Coated solid dosage form, coating composition, method for improving the ease of administration of solid dosage form

Abstract

The present invention aims to provide a coated solid dosage form that is easy to administer and has high manufacturing efficiency, in a simple manner. [Solution] In order to solve the above problem, a coated solid preparation is provided in which the surface of the solid preparation is covered with a coating layer, and the coating layer contains the following components (A) and (B), (A) Tremella fuciformis polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose A coated solid dosage form is provided, characterized in that the ratio (B / A) of the content of component (B) to the content of component (A) is 0.35 to 15. This makes it possible to easily provide a coated solid dosage form with improved ease of administration and manufacturing efficiency.

Description

Technical Field

[0001] The present invention relates to a coated solid preparation coated 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] In pharmaceuticals and supplements, various active ingredients are formulated to exhibit their medicinal effects. In some cases, the formulations are 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, by containing many such functional components or adding ingenuity to the formulation, the diameter and thickness of the formulation increase, making it easier to get stuck in the throat. Also, due to the bitterness and flavor of the added functional components, there is a tendency for it to be difficult to take. As a result, there has been a problem that compliance decreases especially among middle-aged and elderly consumers whose swallowing function has declined, and it also becomes a factor that reduces the market value of the product for general consumers.

[0003] Regarding 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. Further, 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 starch, xanthan gum, and roasted bean gum, which are slimy materials, is adhered to improve the swallowability of the slimy material-containing layer. Also, 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 contained in a naked tablet to improve swallowability.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

[0005] However, while the methods described in Patent Documents 1 and 2 above show improvement in swallowability, they require the formation of multiple layer structures and the formation of a binder layer as a pretreatment, resulting in problems such as larger tablets and increased costs due to the need for special equipment and processes. On the other hand, when a bare tablet is constructed without a coating layer, as in Patent Document 3, the amount of additives increases, resulting in problems such as larger formulations and limitations on the freedom of formulation design in terms of adding value. Therefore, an inexpensive and simple method for improving the ease of taking solid dosage forms has not yet been established.

[0006] In view of these problems, the inventors focused on the potential use of Tremella fuciformis polysaccharide, an extract of Tremella fuciformis, as a component of the coating layer. It was found that Tremella fuciformis polysaccharide does not have the distinctive flavor of HPMC or HPC, which are commonly used as components of coating layers, and does not adhere to mucous membranes, thus enabling the miniaturization of formulations while also being easy to swallow. However, coating with a coating composition using Tremella fuciformis polysaccharide presented a manufacturing problem: the time required for the coating process was prolonged due to its properties such as water solubility and viscosity.

[0007] Therefore, the present invention aims to provide a coated solid dosage form that is easy to take and has high manufacturing efficiency in a simple manner. [Means for solving the problem]

[0008] As a result of diligent research into the above-mentioned problems, the present inventors have discovered that by incorporating hydroxypropyl methylcellulose or hydroxypropyl cellulose in a specific proportion into Tremella fuciformis polysaccharide as a coating composition for coating solid dosage forms, the solid dosage forms coated with this coating composition can have a moderate sliminess, be easy to swallow without getting stuck in the throat, and be easy to take, while simultaneously enabling coating of solid dosage forms with sufficient manufacturing efficiency. Thus, the present invention has been completed.

