WO2004108164A1 - Composition d'enrobage et preparation enrobee - Google Patents

Composition d'enrobage et preparation enrobee Download PDF

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Publication number
WO2004108164A1
WO2004108164A1 PCT/JP2004/008166 JP2004008166W WO2004108164A1 WO 2004108164 A1 WO2004108164 A1 WO 2004108164A1 JP 2004008166 W JP2004008166 W JP 2004008166W WO 2004108164 A1 WO2004108164 A1 WO 2004108164A1
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WO
WIPO (PCT)
Prior art keywords
coating
cellulose
preparation
microfibrous
composition
Prior art date
Application number
PCT/JP2004/008166
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English (en)
Japanese (ja)
Inventor
Tuneaki Tottori
Hiroko Kusano
Yasuki Kato
Original Assignee
Kyowa Hakko Kogyo Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kyowa Hakko Kogyo Co., Ltd. filed Critical Kyowa Hakko Kogyo Co., Ltd.
Priority to JP2005506843A priority Critical patent/JPWO2004108164A1/ja
Publication of WO2004108164A1 publication Critical patent/WO2004108164A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods

Definitions

  • the present invention relates to a composition which can be used for a coating film in a coating preparation, a coating preparation comprising a core substance and a coating film covering the core substance, and the like.
  • coating preparations comprising a core substance and a coating film covering the core substance are widely used.
  • Coating is a technique widely used in the pharmaceutical field for the purpose of masking the taste or odor of an active ingredient and improving light stability.
  • a coating composition containing a conventionally known coating base for a preparation. Widely used.
  • the coating film In such a coating preparation, if the coating film is peeled or cracked during the production and / or storage of the preparation, the quality of the product may be deteriorated, and particularly, the product may come into contact with moisture. In some cases, the strength of the coating film is reduced, and peeling, cracking, and the like may easily occur. In addition, the strength of the coating film decreases due to contact with water after taking the drug, and due to the peeling or cracking of the coating film, the release of the drug or the masking of taste or smell cannot be controlled, and sufficient functions are not achieved. Sometimes I can't do it. Therefore, it is required to increase the strength of the coating film, particularly when the film comes into contact with moisture or moisture.
  • microfibrous cellulose (see JP-A-56-100801) produced by passing a suspension of fibrous cell mouth through a small-diameter orifice at high pressure is known.
  • microfibrous cellulose has been used for the purpose of maintaining the viscosity of foods, cosmetics, paints, etc., strengthening food raw materials, retaining moisture, improving food stability, etc., as well as adding low calorie additives or emulsifying stability. It is known to use as a cellulose coating or the like characterized by being produced by spraying a chemical aid on a substrate (see JP-A-10-95803).
  • microfibrous cellulose A coating composition containing chitosan is also known (see JP-A-7-2701).
  • compositions containing bacterial cellulose see JP-A-10-95803
  • a capsulated microfibril cellulose and a composition containing the same see Japanese Patent Application Laid-Open No. 9-509694
  • a microcrystalline cellulose An aqueous suspension of microcrystalline cellulose produced by passing a suspension through a small diameter orifice at a high pressure (see Japanese Patent Publication No. 57-234642), a non-woody microfibrous cellulose and a coating containing the same for coating.
  • Compositions see JP-T-2002-521577) and the like are also known.
  • An object of the present invention is to provide a coating preparation comprising a core substance containing an active ingredient such as a drug, food, agrochemical, and veterinary drug, and a coating film covering the core substance.
  • the present invention relates to the following (1) to (31).
  • a composition comprising microfibrous cellulose and a pharmaceutical coating base, and substantially free of chitosan.
  • microfibrous cellulose is microfibrous cellulose produced by treating woody cellulose, powdered cellulose or cellulose containing crystal cell mouth with a high-pressure homogenizer.
  • a coating preparation comprising a core substance containing an active ingredient, and a coating film containing the microfibrous cellulose covering the core substance and a coating base for preparations.
  • the content of microfibrous cellulose in the coating film is 0.1 to 95 mass based on the total solid content in the film. /.
  • the coating base for the preparation is a cellulose-based polymer, an acrylic acid-based polymer, a coating base for sugar coating, shellac or zein. Formulation.
  • microfibrous cellulose is microfibrous cellulose produced by treating woody cellulose, powdered cellulose, or cellulose containing crystal cellulose with a high-pressure homogenizer.
  • microfibrous cellulose is bacterial cellulose or microfibrillated cellulose.
  • microfibrous cellulose is present in the coating film.
  • a coating preparation comprising a core substance containing an active ingredient and a coating film containing a coating base for pharmaceutical preparation covering the core substance, a microfibrous cellulose and coating for pharmaceutical preparation are formed on the core substance.
  • a method for imparting strength to the coating preparation characterized by forming a coating film by spraying a composition containing a base.
  • microfibrous cellulose as described in (15), wherein the microfibrous cell opening is a microfibrous cellulose produced by treating a woody cell opening, powdered cellulose or cellulose containing crystalline cell opening with a high-pressure homogenizer.
