JP2018515455A5 - - Google Patents
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- JP2018515455A5 JP2018515455A5 JP2017555513A JP2017555513A JP2018515455A5 JP 2018515455 A5 JP2018515455 A5 JP 2018515455A5 JP 2017555513 A JP2017555513 A JP 2017555513A JP 2017555513 A JP2017555513 A JP 2017555513A JP 2018515455 A5 JP2018515455 A5 JP 2018515455A5
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- JP
- Japan
- Prior art keywords
- dosage form
- pharmacologically active
- form according
- active ingredient
- particles
- Prior art date
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- 239000002552 dosage form Substances 0.000 claims description 100
- 239000002245 particle Substances 0.000 claims description 69
- 239000002831 pharmacologic agent Substances 0.000 claims description 42
- -1 ethensamide Chemical compound 0.000 claims description 14
- 239000011159 matrix material Substances 0.000 claims description 12
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims description 11
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 9
- 229920000642 polymer Polymers 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 8
- 229960005489 paracetamol Drugs 0.000 claims description 5
- CNBGNNVCVSKAQZ-UHFFFAOYSA-N benzydamine Chemical compound C12=CC=CC=C2C(OCCCN(C)C)=NN1CC1=CC=CC=C1 CNBGNNVCVSKAQZ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- RBBWCVQDXDFISW-UHFFFAOYSA-N Feprazone Chemical compound O=C1C(CC=C(C)C)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 RBBWCVQDXDFISW-UHFFFAOYSA-N 0.000 claims description 3
- 229960000489 feprazone Drugs 0.000 claims description 3
- 238000000338 in vitro Methods 0.000 claims description 3
- 229940127240 opiate Drugs 0.000 claims description 3
- LJRDOKAZOAKLDU-UDXJMMFXSA-N (2s,3s,4r,5r,6r)-5-amino-2-(aminomethyl)-6-[(2r,3s,4r,5s)-5-[(1r,2r,3s,5r,6s)-3,5-diamino-2-[(2s,3r,4r,5s,6r)-3-amino-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-hydroxycyclohexyl]oxy-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]oxyoxane-3,4-diol;sulfuric ac Chemical compound OS(O)(=O)=O.N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)N)O[C@@H]1CO LJRDOKAZOAKLDU-UDXJMMFXSA-N 0.000 claims description 2
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims description 2
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 claims description 2
- 229920001287 Chondroitin sulfate Polymers 0.000 claims description 2
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 claims description 2
- 229920002683 Glycosaminoglycan Polymers 0.000 claims description 2
- JUUFBMODXQKSTD-UHFFFAOYSA-N N-[2-amino-6-[(4-fluorophenyl)methylamino]-3-pyridinyl]carbamic acid ethyl ester Chemical compound N1=C(N)C(NC(=O)OCC)=CC=C1NCC1=CC=C(F)C=C1 JUUFBMODXQKSTD-UHFFFAOYSA-N 0.000 claims description 2
