DK200800075A - Krystallinsk base af escitalopram og orodispergerbare tabletter indeholdende escitaloprambase - Google Patents
Krystallinsk base af escitalopram og orodispergerbare tabletter indeholdende escitaloprambase Download PDFInfo
- Publication number
- DK200800075A DK200800075A DK200800075A DKPA200800075A DK200800075A DK 200800075 A DK200800075 A DK 200800075A DK 200800075 A DK200800075 A DK 200800075A DK PA200800075 A DKPA200800075 A DK PA200800075A DK 200800075 A DK200800075 A DK 200800075A
- Authority
- DK
- Denmark
- Prior art keywords
- escitalopram
- free base
- salt
- crystalline
- base
- Prior art date
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- WSEQXVZVJXJVFP-FQEVSTJZSA-N escitalopram Chemical compound C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-FQEVSTJZSA-N 0.000 title claims 37
- 229960004341 escitalopram Drugs 0.000 title claims 36
- 238000000034 method Methods 0.000 claims 18
- 239000012458 free base Substances 0.000 claims 15
- 238000002844 melting Methods 0.000 claims 11
- 230000008018 melting Effects 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 239000008186 active pharmaceutical agent Substances 0.000 claims 7
- 239000000945 filler Substances 0.000 claims 7
- 239000012535 impurity Substances 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 239000002585 base Substances 0.000 claims 5
- WIHMBLDNRMIGDW-BDQAORGHSA-N escitalopram hydrobromide Chemical compound Br.C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WIHMBLDNRMIGDW-BDQAORGHSA-N 0.000 claims 5
- 150000003891 oxalate salts Chemical class 0.000 claims 5
- WSEQXVZVJXJVFP-HXUWFJFHSA-N (R)-citalopram Chemical compound C1([C@@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-HXUWFJFHSA-N 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000002904 solvent Substances 0.000 claims 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 3
- 239000007884 disintegrant Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 239000007787 solid Substances 0.000 claims 3
- KTGRHKOEFSJQNS-BDQAORGHSA-N (1s)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3h-2-benzofuran-5-carbonitrile;oxalic acid Chemical compound OC(=O)C(O)=O.C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 KTGRHKOEFSJQNS-BDQAORGHSA-N 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- AUZONCFQVSMFAP-UHFFFAOYSA-N disulfiram Chemical compound CCN(CC)C(=S)SSC(=S)N(CC)CC AUZONCFQVSMFAP-UHFFFAOYSA-N 0.000 claims 2
- 229960005086 escitalopram oxalate Drugs 0.000 claims 2
- 238000002156 mixing Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000002674 ointment Substances 0.000 claims 2
- 239000005426 pharmaceutical component Substances 0.000 claims 2
- 238000000746 purification Methods 0.000 claims 2
- 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 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- HSRJKNPTNIJEKV-UHFFFAOYSA-N Guaifenesin Chemical compound COC1=CC=CC=C1OCC(O)CO HSRJKNPTNIJEKV-UHFFFAOYSA-N 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- GQYIWUVLTXOXAJ-UHFFFAOYSA-N Lomustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- RGCVKNLCSQQDEP-UHFFFAOYSA-N Perphenazine Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 RGCVKNLCSQQDEP-UHFFFAOYSA-N 0.000 claims 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 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 229960004587 carisoprodol Drugs 0.000 claims 1
- OFZCIYFFPZCNJE-UHFFFAOYSA-N carisoprodol Chemical compound NC(=O)OCC(C)(CCC)COC(=O)NC(C)C OFZCIYFFPZCNJE-UHFFFAOYSA-N 0.000 claims 1
- 229960004630 chlorambucil Drugs 0.000 claims 1
- JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 150000002016 disaccharides Chemical class 0.000 claims 1
- 229960002563 disulfiram Drugs 0.000 claims 1
- 229960002767 ethosuximide Drugs 0.000 claims 1
- HAPOVYFOVVWLRS-UHFFFAOYSA-N ethosuximide Chemical compound CCC1(C)CC(=O)NC1=O HAPOVYFOVVWLRS-UHFFFAOYSA-N 0.000 claims 1
- 229960002297 fenofibrate Drugs 0.000 claims 1
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 150000004676 glycans Chemical class 0.000 claims 1
- 229960002146 guaifenesin Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 229960002247 lomustine Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 150000002772 monosaccharides Chemical group 0.000 claims 1
- 229960000762 perphenazine Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001282 polysaccharide Polymers 0.000 claims 1
- 239000005017 polysaccharide Substances 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229940069328 povidone Drugs 0.000 claims 1
- 238000003825 pressing Methods 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 150000005846 sugar alcohols Chemical class 0.000 claims 1
- 229960004453 trimethadione Drugs 0.000 claims 1
- IRYJRGCIQBGHIV-UHFFFAOYSA-N trimethadione Chemical compound CN1C(=O)OC(C)(C)C1=O IRYJRGCIQBGHIV-UHFFFAOYSA-N 0.000 claims 1
Classifications
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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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B63/00—Purification; Separation; Stabilisation; Use of additives
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Furan Compounds (AREA)
Claims (34)
