JP2010511683A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010511683A5 JP2010511683A5 JP2009539799A JP2009539799A JP2010511683A5 JP 2010511683 A5 JP2010511683 A5 JP 2010511683A5 JP 2009539799 A JP2009539799 A JP 2009539799A JP 2009539799 A JP2009539799 A JP 2009539799A JP 2010511683 A5 JP2010511683 A5 JP 2010511683A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- opioid
- opioid analgesic
- particles
- weight
- Prior art date
- 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
- 239000000203 mixture Substances 0.000 claims 49
- 239000002245 particle Substances 0.000 claims 17
- 239000000014 opioid analgesic Substances 0.000 claims 12
- 239000003401 opiate antagonist Substances 0.000 claims 6
- 235000002639 sodium chloride Nutrition 0.000 claims 6
- 208000002193 Pain Diseases 0.000 claims 5
- 230000035587 bioadhesion Effects 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 5
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 5
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 229920002472 Starch Polymers 0.000 claims 4
- 229960002428 fentanyl Drugs 0.000 claims 4
- 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 4
- 238000000034 method Methods 0.000 claims 4
- 239000008107 starch Substances 0.000 claims 4
- 235000019698 starch Nutrition 0.000 claims 4
- 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 3
- 239000007884 disintegrant Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- -1 methopone Chemical compound 0.000 claims 3
- FEBUJFMRSBAMES-UHFFFAOYSA-N 2-[(2-{[3,5-dihydroxy-2-(hydroxymethyl)-6-phosphanyloxan-4-yl]oxy}-3,5-dihydroxy-6-({[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}methyl)oxan-4-yl)oxy]-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl phosphinite Chemical compound OC1C(O)C(O)C(CO)OC1OCC1C(O)C(OC2C(C(OP)C(O)C(CO)O2)O)C(O)C(OC2C(C(CO)OC(P)C2O)O)O1 FEBUJFMRSBAMES-UHFFFAOYSA-N 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 2
- 229920001661 Chitosan Polymers 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- 229920002907 Guar gum Polymers 0.000 claims 2
- 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 2
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 claims 2
- 229920000881 Modified starch Polymers 0.000 claims 2
- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical group C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 claims 2
- ONBWJWYUHXVEJS-ZTYRTETDSA-N Normorphine Chemical compound C([C@@H](NCC1)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 ONBWJWYUHXVEJS-ZTYRTETDSA-N 0.000 claims 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
- ZTVQQQVZCWLTDF-UHFFFAOYSA-N Remifentanil Chemical compound C1CN(CCC(=O)OC)CCC1(C(=O)OC)N(C(=O)CC)C1=CC=CC=C1 ZTVQQQVZCWLTDF-UHFFFAOYSA-N 0.000 claims 2
- 229920002305 Schizophyllan Polymers 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- 229960001391 alfentanil Drugs 0.000 claims 2
- TZCXTZWJZNENPQ-UHFFFAOYSA-L barium sulfate Chemical compound [Ba+2].[O-]S([O-])(=O)=O TZCXTZWJZNENPQ-UHFFFAOYSA-L 0.000 claims 2
- 239000000227 bioadhesive Substances 0.000 claims 2
- 229960001736 buprenorphine Drugs 0.000 claims 2
- 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 2
- 239000001506 calcium phosphate Substances 0.000 claims 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- 229920002678 cellulose Polymers 0.000 claims 2
- 239000001913 cellulose Substances 0.000 claims 2
- 235000010980 cellulose Nutrition 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