  • the method for imparting strength to a coating preparation according to any one of claims to (19).
  • (23) a step of mixing components other than water and / or an organic solvent of a liquid composition containing microfibrous cellulose and a coating base for pharmaceutical preparations in water and / or an organic solvent; and
  • a method for producing a coating preparation which comprises a step of spraying a mixture onto a core substance containing an active ingredient to form a coating film.
  • microfibrous cellulose is microfibrous cellulose produced by treating woody cellulose, powdered cellulose, or cellulose containing crystalline cellulose with a high-pressure homogenizer. Manufacturing method.
  • microfibrous cellulose used in the present invention is not particularly limited.
  • Fibrous cellulose and the like can be mentioned, and preferably, a microfibrillated cell mouth is obtained by treatment with the high-pressure homogenizer.
  • cellulose fibers such as wood pulp are finely ground or beaten by various conventionally known methods (JP-A-3-163135, JP-A-56-100801, etc.), and commercially available Fibrous cellulose (for example, trade name: SEritsch (Daicel Chemical Industries, Ltd.)) and the like.
  • Fibrous cellulose for example, trade name: SEritsch (Daicel Chemical Industries, Ltd.)
  • bacterial cellulose and the like can be used.
  • the specific surface area of the microfibrous cellulose used in the present invention is preferably 3 m 2 / g or more, and more preferably 5 m 2 / g or more.
  • the coating base for pharmaceutical preparation in the present invention is not particularly limited as long as it is acceptable for use in pharmaceuticals, foods, agricultural chemicals, veterinary drugs, etc., and is preferably a pharmaceutical, food, agricultural chemical, veterinary drug, etc.
  • ethyl cellulose hydroxypropyl methylcellulose, hydroxypropylmethyl cellulose sulfate, hydroxypropyl methylcellulose acetate succinate,
  • Cellulose polymers such as cellulose acetate fluorocarboxylate, carboxymethylethylcellulose, cellulose acetate, etc .
  • ethyl acrylate / methyl methacrylate copolymer amino alkyl methacrylate copolymer E, amino alkyl methacrylate copolymer RS, methyl acryl
  • Acrylic acid polymers such as acid copolymer L, methacrylic acid copolymer LD, and methacrylic acid copolymer S
  • coating bases for sugar coating such as sucrose and maltitol
  • polysaccharides such as pullulan, dextrin, sodium alginate, xanthan gum
  • Cellulose-based polymer, acrylic acid-based polymer, coating base for sugar coating, shellac, zein, etc. are preferable.
  • Cellulose-based polymer, acrylic acid-based polymer, cerac, zein, etc. are preferable.
  • an aqueous dispersion of ethyl cellulose [trade name: Aquacoat (Asahi Kasei), Sureis (Colorcon)], aminoalkylmethacrylate Evening acrylate copolymer RS aqueous dispersion [trade name: Oy Dragit RS30D, Oy Dragit RL30D (Higuchi Shokai)], Ethyl acrylate / methyl methacrylate methyl copolymer aqueous dispersion [trade name: Oy Dragit NE30D (Higuchi Shokai) )], Aqueous shellac (Freund Corporation) and the like.
  • the composition of the present invention is a composition containing microfibrous cellulose and a pharmaceutical coating base, and substantially free of chitosan, and preferably contains water and / or an organic solvent, more preferably water. It is a liquid composition or a composition obtained by solidifying the liquid composition by a formulation technique well known in the art.
  • the content of the microfibrous cellulose in the composition of the present invention is not particularly limited, but is preferably from 0.1 to 95% by mass, and more preferably from 10 to 80% by mass based on the total solid content in the composition. Is more preferable, and more preferably 20 to 50% by mass.
  • the ratio of the content of the base material is preferably 1:99 to 19: 1, more preferably 1:19 to 9: 1, and further preferably 3: 7 to 7: 3.
  • the ratio is 4: 6 to 5: 5, and most preferably.
  • composition of the present invention may contain any of various plasticizers and / or water-soluble components.
  • the plasticizer include triethyl citrate, getyl furate, macrogol, and glycerin.
  • glycerin fatty acid ester triacetin, propylene glycol and the like, and preferably, triethyl citrate, glycerin fatty acid ester and the like.
  • the water-soluble component is not particularly limited as long as it is soluble in water and is acceptable for use in pharmaceuticals, foods, agricultural chemicals, veterinary drugs, and the like. Examples thereof include lactose, sucrose, D-mannitol, sorbitol, and erythritol.
  • a lubricant eg, talc, glyceryl monostearate, etc.
  • a coloring agent eg, titanium oxide, iron sesquioxide, yellow sesquioxide, etc.
  • the composition of the present invention can be obtained as a liquid composition by mixing and dissolving and dispersing components other than water and / or an organic solvent in water and / or an organic solvent.
  • woody cellulose, powdered cellulose, crystalline cellulose, or the like which is a raw material of microfibrous cellulose, may be suspended in water and / or an organic solvent, preferably water, together with other components, if desired, to obtain a high-pressure liquid.