[0009] In other words, the present invention provides the following [1] to [7]. [1] Solid dosage form most A coated solid dosage form in which the surface is covered with a coating layer, The coating layer contains the following components (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 A coated solid dosage form characterized by being ~15. According to the present invention, by coating the surface of a solid dosage form with a coating layer using a coating composition containing hydroxypropyl methylcellulose or hydroxypropyl cellulose in a specific ratio to Tremella fuciformis polysaccharide, it is possible to easily provide a coated solid dosage form that is easy to take and has high manufacturing efficiency. [2] The coated solid preparation according to [1], characterized in that the content of component (A) Tremella fuciformis polysaccharide in the coating layer is 7 to 70% by mass. According to this feature, by keeping the content of Tremella fuciformis polysaccharide in the coating layer of the coated solid dosage form within a specific range, it is possible to provide a coated solid dosage form that more reliably improves ease of administration and manufacturing efficiency. [3] The coated solid preparation according to [1] or [2], wherein the solid preparation is covered with the single-layer coating layer. [ 4 The coated solid preparation is a tablet or a capsule. The tablets are characterized by having a diameter of 7-10 mm for round tablets, a major axis of 10-25 mm for caplets, or by having a capsule size of 3-000 for hard capsules, or a major axis of 10-15 mm for soft capsules. [1] ~[3] A coated solid preparation as described in any of the following. This feature allows for the provision of coated solid dosage forms that are even easier to administer by limiting their size. [ 5 It contains the following ingredients (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 Characterized by being ~15, For coating the outermost layer of a solid dosage form Coating composition. According to the present invention, by providing a coating composition containing hydroxypropyl methylcellulose or hydroxypropyl cellulose in a specific ratio to Tremella fuciformis polysaccharide, it is possible to easily provide a coated solid dosage form that is easy to take and has high manufacturing efficiency when the coating composition is applied. [ 6 The above-mentioned component (A) Tremella fuciformis polysaccharide content is characterized by being 7 to 70% by mass, 5 The coating composition described in [ ]. According to this feature, by keeping the content of Tremella fuciformis polysaccharide in the coating layer of the coated solid dosage form within a specific range, it is possible to provide a coated solid dosage form to which the ease of administration and manufacturing efficiency of the coated solid dosage form have been more reliably improved. . [ 7 A method for improving the ease of taking solid dosage forms, A coating layer is provided on the surface of the solid dosage form. The coating layer contains the following components (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropylmethylcellulose or hydroxypropylcellulose The ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 ~15, and it is a method for improving the ease of taking solid preparations. According to the present invention, by coating a coating layer on the surface of a solid preparation using a coating composition containing hydroxypropylmethylcellulose or hydroxypropylcellulose in a specific ratio on the surface of the solid preparation with a silkworm chrysalis polysaccharide, it is possible to easily provide a method capable of improving the ease of taking the solid preparation and at the same time enhancing the production efficiency.

Effects of the Invention

[0010] According to the present invention, it is possible to easily provide a coated solid preparation that is easy to take and has high production efficiency.

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 production method, and method for improving the ease of taking 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, it is possible to easily provide a coated solid preparation that is easy to take and has high production efficiency.

[0013] The content of the coating composition (coating layer) relative to the weight of the solid dosage form is not particularly limited, and is, for example, 0.02 to 20 parts by mass of the coating composition per 100 parts by mass of the solid dosage form. The lower limit is more preferably 0.5 parts by mass or more, and even more preferably 1 part by mass or more. On the other hand, the upper limit 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 adjusting the content of the coating composition relative to the weight of the solid dosage form to fall within the aforementioned range, the coated solid dosage form can be miniaturized while simultaneously achieving a more reliable improvement in ease of administration.

[0014] The content of component (A) Tremella fuciformis polysaccharide relative to the weight of the solid dosage form is not particularly limited, and is, for example, 0.002 to 18 parts by mass of component (A) per 100 parts by mass of the solid dosage form. The lower limit is more preferably 0.005 parts by mass or more, and even more preferably 0.1 parts by mass or more. On the other hand, the upper limit 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 adjusting the content of component (A) relative to the weight of the solid dosage form to fall within the aforementioned range, a coated solid dosage form with improved ease of administration can be provided.

[0015] The content of component (B) hydroxypropyl methylcellulose or hydroxypropyl cellulose relative to the weight of the solid preparation is not particularly limited, and is, for example, 0.02 to 20 parts by mass of component (B) per 100 parts by mass of the solid preparation. The lower limit is more preferably 0.1 parts by mass or more, and even more preferably 0.2 parts by mass or more. On the other hand, the upper limit is preferably 8 parts by mass or less, more preferably 3 parts by mass or less, and even more preferably 2 parts by mass or less. By adjusting the content of component (B) relative to the weight of the solid dosage form to fall within the aforementioned range, a coated solid dosage form with improved ease of administration can be provided.

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

[0017] The thickness of the tablet is not particularly limited, for example, 1.0 to 10 mm. The lower limit 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, the upper limit is more preferably 8 mm or less, and even more preferably 6 mm or less.

[0018] While there are no particular restrictions on the size of capsules, for example, hard capsules range from size 3 to 000. For example, soft capsules have a major diameter of 5 to 20 mm. More preferably, the lower limit is 10 mm or more. On the other hand, more preferably, the upper limit is 15 mm or less. By setting the size, thickness, and size of the tablets and capsules within the aforementioned ranges, it is possible to create coated solid dosage forms that are easier to take.

