CA2683692A1 - Pharmaceutical compositions - Google Patents

Info

Publication number

CA2683692A1

CA2683692A1 CA002683692A CA2683692A CA2683692A1 CA 2683692 A1 CA2683692 A1 CA 2683692A1 CA 002683692 A CA002683692 A CA 002683692A CA 2683692 A CA2683692 A CA 2683692A CA 2683692 A1 CA2683692 A1 CA 2683692A1

Authority

CA

Canada

Prior art keywords

trimipramine

composition

release

hours

component

Prior art date

2007-04-13

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.)

Abandoned

Links

• Espacenet
• Global Dossier
• CIPO
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 13
• ZSCDBOWYZJWBIY-UHFFFAOYSA-N trimipramine Chemical compound C1CC2=CC=CC=C2N(CC(CN(C)C)C)C2=CC=CC=C21 ZSCDBOWYZJWBIY-UHFFFAOYSA-N 0.000 claims abstract description 310
• 239000000203 mixture Substances 0.000 claims abstract description 308
• 229960002431 trimipramine Drugs 0.000 claims abstract description 307
• 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 34
• -1 clozepine Chemical compound 0.000 claims description 106
• 239000002552 dosage form Substances 0.000 claims description 97
• 238000000034 method Methods 0.000 claims description 60
• 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 38
• 238000013268 sustained release Methods 0.000 claims description 25
• 239000012730 sustained-release form Substances 0.000 claims description 25
• 238000011282 treatment Methods 0.000 claims description 23
• 238000004090 dissolution Methods 0.000 claims description 22
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 20
• 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 18
• 239000013543 active substance Substances 0.000 claims description 17
• 238000007922 dissolution test Methods 0.000 claims description 17
• 238000000338 in vitro Methods 0.000 claims description 16
• 238000013270 controlled release Methods 0.000 claims description 15
• 206010022437 insomnia Diseases 0.000 claims description 15
• 239000003814 drug Substances 0.000 claims description 13
• 238000004519 manufacturing process Methods 0.000 claims description 12
• QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 12
• 229940079593 drug Drugs 0.000 claims description 11
• 230000000926 neurological effect Effects 0.000 claims description 11
• 230000036470 plasma concentration Effects 0.000 claims description 11
• 238000001727 in vivo Methods 0.000 claims description 10
• 230000000694 effects Effects 0.000 claims description 9
• 238000010521 absorption reaction Methods 0.000 claims description 8
• 239000000935 antidepressant agent Substances 0.000 claims description 7
• 229940005513 antidepressants Drugs 0.000 claims description 7
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• 229940123445 Tricyclic antidepressant Drugs 0.000 claims description 6
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• 208000020401 Depressive disease Diseases 0.000 claims description 5
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• 239000000939 antiparkinson agent Substances 0.000 claims description 5
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• 206010003591 Ataxia Diseases 0.000 claims description 4
• 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 4
• 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 4
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• 206010012335 Dependence Diseases 0.000 claims description 4
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• 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 claims description 2
• SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 2
• YWPHCCPCQOJSGZ-LLVKDONJSA-N (2r)-2-[(2-ethoxyphenoxy)methyl]morpholine Chemical compound CCOC1=CC=CC=C1OC[C@@H]1OCCNC1 YWPHCCPCQOJSGZ-LLVKDONJSA-N 0.000 claims description 2
• DIWRORZWFLOCLC-HNNXBMFYSA-N (3s)-7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one Chemical compound N([C@H](C(NC1=CC=C(Cl)C=C11)=O)O)=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-HNNXBMFYSA-N 0.000 claims description 2
• RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 claims description 2
• ZEUITGRIYCTCEM-KRWDZBQOSA-N (S)-duloxetine Chemical compound C1([C@@H](OC=2C3=CC=CC=C3C=CC=2)CCNC)=CC=CS1 ZEUITGRIYCTCEM-KRWDZBQOSA-N 0.000 claims description 2
• WIHMBLDNRMIGDW-UHFFFAOYSA-N 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3h-2-benzofuran-5-carbonitrile;hydron;bromide Chemical compound [Br-].O1CC2=CC(C#N)=CC=C2C1(CCC[NH+](C)C)C1=CC=C(F)C=C1 WIHMBLDNRMIGDW-UHFFFAOYSA-N 0.000 claims description 2
• SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 2
• GLQPTZAAUROJMO-UHFFFAOYSA-N 4-(3,4-dimethoxyphenyl)benzaldehyde Chemical compound C1=C(OC)C(OC)=CC=C1C1=CC=C(C=O)C=C1 GLQPTZAAUROJMO-UHFFFAOYSA-N 0.000 claims description 2
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• 241000238097 Callinectes sapidus Species 0.000 claims description 2
• 208000022526 Canavan disease Diseases 0.000 claims description 2
• 208000019888 Circadian rhythm sleep disease Diseases 0.000 claims description 2
• GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 claims description 2
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• 206010018429 Glucose tolerance impaired Diseases 0.000 claims description 2
