JP2018513872A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018513872A5 JP2018513872A5 JP2017555531A JP2017555531A JP2018513872A5 JP 2018513872 A5 JP2018513872 A5 JP 2018513872A5 JP 2017555531 A JP2017555531 A JP 2017555531A JP 2017555531 A JP2017555531 A JP 2017555531A JP 2018513872 A5 JP2018513872 A5 JP 2018513872A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- particle
- pharmacologically active
- form according
- active ingredient
- 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.)
- Withdrawn
Links
- 239000002245 particle Substances 0.000 claims description 95
- 239000002552 dosage form Substances 0.000 claims description 93
- 239000002831 pharmacologic agent Substances 0.000 claims description 45
- -1 ethensamide Chemical compound 0.000 claims description 17
- 239000007884 disintegrant Substances 0.000 claims description 13
- 239000011159 matrix material Substances 0.000 claims description 13
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 11
- 229920000642 polymer Polymers 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 6
- 229960005489 paracetamol Drugs 0.000 claims description 6
- 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
- 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
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical group CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 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
- 229960001680 ibuprofen 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
- 229960003251 morniflumate Drugs 0.000 claims description 2
- LDXSPUSKBDTEKA-UHFFFAOYSA-N morniflumate Chemical compound FC(F)(F)C1=CC=CC(NC=2C(=CC=CN=2)C(=O)OCCN2CCOCC2)=C1 LDXSPUSKBDTEKA-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
- 229940005483 opioid analgesics Drugs 0.000 claims description 2
- 229960004534 orgotein Drugs 0.000 claims description 2
- 108010070915 orgotein Proteins 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
- TUGDLVFMIQZYPA-UHFFFAOYSA-N tetracopper;tetrazinc Chemical compound [Cu+2].[Cu+2].[Cu+2].[Cu+2].[Zn+2].[Zn+2].[Zn+2].[Zn+2] TUGDLVFMIQZYPA-UHFFFAOYSA-N 0.000 claims description 2
- 239000003204 tranquilizing agent Substances 0.000 claims description 2
- 230000002936 tranquilizing effect Effects 0.000 claims description 2
- 229960002811 ziconotide Drugs 0.000 claims description 2
- BPKIMPVREBSLAJ-QTBYCLKRSA-N ziconotide Chemical compound C([C@H]1C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]2C(=O)N[C@@H]3C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@H](C(N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSSC2)C(N)=O)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(N1)=O)CCSC)[C@@H](C)O)C1=CC=C(O)C=C1 BPKIMPVREBSLAJ-QTBYCLKRSA-N 0.000 claims description 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
- 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
- ZISSAWUMDACLOM-UHFFFAOYSA-N triptane Chemical compound CC(C)C(C)(C)C ZISSAWUMDACLOM-UHFFFAOYSA-N 0.000 claims 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 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 compound 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
- 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
- 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
- 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
- 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
- 229960001850 droxicam Drugs 0.000 claims 1
- OEHFRZLKGRKFAS-UHFFFAOYSA-N droxicam Chemical compound C12=CC=CC=C2S(=O)(=O)N(C)C(C2=O)=C1OC(=O)N2C1=CC=CC=N1 OEHFRZLKGRKFAS-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 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
