CN1298301A - 用帕罗西汀治疗一般性焦虑症 - Google Patents
用帕罗西汀治疗一般性焦虑症 Download PDFInfo
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- CN1298301A CN1298301A CN99805328A CN99805328A CN1298301A CN 1298301 A CN1298301 A CN 1298301A CN 99805328 A CN99805328 A CN 99805328A CN 99805328 A CN99805328 A CN 99805328A CN 1298301 A CN1298301 A CN 1298301A
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- paroxetine
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- general anxiety
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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
- A61K31/435—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
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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
- A61K31/435—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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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Abstract
治疗一般性焦虑症的方法,所述方法包括将有效、无毒量的帕罗西汀或其可药用盐或溶剂合物对需要这种治疗人或非人动物给药。
Description
本发明涉及治疗一般性焦虑症的方法，以及尤其是帕罗西汀在这种治疗中的应用。
US-A-3912743和US-A-4007196中描述了具有抗抑郁和抗帕金森氏病特性的药物。在这些公开的药物中，尤其重要的化合物是帕罗西汀，即4-(4’-氟苯基)-3-(3’,4’-亚甲基二氧苯氧基甲基)哌啶的(-)反式异构体(参见US-A-4007196的实施例2)。帕罗西汀盐酸盐已被批准用于特别是抑郁症、强迫性神经失调(OCD)和恐慌症的人体治疗。
在商业应用中，帕罗西汀盐酸盐是以结晶半水合物(参见BeechamGroup的EP-A-0223403)形式提供的。各种脱水结晶形式也是已知的(参见SmithKline Beecham plc的WO96/24595)。
我们现在已经惊奇地发现，帕罗西汀具有作为治疗一般性焦虑症的药物的潜在治疗用途。
因此，本发明提供了治疗一般性焦虑症的方法，所述方法包括将有效、无毒量的帕罗西汀或其可药用盐或溶剂合物对需要这种治疗的人或非人动物给药。
本发明还提供了帕罗西汀或其可药用盐或溶剂合物在制备用于治疗一般性焦虑症的药物中的应用。
优选的帕罗西汀可药用盐是其结晶盐酸盐。制备帕罗西汀盐酸盐的合适方法包括在US 4009196、US 4721723、US 4902801、US4861 893、US 5039803和PCT/GB93/00721中提及的方法。如EP-A-0223403所述制得的半水合物是特别优选的。
用于治疗一般性焦虑症的药物可通过将帕罗西汀或其可药用盐或溶剂合物与适当载体以常规方式混合而制得，所述载体可包括稀释剂、粘合剂、填充剂、崩解剂、矫味剂、着色剂、润滑剂或防腐剂。
优选将药物制成适于药物或兽药使用的单位剂型。例如，这类制剂可以药包形式，其中附有用于治疗一般性焦虑症的书面或印刷说明。
帕罗西汀或其可药用盐或溶剂合物的合适剂量取决于患者一般性焦虑症的严重程度和身体状况。还取决于特别是吸收效力、给药频率和途径。
可将帕罗西汀或其可药用盐或溶剂合物制剂以通过任意途径给药，所述给药途径的实例有口服给药、舌下给药、直肠给药、局部给药、非胃肠道给药、静脉内给药或肌内给药。如果需要的话，可将制剂设计成缓慢释放帕罗西汀或其可药用盐或溶剂合物的缓释剂型。
药剂可呈例如片剂、胶囊剂、药囊、小瓶装制剂、粉剂、粒剂、锭剂、可重配粉剂，或液体制剂例如溶液剂或悬浮剂，或栓剂。
药剂，例如适于口服给药的药剂可含有常规赋形剂例如粘合剂如糖浆、阿拉伯胶、明胶、山梨醇、黄蓍胶、或聚乙烯吡咯烷酮；填充剂，例如乳糖、糖、玉米淀粉、磷酸钙、山梨醇或甘油；制片润滑剂，例如硬脂酸镁；崩解剂，例如淀粉、聚乙烯吡咯烷酮、羟乙酸淀粉钠或微晶纤维素；或可药用调整剂，例如十二烷基硫酸钠。
固体药剂可通过混合、填充、制片等常规方法制得。可使用重复混合操作将帕罗西汀或其可药用盐或溶剂合物分布在采用大量填充剂的药物中。当药物呈片剂、粉剂、或锭剂形式时，可使用适于配制固体药物组合物的所有载体，例如硬脂酸镁、淀粉、葡萄糖、乳糖、蔗糖、米粉和白垩。可依据标准制药实践中众所周知的方法将片剂包衣，尤其是进行肠溶衣包衣。药物可以呈可吞服胶囊形式，例如包含帕罗西汀或其盐、如果需要的话和载体或其它赋形剂的明胶胶囊。
