DD242349A5 - Verfahren zur herstellung einer synergistischen kombination von flupirtin und 4-acetamido-phenol - Google Patents
Verfahren zur herstellung einer synergistischen kombination von flupirtin und 4-acetamido-phenol Download PDFInfo
- Publication number
- DD242349A5 DD242349A5 DD86285896A DD28589686A DD242349A5 DD 242349 A5 DD242349 A5 DD 242349A5 DD 86285896 A DD86285896 A DD 86285896A DD 28589686 A DD28589686 A DD 28589686A DD 242349 A5 DD242349 A5 DD 242349A5
- Authority
- DD
- German Democratic Republic
- Prior art keywords
- flupirtine
- weight
- phenol
- physiologically acceptable
- acetamido
- Prior art date
Links
- JUUFBMODXQKSTD-UHFFFAOYSA-N N-[2-amino-6-[(4-fluorophenyl)methylamino]-3-pyridinyl]carbamic acid ethyl ester Chemical compound N1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 JUUFBMODXQKSTD-UHFFFAOYSA-N 0.000 title claims abstract description 53
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 title claims abstract description 48
- 238000004519 manufacturing process Methods 0.000 title claims 3
- 239000011885 synergistic combination Substances 0.000 title abstract description 5
- 229960003667 flupirtine Drugs 0.000 claims abstract description 46
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- 238000000034 method Methods 0.000 claims abstract description 11
- 239000002253 acid Substances 0.000 claims abstract description 8
- 150000007513 acids Chemical class 0.000 claims abstract description 7
- 239000003814 drug Substances 0.000 claims abstract description 7
- 239000004480 active ingredient Substances 0.000 claims abstract description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 3
- 229910052751 metal Inorganic materials 0.000 claims abstract 5
- 239000002184 metal Substances 0.000 claims abstract 5
- 150000002739 metals Chemical class 0.000 claims abstract 5
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 4
- 239000012050 conventional carrier Substances 0.000 claims abstract 3
- 239000000203 mixture Substances 0.000 claims description 7
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 3
- 229920002261 Corn starch Polymers 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- 239000004368 Modified starch Substances 0.000 claims description 2
- 239000008120 corn starch Substances 0.000 claims description 2
- 229910021485 fumed silica Inorganic materials 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 229940116364 hard fat Drugs 0.000 claims description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 2
- 235000019426 modified starch Nutrition 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims 2
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims 1
- 229940083466 soybean lecithin Drugs 0.000 claims 1
- 230000000202 analgesic effect Effects 0.000 abstract description 11
- 230000002195 synergetic effect Effects 0.000 abstract description 4
- 230000003389 potentiating effect Effects 0.000 abstract description 3
- 230000001741 anti-phlogistic effect Effects 0.000 abstract description 2
- 239000007884 disintegrant Substances 0.000 abstract 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 abstract 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 abstract 1
- 229960005489 paracetamol Drugs 0.000 description 32
- DPYIXBFZUMCMJM-BTJKTKAUSA-N (z)-but-2-enedioic acid;ethyl n-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate Chemical compound OC(=O)\C=C/C(O)=O.N1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 DPYIXBFZUMCMJM-BTJKTKAUSA-N 0.000 description 7
- 208000002193 Pain Diseases 0.000 description 6
- 229960001655 flupirtine maleate Drugs 0.000 description 6
- 230000036407 pain Effects 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 241000700159 Rattus Species 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- SSOLNOMRVKKSON-UHFFFAOYSA-N proguanil Chemical compound CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C=C1 SSOLNOMRVKKSON-UHFFFAOYSA-N 0.000 description 4
- 239000000829 suppository Substances 0.000 description 4
- 208000025747 Rheumatic disease Diseases 0.000 description 3
- 201000009030 Carcinoma Diseases 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 229940050410 gluconate Drugs 0.000 description 2
- 230000002757 inflammatory effect Effects 0.000 description 2
- 208000014674 injury Diseases 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 230000000552 rheumatic effect Effects 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 230000008733 trauma Effects 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 description 1
- 229910002016 Aerosil® 200 Inorganic materials 0.000 description 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
- WHXDLJOHWHFXJR-UHFFFAOYSA-N CC(=O)NC1=CC=C(O)C=C1.CC(=O)NC1=CC=C(O)C=C1 Chemical compound CC(=O)NC1=CC=C(O)C=C1.CC(=O)NC1=CC=C(O)C=C1 WHXDLJOHWHFXJR-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 208000005171 Dysmenorrhea Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 208000004145 Endometritis Diseases 0.000 description 1
