CN1308521A - 含帕罗西丁的新制剂 - Google Patents
含帕罗西丁的新制剂 Download PDFInfo
- Publication number
- CN1308521A CN1308521A CN99808325A CN99808325A CN1308521A CN 1308521 A CN1308521 A CN 1308521A CN 99808325 A CN99808325 A CN 99808325A CN 99808325 A CN99808325 A CN 99808325A CN 1308521 A CN1308521 A CN 1308521A
- Authority
- CN
- China
- Prior art keywords
- paroxetine
- anhydrous
- hydrochlorate
- tablet
- semihydrate
- 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.)
- Pending
Links
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 title claims abstract description 52
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 title claims description 50
- 229960002296 paroxetine Drugs 0.000 title claims description 50
- 239000000203 mixture Substances 0.000 title description 6
- 238000009472 formulation Methods 0.000 title description 4
- 238000000034 method Methods 0.000 claims abstract description 23
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 13
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 8
- 239000008101 lactose Substances 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 7
- 239000007888 film coating Substances 0.000 claims description 5
- 238000009501 film coating Methods 0.000 claims description 5
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 4
- 239000002274 desiccant Substances 0.000 claims description 3
- 238000005453 pelletization Methods 0.000 claims description 3
- 239000002002 slurry Substances 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- 150000002016 disaccharides Chemical class 0.000 claims description 2
- 150000002772 monosaccharides Chemical class 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 229960005183 paroxetine hydrochloride Drugs 0.000 abstract 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 38
- 235000019359 magnesium stearate Nutrition 0.000 description 19
- 229940080313 sodium starch Drugs 0.000 description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- UKMSUNONTOPOIO-UHFFFAOYSA-N Behenic acid Natural products CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 description 4
- 235000021357 Behenic acid Nutrition 0.000 description 4
- 229940116226 behenic acid Drugs 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 3
- 230000009747 swallowing Effects 0.000 description 3
- DMBUODUULYCPAK-UHFFFAOYSA-N 1,3-bis(docosanoyloxy)propan-2-yl docosanoate Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCCCCCC DMBUODUULYCPAK-UHFFFAOYSA-N 0.000 description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 206010041250 Social phobia Diseases 0.000 description 2
- 239000003513 alkali Substances 0.000 description 2
- 239000000935 antidepressant agent Substances 0.000 description 2
- 229940005513 antidepressants Drugs 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 238000007907 direct compression Methods 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 238000003825 pressing Methods 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010020710 Hyperphagia Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 206010029897 Obsessive thoughts Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 206010036618 Premenstrual syndrome Diseases 0.000 description 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000001430 anti-depressive effect Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000005056 compaction Methods 0.000 description 1
- 229960005168 croscarmellose Drugs 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000012943 hotmelt Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 235000019629 palatability Nutrition 0.000 description 1
- 208000019906 panic disease Diseases 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 208000022530 polyphagia Diseases 0.000 description 1
- 201000000484 premenstrual tension Diseases 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 238000003908 quality control method Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
-
- 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
- A61K9/2095—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
-
- 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
- A61P25/24—Antidepressants
