TWI404546B - Coating composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a film-coated preparation having a highly glossy surface, even when a sugar coating is not applied. <P>SOLUTION: This film coating composition is characterized by comprising (A) hydroxypropyl methyl cellulose, (B) polyethylene glycol, and (C) talc, wherein the mass ratio (A:B) of the components (A) to (B) is 1:0.22 to 1.25; and the mass ratio (A:C) of the components (A) to (C) is 1:0.8 to 3.8. <P>COPYRIGHT: (C)2008,JPO&amp;INPIT

Description

Coating composition

The present invention relates to a coating composition, and more particularly to a coating composition which can be used as a coating agent for a solid preparation.

The envelope or the sugar coating is wrapped on the tablet to improve the stability of the drug substance to light or humidity, or to prevent bitterness, odor, irritation, etc., or to prevent the generation of whiskers, or to improve the appearance as a product. However, in terms of the aesthetics of the product, especially the gloss or moisturization of the surface, the previous envelope is inferior to the sugar coating. On the other hand, although the surface of the tablet coated with the sugar coating has a high gloss, since the sugar coating step takes a long time, not only the manufacturing cost rises, but also the preparation becomes large and heavy due to the sugar coating, thereby carrying Poorness, and further, the state of high temperature and high humidity in the sugar coating step lasts for a long period of time, and thus sometimes affects the stability of the active ingredient.

Therefore, attempts have been made to impart a high gloss such as a sugar-coated sheet to the surface of the coated sheet. For example, a film for glazing using a mixture of a sweet component and a glazing wax has been proposed (Patent Document 1); a dry powder composition using gum arabic (Patent Document 2); and hydroxypropylcellulose and carboxymethylcellulose are formulated. A coating composition of sodium sodium (Patent Document 3) or the like. However, the gloss obtained from such compositions is not sufficient.

[Patent Document 1] Japanese Laid-Open Patent Publication No. 2001-89361 (Patent Document 2) International Publication No. 2002/019987 pamphlet [Patent Document 3] Japanese Patent Laid-Open Publication No. 2002-534373

It is an object of the present invention to provide a coated preparation which has a high gloss surface even without being coated with a sugar coating.

The inventors of the present invention conducted intensive studies in order to achieve the above object, and as a result, unexpectedly found that hydroxypropylmethylcellulose, polyethylene, which was previously formulated as a coating agent component previously used as a solid preparation, was used in a specific ratio. The composition of the diol and talc imparts a high gloss to the surface of the preparation, thereby completing the present invention.

That is, the present invention provides a composition for a coating comprising: (A) hydroxypropylmethylcellulose, (B) polyethylene glycol, and (C) talc, the mass of components (A) and (B) The ratio (A:B) is 1:0.22 to 1.25, and the mass ratio (A:C) of the components (A) to (C) is 1:0.8 to 3.8.

Further, the present invention provides a coating preparation which is coated with an envelope having a thickness of from 20 μm to 200 μm by the above composition.

When the tablet is coated with the composition for a coating of the present invention, a film having a beautiful gloss can be formed, and a coating preparation having improved appearance quality can be obtained. Moreover, according to the present invention, since the sugar coating step is not required, not only the weight and size of the tablet can be reduced, but also the manufacturing cost can be reduced, and further, the moisture of the final preparation can be easily controlled, so that the stability of the active ingredient can be maintained. It also prevents discoloration of the formulation.

The coating composition of the present invention contains (A) hydroxypropylmethylcellulose, (B) Polyethylene glycol and (C) talc.

The component (A) hydroxypropylmethylcellulose used herein is not particularly limited, but from the viewpoint of imparting high gloss, it is preferred that the degree of substitution of the methoxy group is from 16.5 to 30.0, which is particularly preferable. It is 28.0~30.0, and the degree of substitution of hydroxypropoxy is 4.0~32.0, especially 7.0~12.0. Further, the viscosity of the hydroxypropylmethylcellulose is preferably from 3 to 10,000 mPa·s, particularly preferably from 3 to 15 mPa, based on the viscosity of a 2% aqueous solution at 20 ° C. s.

Examples of commercially available hydroxypropylmethylcellulose include hydroxypropylmethylcellulose 2208, hydroxypropylmethylcellulose 2906, and hydroxypropylmethylcellulose 2910. These may be used alone or in combination of two. More than one species.

The content of hydroxypropylmethylcellulose in the composition relative to the total solid content of the coating composition of the present invention is in terms of film strength, adhesion at the time of coating, and high gloss. The good is 5 to 80% by mass, particularly preferably 10 to 60% by mass, more preferably 15 to 35% by mass.

The polyethylene glycol which is the component (B) used in the present invention is not particularly limited, but is preferably a solid at 25 ° C, and preferably has a weight average molecular weight of 190 to 42,000, particularly preferably 7,300. 9,300. Further, the weight average molecular weight of the polyethylene glycol is a value in terms of polystyrene measured by GPC.