[0019] [Coating composition] The coating composition of the present invention is a coating composition for coating a solid formulation, and is characterized in that it contains Tremella fuciformis polysaccharide as component (A) and hydroxypropyl methylcellulose or hydroxypropyl cellulose as component (B), and the ratio of the content of component (B) to the content of component (A) (B / A) is 0.35 to 15. First, the components contained in the coating composition used in the present invention will be described in detail.

[0020] <Component (A) Tremella fuciformis polysaccharide> This invention contains Tremella fuciformis polysaccharide, a thickening polysaccharide. Tremella fuciformis polysaccharide can be obtained by extraction from the fruiting body of Tremella fuciformis (scientific name: Tremella fuciformis), a basidiomycete of the family Tremellaceae, with water, ethanol, butylene glycol, or a mixture thereof. The structure of this Tremella fuciformis polysaccharide is an acidic complex polysaccharide with a molecular weight of 800,000 to 1,000,000, with a typical structure consisting of a repeating unit in which nine mannose units are linked by α-1,3 bonds, and D-fucose, D-xylose, and D-glucuronic acid are attached to the side chains in a 1:4:3 ratio. Furthermore, in this invention, two or more types of Tremella fuciformis polysaccharide with different physical properties and characteristics can be mixed in any combination. These Tremella fuciformis polysaccharides can be manufactured industrially or commercially available products can be used.

[0021] The content of component (A) Tremella fuciformis polysaccharide in the coating composition of the present invention is not particularly limited, but for example, it is 7 to 70% by mass of the total amount of the coating composition. The lower limit is not particularly limited, but 10% by mass or more is more preferred, 20% by mass or more is even more preferred, 30% by mass or more is particularly preferred, and 35% by mass or more is most preferred. On the other hand, the upper limit is not particularly limited, but 65% by mass or less is more preferred, and 55% by mass or less is even more preferred. By setting the content of component (A) in the coating composition to above the lower limit, the effect of improving the ease of administration of the coated solid dosage form of the present invention can be achieved more reliably. On the other hand, by setting it to below the upper limit, the manufacturing time required for coating the solid dosage form can be shortened, and manufacturing efficiency can be improved. Furthermore, it becomes easier to miniaturize the coated solid dosage form.

[0022] <Ingredient (B) Hydroxypropyl methylcellulose or hydroxypropylcellulose> Hydroxypropyl methylcellulose (hereinafter also referred to as "HPMC") is a nonionic polymer in which some of the hydroxyl groups of methylcellulose are etherified and hydroxypropyl groups are bonded to them. On the other hand, hydroxypropyl cellulose (hereinafter also referred to as "HPC") is a nonionic polymer in which some of the hydroxyl groups of cellulose are etherified and hydroxypropyl groups are bonded to them.

[0023] Furthermore, the number of hydroxypropyl groups, the number of methyl groups, and the molecular weight of component (B) hydroxypropyl methylcellulose or hydroxypropyl cellulose used in the present invention are not particularly limited. The viscosity of component (B) is not particularly limited, but it is preferable that the viscosity at 20°C, with a shear rate of 10 / s and 1 min, when it is a 2% aqueous solution, is 1 to 800 mPa·s. The lower limit of viscosity is more preferably 2 mPa·s or more. On the other hand, the upper limit of viscosity is more preferably 600 mPa·s or less, even more preferably 200 mPa·s or less, particularly preferably 30 mPa·s or less, and most preferably 10 mPa·s or less. By setting the viscosity above the lower limit, appropriate strength and tackiness can be imparted. Furthermore, by setting it below the upper limit, uniformly dispersed spray application becomes possible, and the coating layer can be controlled according to the purpose.

[0024] Furthermore, component (B) hydroxypropyl methylcellulose or hydroxypropyl cellulose of the present invention may be used alone if it has the same viscosity, number of hydroxypropyl groups, molecular weight, etc., or two or more types with different viscosities, number of hydroxypropyl groups, molecular weight, etc., may be used in any formulation. These hydroxypropyl methylcellulose or hydroxypropyl cellulose may be industrially produced or commercially available products on the market.