- BLXXJMDCKKHMKV-UHFFFAOYSA-N Nabumetone Chemical compound C1=C(CCC(C)=O)C=CC2=CC(OC)=CC=C21 BLXXJMDCKKHMKV-UHFFFAOYSA-N 0.000 claims description 2
- RGPDEAGGEXEMMM-UHFFFAOYSA-N Nefopam Chemical compound C12=CC=CC=C2CN(C)CCOC1C1=CC=CC=C1 RGPDEAGGEXEMMM-UHFFFAOYSA-N 0.000 claims description 2
- JZFPYUNJRRFVQU-UHFFFAOYSA-N Niflumic acid Chemical compound OC(=O)C1=CC=CN=C1NC1=CC=CC(C(F)(F)F)=C1 JZFPYUNJRRFVQU-UHFFFAOYSA-N 0.000 claims description 2
- 229960001671 azapropazone Drugs 0.000 claims description 2
- WOIIIUDZSOLAIW-NSHDSACASA-N azapropazone Chemical compound C1=C(C)C=C2N3C(=O)[C@H](CC=C)C(=O)N3C(N(C)C)=NC2=C1 WOIIIUDZSOLAIW-NSHDSACASA-N 0.000 claims description 2
- 229960000333 benzydamine Drugs 0.000 claims description 2
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 claims description 2
- 229940059329 chondroitin sulfate Drugs 0.000 claims description 2
- 229960002896 clonidine Drugs 0.000 claims description 2
- 229960001640 dimetotiazine Drugs 0.000 claims description 2
- VWNWVCJGUMZDIU-UHFFFAOYSA-N dimetotiazine Chemical compound C1=C(S(=O)(=O)N(C)C)C=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 VWNWVCJGUMZDIU-UHFFFAOYSA-N 0.000 claims description 2
- 229960003667 flupirtine Drugs 0.000 claims description 2
- 229960002442 glucosamine Drugs 0.000 claims description 2
- 229940059346 glucosaminoglycan polysulfate Drugs 0.000 claims description 2
- 229960004147 iprazochrome Drugs 0.000 claims description 2
- XZKVIDLLLOUTSS-ZSOIEALJSA-N iprazochrome Chemical compound NC(=O)N/N=C/1C(=O)C=C2N(C(C)C)CC(O)C2=C\1 XZKVIDLLLOUTSS-ZSOIEALJSA-N 0.000 claims description 2
- 229960002455 methoxyflurane Drugs 0.000 claims description 2
- RFKMCNOHBTXSMU-UHFFFAOYSA-N methoxyflurane Chemical compound COC(F)(F)C(Cl)Cl RFKMCNOHBTXSMU-UHFFFAOYSA-N 0.000 claims description 2
- 229960004270 nabumetone Drugs 0.000 claims description 2
- 239000004081 narcotic agent Substances 0.000 claims description 2
- 229960000751 nefopam Drugs 0.000 claims description 2
- 229960000916 niflumic acid Drugs 0.000 claims description 2
- 229960000965 nimesulide Drugs 0.000 claims description 2
- HYWYRSMBCFDLJT-UHFFFAOYSA-N nimesulide Chemical compound CS(=O)(=O)NC1=CC=C([N+]([O-])=O)C=C1OC1=CC=CC=C1 HYWYRSMBCFDLJT-UHFFFAOYSA-N 0.000 claims description 2
- 229940121367 non-opioid analgesics Drugs 0.000 claims description 2
- 229940005483 opioid analgesics Drugs 0.000 claims description 2
- 229960001639 penicillamine Drugs 0.000 claims description 2
- 229960004572 pizotifen Drugs 0.000 claims description 2
- FIADGNVRKBPQEU-UHFFFAOYSA-N pizotifen Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CCC2=C1C=CS2 FIADGNVRKBPQEU-UHFFFAOYSA-N 0.000 claims description 2
- 230000000506 psychotropic effect Effects 0.000 claims description 2
- 239000000021 stimulant Substances 0.000 claims description 2