Commercial products of polyethylene glycol include polyethylene glycol 200, polyethylene glycol 400, polyethylene glycol 600, polyethylene glycol 1000, polyethylene glycol 1500, polyethylene glycol 1540, and polycondensation. Ethylene glycol 4000, polyethylene glycol 6000, polyethylene glycol 20000, polyethylene glycol 35000, etc. These may be used individually or in combination of 2 or more types.

The envelope group of the present invention is used with respect to 1 part by mass of hydroxypropylmethylcellulose The content of the polyethylene glycol in the compound is from 0.22 to 1.25 parts by mass, preferably from 0.25 to 1.0 part by mass, particularly preferably from 0.4 to 0.8 part by mass. When the content of the polyethylene glycol is small, the gloss is poor. On the other hand, when a large amount of polyethylene glycol is blended, the adhesion rate at the time of coating is lowered, and the smoothness of the surface is liable to disappear.

The average particle diameter of the component (C) talc used in the present invention (measured according to JIS M8016) is preferably from 0.1 to 20 μm, particularly preferably from 1 to 12, from the viewpoint of imparting high gloss. Μm, more preferably 2~7 μm. If the particle size of the talc is too large, the surface is rough and it is difficult to obtain sufficient gloss. Further, as for the particle size of the talc, it is preferable that the particle size exceeds 75 μm (the sieve which cannot pass through the mesh of 75 μm) is 0.2% by mass or less, and particularly preferably the particle size exceeds 45 μm (cannot pass The mesh having a mesh size of 45 μm is 0.3% by mass or less.

Further, in the present invention, in order to obtain a high gloss, the whiteness of talc is important. It is preferred that the whiteness of the talc (measured according to JIS M8016) is 90 or more, and it is particularly preferable to use a whiteness of 93 or more. If the whiteness is small, it is difficult to express the luster of the sparkle.

The content of the talc in the coating composition of the present invention is from 0.8 to 3.8 parts by mass, preferably from 1.2 to 3.8 parts by mass, particularly preferably from 1.6 to 2.4, based on 1 part by mass of the hydroxypropylmethylcellulose. Parts by mass. If the content of talc is small, it is difficult to express the luster of glare. On the other hand, if a large amount of talc is blended, the coating film becomes weak, and dust is generated in the coating device, and even dust adheres to the surface of the tablet. .

In the composition for a coating of the present invention, it is preferred to The colorant is further formulated externally. Examples of the coloring agent include catechin tannin powder, turmeric extract, yellow ferric oxide, Opaspray K-1-24904, orange flavor, brown iron oxide, carbon black, caramel, magenta, carotenoid solution, and β. Carotene, licorice extract, gold foil, black iron oxide, light anhydrous citric acid, titanium oxide, ferric oxide, edible blue No. 1, edible yellow No. 4, edible yellow No. 4 aluminum lake, edible yellow 5 No., edible red No. 2, edible red No. 3, edible red No. 102, sodium hydroxide, copper chlorophyll sodium, chlorophyll copper, rye green leaf extract, d-borneol, octyl dodecyl myristate, medicinal Carbon, riboflavin butyrate, riboflavin, green tea powder, riboflavin sodium phosphate, rose oil, etc., may be used singly or in combination of two or more.

The content of the coloring agent in the composition is preferably 5 parts or less, particularly preferably 2 parts or less, more preferably 1 part or less, based on 1 part by weight of hydroxypropylmethylcellulose.

In the coating composition of the present invention, in addition to the above components, a pharmaceutical additive such as a plasticizer, a coating agent, a dispersing agent, or a defoaming agent used in a coating of a general oral pharmaceutical product may be added as needed. Agents, etc.

Specific examples of the plasticizer include karion 83, triethyl citrate, glycerin, fatty acid glyceride, sesame oil, dimethyl polyoxyalkylene cerium oxide mixture, D-sorbitol, and medium long chain. Triglyceride, sugar alcohol liquid derived from corn starch, triacetin, concentrated glycerin, castor oil, diethyl phthalate, dibutyl phthalate, butyl phthalate Butyl glycolate, polyoxyethylene (105) polyoxypropylene (5) diol, propylene glycol, polysorbate 80, cottonseed oil. Soybean oil mixture, glyceryl monostearate Etc., these may be used singly or in combination of two or more. In the case where a plasticizer is added, the content in the composition is preferably 40% by mass or less.