[0025] The content of component (B) hydroxypropyl methylcellulose or hydroxypropyl cellulose in the coating composition is not particularly limited and can be changed according to the content of component (B), the target of administration of the formulation, the purpose of use, etc., but for example it is 3 to 85% by mass. The lower limit is more preferably 10% by mass or more, even more preferably 15% by mass or more, particularly preferably 25% by mass or more, and most preferably 30% by mass or more. On the other hand, the upper limit is preferably 75% by mass or less, more preferably 65% ​​by mass or less. By setting the content of hydroxypropyl methylcellulose or hydroxypropyl cellulose in the coating composition within the aforementioned range, the effect of improving ease of administration in the coated solid formulation of the present invention can be achieved more reliably, while simultaneously ensuring high manufacturing efficiency and facilitating miniaturization of the coated solid formulation.

[0026] Furthermore, it is more preferable that the content of component (A) and component (B) as described above simultaneously satisfies either the lower limit or the upper limit. For example, the lower limit could be 7% by mass or more of component (A) and 3% by mass or more of component (B), or 30% by mass or more of component (A) and 25% by mass or more of component (B). On the other hand, the upper limit could be 70% by mass or less of component (A) and 85% by mass or less of component (B), or 55% by mass or less of component (A) and 65% by mass or less of component (B). By satisfying both the lower or upper limits of component (A) and component (B), the improvement in ease of administration and the realization of high manufacturing efficiency of the coated solid dosage form of the present invention become more certain.

[0027] (Ratio of the content of component (B) to the content of component (A)) The coating composition of the present invention is characterized in that the ratio of the content of component (A) to the content of component (B) (B / A) is 0.35 to 15. The lower limit is more preferably 0.6 or more, even more preferably 1 or more, and particularly preferably 1.2 or more. On the other hand, the upper limit is more preferably 9 or less, even more preferably 5 or less, and particularly preferably 3 or less. By setting the ratio (B / A) of the content of component (B) to the content of component (A) in the coating composition to the aforementioned range, a coated solid dosage form with an appropriate sliminess, no sticking in the throat, and improved ease of administration can be easily and efficiently manufactured. Furthermore, the unique flavor that HPMC has when formulated alone is improved to the point where it is not noticeable at all.

[0028] (Coating rate) In this invention, the coating rate is calculated as the percentage (by mass) of the coated layer relative to the solid dosage form. This coating rate is not particularly limited and can be changed depending on the dosage form, dissolution method, and raw material composition, but for example, it is 0.5 to 10% by mass. The lower limit is more preferably 1% by mass or more, and even more preferably 1.5% by mass or more. The upper limit is more preferably 5% by mass or less, and even more preferably 3% by mass or less. By satisfying the lower limit, the ease of swallowing can be improved by imparting sufficient slipperiness to the solid dosage form. On the other hand, by satisfying the upper limit, the coated solid dosage form can be made smaller, further improving ease of swallowing.

[0029] (viscosity) The viscosity of the coating composition is not particularly limited, but it is preferable that the viscosity at 20°C when it is a 2% aqueous solution is 700 mPa·s or less as an upper limit. More preferably it is 500 mPa·s or less, even more preferably 400 mPa·s or less, and particularly preferably 300 mPa·s or less. The lower limit is not particularly limited, but for example it is 1 mPa·s or more. By keeping the viscosity below the upper limit, uniformly dispersed spray atomization becomes possible, and at the same time, the spraying speed can be increased, improving manufacturing efficiency. The specific measurement conditions for the viscosity are as follows: when using a Type B viscometer (LVDV3T: manufactured by Eiko Seiki Co., Ltd.), the measurement can be performed using a spindle 62 at 30 rpm for a measurement time of 1 minute. The viscosity of the coating composition in the examples described later was measured under the above measurement conditions.

[0030] <Other ingredients> The coating composition of the present invention may contain, as necessary, other components in addition to component (A) Tremella fuciformis polysaccharide and component (B) hydroxypropyl methylcellulose or hydroxypropylcellulose, provided that they do not affect the effects of the present invention. Specific examples of added components include, for example, zein, plasticizers, flavoring agents, coloring agents, and other thickening polysaccharides.