  • Microfibrous cellulose is produced by treating with a homogenizer, etc., followed by dissolution and dispersion by mixing the remaining components other than water and / or organic solvent in water and / or organic solvent, preferably in water Liquid by doing
  • the composition can be obtained in the form of a solid.
  • the components of the composition of the present invention other than water and / or the organic solvent in the water and / or the organic solvent a method known in the art is used, but a method of mixing with a homogenizer is preferable. .
  • the water and / or the organic solvent solution or suspension of the microfibrous cellulose is mixed. Is preferably stirred with a homogenizer.
  • composition of the present invention can be used, for example, as a coating agent for a coating preparation.
  • the coating preparation of the present invention comprises a core substance containing an active ingredient such as a pharmaceutical, a food, a pesticide, or an animal drug, a coating film containing the microfibrous cellulose covering the core substance and a coating base for a preparation.
  • an active ingredient such as a pharmaceutical, a food, a pesticide, or an animal drug
  • a coating film containing the microfibrous cellulose covering the core substance and a coating base for a preparation which is in the form of tablets, pills, granules, fine granules, capsules, etc., but is preferably a tablet or a granule, and more preferably a tablet.
  • a coated preparation obtained by coating the composition of the present invention on the core substance.
  • the coating formulation of the present invention can be obtained by formulation techniques well known in the art, for example, water and / or a liquid composition containing microfibrous cellulose and a formulation coating base. Or a process for preparing a composition by mixing components other than the organic solvent in water and / or an organic solvent, and a process of coating the obtained composition on a core material to form a coating film. And so on.
  • Coating of the above core material can be performed using existing pharmaceutical equipment such as a fluidized bed coating device, a tumbling fluidized bed coating device, a centrifugal tumbling fluidized coating device, and a pan coating device.
  • a method known in the art is used.
  • a composition obtained by dissolving and dispersing components other than water and / or an organic solvent in a liquid composition containing microfibrillated cellulose and a coating base for pharmaceutical preparations in water and / or an organic solvent is used.
  • Spray coating method for spraying the product with existing formulation equipment sugar coating method for spraying and spreading the composition with existing formulation equipment, mixing microfibrous cellulose and formulation coating base Spraying and laminating the mixed powder with existing pharmaceutical equipment Powder laminating coating method, in which the mixed powder is compression-molded around the core material with existing pharmaceutical equipment, etc. Coating or sugar coating
  • the spray coating method is preferred, and the spray coating method is more preferred.
  • the amount of the coating film in the coating preparation is not particularly limited, but is preferably 0.5 to 100% by mass, and preferably 0.5 to 50% by mass with respect to the core substance. /. And more preferably 1 to 30 mass. /. Is more preferable.
  • the core substance may be in any form of tablets, pills, granules, fine granules, capsules and the like, but is preferably a tablet or a granule, more preferably a tablet, and Can be manufactured by a known method.
  • a tablet can be produced by mixing and compressing the active ingredient and a pharmaceutical additive. Before the compression molding, if necessary, a conventional formulation treatment such as wet or dry granulation may be performed. Pills can be manufactured by mixing an active ingredient and a pharmaceutical additive, kneading, dividing, molding, and coating with starch or the like.
  • Condyle granules can be produced by wet or dry granulation after mixing the active ingredient and excipients, and after granulation, the granules may be subjected to a rounding treatment.
  • Capsules can be made by filling granules and / or tablets into capsules.
  • formulation additives are not particularly limited, and any of them that can be used as a solid formulation can be used.
  • Excipients such as lactose, sucrose, D-mannitol, xylidol, erythritol, sorbitol, maltitol, calcium citrate, calcium phosphate, crystalline cellulose, magnesium aluminate metasilicate, etc .
  • corn starch potato Disintegrants such as starch, sodium carboxymethylsulfate, partially starch arsenide, carboxymethylcellulose calcium, carboxymethylcellulose, low-substituted hydroxypropylcellulose, crosslinked carboxymethylcellulose sodium, crosslinked polyvinylpyrrolidone
  • Binders such as propylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol, dextrin, and arsenic starch
  • stearin Lubricants such as magnesium phosphate, calcium stearate
  • Flavors such as orange and strawberry; iron sesquioxide, yellow iron sesquioxide, food yellow 5, food yellow 4, coloring agents such as aluminum chelate; sweeteners such as saccharin and aspartame; citric acid, citric acid Flavoring agents such as sodium, succinic acid, tartaric acid, fumaric acid, and glutamic acid; and solubilizing agents such as cyclodextrin, arginine, lysine, and triaminomethane.
  • Examples of the capsule include, but are not particularly limited to, a gelatin capsule, a hydroxymethylpyrmethylcellulose capsule, a chitosan capsule, a pullulan capsule and the like.
  • the active ingredient that can be used in the present invention is not particularly limited as long as it is acceptable for uses such as pharmaceuticals, foods, agricultural chemicals, and veterinary drugs, and is intended for oral administration or ingestion.
