WO2006123765A1 - Preparation recouverte d’un film - Google Patents
Preparation recouverte d’un film Download PDFInfo
- Publication number
- WO2006123765A1 WO2006123765A1 PCT/JP2006/309993 JP2006309993W WO2006123765A1 WO 2006123765 A1 WO2006123765 A1 WO 2006123765A1 JP 2006309993 W JP2006309993 W JP 2006309993W WO 2006123765 A1 WO2006123765 A1 WO 2006123765A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- film
- film coating
- coating preparation
- preparation according
- film layer
- Prior art date
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- 238000002360 preparation method Methods 0.000 title claims abstract description 51
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000000203 mixture Substances 0.000 claims abstract description 13
- 238000009472 formulation Methods 0.000 claims abstract description 12
- 229940079593 drug Drugs 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims abstract description 11
- 239000007888 film coating Substances 0.000 claims description 53
- 238000009501 film coating Methods 0.000 claims description 53
- 239000011248 coating agent Substances 0.000 claims description 24
- 238000000576 coating method Methods 0.000 claims description 24
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims description 13
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 11
- 239000004014 plasticizer Substances 0.000 claims description 11
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
- 239000002051 C09CA08 - Olmesartan medoxomil Substances 0.000 claims description 8
- UQGKUQLKSCSZGY-UHFFFAOYSA-N Olmesartan medoxomil Chemical compound C=1C=C(C=2C(=CC=CC=2)C2=NNN=N2)C=CC=1CN1C(CCC)=NC(C(C)(C)O)=C1C(=O)OCC=1OC(=O)OC=1C UQGKUQLKSCSZGY-UHFFFAOYSA-N 0.000 claims description 8
- 235000013773 glyceryl triacetate Nutrition 0.000 claims description 8
- 229960001199 olmesartan medoxomil Drugs 0.000 claims description 8
- 229960002622 triacetin Drugs 0.000 claims description 8
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 7
- 239000008121 dextrose Substances 0.000 claims description 7
- 239000004375 Dextrin Substances 0.000 claims description 6
- 229920001353 Dextrin Polymers 0.000 claims description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- 235000019425 dextrin Nutrition 0.000 claims description 6
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims description 6
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 5
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 5
- 239000005913 Maltodextrin Substances 0.000 claims description 5
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
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- 239000008101 lactose Substances 0.000 claims description 5
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- 239000000600 sorbitol Substances 0.000 claims description 5
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- 239000008199 coating composition Substances 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 229920000609 methyl cellulose Polymers 0.000 claims description 4
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- 235000010981 methylcellulose Nutrition 0.000 claims description 4
- 125000005541 phosphonamide group Chemical group 0.000 claims description 4
- 239000001856 Ethyl cellulose Substances 0.000 claims description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 3
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- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 3
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- 229920003144 amino alkyl methacrylate copolymer Polymers 0.000 claims description 3
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 3
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- 239000011734 sodium Substances 0.000 claims description 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- PGIBJVOPLXHHGS-UHFFFAOYSA-N Di-n-decyl phthalate Chemical compound CCCCCCCCCCOC(=O)C1=CC=CC=C1C(=O)OCCCCCCCCCC PGIBJVOPLXHHGS-UHFFFAOYSA-N 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
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- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 abstract description 9
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 abstract description 9
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 abstract description 9
- 239000003826 tablet Substances 0.000 description 20
- 235000019645 odor Nutrition 0.000 description 17
- 239000007941 film coated tablet Substances 0.000 description 9
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- -1 D-mannthol Polymers 0.000 description 6
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- 201000001421 hyperglycemia Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 229960003963 manidipine Drugs 0.000 description 1