[0031] Zein is a type of corn protein that is extracted using alcohol. Adding zein can increase the strength of the coating layer. It can also improve functions such as moisture barrier properties, sustained release of active ingredients, and enteric coating. By adding plasticizers, the flexibility of the coating composition can be adjusted, thereby improving its application performance. Other thickening polysaccharides include pectin and tamarind seed gum, which can add value to solid dosage forms, such as providing sustained-release properties.

[0032] Furthermore, the form in which the coating composition of the present invention is applied is not particularly limited, and may be, for example, a powder, a solution, or a suspension. When used in the form of a solution, it is preferably an aqueous ethanol solution prepared by dissolving the composition in a mixed solvent of ethanol and water. The descriptions of the content of each component in the coating composition mentioned above refer to their content as solids.

[0033] [Coating Method] The coating method of the present invention is characterized by coating a solid formulation with the coating composition of the present invention. This coating method for solid formulations provides a coating method with excellent coating performance.

[0034] The specific means of the coating method of the present invention are not particularly limited, but may include, for example, the following steps. Step (I): A step of preparing a coating solution by dissolving or dispersing the coating composition. Process (II): The process of applying the coating solution to the solid formulation (coating process). Process (III): The process of drying the solid dosage form.

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

[0036] The liquid used to dissolve or disperse the coating composition is not particularly limited as long as it allows for spray application for coating, but examples include water, alcohols such as ethanol, organic solvents such as hexane, ethyl acetate, and isopropyl alcohol, or mixtures thereof. From the viewpoint of easily dissolving the coating composition, water, ethanol, or an aqueous ethanol solution (a mixture of water and ethanol) can be preferably used.

[0037] The mixing ratio of ethanol to water in the ethanol aqueous solution is not particularly limited and can be changed by other formulations and coating rates, but for example, ethanol:water is 20:1 to 1:20. More preferably, it is 10:1 to 1:10, and even more preferably 1:1 to 1:5.

[0038] 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. The lower limit is preferably 1% by mass or more, more preferably 3% by mass or more, even more preferably 5% by mass or more, and particularly preferably 10% by mass or more. On the other hand, the upper limit is preferably 70% by mass or less, more preferably 50% by mass or more, even 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 application solution within the aforementioned range, a thin and uniform coating layer can be formed on the surface of the solid dosage form.

[0039] Step (II) is the step of applying the coating solution to the solid formulation (coating step). The means of application are not particularly limited and include, for example, applying the coating solution by spraying it onto the surface of the solid formulation using a sprayer, applying the coating solution by pouring it onto the surface of the solid formulation, applying the coating solution by immersing the solid formulation in the coating solution, and applying the coating solution to the surface of the solid formulation using an application tool such as a brush. Since a thin, dense coating layer can be formed, a method of applying the coating solution by spraying it onto the surface of a solid formulation is preferred.

[0040] (Manufacturing time) In the coating step (II) described above, the manufacturing time (spraying time for spraying the coating solution) is not particularly limited and can be adjusted by the solvent composition, solid content ratio, and coating rate, but for example, it is 5 to 30 minutes. The upper limit is more preferably 20 minutes or less, and even more preferably 15 minutes or less. The lower limit is more preferably 10 minutes or more. By keeping it below the upper limit, it is possible to coat the solid dosage form with sufficient manufacturing efficiency, and by keeping it above the lower limit, it is possible to manufacture a uniform and stable solid dosage form. Furthermore, the manufacturing time is preferably shorter than the manufacturing time when using a coating composition containing only component (A) Tremella fuciformis polysaccharide, and more preferably 0.7 times or less.

[0041] This manufacturing time can be shortened by increasing the ethanol content in the coating solution by keeping the Tremella fuciformis polysaccharide content of the coating layer below a certain level. Furthermore, by keeping the content of the highly viscous Tremella fuciformis polysaccharide below a certain level, the solid content of the coating solution can be increased, resulting in an even more significant reduction in manufacturing time. In this case, by adding hydroxypropyl methylcellulose or hydroxypropyl cellulose in the proportions specified in the present invention, a coated solid dosage form that balances ease of swallowing and manufacturing efficiency can be easily provided.

[0042] Step (III) is a step of drying the solid formulation to which the coating solution has been applied. The means of drying are not particularly limited, but examples include drying by heating, drying with dehumidified air, or drying by natural drying. From the viewpoint of shortening the drying time, drying by heating or drying with dehumidified air is more preferable. Even more preferable is drying by dehumidified and heated air.