  • Antipyretic analgesic and anti-inflammatory IJ for example, indomethacin, acetylsalicylic acid, diclofenac sodium, ketoprofen, ibuprofen, mefenamic acid, azulene, phenacetin, isopropylantipyrine, acetaminophen, benzazac, phenylbuzon, flufenamic acid
  • steroid anti-inflammatory agents eg, dexamethasone, hydrocortisone, prednisolone, triamcinolone, etc.
  • anti-ulcer agents eg, e.
  • calcium antagonists e.g., benidipine, benidivine hydrochloride, besylidine
  • Peripheral vasodilators eg, ifenprodil tartrate, cinepaside maleate, cyclanderate, cinnarizine, pentoxifylline, etc.
  • antibiotics eg, ampicillin, ⁇ Xicillin, acetylsviramycin, cephalexin, erythromycin ethyl succinate, bacanpicillin hydrochloride, minocycline hydrochloride, chloramphenicol, tetracycline, erythromycin, cefujidimim, cefuroxime sodium, aspoxicillin, litidene mucoxyl hydrate, etc.
  • Synthetic antibacterial agents for example, nalidixic acid, pyromidic acid, Mimic acid trihydrate, enoxacin, sinoxacin, ofloxacin, norfloxacin, ciprofloxacin hydrochloride, sulfamethoxazole'trimethoprim, etc.
  • antiviral agents eg, acyclovir, .gancyclovir, etc.
  • Fungicides eg, ditraconazole, fluconazole, etc.
  • antiseptic agents eg, propantheline bromide, atropine sulfate, oxapium bromide, timevidium bromide, butylscopolamine bromide, trospium chloride, Butium bromide, N-methylscopolamine methyl sulfate, Methyloctabromide pin, etc.
  • Antitussives for example, Tipididine hibenzate, Methyl edrine hydroch
  • bronchodilators e.g., theophylline, aminophylline, sodium chromoglycate, propoterol hydrochloride, trimethokinol hydrochloride, diprofyl
  • Phosphorus Salbuyl sulfate, Chlorprenaline hydrochloride, Formoterol fumarate, Orciprenaline sulfate, Pilbuterol hydrochloride, Hexoprenaline sulfate, Bitolterol mesylate, Clenbuterol hydrochloride, Terbuyuline sulfate, Mabuterol hydrochloride ,
  • -Blocker For example, pisoprol fumarate, pindolol, propranolol hydrochloride, carteolol hydrochloride, metoprolol tartrate, labetrol hydrochloride, acebutolol hydrochloride, butyl alcohol hydrochloride, alprenolol hydrochloride, arotinolol hydrochloride, oxprenolol hydrochloride , Nadolol, bucmorol hydrochloride, indenolol hydrochloride, timolol maleate, befnolol hydrochloride, bupranolol hydrochloride, etc.), (21) antiarrhythmic agents (for example, proamide hydrochloride, disopyramide, adimarin, quinidine sulfate) , salt Aprindin acid, propafenone hydrochloride, mexiletine hydrochloride, azimilide
  • NGF platelet-derived growth factor
  • TGF transforming growth factor
  • ECGF endothelial cell growth factor
  • FGF fibroblast growth factor
  • GGF glial cell growth factor
  • thymosin specific antibody (for example, anti-EGF receptor antibody, etc.), soy protein, phospholipid binding Bean peptide, lactotripeptide, casein phosphopeptide, casein decapeptide, collagen peptide, etc.), (40) nucleic acids (eg, antisense oligonucleotides), (41) sugars (eg, chondroitin sulfate sodium, heparin) Sodium, dextranfluorescein, etc.), (42) live fungi (Bifid Bacteria, lactic acid bacteria, yeast, etc.), (43) oligosaccharides (xylose oligosaccharides, fructooligosaccharides, soybean oligosaccharides, isomaltoligosaccharide
  • the coating preparation of the present invention can be orally administered or ingested, and the administration or ingestion amount varies depending on various conditions such as the type of the active ingredient, the condition of the patient or consumer, and body weight. For example, about 0.01 to 100 mg / lig of the active ingredient per day can be administered or taken.
  • the administration or the number of times of administration is preferably 1 to 3 times a day.
  • imparting strength to the coating formulation refers to increasing the strength of the coating formulation and / or coating film during production and / or storage of the coating formulation. Or to increase the strength of the coating formulation and / or coating when exposed to moisture or moisture.
  • the strength imparting to the coated preparation of the present invention can be achieved by a coating preparation comprising a core substance containing an active ingredient and a coating film containing a coating base for preparation which covers the core substance. It can be carried out in the presence of fibrous cellulose, for example, by producing a coating preparation by the method for producing a coating preparation of the present invention.
  • compositions obtained in Examples 1 to 4 and Comparative Example 1 to be described later were weighed into a petri dish (diameter: 5.8 cm) 3800 mg (300 mg as a solid content) and weighed into a small hot air circulating thermostat (Mini Jet Oven, Toyama Sangyo) After drying at 40 ° C for 2 hours, the film was further dried at 70 ° C for 1 hour to prepare a cast film. Each of the obtained cast membranes was cut into a size of 10 ⁇ 20 to obtain a test piece. Each specimen was immersed in water at 37 ° C for 4 hours in advance.
