CN1688297A - 包含西布曲明甲磺酸盐半水合物晶体的药物组合物 - Google Patents
包含西布曲明甲磺酸盐半水合物晶体的药物组合物 Download PDFInfo
- Publication number
- CN1688297A CN1688297A CNA038238195A CN03823819A CN1688297A CN 1688297 A CN1688297 A CN 1688297A CN A038238195 A CNA038238195 A CN A038238195A CN 03823819 A CN03823819 A CN 03823819A CN 1688297 A CN1688297 A CN 1688297A
- Authority
- CN
- China
- Prior art keywords
- sibutramine
- formula
- ether
- acetate
- crystalline
- 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
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Classifications
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
- C07C211/16—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings
- C07C211/17—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings containing only non-condensed rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Emergency Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
2θ±0.2 d I/Io | 2θ±0.2 d I/Io |
8.2 10.8 86810.8 8.17 21811.7 7.53 21012.0 7.36 27612.3 7.19 66115.8 5.61 71616.4 5.39 72517.4 5.10 79217.8 4.97 49819.0 4.68 556 | 21.2 4.19 78521.9 4.06 64622.2 4.00 31522.8 3.90 28623.3 3.81 45624.4 3.65 53724.9 3.58 59625.3 3.52 32225.6 3.47 35126.8 3.33 1000 |
化合物 | 水中的溶解度(mg/ml,pH5.2) |
式(IV)的西布曲明盐酸盐单水合物 | 2.8 |
式(I)的西布曲明甲磺酸盐半水合物 | 2500 |
化合物 | 初始 | 1个月后的残留率 | 2个月后的残留率 | 3个月后的残留率 | 6个月后的残留率 |
式(IV)的西布曲明盐酸盐单水合物 | 1.000 | 1.000 | 0.999 | 0.999 | 0.992 |
式(I)的西布曲明甲磺酸盐半水合物 | 1.000 | 1.001 | 0.999 | 0.999 | 1.000 |
温度(℃)相对湿度(℃) | 储存时间(天) | 式(I)的西布曲明甲磺酸盐半水合物 | 式(IV)的西布曲明盐酸盐单水合物 | 无水西布曲明甲磺酸盐 |
40℃75% | 125 | 2.272.302.30 | 5.405.455.48 | 0.602.202.25 |
40℃10% | 125 | 2.272.252.26 | 5.405.365.36 | 0.600.710.70 |
超重的Zuker大鼠 | 瘦的Zuker大鼠 | |||
给药组 | 对照组 | 给药组 | 对照组 | |
测试前的平均体重(g:A) | 332.2 | 333.2 | 245.0 | 244.8 |
测试后的平均体重(g:B) | 455.6 | 486.2 | 303.4 | 323.6 |
重量增加(g:B-A) | 123.4 | 153.0 | 58.4 | 78.8 |
重量减轻作用(g:(对照组的重量增加)-(给药组的重量增加)) | 29.6 | 20.4 |
Claims (15)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020020060798 | 2002-10-05 | ||
KR20020060798 | 2002-10-05 | ||
KR1020030053752 | 2003-08-04 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1688297A true CN1688297A (zh) | 2005-10-26 |
CN100342851C CN100342851C (zh) | 2007-10-17 |
Family
ID=36675124
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB038238195A Expired - Fee Related CN100342851C (zh) | 2002-10-05 | 2003-09-25 | 包含西布曲明甲磺酸盐半水合物晶体的药物组合物 |
Country Status (6)
Country | Link |
---|---|
KR (1) | KR100536750B1 (zh) |
CN (1) | CN100342851C (zh) |
IL (1) | IL167659A (zh) |
RS (1) | RS20050272A (zh) |
UA (1) | UA76913C2 (zh) |
ZA (1) | ZA200502691B (zh) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100618176B1 (ko) * | 2004-12-02 | 2006-09-01 | 휴먼팜 주식회사 | 시부트라민 주석산염, 이의 제조 방법 및 이를 포함하는약학적 조성물 |
KR100830002B1 (ko) * | 2005-01-06 | 2008-05-15 | 씨제이제일제당 (주) | 시부트라민의 무기산염 |
KR100632470B1 (ko) * | 2005-02-25 | 2006-10-12 | 민연식 | 결정성 시부트라민 캄실레이트염과 이의 제조방법 |
KR100814384B1 (ko) * | 2006-02-10 | 2008-03-18 | 대화제약 주식회사 | 시부트라민 염을 함유하는 약학 조성물 및 이의 제조방법 |
KR100800561B1 (ko) * | 2006-03-29 | 2008-02-04 | 주식회사 삼오제약 | 시부트라민 술포닐염의 제조방법 및 이를 포함하는비만관련 질환 예방 및 치료용 약학조성물 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA821577B (en) * | 1981-04-06 | 1983-03-30 | Boots Co Plc | Therapeutic agents |
IE52768B1 (en) * | 1981-04-06 | 1988-02-17 | Boots Co Ltd | 1-arylcyclobutylalkylamine compounds useful as therapeutic agents |
GB8531071D0 (en) * | 1985-12-17 | 1986-01-29 | Boots Co Plc | Therapeutic compound |
US6399826B1 (en) * | 1999-08-11 | 2002-06-04 | Sepracor Inc. | Salts of sibutramine metabolites, methods of making sibutramine metabolites and intermediates useful in the same, and methods of treating pain |
AU2002210816A1 (en) * | 2000-11-02 | 2002-05-15 | Torrent Pharmaceuticals Ltd | Process for preparation of beta-phenethylamine derivative |
-
2003
- 2003-08-04 KR KR10-2003-0053752A patent/KR100536750B1/ko not_active IP Right Cessation
- 2003-09-25 UA UAA200503096A patent/UA76913C2/uk unknown
- 2003-09-25 RS YUP-2005/0272A patent/RS20050272A/sr unknown
- 2003-09-25 CN CNB038238195A patent/CN100342851C/zh not_active Expired - Fee Related
-
2005
- 2005-03-24 IL IL167659A patent/IL167659A/en not_active IP Right Cessation
- 2005-04-04 ZA ZA200502691A patent/ZA200502691B/en unknown
Also Published As
Publication number | Publication date |
---|---|
ZA200502691B (en) | 2005-11-02 |
UA76913C2 (uk) | 2006-09-15 |
RS20050272A (en) | 2007-09-21 |
CN100342851C (zh) | 2007-10-17 |
KR100536750B1 (ko) | 2005-12-16 |
IL167659A (en) | 2010-04-29 |
KR20040031574A (ko) | 2004-04-13 |
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Owner name: HANMI PHARMACEUTICAL INDUSTRIAL CO., LTD. Free format text: FORMER OWNER: HANMI PHARM. CO., LTD. Effective date: 20110315 |
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Free format text: CORRECT: ADDRESS; FROM: GYEONGGI, SOUTH KOREA TO: SEOUL, SOUTH KOREA |
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Effective date of registration: 20110315 Address after: Seoul, South Kerean Patentee after: Hanmi Pharm Ind Co.,Ltd. Address before: Gyeonggi Do, South Korea Patentee before: Hanmi Pharm. Co., Ltd. |
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CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20071017 Termination date: 20110925 |