[0043] The coating method of the present invention is not particularly limited, and conventionally known coating methods such as pan coating, fluid coating, and rolling coating can be used. The spraying device attached to the pan coating apparatus, drum-type coating apparatus, etc. used in these coating methods may be an air spray type, an airless spray type, etc.

[0044] [Solid Dosage Forms] The solid dosage form can be any article that is coated with the coating composition of the present invention, and its size and shape are not limited. Examples include tablets, powders, granules, fine granules, pills, lozenges, capsules, etc. Capsules may be hard capsules, soft capsules, microcapsules, etc. Tablets are preferred from the viewpoint of ease of forming the coating layer.

[0045] The shape of the tablets is not particularly limited and examples include round tablets, oval tablets, flower-shaped tablets, etc. Furthermore, the tablets may have one or two lines to allow for division into two or four parts, as needed.

[0046] The solid dosage form may contain, as needed, active ingredients and additives such as excipients, binders, disintegrants, lubricants, stabilizers, preservatives, fluidizers, and colorants. Furthermore, to the extent that the effects of the present invention are achieved, Tremella fuciformis polysaccharide and hydroxypropyl methylcellulose or other thickening polysaccharides or cellulose derivatives other than hydroxypropyl cellulose may be added.

[0047] The active ingredients are not particularly limited and include, for example, pharmaceutical ingredients and functional ingredients used in pharmaceuticals, quasi-drugs, over-the-counter (OTC) drugs, herbal medicines, crude drugs, cosmetics, health foods, supplements, veterinary drugs, etc. Specific examples of pharmaceutical and functional ingredients include, for example, lipid regulators, antidiabetic agents, appetite suppressants, antihypertensive agents, vasodilators, β-adrenergic receptor blockers, cardiac ion channel agents, antiarrhythmic agents, anticoagulants, hemostatic agents, anti-inflammatory agents, analgesics, anti-allergic agents, immunosuppressants, corticosteroids, steroids, antitumor agents, sympathomimetic agents, parasympathomimetic agents, antimuscarinic agonists, dopamine agonists, antidiarrheal agents, antiemetic agents, sedatives, astringents, tranquilizers, antidepressants, antiepileptic agents, anxiolytics, hypnotics, stimulants, bronchodilators, antitussives, diuretics, muscle relaxants, bisphosphonates, antibiotics, antiviral agents, diagnostic agents, imaging agents, and radiopharmaceuticals. These pharmaceutical and functional ingredients may be combined individually or in combination of two or more.

[0048] Other additives include solubilizers, surfactants, emulsifiers, antioxidants, glazing agents, foaming agents, moisture-proofing agents, preservatives, sweeteners, flavoring agents, cooling agents, flavoring agents, fragrances, air fresheners, and disintegration aids. These additives may be blended individually or in combination of two or more types.

[0049] [Coating layer] The coating layer is a film portion formed on the surface of a solid formulation by applying or spraying the coating composition of the present invention.

[0050] The thickness of the coating layer in the coated solid formulation of the present invention is not particularly limited, and is, for example, 1 μm to 1000 μm. The lower limit is more preferably 3 μm or more. On the other hand, the upper limit is more preferably 500 μm or less. By setting the thickness of the coating layer within the aforementioned range, it becomes easier to miniaturize the coated solid dosage form and improve its ease of administration.

[0051] Furthermore, the coated solid formulation of the present invention may have another coating layer formed below or above the coating layer. Examples of the other coating layer include sugar coating, gelatin coating, enteric coating, etc. However, from the viewpoint of simplification and cost reduction of the present invention, a single-layer structure is preferable. By containing two commonly used additives in specific ratios, the coated solid formulation of the present invention can improve ease of administration even with a single-layer coating, while simultaneously enabling miniaturization of the formulation and convenient and efficient provision.

[0052] [Method for manufacturing coated solid dosage forms] The present invention provides a method for producing a coated solid formulation, characterized by coating the solid formulation with the coating composition of the present invention. The method for producing coated solid formulations involves the same steps as the coating method of the present invention, but since these steps overlap with the description of the coating method described above, their explanation is omitted here.

