JP2015514743A5 - - Google Patents

Info

Publication number

JP2015514743A5

JP2015514743A5 JP2015506317A JP2015506317A JP2015514743A5 JP 2015514743 A5 JP2015514743 A5 JP 2015514743A5 JP 2015506317 A JP2015506317 A JP 2015506317A JP 2015506317 A JP2015506317 A JP 2015506317A JP 2015514743 A5 JP2015514743 A5 JP 2015514743A5

Authority

JP

Japan

Prior art keywords

buprenorphine

pharmaceutical composition

opioid

formulated

composition according

Prior art date

2013-04-17

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims 28
• 229960001736 buprenorphine Drugs 0.000 claims 28
• 239000008194 pharmaceutical composition Substances 0.000 claims 24
• 230000002411 adverse Effects 0.000 claims 8
• 230000003285 pharmacodynamic effect Effects 0.000 claims 8
• 238000013270 controlled release Methods 0.000 claims 6
• BQNSLJQRJAJITR-UHFFFAOYSA-N 1,1,2-trichloro-1,2-difluoroethane Chemical compound FC(Cl)C(F)(Cl)Cl BQNSLJQRJAJITR-UHFFFAOYSA-N 0.000 claims 5
• OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims 5
• 229960003617 oxycodone hydrochloride Drugs 0.000 claims 5
• OROGSEYTTFOCAN-DNJOTXNNSA-N codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims 4
• BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims 4
• 239000008184 oral solid dosage form Substances 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• 208000019901 Anxiety disease Diseases 0.000 claims 3
• 230000036592 analgesia Effects 0.000 claims 3
• 230000036506 anxiety Effects 0.000 claims 3
• XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 3
• LLPOLZWFYMWNKH-CMKMFDCUSA-N hydrocodone Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)CC(=O)[C@@H]1OC1=C2C3=CC=C1OC LLPOLZWFYMWNKH-CMKMFDCUSA-N 0.000 claims 3
• 229960000240 hydrocodone Drugs 0.000 claims 3
• 239000012729 immediate-release (IR) formulation Substances 0.000 claims 3
• LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 3
• GTPHQORJKFJIRB-JTQLPTLWSA-N (2s)-2-amino-n-[(2r)-1-[[(2s)-1-[[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-3-(4-hydroxyphenyl)propanamide Chemical compound C([C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](CC=1C=CC(F)=CC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)C1=CC=C(O)C=C1 GTPHQORJKFJIRB-JTQLPTLWSA-N 0.000 claims 2
• TVYLLZQTGLZFBW-ZBFHGGJFSA-N (R,R)-tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 claims 2
• 206010011224 Cough Diseases 0.000 claims 2
• 206010012735 Diarrhoea Diseases 0.000 claims 2
• 208000014540 Functional gastrointestinal disease Diseases 0.000 claims 2
• 208000004454 Hyperalgesia Diseases 0.000 claims 2
• BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims 2
• UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims 2
• 230000000202 analgesic effect Effects 0.000 claims 2
• 201000007637 bowel dysfunction Diseases 0.000 claims 2
• 229960004126 codeine Drugs 0.000 claims 2
• 229960002428 fentanyl Drugs 0.000 claims 2
• PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 claims 2
• 229950001535 frakefamide Drugs 0.000 claims 2
• 108010028490 frakefamide Proteins 0.000 claims 2
• WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical compound O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 claims 2
• 229960001410 hydromorphone Drugs 0.000 claims 2
• 229960005181 morphine Drugs 0.000 claims 2
• 229960002085 oxycodone Drugs 0.000 claims 2
• 229960005118 oxymorphone Drugs 0.000 claims 2
• 229960004380 tramadol Drugs 0.000 claims 2
• TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 claims 2