Specific examples of the coating agent include ethyl acrylate/methyl methacrylate copolymer dispersion, acetamidine glycerin fatty acid ester, aminoalkyl methacrylate copolymer E, and aminoalkyl methacrylate. Ester copolymer RS, gum arabic, gum arabic powder, ethyl cellulose, ethyl cellulose aqueous dispersion, octyl decyl triglyceride, Opadry AMB, Opadry OY-6950, Opadry OY-S-7135, Opadry OY-S-8471, Opadry OY-S-9607, Opadry OY-S-22829, Opadry OY-S-22835, Opadry OY-S-22961, olive oil, kaolin, cocoa butter, Prunella vulgaris, ramie wax, coke Sugar, carnauba wax, carboxyvinyl polymer, carboxymethyl ethyl cellulose, sodium carboxymethyl starch, calcium carboxymethyl cellulose, sodium carboxymethyl cellulose, hydrated cerium oxide, dried aluminum hydroxide gel, dried Milky white shellac, dry methacrylic acid copolymer LD, cold plum powder, fish scale foil, gold foil, silver foil, triethyl citrate, glycerin, fatty acid glyceride, magnesium citrate, light anhydrous citric acid, light and anhydrous Hydroxypropyl cellulose of citric acid, dilute liquid paraffin, cetyl wax, Crystal cellulose, hardened oil, synthetic aluminum silicate, synthetic wax, high glucose leeches, hard wax, amber gelatin, wheat flour, wheat starch, rice starch, cellulose acetate, vinyl acetate resin, phthalic acid acetate , white beeswax, titanium oxide, magnesium oxide, dimethylaminoethyl methacrylate·methyl methacrylate copolymer, dimethyl polyoxyalkylene (administered internally), dimethyl polyoxane Ceria mixture, calcined gypsum, sucrose fatty acid ester, agarwood powder, aluminum hydroxide gel, hydrogenated rosin glyceride, stearyl alcohol, stearic acid, aluminum stearate, calcium stearate, stearic acid polyhydrocarbon Oxygen ester 40, hard fat Magnesium sulphate, refined gelatin, refined shellac, refined white sugar, zein, sesquisulphate sorbitan, cetyl alcohol, gypsum, gelatin, shellac, sorbitan fatty acid ester, D-sorbose Alcohol, D-sorbitol liquid, tricalcium phosphate, calcium carbonate, magnesium carbonate, monosaccharide syrup, medium gold foil, precipitated calcium carbonate, low-substituted hydroxypropyl cellulose, terpene resin, starch (soluble), corn syrup, corn Oil, triacetin, calcium lactate, lactose, concentrated glycerin, white shellac, white sugar, honey, paraffin, pearl powder, potato starch, hydroxypropyl cellulose, hydroxypropyl methyl cellulose phthalate , piperonyl butoxide, castor oil, diethyl phthalate, dibutyl phthalate, butyl phthalate, butyl phthalate, glucose, fumaric acid. Stearic acid·polyvinyl acetal diethylamine acetate. Hydroxypropyl methylcellulose 2910 mixture, polytriglucose, propylene glycol, bentonite, povidone, polyoxyethylene hardened castor oil 40, polyoxyethylene hardened castor oil 60, polyoxyethylene (105) polyoxypropylene (5) two Alcohol, polyoxyethylene (160) polyoxypropylene (30) diol, polysorbate 80, polyvinyl acetal diethylamine acetate, D-mannitol, leeches, beeswax, myristyl alcohol, Anhydrous citric acid hydrate, phthalic anhydride, anhydrous calcium hydrogen phosphate, methacrylic acid copolymer L, methacrylic acid copolymer LD, methacrylic acid copolymer S, magnesium metasilicate aluminate, methyl cellulose, acrylic acid 2-methyl-5-vinylpyridylmethyl ester. Methacrylic acid copolymer, lacquer wax, aluminum monostearate, glyceryl monostearate, sorbitan monolaurate, montan acid ester wax, medicinal carbon, polyglycerol, calcium sulfate, liquid paraffin, DL-malic acid, calcium hydrogen orthophosphate, calcium hydrogen phosphate, sodium hydrogen phosphate, calcium dihydrogen phosphate, rosin, etc., may be used alone or in combination of two or more. In the case of adding a coating agent, the content in the composition is preferably 40 mass. %the following.

Specific examples of the dispersing agent include aminoalkyl methacrylate copolymer RS, gum arabic, gum arabic powder, propylene glycol alginate, ethanol, oleic acid, carboxyvinyl polymer, sodium carboxymethylcellulose, Agar powder, citric acid, sodium citrate, glycerin, fatty acid glyceride, magnesium citrate, light anhydrous citric acid, crystalline cellulose, hardened oil, synthetic aluminum citrate, phosphoric acid choline, safflower oil, white beeswax, oxidation Titanium, sodium sulfosuccinate dioctyl ester, sucrose fatty acid ester, sodium hydroxide, stearic acid, magnesium stearate, refined oleic acid, refined soy lecithin, sesquistea sulphate, sorbose Alcohol fatty acid ester, D-sorbitol, soybean oil, soy lecithin, low-substituted hydroxypropyl cellulose, dextrin, corn starch, gum tragacanth powder, sorbitan trioleate, lactose, concentrated glycerin , potato starch, hydroxyethyl cellulose, hydroxypropyl starch, hydroxypropyl cellulose, propylene glycol, propylene glycol fatty acid ester, bentonite, povidone, polyoxyethylene hardened castor oil, polyoxyethylene hardened castor oil 40, poly Oxyethylene hardened castor oil 60 , polyoxyethylene (105) polyoxypropylene (5) diol, polyoxyethylene (160) polyoxypropylene (30) diol, polysorbate 20, polysorbate 60, polysorbate 80, poly Sodium phosphate, anhydrous sodium citrate, anhydrous sodium pyrophosphate, magnesium metasilicate aluminate, sodium metaphosphate, methylcellulose, lacquer wax, sorbitan monooleate, aluminum monostearate, monostearic acid Glyceryl ester, sorbitan monopalmitate, sorbitan monolaurate, sodium lauryl sulfate, polyglycerol, liquid paraffin, calcium hydrogen phosphate, etc., which may be used alone or in combination. More than one species. In the case where a dispersing agent is added, the content in the composition is preferably 25% by mass or less.