[0053] [Method of manufacturing tablets] The method for manufacturing the tablets of the present invention is not particularly limited, and the present invention, when used as a food or pharmaceutical, can be manufactured using known additives that are acceptable as food or pharmaceuticals, and ordinary formulation methods used in the food or pharmaceutical field can be applied.

[0054] For example, methods include compressing a mixed powder containing various raw materials such as active ingredients, excipients, binders, and lubricants into tablets, or granulating the various raw materials using a stirring and mixing granulation method or a fluidized bed granulation method, then adding and mixing a lubricant, and finally compressing the mixture into tablets. The timing of adding the tablet components is not limited to these methods.

[0055] The equipment used for tableting can be any general tableting device, such as a rotary tablet press used in tablet manufacturing. For tablets with a diameter of 6-10 mm, the compression pressure is preferably 500-2000 kgf.

[0056] [Methods to improve the ease of taking solid dosage forms] In the present invention, as another embodiment, a method for improving the ease of administration of solid dosage forms can also be provided. For example, the ease of administration of solid dosage forms can be improved by applying or spraying a coating layer of the coating composition of the present invention, which contains components (A) and (B) such that the ratio (B / A) of component (A) Tremella fuciformis polysaccharide to component (B) is 0.35 to 15, onto the surface of uncoated tablets or capsules. Similarly, the ease of administration of coated solid dosage forms coated with the coating composition can be efficiently improved by adding components (A) and (B) to the coating composition in a predetermined ratio according to the present invention. [Examples]

[0057] The following describes embodiments of the present invention, but the present invention is not limited to these embodiments, and various modifications are possible within the technical concept of the present invention.

[0058] (1) Test Example 1: Effect of improving ease of administration in coated solid preparations having a coating layer containing Tremella fuciformis polysaccharide and hydroxypropyl methylcellulose or hydroxypropyl cellulose. The effect of including Tremella fuciformis polysaccharide and hydroxypropyl methylcellulose or hydroxypropyl cellulose in the coating layer on the ease of swallowing tablets was tested. More specifically, coating compositions prepared with the formulations shown in Table 2 were applied to uncoated tablets to produce coated tablets of Examples 1-8 and Comparative Examples 1-4, and subjective sensory evaluations were conducted on the ease of swallowing the tablets. The raw materials used for the coated tablets in the Examples and Comparative Examples are shown in Table 1 below.

[0059] [Table 1]

[0060] [Manufacturing of coated tablets] Coated tablets of Examples 1-8 and Comparative Examples 1-4 were manufactured using the following procedure.

[0061] <Preparation of uncoated 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 Co., Ltd.)), 1.55 kg of silicon dioxide (Silopage 720 (manufactured by Fuji Silysia Chemical Co., Ltd.)), and 3.1 kg of calcium stearate (food additive calcium stearate (manufactured by Taihei Chemical Industry Co., Ltd.)) were mixed and compressed using a rotary tablet press (AP-15 (manufactured by Hata Iron Works Co., Ltd.)) with a punch shape of φ8 mm and R10, at a compression pressure of 1000 kgf to obtain round tablets with a diameter of approximately 8 mm and a particle mass of 270 mg.

[0062] <Preparation of coating solution> In the examples, coating compositions were prepared by dissolving the raw materials in the mixing ratios (mass%) shown in Table 2 below in a solvent adjusted to ethanol:water = 1:2, and each was prepared as a coating solution. On the other hand, for the comparative examples, similar to the examples, a coating composition was dissolved in a solvent adjusted to ethanol:water = 1:2 (only for Comparative Example 2, ethanol:water = 4:1) at the mixing ratio (mass%) of the raw materials shown in Table 2 below, to obtain the respective coating solutions. The solid content concentration in the coating solution was adjusted as appropriate to allow for spray application.

[0063] <Coating Process> A coating apparatus, DRC-200 (manufactured by Pawrec Co., Ltd.), was used. 200g of the uncoated tablets obtained in the above process were placed in the coating apparatus, and the coating solution was sprayed to obtain coated tablets of Examples 1-8 and Comparative Examples 1-4.

[0064] [Sensory evaluation of ease of administration] The aforementioned coated tablets were subjected to sensory evaluation in terms of ease of swallowing using the following method.

[0065] <Evaluation Criteria for Ease of Administration> Coated tablets that received a "○" rating in both of the following evaluation criteria were considered acceptable. The results are shown in Table 2. The coated tablets were evaluated after being taken with water.