• PPKXEPBICJTCRU-XMZRARIVSA-N (R,R)-tramadol hydrochloride Chemical compound Cl.COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 PPKXEPBICJTCRU-XMZRARIVSA-N 0.000 claims 1
• DYUTXEVRMPFGTH-UHFFFAOYSA-N 4-(2,5-dimethylphenyl)-5-methyl-1,3-thiazol-2-amine Chemical compound S1C(N)=NC(C=2C(=CC=C(C)C=2)C)=C1C DYUTXEVRMPFGTH-UHFFFAOYSA-N 0.000 claims 1
• 206010000060 Abdominal distension Diseases 0.000 claims 1
• 206010010774 Constipation Diseases 0.000 claims 1
• 206010012218 Delirium Diseases 0.000 claims 1
• 206010019233 Headaches Diseases 0.000 claims 1
• 208000035154 Hyperesthesia Diseases 0.000 claims 1
• 208000001953 Hypotension Diseases 0.000 claims 1
• 206010027646 Miosis Diseases 0.000 claims 1
• 208000007101 Muscle Cramp Diseases 0.000 claims 1
• 206010028813 Nausea Diseases 0.000 claims 1
• BCGJBQBWUGVESK-KCTCKCTRSA-N Oxymorphone hydrochloride Chemical compound Cl.O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BCGJBQBWUGVESK-KCTCKCTRSA-N 0.000 claims 1
• 208000002193 Pain Diseases 0.000 claims 1
• 208000003251 Pruritus Diseases 0.000 claims 1
• 208000004756 Respiratory Insufficiency Diseases 0.000 claims 1
• 206010038678 Respiratory depression Diseases 0.000 claims 1
• 206010039897 Sedation Diseases 0.000 claims 1
• 208000032140 Sleepiness Diseases 0.000 claims 1
• 206010041349 Somnolence Diseases 0.000 claims 1
• 208000005392 Spasm Diseases 0.000 claims 1
• 206010046555 Urinary retention Diseases 0.000 claims 1
• 208000024780 Urticaria Diseases 0.000 claims 1
• 206010047700 Vomiting Diseases 0.000 claims 1
• 230000003187 abdominal effect Effects 0.000 claims 1
• 206010053552 allodynia Diseases 0.000 claims 1
• 206010003549 asthenia Diseases 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 208000024330 bloating Diseases 0.000 claims 1
• 239000002775 capsule Substances 0.000 claims 1
• 208000002173 dizziness Diseases 0.000 claims 1
• 230000004064 dysfunction Effects 0.000 claims 1
• 230000002496 gastric effect Effects 0.000 claims 1
• 230000030136 gastric emptying Effects 0.000 claims 1
• 231100000869 headache Toxicity 0.000 claims 1
• 229960002738 hydromorphone hydrochloride Drugs 0.000 claims 1
• 230000036543 hypotension Effects 0.000 claims 1
• 230000000968 intestinal effect Effects 0.000 claims 1
• 238000007918 intramuscular administration Methods 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• RDOIQAHITMMDAJ-UHFFFAOYSA-N loperamide Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 RDOIQAHITMMDAJ-UHFFFAOYSA-N 0.000 claims 1
• 229960001571 loperamide Drugs 0.000 claims 1
• 230000003547 miosis Effects 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 210000004877 mucosa Anatomy 0.000 claims 1
• 230000008693 nausea Effects 0.000 claims 1
• 210000005036 nerve Anatomy 0.000 claims 1
• 229940005483 opioid analgesics Drugs 0.000 claims 1
• 239000006186 oral dosage form Substances 0.000 claims 1
• 229960005374 oxymorphone hydrochloride Drugs 0.000 claims 1
• 230000036407 pain Effects 0.000 claims 1
• 230000036280 sedation Effects 0.000 claims 1
• 239000007787 solid Substances 0.000 claims 1
• 239000012453 solvate Substances 0.000 claims 1
• 238000007920 subcutaneous administration Methods 0.000 claims 1
• 210000004243 sweat Anatomy 0.000 claims 1
• 230000001225 therapeutic effect Effects 0.000 claims 1
• 230000035922 thirst Effects 0.000 claims 1
• 229960003107 tramadol hydrochloride Drugs 0.000 claims 1
• 230000008673 vomiting Effects 0.000 claims 1