- ANEBWFXPVPTEET-UHFFFAOYSA-N manidipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN2CCN(CC2)C(C=2C=CC=CC=2)C=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ANEBWFXPVPTEET-UHFFFAOYSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- 239000004570 mortar (masonry) Substances 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 201000009925 nephrosclerosis Diseases 0.000 description 1
- PKWDZWYVIHVNKS-UHFFFAOYSA-N netoglitazone Chemical compound FC1=CC=CC=C1COC1=CC=C(C=C(CC2C(NC(=O)S2)=O)C=C2)C2=C1 PKWDZWYVIHVNKS-UHFFFAOYSA-N 0.000 description 1
- 229960001597 nifedipine Drugs 0.000 description 1
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 229950003510 pactimibe Drugs 0.000 description 1
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 1
- 229960005095 pioglitazone Drugs 0.000 description 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229960002965 pravastatin Drugs 0.000 description 1
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- XMSXOLDPMGMWTH-UHFFFAOYSA-N rivoglitazone Chemical compound CN1C2=CC(OC)=CC=C2N=C1COC(C=C1)=CC=C1CC1SC(=O)NC1=O XMSXOLDPMGMWTH-UHFFFAOYSA-N 0.000 description 1
- 229950010764 rivoglitazone Drugs 0.000 description 1
- 229960004586 rosiglitazone Drugs 0.000 description 1
- 229960000672 rosuvastatin Drugs 0.000 description 1
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 description 1
- 229960002855 simvastatin Drugs 0.000 description 1
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 description 1
- 238000004513 sizing Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 150000007944 thiolates Chemical class 0.000 description 1
- 229960004813 trichlormethiazide Drugs 0.000 description 1
- LMJSLTNSBFUCMU-UHFFFAOYSA-N trichlormethiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC(C(Cl)Cl)NS2(=O)=O LMJSLTNSBFUCMU-UHFFFAOYSA-N 0.000 description 1
- UJMBCXLDXJUMFB-UHFFFAOYSA-K trisodium;5-oxo-1-(4-sulfonatophenyl)-4-[(4-sulfonatophenyl)diazenyl]-4h-pyrazole-3-carboxylate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-UHFFFAOYSA-K 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Definitions
- the present invention relates to a film coating preparation.
- Patent Document 1 Japanese Patent Laid-Open No. 2003-300883
- An object of the present invention is to provide a film coating preparation capable of reducing the odor of a drug.
- the present inventors have surprisingly found that the odor of the formulation can be reduced by coating with a film layer containing sodium carboxymethyl cellulose, and the present invention has been completed. I let you.
- the present invention provides:
- Plasticizer strength Macrogol 6000 propylene glycol, polyethylene glycol, polypropylene glycol, glycerin and sorbitol, glycerin triacetate, phthalate, ethyl triethyl thiolate, lauric acid, sucrose, dextrose, sorbitol, triacetin, aceti (1) a film coating preparation according to (8), which is one or more compounds selected from noretretino recitrate, tritino recitrate, tributino recitrate, and acetiltyl butyl titrate;
- the film coating preparation of the present invention contains sodium carboxymethyl cellulose (CMC-Na) in the film layer.
- CMC-Na sodium carboxymethyl cellulose
- the content of sodium carboxymethylcellulose in the film layer is not particularly limited as long as it can effectively reduce the odor of the drug, but usually the lower limit is 20% (w / w) or more. 30% (w / w) or more, more preferably 40% (w / w) or more, and the upper limit is 90% (w / w) or less, preferably 80% (w / w) ) Or less, more preferably 70% (w / w) or less.
- coating bases or excipients can be blended as necessary.
- the type of coating base or excipient is not particularly limited and can be appropriately selected by those skilled in the art. Can be selected.
- Such coating bases or excipients include, for example, polyvinylbiridone (PVP), polyvinyl alcohol (PVA), methylcellulose, ethylcellulose, hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), dextrin, malto Mention may be made of dextrin, lactose, D-mannthol, polybutyl alcohol polymer, methacrylic acid copolymer, aminoalkyl methacrylate copolymer and ethyl acrylate 'methyl methacrylate copolymer.
- PVP polyvinylbiridone
- PVA polyvinyl alcohol
- HPMC hydroxypropylmethylcellulose
- dextrin malto Mention may be made of dextrin, lactose, D-mannthol,
- the coating composition may be added with one or more additives such as plasticizers, excipients, lubricants, hiding agents, colorants, preservatives and the like in the usual amounts. Can be included.
- additives such as plasticizers, excipients, lubricants, hiding agents, colorants, preservatives and the like in the usual amounts. Can be included.
- plasticizer that can be used in the present invention is not particularly limited, and can be appropriately selected by those skilled in the art.