  • each of the compositions containing 150 mg as a solid content was placed on a petri dish (diameter 5.8 cm) under hot air of a dryer using a two-fluid nozzle (nozzle). It was sprayed with a diameter of 0.8 o'clock / 2.5 mm). Using a small hot air circulating thermostat (Mini Jet Oven, manufactured by Toyama Sangyo), the film was dried at 70 ° C for 1 hour to prepare a cast film. Each of the obtained cast membranes was cut into a size of X20 thighs in five countries to obtain test pieces. Each specimen was immersed in water at 37 ° C for 4 hours.
  • test piece was clamped, and the tensile strength until the test piece was broken was measured at 37 ° C in water at a tensile speed of 10 mm / min using an autograph (AG-20kNG, manufactured by Shimadzu Corporation). Further, cast films prepared from the compositions obtained in Example 5 6 10 and Comparative Example 2 were cut into a size of 5 mm X 20 mm to obtain test pieces. Each test piece was inserted with a clamp, and the tensile strength until the test piece was broken at a tensile speed of 10 mm / min was measured using an autograph (AG-20kNG, manufactured by Shimadzu Corporation) in the air. Table 2 shows the results. Table i3 ⁇ 4 w3 ⁇ 4g ..2
  • Example 1 1 66.0% 7: 3 1.49
  • the cast film of Comparative Example 2 of Experimental Example 2 was compared with the ratio of the strength increase of each cast film of Examples 1 to 4 to the cast film of Comparative Example 1 in which the composition was dried.
  • the percentage of increase in the strength of each cast film in Examples 5 to 8 was larger than that of Example 5.
  • Example 13 With respect to the compositions obtained in Example 13 and Comparative Example 3 described below, an amount of each composition containing 150 mg as a solid content was placed on a petri dish (5.8 cm in diameter) under hot air of a drier using a two-fluid nozzle (nozzle diameter). 0.8 ⁇ / 2.5 ⁇ ). It was dried at 70 ° C for 1 hour using a small hot air circulating thermostat (MiniJittoven, manufactured by Toyama Sangyo) to prepare a cast membrane.
  • a small hot air circulating thermostat MiniJittoven, manufactured by Toyama Sangyo
  • Each of the obtained cast films was cut into a size of 5 strokes ⁇ 20 thighs to obtain test pieces.
  • Each specimen was immersed in water at 37 ° C for 4 hours. Insert the test piece with a clamp, and test it in water at 37 ° C using an autograph (AG-20kNG, manufactured by Shimadzu Corporation) at a pulling speed of 10 mm / min. The tensile strength until the specimen was broken was measured.
  • Example 13 In the cast membrane containing microfibrous cellulose (Example 13), the tensile strength before the test piece was broken was 2.36N.
  • the cast membrane containing untreated powdered cellulose (Comparative Example 3) was broken when inserted with a clamp, and could not be measured. In other words, it was shown that the presence of microfibrous cellulose in the coating film can improve the strength of the coating film when exposed to moisture.
  • the coating preparations obtained in Examples 15 and 16 and Comparative Examples 5 and 6 were subjected to a temperature of 40 ° C and a relative humidity of 75 ° /. For 2 weeks. Each coated preparation before and after storage was compressed with a hardness meter (PTB31K manufactured by Japan Machinery) at a rate of 10 Omni / min in the diameter direction, and the hardness when the preparation was broken was measured. Table 3 shows the results.
  • Formulation strength (N) Formulation strength (N)
  • Example 1 5 30.0% 1: 2 3% 78.0 60.6
  • Example 16 30.03 ⁇ 4 1: 2 5% 104.7 88.9 Comparative example 5 0.0% 0: 1 '3% 75.9 51.4
  • Comparative Example 6 0.0% 0: 1 '5% 113.8 72.4
  • a coating preparation made from a composition containing hydroxypropyl methylcellulose as a main component (Comparative Examples 5 and 6)
  • a coating preparation made from a composition containing microfibrous cellulose (Examples 15 and 16) was used. ) Improves the hardness after storage under humidification. That is, the presence of microfibrous cellulose in the coating film can improve the strength of the coating film in contact with moisture. It has been shown.
  • Example 1 Ethylcellulose (Ethosel, manufactured by Dada Chemical Co., Ltd.) 365.8 mg is sufficiently dissolved in 3222 mg of ethyl cellulose (Kanto Chemical Co., Ltd.), and then glycerin fatty acid ester (Maibaset 9-40, manufactured by Westman Kodak Co., Ltd.) 73. 2 mg and microfibrous cellulose (Selish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) 407. Orag (40, 7 mg as microfibrous cell mouth) were added, and the mixture was stirred and dissolved and dispersed.
  • Ethanol manufactured by Kanto Chemical Co., Ltd.
  • purified water were added in an amount of 1194 mg and 738 mg, respectively, so that the mixing ratio of ethanol: purified water was 8: 2, and the mixture was further stirred to obtain a coating composition.
