KR20080090661A - 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 - Google Patents
결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 Download PDFInfo
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- KR20080090661A KR20080090661A KR1020070033756A KR20070033756A KR20080090661A KR 20080090661 A KR20080090661 A KR 20080090661A KR 1020070033756 A KR1020070033756 A KR 1020070033756A KR 20070033756 A KR20070033756 A KR 20070033756A KR 20080090661 A KR20080090661 A KR 20080090661A
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- KR
- South Korea
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- bepotastine
- metal salt
- salt hydrate
- calcium
- salt
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
-
- 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
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
Claims (14)
- 제1항에 있어서,M이 칼슘인 것을 특징으로 하는, 결정형의 베포타스틴 금속염 수화물.
- 제2항에 있어서,X-선 분말 회절분광도에서 15% 이상의 상대 강도 (I/Io : I는 각 피크의 강도; Io는 가장 큰 피크의 강도)를 갖는 피크가 2.3, 14.2, 14.7, 15.1, 16.5, 17.0, 18.7, 19.1, 20.6, 22.8, 23.8, 24.2, 25.5, 28.6 및 31.8의 회절각(2θ±0.2)에서 나타나는 것을 특징으로 하는, 결정형의 베포타스틴 금속염 수화물.
- 제1항에 있어서,M이 스트론튬인 것을 특징으로 하는, 결정형의 베포타스틴 금속염 수화물.
- 제4항에 있어서,X-선 분말 회절분광도에서 15% 이상의 상대 강도 (I/Io)를 갖는 피크가 4.8, 6.2, 7.3, 8.4, 9.5, 10.6, 12.2, 12.5, 13.3, 14.1, 14.3, 14.6, 16.5, 16.9, 18.7, 19.1, 20.2, 21.3, 22.2, 23.0, 23.9, 25.5, 28.4, 29.7 및 31.8의 회절각(2θ±0.2)에서 나타나는 것을 특징으로 하는, 결정형의 베포타스틴 금속염 수화물.
- 물, 또는 물과 메탄올, 에탄올, 2-프로판올, 아세토니트릴 및 아세톤으로 구성된 군에서 선택된 1종 이상의 유기용매의 혼합용매 중에서,a) 베포타스틴을 수산화칼슘 또는 수산화스트론튬과 반응시키거나,b) 베포타스틴을 수산화나트륨, 수산화칼륨, 암모니아 및 유기 아민으로부터 선택된 염기와 접촉시켜 베포타스틴의 나트륨염, 칼륨염, 암모늄염 또는 유기 아민염을 제조한 다음, 이를 칼슘 또는 스트론튬의 반응성염과 반응시킨 후, 침전된 결정을 회수하는 것을 포함하는, 제1항에 따른 화학식 1의 결정형의 베포타스틴 금속염 수화물을 제조하는 방법.
- 제6항에 있어서,상기 a)에서 수산화칼슘 또는 수산화스트론튬이 베포타스틴 1몰 당량에 대하여 0.5 내지 0.75몰 당량으로 사용되는 것을 특징으로 하는 방법.
- 제6항에 있어서,상기 b)에서 염기가 베포타스틴 1몰 당량에 대하여 1.0 내지 1.4몰 당량으로 사용되는 것을 특징으로 하는 방법.
- 제6항에 있어서,상기 b)에서 칼슘 또는 스트론튬의 반응성염이 염기 1몰 당량에 대하여 0.5 내지 0.75몰 당량으로 사용되는 것을 특징으로 하는 방법.
- 유효성분으로 제1항에 따른 결정형의 베포타스틴 금속염 수화물 및 약학적으로 허용가능한 담체를 포함하는, 항히스타민 또는 항알러지용 약학 조성물.
- 제10항에 있어서,상기 약학 조성물이 알러지성 비염, 두드러기, 소양증, 비강 장애, 피부염 또는 습진의 예방 또는 치료용인 것을 특징으로 하는 조성물.
- 제10항에 있어서,경구투여 제제로 제형화된 것임을 특징으로 하는 조성물.
- 제12항에 있어서,상기 경구투여 제제가 결정형의 베포타스틴 금속염 수화물을 0.1 내지 95 중량%의 양으로 포함하는 것을 특징으로 하는 조성물.
- 제13항에 있어서,상기 경구투여 제제가 결정형의 베포타스틴 금속염 수화물을 1 내지 70 중량%의 양으로 포함하는 것을 특징으로 하는 조성물.
