to claim 3, wherein the coating composition contains 20% by mass or more of component (A) and 10% by mass or more of component (B).

5. A method for improving the ease of taking a solid preparation, wherein a coating layer is provided on the surface of the solid preparation, wherein the coating layer contains the following components (A) and (B), (A) One or more thickening polysaccharides selected from pectin, tamarind seed gum, and jellyfish polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The method for improving the ease of taking a solid preparation is characterized in that the ratio (A / B) of the content of component (A) to the content of component (B) is 1 to 9.

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