JP2010509288A - 溶融処理イマチニブ剤形 - Google Patents
溶融処理イマチニブ剤形 Download PDFInfo
- Publication number
- JP2010509288A JP2010509288A JP2009535736A JP2009535736A JP2010509288A JP 2010509288 A JP2010509288 A JP 2010509288A JP 2009535736 A JP2009535736 A JP 2009535736A JP 2009535736 A JP2009535736 A JP 2009535736A JP 2010509288 A JP2010509288 A JP 2010509288A
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- Prior art keywords
- dosage form
- imatinib
- form according
- polymeric binder
- fatty acid
- Prior art date
- Legal status (The legal status 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 status listed.)
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Abstract
【解決手段】本発明は、(a)イマチニブまたはその塩の薬学的有効量、(b)少なくとも1種の高分子性結合剤、および(c)少なくとも1種の薬学的に許容できる非イオン性界面活性剤の溶融処理混合物を含む剤形を提供する。
【選択図】なし
Description
(a)イマチニブまたはその塩の薬学的有効量、および
(b)少なくとも1種の高分子性結合剤、および
(c)少なくとも1種の薬学的に許容できる非イオン性界面活性剤、
の溶融処理混合物を含む剤形を提供することである。
(a)イマチニブまたはその塩、少なくとも1種の高分子性結合剤、および少なくとも1種の薬学的に許容できる非イオン性界面活性剤、および任意の成分類を混合加熱し、粘着性の成形可能な塊を得ること、および
(b)前記塊をダイに通すこと。
図1〜5は、異なるpH値における本発明の剤形の薬物放出を示している。
下記の表1に示した成分類を、高せん断ミキサーを用いて配合した。液体賦形剤類は、固体原料とともに顆粒化した。次に、粉末混合物を二軸押出機(Rheomex PTW16、Thermo Electron、Karlsruhe、Germany)に速度0.8kg/hかつ処理温度130℃で供給した。押出し物は次に、相互に合致する空洞を表面に有する2個の逆回転ローラーを備えたカレンダーに供給した。約1200mg(イマチニブ遊離塩基800mgに対応)の長さ18.8mmで直径が9.55mmの楕円錠剤類が得られた。
Claims (12)
- (a)イマチニブまたはその塩の薬学的有効量、
(b)少なくとも1種の高分子性結合剤、および
(c)少なくとも1種の薬学的に許容できる非イオン性界面活性剤、
の溶融処理混合物を含む剤形。 - イマチニブまたはその塩は、前記溶融処理混合物の総重量に対して少なくとも50重量%の量で存在する請求項1記載の剤形。
- 直接形状化される請求項1または2記載の剤形。
- 直接形状化が、カレンダリング、射出成形または熱形成によって行われる請求項3記載の剤形。
- 前記剤形からの薬物放出が、本質的にpHに依存しない請求項1〜4のいずれか一項に記載の剤形。
- 8時間における薬物放出が、pH1.0における放出値に対するpH6.8における放出値の比が少なくとも0.6である請求項1〜5のいずれか一項に記載の剤形。
- 前記非イオン性界面活性剤が、ポリオール脂肪酸エステル、ポリアルコキシル化ポリオール脂肪酸エステル、ポリアルコキシル化脂肪アルコールエーテルまたはその混合物である請求項1〜6のいずれか一項に記載の剤形。
- 前記可溶化剤が、プロピレングリコール脂肪酸モノまたはジエステルあるいはその混合物である請求項7記載の剤形。
- 前記非イオン性界面活性剤が、HLB4以下を有する請求項1〜8のいずれか一項に記載の剤形。
- 前記高分子性結合剤が、セルロース誘導体類、および、ビニルピロリドンのホモ−またはコポリマー類、およびその混合物類、から構成される群から選択される請求項1〜9のいずれか一項に記載の剤形。
- (a)イマチニブまたはその塩、少なくとも1種の高分子性結合剤、および少なくとも1種の薬学的に許容できる非イオン性界面活性剤、および任意の成分類を混合並びに加熱し、粘着性の成形可能な塊を得ること;および
(b)前記塊をダイに通すこと、
を含む請求項1記載の剤形を調製する方法。 - 前記粘着性の成形可能な塊を、前記剤形の所望の形状に直接至らしめることを含む請求項11記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06023367A EP1920767A1 (en) | 2006-11-09 | 2006-11-09 | Melt-processed imatinib dosage form |
EP06023367.3 | 2006-11-09 | ||
PCT/EP2007/062100 WO2008055965A1 (en) | 2006-11-09 | 2007-11-08 | Melt-processed imatinib dosage form |
Publications (2)
Publication Number | Publication Date |
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JP2010509288A true JP2010509288A (ja) | 2010-03-25 |
JP5280369B2 JP5280369B2 (ja) | 2013-09-04 |
Family
ID=38291110
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009535736A Expired - Fee Related JP5280369B2 (ja) | 2006-11-09 | 2007-11-08 | 溶融処理イマチニブ剤形 |