- 229960004193 dextropropoxyphene Drugs 0.000 claims 2
- XLMALTXPSGQGBX-GCJKJVERSA-N dextropropoxyphene Chemical compound C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 XLMALTXPSGQGBX-GCJKJVERSA-N 0.000 claims 2
- 229960000920 dihydrocodeine Drugs 0.000 claims 2
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 claims 2
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000000665 guar gum Substances 0.000 claims 2
- 235000010417 guar gum Nutrition 0.000 claims 2
- 229960002154 guar gum Drugs 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
- 239000008101 lactose Substances 0.000 claims 2
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical compound COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 claims 2
- 239000011859 microparticle Substances 0.000 claims 2
- 235000019426 modified starch Nutrition 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
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims 2
- 229960004127 naloxone Drugs 0.000 claims 2
- 229950006134 normorphine Drugs 0.000 claims 2
- 229960000482 pethidine Drugs 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 229960003394 remifentanil Drugs 0.000 claims 2
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical compound C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 claims 2
- 229960004739 sufentanil Drugs 0.000 claims 2
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 2
- 239000000230 xanthan gum Substances 0.000 claims 2
- 235000010493 xanthan gum Nutrition 0.000 claims 2
- 229920001285 xanthan gum Polymers 0.000 claims 2
- 229940082509 xanthan gum Drugs 0.000 claims 2
- YQYVFVRQLZMJKJ-JBBXEZCESA-N (+)-cyclazocine Chemical compound C([C@@]1(C)C2=CC(O)=CC=C2C[C@@H]2[C@@H]1C)CN2CC1CC1 YQYVFVRQLZMJKJ-JBBXEZCESA-N 0.000 claims 1
- JVLBPIPGETUEET-WIXLDOGYSA-O (3r,4r,4as,7ar,12bs)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1h-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one Chemical compound C([N@+]1(C)[C@@H]2CC=3C4=C(C(=CC=3)O)O[C@@H]3[C@]4([C@@]2(O)CCC3=O)CC1)C1CC1 JVLBPIPGETUEET-WIXLDOGYSA-O 0.000 claims 1
- 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
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- LLSKXGRDUPMXLC-UHFFFAOYSA-N 1-phenylpiperidine Chemical compound C1CCCCN1C1=CC=CC=C1 LLSKXGRDUPMXLC-UHFFFAOYSA-N 0.000 claims 1
- KISZTEOELCMZPY-UHFFFAOYSA-N 3,3-diphenylpropylamine Chemical class C=1C=CC=CC=1C(CCN)C1=CC=CC=C1 KISZTEOELCMZPY-UHFFFAOYSA-N 0.000 claims 1
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 1
- 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
- 208000000003 Breakthrough pain Diseases 0.000 claims 1
- 238000005698 Diels-Alder reaction Methods 0.000 claims 1
- 229920000896 Ethulose Polymers 0.000 claims 1
- 239000001859 Ethyl hydroxyethyl cellulose Substances 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- ALFGKMXHOUSVAD-UHFFFAOYSA-N Ketobemidone Chemical compound C=1C=CC(O)=CC=1C1(C(=O)CC)CCN(C)CC1 ALFGKMXHOUSVAD-UHFFFAOYSA-N 0.000 claims 1
- MKXZASYAUGDDCJ-SZMVWBNQSA-N LSM-2525 Chemical compound C1CCC[C@H]2[C@@]3([H])N(C)CC[C@]21C1=CC(OC)=CC=C1C3 MKXZASYAUGDDCJ-SZMVWBNQSA-N 0.000 claims 1
- UXBPQRGCVJOTNT-COBSGTNCSA-N Levomethadyl acetate hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(C[C@H](C)N(C)C)([C@@H](OC(C)=O)CC)C1=CC=CC=C1 UXBPQRGCVJOTNT-COBSGTNCSA-N 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 239000004368 Modified starch Substances 0.000 claims 1