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9810181.9A GB9810181D0 (en) | 1998-05-13 | 1998-05-13 | Novel formulations |
| GB9810181.9 | 1998-05-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1308521A true CN1308521A (zh) | 2001-08-15 |
Family
ID=10831927
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99808325A Pending CN1308521A (zh) | 1998-05-13 | 1999-05-13 | 含帕罗西丁的新制剂 |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1077682A2 (no) |
| JP (1) | JP2002514591A (no) |
| KR (1) | KR20010043574A (no) |
| CN (1) | CN1308521A (no) |
| AP (1) | AP2000002019A0 (no) |
| AU (1) | AU3940999A (no) |
| BG (1) | BG105010A (no) |
| BR (1) | BR9910401A (no) |
| CA (1) | CA2331871A1 (no) |
| EA (1) | EA200001174A1 (no) |
| GB (1) | GB9810181D0 (no) |
| HU (1) | HUP0102064A2 (no) |
| ID (1) | ID28019A (no) |
| IL (1) | IL139594A0 (no) |
| NO (1) | NO20005683L (no) |
| PL (1) | PL344573A1 (no) |
| SK (1) | SK17142000A3 (no) |
| TR (1) | TR200003350T2 (no) |
| WO (1) | WO1999058113A2 (no) |
| ZA (1) | ZA200006562B (no) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0003232D0 (en) * | 2000-02-11 | 2000-04-05 | Smithkline Beecham Plc | Novel composition |
| CA2359812C (en) | 2000-11-20 | 2004-02-10 | The Procter & Gamble Company | Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures |
| AU2002330771A1 (en) * | 2001-10-22 | 2003-06-10 | Synthon B.V. | N-formyl derivatives of paroxetine |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9325644D0 (en) * | 1993-12-15 | 1994-02-16 | Smithkline Beecham Plc | Novel formulation |
| US5672612A (en) * | 1996-09-09 | 1997-09-30 | Pentech Pharmaceuticals, Inc. | Amorphous paroxetine composition |
| EA002034B1 (ru) * | 1997-01-15 | 2001-12-24 | Смитклайн Бичам Плс | Композиция на основе пароксетина |
| BR9813808A (pt) * | 1997-12-19 | 2002-05-28 | Smithkline Beecham Corp | Processo para produção de comprimidos para dispersão na mordida |
-
1998
- 1998-05-13 GB GBGB9810181.9A patent/GB9810181D0/en not_active Ceased
-
1999
- 1999-05-13 HU HU0102064A patent/HUP0102064A2/hu unknown
- 1999-05-13 CA CA002331871A patent/CA2331871A1/en not_active Abandoned
- 1999-05-13 EA EA200001174A patent/EA200001174A1/ru unknown
- 1999-05-13 CN CN99808325A patent/CN1308521A/zh active Pending
- 1999-05-13 JP JP2000547965A patent/JP2002514591A/ja active Pending
- 1999-05-13 AU AU39409/99A patent/AU3940999A/en not_active Abandoned
- 1999-05-13 ID IDW20002347A patent/ID28019A/id unknown
- 1999-05-13 EP EP99922302A patent/EP1077682A2/en not_active Withdrawn
- 1999-05-13 KR KR1020007012706A patent/KR20010043574A/ko not_active Application Discontinuation
- 1999-05-13 PL PL99344573A patent/PL344573A1/xx unknown
- 1999-05-13 TR TR2000/03350T patent/TR200003350T2/xx unknown
- 1999-05-13 SK SK1714-2000A patent/SK17142000A3/sk unknown
- 1999-05-13 BR BR9910401-6A patent/BR9910401A/pt not_active Application Discontinuation
- 1999-05-13 WO PCT/GB1999/001520 patent/WO1999058113A2/en not_active Application Discontinuation
- 1999-05-13 IL IL13959499A patent/IL139594A0/xx unknown
- 1999-05-13 AP APAP/P/2000/002019A patent/AP2000002019A0/en unknown
-
2000
- 2000-11-10 NO NO20005683A patent/NO20005683L/no not_active Application Discontinuation
- 2000-11-13 ZA ZA200006562A patent/ZA200006562B/en unknown
- 2000-11-30 BG BG105010A patent/BG105010A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200006562B (en) | 2002-02-13 |
| GB9810181D0 (en) | 1998-07-08 |
| HUP0102064A2 (hu) | 2002-05-29 |
| ID28019A (id) | 2001-05-03 |
| WO1999058113A3 (en) | 2000-02-17 |
| NO20005683D0 (no) | 2000-11-10 |
| TR200003350T2 (tr) | 2001-03-21 |
| AP2000002019A0 (en) | 2000-12-31 |
| AU3940999A (en) | 1999-11-29 |
| BR9910401A (pt) | 2001-01-09 |
| WO1999058113A2 (en) | 1999-11-18 |
| NO20005683L (no) | 2000-12-05 |
| PL344573A1 (en) | 2001-11-05 |
| EP1077682A2 (en) | 2001-02-28 |
| SK17142000A3 (sk) | 2001-06-11 |
| EA200001174A1 (ru) | 2001-06-25 |
| IL139594A0 (en) | 2002-02-10 |
| CA2331871A1 (en) | 1999-11-18 |
| BG105010A (en) | 2001-07-31 |
| KR20010043574A (ko) | 2001-05-25 |
| JP2002514591A (ja) | 2002-05-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |