JPH07501533A - エバスタイムまたはその類似体に基づく医薬組成物 - Google Patents
エバスタイムまたはその類似体に基づく医薬組成物Info
- Publication number
- JPH07501533A JPH07501533A JP5509889A JP50988993A JPH07501533A JP H07501533 A JPH07501533 A JP H07501533A JP 5509889 A JP5509889 A JP 5509889A JP 50988993 A JP50988993 A JP 50988993A JP H07501533 A JPH07501533 A JP H07501533A
- Authority
- JP
- Japan
- Prior art keywords
- carbon atoms
- formula
- group
- active ingredient
- group containing
- 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.)
- Granted
Links
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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- A61P9/08—Vasodilators for multiple indications
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Description
Claims (8)
- 1.式 ▲数式、化学式、表等があります▼式(II)式中、 −R1はチエニル基、場合によりハロゲンで置換されていてもよいフェニル基、 1〜6個の炭素原子を含有するアルコキシ基、または1〜6個の炭素原子を含有 するアルキル基を表し、−R2はハロゲン原子、水素原子、1〜6個の炭素原子 を含有するアルコキシ基、または1〜6個の炭素原子を含有するアルキル基を表 し、 −R3はハロゲン原子、水素原子、1〜6個の炭素原子を含有するアルコキシ基 、1〜6個の炭素原子を含有するアルキル基、1〜6個の炭素原子を含有するア ルキルチオ基、5または6個の炭素原子を含有するシクロアルキル基、または式 : ▲数式、化学式、表等があります▼ の基、式中R4およびR5は互いに独立して水素原子または1から6個の炭素原 子を含有するアルキル基を表し、R6は3〜6個の炭素原子を含有するシクロア ルキル基、またはヒドロキシメチルもしくはカルボキシル基、または2〜7個の 炭素原子を含有するアルコキシカルボニル基を表し、 −Wはカルボニルもしくはヒドロキシメチレン基、およびそれらの塩を表す に対応する化合物限含有し;式(II)の化合物は微細粉粒化されていることを 特徴とする、改良された溶解特性を持つ固体医薬組成物。
- 2.有効成分が、 −R1はフェニル基を表し、 −R2は水素を表し、 −R3はtert−ブチル基を表し、 −Wはカルボニル基を表す 式(II)に対応することを特徴とする請求の範囲第1項記載の組成物。
- 3.式(II)の有効成分が親水性化されていることを特徴とする、請求の範囲 第1項および第2項記載の組成物。
- 4.式(II)の有効成分が以下の特徴;−200μmより小さい最大サイズ −0.5から15μmの間の数平均粒子サイズ−25μmより小さい、および好 ましくは20μmよりも小さい粒子サイズを有する好ましくは数基準で90%の 粒子を有することを特徴とする請求の範囲第1項記載の組成物。
- 5.請求の範囲第4項目に記載された有効成分を含むことを特徴とする圧縮剤形 の組成物
- 6.−第一工程で式(II)の化合物の微細粉粒化を行い、−第二工程で直接圧 縮を行う ことを特徴とする請求の範囲第5項記載の組成物の製造法。
- 7.−第一工程で式(II)の化合物の微細粉粒化を行い、−第二工程で湿式造 粒、続いて圧縮を行うことを特徴とする請求の範囲第5項記載の組成物の製造法 。
- 8.請求の範囲第4項記載の有効成分、ガム類から選択される沈殿防止剤、甘味 剤および希釈剤を含有することを特徴とする経口凍結乾燥剤形である組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR9114936A FR2684298B1 (fr) | 1991-12-03 | 1991-12-03 | Nouvelles compositions pharmaceutiques solides a base de derives de lapiperidine substitues en 1,4. |
FR91/14936 | 1991-12-03 | ||
PCT/FR1992/001116 WO1993010782A1 (fr) | 1991-12-03 | 1992-12-01 | Compositions pharmaceutiques a base d'ebastime ou de ses analoques |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH07501533A true JPH07501533A (ja) | 1995-02-16 |
JP3518601B2 JP3518601B2 (ja) | 2004-04-12 |
Family
ID=9419600
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50988993A Expired - Lifetime JP3518601B2 (ja) | 1991-12-03 | 1992-12-01 | エバスタイムまたはその類似体に基づく医薬組成物 |
Country Status (12)
Country | Link |
---|---|
US (1) | US5460829A (ja) |
EP (1) | EP0614362B1 (ja) |
JP (1) | JP3518601B2 (ja) |
AT (1) | ATE148990T1 (ja) |
CA (1) | CA2123232C (ja) |
DE (1) | DE69217554T2 (ja) |
DK (1) | DK0614362T5 (ja) |
ES (1) | ES2097490T3 (ja) |
FR (1) | FR2684298B1 (ja) |
GR (1) | GR3022615T3 (ja) |
HK (1) | HK1006273A1 (ja) |