- WJBLNOPPDWQMCH-MBPVOVBZSA-N Nalmefene Chemical group N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=C)O)CC1)O)CC1CC1 WJBLNOPPDWQMCH-MBPVOVBZSA-N 0.000 claims 1
- 239000008896 Opium Substances 0.000 claims 1
- 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 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
- 229920002125 Sokalan® Polymers 0.000 claims 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 229960002512 anileridine Drugs 0.000 claims 1
- LKYQLAWMNBFNJT-UHFFFAOYSA-N anileridine Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC1=CC=C(N)C=C1 LKYQLAWMNBFNJT-UHFFFAOYSA-N 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 229940092690 barium sulfate Drugs 0.000 claims 1
- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical compound N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims 1
- 229960001113 butorphanol Drugs 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 229960003563 calcium carbonate Drugs 0.000 claims 1
- XAAHAAMILDNBPS-UHFFFAOYSA-L calcium hydrogenphosphate dihydrate Chemical compound O.O.[Ca+2].OP([O-])([O-])=O XAAHAAMILDNBPS-UHFFFAOYSA-L 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- HUSUHZRVLBSGBO-UHFFFAOYSA-L calcium;dihydrogen phosphate;hydroxide Chemical compound O.[Ca+2].OP([O-])([O-])=O HUSUHZRVLBSGBO-UHFFFAOYSA-L 0.000 claims 1
- 235000014633 carbohydrates Nutrition 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 229960001631 carbomer Drugs 0.000 claims 1
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 229940105329 carboxymethylcellulose Drugs 0.000 claims 1
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims 1
- 229960004126 codeine Drugs 0.000 claims 1
- 229920001577 copolymer Polymers 0.000 claims 1
- 229960005168 croscarmellose Drugs 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 229950002213 cyclazocine Drugs 0.000 claims 1
- NLBUEDSBXVNAPB-DFQSSKMNSA-N cyclorphan Chemical compound C([C@]12CCCC[C@H]1[C@H]1CC3=CC=C(C=C32)O)CN1CC1CC1 NLBUEDSBXVNAPB-DFQSSKMNSA-N 0.000 claims 1
- WDEFBBTXULIOBB-WBVHZDCISA-N dextilidine Chemical compound C=1C=CC=CC=1[C@@]1(C(=O)OCC)CCC=C[C@H]1N(C)C WDEFBBTXULIOBB-WBVHZDCISA-N 0.000 claims 1
- 229960001985 dextromethorphan Drugs 0.000 claims 1
- INUNXTSAACVKJS-OAQYLSRUSA-N dextromoramide Chemical compound C([C@@H](C)C(C(=O)N1CCCC1)(C=1C=CC=CC=1)C=1C=CC=CC=1)N1CCOCC1 INUNXTSAACVKJS-OAQYLSRUSA-N 0.000 claims 1
- 229960003701 dextromoramide Drugs 0.000 claims 1
- 229960003461 dezocine Drugs 0.000 claims 1
- VTMVHDZWSFQSQP-VBNZEHGJSA-N dezocine Chemical compound C1CCCC[C@H]2CC3=CC=C(O)C=C3[C@]1(C)[C@H]2N VTMVHDZWSFQSQP-VBNZEHGJSA-N 0.000 claims 1
- 229960002069 diamorphine Drugs 0.000 claims 1
- 229960004192 diphenoxylate Drugs 0.000 claims 1
- HYPPXZBJBPSRLK-UHFFFAOYSA-N diphenoxylate Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 HYPPXZBJBPSRLK-UHFFFAOYSA-N 0.000 claims 1
- 238000007908 dry granulation Methods 0.000 claims 1
- 238000007580 dry-mixing Methods 0.000 claims 1
- 235000019326 ethyl hydroxyethyl cellulose Nutrition 0.000 claims 1
- 229950004155 etorphine Drugs 0.000 claims 1
- CAHCBJPUTCKATP-FAWZKKEFSA-N etorphine Chemical compound O([C@H]1[C@@]2(OC)C=C[C@@]34C[C@@H]2[C@](C)(O)CCC)C2=C5[C@]41CCN(C)[C@@H]3CC5=CC=C2O CAHCBJPUTCKATP-FAWZKKEFSA-N 0.000 claims 1
- 239000004744 fabric Substances 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 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
- 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 1
- 229960001410 hydromorphone Drugs 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- 229950009272 isomethadone Drugs 0.000 claims 1
- IFKPLJWIEQBPGG-UHFFFAOYSA-N isomethadone Chemical compound C=1C=CC=CC=1C(C(C)CN(C)C)(C(=O)CC)C1=CC=CC=C1 IFKPLJWIEQBPGG-UHFFFAOYSA-N 0.000 claims 1
- 229960003029 ketobemidone Drugs 0.000 claims 1
- 229940018399 levomethadyl acetate hydrochloride Drugs 0.000 claims 1
- 229960003406 levorphanol Drugs 0.000 claims 1
- 229960001571 loperamide Drugs 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
- FQXXSQDCDRQNQE-UHFFFAOYSA-N markiertes Thebain Natural products COC1=CC=C2C(N(CC3)C)CC4=CC=C(OC)C5=C4C23C1O5 FQXXSQDCDRQNQE-UHFFFAOYSA-N 0.000 claims 1
- 229960001797 methadone Drugs 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 229960002921 methylnaltrexone Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- INAXVFBXDYWQFN-XHSDSOJGSA-N morphinan Chemical class C1C2=CC=CC=C2[C@]23CCCC[C@H]3[C@@H]1NCC2 INAXVFBXDYWQFN-XHSDSOJGSA-N 0.000 claims 1
- 229960005181 morphine Drugs 0.000 claims 1
- 239000003612 morphinomimetic agent Substances 0.000 claims 1
- 238000000465 moulding Methods 0.000 claims 1
- 229960000805 nalbuphine Drugs 0.000 claims 1
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims 1
- 229960005297 nalmefene Drugs 0.000 claims 1
- 229960003086 naltrexone Drugs 0.000 claims 1
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims 1
- 229920005615 natural polymer Polymers 0.000 claims 1
- 229960004300 nicomorphine Drugs 0.000 claims 1
- HNDXBGYRMHRUFN-CIVUWBIHSA-N nicomorphine Chemical compound O([C@H]1C=C[C@H]2[C@H]3CC=4C5=C(C(=CC=4)OC(=O)C=4C=NC=CC=4)O[C@@H]1[C@]52CCN3C)C(=O)C1=CC=CN=C1 HNDXBGYRMHRUFN-CIVUWBIHSA-N 0.000 claims 1
- 229940127240 opiate Drugs 0.000 claims 1
- 229960001027 opium Drugs 0.000 claims 1
- 229960002085 oxycodone Drugs 0.000 claims 1
- 229960005118 oxymorphone Drugs 0.000 claims 1
- 229920001277 pectin Polymers 0.000 claims 1
- 239000001814 pectin Substances 0.000 claims 1
- 235000010987 pectin Nutrition 0.000 claims 1
- VOKSWYLNZZRQPF-GDIGMMSISA-N pentazocine Chemical compound C1C2=CC=C(O)C=C2[C@@]2(C)[C@@H](C)[C@@H]1N(CC=C(C)C)CC2 VOKSWYLNZZRQPF-GDIGMMSISA-N 0.000 claims 1
- 229960005301 pentazocine Drugs 0.000 claims 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229920000058 polyacrylate Polymers 0.000 claims 1
- 229950011009 racemorphan Drugs 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 235000015424 sodium Nutrition 0.000 claims 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
- 239000000661 sodium alginate Substances 0.000 claims 1
- 229940005550 sodium alginate Drugs 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 235000000346 sugar Nutrition 0.000 claims 1
- 229930003945 thebaine Natural products 0.000 claims 1
- FQXXSQDCDRQNQE-VMDGZTHMSA-N thebaine Chemical compound C([C@@H](N(CC1)C)C2=CC=C3OC)C4=CC=C(OC)C5=C4[C@@]21[C@H]3O5 FQXXSQDCDRQNQE-VMDGZTHMSA-N 0.000 claims 1
- 229960001402 tilidine Drugs 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
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 1
- 229940078499 tricalcium phosphate Drugs 0.000 claims 1
- 235000019731 tricalcium phosphate Nutrition 0.000 claims 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 claims 1
- 238000005550 wet granulation Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87249606P | 2006-12-04 | 2006-12-04 | |
| US60/872,496 | 2006-12-04 | ||