- 229960003676 tenidap Drugs 0.000 claims description 2
- LXIKEPCNDFVJKC-QXMHVHEDSA-N tenidap Chemical compound C12=CC(Cl)=CC=C2N(C(=O)N)C(=O)\C1=C(/O)C1=CC=CS1 LXIKEPCNDFVJKC-QXMHVHEDSA-N 0.000 claims description 2
- 239000003204 tranquilizing agent Substances 0.000 claims description 2
- 230000002936 tranquilizing effect Effects 0.000 claims description 2
- RJMIEHBSYVWVIN-LLVKDONJSA-N (2r)-2-[4-(3-oxo-1h-isoindol-2-yl)phenyl]propanoic acid Chemical compound C1=CC([C@H](C(O)=O)C)=CC=C1N1C(=O)C2=CC=CC=C2C1 RJMIEHBSYVWVIN-LLVKDONJSA-N 0.000 claims 2
- MITFXPHMIHQXPI-UHFFFAOYSA-N Oraflex Chemical compound N=1C2=CC(C(C(O)=O)C)=CC=C2OC=1C1=CC=C(Cl)C=C1 MITFXPHMIHQXPI-UHFFFAOYSA-N 0.000 claims 2
- YNPNZTXNASCQKK-UHFFFAOYSA-N Phenanthrene Natural products C1=CC=C2C3=CC=CC=C3C=CC2=C1 YNPNZTXNASCQKK-UHFFFAOYSA-N 0.000 claims 2
- DGEZNRSVGBDHLK-UHFFFAOYSA-N [1,10]phenanthroline Chemical compound C1=CN=C2C3=NC=CC=C3C=CC2=C1 DGEZNRSVGBDHLK-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 2
- 229960004187 indoprofen Drugs 0.000 claims 2
- CPJSUEIXXCENMM-UHFFFAOYSA-N phenacetin Chemical compound CCOC1=CC=C(NC(C)=O)C=C1 CPJSUEIXXCENMM-UHFFFAOYSA-N 0.000 claims 2
- WVYADZUPLLSGPU-UHFFFAOYSA-N salsalate Chemical compound OC(=O)C1=CC=CC=C1OC(=O)C1=CC=CC=C1O WVYADZUPLLSGPU-UHFFFAOYSA-N 0.000 claims 2
- RDJGLLICXDHJDY-NSHDSACASA-N (2s)-2-(3-phenoxyphenyl)propanoic acid Chemical compound OC(=O)[C@@H](C)C1=CC=CC(OC=2C=CC=CC=2)=C1 RDJGLLICXDHJDY-NSHDSACASA-N 0.000 claims 1
- MDKGKXOCJGEUJW-VIFPVBQESA-N (2s)-2-[4-(thiophene-2-carbonyl)phenyl]propanoic acid Chemical compound C1=CC([C@@H](C(O)=O)C)=CC=C1C(=O)C1=CC=CS1 MDKGKXOCJGEUJW-VIFPVBQESA-N 0.000 claims 1
- KPJZHOPZRAFDTN-ZRGWGRIASA-N (6aR,9R)-N-[(2S)-1-hydroxybutan-2-yl]-4,7-dimethyl-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-9-carboxamide Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@H](CO)CC)C2)=C3C2=CN(C)C3=C1 KPJZHOPZRAFDTN-ZRGWGRIASA-N 0.000 claims 1
- XCHHJFVNQPPLJK-UHFFFAOYSA-N 2-carboxyphenolate;1h-imidazol-1-ium Chemical compound C1=CNC=N1.OC(=O)C1=CC=CC=C1O XCHHJFVNQPPLJK-UHFFFAOYSA-N 0.000 claims 1
- MECVOSKQBMPUFG-UHFFFAOYSA-N 2-carboxyphenolate;morpholin-4-ium Chemical compound C1COCCN1.OC(=O)C1=CC=CC=C1O MECVOSKQBMPUFG-UHFFFAOYSA-N 0.000 claims 1
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical group CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 claims 1
- WKEMJKQOLOHJLZ-UHFFFAOYSA-N Almogran Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1CS(=O)(=O)N1CCCC1 WKEMJKQOLOHJLZ-UHFFFAOYSA-N 0.000 claims 1
- RLFWWDJHLFCNIJ-UHFFFAOYSA-N Aminoantipyrine Natural products CN1C(C)=C(N)C(=O)N1C1=CC=CC=C1 RLFWWDJHLFCNIJ-UHFFFAOYSA-N 0.000 claims 1
- RMMXTBMQSGEXHJ-UHFFFAOYSA-N Aminophenazone Chemical compound O=C1C(N(C)C)=C(C)N(C)N1C1=CC=CC=C1 RMMXTBMQSGEXHJ-UHFFFAOYSA-N 0.000 claims 1