  • Ethyl cellulose (Ethocel, Dow Chemical Co., Ltd.) 330.8 mg was sufficiently dissolved in ethanol (Kanto Chemical Co., Ltd.) 2913 mg, and then glycerin fatty acid ester (Mybasset 9-40, Eastman Kodak Co., Ltd.) 66.2 mg and Microfibrous cellulose (Serish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) 828. Omg (82.8 mg as microfibrous cellulose) was added, and the mixture was stirred and dissolved and dispersed.
  • Ethanol manufactured by Kanto Chemical Co., Ltd.
  • purified water 1503 mg 'and 359 mg, respectively
  • Ethylcellulose (Ethosel, manufactured by Dow Chemical Company) 295. Omg was sufficiently dissolved in ethanol (manufactured by Kanto Chemical Co., Ltd.) 2594mg, and then glycerin fatty acid ester (Myvaset 9-40, manufactured by Eastman Kodak Company) 59. Omg and 1263 mg of fine fibrous cellulose (Selish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (126.3 mg as fine fibrous cellulose) was added, and the mixture was stirred and dissolved and dispersed. Ethanol (manufactured by Kanto Kagaku) and purified water (3422 mg and 367 mg) were added so that the mixing ratio of ethanol: purified water was 8: 2, and the mixture was further stirred to obtain a coating composition.
  • ethyl cellulose (Ethocel, manufactured by Dow Chemical Company) is sufficiently dissolved in 2263 mg of ethanol (manufactured by Kanto Kagaku Co., Ltd.), and then glycerin fatty acid ester (Myvaset 9-40, manufactured by Eastman Kodak Company) 1714 mg of microfibrillated cellulose (Serish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (171.4 mg as microfibrous cellulose) was added, and the mixture was stirred and dissolved and dispersed.
  • glycerin fatty acid ester (Myvaset 9-40, manufactured by Eastman Kodak Company) 1714 mg of microfibrillated cellulose (Serish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (171.4 mg as microfibrous cellulose) was added, and the mixture was stirred and dissolved and dispersed.
  • Ethanol so that the mixing ratio of ethanol: purified water is 8: 2 (Manufactured by Kagaku) and purified water were added in amounts of 5353 mg and 361 mg, respectively, and further stirred to obtain a coating composition.
  • ethyl cellulose Ethocel, manufactured by Dow Chemical Co.
  • glycerin fatty acid ester (mybaset 9 -40, manufactured by Eastman Kodak Co., Ltd.), and dissolved sufficiently to obtain a coating composition.
  • Example 7 To 10.3 g of solution A in Example 5, 13.7 g of ethanol, 3.4 g of purified water, and 2.6 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (0.26 g of fine fibrous cellulose) were added. The mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 7 To 10.3 g of solution A in Example 5, 13.7 g of ethanol, 3.4 g of purified water, and 2.6 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (0.26 g of fine fibrous cellulose) were added. The mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 7 To 10.3 g of solution A in Example 5, 13.7 g of ethanol, 3.4 g of purified water, and 2.6 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical
  • Example 8 To 9.2 g of solution A in Example 5, 22.3 g of ethanol, 4.Og of purified water and 3.9 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (0.39 g as fine fibrous cellulose) were added. The mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 8 To 9.2 g of solution A in Example 5, 22.3 g of ethanol, 4.Og of purified water and 3.9 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (0.39 g as fine fibrous cellulose) were added. The mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 8 To 9.2 g of solution A in Example 5, 22.3 g of ethanol, 4.Og of purified water and 3.9 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (0
  • Example 9 Solution A in Example 5 8. Og was mixed with 34.6 g of ethanol, 5.6 g of purified water, and 5.4 g of microfibrous cellulose (Selish FD-100Gs manufactured by Daicel Chemical Industries, Ltd.) (0.54 g as microfibrous cellulose). In addition, the mixture was stirred with a homogenizer to obtain a composition for coating.
  • Example 9
  • Example 5 Solution A in Example 5 was mixed with 6,8 g of solution A in an amount of 47.3 g of ethanol, 7.2 g of purified water, and a fine fibrous cell. 6.8 g (0.68 g as microfibrous cellulose) of Lurose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) was added, and the mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 10
  • Example 11 To 5 and 0 g of solution A in Example 5, 54.5 g of ethanol, 8.50 g of purified water and fine fibrous cellulose (Seritsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) 7.5 g (0.75 g as fine fibrous cellulose) was added and stirred with a homogenizer to obtain a coating composition.
  • Example 11 To 5 and 0 g of solution A in Example 5, 54.5 g of ethanol, 8.50 g of purified water and fine fibrous cellulose (Seritsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) 7.5 g (0.75 g as fine fibrous cellulose) was added and stirred with a homogenizer to obtain a coating composition.