- 229960001395 fenbufen Drugs 0.000 claims 1
- ZPAKPRAICRBAOD-UHFFFAOYSA-N fenbufen Chemical compound C1=CC(C(=O)CCC(=O)O)=CC=C1C1=CC=CC=C1 ZPAKPRAICRBAOD-UHFFFAOYSA-N 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
- 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
- 229960004187 indoprofen 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
- 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
- 229960002202 lornoxicam Drugs 0.000 claims 1
- OXROWJKCGCOJDO-JLHYYAGUSA-N lornoxicam Chemical compound O=C1C=2SC(Cl)=CC=2S(=O)(=O)N(C)\C1=C(\O)NC1=CC=CC=N1 OXROWJKCGCOJDO-JLHYYAGUSA-N 0.000 claims 1
- 229960000994 lumiracoxib Drugs 0.000 claims 1
- KHPKQFYUPIUARC-UHFFFAOYSA-N lumiracoxib Chemical compound OC(=O)CC1=CC(C)=CC=C1NC1=C(F)C=CC=C1Cl KHPKQFYUPIUARC-UHFFFAOYSA-N 0.000 claims 1
- 229960003803 meclofenamic acid Drugs 0.000 claims 1
- 229960003464 mefenamic acid Drugs 0.000 claims 1
- HYYBABOKPJLUIN-UHFFFAOYSA-N mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 claims 1
- 229960000362 metamizole sodium Drugs 0.000 claims 1
- DJGAAPFSPWAYTJ-UHFFFAOYSA-M metamizole sodium Chemical compound [Na+].O=C1C(N(CS([O-])(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 DJGAAPFSPWAYTJ-UHFFFAOYSA-M 0.000 claims 1
- 229960001186 methysergide Drugs 0.000 claims 1
- 229960005285 mofebutazone Drugs 0.000 claims 1
- REOJLIXKJWXUGB-UHFFFAOYSA-N mofebutazone Chemical compound O=C1C(CCCC)C(=O)NN1C1=CC=CC=C1 REOJLIXKJWXUGB-UHFFFAOYSA-N 0.000 claims 1
- 229960002186 morpholine salicylate Drugs 0.000 claims 1
- 229960002187 nifenazone Drugs 0.000 claims 1
- 229960000273 oxametacin Drugs 0.000 claims 1
- AJRNYCDWNITGHF-UHFFFAOYSA-N oxametacin Chemical compound CC1=C(CC(=O)NO)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 AJRNYCDWNITGHF-UHFFFAOYSA-N 0.000 claims 1
- 229960002739 oxaprozin Drugs 0.000 claims 1
- OFPXSFXSNFPTHF-UHFFFAOYSA-N oxaprozin Chemical compound O1C(CCC(=O)O)=NC(C=2C=CC=CC=2)=C1C1=CC=CC=C1 OFPXSFXSNFPTHF-UHFFFAOYSA-N 0.000 claims 1
- 229960000649 oxyphenbutazone Drugs 0.000 claims 1
- HFHZKZSRXITVMK-UHFFFAOYSA-N oxyphenbutazone Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=C(O)C=C1 HFHZKZSRXITVMK-UHFFFAOYSA-N 0.000 claims 1
- 229960004662 parecoxib Drugs 0.000 claims 1
- TZRHLKRLEZJVIJ-UHFFFAOYSA-N parecoxib Chemical compound C1=CC(S(=O)(=O)NC(=O)CC)=CC=C1C1=C(C)ON=C1C1=CC=CC=C1 TZRHLKRLEZJVIJ-UHFFFAOYSA-N 0.000 claims 1
- 229960003893 phenacetin Drugs 0.000 claims 1
- 229960005222 phenazone Drugs 0.000 claims 1
- 229960002895 phenylbutazone Drugs 0.000 claims 1
- VYMDGNCVAMGZFE-UHFFFAOYSA-N phenylbutazonum Chemical compound O=C1C(CCCC)C(=O)N(C=2C=CC=CC=2)N1C1=CC=CC=C1 VYMDGNCVAMGZFE-UHFFFAOYSA-N 0.000 claims 1
- 229960002702 piroxicam Drugs 0.000 claims 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims 1
- 229960000851 pirprofen Drugs 0.000 claims 1
- PIDSZXPFGCURGN-UHFFFAOYSA-N pirprofen Chemical compound ClC1=CC(C(C(O)=O)C)=CC=C1N1CC=CC1 PIDSZXPFGCURGN-UHFFFAOYSA-N 0.000 claims 1
- FRMWBRPWYBNAFB-UHFFFAOYSA-M potassium salicylate Chemical compound [K+].OC1=CC=CC=C1C([O-])=O FRMWBRPWYBNAFB-UHFFFAOYSA-M 0.000 claims 1
- 229960003629 potassium salicylate Drugs 0.000 claims 1
- 229960003192 propacetamol Drugs 0.000 claims 1
- QTGAJCQTLIRCFL-UHFFFAOYSA-N propacetamol Chemical compound CCN(CC)CC(=O)OC1=CC=C(NC(C)=O)C=C1 QTGAJCQTLIRCFL-UHFFFAOYSA-N 0.000 claims 1
- PXWLVJLKJGVOKE-UHFFFAOYSA-N propyphenazone Chemical compound O=C1C(C(C)C)=C(C)N(C)N1C1=CC=CC=C1 PXWLVJLKJGVOKE-UHFFFAOYSA-N 0.000 claims 1
- 229960002189 propyphenazone Drugs 0.000 claims 1
