JP5758899B2 - 活性物質を含有するコーティングにより被覆されたペレット - Google Patents
活性物質を含有するコーティングにより被覆されたペレット Download PDFInfo
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- JP5758899B2 JP5758899B2 JP2012529229A JP2012529229A JP5758899B2 JP 5758899 B2 JP5758899 B2 JP 5758899B2 JP 2012529229 A JP2012529229 A JP 2012529229A JP 2012529229 A JP2012529229 A JP 2012529229A JP 5758899 B2 JP5758899 B2 JP 5758899B2
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- COHYTHOBJLSHDF-UHFFFAOYSA-N indigo powder Natural products N1C2=CC=CC=C2C(=O)C1=C1C(=O)C2=CC=CC=C2N1 COHYTHOBJLSHDF-UHFFFAOYSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000001023 inorganic pigment Substances 0.000 description 1
- 229910003480 inorganic solid Inorganic materials 0.000 description 1
- 239000002917 insecticide Substances 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000010410 layer Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 1
- GVALZJMUIHGIMD-UHFFFAOYSA-H magnesium phosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 description 1
- 239000004137 magnesium phosphate Substances 0.000 description 1
- 229910000157 magnesium phosphate Inorganic materials 0.000 description 1
- 229960002261 magnesium phosphate Drugs 0.000 description 1
- 235000010994 magnesium phosphates Nutrition 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229910052919 magnesium silicate Inorganic materials 0.000 description 1
- 235000019792 magnesium silicate Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- NMJORVOYSJLJGU-UHFFFAOYSA-N methane clathrate Chemical compound C.C.C.C.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O.O NMJORVOYSJLJGU-UHFFFAOYSA-N 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- 239000003158 myorelaxant agent Substances 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 239000011356 non-aqueous organic solvent Substances 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- JFOJYGMDZRCSPA-UHFFFAOYSA-J octadecanoate;tin(4+) Chemical compound [Sn+4].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O JFOJYGMDZRCSPA-UHFFFAOYSA-J 0.000 description 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000003605 opacifier Substances 0.000 description 1
- 229940023490 ophthalmic product Drugs 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 239000008012 organic excipient Substances 0.000 description 1
- 239000012860 organic pigment Substances 0.000 description 1
- QUANRIQJNFHVEU-UHFFFAOYSA-N oxirane;propane-1,2,3-triol Chemical compound C1CO1.OCC(O)CO QUANRIQJNFHVEU-UHFFFAOYSA-N 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 239000000575 pesticide Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000106 platelet aggregation inhibitor Substances 0.000 description 1
- 229960000502 poloxamer Drugs 0.000 description 1
- 229920000233 poly(alkylene oxides) Polymers 0.000 description 1
- 229920001748 polybutylene Polymers 0.000 description 1
- 239000008389 polyethoxylated castor oil Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 230000000379 polymerizing effect Effects 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229920000909 polytetrahydrofuran Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 238000003672 processing method Methods 0.000 description 1
- 229940001470 psychoactive drug Drugs 0.000 description 1
- 239000004089 psychotropic agent Substances 0.000 description 1