- plasticizers include, for example, Macrogol 6000, propylene glycol, polyethylene glycol, polypropylene glycol, glycerin and sorbitol, glycerin triacetate, ethyl phthalate and triethyl taenoate, lauric acid, sucrose, dextrose, sonolebithonole, Examples include triacetin, acetinoretretinorecitrate, trietinoretrate, tributyltitrate, and acetitributylbutyrate.
- excipients examples include lactose, mannitol, crystalline cellulose, dextrose, maltodextrin, and the like.
- Examples of the lubricant that can be used in the present invention include talc, magnesium stearate, calcium stearate, and stearic acid.
- Examples of the concealing agent that can be used in the present invention include titanium oxide.
- Examples of the colorant that can be used in the present invention include titanium oxide, iron oxide, iron sesquioxide, yellow iron sesquioxide, yellow No. 5 aluminum lake talc and the like.
- antiseptics examples include novene and the like.
- the active ingredient contained in the film coating preparation is not limited by the structure, degree, etc. as long as it is a odorous drug, but preferably olmesartan medoxomil or 2-amino-5 -Isobutyl-4- ⁇ 2- [5- ( ⁇ , ⁇ '-bis ((S) -l-ethoxycarbol) ethyl) phosphonamide] fuller ⁇ thiazole, particularly preferably olmesartan Medoxomil. Olmesartan medoxomil is not suitable for hypertension or hypertension.
- Blood pressure more specifically, hypertension, heart disease [angina, myocardial infarction, arrhythmia, heart failure or cardiac hypertrophy], kidney disease [diabetic nephropathy, glomerulonephritis or nephrosclerosis] Or cerebrovascular disease [cerebral infarction or cerebral hemorrhage]
- 2-amino-5-isobutyl-4- ⁇ 2- [5- ( ⁇ , ⁇ '-bis ((S) -l-ethoxycarbol) ethyl) phosphonamide] fuller ⁇ thiazole is a diabetic It is effective for the prevention or treatment of hyperglycemia, glucose intolerance, obesity, diabetic complications, etc. (preferably prevention or treatment of diabetes), and easily according to the method described in WO 01Z47935 pamphlet etc. Can be manufactured.
- the film coating preparation of the present invention may contain other effective components as necessary.
- the active ingredient include diuretics such as Trichlor omethiazide, Hydrochlorothiazide ⁇ Benzylhydrochlorothiazide; Azelnidipine, Amlodipine ), Vedipine, -Trendepin, Manidipine, -Cardipine, Nifedipine, Sildidipine, Efonidipine, Calcium antagonists such as rudidipine (Barnidipine) and ferrodipine (Fel odipine); pioglitazone (Rosigl itazone), riboglitazone (Rivoglitazone), MCC-555, NN-2344, BMS-298585, AZ -242, LY-519818, insulin resistance improvers such as TAK-559; pravastatin, simvastatin, atorvastatin HMG-CoA reductase inhibitors such as (A)
- Examples of the film coating preparation in the present invention include tablets, capsules, powders, fine granules, granules, troches and the like, and tablets are preferred.
- the film coating preparation prepared by this method is obtained by spraying a film coating solution containing carboxymethyl cellulose sodium as a coating base onto an object to be coated such as a tablet or drug substance. Can do.
- the object to be coated may be sub-coated if desired.
- the film coating solution is obtained by suspending and dissolving sodium carboxymethylcellulose and the above-mentioned additive blended if necessary in water.
- the spraying of the film coating solution may be performed by a known method such as using a commercially available film coating machine. These production conditions may be the same as those used in the production of ordinary film coating preparations.
- the amount of the film coating is not particularly limited as long as it is an amount that can effectively reduce the odor of the drug, but usually the lower limit is 1% (w / w) or more with respect to the prescription weight, preferably 3% (w / w) or more, more preferably 6% (w / w) or more, and the upper limit is 50% (w / w) or less, preferably 20% (w / w) or less, based on the prescription weight, More preferably, the concentration is 10% (w / w) or less.