Specific examples of the antifoaming agent include ethanol and fatty acid glycerides. Dimethylpolyoxane (internal administration), dimethyl polyoxane·cerium oxide mixture, sucrose fatty acid ester, oxime resin emulsion, bismuth defoamer, polyoxyl stearate 40, sorbose The alcoholic anhydride fatty acid ester, the sorbitan trioleate, the polysorbate 80, etc. may be added individually or in mixture of two or more types. In the case where an antifoaming agent is added, the content in the composition is preferably 10% by mass or less.

The coating preparation of the present invention is produced by dissolving a composition for a coating containing hydroxypropylmethylcellulose, polyethylene glycol and talc. The coating liquid is suspended and spray coated on the outermost surface of the solid preparation. As a dosage form of the solid preparation, a tablet is preferred.

In the solid preparation, various medicinal ingredients can be suitably formulated, and examples thereof include vitamin C such as ascorbic acid, calcium ascorbate, and sodium ascorbate; calcium pantothenate, thiamine nitrate, thiamine hydrochloride, dithiamine nitrate, and dithiothiamine. , cetyl sulphate sulphate sulphate, sulphate sulphate hydrochloride, hydrazine hydrazine, olto thiamine, seleton sulphate, bis-isobutyl sulphate, bis-benzopyramine, phenylphosphine sulphate, nuclear yellow , riboflavin butyrate, riboflavin sodium phosphate, pyridoxine hydrochloride, pyridoxal phosphate, cyanocobalamin, hydroxycobaltium hydrochloride, hydroxycobalt ammonium sulphate, methylcobalamin, nicotinic acid, nicotinamide , biotin, folic acid and other vitamin B; γ-oryzanol and other autonomic nervous regulators; sulphuric acid, whey acid and other vitamin-like substances; calcium hydrogen phosphate, calcium lactate and other minerals; acetic acid d-α- Vitamin E such as tocopherol ester, dl-α-tocopheryl acetate, d-α-tocopheryl succinate, dl-α-tocopheryl succinate, vitamin D such as ergocalciferol and cholecalciferol; - amino acid such as cysteine, methionine, glycine, arginine hydrochloride; amine B Acid, glucuronic Amides, the glucuronic acid Herbal acid such as ester, glycyrrhizic acid, and ursodeoxycholic acid; Polygonum multiflorum extract, European hawthorn extract, Acanthopanax senticosus extract, Epimedium extract, Coix seed extract, liver hydrolysate, bile extract powder, Natural extracts such as Bupleurum dry extract, dried extract of Chuanxiong, dried red extract of mountain, dried extract of medlar, and the like.

The method of producing the preparation is not particularly limited, and a preparation additive may be added to the medicinal ingredient as needed, and it may be produced by a conventional method. For example, the general formulation method that is usually used (Tsujin Kousuke. Ueno Shou, "Medical Development Basic Lecture XI Pharmaceutical Manufacturing Law (I), (below)", "People's Library", issued in 1971; , "Manufacturing Engineering Handbook", and the People's Library, issued in 1983; Nakai Yusuke, "The Latest Powder Material Design", Techno System, issued in 1988; Arakawa Text, "Pharmaceutical Development II Preparation Unit Operation & Machinery", Hirokawa Bookstore, issued in 1989; Hiroshi Hiroshi, "Design and Evaluation of Oral Formulations", Pharmaceutical Times, 1995, Hiroshi Hiroshi, "Design of Oral Formulations", Pharmaceutical Times, Released in 1995). Further, when it is necessary to prepare a granulated powder, it can be prepared by a granulation method which is generally used (a spray granulation method using a solution or dispersion containing water or an organic solvent, stirring granulation method) And the original powder produced by a fluid granulation method, a rotary granulation method, a rotary granulation method or the like, a wet granulation method, a dry granulation method such as a compact granulation method using a powdery binder, and the like. Powder. Fine granules. The granules and the like are mixed with the formulation additive and compression molded. Further, the underside of the film layer obtained from the coating composition of the present invention may be subjected to a primer coating to prepare a coating film having a multilayer film layer of two or three layers.

As the preparation additive used in the formulation, a pharmaceutically acceptable carrier such as a stabilizer, a surfactant, a lubricating agent, a lubricant, a solvent, a buffer, a sweetener, a matrix, and an adsorbent may be mentioned. , flavoring agents, adhesives, suspending (chemical) agents, antioxidants, brighteners, perfumes, coating agents, wetting agents, wetting regulators, fillers, defoamers, cooling agents, flavoring agents. Perfume, colorant, isotonic agent, softener, emulsifier, viscous agent, foaming agent, pH adjuster, excipient, dispersant, disintegrant, disintegration aid, fragrance, moisture proof As a specific example of the additives of the preparations, for example, a binding book (Japanese Pharmaceutical Additives Association, "Pharmaceutical Additives Code 2005", etc., may be used as a specific example of the additives of the preparations, such as a preservative, a preservative, a preservative, a dissolving agent, a dissolving agent, a solvent, a fluidizing agent, and the like. Revealed in the Pharmaceutical Daily, issued in 2005).