- XHVAWZZCDCWGBK-WYRLRVFGSA-M Aurothioglucose Chemical compound OC[C@H]1O[C@H](S[Au])[C@H](O)[C@@H](O)[C@@H]1O XHVAWZZCDCWGBK-WYRLRVFGSA-M 0.000 claims 1
- MNIPYSSQXLZQLJ-UHFFFAOYSA-N Biofenac Chemical compound OC(=O)COC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl MNIPYSSQXLZQLJ-UHFFFAOYSA-N 0.000 claims 1
- LIAWQASKBFCRNR-UHFFFAOYSA-N Bucetin Chemical compound CCOC1=CC=C(NC(=O)CC(C)O)C=C1 LIAWQASKBFCRNR-UHFFFAOYSA-N 0.000 claims 1
- UDKCHVLMFQVBAA-UHFFFAOYSA-M Choline salicylate Chemical compound C[N+](C)(C)CCO.OC1=CC=CC=C1C([O-])=O UDKCHVLMFQVBAA-UHFFFAOYSA-M 0.000 claims 1
- SBDNJUWAMKYJOX-UHFFFAOYSA-N Meclofenamic Acid Chemical compound CC1=CC=C(Cl)C(NC=2C(=CC=CC=2)C(O)=O)=C1Cl SBDNJUWAMKYJOX-UHFFFAOYSA-N 0.000 claims 1
- BRZANEXCSZCZCI-UHFFFAOYSA-N Nifenazone Chemical compound O=C1N(C=2C=CC=CC=2)N(C)C(C)=C1NC(=O)C1=CC=CN=C1 BRZANEXCSZCZCI-UHFFFAOYSA-N 0.000 claims 1
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 claims 1
- SKZKKFZAGNVIMN-UHFFFAOYSA-N Salicilamide Chemical compound NC(=O)C1=CC=CC=C1O SKZKKFZAGNVIMN-UHFFFAOYSA-N 0.000 claims 1
- ABBQHOQBGMUPJH-UHFFFAOYSA-M Sodium salicylate Chemical compound [Na+].OC1=CC=CC=C1C([O-])=O ABBQHOQBGMUPJH-UHFFFAOYSA-M 0.000 claims 1
- 229960004420 aceclofenac Drugs 0.000 claims 1
- 229960004892 acemetacin Drugs 0.000 claims 1
- FSQKKOOTNAMONP-UHFFFAOYSA-N acemetacin Chemical compound CC1=C(CC(=O)OCC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 FSQKKOOTNAMONP-UHFFFAOYSA-N 0.000 claims 1
- 229960005142 alclofenac Drugs 0.000 claims 1
- ARHWPKZXBHOEEE-UHFFFAOYSA-N alclofenac Chemical compound OC(=O)CC1=CC=C(OCC=C)C(Cl)=C1 ARHWPKZXBHOEEE-UHFFFAOYSA-N 0.000 claims 1
- 229960002133 almotriptan Drugs 0.000 claims 1
- 229960000212 aminophenazone Drugs 0.000 claims 1
- VEQOALNAAJBPNY-UHFFFAOYSA-N antipyrine Chemical compound CN1C(C)=CC(=O)N1C1=CC=CC=C1 VEQOALNAAJBPNY-UHFFFAOYSA-N 0.000 claims 1
- AUJRCFUBUPVWSZ-XTZHGVARSA-M auranofin Chemical compound CCP(CC)(CC)=[Au]S[C@@H]1O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]1OC(C)=O AUJRCFUBUPVWSZ-XTZHGVARSA-M 0.000 claims 1
- 229960005207 auranofin Drugs 0.000 claims 1
- 229960001799 aurothioglucose Drugs 0.000 claims 1
- 229960005430 benoxaprofen Drugs 0.000 claims 1
- 229960005470 bucetin Drugs 0.000 claims 1
- 229960000962 bufexamac Drugs 0.000 claims 1
- MXJWRABVEGLYDG-UHFFFAOYSA-N bufexamac Chemical compound CCCCOC1=CC=C(CC(=O)NO)C=C1 MXJWRABVEGLYDG-UHFFFAOYSA-N 0.000 claims 1
- 229960003354 bumadizone Drugs 0.000 claims 1
- FLWFHHFTIRLFPV-UHFFFAOYSA-N bumadizone Chemical compound C=1C=CC=CC=1N(C(=O)C(C(O)=O)CCCC)NC1=CC=CC=C1 FLWFHHFTIRLFPV-UHFFFAOYSA-N 0.000 claims 1
- QCVZVMTWFMXZEU-UHFFFAOYSA-L calcium;dicarbamate Chemical compound [Ca+2].NC([O-])=O.NC([O-])=O QCVZVMTWFMXZEU-UHFFFAOYSA-L 0.000 claims 1
- 229960000590 celecoxib Drugs 0.000 claims 1
- RZEKVGVHFLEQIL-UHFFFAOYSA-N celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 claims 1
- 229960002688 choline salicylate Drugs 0.000 claims 1
- 229960003140 clofezone Drugs 0.000 claims 1
- 229960003428 dexibuprofen Drugs 0.000 claims 1
- HEFNNWSXXWATRW-JTQLQIEISA-N dexibuprofen Chemical compound CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 HEFNNWSXXWATRW-JTQLQIEISA-N 0.000 claims 1
- 229960002783 dexketoprofen Drugs 0.000 claims 1
- DKYWVDODHFEZIM-NSHDSACASA-N dexketoprofen Chemical compound OC(=O)[C@@H](C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-NSHDSACASA-N 0.000 claims 1
- 229960001259 diclofenac Drugs 0.000 claims 1
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims 1
- 229960001536 difenpiramide Drugs 0.000 claims 1
- PWHROYKAGRUWDQ-UHFFFAOYSA-N difenpiramide Chemical compound C=1C=CC=NC=1NC(=O)CC(C=C1)=CC=C1C1=CC=CC=C1 PWHROYKAGRUWDQ-UHFFFAOYSA-N 0.000 claims 1
- 229960000616 diflunisal Drugs 0.000 claims 1
- HUPFGZXOMWLGNK-UHFFFAOYSA-N diflunisal Chemical compound C1=C(O)C(C(=O)O)=CC(C=2C(=CC(F)=CC=2)F)=C1 HUPFGZXOMWLGNK-UHFFFAOYSA-N 0.000 claims 1
- 229960004704 dihydroergotamine Drugs 0.000 claims 1
- HESHRHUZIWVEAJ-JGRZULCMSA-N dihydroergotamine Chemical compound C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2[C@@H](C3=CC=CC4=NC=C([C]34)C2)C1)C)C1=CC=CC=C1 HESHRHUZIWVEAJ-JGRZULCMSA-N 0.000 claims 1
- 229960002472 eletriptan Drugs 0.000 claims 1
- OTLDLQZJRFYOJR-LJQANCHMSA-N eletriptan Chemical compound CN1CCC[C@@H]1CC1=CN=C2[C]1C=C(CCS(=O)(=O)C=1C=CC=CC=1)C=C2 OTLDLQZJRFYOJR-LJQANCHMSA-N 0.000 claims 1
- 229960004943 ergotamine Drugs 0.000 claims 1
- OFKDAAIKGIBASY-VFGNJEKYSA-N ergotamine Chemical compound C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2C(C3=CC=CC4=NC=C([C]34)C2)=C1)C)C1=CC=CC=C1 OFKDAAIKGIBASY-VFGNJEKYSA-N 0.000 claims 1
- XCGSFFUVFURLIX-UHFFFAOYSA-N ergotaminine Natural products C1=C(C=2C=CC=C3NC=C(C=23)C2)C2N(C)CC1C(=O)NC(C(N12)=O)(C)OC1(O)C1CCCN1C(=O)C2CC1=CC=CC=C1 XCGSFFUVFURLIX-UHFFFAOYSA-N 0.000 claims 1
- 229960005293 etodolac Drugs 0.000 claims 1
- XFBVBWWRPKNWHW-UHFFFAOYSA-N etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 claims 1
- 229960004945 etoricoxib Drugs 0.000 claims 1
- MNJVRJDLRVPLFE-UHFFFAOYSA-N etoricoxib Chemical compound C1=NC(C)=CC=C1C1=NC=C(Cl)C=C1C1=CC=C(S(C)(=O)=O)C=C1 MNJVRJDLRVPLFE-UHFFFAOYSA-N 0.000 claims 1
- 229960001419 fenoprofen Drugs 0.000 claims 1
- 229960004369 flufenamic acid Drugs 0.000 claims 1
- LPEPZBJOKDYZAD-UHFFFAOYSA-N flufenamic acid Chemical compound OC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 LPEPZBJOKDYZAD-UHFFFAOYSA-N 0.000 claims 1
- CDZJOBWKHSYNMO-SCUQKFFVSA-N flumedroxone Chemical compound C1([C@H](C2)C(F)(F)F)=CC(=O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@@](C(=O)C)(O)[C@@]2(C)CC1 CDZJOBWKHSYNMO-SCUQKFFVSA-N 0.000 claims 1