1. Escitalopram fri base i fast form.
2. Escitalopram fri base ifølge krav 1,kendetegnet ved, at den omfatter krystallinsk escitalopram.
3. Escitalopram fri base ifølge krav 2, kendetegnet ved, at den er mindst 90 % krystallinsk, navnlig mindst 95 % krystallinsk og nærmere bestemt mindst 98. krystallinsk.
4. Escitalopram fri base ifølge krav 1, kendetegnet ved, at den er krystallinsk.
5. Farmaceutisk sammensætning, der indeholder escitalopram fri base ifølge kravene 1 til 4.
6. Fremgangsmåde til fremstilling af escitalopram fri base eller et salt deraf, kendetegnet ved, at escitalopramhydrobromid udfældes i krystallinsk form fra et opløsningsmiddel og separeres fra opløsningsmidlet, eventuelt omkrystalliseres én eller flere gange og derefter omdannes til escitalopram fri base eller et salt deraf, forudsat, at det fremstillede escitalopram-salt ikke er hydrobromidet.
7. Fremgangsmåde ifølge krav 6 til fremstilling af escitalopram fri base eller et salt deraf, kendetegnet ved, at escitalopramhydrobromidet udfældes fra et råt escitalopram.
8. Fremgangsmåde ifølge krav 6 eller 7 til fremstilling af escitalopram fri base eller et salt deraf, kendetegnet ved, at én eller flere urenheder med formlerne (II) eller (III)
hvor Z er halogen, cyano eller -CONHz, R1 og R2 uafhængigt er hydrogen eller methyl, forudsat, at hvis både R1 og R2 er methyl, så kan Z ikke være cyano, og bindingen, som er tegnet som en siksaklinje i formlen (III), angiver, at konfigurationen omkring dobbeltbindingen kan være E- eller Z-; fjernes fra eller reduceres i escitalopramet ved fremgangsmåden.
9. Fremgangsmåde ifølge krav 8, hvor urenhederne har formlen (II), hvor Z er brom eller chlor, og R1 og R2 begge er methyl, Z er -CONH2, og R1 og R2 begge er methyl, eller Z er cyano, R1 er hydrogen, og R2 er methyl; eller med formlen (III), hvor konfigurationen omkring dobbeltbindingen erZ.
10. Fremgangsmåde ifølge et hvilket som helst af kravene 7 til 9, hvor det rå escitalopram underkastes en indledende oprensning, før escitalopramhydrobromidet udfældes i krystallinsk form.
11. Fremgangsmåde ifølge et hvilket som helst af kravene 6 til 10, kendetegnet ved, at escitalopramhydrobromidet omdannes til escitalopram fri base eller escitalopram-oxalat.
12. Krystallinsk base af escitalopram eller et oxalatsalt af escitalopram, kendetegnet ved, at den(det) indeholder mindre end 0,20% urenheder bortset fra R-citalopram, navnlig mindre end 0,10 %.
13. Krystallinsk base eller oxalatsalt ifølge krav 12, kendetegnet ved, at den(det) indeholder mindre end 0,10% af en hvilken som helst særskilt urenhed bortset fra R-citalopram.
14. Krystallinsk base af escitalopram eller et oxalatsalt af escitalopram fremstillet ved fremgangsmåden ifølge et hvilket som helst af kravene 6-11.
15. Base eller oxalatsalt ifølge krav 14, kendetegnet ved, at den(det) indeholder mindre end 0,20 % urenheder bortset fra R-citalopram, navnlig mindre end 0,10 %.
16. Krystallinsk base eller oxalatsalt ifølge krav 15, kendetegnet ved, at den(det) indeholder mindre end 0,10 % af en hvilken som helst særskilt urenhed bortset fra R-citalopram.
17. Fremgangsmåde til fremstilling af et salt af escitalopram, kendetegnet ved, at escitalopram fri base udfældes i fast form fra et opløsningsmiddel og separeres fra opløsningsmidlet, eventuelt omkrystalliseres én eller flere gange og derefter omdannes til et salt af escitalopram.
18. Fremgangsmåde ifølge krav 17 til fremstilling af et salt af escitalopram, kendetegnet ved, at escitalopram fri base udfældes fra et råt escitalopram.