液体口服药物可呈例如乳剂、糖浆剂、或酏剂形式，或者可制成在使用前用水或其它适当载体重新配制的干燥产品。这种液体药物可含有常规添加剂例如混悬剂，例如山梨醇、糖浆、甲基纤维素、明胶、羟乙基纤维素、羧甲基纤维素、硬脂酸铝凝胶、氢化可食用脂肪；乳化剂，例如卵磷脂、脱水山梨醇一油酸酯、或阿拉伯胶；水或非水载体，包括食用油例如杏仁油、分馏椰子油，油酯例如甘油酯，或丙二醇、乙醇、甘油、水或标准盐水；防腐剂，例如对羟基苯甲酸甲酯或对羟基苯甲酸丙酯或山梨酸；以及如果需要可添加矫味剂或着色剂。
帕罗西汀或其可药用盐或溶剂合物还可通过非口服途径给药。可依据常规制药方法配制这种药物，例如配制成直肠给药的栓剂。还可将这种药物配制成注射剂，例如水或非水溶液，在可药用液体例如无菌不合热源的水或非胃肠道可接受油或液体混合物中的悬浮剂或乳剂。这种液体制剂可含有抑菌剂、抗氧化剂或其它防腐剂，缓冲剂或使溶液与血液等渗的溶质，增稠剂，悬浮剂或其它可药用添加剂。这种剂型可呈单位剂型，例如装有注射剂的安瓿或一次性应用注射装置，或多剂量剂型，例如可从中抽出适当剂量的瓶子，或可用来配制注射剂的固体剂型或浓缩物。
如上所述，帕罗西汀或其可药用盐或溶剂合物的有效剂量取决于欲治疗的一般性焦虑症的严重程度、患者的身体状况、以及给药频率和途径。单位剂量通常包含2-1000mg，优选包含30-500mg，特别是20、50、100、150、200、250、300、350、400、450、或500mg。组合物每天可给药一次或多次，例如每天给药2、3或4次，对于体重为70kg的成年患者，总日剂量一般为100-3000mg。优选的单位剂量包含2-20mg帕罗西汀(按游离碱计)，并且如果需要的话可给药多次以达到预定日剂量。
本发明还提供了用于治疗一般性焦虑症的药物组合物，其中含有有效量的帕罗西汀或其可药用盐或溶剂合物、和可药用载体。这种组合物可通过上述方法制得。
下述实施例公开了适用于本发明的药物组合物。
实施例
以常规方式将下述组分混合在一起，并压制成含有约20mg帕罗西汀(按游离碱计)、重量约为300mg的片剂。
帕罗西汀盐酸盐半水合物 228.8g
磷酸氢二钠二水合物 2441.2g
羟丙基甲基纤维素2910 150.0g
羟乙酸淀粉钠 150.0g
硬脂酸镁 30.0g
总重量 3000.0g
Claims (4)
1．治疗一般性焦虑症的方法，所述方法包括将有效、无毒量的帕罗西汀或其可药用盐或溶剂合物对需要这种治疗人或非人动物给药。
2．帕罗西汀或其可药用盐或溶剂合物在制备用于治疗一般性焦虑症的药物中的应用。
3．用于治疗一般性焦虑症的药物组合物，其中含有有效量的帕罗西汀或其可药用盐或溶剂合物、和可药用载体。
4．权利要求1的方法、权利要求2的应用、或权利要求3的药物组合物，其中所述帕罗西汀的可药用盐是其盐酸盐。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9808479.1A GB9808479D0 (en) | 1998-04-22 | 1998-04-22 | Method of treatment |
| GB9808479.1 | 1998-04-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1298301A true CN1298301A (zh) | 2001-06-06 |
Family
ID=10830715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99805328A Pending CN1298301A (zh) | 1998-04-22 | 1999-04-22 | 用帕罗西汀治疗一般性焦虑症 |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1073437A4 (zh) |
| JP (1) | JP2002512189A (zh) |
| KR (1) | KR20010034817A (zh) |
| CN (1) | CN1298301A (zh) |
| AP (1) | AP2000001959A0 (zh) |
| AU (1) | AU3864899A (zh) |
| BG (1) | BG104939A (zh) |
| BR (1) | BR9909791A (zh) |
| CA (1) | CA2328896A1 (zh) |
| CZ (1) | CZ20003885A3 (zh) |
| EA (1) | EA200001088A1 (zh) |
| GB (1) | GB9808479D0 (zh) |
| HU (1) | HUP0101350A3 (zh) |
| ID (1) | ID27546A (zh) |
| IL (1) | IL139167A0 (zh) |
| NO (1) | NO20005286L (zh) |
| PL (1) | PL343494A1 (zh) |
| SK (1) | SK15672000A3 (zh) |
| TR (1) | TR200003082T2 (zh) |
| WO (1) | WO1999053919A1 (zh) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2297550B (en) * | 1995-02-06 | 1997-04-09 | Smithkline Beecham Plc | Paroxetine hydrochloride anhydrate substantially free of bound organic solvent |