- 229920005604 random copolymer Polymers 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 238000007873 sieving Methods 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- 229910052814 silicon oxide Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 230000003381 solubilizing effect Effects 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
- 239000002700 tablet coating Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- OPQYOFWUFGEMRZ-UHFFFAOYSA-N tert-butyl 2,2-dimethylpropaneperoxoate Chemical compound CC(C)(C)OOC(=O)C(C)(C)C OPQYOFWUFGEMRZ-UHFFFAOYSA-N 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 230000008646 thermal stress Effects 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- FOZHTJJTSSSURD-UHFFFAOYSA-J titanium(4+);dicarbonate Chemical compound [Ti+4].[O-]C([O-])=O.[O-]C([O-])=O FOZHTJJTSSSURD-UHFFFAOYSA-J 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 125000002889 tridecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- AAAQKTZKLRYKHR-UHFFFAOYSA-N triphenylmethane Chemical compound C1=CC=CC=C1C(C=1C=CC=CC=1)C1=CC=CC=C1 AAAQKTZKLRYKHR-UHFFFAOYSA-N 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
- C08F226/00—Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen
- C08F226/06—Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen by a heterocyclic ring containing nitrogen
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
- C08F283/00—Macromolecular compounds obtained by polymerising monomers on to polymers provided for in subclass C08G
- C08F283/06—Macromolecular compounds obtained by polymerising monomers on to polymers provided for in subclass C08G on to polyethers, polyoxymethylenes or polyacetals
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L1/00—Compositions of cellulose, modified cellulose or cellulose derivatives
- C08L1/02—Cellulose; Modified cellulose
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L5/00—Compositions of polysaccharides or of their derivatives not provided for in groups C08L1/00 or C08L3/00
-
- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
- C09D151/00—Coating compositions based on graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Coating compositions based on derivatives of such polymers
- C09D151/08—Coating compositions based on graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Coating compositions based on derivatives of such polymers grafted on to macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
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- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09D—COATING COMPOSITIONS, e.g. PAINTS, VARNISHES OR LACQUERS; FILLING PASTES; CHEMICAL PAINT OR INK REMOVERS; INKS; CORRECTING FLUIDS; WOODSTAINS; PASTES OR SOLIDS FOR COLOURING OR PRINTING; USE OF MATERIALS THEREFOR
- C09D171/00—Coating compositions based on polyethers obtained by reactions forming an ether link in the main chain; Coating compositions based on derivatives of such polymers
- C09D171/02—Polyalkylene oxides
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
- C08F218/00—Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an acyloxy radical of a saturated carboxylic acid, of carbonic acid or of a haloformic acid
- C08F218/02—Esters of monocarboxylic acids
- C08F218/04—Vinyl esters
- C08F218/08—Vinyl acetate
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
- C08L51/00—Compositions of graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Compositions of derivatives of such polymers