- 229960002960 flumedroxone Drugs 0.000 claims 1
- 229960001321 flunoxaprofen Drugs 0.000 claims 1
- ARPYQKTVRGFPIS-VIFPVBQESA-N flunoxaprofen Chemical compound N=1C2=CC([C@@H](C(O)=O)C)=CC=C2OC=1C1=CC=C(F)C=C1 ARPYQKTVRGFPIS-VIFPVBQESA-N 0.000 claims 1
- 229960002390 flurbiprofen Drugs 0.000 claims 1
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims 1
- 229960004478 guacetisal Drugs 0.000 claims 1
- HSJFYRYGGKLQBT-UHFFFAOYSA-N guacetisal Chemical compound COC1=CC=CC=C1OC(=O)C1=CC=CC=C1OC(C)=O HSJFYRYGGKLQBT-UHFFFAOYSA-N 0.000 claims 1
- 229960002595 ibuproxam Drugs 0.000 claims 1
- BYPIURIATSUHDW-UHFFFAOYSA-N ibuproxam Chemical compound CC(C)CC1=CC=C(C(C)C(=O)NO)C=C1 BYPIURIATSUHDW-UHFFFAOYSA-N 0.000 claims 1
- 229960004769 imidazole salicylate Drugs 0.000 claims 1
- 229960000905 indomethacin Drugs 0.000 claims 1
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims 1
- 229960000991 ketoprofen Drugs 0.000 claims 1
- 229960004752 ketorolac Drugs 0.000 claims 1
- OZWKMVRBQXNZKK-UHFFFAOYSA-N ketorolac Chemical compound OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 claims 1
- 229960003587 lisuride Drugs 0.000 claims 1
- 229960003768 lonazolac Drugs 0.000 claims 1
- XVUQHFRQHBLHQD-UHFFFAOYSA-N lonazolac Chemical compound OC(=O)CC1=CN(C=2C=CC=CC=2)N=C1C1=CC=C(Cl)C=C1 XVUQHFRQHBLHQD-UHFFFAOYSA-N 0.000 claims 1
- 229960000994 lumiracoxib Drugs 0.000 claims 1
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| PCT/EP2016/058978 WO2016170094A1 (en) | 2015-04-24 | 2016-04-22 | Tamper-resistant fixed dose combination providing fast release of two drugs from particles |
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| CA2767576C (en) | 2009-07-08 | 2020-03-10 | Charleston Laboratories Inc. | Pharmaceutical compositions comprising an antiemetic and an opioid analgesic |
| CA3055170A1 (en) | 2016-03-04 | 2017-09-08 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| EP3473246A1 (en) | 2017-10-19 | 2019-04-24 | Capsugel Belgium NV | Immediate release abuse deterrent formulations |
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| US20030092724A1 (en) | 2001-09-18 | 2003-05-15 | Huaihung Kao | Combination sustained release-immediate release oral dosage forms with an opioid analgesic and a non-opioid analgesic |
| EP1658054B1 (de) | 2003-08-06 | 2007-06-27 | Grünenthal GmbH | Gegen missbrauch gesicherte darreichungsform |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| US7201920B2 (en) | 2003-11-26 | 2007-04-10 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of opioid containing dosage forms |
| PL1740156T3 (pl) | 2004-04-22 | 2011-12-30 | Gruenenthal Gmbh | Sposób wytwarzania zabezpieczonej przed nadużyciem, stałej postaci aplikacyjnej |