- the thickness of the film layer is not particularly limited as long as it can effectively reduce the odor of the drug, but the lower limit is usually 1 m or more, preferably 5 m or more, more preferably 10 m or more. Particularly preferably, it is 20 ⁇ m or more, and the upper limit is 1000 ⁇ m or less, preferably 500 ⁇ m or less, more preferably 200 ⁇ m or less, and particularly preferably 100 ⁇ m or less.
- the film thickness of the film layer can be measured with an ultra-deep color 3D shape measuring microscope VK-9500 (Keyence Co., Ltd.).
- the film coating preparation of the present invention obtained by caulking may be administered in the same manner as a normal preparation.
- Olmesartan medoxomil 300g, lactose 1850g, hydroxypropylmethylcellulose 60g, croscarmellose sodium 175g are mixed with a high-speed stirring granulator (VG-10, Baurec), granulated with 500g of purified water, and fluidized bed dryer (Baurec).
- the granulated product was sized with a sizing machine (Comil, Norrec) and mixed with 15 g of magnesium stearate in a mixer (V-type mixer, Tokuju Seisakusho).
- Tablets and uncoated tablets were obtained with a rotary tableting machine (Kikusui Seisakusho) using a mortar with a diameter of 7 mm and an R face with a curvature radius of 8 mm so that the weight of each tablet was 160 mg.
- a coating solution in which hydroxypropylmethylcellulose 140 g, talc 30 g, and titanium oxide 30 g are suspended in 1800 g of purified water, 1000 g of the uncoated tablet obtained in Example 1, a coating machine (Driacoater DRC-300, Norec) is used.
- the film-coated tablet (B) was obtained by coating 6% (w / w) with respect to the uncoated tablet weight.
- the uncoated tablet and film-coated tablet (A) produced in Example 1 and 30 film-coated tablets (B) produced in Comparative Example 1 were placed in a glass bottle and stored at 40 ° C. for 3 hours. The glass bottle was opened, and five subjects performed a sensory test of odor according to the following evaluation criteria. The results are shown in Table 1.
- Example 2 Using the coating solution obtained by suspending 140 g of hydroxypropylmethylcellulose, 30 g of talc, and 30 g of titanium oxide in 1800 g of purified water to the plain tablet lOOOOg obtained in Example 1, it was applied to a coating machine (Driacoater DRC-300, Palek). Then, 6% (w / w) coating was performed on the weight of the uncoated tablet to obtain a film-coated tablet (D).
- a coating machine Driacoater DRC-300, Palek
- Example 2 In a glass bottle, the uncoated tablet produced in Example 1 and the film-coated tablet produced in Example 2 ( C), film-coated tablets produced in Comparative Example 2 (D) 30 tablets each, 40 Stored at C for 3 hours. The glass bottle was opened, and the odor sensory test was conducted by the five subjects according to the following evaluation criteria. The results are shown in Table 2.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2007516344A JP5000491B2 (ja) | 2005-05-20 | 2006-05-19 | フィルムコーティング製剤 |
CN2006800157266A CN101171006B (zh) | 2005-05-20 | 2006-05-19 | 薄膜包衣制剂 |
KR1020077026731A KR101318032B1 (ko) | 2005-05-20 | 2006-05-19 | 필름 코팅 제제 |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005147436 | 2005-05-20 | ||