- C08L51/08—Compositions of graft polymers in which the grafted component is obtained by reactions only involving carbon-to-carbon unsaturated bonds; Compositions of derivatives of such polymers grafted on to macromolecular compounds obtained otherwise than by reactions only involving unsaturated carbon-to-carbon bonds
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- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Wood Science & Technology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Manufacturing And Processing Devices For Dough (AREA)
- Confectionery (AREA)
- Attitude Control For Articles On Conveyors (AREA)
Description
i) 30〜80重量%のN-ビニルラクタム、
ii) 10〜50重量%の酢酸ビニル、および
iii) 10〜50重量%のポリエーテル
(ただし、i)、ii)およびiii)の合計は100重量%である)
の混合物の、フリーラジカル開始重合により得られる。
i) 30〜70重量%のN-ビニルラクタム、
ii) 15〜35重量%の酢酸ビニル、および
iii) 10〜35重量%のポリエーテル
より得られる好ましいコポリマーを使用する。
i) 40〜60重量%のN-ビニルラクタム、
ii) 15〜35重量%の酢酸ビニル、および
iii) 10〜30重量%のポリエーテル
より得ることができる。
i) 50〜60重量%のN-ビニルラクタム、
ii) 25〜35重量%の酢酸ビニル、および
iii) 10〜20重量%のポリエーテル
より得ることができる。
攪拌した装置の中で、フィード2の一部を除く初期チャージをN2雰囲気下で77℃に加熱した。77℃の内部温度に到達した時に、フィード2の一部を加えて、15分間に渡って部分的に重合させた。次に、フィード1を5時間以内に計量添加し、フィード2を2時間以内に計量添加した。すべてのフィードを計量添加した後、反応混合物をさらに3時間重合させた。さらなる重合の後、溶液を50重量%の固体含有量に調節した。
104.0 g PEG 6000
1.0 gのフィード2
フィード1:240 gの酢酸ビニル
456 gのビニルカプロラクタム
240 gの酢酸エチル
フィード2:10.44 gのtert-ブチルペルピバレート(脂肪族混合物中75重量%)
67.90 gの酢酸エチル
次に、噴霧法により溶媒を除去して粉末状の製品を得た。K値は、1重量%のエタノール溶液において測定して、36であった。ガラス転移温度は70℃であった。
装置:9管の試料交換装置を有するD 8 Advance回折計(Bruker/AXS製)
測定方法:反射におけるθ-θジオメトリー
角度範囲2シータ:2〜80°
ステップ幅:0.02°
角度ステップあたりの測定時間:4.8秒
発散スリット:0.4 mmの挿入されたアパーチャを有するGoebel鏡
散乱防止スリット:Sollerスリット
検出器:Sol-X検出器
温度:室温
発電機の設定:40kV/50mA
DSC Q 2000(TA Instruments製)
パラメーター:
開始時の重さ:約8.5 mg
加熱速度:20K/分
使用した開始剤粒子は、コポリマーおよびカルバマゼピン(carbamazepine)の固溶体(組成60:40)を粉砕したもの(<500μm押出物)であった。
使用した開始剤粒子は、コポリマーおよびダナゾール(danazole)の固溶体(組成70:30)を粉砕したもの(<500μm押出物)であった。
Claims (11)
- 水に難溶性の活性成分の製剤であって、活性成分を含有するコーティングを施された担体粒子を含み、難溶性活性成分が両親媒性コポリマーを含むコーティング中に埋め込まれており、両親媒性コポリマーが、
i) 40〜60重量%のN-ビニルラクタム、
ii) 15〜35重量%の酢酸ビニル、および
iii) 10〜30重量%のポリエーテル
(ただし、i)、ii)およびiii)の合計は100重量%である)
より得られる前記製剤。 - コポリマーが、
i) 50〜60重量%のN-ビニルラクタム、
ii) 25〜35重量%の酢酸ビニル、および
iii) 10〜20重量%のポリエーテル
より得られる、請求項1に記載の製剤。 - 使用される担体粒子が、医薬品賦形剤を含むペレットである、請求項1または2に記載の製剤。
- 担体粒子が、スクロース、カラギーナン、デンプンまたは微結晶セルロースを含む、請求項1〜3のいずれか1項に記載の製剤。
- 担体粒子が、100〜2000μmの粒径を有する、請求項1〜4のいずれか1項に記載の製剤。
- 使用される担体粒子が、活性成分および両親媒性ポリマーを含む粒子である、請求項1または2に記載の製剤。
- コーティングがさらに医薬品賦形剤を含む、請求項1〜6のいずれか1項に記載の製剤。
- コーティングが、20〜99重量%の両親媒性ポリマーを含む、請求項1〜7のいずれか1項に記載の製剤。
- 1種以上の活性成分および両親媒性コポリマーを有機溶媒中に含む溶液を担体粒子を含む流動層上に噴霧することにより製剤を製造することを含む、請求項1〜8のいずれか1項に記載の製剤を製造する方法。
- 有機溶媒が、常圧で160℃よりも低い温度で蒸発可能である、請求項9に記載の方法。
- 使用される溶媒が、エタノール、メタノール、イソプロパノール、アセトン、酢酸エチル、ジクロロメタン、クロロホルム、ジメチルホルムアミド、メチルエチルケトンまたはそれらの混合物である、請求項9または10に記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09170553.3 | 2009-09-17 | ||
EP09170553 | 2009-09-17 | ||
PCT/EP2010/063393 WO2011032916A1 (de) | 2009-09-17 | 2010-09-13 | Mit wirkstoffhaltigen überzügen beschichtete pellets |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2013505212A JP2013505212A (ja) | 2013-02-14 |
JP5758899B2 true JP5758899B2 (ja) | 2015-08-05 |
Family
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EP (1) | EP2478019B1 (ja) |
JP (1) | JP5758899B2 (ja) |
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US9032390B2 (en) * | 2008-07-29 | 2015-05-12 | Qualcomm Incorporated | Framework versioning |
US8636929B2 (en) | 2010-05-21 | 2014-01-28 | Basf Se | Nanoporous foamed active compound-containing preparations based on pharmaceutically acceptable thermoplastically workable polymers |