- 206010022714 Intestinal ulcer Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000029082 Pelvic Inflammatory Disease Diseases 0.000 description 1
- 206010036030 Polyarthritis Diseases 0.000 description 1
- 208000004550 Postoperative Pain Diseases 0.000 description 1
- 240000001987 Pyrus communis Species 0.000 description 1
- 206010049677 Salpingo-oophoritis Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000007107 Stomach Ulcer Diseases 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 230000003412 degenerative effect Effects 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 210000004392 genitalia Anatomy 0.000 description 1
- 239000008240 homogeneous mixture Substances 0.000 description 1
- 238000000265 homogenisation Methods 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000004968 inflammatory condition Effects 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000006201 parenteral dosage form Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 206010034674 peritonitis Diseases 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000008347 soybean phospholipid Substances 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/33—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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE3523120 | 1985-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DD242349A5 true DD242349A5 (de) | 1987-01-28 |
Family
ID=6274416
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DD86285896A DD242349A5 (de) | 1985-06-28 | 1986-01-02 | Verfahren zur herstellung einer synergistischen kombination von flupirtin und 4-acetamido-phenol |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP0207193A2 (fr) |
| JP (1) | JPS624229A (fr) |
| AU (1) | AU570582B2 (fr) |
| DD (1) | DD242349A5 (fr) |
| DE (1) | DE3545201A1 (fr) |
| DK (1) | DK596785A (fr) |
| ES (1) | ES8702142A1 (fr) |
| FI (1) | FI855016A7 (fr) |
| GR (1) | GR860120B (fr) |
| HU (1) | HU193845B (fr) |
| PT (1) | PT81848B (fr) |
| ZA (1) | ZA859770B (fr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN172468B (fr) * | 1990-07-14 | 1993-08-14 | Asta Medica Ag | |
| DE4236752A1 (de) * | 1992-10-30 | 1994-05-05 | Asta Medica Ag | Kombinationspräparat aus Flupirtin und Morphin zur Behandlung von Schmerzen und zur Vermeidung der Morphin-Abhängigkeit |
| DE4319649A1 (de) * | 1993-03-18 | 1994-09-22 | Asta Medica Ag | Feste Flupirtin enthaltende orale Darreichungsformen mit kontrollierter Wirkstoffabgabe |
| KR20020040767A (ko) * | 1999-08-03 | 2002-05-30 | 아베데 파르마 게엠베하 운트 콤파니 카게 | 개와 고양이에서 퇴행성 관절 질환으로 인한 통증을경감시키기 위한 플루피르틴의 용도 |
| EP1701725B1 (fr) | 2003-12-16 | 2013-07-31 | Relevare Aust. Pty Ltd | Compositions comprenant le flupiritne et un opioide pour le traitement de la douleur neuropathique |
| JP5909750B2 (ja) * | 2007-11-13 | 2016-04-27 | マリンクロット アイピー | 低用量静脈内アセトアミノフェン |
| DE102010063612A1 (de) | 2010-12-20 | 2012-06-21 | Awd.Pharma Gmbh & Co. Kg | Neue Multikomponentenkristalle aus ([2-Amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamidsäureethylester und 2-[2-[(2,6-Dichlorphenyl)-amino]-phenyl]-essigsäure |
| DE102010063609A1 (de) | 2010-12-20 | 2012-06-21 | Awd.Pharma Gmbh & Co. Kg | Neue Multikomponentenkristalle aus ([2-Amino-6-(4-fluoro-benzylamino)-pyridin-3yl)-carbamidsäureethylester und einer Arylpropionsäure |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO860825L (no) * | 1985-03-23 | 1986-09-24 | Degussa | Fremgangsmaate til fremstilling av 2-amino-3-nitro-6-(4-fluor-benzylamino)-pyridin samt 2-amino-3-karbetoksyamino-6-(4-fluor-benzylamino)-pyridin. |
-
1985
- 1985-12-17 FI FI855016A patent/FI855016A7/fi not_active IP Right Cessation
- 1985-12-20 DK DK596785A patent/DK596785A/da not_active Application Discontinuation
- 1985-12-20 DE DE19853545201 patent/DE3545201A1/de not_active Withdrawn
- 1985-12-20 ZA ZA859770A patent/ZA859770B/xx unknown
- 1985-12-20 EP EP85116358A patent/EP0207193A2/fr not_active Withdrawn
-
1986
- 1986-01-02 DD DD86285896A patent/DD242349A5/de unknown
- 1986-01-06 HU HU8633A patent/HU193845B/hu unknown
- 1986-01-16 PT PT81848A patent/PT81848B/pt not_active IP Right Cessation
- 1986-01-17 GR GR860120A patent/GR860120B/el unknown
- 1986-01-21 AU AU52548/86A patent/AU570582B2/en not_active Expired - Fee Related
- 1986-01-24 JP JP61012242A patent/JPS624229A/ja active Pending
- 1986-02-03 ES ES551584A patent/ES8702142A1/es not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| FI855016L (fi) | 1986-12-29 |
| FI855016A7 (fi) | 1986-12-29 |
| DE3545201A1 (de) | 1987-01-02 |
| ES551584A0 (es) | 1986-12-16 |
| DK596785A (da) | 1986-12-29 |
| ES8702142A1 (es) | 1986-12-16 |
| EP0207193A2 (fr) | 1987-01-07 |
| GR860120B (en) | 1986-05-19 |
| HU193845B (en) | 1987-12-28 |
| JPS624229A (ja) | 1987-01-10 |
| ZA859770B (en) | 1986-08-27 |
| PT81848B (pt) | 1990-11-20 |
| PT81848A (de) | 1986-02-01 |
| AU570582B2 (en) | 1988-03-17 |
| AU5254886A (en) | 1987-01-08 |
| DK596785D0 (da) | 1985-12-20 |
| HUT40566A (en) | 1987-01-28 |
| FI855016A0 (fi) | 1985-12-17 |
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