JP2015501808A - 医薬製剤 - Google Patents
医薬製剤 Download PDFInfo
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- JP2015501808A JP2015501808A JP2014543550A JP2014543550A JP2015501808A JP 2015501808 A JP2015501808 A JP 2015501808A JP 2014543550 A JP2014543550 A JP 2014543550A JP 2014543550 A JP2014543550 A JP 2014543550A JP 2015501808 A JP2015501808 A JP 2015501808A
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
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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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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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
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
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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
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Nutrition Science (AREA)
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- Inorganic Chemistry (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
(a)化合物Aを含む固体分散体である内部相と、
(b)付加的な添加剤を含む外部相と
を含む、固体経口医薬製剤である。
(a)化合物A、親水性結合剤、および界面活性剤を含む固体分散体である内部相と、
(b)付加的な添加剤を含む外部相と
を含む、固体経口医薬製剤に関する。
(a)化合物A、親水性結合剤、界面活性剤を含む固体分散体である内部相と、
(b)酸性化剤、賦形剤、崩壊剤、流動促進剤、および滑沢剤の1種以上を含む外部相と
を含む、固体経口医薬製剤である。
以下の組成物を、一定の薬物添加率15%で調製し、10mg、25mg、50mg、および100mgのカプセル剤に製剤化する。
加工は、18mm二軸Leistriez押出機を用いた熱溶融押出の後、押出物を粉砕し、外部相と混和し、篩過することによって行う。混和の後、混和物を、サイズ0および00のピンク色の硬ゼラチンカプセルに、それぞれ50mgおよび100mgの薬物用量で封入する。段階的手法を以下に示す:
所要量の化合物A、Kollidon VA64、およびPoloxamer188を秤量する
混合物を混和する
混和物を、18mm Leistreiz二軸押出機にて、1kg/時の供給速度で、押出機内の温度を50〜160℃に維持して押し出す
押出物を粉砕する
篩過したコハク酸および微結晶性セルロースを加える
粉砕した押出物、コハク酸および微結晶性セルロースを加え、混和する
クロスポビドンおよびアエロジルを加える
混合物を混和する
予め篩過した(prescreen)ステアリン酸マグネシウムを加える
混合物を混和する
H&Kカプセル封入器を用いてカプセル化する
以下の製剤を、実施例1に記載したのと同様の様式で調製する。
以下の表は、50mg/kgで投与したマイクロエマルションとして製剤化された化合物A、ならびに化合物Aの用量200mgの実施例1(固体分散体1)および実施例2(固体分散体2)の製剤についての、サルにおける薬物動態試験の結果を記載したものである。
以下の製剤を、実施例1に記載したのと同様の技法により、ただし単相で調製する。製剤の溶解プロファイルは、図2に報告される。
以下の製剤を、実施例1に記載したのと同様の技法により、ただし錠剤剤形に調製する。製剤の0.1N HCl媒質中の溶解プロファイルは、図3に報告される。
Claims (10)
- 化合物Aを含む固体分散体を含む、固体経口医薬製剤。
- 前記化合物Aを含む固体分散体である内部相と、
付加的な添加剤を含む外部相と
を含む、請求項1に記載の固体経口医薬製剤。 - 前記内部相または前記外部相が酸性化剤を含む、請求項2に記載の固体経口医薬製剤。
- 本発明はさらに、
前記化合物A、親水性結合剤、および界面活性剤を含む固体分散体である内部相と、
付加的な添加剤を含む外部相と
を含む、請求項2に記載の固体経口医薬製剤に関する。 - 前記化合物A、親水性結合剤、界面活性剤を含む固体分散体である内部相と、
酸性化剤、賦形剤、崩壊剤、流動促進剤、および滑沢剤の1種以上を含む外部相と
を含む、請求項1に記載の固体経口医薬製剤。 - 増殖性疾患の治療のための医薬を調製するための、請求項1に記載の固体経口医薬製剤の使用。
- 治療を必要とする患者に治療有効量の請求項1に記載の製剤を投与することを含む、増殖性疾患を治療する方法。
- B−RAFの阻害に応答する疾患を治療するための、請求項1に記載の固体経口製剤の使用。
- 前記疾患がB−RAFの変異によって特徴づけられる、請求項8に記載の使用。
- 前記疾患が黒色腫または結腸直腸がんである、請求項9に記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161563229P | 2011-11-23 | 2011-11-23 | |
US61/563,229 | 2011-11-23 | ||
PCT/US2012/066185 WO2013078264A1 (en) | 2011-11-23 | 2012-11-21 | Pharmaceutical formulations |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2017182214A Division JP2018035171A (ja) | 2011-11-23 | 2017-09-22 | 医薬製剤 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015501808A true JP2015501808A (ja) | 2015-01-19 |
JP2015501808A5 JP2015501808A5 (ja) | 2016-01-14 |
JP6216325B2 JP6216325B2 (ja) | 2017-10-18 |
Family
ID=47501412
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Application Number | Title | Priority Date | Filing Date |
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JP2014543550A Active JP6216325B2 (ja) | 2011-11-23 | 2012-11-21 | 医薬製剤 |
JP2017182214A Pending JP2018035171A (ja) | 2011-11-23 | 2017-09-22 | 医薬製剤 |
Family Applications After (1)
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JP2017182214A Pending JP2018035171A (ja) | 2011-11-23 | 2017-09-22 | 医薬製剤 |
Country Status (38)
Country | Link |
---|---|
US (4) | US9387208B2 (ja) |
EP (2) | EP2782557B1 (ja) |
JP (2) | JP6216325B2 (ja) |
KR (1) | KR102091295B1 (ja) |
CN (2) | CN105708819B (ja) |
AR (1) | AR088936A1 (ja) |
AU (1) | AU2012340759C1 (ja) |
BR (1) | BR112014011981B8 (ja) |
CA (1) | CA2856406C (ja) |
CL (1) | CL2014001337A1 (ja) |
CO (1) | CO6940426A2 (ja) |
CY (1) | CY1121421T1 (ja) |
DK (1) | DK2782557T3 (ja) |
EA (1) | EA025389B1 (ja) |
EC (1) | ECSP23034537A (ja) |
ES (1) | ES2695099T3 (ja) |
GT (1) | GT201400100A (ja) |
HK (1) | HK1197024A1 (ja) |
HR (1) | HRP20181896T1 (ja) |
HU (1) | HUE040370T2 (ja) |
IL (1) | IL232305B (ja) |
JO (1) | JO3493B1 (ja) |
LT (1) | LT2782557T (ja) |
MA (1) | MA35716B1 (ja) |
MX (1) | MX353446B (ja) |
MY (1) | MY172729A (ja) |
PE (1) | PE20141994A1 (ja) |
PH (1) | PH12014501157B1 (ja) |
PL (1) | PL2782557T3 (ja) |
PT (1) | PT2782557T (ja) |
RS (1) | RS58048B1 (ja) |
SG (1) | SG11201401260QA (ja) |
SI (1) | SI2782557T1 (ja) |
TN (1) | TN2014000145A1 (ja) |
TW (1) | TWI649098B (ja) |
UA (1) | UA115039C2 (ja) |
WO (1) | WO2013078264A1 (ja) |
ZA (1) | ZA201402418B (ja) |
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JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
EP2776037B1 (en) | 2011-11-11 | 2019-01-09 | Novartis AG | Method of treating a proliferative disease |
JP6216325B2 (ja) | 2011-11-23 | 2017-10-18 | ノバルティス アーゲー | 医薬製剤 |
KR102369405B1 (ko) | 2015-06-04 | 2022-03-02 | 화이자 인코포레이티드 | 팔보시클립의 고체 투여 형태 |
RU2615986C1 (ru) * | 2016-02-25 | 2017-04-12 | Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") | Замещенные метил (2-{ 4-[3-(3-метансульфониламино-2-фтор-5-хлор-фенил)-1Н-пиразол-4-ил]пиримидин-2-иламино} -этил)карбаматы, способ их получения и применения |
US10449195B2 (en) | 2016-03-29 | 2019-10-22 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
HUE060653T2 (hu) | 2016-06-03 | 2023-04-28 | Array Biopharma Inc | Gyógyászati kombinációk |
CN106000220A (zh) * | 2016-06-30 | 2016-10-12 | 东华大学 | 一种含化学试剂的有机溶剂崩解片的制备方法与应用 |
CN114306245A (zh) | 2020-09-29 | 2022-04-12 | 深圳市药欣生物科技有限公司 | 无定形固体分散体的药物组合物及其制备方法 |
AU2021358394A1 (en) | 2020-10-05 | 2023-04-13 | Pierre Fabre Medicament | Combination of encorafenib and binimetinib as adjuvant treatment for resected stage II melanoma |
CN114557977A (zh) * | 2022-02-16 | 2022-05-31 | 北京康立生医药技术开发有限公司 | 一种治疗肠癌的药物的制备方法、制剂及纯度分析方法 |
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