The coating method of the coating composition for a solid preparation such as a die or a coated sheet produced as described above is not particularly limited, and examples thereof include a pan coating method and a fluidized layer package. A clothing method, a spin coating method, a dry coating method, or a combination method of the above. The coating liquid containing the coating composition of the present invention is used in hydroxypropylmethylcellulose, polyethylene glycol, and talc, and further, if necessary, a pharmaceutical additive is added and the coating composition is weighed, and the combination is used. The product is prepared by dissolving/suspending in a purified alcohol or a lower alcohol such as ethanol or a mixture thereof. The coating liquid is preferably adjusted to have a solid content of usually 1 to 50% by mass, particularly preferably 2 to 30% by mass, more preferably 5 to 20% by mass.

In the present invention, the thickness of the film layer formed on the preparation varies depending on the shape or size of the preparation, but from the viewpoint of obtaining a surface having a beautiful luster, it is preferably 20 μm to 200 μm, particularly preferably. Is 30 μm~100 Μm, more preferably 40 μm~80 μm. For example, a tablet having a diameter of 9 mm and a mass of about 200 mg, in order to obtain the thickness of the above-mentioned film layer, is preferably coated at about 3 to 30 mg/tablet, more preferably about 3 to 15 mg/ The tablets are coated, and it is especially preferred to coat them at about 6 to 12 mg per tablet. If the thickness of the film layer is too thin, sufficient gloss cannot be obtained. On the other hand, if the thickness of the film layer is large, the time necessary for coating is required.

The preparation of the present invention may be subjected to a primer coating on the lower side of the film layer obtained from the coating composition to form a coating preparation having a plurality of film layers.

For example, when the solid preparation contains a medicinal ingredient such as L-cysteine which causes an unpleasant odor, it is preferred to coat the envelope in order to mask the odor. In the envelope, a pharmaceutical additive used in the coating of the above oral pharmaceutical product can be suitably added, and in particular, from the viewpoint of the deodorizing effect, it is preferred to add a partial saponified product of polyvinyl alcohol. The degree of saponification of the partially saponified polyvinyl alcohol is preferably from 70 to 97 mol%, particularly preferably from 78 to 96 mol%, and the average degree of polymerization, from the viewpoint of an unpleasant odor reduction effect. It is preferably 200 to 3,300, and particularly preferably 300 to 1,500. Here, the degree of saponification is measured in accordance with JIS K6726 (polyvinyl alcohol test method). Further, the content of the polyvinyl alcohol in the coating film is preferably from 30 to 100% by mass, particularly preferably from 40 to 95% by mass, from the viewpoint of the deodorizing effect, the film strength, and the ease of coating.

Further, when the solid preparation contains calcium phytate and L-cysteine, and the like, which has a function of decomposing calcium pantothenate to impair the stability thereof, it is preferred to prepare an activity other than calcium pantothenate in the solid preparation. Ingredients, and calcium pantothenate is formulated in the film layer covering the formulation. In this case, in order to cover up The coating film wrapped with the medicinal ingredient which emits unpleasant odor may be wrapped on the upper side or the lower side or both sides of the film layer containing pantothenic acid or a salt thereof. In the film layer containing calcium pantothenate, a pharmaceutical additive used for the coating of the above oral pharmaceutical product may be suitably added, and it is particularly preferable to add a water-soluble or gastric-soluble film substrate such as self-methyl cellulose or hydroxypropyl fiber. Selected from hydroxypropylmethylcellulose, polyvinylpyrrolidone, carboxyvinyl polymer, polyvinyl alcohol, aminoalkyl methacrylate copolymer E, polyvinyl acetal diethylaminoacetic acid, etc. Kind or more than two.

Therefore, a formulation having a beautifully glossy surface can be provided by the envelope.

[Examples]

Hereinafter, the present invention will be specifically described by way of examples, but the present invention is not limited to the examples.

Example 1

960 g of L-cysteine (manufactured by Kyowa Mastic), 1237.2 g of ascorbic acid for direct compression (BASF made in Japan), 147.6 g of calcium pantothenate type S (BASF made in Japan), and 567.2 g of crystalline cellulose (VIVAPUR12: manufactured by RETTENMAIER), 200 g of crystalline cellulose (Ceolus KG802: manufactured by Asahi Kasei Chemicals), 200 g of low-substituted hydroxypropylcellulose (LH-11: manufactured by Shin-Etsu Chemical Co., Ltd.), and 16 g of light-weight anhydrous citric acid (Adsolider 101: manufactured by FREUND), 32 g of magnesium stearate (manufactured by Taiping Chemical Co., Ltd.), and a mixed powder for tableting, which was produced by a rotary tableting machine (VIRGO-0512 tableting machine: manufactured by Kikusui Seisakusho Co., Ltd.) A 9 mm Φ mortar rod was pressed until each piece reached a mass of 210 mg, and a bare piece was obtained. Next, 36 g of hydroxypropylmethylcellulose 2910 (TC-5RW: manufactured by Shin-Etsu Chemical Co., Ltd.), 21 g of polyethylene glycol 6000 (made by Nippon Oil & Fats), 69 g of talc (Shengguangshan Mining Institute; average particle size of 4.6 μm, particle size 45 μm sieve margin 0.1%, whiteness 93.6%), 24 g Titanium oxide (made by Ishihara Industry), dissolved. Suspended in purified water: 850 g of a mixture of Japanese Pharmacopoeia ethanol (3:1) to obtain a coating liquid. Then, 3000 g of the die was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and the coating was applied until the mass of the die increased by 10 mg per piece, and the mass per piece was 220. Mg coated film (film thickness 64.5 μm: n = 10 average, image analysis method).

Comparative example 1

3000 g of the obtained die in the same manner as in Example 1 was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and 80 g of hydroxypropylmethylcellulose 2910 (TC-5RW: It is dissolved in purified water: the coating liquid obtained in 920 g of the Japanese Pharmacopoeia ethanol (3:1) mixture, and coated until the mass of the bare piece reaches 10 mg per piece, and each piece is obtained. A mass of 220 mg of the envelope (film thickness of 62.9 μm: n = 10 average, image analysis method).

Example 2

4.8 kg of diphenhydramine hydrochloride (manufactured by King Kong Chemical Co., Ltd.), 4.8 kg of glycine (manufactured by Kyowa Mastic), 6.36 kg of lactose (Tablettose 80: manufactured by Megle Japan), and 19.2 kg of crystalline cellulose (Ceolus KG) -802: manufactured by Asahi Kasei Chemicals Co., Ltd., 1152 g of low-substituted hydroxypropylcellulose (L-HPC LH-11: manufactured by Shin-Etsu Chemical Co., Ltd.), 960 g of croscarmellose sodium (Kiccolate: manufactured by Asahi Kasei Chemicals), 384 g of light anhydrous citric acid (Adsolider 101: manufactured by FREUND), 384 g of magnesium stearate (too Manufactured into a talc of 384 g (manufactured by Kihara Kasei), a mixed powder for tableting, using a rotary tablet press (VIRGO-0512 tablet press: manufactured by Kikusui Seisakusho Co., Ltd.), with a 9 mm Φ mortar rod Tablets were pressed until a mass of 200 mg per sheet was obtained, and a bare piece of about 37.5 kg was obtained. Next, 36 g of hydroxypropylmethylcellulose 2910 (TC-5RW: manufactured by Shin-Etsu Chemical Co., Ltd.), 8 g of polyethylene glycol 6000 (manufactured by Nippon Oil & Fats Co., Ltd.), and 69 g of talc (Shengguangshan Mining Institute: average grain) The diameter is 4.6 μm, the particle size is 45 μm, the residual amount is 0.1%, the whiteness is 93.6%), and 24 g of titanium oxide (manufactured by Ishihara Industry Co., Ltd.) is dissolved. It was suspended in 863 g of purified water to obtain a coating liquid. Then, a 3 kg piece of the die was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and the coating was applied until the mass of the die reached 10 mg per piece, and the mass per piece was 210. Mg coated film (film thickness 65.7 μm: n = 10 average, image analysis method).

Example 3

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 10 g and changing the purified water to 861 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film of a mass of 210 mg (film thickness of 65.4 μm) per one piece of the present invention was obtained.

Example 4

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 13 g and changing the purified water to 858 g, and the same as in Example 2. 3 kg of the die fabricated in Example 2 was coated to obtain a 210 mg mass of the coated film per piece. (film thickness 65.9 μm).

Example 5

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 15 g and changing the purified water to 856 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film having a mass of 210 mg per film (film thickness of 63.9 μm) was obtained.

Example 6

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 21 g and changing the purified water to 850 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film having a mass of 210 mg per film (film thickness: 65.8 μm) was obtained.

Example 7

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 28 g and changing the purified water to 843 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film having a mass of 210 mg per film (film thickness of 64.4 μm) was obtained.

Example 8

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 35 g and changing the purified water to 836 g, and was the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, the mass of each of the tablets of the present invention was 210 mg. The envelope film (film thickness is 65.7 μm).

Example 9

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 40 g and changing the purified water to 831 g, and the same as in Example 2. In the manner of 3 kg of the die fabricated in Example 2, a coated film having a mass of 210 mg per film (film thickness of 66.1 μm) was obtained.

Example 10

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 43 g and changing the purified water to 828 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film having a mass of 210 mg per film (film thickness: 65.8 μm) was obtained.

Example 11

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 45 g and changing the purified water to 826 g, and the same as in Example 2. Membrane 3 kg of the die fabricated in Example 2 was coated to obtain a coated film of 210 mg each (film thickness 66.3 μm).