| PL1765298T3 (pl) | 2004-07-01 | 2013-01-31 | Gruenenthal Gmbh | Sposób wytwarzania stałej postaci dawkowania, która jest zabezpieczona przez nadużywaniem, wykorzystujący wytłaczarkę z przekładnią planetarną |
| AR049562A1 (es) | 2004-07-01 | 2006-08-16 | Gruenenthal Gmbh | Formas farmaceuticas orales, con liberacion controlada de opioides, protegidas frente al abuso y procedimiento para su preparacion |
| BRPI0513300B1 (pt) | 2004-07-01 | 2018-11-06 | Gruenenthal Gmbh | forma farmacêutica oral, protegida frente ao abuso, contendo (1r, 2r)-3-(3-dimetilamino-1-etil-2- metil-lpropil)-fenol |
| DE102005005449A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| NZ562304A (en) | 2005-05-10 | 2010-06-25 | Novartis Ag | Extrusion process for making compositions with poorly compressible therapeutic compounds e.g. metformin hydrochloride |
| US8652529B2 (en) | 2005-11-10 | 2014-02-18 | Flamel Technologies | Anti-misuse microparticulate oral pharmaceutical form |
| US20070292508A1 (en) | 2006-06-05 | 2007-12-20 | Balchem Corporation | Orally disintegrating dosage forms |
| US20080069891A1 (en) | 2006-09-15 | 2008-03-20 | Cima Labs, Inc. | Abuse resistant drug formulation |
| SA07280459B1 (ar) | 2006-08-25 | 2011-07-20 | بيورديو فارما إل. بي. | أشكال جرعة صيدلانية للتناول عن طريق الفم مقاومة للعبث تشتمل على مسكن شبه أفيوني |
| DE102007011485A1 (de) | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Darreichungsform mit erschwertem Missbrauch |
| CA2713128C (en) | 2008-01-25 | 2016-04-05 | Gruenenthal Gmbh | Pharmaceutical dosage form |
| AU2009243681B2 (en) | 2008-05-09 | 2013-12-19 | Grunenthal Gmbh | Process for the preparation of an intermediate powder formulation and a final solid dosage form under usage of a spray congealing step |
| GB0909680D0 (en) | 2009-06-05 | 2009-07-22 | Euro Celtique Sa | Dosage form |
| CN102639118B (zh) | 2009-07-22 | 2015-07-29 | 格吕伦塔尔有限公司 | 氧化稳定的抗干扰剂型 |
| KR101738369B1 (ko) | 2009-07-22 | 2017-05-22 | 그뤼넨탈 게엠베하 | 핫 멜트 압출된 제어 방출 투여형 |
| ES2606227T3 (es) | 2010-02-03 | 2017-03-23 | Grünenthal GmbH | Preparación de una composición farmacéutica en polvo mediante una extrusora |
| CN107308124A (zh) | 2010-09-02 | 2017-11-03 | 格吕伦塔尔有限公司 | 包含阴离子聚合物的抗破碎剂型 |
| BR112013005194A2 (pt) | 2010-09-02 | 2016-05-03 | Gruenenthal Gmbh | forma de dosagem resistente à violação compreendendo sal inorgânico |
| TWI516286B (zh) | 2010-09-02 | 2016-01-11 | 歌林達股份有限公司 | 含陰離子聚合物之抗破碎劑型 |
| WO2012061779A1 (en) | 2010-11-04 | 2012-05-10 | Abbott Gmbh & Co. Kg | Drug formulations |
| GB201020895D0 (en) | 2010-12-09 | 2011-01-26 | Euro Celtique Sa | Dosage form |
| US8858963B1 (en) * | 2011-05-17 | 2014-10-14 | Mallinckrodt Llc | Tamper resistant composition comprising hydrocodone and acetaminophen for rapid onset and extended duration of analgesia |