| GB9514842D0 (en) * | 1995-07-20 | 1995-09-20 | Smithkline Beecham Plc | Novel formulation |
-
1998
- 1998-04-22 GB GBGB9808479.1A patent/GB9808479D0/en not_active Ceased
-
1999
- 1999-04-22 AP APAP/P/2000/001959A patent/AP2000001959A0/en unknown
- 1999-04-22 ID IDW20002124A patent/ID27546A/id unknown
- 1999-04-22 HU HU0101350A patent/HUP0101350A3/hu unknown
- 1999-04-22 EP EP99921431A patent/EP1073437A4/en not_active Withdrawn
- 1999-04-22 WO PCT/US1999/008786 patent/WO1999053919A1/en not_active Ceased
- 1999-04-22 CZ CZ20003885A patent/CZ20003885A3/cs unknown
- 1999-04-22 BR BR9909791-5A patent/BR9909791A/pt not_active IP Right Cessation
- 1999-04-22 AU AU38648/99A patent/AU3864899A/en not_active Abandoned
- 1999-04-22 CN CN99805328A patent/CN1298301A/zh active Pending
- 1999-04-22 JP JP2000544323A patent/JP2002512189A/ja not_active Withdrawn
- 1999-04-22 EA EA200001088A patent/EA200001088A1/ru unknown
- 1999-04-22 PL PL99343494A patent/PL343494A1/xx not_active Application Discontinuation
- 1999-04-22 SK SK1567-2000A patent/SK15672000A3/sk unknown
- 1999-04-22 CA CA002328896A patent/CA2328896A1/en not_active Abandoned
- 1999-04-22 KR KR1020007011729A patent/KR20010034817A/ko not_active Withdrawn
- 1999-04-22 IL IL13916799A patent/IL139167A0/xx unknown
- 1999-04-22 TR TR2000/03082T patent/TR200003082T2/xx unknown
-
2000
- 2000-10-20 NO NO20005286A patent/NO20005286L/no not_active Application Discontinuation
- 2000-11-13 BG BG104939A patent/BG104939A/bg unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TR200003082T2 (tr) | 2001-01-22 |
| AP2000001959A0 (en) | 2000-12-31 |
| KR20010034817A (ko) | 2001-04-25 |
| PL343494A1 (en) | 2001-08-27 |
| WO1999053919A1 (en) | 1999-10-28 |
| JP2002512189A (ja) | 2002-04-23 |
| HUP0101350A2 (hu) | 2002-05-29 |
| CA2328896A1 (en) | 1999-10-28 |
| BR9909791A (pt) | 2000-12-26 |
| ID27546A (id) | 2001-04-12 |
| HUP0101350A3 (en) | 2002-06-28 |
| CZ20003885A3 (cs) | 2001-09-12 |
| IL139167A0 (en) | 2001-11-25 |
| EP1073437A1 (en) | 2001-02-07 |
| NO20005286L (no) | 2000-12-20 |
| AU3864899A (en) | 1999-11-08 |
| EP1073437A4 (en) | 2003-04-16 |
| GB9808479D0 (en) | 1998-06-17 |
| SK15672000A3 (sk) | 2001-04-09 |
| NO20005286D0 (no) | 2000-10-20 |
| EA200001088A1 (ru) | 2001-04-23 |
| BG104939A (bg) | 2001-09-28 |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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