Comparative example 2

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 5 g and changing the purified water to 866 g, and the same as in Example 2. Method 3 kg of the die fabricated in Example 2 was coated to obtain a film of 210 mg per film (film film) The thickness is 63.7 μm).

Comparative example 3

The coating liquid was obtained in the same manner as in Example 2 by adjusting the coating liquid of Example 2, changing the polyethylene glycol 6000 to 60 g and changing the purified water to 811 g, and the same as in Example 2. In the manner of 3 kg of the die manufactured in Example 2, a coated film having a mass of 210 mg per film (film thickness: 63.7 μm) was obtained.

Test example 1

The surface gloss of the coated sheets of Examples 1 to 11 and Comparative Examples 1 to 3 was evaluated in accordance with the following five grades. The results are shown in Table 1.

As is evident from Table 1, the tablets of the present invention were able to obtain a higher gloss than the comparative examples.

Matte: - only a little gloss: ± shiny: + has a strong gloss: ++ has a very strong luster: +++

Example 12

7.2 kg of ibuprofen (manufactured by BASF Japan), 11.136 kg of lactose (Tablettose 80: manufactured by Megle Japan), 16.8 kg of crystalline cellulose (Ceolus KG-802: manufactured by Asahi Kasei Chemicals), and 1152 g of low-substituted hydroxypropyl Cellulose (L-HPC LH-11: manufactured by Shin-Etsu Chemical Co., Ltd.), 960 g of croscarmellose sodium (Kiccolate: manufactured by Asahi Kasei Chemicals), 384 g of light anhydrous citric acid (Adsolider 101: manufactured by FREUND) ), 384 g of magnesium stearate (made by Taiping Chemical Industry Co., Ltd.) and 384 g of talc (manufactured by Kihara Kasei), for the production of mixed powder for tableting, using a rotary tablet press (VIRGO-0512 tablet press: Kikusui Manufacturing Co., Ltd.) Manufactured), pressed with a 9 mm Φ mortar bar until each piece reached a mass of 200 mg, and a bare piece of about 37 kg was obtained. Next, 36 g of hydroxypropylmethylcellulose 2910 (TC-5RW: manufactured by Shin-Etsu Chemical Co., Ltd.), 21 g of polyethylene glycol 6000 (manufactured by Nippon Oil & Fats Co., Ltd.), and 30 g of talc (Shengguangshan Mining Institute: average grain) The diameter is 4.6 μm, the particle size is 45 μm, the residual amount is 0.1%, the whiteness is 93.6%), and 24 g of titanium oxide (manufactured by Ishihara Industry Co., Ltd.) is dissolved. It was suspended in 889 g of purified water to obtain a coating liquid. Then, 3 kg of the die was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and the coating was applied until the mass of the die reached 7.5 mg per piece, and the mass per piece was 207.5. Mg coated film (film thickness is 50.8 μm: n=10 average, image analysis method).

Example 13

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 44 g and changing the purified water to 875 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 49.9 μm).

Example 14

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 60 g and changing the purified water to 859 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 51.4 μm).

Example 15

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 69 g and changing the purified water to 850 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 50.1 μm).

Example 16

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 85 g and changing the purified water to 834 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet of 207.5 mg mass per sheet. The film thickness is 53.8 μm).

Example 17

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 105 g and changing the purified water to 1014 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 51.7 μm).

Example 18

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 135 g and changing the purified water to 984 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 51.9 μm).

Comparative example 4

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 10 g and changing the purified water to 909 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated sheet having a mass of 207.5 mg per film (film thickness: 51.9 μm).

Comparative Example 5

The coating liquid was obtained in the same manner as in Example 12 by adjusting the coating liquid of Example 12, changing the talc to 180 g and changing the purified water to 1239 g, and in the same manner as in Example 2, The pellets produced in Example 2 of kg were coated to obtain a coated film of 207.5 mg each. The thickness is 52.1 μm).

Test example 2

In the same manner as in Test Example 1, the surface gloss of the coated sheets of Examples 12 to 18 and Comparative Examples 4 to 5 was evaluated in five grades, and the results are shown in Table 2. As evident from Table 2, the tablets of the present invention were obtained with higher gloss than the comparative examples.