| PCT/GB2007/004627 WO2008068471A1 (en) | 2006-12-04 | 2007-12-03 | New non-abusable pharmaceutical composition comprising opioids |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013181931A Division JP2013249312A (ja) | 2006-12-04 | 2013-09-03 | オピオイドを含む新規の非−乱用性医薬組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511683A JP2010511683A (ja) | 2010-04-15 |
| JP2010511683A5 true JP2010511683A5 (enExample) | 2011-01-20 |
| JP5484062B2 JP5484062B2 (ja) | 2014-05-07 |
Family
ID=37781988
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009539799A Expired - Fee Related JP5484062B2 (ja) | 2006-12-04 | 2007-12-03 | オピオイドを含む新規の非−乱用性医薬組成物 |
| JP2013181931A Pending JP2013249312A (ja) | 2006-12-04 | 2013-09-03 | オピオイドを含む新規の非−乱用性医薬組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013181931A Pending JP2013249312A (ja) | 2006-12-04 | 2013-09-03 | オピオイドを含む新規の非−乱用性医薬組成物 |
Country Status (9)
| Country | Link |
|---|---|
| US (5) | US8470361B2 (enExample) |
| EP (1) | EP2101740B1 (enExample) |
| JP (2) | JP5484062B2 (enExample) |
| DK (1) | DK2101740T3 (enExample) |
| ES (1) | ES2439581T3 (enExample) |
| PL (1) | PL2101740T3 (enExample) |
| PT (1) | PT2101740E (enExample) |
| SI (1) | SI2101740T1 (enExample) |
| WO (1) | WO2008068471A1 (enExample) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003024429A1 (en) | 2001-09-21 | 2003-03-27 | Egalet A/S | Polymer release system |
| US20040253310A1 (en) | 2001-09-21 | 2004-12-16 | Gina Fischer | Morphine polymer release system |
| US8877241B2 (en) | 2003-03-26 | 2014-11-04 | Egalet Ltd. | Morphine controlled release system |
| US8470361B2 (en) * | 2006-12-04 | 2013-06-25 | Orexo Ab | Non-abusable pharmaceutical composition comprising opioids |
| US8821928B2 (en) | 2007-06-04 | 2014-09-02 | Egalet Ltd. | Controlled release pharmaceutical compositions for prolonged effect |
| CN105833420A (zh) * | 2008-06-23 | 2016-08-10 | 生物递送科学国际公司 | 多向粘膜给药装置及使用方法 |
| EP2379111B1 (en) | 2008-12-12 | 2013-03-20 | Paladin Labs Inc. | Narcotic drug formulations with decreased abuse potential |
| NZ594207A (en) | 2009-02-06 | 2013-03-28 | Egalet Ltd | Immediate release composition resistant to abuse by intake of alcohol |
| AU2010265213B2 (en) | 2009-06-24 | 2012-08-23 | Egalet Ltd. | Controlled release formulations |
| US8475832B2 (en) | 2009-08-07 | 2013-07-02 | Rb Pharmaceuticals Limited | Sublingual and buccal film compositions |
| WO2011053251A1 (en) | 2009-10-30 | 2011-05-05 | Ix Biopharma Pte Ltd | Fast dissolving solid dosage form |
| US12186426B2 (en) | 2009-10-30 | 2025-01-07 | Ix Biopharma Ltd. | Solid dosage form |
| ME02153B (me) | 2011-09-19 | 2015-10-20 | Orexo Ab | Nove farmaceutske kompozicije, otporne na zloupotrebu, za tretman zavisnosti od opioida |
| WO2013164617A1 (en) * | 2012-05-02 | 2013-11-07 | Orexo Ab | New sufentanil composition for the treatment of acute pain |
| HRP20161634T1 (hr) | 2012-05-02 | 2017-01-13 | Orexo Ab | Novi pripravak alfentanila za liječenje akutne boli |
| JP2015521988A (ja) | 2012-07-06 | 2015-08-03 | イガレット・リミテッド | 制御放出用乱用防止性医薬組成物 |
| US9675587B2 (en) | 2013-03-14 | 2017-06-13 | Allergan Holdings Unlimited Company | Opioid receptor modulator dosage formulations |
| US11931227B2 (en) | 2013-03-15 | 2024-03-19 | Cook Medical Technologies Llc | Bimodal treatment methods and compositions for gastrointestinal lesions with active bleeding |
| CN103304570A (zh) * | 2013-07-12 | 2013-09-18 | 四川省惠达药业有限公司 | 一种盐酸纳洛酮化合物、其制备方法及其药物组合物 |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9770514B2 (en) | 2013-09-03 | 2017-09-26 | ExxPharma Therapeutics LLC | Tamper-resistant pharmaceutical dosage forms |