WO (1) | WO1993010782A1 (ja) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPWO2003103713A1 (ja) * | 2002-06-10 | 2005-10-06 | 大日本製薬株式会社 | 速崩壊性錠剤及びその製造方法 |
JP2007246539A (ja) * | 1997-10-20 | 2007-09-27 | Dainippon Sumitomo Pharma Co Ltd | 速溶性医薬組成物 |
JP2008543766A (ja) * | 2005-06-09 | 2008-12-04 | エラン ファーマ インターナショナル リミテッド | ナノ粒子エバスチン製剤 |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5717025A (en) * | 1996-09-16 | 1998-02-10 | H. B. Fuller Licensing & Financing, Inc. | Melamine-formaldehyde resin based adhesive compositions |
WO2002100339A2 (en) | 2001-06-13 | 2002-12-19 | Biogal Gyogyszergyar Rt. | Novel process for preparing rac-bicalutamide and its intermediates |
CA2478897A1 (en) * | 2002-03-12 | 2003-09-18 | Y's Therapeutics Co., Limited | Compounds capable of inhibiting immunocyte-related allergic immune reactions |
US20050008691A1 (en) * | 2003-05-14 | 2005-01-13 | Arturo Siles Ortega | Bicalutamide compositions |
ES2231043B2 (es) * | 2004-10-29 | 2005-10-01 | Laboratorios Cinfa, S.A. | Composicion farmaceutica de ebastina de liberacion inmediata y su proceso de fabricacion. |
DE602005000992D1 (de) * | 2005-04-25 | 2007-06-06 | Alter Lab | Feste Arzneizubereitung enthaltend ein kristallines in 1,4-Stellungen substituiertes Piperidinderivat |
ES2277767B1 (es) * | 2005-11-04 | 2008-04-01 | Simbec Iberica, S.L. | Formas orales solidas de ebastina. |
JP2007297348A (ja) * | 2006-05-02 | 2007-11-15 | Daito Kk | エバスチンを含有する錠剤 |
US8617597B2 (en) | 2006-07-06 | 2013-12-31 | Bayer Intellectual Property Gmbh | Pharmaceutical composition containing a tetrahydrofolic acid |
DE102008000351B4 (de) | 2008-02-20 | 2017-08-10 | Aristo Pharma Gmbh | Verfahren zur Herstellung eines Ebastin enthaltenden Granulats sowie einer festen pharmazeutischen Zusammensetzung, Ebastin enthaltendes Granulat und dessen Verwendung |
DE202011000756U1 (de) | 2011-03-31 | 2011-10-12 | Micro Labs Limited | Ebastine, nicht-mikronisierte Ebastinepartikel und pharmazeutische Zusammensetzungen umfassend Ebastine |
WO2013081562A1 (en) | 2011-10-13 | 2013-06-06 | Mahmut Bilgic | Oral formulations comprising ebastine |
WO2013062498A1 (en) * | 2011-10-13 | 2013-05-02 | Mahmut Bilgic | Solid oral formulations comprising ebastine |
EP2589376B1 (en) | 2011-11-01 | 2016-09-21 | Inopharm Limited | Oral disintegrating composition of anti-histamine agents |
US10058542B1 (en) | 2014-09-12 | 2018-08-28 | Thioredoxin Systems Ab | Composition comprising selenazol or thiazolone derivatives and silver and method of treatment therewith |
CN105326802A (zh) * | 2015-09-01 | 2016-02-17 | 杭州澳医保灵药业有限公司 | 一种依巴斯汀分散片及其制备方法 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8321157D0 (en) * | 1983-08-05 | 1983-09-07 | Fordonal Sa | Piperidine derivatives |
US4783465A (en) * | 1984-04-09 | 1988-11-08 | Analgesic Associates | Cough/cold mixtures comprising non-sedating antihistamine drugs |