Example 19

2.4 kg of L-cysteine (manufactured by Kyowa Mastic), 1.5 kg of ascorbic acid (BASF made in Japan), 1.5 kg of pyridoxine hydrochloride (manufactured by First Precision Chemical Co., Ltd.), 1.2 kg of nicotine guanamine (1.2 kg) Made by DSM NUTRITIONAL), 1.14 kg of riboflavin sodium phosphate (manufactured by Iwao Pharmaceutical Co., Ltd.), 300 g of thiamine nitrate (manufactured by Takeda Pharmaceutical Co., Ltd.), 3 g of biotin (manufactured by SUN CHEMICAL), and 30 g of corn starch (SAN- A saccharification manufacturing), 2.547 kg of crystalline cellulose (manufactured by Asahi Kasei Chemicals), 1.2 kg of hydroxypropyl cellulose (manufactured by Japan Soda), 660 g of low-substituted hydroxypropyl cellulose (manufactured by Shin-Etsu Chemical Co., Ltd.), 60 g Magnesium stearate (made by Taiping Chemical Industry), 60 g of talc (Kihara Kasei) Manufactured, the powder for tableting was produced by a conventional method, and the obtained mixed powder was tableted by a rotary tableting machine with a 9 mm Φ mortar bar until the mass of each piece reached 210 mg, and a bare piece was obtained. Next, 3 kg of the die was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and purified using 20% by mass of Opadry AMB White (premix of polyvinyl alcohol: manufactured by COLORCON, Japan). The water-coating liquid was subjected to the undercoating until the mass increase amount of each of the tablets reached 7 mg, and then, 8% by mass of calcium pantothenate (manufactured by ALPS Pharmaceutical Industries) and 8 mass% of hydroxypropylmethylcellulose 2910 (using 8%) were used. Ethyl alcohol of TC-5 Shin-Etsu Chemical Co., Ltd.): a coating solution of purified water = 1:1, and coating the bottom layer until the mass increase of each tablet reaches 20 mg, and the mass per piece is 237 mg. The coated film is coated with the bottom layer.

Next, 36 g of hydroxypropylmethylcellulose 2910 (TC-5RW: manufactured by Shin-Etsu Chemical Co., Ltd.), 21 g of polyethylene glycol 6000 (manufactured by Nippon Oil & Fats Co., Ltd.), and 30 g of talc (Shengguangshan Mining Institute: average grain) The diameter is 4.6 μm, the particle size is 45 μm, the residual amount is 0.1%, the whiteness is 93.6%), and 24 g of titanium oxide (manufactured by Ishihara Industry Co., Ltd.) is dissolved. It was suspended in 889 g of purified water to obtain a coating liquid. Then, 3 kg of the undercoated coated film was placed in a coating machine (Hi-Coater HCT-48, FREUND industry), and the coating was applied until the mass increase of each tablet reached 8 mg. Each piece of the mass of 245 mg of the coated film (film thickness of 53.4 μm: n = 10 average, image analysis method).

Comparative Example 6

3 kg of the dies manufactured in Example 19 were placed in a coating machine (Hi-Coater HCT-48, FREUND Industries), and a double undercoat was applied in the same manner as in Example 19, and the mass per one piece was obtained. 237 mg bottom coat The envelope film. Then, using the coating of the composition of the present invention produced in Example 19, the coating was applied until the mass increase per tablet of the tablet reached 1 mg, and a coated tablet having a mass of 238 mg per tablet was obtained ( The film thickness is 6.5 μm).

Example 20

3 kg of the dies manufactured in Example 19 were placed in a coating machine (Hi-Coater HCT-48, FREUND Industries), and a double undercoat was applied in the same manner as in Example 19, and the mass per one piece was obtained. 237 mg of the undercoated coating. Then, using the coating liquid of the composition of the present invention produced in Example 19, the coating was applied until the mass increase per tablet of the tablet reached 3 mg, and a film of 240 mg per piece was obtained. The film thickness was 20.7 μm).

Example 21

3 kg of the dies manufactured in Example 19 were placed in a coating machine (Hi-Coater HCT-48, FREUND Industries), and a double undercoat was applied in the same manner as in Example 19, and the mass per one piece was obtained. 237 mg of the undercoated coating. Then, using the coating liquid of the composition of the present invention produced in Example 19, the coating was applied until the mass increase per tablet of the tablet reached 5 mg, and the package of the present invention having a mass of 242 mg per tablet was obtained. Diaphragm (film thickness 32.9 μm).

Test Example 3

The surface gloss of the coated sheets of Examples 19 to 21 and Comparative Example 6 was evaluated in five stages in the same manner as in Test Example 1, and the results are shown in Table 3. As is clear from Table 3, the tablets of the present invention can be obtained more than the comparative examples. High gloss.

Claims (8)

A coating composition comprising (A) hydroxypropylmethylcellulose, (B) polyethylene glycol, and (C) talc, a mass ratio of components (A) to (B) (A: B) is 1:0.22 to 1.25, and the mass ratio (A:C) of the components (A) to (C) is 1:0.8 to 3.8. The composition for a coating of claim 1, wherein the content of (A) hydroxypropylmethylcellulose is from 5 to 80% by mass based on the total solid content of the composition. The composition for a coating of claim 1, wherein (A) hydroxypropylmethylcellulose has a methoxyl degree of substitution of 16.5 to 30.0 and a hydroxypropoxyl degree of substitution of 4.0 to 32.0. The composition for a coating of claim 1, wherein the weight average molecular weight of the (B) polyethylene glycol is from 190 to 42,000. The coating composition according to claim 1, wherein the (C) talc has an average particle diameter of 0.1 to 20 μm and a whiteness of 90 or more. The composition for a coating of claim 1, which further contains a colorant. The coating composition according to claim 6, wherein the content of the colorant is 5 parts by mass or less based on 1 part by mass of the (A) hydroxypropylmethylcellulose. A coated preparation which is coated with a coating having a thickness of from 20 μm to 200 μm by using the composition according to any one of claims 1 to 7.