| KR20160108828A (ko) | 2013-11-11 | 2016-09-20 | 임팩스 라보라토리즈, 인코포레이티드 | 신속하게 붕괴되는 제형 및 사용 방법 |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US10617686B2 (en) | 2014-07-08 | 2020-04-14 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| EP3177146A4 (en) | 2014-07-08 | 2018-01-03 | Insys Pharma, Inc. | Sublingual naloxone spray |
| US10722510B2 (en) | 2014-07-08 | 2020-07-28 | Hikma Pharmaceuticals Usa Inc. | Liquid naloxone spray |
| DK3169315T3 (da) | 2014-07-17 | 2020-08-10 | Pharmaceutical Manufacturing Res Services In | Væskefyldt doseringsform til forhindring af misbrug med øjeblikkelig frigivelse |
| AU2015336065A1 (en) | 2014-10-20 | 2017-05-04 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| WO2016118515A1 (en) | 2015-01-20 | 2016-07-28 | Handa Pharmaceuticals, Llc | Stable solid fingolimod dosage forms |
| MA43313B1 (fr) | 2015-09-02 | 2022-06-30 | Trevena Inc | Aza-hétérocyclique à 6 éléments contenant des composés modulateurs de récepteurs opioïdes delta, et leurs procédés de fabrication et d'utilisation |
| EP3210596A1 (en) * | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical composition |
| EP3210630A1 (en) * | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical compositions |
| JP7076171B2 (ja) * | 2016-12-26 | 2022-05-27 | 塩野義製薬株式会社 | 含量均一性を改善した製剤の製造方法 |
| CN110446495B (zh) | 2017-02-17 | 2023-09-05 | 特维娜有限公司 | 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法 |
| CN110520129A (zh) | 2017-02-17 | 2019-11-29 | 特维娜有限公司 | 含有5元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法 |
| US12161754B2 (en) | 2017-12-20 | 2024-12-10 | Purdue Pharma L.P. | Abuse deterrent morphine sulfate dosage forms |
| CA3166250A1 (en) | 2020-02-05 | 2021-08-12 | Gregory G. Plucinski | Drug products for intranasal administration and uses thereof |
| CN116406268A (zh) | 2020-10-27 | 2023-07-07 | 特维娜有限公司 | δ-阿片样物质调节剂的结晶和无定形形式 |
| EP4548911A1 (en) | 2023-11-06 | 2025-05-07 | Extrovis AG | Pharmaceutical compositions |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5138412A (en) | 1974-09-24 | 1976-03-31 | Nippon Kayaku Kk | Kokoseizai no seiho |
| GB8332556D0 (en) | 1983-12-06 | 1984-01-11 | Reckitt & Colmann Prod Ltd | Analgesic compositions |
| FR2562313B1 (fr) | 1984-04-03 | 1989-04-07 | Cogema | Procede de decontamination en uranium et en radium de solutions uraniferes acides par addition d'un sel d'aluminium |
| GB8430346D0 (en) | 1984-11-30 | 1985-01-09 | Reckitt & Colmann Prod Ltd | Analgesic compositions |
| US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| GB8728294D0 (en) | 1987-12-03 | 1988-01-06 | Reckitt & Colmann Prod Ltd | Treatment compositions |
| SE9803240D0 (sv) | 1998-09-24 | 1998-09-24 | Diabact Ab | A pharmaceutical composition having a rapid action |
| SE9803239D0 (sv) * | 1998-09-24 | 1998-09-24 | Diabact Ab | Composition for the treatment of acute pain |
| US6716449B2 (en) | 2000-02-08 | 2004-04-06 | Euro-Celtique S.A. | Controlled-release compositions containing opioid agonist and antagonist |
| SI2283842T1 (sl) | 2000-02-08 | 2015-07-31 | Euro-Celtique S.A. | Oralne formulacije opioidnih agonistov, varne pred zlorabo |
| EP1387673B1 (en) | 2001-05-11 | 2010-12-29 | Endo Pharmaceuticals Inc. | Abuse-resistant controlled-release opioid dosage form |
| US7842307B2 (en) | 2001-08-06 | 2010-11-30 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and gelling agent |
| US7144587B2 (en) * | 2001-08-06 | 2006-12-05 | Euro-Celtique S.A. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and bittering agent |