[0066] (Ease of swallowing) Compared to shellac-coated tablets, ○: Easy to swallow △: It feels slightly easier to swallow. ×: Equivalent

[0067] (flavor) Compared to HPMC-coated tablets (Comparative Example 2), ○: No flavor. △: The flavor is slightly subdued. ×: I can taste the same flavor.

[0068] [Manufacturing example] Using the formulations of Examples 1-8 and Comparative Examples 1-4, the manufacturing scale was increased, and production tests were conducted with a Hi-Coater FZ (HC-FZ-130 (manufactured by Freund Industrial Co.)) at a tablet input volume of 200 kg each. The coating rate was sprayed so that the solid content relative to the tablet was as shown in Table 2. Table 2 also shows the manufacturing time (spraying time) for the coating layer in the example manufacturing at this scale.

[0069] [Table 2]

[0070] <Result> As shown in the results of Examples 1 to 8, coated solid formulations containing component (A) white jelly polysaccharide and component (B) hydroxypropyl methylcellulose in a ratio (B / A) of component (A) to component (B) within the range of the present invention received the highest ratings in terms of ease of swallowing and flavor, demonstrating a significant improvement in ease of administration. Furthermore, as shown in Examples 1 to 8, it was found that the manufacturing time could be comparable to that of HPMC alone, achieving the same manufacturing efficiency.

[0071] On the other hand, in Comparative Example 1, which used component (A) alone, and in Comparative Example 4, where the B / A ratio fell below the lower limit of the present invention, the sensory evaluation met the criteria, but the manufacturing time was significantly inferior compared to Comparative Example 2, which used HPMC alone. Furthermore, in Comparative Example 2, which used component (B) alone, and in Comparative Example 3, where the B / A ratio exceeded the upper limit of the present invention, the manufacturing time was equivalent to that of Comparative Example 2, which used HPMC alone, but the sensory evaluation of ease of swallowing did not meet the criteria.

[0072] The results of the aforementioned tests showed that by incorporating components (A) and (B) in a specific ratio within the coating layer of a coated solid dosage form, the ease of administration of the solid dosage form is significantly improved, and at the same time, coated solid dosage forms can be provided with high manufacturing efficiency. [Industrial applicability]

[0073] The present invention makes it possible to efficiently and simply manufacture coated solid dosage forms with improved ease of administration by incorporating Tremella fuciformis polysaccharide and hydroxypropyl methylcellulose or hydroxypropyl cellulose, which are common additives, into the coating layer of solid dosage forms. The present invention can be effectively utilized in the design of the composition of solid dosage forms in various fields such as pharmaceuticals, quasi-drugs, veterinary products, foods, and supplements, depending on the intended use.

Claims

1. A coated solid dosage form in which the outermost surface of the solid dosage form is covered with a coating layer, The coating layer contains the following components (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropyl methylcellulose or hydroxypropylcellulose A coated solid preparation characterized in that the ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 to 15.

2. The coated solid preparation according to claim 1, characterized in that the content of component (A) Tremella fuciformis polysaccharide in the coating layer is 7 to 70% by mass.

3. The coated solid preparation according to claim 1 or 2, wherein the solid preparation is covered with the single-layer coating layer.

4. The coated solid preparation is a tablet or a capsule. The coated solid preparation according to claim 1 or 2, characterized in that the tablet size is 7 to 10 mm in diameter for round tablets, or 10 to 25 mm in length for caplets, or the capsule size is 3 to 000 for hard capsules, or 10 to 15 mm in length for soft capsules.

5. It contains the following ingredients (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropyl methylcellulose or hydroxypropylcellulose A coating composition for covering the outermost layer of a solid dosage form, characterized in that the ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 to 15.

6. The coating composition according to claim 5, characterized in that the content of component (A) Tremella fuciformis polysaccharide is 7 to 70% by mass.

7. A method for improving the ease of taking solid dosage forms, A coating layer is provided on the surface of the solid dosage form. The coating layer contains the following components (A) and (B): (A) Tremella fuciformis polysaccharide (B) Hydroxypropyl methylcellulose or hydroxypropylcellulose A method for improving the ease of administration of a solid dosage form, characterized in that the ratio (B / A) of the content of component (B) to the content of component (A) is 1.20 to 15.

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