GB201119985D0 (en) * | 2011-11-19 | 2012-01-04 | Diurnal Ltd | Treatment of adrenal insufficiency |
WO2024126560A1 (en) | 2022-12-14 | 2024-06-20 | BASF Agro B.V. | Liquid agricultural formulations of ppo-inhibitor herbicides |
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US5840881A (en) * | 1992-11-27 | 1998-11-24 | Takeda Chemical Industries, Ltd. | Composition containing a water-insoluble or slightly water-soluble compound with enhanced water-solubility |
JP3469926B2 (ja) * | 1993-11-04 | 2003-11-25 | 太田製薬株式会社 | 大腸内放出型医薬製剤用粒状物 |
US20030032879A1 (en) * | 1997-07-07 | 2003-02-13 | Steven Quay | Microbubble formation using ultrasound |
IE980115A1 (en) | 1998-02-16 | 2000-02-09 | Biovail Internat Ltd | Solubilizing delivery systems and method of manufacture |
US7374779B2 (en) * | 1999-02-26 | 2008-05-20 | Lipocine, Inc. | Pharmaceutical formulations and systems for improved absorption and multistage release of active agents |
DE19935063A1 (de) | 1999-07-28 | 2001-02-01 | Basf Ag | Pfropfpolymerisate als Gashydratinhibitoren |
US20040043070A1 (en) * | 2002-05-14 | 2004-03-04 | Ayres James W. | Hot melt coating by direct blending and coated substrates |
CN1897924B (zh) | 2003-09-26 | 2011-09-21 | 阿尔扎公司 | 能提供高载药量的药物包衣和提供它的方法 |
WO2006037344A1 (en) * | 2004-10-01 | 2006-04-13 | Lifecycle Pharma A/S | Pharmaceutical compositions comprising fenofibrate and atorvastatin |
CA2552241C (en) * | 2003-12-30 | 2013-10-01 | Durect Corporation | Co-polymeric devices for controlled release of active agents |
US20070292523A1 (en) * | 2004-09-27 | 2007-12-20 | Joey Moodley | Dihydropyrimidine Formulations |
DE102005053066A1 (de) * | 2005-11-04 | 2007-05-10 | Basf Ag | Verwendung von Copolymeren als Solubilisatoren für in Wasser schwerlöslichen Verbindungen |
ES2953390T3 (es) | 2006-08-31 | 2023-11-10 | Adare Pharmaceuticals Inc | Sistemas de administración de fármacos que comprenden disoluciones sólidas de fármacos débilmente básicos |
WO2009013202A1 (de) | 2007-07-26 | 2009-01-29 | Basf Se | Verfahren zur herstellung von durch pfropfpolymerisation in lösung erhaltenen copolymeren auf basis von polyethern in fester form |
US20110178183A1 (en) | 2008-09-25 | 2011-07-21 | Meyer-Boehm Kathrin | Use Of Polyether-Based And Vinyl Monomer-Based Copolymers As Binders For Dosing Forms Comprising Solid Active Ingredients |
EP2349218B1 (de) | 2008-10-07 | 2013-09-18 | Basf Se | Verfahren zur herstellung oraler darreichungsformen mit kontrollierter freisetzung |
CN102264462A (zh) | 2008-12-23 | 2011-11-30 | 巴斯夫欧洲公司 | 基于聚醚和乙烯基单体的共聚物作为乳状液的稳定剂的用途 |
BRPI1012651A2 (pt) | 2009-03-31 | 2016-04-05 | Basf Se | processo para produzir preparações de substâncias fracamente solúveis em água |
EP2429492B1 (de) | 2009-05-13 | 2014-06-25 | Basf Se | Feste pharmazeutische Zubereitungen enthaltend Copolymere auf Basis von Polyethern in Kombination mit wasserschwerlöslichen Polymeren |
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CN102549029B (zh) | 2015-03-04 |
CN102549029A (zh) | 2012-07-04 |
BR112012006067A2 (pt) | 2016-03-29 |
EP2478019B1 (de) | 2015-04-01 |
US20120183623A1 (en) | 2012-07-19 |
EP2478019A1 (de) | 2012-07-25 |
WO2011032916A1 (de) | 2011-03-24 |
US8951569B2 (en) | 2015-02-10 |
BR112012006067B1 (pt) | 2019-10-01 |
JP2013505212A (ja) | 2013-02-14 |
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