| US7332182B2 (en) | 2001-08-06 | 2008-02-19 | Purdue Pharma L.P. | Pharmaceutical formulation containing opioid agonist, opioid antagonist and irritant |
| US20030191147A1 (en) | 2002-04-09 | 2003-10-09 | Barry Sherman | Opioid antagonist compositions and dosage forms |
| AU2003296954A1 (en) | 2002-12-13 | 2004-07-09 | The Regents Of The University Of California | Analgesic combination comprising nalbuphine |
| US7524515B2 (en) * | 2003-01-10 | 2009-04-28 | Mutual Pharmaceuticals, Inc. | Pharmaceutical safety dosage forms |
| SI1587514T1 (sl) | 2003-01-31 | 2006-10-31 | Orexo Ab | Hitro ucinkujoc farmacevtski sestavek |
| TWI347201B (en) | 2003-04-21 | 2011-08-21 | Euro Celtique Sa | Pharmaceutical products,uses thereof and methods for preparing the same |
| EP1863456A1 (en) | 2005-03-28 | 2007-12-12 | Orexo AB | New pharmaceutical compositions useful in the treatment of pain |
| US8470361B2 (en) * | 2006-12-04 | 2013-06-25 | Orexo Ab | Non-abusable pharmaceutical composition comprising opioids |
-
2007
- 2007-12-03 US US12/312,995 patent/US8470361B2/en active Active
- 2007-12-03 PL PL07824784T patent/PL2101740T3/pl unknown
- 2007-12-03 JP JP2009539799A patent/JP5484062B2/ja not_active Expired - Fee Related
- 2007-12-03 PT PT78247848T patent/PT2101740E/pt unknown
- 2007-12-03 WO PCT/GB2007/004627 patent/WO2008068471A1/en not_active Ceased
- 2007-12-03 SI SI200731398T patent/SI2101740T1/sl unknown
- 2007-12-03 DK DK07824784.8T patent/DK2101740T3/da active
- 2007-12-03 ES ES07824784.8T patent/ES2439581T3/es active Active
- 2007-12-03 EP EP07824784.8A patent/EP2101740B1/en active Active
-
2013
- 2013-03-13 US US13/799,117 patent/US8658198B2/en active Active
- 2013-03-13 US US13/799,310 patent/US8980305B2/en active Active
- 2013-09-03 JP JP2013181931A patent/JP2013249312A/ja active Pending
-
2014
- 2014-07-25 US US14/340,888 patent/US20140335190A1/en not_active Abandoned
-
2015
- 2015-06-30 US US14/755,091 patent/US20160151351A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008534564A5 (enExample) | ||
| EP2101740B1 (en) | New non-abusable pharmaceutical composition comprising opioids | |
| RU2007139827A (ru) | Фармацевтические композиции для лечения боли | |
| JP6254148B2 (ja) | オピエート腸溶放出ビーズを含む経口フィルム | |
| CA2699172C (en) | Compositions and methods for delivery of poorly soluble drugs | |
| JP2006524249A5 (enExample) | ||
| CA2446738A1 (en) | Abuse-resistant opioid dosage form | |
| JP2012519675A5 (enExample) | ||
| CA2547334A1 (en) | Methods and compositions for deterring abuse of opioid containing dosage forms | |
| JP2011519930A5 (enExample) | ||
| JP2011137020A5 (enExample) | ||
| WO2013003845A1 (en) | Abuse resistant drug forms | |
| EP1981502A2 (en) | Pharmaceutical composition containing a central opioid agonist, a central opioid antagonist, and a peripheral opioid antagonist, and method for making the same | |
| RU2009101082A (ru) | Фармацевтические композиции | |
| HRP20120641T1 (hr) | Oralni farmaceutski oblici doziranja otporni na neovlašteno korištenje koji sadrže opioidni analgetik | |
| JP2009541320A5 (enExample) | ||
| ZA200400893B (en) | Opioid agonist formulations with releasable and sequestered antagonist. | |
| JP2014532078A5 (enExample) | ||
| CA2569742A1 (en) | Opioids for the treatment of the restless leg syndrome | |
| JP7524185B2 (ja) | 経口シン・フィルム | |
| JP2005533046A5 (enExample) | ||
| AU2006228297A1 (en) | New pharmaceutical compositions useful in the treatment of pain |