• GUTXTARXLVFHDK-UHFFFAOYSA-N Haloperidol decanoate Chemical compound C1CC(OC(=O)CCCCCCCCC)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 GUTXTARXLVFHDK-UHFFFAOYSA-N 0.000 claims description 2
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• WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 2
• WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 2
• WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 2
• 208000019693 Lung disease Diseases 0.000 claims description 2
• 206010025323 Lymphomas Diseases 0.000 claims description 2
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• 208000001132 Osteoporosis Diseases 0.000 claims description 2
• 208000002193 Pain Diseases 0.000 claims description 2
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• AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 claims description 2
• RMUCZJUITONUFY-UHFFFAOYSA-N Phenelzine Chemical compound NNCCC1=CC=CC=C1 RMUCZJUITONUFY-UHFFFAOYSA-N 0.000 claims description 2
• 206010036105 Polyneuropathy Diseases 0.000 claims description 2
• 208000001280 Prediabetic State Diseases 0.000 claims description 2
• 206010037779 Radiculopathy Diseases 0.000 claims description 2
• 206010039491 Sarcoma Diseases 0.000 claims description 2
• 206010069141 Septic encephalopathy Diseases 0.000 claims description 2
• 102100036325 Sterol 26-hydroxylase, mitochondrial Human genes 0.000 claims description 2
• 208000006011 Stroke Diseases 0.000 claims description 2
• 208000009205 Tinnitus Diseases 0.000 claims description 2
• 208000032109 Transient ischaemic attack Diseases 0.000 claims description 2
• 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
• 206010044688 Trisomy 21 Diseases 0.000 claims description 2
• 208000012886 Vertigo Diseases 0.000 claims description 2
• 229960004538 alprazolam Drugs 0.000 claims description 2
• VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 claims description 2
• 229960000836 amitriptyline Drugs 0.000 claims description 2
• KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 claims description 2
• 208000022531 anorexia Diseases 0.000 claims description 2
• 230000001078 anti-cholinergic effect Effects 0.000 claims description 2
• 239000002249 anxiolytic agent Substances 0.000 claims description 2
• 230000000949 anxiolytic effect Effects 0.000 claims description 2
• 229940005530 anxiolytics Drugs 0.000 claims description 2
• 230000006907 apoptotic process Effects 0.000 claims description 2
• 208000006673 asthma Diseases 0.000 claims description 2
• 150000001557 benzodiazepines Chemical class 0.000 claims description 2
• FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 claims description 2
• 229960000623 carbamazepine Drugs 0.000 claims description 2
• 206010007776 catatonia Diseases 0.000 claims description 2
• 230000030833 cell death Effects 0.000 claims description 2
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• 208000025434 cerebellar degeneration Diseases 0.000 claims description 2
• 230000002490 cerebral effect Effects 0.000 claims description 2
• 208000001088 cerebrotendinous xanthomatosis Diseases 0.000 claims description 2
• 229960004782 chlordiazepoxide Drugs 0.000 claims description 2
• ANTSCNMPPGJYLG-UHFFFAOYSA-N chlordiazepoxide Chemical compound O=N=1CC(NC)=NC2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 ANTSCNMPPGJYLG-UHFFFAOYSA-N 0.000 claims description 2
• ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 claims description 2
• 229960001076 chlorpromazine Drugs 0.000 claims description 2
• 229960004606 clomipramine Drugs 0.000 claims description 2
• 229960004362 clorazepate Drugs 0.000 claims description 2
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• 206010012601 diabetes mellitus Diseases 0.000 claims description 2
• 229960003529 diazepam Drugs 0.000 claims description 2
• AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 claims description 2
• 235000014632 disordered eating Nutrition 0.000 claims description 2
• 229940052760 dopamine agonists Drugs 0.000 claims description 2
• 239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 2
• 229960005426 doxepin Drugs 0.000 claims description 2
• ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 claims description 2
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• 229960004801 imipramine Drugs 0.000 claims description 2
• BCGWQEUPMDMJNV-UHFFFAOYSA-N imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 claims description 2
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• PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims description 2
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• QSLMDECMDJKHMQ-GSXCWMCISA-N maprotiline Chemical compound C12=CC=CC=C2[C@@]2(CCCNC)C3=CC=CC=C3[C@@H]1CC2 QSLMDECMDJKHMQ-GSXCWMCISA-N 0.000 claims description 2
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• KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 2
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• CTRLABGOLIVAIY-UHFFFAOYSA-N oxcarbazepine Chemical compound C1C(=O)C2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 CTRLABGOLIVAIY-UHFFFAOYSA-N 0.000 claims description 2
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