Priority Applications (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020070033756A KR100878698B1 (ko) | 2007-04-05 | 2007-04-05 | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 |
TW097112166A TW200900392A (en) | 2007-04-05 | 2008-04-03 | Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same |
EP08741162A EP2144896A4 (en) | 2007-04-05 | 2008-04-04 | CRYSTALLINE BEPOTASTIN METAL SALT HYDRATE, PROCESS FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAID HYDRATE |
CA002682822A CA2682822A1 (en) | 2007-04-05 | 2008-04-04 | Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same |
PCT/KR2008/001912 WO2008123701A1 (en) | 2007-04-05 | 2008-04-04 | Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same |
CN200880010709A CN101652358A (zh) | 2007-04-05 | 2008-04-04 | 新型晶体贝他斯汀金属盐水合物、它的制备方法和包含它的药物组合物 |
JP2010500837A JP2010522747A (ja) | 2007-04-05 | 2008-04-04 | 新規な結晶型ベポタスチン金属塩水和物、その製造方法及びこれを含む医薬組成物 |
AU2008235668A AU2008235668A1 (en) | 2007-04-05 | 2008-04-04 | Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same |
US12/531,003 US20100137367A1 (en) | 2007-04-05 | 2008-04-04 | Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020070033756A KR100878698B1 (ko) | 2007-04-05 | 2007-04-05 | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020080121442A Division KR101307712B1 (ko) | 2008-12-02 | 2008-12-02 | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및 이를 포함하는 약학 조성물 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20080090661A true KR20080090661A (ko) | 2008-10-09 |
KR100878698B1 KR100878698B1 (ko) | 2009-01-13 |
Family
ID=39831122
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020070033756A KR100878698B1 (ko) | 2007-04-05 | 2007-04-05 | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및이를 포함하는 약학 조성물 |
Country Status (9)
Country | Link |
---|---|
US (1) | US20100137367A1 (ko) |
EP (1) | EP2144896A4 (ko) |
JP (1) | JP2010522747A (ko) |
KR (1) | KR100878698B1 (ko) |
CN (1) | CN101652358A (ko) |
AU (1) | AU2008235668A1 (ko) |
CA (1) | CA2682822A1 (ko) |
TW (1) | TW200900392A (ko) |
WO (1) | WO2008123701A1 (ko) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100879409B1 (ko) * | 2007-06-11 | 2009-01-19 | 한미약품 주식회사 | (s)-베포타스틴의 제조방법 및 이에 사용되는 중간체 |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101307712B1 (ko) | 2008-12-02 | 2013-09-11 | 한미사이언스 주식회사 | 결정형의 베포타스틴 금속염 수화물, 이의 제조방법 및 이를 포함하는 약학 조성물 |
JP2011195500A (ja) * | 2010-03-19 | 2011-10-06 | Tokuyama Corp | (s)−4−[4−[(4−クロロフェニル)(2−ピリジル)メトキシ]ピペリジノ]ブタン酸一ベンゼンスルホン酸塩の製造方法 |
CN103260623B (zh) * | 2010-10-06 | 2016-11-02 | 伊斯塔制药公司 | 贝托斯汀组合物 |
CN103269687B (zh) * | 2011-01-04 | 2016-09-14 | 伊斯塔制药公司 | 贝托斯汀组合物 |
US9800605B2 (en) * | 2015-01-30 | 2017-10-24 | Securonix, Inc. | Risk scoring for threat assessment |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW486475B (en) * | 1996-12-26 | 2002-05-11 | Ube Industries | Acid addition salt of optically active piperidine compound and process for preparing the same |
JP3909998B2 (ja) * | 2000-03-22 | 2007-04-25 | 田辺製薬株式会社 | 経口投与製剤 |
JP2002212067A (ja) * | 2001-01-15 | 2002-07-31 | Taisho Pharmaceut Co Ltd | 風邪治療用組成物 |
JP4365107B2 (ja) * | 2001-05-25 | 2009-11-18 | エスエス製薬株式会社 | 医薬組成物 |
CN1674916A (zh) * | 2002-08-30 | 2005-09-28 | 奥坦纳医药公司 | 环缩松与抗组胺药的组合用于治疗变应性鼻炎的用途 |
-
2007
- 2007-04-05 KR KR1020070033756A patent/KR100878698B1/ko active IP Right Grant
-
2008
- 2008-04-03 TW TW097112166A patent/TW200900392A/zh unknown
- 2008-04-04 CN CN200880010709A patent/CN101652358A/zh active Pending
- 2008-04-04 AU AU2008235668A patent/AU2008235668A1/en not_active Abandoned
- 2008-04-04 US US12/531,003 patent/US20100137367A1/en not_active Abandoned
- 2008-04-04 EP EP08741162A patent/EP2144896A4/en not_active Withdrawn
- 2008-04-04 WO PCT/KR2008/001912 patent/WO2008123701A1/en active Application Filing
- 2008-04-04 CA CA002682822A patent/CA2682822A1/en not_active Abandoned
- 2008-04-04 JP JP2010500837A patent/JP2010522747A/ja not_active Withdrawn
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100879409B1 (ko) * | 2007-06-11 | 2009-01-19 | 한미약품 주식회사 | (s)-베포타스틴의 제조방법 및 이에 사용되는 중간체 |
Also Published As
Publication number | Publication date |
---|---|
US20100137367A1 (en) | 2010-06-03 |
WO2008123701A1 (en) | 2008-10-16 |
AU2008235668A1 (en) | 2008-10-16 |
KR100878698B1 (ko) | 2009-01-13 |
EP2144896A4 (en) | 2011-06-29 |
EP2144896A1 (en) | 2010-01-20 |
CN101652358A (zh) | 2010-02-17 |
CA2682822A1 (en) | 2008-10-16 |
TW200900392A (en) | 2009-01-01 |
JP2010522747A (ja) | 2010-07-08 |
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