JP2012528845A5 - - Google Patents

Info

Publication number

JP2012528845A5

JP2012528845A5 JP2012513685A JP2012513685A JP2012528845A5 JP 2012528845 A5 JP2012528845 A5 JP 2012528845A5 JP 2012513685 A JP2012513685 A JP 2012513685A JP 2012513685 A JP2012513685 A JP 2012513685A JP 2012528845 A5 JP2012528845 A5 JP 2012528845A5

Authority

JP

Japan

Prior art keywords

dosage form

form according

microparticles

eudragit

melt

Prior art date

2010-06-07

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
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• 239000002552 dosage form Substances 0.000 claims 20
• 239000003795 chemical substances by application Substances 0.000 claims 9
• 239000011859 microparticle Substances 0.000 claims 9
• 229940079593 drug Drugs 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 239000011159 matrix material Substances 0.000 claims 5
• 229920001577 copolymer Polymers 0.000 claims 4
• 239000010419 fine particle Substances 0.000 claims 4
• 239000000203 mixture Substances 0.000 claims 4
• 239000003402 opiate agonist Substances 0.000 claims 4
• NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 2
• 239000001856 Ethyl cellulose Substances 0.000 claims 2
• ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical group CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 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
• 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 2
• 229920001249 ethyl cellulose Polymers 0.000 claims 2
• 235000019325 ethyl cellulose Nutrition 0.000 claims 2
• OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 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
• 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 2
• GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims 2
• 229960002085 oxycodone Drugs 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 1
• QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
• JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims 1
• 229920003164 Eudragit® NE 40 D Polymers 0.000 claims 1
• 229920003155 Eudragit® RL 100 Polymers 0.000 claims 1
• 229920003156 Eudragit® RL PO Polymers 0.000 claims 1
• 229920003159 Eudragit® RS 100 Polymers 0.000 claims 1
• 229920003160 Eudragit® RS PO Polymers 0.000 claims 1
• 229920003134 Eudragit® polymer Polymers 0.000 claims 1
• 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
• 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 1
• 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 1
• 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
• 229920002125 Sokalan® Polymers 0.000 claims 1
• DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims 1
• 239000002253 acid Substances 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 239000002269 analeptic agent Substances 0.000 claims 1
• 230000003042 antagnostic effect Effects 0.000 claims 1
• 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 1
• 229960001736 buprenorphine Drugs 0.000 claims 1
• 229960001631 carbomer Drugs 0.000 claims 1
• 239000001913 cellulose Substances 0.000 claims 1
• 229920002678 cellulose Polymers 0.000 claims 1
• 229960004126 codeine Drugs 0.000 claims 1
• XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 1
• BYNVYIUJKRRNNC-UHFFFAOYSA-N docosanoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCCCCCCCC(O)=O BYNVYIUJKRRNNC-UHFFFAOYSA-N 0.000 claims 1
• 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 1
• 229960002428 fentanyl Drugs 0.000 claims 1
• 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 1
• 229960000240 hydrocodone Drugs 0.000 claims 1
• 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
• 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 239000000314 lubricant Substances 0.000 claims 1
• 239000000155 melt Substances 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 239000003607 modifier Substances 0.000 claims 1
• 229960005181 morphine Drugs 0.000 claims 1
• GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 claims 1
• 239000003401 opiate antagonist Substances 0.000 claims 1
• 229960005118 oxymorphone Drugs 0.000 claims 1
• PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims 1
• 239000004014 plasticizer Substances 0.000 claims 1
• 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 239000000932 sedative agent Substances 0.000 claims 1
• 230000001624 sedative effect Effects 0.000 claims 1
• 229960005126 tapentadol Drugs 0.000 claims 1
• KWTWDQCKEHXFFR-SMDDNHRTSA-N tapentadol Chemical compound CN(C)C[C@H](C)[C@@H](CC)C1=CC=CC(O)=C1 KWTWDQCKEHXFFR-SMDDNHRTSA-N 0.000 claims 1
• 229960004380 tramadol Drugs 0.000 claims 1
• 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 1
• 229940125725 tranquilizer Drugs 0.000 claims 1
• 239000003204 tranquilizing agent Substances 0.000 claims 1
• 230000002936 tranquilizing effect Effects 0.000 claims 1
• LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 1
• 239000001069 triethyl citrate Substances 0.000 claims 1
• VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims 1
• 235000013769 triethyl citrate Nutrition 0.000 claims 1
• 239000002966 varnish Substances 0.000 claims 1