19. Fremgangsmåde ifølge krav 17 eller 18 til fremstilling af et salt af escitalopram, kendetegnet ved, at en urenhed med formlen (li)
hvor Z er cyano, R1 er methyl, og R2 er hydrogen, fjernes fra eller reduceres i escitalopramet ved fremgangsmåden.
20. Fremgangsmåde ifølge krav 19, hvor Z er brom.
21. Fremgangsmåde ifølge et hvilket som helst af kravene 18 til 20, hvor det rå escitalopram underkastes indledende oprensning, før escitalopramhydrobromidet udfældes i krystallinsk form.
22. Fremgangsmåde ifølge et hvilket som helst af kravene 18 til 21, kendetegnet ved, at escitalopram fri base omdannes til escitalopram-oxalat.
23. Fremgangsmåde til reduktion af mængden af escitalopram, W-oxid i escitalopram fri base eller et salt deraf, hvilken fremgangsmåde omfatter opløsning af escitalopram fri base i diethylether og fjernelse af escitalopram, W-oxid som et fast materiale.
24. Smeltetablet, der har en hårdhed på mindst 22 N og en oral desintegrationstid på mindre end 120 s, og som omfatter en aktiv farmaceutisk bestanddel adsorberet på et vandopløseligt fyldstof, ét eller flere desintegrationsmidler og eventuelt yderligere vandopløseligt fyldstof, hvor den aktive farmaceutiske bestanddel har et smeltepunkt i området 40-100 °C.
25. Smeltetablet ifølge krav 23, kendetegnet ved, at den aktive farmaceutiske bestanddel har et smeltepunkt i området 40-90 °C.
26. Smeltetablet ifølge krav 23 eller 24, kendetegnet ved, at den aktive farmaceutiske bestanddel er valgt fra gruppen bestående af escitalopram, ethosuximid, trimethadion, chlorambucil, disulfiram, fenofibrat, guaifenesin, lomustin, carisoprodol og perphenazin.
27. Smeltetablet ifølge krav 25, kendetegnet ved, at den aktive farmaceutiske bestanddel er escitalopram.
28. Smeltetablet ifølge et hvilket som helst af kravene 23-26, kendetegnet ved, at det vandopløselige fyldstof er valgt fra gruppen bestående af monosaccharider, disaccharider, sukkeralkoholer og polysaccharider.
29. Smeltetablet ifølge krav 27, k e n d e t e g n e t ved, at det vandopløselige fyldstof er valgt fra gruppen bestående af mannitol, sorbitol, glucose, mannose og lactose.
30. Smeltetablet ifølge et hvilket som helst af kravene 23-28, kendetegnet ved, at den har en hårdhed på mindst 22 N.
31. Smeltetablet ifølge et hvilket som helst af kravene 23-29, kendetegnet ved, at den har en oral desintegrationstid på mindre end 60 s.
32. Smeltetablet ifølge et hvilket som helst af kravene 23-30, kendetegnet ved, at desintegrationsmidlerne er valgt fra gruppen bestående af mikrokrystallinsk cellulose, natriumstivelsesglycolat, croscarmellose-natrium, crospovidon og povidon.
33. Smeltetablet ifølge et hvilket som helst af kravene 23-31, kendetegnet ved, at den har en slidstyrke på ikke mere end 1 %.
34. Fremgangsmåde til fremstilling af en smeltetablet ifølge et hvilket som helst af kravene 23-32, der omfatter; a) blanding af det vandopløselige fyldstof og den aktive farmaceutiske bestanddel ved en temperatur over, omkring eller lidt under den aktive farmaceutiske bestanddels smeltepunkt, hvorved den aktive farmaceutiske bestanddel adsorberes på det vandopløselige fyldstof; b) efterfulgt af afkøling til en temperatur under 40 °C; c) blanding af blandingen af den aktive farmaceutiske bestanddel og det vandopløselige fyldstof med ét eller flere desintegrationsmidler og eventuelt andre hjælpestoffer og d) presning af blandingen til tabletter med en hårdhed på mindst 22 N.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK200800075A DK200800075A (da) | 2005-06-22 | 2008-01-21 | Krystallinsk base af escitalopram og orodispergerbare tabletter indeholdende escitaloprambase |