  • Example 11 To 5 and 0 g of solution A in Example 5, 54.5 g of ethanol, 8.50 g of purified water and fine fibrous cellulose (Seritsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) 7.5 g (0
  • Example 12 To 6 g of solution A in Example 5, 66.9 g of ethanol, 9.5 g of purified water, and 8.9 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) were added 8.9 g (0.89 g as fine fibrous cellulose). In addition, the mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 12 To 6 g of solution A in Example 5, 66.9 g of ethanol, 9.5 g of purified water, and 8.9 g of fine fibrous cellulose (Selitsch FD-100G, manufactured by Daicel Chemical Industries, Ltd.) were added 8.9 g (0.89 g as fine fibrous cellulose). In addition, the mixture was stirred with a homogenizer to obtain a coating composition.
  • Example 12 To 6 g of solution A in Example 5, 66.9 g of ethanol, 9.5 g of purified water, and 8.9 g of fine fibrous cellulose (S
  • Example 5 2.6 g of solution A in Example 5 was mixed with 79.7 g of ethanol, 11.2 g of purified water, and 10.4 g of fine fibrous cellulose (Selish FD-100G, manufactured by Daicel Chemical Industries, Ltd.) (1.04 g of fine fibrous cell opening). g) was added, and the mixture was stirred with a homogenizer to obtain a coating composition. Comparative Example 2
  • This suspension was diluted with purified water, and 10 g of the suspension (O.lg as microfibrous cellulose) was stirred with a homogenizer (Ultra Yulux T25, manufactured by Japan Co., Ltd.) for 10 minutes at 110 rpm, and then amino Alkyl methacrylate acrylate copolymer RS (Eid Ladgit RS30D, manufactured by Higuchi Shokai) 0.33 g (0.1 g as a solid content), 9.67 g of purified water and 0.02 g of triethyl citrate (Citroflex, Cal Yuichi Food Science) It was added, dissolved and dispersed to obtain a coating composition. Comparative Example 3
  • Example 14 0.1 lg of powdered cellulose (ARBOCEL M80, manufactured by J. RETTE Kako AIER) was dispersed in 9.9 g of purified water. Aminoalkyl methyl acrylate copolymer 0.33 (0.1 g as solid content), purified water 9.67 g and triethyl citrate 0.02 g were added to the resulting dispersion, dissolved and dispersed, and coated. The composition for use was obtained.
  • Example 14 Example 14
  • a homogenizer Ultra Tarax T25, manufactured by Japan Ltd.
  • Example 15 hydroxypropylpyrmethylcellulose (TC-5, Shin-Etsu Chemical Co., Ltd.) and 1.8 g of polyethylene glycol (Macrogol 6000, Nippon Oil & Fats Co., Ltd.) were added to 171 g of ethanol (Kanto Chemical Co., Ltd.) and 171 g of purified water. The composition was dissolved in the mixed solution to obtain a coating composition.
  • TC-5 Shin-Etsu Chemical Co., Ltd.
  • polyethylene glycol Macrogol 6000, Nippon Oil & Fats Co., Ltd.
  • TBM type mixer (TBM-8, manufactured by Tokuju Kogyo Co., Ltd.) containing 4450 g of lactose (Even Bretez 80, manufactured by Megure Japan), 500 g of microcrystalline cellulose (Avicel 1-1101, manufactured by Asahi Kasei Corporation) and 50 g of magnesium stearate ), And the resulting mixed powder is mixed with a punch-type tableting machine (Correct 12HUK, manufactured by Kikusui Seisakusho) using a pestle with a diameter of 7 and a radius of curvature of 10 strokes. Tablets were made to have a thickness of 3.7 thighs to obtain uncoated tablets.
  • Example 14 The composition obtained in Example 14 was applied to 230 g of the uncoated tablet using a pan coating machine (Doriaco Ichiichi DRC200, manufactured by Powrex) until the coating rate became about 3% for 130 mg of uncoated tablet. Spray coated and dried at about 50 ° C. to give a coating formulation of hydroxypropylmethylcellulose and microfibrillated cellulose.
  • a pan coating machine (Doriaco Ichiichi DRC200, manufactured by Powrex) until the coating rate became about 3% for 130 mg of uncoated tablet.
  • Example 16 Example 16
  • Example 14 The composition obtained in Example 14 was coated on the core substance in Example 15 by 5% by mass with respect to the core substance in the same manner as in Example 15 to obtain a coated preparation.
  • Comparative Example 4 The composition obtained in Comparative Example 4 was added to the core substance in Example 15 in the same manner as in Example 15, and 3 parts by weight based on the core substance. /. Coating yielded a coated formulation.
  • composition obtained in Comparative Example 4 was coated on the core substance in Example 15 by 5% by mass with respect to the core substance in the same manner as in Example 15 to obtain a coating preparation.
  • a coating preparation comprising a core substance containing an active ingredient such as a drug, food, agrochemical, veterinary drug, etc. and a coating film covering the core substance, during the production and / or storage of the coating preparation.
  • a composition useful for preparing a coating film having high strength even when the coating formulation comes into contact with moisture or water-a coating formulation containing the composition in a coating film Etc. are provided.