JP2005-147436 | 2005-05-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2006123765A1 true WO2006123765A1 (fr) | 2006-11-23 |
Family
ID=37431333
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/JP2006/309993 WO2006123765A1 (fr) | 2005-05-20 | 2006-05-19 | Preparation recouverte d’un film |
Country Status (5)
Country | Link |
---|---|
JP (1) | JP5000491B2 (fr) |
KR (1) | KR101318032B1 (fr) |
CN (1) | CN101171006B (fr) |
TW (1) | TWI367755B (fr) |
WO (1) | WO2006123765A1 (fr) |
Cited By (15)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2008050714A1 (fr) * | 2006-10-25 | 2008-05-02 | Daiichi Sankyo Company, Limited | Matériel de conditionnement |
WO2008078727A1 (fr) * | 2006-12-26 | 2008-07-03 | Daiichi Sankyo Company, Limited | Composition pharmaceutique à capacité de dissolution améliorée |
WO2008078728A1 (fr) * | 2006-12-26 | 2008-07-03 | Daiichi Sankyo Company, Limited | Composition pharmaceutique contenant de l'acide ascorbique |
WO2009057569A1 (fr) * | 2007-10-29 | 2009-05-07 | Daiichi Sankyo Company, Limited | Préparation pelliculée |
WO2010018777A1 (fr) * | 2008-08-11 | 2010-02-18 | 第一三共株式会社 | Procédé de lutte contre les mauvaises odeurs |
JPWO2008069262A1 (ja) * | 2006-12-07 | 2010-03-25 | 第一三共株式会社 | 安定性が改善されたフィルムコーティング製剤 |
CN102028663A (zh) * | 2010-12-14 | 2011-04-27 | 北京万生药业有限责任公司 | 一种稳定的奥美沙坦酯固体制剂 |
JP2011195567A (ja) * | 2010-02-26 | 2011-10-06 | Daiichi Sankyo Co Ltd | 錠剤 |
WO2012029820A1 (fr) | 2010-08-31 | 2012-03-08 | 東レ株式会社 | Agent de revêtement pour préparation solide pharmaceutique, formulation de film pharmaceutique, et préparation solide pharmaceutique revêtue |
JP2014517046A (ja) * | 2011-06-24 | 2014-07-17 | アセンダ ファーマ インコーポレイテッド | エステルプロドラッグの吸収を改善するための方法及び改善された医薬組成物 |
WO2014188728A1 (fr) * | 2013-05-24 | 2014-11-27 | 持田製薬株式会社 | Composition pour enrobage par film |
JP2016044170A (ja) * | 2014-08-27 | 2016-04-04 | 日本ケミファ株式会社 | オルメサルタンのプロドラッグ製剤 |
JP2017001999A (ja) * | 2015-06-12 | 2017-01-05 | 富士フイルム株式会社 | 薬物含有粒子の製造方法、薬物含有粒子、医薬組成物、及び口腔内崩壊錠 |
WO2017164208A1 (fr) * | 2016-03-24 | 2017-09-28 | 第一三共株式会社 | Médicament pour le traitement d'une maladie rénale |
CN114522146A (zh) * | 2022-01-21 | 2022-05-24 | 上海睿奕生物科技有限公司 | 白色无钛薄膜包衣材料及其制备方法和制备应用 |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
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TWI461215B (zh) * | 2011-06-24 | 2014-11-21 | Acenda Pharma Inc | 用以改善酯類前驅藥吸收率的方法與改良之藥學組合物 |
KR102103530B1 (ko) * | 2018-06-29 | 2020-04-22 | 주식회사 코피텍 | 필름 코팅용 조성물 및 이를 코팅한 정제 |
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JP2003048852A (ja) * | 2000-11-21 | 2003-02-21 | Sankyo Co Ltd | 医薬組成物 |
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CA2322293A1 (fr) * | 1998-12-31 | 2000-07-13 | Hercules Incorporated | Compositions d'hydroxypropylcellulose et de polymere anionique et leur emploi comme enrobage par film pour produits pharmaceutiques |
HUP0204092A3 (en) * | 1999-12-22 | 2005-02-28 | Metabasis Therapeutics Inc San | Novel bisamidate phosphononate prodrugs |
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BR0115516A (pt) * | 2000-11-21 | 2004-02-03 | Sankyo Co | Composição farmacêutica, e, método para prevenir ou tratar hipertensão |
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2006