| DKPA200900284A DK200900284A (da) | 2005-06-22 | 2009-02-27 | Krystallinsk base af escitalopram og smeltetabletter indeholdende escitalopram base |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200500912 | 2005-06-22 | ||
| DK200500912 | 2005-06-22 | ||
| DK200800075 | 2008-01-21 | ||
| DK200800075A DK200800075A (da) | 2005-06-22 | 2008-01-21 | Krystallinsk base af escitalopram og orodispergerbare tabletter indeholdende escitaloprambase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK200800075A true DK200800075A (da) | 2008-03-15 |
Family
ID=37546630
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK06742481.2T DK1896439T4 (da) | 2005-06-22 | 2006-06-22 | Krystallinsk base af escitalopram og orodispergerbare tabletter, der omfatter escitaloprambase |
| DK200800075A DK200800075A (da) | 2005-06-22 | 2008-01-21 | Krystallinsk base af escitalopram og orodispergerbare tabletter indeholdende escitaloprambase |
| DKPA200900284A DK200900284A (da) | 2005-06-22 | 2009-02-27 | Krystallinsk base af escitalopram og smeltetabletter indeholdende escitalopram base |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK06742481.2T DK1896439T4 (da) | 2005-06-22 | 2006-06-22 | Krystallinsk base af escitalopram og orodispergerbare tabletter, der omfatter escitaloprambase |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
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| DKPA200900284A DK200900284A (da) | 2005-06-22 | 2009-02-27 | Krystallinsk base af escitalopram og smeltetabletter indeholdende escitalopram base |
Country Status (39)
| Country | Link |
|---|---|
| EP (3) | EP2325177A1 (da) |
| JP (5) | JP4906852B2 (da) |
| KR (5) | KR20110084341A (da) |
| CN (2) | CN101189220A (da) |
| AR (2) | AR055062A1 (da) |
| AT (3) | AT10983U1 (da) |
| AU (2) | AU2006261452B2 (da) |
| BG (1) | BG66086B1 (da) |
| BR (1) | BRPI0612295A2 (da) |
| CA (2) | CA2646780A1 (da) |
| CY (1) | CY1112392T1 (da) |
| CZ (3) | CZ299906B6 (da) |
| DE (2) | DE112006001619T5 (da) |
| DK (3) | DK1896439T4 (da) |
| EA (2) | EA201001108A1 (da) |
| EE (1) | EE00773U1 (da) |
| ES (2) | ES2356838T5 (da) |
| FI (2) | FI20077133A (da) |
| GB (2) | GB2442160B (da) |
| HR (1) | HRP20110093T4 (da) |
| HU (1) | HUP0800135A3 (da) |
| IL (1) | IL187454A0 (da) |
| IS (1) | IS8705A (da) |
| LT (1) | LT5550B (da) |
| LV (1) | LV13677B (da) |
| MX (1) | MX2007015328A (da) |
| MY (2) | MY143239A (da) |
| NO (2) | NO20080359L (da) |
| PL (2) | PL1896439T5 (da) |
| PT (1) | PT1896439E (da) |
| RS (1) | RS51575B2 (da) |
| SG (1) | SG169358A1 (da) |
| SI (1) | SI1896439T2 (da) |
| SK (1) | SK500402007A3 (da) |
| TR (2) | TR200708792T1 (da) |
| TW (2) | TWI347942B (da) |
| UA (1) | UA86536C2 (da) |
| WO (1) | WO2006136169A2 (da) |
| ZA (2) | ZA200711066B (da) |
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| GB0123400D0 (en) | 2001-09-28 | 2001-11-21 | Novartis Ag | Organic compounds |
| WO2008059514A2 (en) * | 2006-07-31 | 2008-05-22 | Cadila Healthcare Limited | Process for preparing escitalopram |
| EP2134325A2 (en) * | 2007-03-01 | 2009-12-23 | Aurobindo Pharma Limited | Stable solid dosage forms of an antidepressant |
| ME02391B (me) | 2010-07-23 | 2016-09-20 | H Lundbeck As | Postupak za prečišćavanje farmaceutski prihvatljivih soli escitaloprama |
| CN103360353A (zh) * | 2013-08-07 | 2013-10-23 | 中国药科大学 | 草酸艾司西酞普兰杂质的制备方法 |
| JP2018016569A (ja) * | 2016-07-26 | 2018-02-01 | 株式会社トクヤマ | （１ｓ）−１−［３−（ジメチルアミノ）プロピル］−１−（４−フルオロフェニル）−１，３−ジヒドロイソベンゾフラン−５−カルボニトリル蓚酸塩の製造方法 |
| WO2018190294A1 (ja) * | 2017-04-10 | 2018-10-18 | 東和薬品株式会社 | エスシタロプラム医薬組成物 |
| CN110711198B (zh) * | 2018-07-12 | 2022-03-15 | 山东大学 | D-甘露糖在制备抗抑郁药物中的应用 |
| KR102331187B1 (ko) | 2019-04-09 | 2021-11-26 | 주식회사 라이트팜텍 | 에스시탈로프람을 함유하는 안정성이 우수한 경구용 액제 조성물 및 그의 제조방법 |
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