| EA201400172A1 (ru) | 2011-07-29 | 2014-06-30 | Грюненталь Гмбх | Устойчивая к разрушению таблетка, которая обеспечивает немедленное высвобождение лекарственного средства |
| BR112014001091A2 (pt) | 2011-07-29 | 2017-02-14 | Gruenenthal Gmbh | comprimido resistente à adulteração que fornece liberação imediata do fármaco |
| FR2979242A1 (fr) | 2011-08-29 | 2013-03-01 | Sanofi Sa | Comprime contre l'usage abusif, a base de paracetamol et d'oxycodone |
| PE20141171A1 (es) | 2011-10-06 | 2014-09-21 | Gruenenthal Chemie | Forma de dosificacion farmaceutica oral resistente a alteracion comprendiendo agonista opioide y antagonista opioide |
| PE20141671A1 (es) | 2011-11-17 | 2014-11-22 | Gruenenthal Chemie | Forma de dosis farmaceutica oral a prueba de manipulacion que comprende un agente antagonista y/o repelente opioide, oxido de polialquileno y un polimero anionico |
| US20130225625A1 (en) | 2012-02-28 | 2013-08-29 | Grunenthal Gmbh | Tamper-resistant pharmaceutical dosage form comprising nonionic surfactant |
| MX356421B (es) | 2012-02-28 | 2018-05-29 | Gruenenthal Gmbh | Forma de dosificacion resistente a la manipulacion indebida que comprende un compuesto farmacologicamente activo y un polimero anionico. |
| CN109820830A (zh) * | 2012-03-02 | 2019-05-31 | 罗德兹制药股份有限公司 | 抗破坏性立即释放型制剂类 |
| EP2838512B1 (en) | 2012-04-18 | 2018-08-22 | Grünenthal GmbH | Tamper resistant and dose-dumping resistant pharmaceutical dosage form |
| SI2846835T1 (en) | 2012-05-11 | 2018-01-31 | Gruenenthal Gmbh | Heat-formed pharmaceutical dosage form, resistant to abuse and containing zinc |
| US9517208B2 (en) * | 2013-03-15 | 2016-12-13 | Purdue Pharma L.P. | Abuse-deterrent dosage forms |
| EP3003279A1 (en) | 2013-05-29 | 2016-04-13 | Grünenthal GmbH | Tamper-resistant dosage form containing one or more particles |
| US9737490B2 (en) | 2013-05-29 | 2017-08-22 | Grünenthal GmbH | Tamper resistant dosage form with bimodal release profile |
| CA2817728A1 (en) | 2013-05-31 | 2014-11-30 | Pharmascience Inc. | Abuse deterrent immediate release formulation |
| BR112016000194A8 (pt) | 2013-07-12 | 2019-12-31 | Gruenenthal Gmbh | forma de dosagem resistente à violação contendo o polímero de acetato de etileno-vinila |
-
2016
- 2016-04-22 AU AU2016251851A patent/AU2016251851A1/en not_active Abandoned
- 2016-04-22 MX MX2017013633A patent/MX2017013633A/es unknown
- 2016-04-22 EP EP16721716.5A patent/EP3285747A1/en not_active Withdrawn
- 2016-04-22 JP JP2017555513A patent/JP2018515455A/ja not_active Withdrawn
- 2016-04-22 CA CA2983634A patent/CA2983634A1/en not_active Abandoned
- 2016-04-22 US US15/135,591 patent/US20160310437A1/en not_active Abandoned
- 2016-04-22 BR BR112017022856A patent/BR112017022856A2/pt active Search and Examination
- 2016-04-22 WO PCT/EP2016/058978 patent/WO2016170094A1/en not_active Ceased
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