- 2006-05-19 TW TW095117776A patent/TWI367755B/zh not_active IP Right Cessation
- 2006-05-19 KR KR1020077026731A patent/KR101318032B1/ko active Active
- 2006-05-19 WO PCT/JP2006/309993 patent/WO2006123765A1/fr active Application Filing
- 2006-05-19 JP JP2007516344A patent/JP5000491B2/ja not_active Expired - Fee Related
- 2006-05-19 CN CN2006800157266A patent/CN101171006B/zh active Active
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WO2008050714A1 (fr) * | 2006-10-25 | 2008-05-02 | Daiichi Sankyo Company, Limited | Matériel de conditionnement |
JPWO2008069262A1 (ja) * | 2006-12-07 | 2010-03-25 | 第一三共株式会社 | 安定性が改善されたフィルムコーティング製剤 |
JP5241511B2 (ja) * | 2006-12-26 | 2013-07-17 | 第一三共株式会社 | 溶出性の改善された医薬組成物 |
WO2008078728A1 (fr) * | 2006-12-26 | 2008-07-03 | Daiichi Sankyo Company, Limited | Composition pharmaceutique contenant de l'acide ascorbique |
WO2008078727A1 (fr) * | 2006-12-26 | 2008-07-03 | Daiichi Sankyo Company, Limited | Composition pharmaceutique à capacité de dissolution améliorée |
TWI414310B (zh) * | 2006-12-26 | 2013-11-11 | Daiichi Sankyo Co Ltd | 溶出性改善之醫藥品組成物 |
WO2009057569A1 (fr) * | 2007-10-29 | 2009-05-07 | Daiichi Sankyo Company, Limited | Préparation pelliculée |
JPWO2009057569A1 (ja) * | 2007-10-29 | 2011-03-10 | 第一三共株式会社 | フィルムコーティング製剤 |
WO2010018777A1 (fr) * | 2008-08-11 | 2010-02-18 | 第一三共株式会社 | Procédé de lutte contre les mauvaises odeurs |
JP5688799B2 (ja) * | 2008-08-11 | 2015-03-25 | 第一三共株式会社 | におい抑制方法 |
JP2015017136A (ja) * | 2008-08-11 | 2015-01-29 | 第一三共株式会社 | におい抑制方法 |
JP2011195567A (ja) * | 2010-02-26 | 2011-10-06 | Daiichi Sankyo Co Ltd | 錠剤 |
WO2012029820A1 (fr) | 2010-08-31 | 2012-03-08 | 東レ株式会社 | Agent de revêtement pour préparation solide pharmaceutique, formulation de film pharmaceutique, et préparation solide pharmaceutique revêtue |
US9381248B2 (en) | 2010-08-31 | 2016-07-05 | Toray Industries, Inc. | Coating agent for pharmaceutical solid preparation, pharmaceutical film formulation, and coated pharmaceutical solid preparation |
CN102028663A (zh) * | 2010-12-14 | 2011-04-27 | 北京万生药业有限责任公司 | 一种稳定的奥美沙坦酯固体制剂 |
JP2014517046A (ja) * | 2011-06-24 | 2014-07-17 | アセンダ ファーマ インコーポレイテッド | エステルプロドラッグの吸収を改善するための方法及び改善された医薬組成物 |
WO2014188728A1 (fr) * | 2013-05-24 | 2014-11-27 | 持田製薬株式会社 | Composition pour enrobage par film |
JPWO2014188728A1 (ja) * | 2013-05-24 | 2017-02-23 | 持田製薬株式会社 | フィルムコーティング用組成物 |
JP2016044170A (ja) * | 2014-08-27 | 2016-04-04 | 日本ケミファ株式会社 | オルメサルタンのプロドラッグ製剤 |
JP2017001999A (ja) * | 2015-06-12 | 2017-01-05 | 富士フイルム株式会社 | 薬物含有粒子の製造方法、薬物含有粒子、医薬組成物、及び口腔内崩壊錠 |
WO2017164208A1 (fr) * | 2016-03-24 | 2017-09-28 | 第一三共株式会社 | Médicament pour le traitement d'une maladie rénale |
CN108778334A (zh) * | 2016-03-24 | 2018-11-09 | 第三共株式会社 | 用于治疗肾脏疾病的药物 |
CN114522146A (zh) * | 2022-01-21 | 2022-05-24 | 上海睿奕生物科技有限公司 | 白色无钛薄膜包衣材料及其制备方法和制备应用 |
Also Published As
Publication number | Publication date |
---|---|
TWI367755B (en) | 2012-07-11 |
KR20080011394A (ko) | 2008-02-04 |
TW200719891A (en) | 2007-06-01 |
CN101171006B (zh) | 2010-12-01 |
CN101171006A (zh) | 2008-04-30 |
KR101318032B1 (ko) | 2013-10-14 |
JP5000491B2 (ja) | 2012-08-15 |
JPWO2006123765A1 (ja) | 2008-12-25 |
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