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Abstract

L'invention concerne une composition caractérisée en ce qu'elle comprend des fibres fines de cellulose et une base d'enrobage pour des préparations sensiblement exemptes de chitosane. Cette composition est utilisée pour produire une préparation enrobée comprenant une substance de noyau contenant un ingrédient actif, tel qu'un agent pharmaceutique, un produit alimentaire, un produit agrochimique ou un produit chimique pour animaux, ainsi qu'un film d'enrobage enrobant le noyau. Cette composition est utile pour former le film d'enrobage, qui possède une résistance accrue au cours de la production et/ou du stockage de la préparation enrobée ou même lorsque ladite préparation vient en contact avec de l'humidité ou de l'eau. L'invention concerne également une préparation enrobée comprenant un film d'enrobage contenant ladite composition.
PCT/JP2004/008166 2003-06-04 2004-06-04 Composition d'enrobage et preparation enrobee WO2004108164A1 (fr)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006289164A (ja) * 2005-04-06 2006-10-26 Agri Future Joetsu Co Ltd バイオマス由来成分が分散した液状組成物、その製造方法及びこの液状組成物から製造される製品
WO2008013084A1 (fr) * 2006-07-25 2008-01-31 Kowa Company, Ltd. Préparation enrobée de sucre et son procédé de fabrication
JP5669050B2 (ja) * 2010-01-15 2015-02-12 国立大学法人島根大学 骨セメント
WO2015163135A1 (fr) * 2014-04-21 2015-10-29 株式会社ダイセル Composition particulaire apte à se désagréger comprenant de la cellulose microfibreuse
JP2016537429A (ja) * 2013-11-22 2016-12-01 シノセラピューティックス、インコーポレイテッドＳｉｎｏｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． フェロポルフィリン固体分散体およびその製造方法

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JPS58191296A (ja) * 1982-05-04 1983-11-08 ダイセル化学工業株式会社 紙用塗料組成物
JPH072701A (ja) * 1993-06-17 1995-01-06 Aisero Kagaku Kk 大腸崩壊性組成物及びその製造法
JPH09509694A (ja) * 1994-03-01 1997-09-30 エルフ アトケム ソシエテ アノニム ミクロフィブリルセルロース強化ポリマーとその利用
JPH1095803A (ja) * 1995-11-02 1998-04-14 Bio Polymer Res:Kk セルロース被膜及びその形成方法
JP2002521577A (ja) * 1998-07-24 2002-07-16 リージェンツ オブ ザ ユニバーシティ オブ ミネソタ セルロース繊維をベースとした組成物およびフィルム
JP2002536507A (ja) * 1999-02-10 2002-10-29 ハーキュリーズ・インコーポレイテッド 誘導微小繊維ポリサッカライド

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Publication number Priority date Publication date Assignee Title
JPS58191296A (ja) * 1982-05-04 1983-11-08 ダイセル化学工業株式会社 紙用塗料組成物
JPH072701A (ja) * 1993-06-17 1995-01-06 Aisero Kagaku Kk 大腸崩壊性組成物及びその製造法
JPH09509694A (ja) * 1994-03-01 1997-09-30 エルフ アトケム ソシエテ アノニム ミクロフィブリルセルロース強化ポリマーとその利用
JPH1095803A (ja) * 1995-11-02 1998-04-14 Bio Polymer Res:Kk セルロース被膜及びその形成方法
JP2002521577A (ja) * 1998-07-24 2002-07-16 リージェンツ オブ ザ ユニバーシティ オブ ミネソタ セルロース繊維をベースとした組成物およびフィルム
JP2002536507A (ja) * 1999-02-10 2002-10-29 ハーキュリーズ・インコーポレイテッド 誘導微小繊維ポリサッカライド

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006289164A (ja) * 2005-04-06 2006-10-26 Agri Future Joetsu Co Ltd バイオマス由来成分が分散した液状組成物、その製造方法及びこの液状組成物から製造される製品
WO2008013084A1 (fr) * 2006-07-25 2008-01-31 Kowa Company, Ltd. Préparation enrobée de sucre et son procédé de fabrication
JPWO2008013084A1 (ja) * 2006-07-25 2009-12-17 興和株式会社 糖衣製剤およびその製造方法
JP5669050B2 (ja) * 2010-01-15 2015-02-12 国立大学法人島根大学 骨セメント
JP2016537429A (ja) * 2013-11-22 2016-12-01 シノセラピューティックス、インコーポレイテッドＳｉｎｏｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． フェロポルフィリン固体分散体およびその製造方法
WO2015163135A1 (fr) * 2014-04-21 2015-10-29 株式会社ダイセル Composition particulaire apte à se désagréger comprenant de la cellulose microfibreuse
JPWO2015163135A1 (ja) * 2014-04-21 2017-04-13 株式会社ダイセル 微小繊維状セルロースを含む崩壊性粒子組成物
EP3135300A4 (fr) * 2014-04-21 2017-09-20 Daicel Corporation Composition particulaire apte à se désagréger comprenant de la cellulose microfibreuse
AU2015251692B2 (en) * 2014-04-21 2019-12-19 Daicel Corporation Disintegrating particle composition including microfibrous cellulose
US10828257B2 (en) 2014-04-21 2020-11-10 Daicel Corporation Disintegrating particle composition including microfibrous cellulose

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