US4871733A (en) * | 1984-04-09 | 1989-10-03 | Analgesic Associates | Cough/cold mixtures comprising non-sedating antihistamine drugs |
US4975426A (en) * | 1987-06-08 | 1990-12-04 | Analgesic Associates | Cough/cold mixtures comprising non-sedating antihistamine drugs |
US4829064A (en) * | 1987-06-08 | 1989-05-09 | Analgesic Associates | Cough/cold mixtures comprising non-sedating antihistamine drugs |
DE3720493A1 (de) * | 1987-06-20 | 1989-01-26 | Nattermann A & Cie | Arzneizubereitungen mit mikronisierten ebselen-kristallen |
EP0402422A1 (en) * | 1988-04-27 | 1990-12-19 | Schering Corporation | Certain paf antagonist antihistamine combinations and methods |
JP2642486B2 (ja) * | 1989-08-04 | 1997-08-20 | 田辺製薬株式会社 | 難溶性薬物の超微粒子化法 |
US5356887A (en) * | 1990-01-31 | 1994-10-18 | Merck & Co., Inc. | Pharmaceutical compositions containing insoluble calcium salts of amino-hydroxybutylidene bisphoshonic acids |
US5271944A (en) * | 1991-04-05 | 1993-12-21 | Biofor, Ltd. | Pharmacologically enhanced formulations |
-
1991
- 1991-12-03 FR FR9114936A patent/FR2684298B1/fr not_active Expired - Fee Related
-
1992
- 1992-12-01 CA CA002123232A patent/CA2123232C/fr not_active Expired - Lifetime
- 1992-12-01 DE DE69217554T patent/DE69217554T2/de not_active Expired - Lifetime
- 1992-12-01 US US08/244,204 patent/US5460829A/en not_active Expired - Lifetime
- 1992-12-01 AT AT93901804T patent/ATE148990T1/de active
- 1992-12-01 EP EP93901804A patent/EP0614362B1/fr not_active Expired - Lifetime
- 1992-12-01 DK DK93901804T patent/DK0614362T5/da active
- 1992-12-01 ES ES93901804T patent/ES2097490T3/es not_active Expired - Lifetime
- 1992-12-01 WO PCT/FR1992/001116 patent/WO1993010782A1/fr active IP Right Grant
- 1992-12-01 JP JP50988993A patent/JP3518601B2/ja not_active Expired - Lifetime
-
1997
- 1997-02-20 GR GR960402655T patent/GR3022615T3/el unknown
-
1998
- 1998-06-13 HK HK98105265A patent/HK1006273A1/xx not_active IP Right Cessation
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2007246539A (ja) * | 1997-10-20 | 2007-09-27 | Dainippon Sumitomo Pharma Co Ltd | 速溶性医薬組成物 |
JPWO2003103713A1 (ja) * | 2002-06-10 | 2005-10-06 | 大日本製薬株式会社 | 速崩壊性錠剤及びその製造方法 |
JP2008543766A (ja) * | 2005-06-09 | 2008-12-04 | エラン ファーマ インターナショナル リミテッド | ナノ粒子エバスチン製剤 |
Also Published As
Publication number | Publication date |
---|---|
WO1993010782A1 (fr) | 1993-06-10 |
DE69217554D1 (de) | 1997-03-27 |
FR2684298B1 (fr) | 1994-03-11 |
FR2684298A1 (fr) | 1993-06-04 |
JP3518601B2 (ja) | 2004-04-12 |
US5460829A (en) | 1995-10-24 |
DK0614362T5 (da) | 2008-11-10 |
EP0614362A1 (fr) | 1994-09-14 |
GR3022615T3 (en) | 1997-05-31 |
EP0614362B1 (fr) | 1997-02-19 |
CA2123232A1 (fr) | 1993-06-10 |
HK1006273A1 (en) | 1999-02-19 |
CA2123232C (fr) | 2005-02-15 |
ATE148990T1 (de) | 1997-03-15 |
ES2097490T3 (es) | 1997-04-01 |
DK0614362T3 (da) | 1997-03-10 |
DE69217554T2 (de) | 1997-08-07 |
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