Country Status (13)
Country | Link |
---|---|
US (1) | US8841303B2 (ja) |
EP (2) | EP1920767A1 (ja) |
JP (1) | JP5280369B2 (ja) |
CN (3) | CN101594851B (ja) |
AU (1) | AU2007316557B2 (ja) |
BR (2) | BRPI0718523B8 (ja) |
CA (1) | CA2668775C (ja) |
ES (1) | ES2565036T3 (ja) |
MX (1) | MX2009004858A (ja) |
PL (1) | PL2086516T3 (ja) |
RU (1) | RU2468788C2 (ja) |
WO (1) | WO2008055965A1 (ja) |
ZA (1) | ZA200903929B (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2013245202A (ja) * | 2012-05-28 | 2013-12-09 | Nipro Corp | 医薬組成物 |
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EP1920767A1 (en) | 2006-11-09 | 2008-05-14 | Abbott GmbH & Co. KG | Melt-processed imatinib dosage form |
WO2009100176A2 (en) * | 2008-02-07 | 2009-08-13 | Abbott Laboratories | Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor |
GB2488788B (en) * | 2011-03-07 | 2013-07-10 | Natco Pharma Ltd | Oral formulation of phenylaminopyrymidine compound with enhanced bioavailability and pharmacological response |
CN102836159B (zh) * | 2011-06-24 | 2014-12-10 | 南京圣和药业股份有限公司 | 达沙替尼分散体及其制备方法和其在片剂中的应用 |
US9216172B2 (en) | 2011-08-04 | 2015-12-22 | National Cancer Center | Method for determining effectiveness of cancer treatment by assessing the presence of a KIF5B-RET chimeric gene |
MX2014006201A (es) | 2011-11-24 | 2014-12-05 | Imuneks Farma Ilaç Sanayi Ve Ticaret A S | Formas de dosificaciones solidas de imatinib reconstituidas justo antes de usarse. |
CA2860932C (en) | 2012-01-13 | 2021-02-16 | Magnus Brisander | A pharmaceutical composition comprising stable, amorphous hybrid nanoparticles of at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component |
CN103301067B (zh) * | 2012-03-15 | 2018-09-11 | 苏州泽璟生物制药有限公司 | 一种改善吸收性能的固体分散体及其制备 |
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CN101594852A (zh) | 2009-12-02 |
US8841303B2 (en) | 2014-09-23 |
RU2468788C2 (ru) | 2012-12-10 |
CN101594851A (zh) | 2009-12-02 |
RU2009121653A (ru) | 2010-12-20 |
AU2007316557B2 (en) | 2013-10-31 |
WO2008055965A1 (en) | 2008-05-15 |
PL2086516T3 (pl) | 2016-08-31 |
AU2007316557A1 (en) | 2008-05-15 |
CN101594852B (zh) | 2013-04-03 |
BRPI0718523B8 (pt) | 2022-09-13 |
BRPI0718523B1 (pt) | 2022-03-03 |
EP1920767A1 (en) | 2008-05-14 |
CN102512680A (zh) | 2012-06-27 |
BRPI0718521A2 (pt) | 2013-11-19 |
US20100240672A1 (en) | 2010-09-23 |
EP2086516A1 (en) | 2009-08-12 |
ES2565036T3 (es) | 2016-03-30 |
CN101594851B (zh) | 2013-01-02 |
JP5280369B2 (ja) | 2013-09-04 |
BRPI0718523A2 (pt) | 2013-11-19 |
MX2009004858A (es) | 2009-05-21 |
EP2086516B1 (en) | 2016-01-06 |
ZA200903929B (en) | 2010-03-31 |
CA2668775A1 (en) | 2008-05-15 |
CA2668775C (en) | 2014-08-12 |
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