- 229960000425 rizatriptan Drugs 0.000 claims 1
- TXHZXHICDBAVJW-UHFFFAOYSA-N rizatriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1CN1C=NC=N1 TXHZXHICDBAVJW-UHFFFAOYSA-N 0.000 claims 1
- 229960000371 rofecoxib Drugs 0.000 claims 1
- RZJQGNCSTQAWON-UHFFFAOYSA-N rofecoxib Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)C(=O)OC1 RZJQGNCSTQAWON-UHFFFAOYSA-N 0.000 claims 1
- 229960000581 salicylamide Drugs 0.000 claims 1
- 229960000953 salsalate Drugs 0.000 claims 1
- 229960004025 sodium salicylate Drugs 0.000 claims 1
- AGHLUVOCTHWMJV-UHFFFAOYSA-J sodium;gold(3+);2-sulfanylbutanedioate Chemical compound [Na+].[Au+3].[O-]C(=O)CC(S)C([O-])=O.[O-]C(=O)CC(S)C([O-])=O AGHLUVOCTHWMJV-UHFFFAOYSA-J 0.000 claims 1
- 229960000894 sulindac Drugs 0.000 claims 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 1
- 229960004492 suprofen Drugs 0.000 claims 1
- 229960002871 tenoxicam Drugs 0.000 claims 1
- WZWYJBNHTWCXIM-UHFFFAOYSA-N tenoxicam Chemical compound O=C1C=2SC=CC=2S(=O)(=O)N(C)C1=C(O)NC1=CC=CC=N1 WZWYJBNHTWCXIM-UHFFFAOYSA-N 0.000 claims 1
- 229960001017 tolmetin Drugs 0.000 claims 1
- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 claims 1
- UCGZDNYYMDPSRK-UHFFFAOYSA-L trisodium;gold;hydroxy-oxido-oxo-sulfanylidene-$l^{6}-sulfane Chemical compound [Na+].[Na+].[Na+].[Au].OS([S-])(=O)=O.OS([S-])(=O)=O UCGZDNYYMDPSRK-UHFFFAOYSA-L 0.000 claims 1
- 229960002004 valdecoxib Drugs 0.000 claims 1
- LNPDTQAFDNKSHK-UHFFFAOYSA-N valdecoxib Chemical compound CC=1ON=C(C=2C=CC=CC=2)C=1C1=CC=C(S(N)(=O)=O)C=C1 LNPDTQAFDNKSHK-UHFFFAOYSA-N 0.000 claims 1
- 229960001360 zolmitriptan Drugs 0.000 claims 1
- UTAZCRNOSWWEFR-ZDUSSCGKSA-N zolmitriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1C[C@H]1COC(=O)N1 UTAZCRNOSWWEFR-ZDUSSCGKSA-N 0.000 claims 1
- 229920000233 poly(alkylene oxides) Polymers 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 5
- 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 description 4
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 description 4
- 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 description 4
- 229960000240 hydrocodone Drugs 0.000 description 4
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 description 4
- 229960002085 oxycodone Drugs 0.000 description 4
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 4
- 229920002472 Starch Chemical class 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 239000004067 bulking agent Substances 0.000 description 3
- 235000019698 starch Nutrition 0.000 description 3
- 229920002785 Croscarmellose sodium Polymers 0.000 description 2
- 229920000881 Modified starch Chemical class 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 229930013930 alkaloid Natural products 0.000 description 2
- 150000003797 alkaloid derivatives Chemical class 0.000 description 2
- 239000002775 capsule Substances 0.000 description 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 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 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 description 1
- VBRYAQVRADPLST-UHFFFAOYSA-N 1-butylpyrazolidine Chemical compound CCCCN1CCCN1 VBRYAQVRADPLST-UHFFFAOYSA-N 0.000 description 1
- LLSKXGRDUPMXLC-UHFFFAOYSA-N 1-phenylpiperidine Chemical class C1CCCCN1C1=CC=CC=C1 LLSKXGRDUPMXLC-UHFFFAOYSA-N 0.000 description 1
- KISZTEOELCMZPY-UHFFFAOYSA-N 3,3-diphenylpropylamine Chemical class C=1C=CC=CC=1C(CCN)C1=CC=CC=C1 KISZTEOELCMZPY-UHFFFAOYSA-N 0.000 description 1
- TYNLGDBUJLVSMA-UHFFFAOYSA-N 4,5-diacetyloxy-9,10-dioxo-2-anthracenecarboxylic acid Chemical compound O=C1C2=CC(C(O)=O)=CC(OC(C)=O)=C2C(=O)C2=C1C=CC=C2OC(=O)C TYNLGDBUJLVSMA-UHFFFAOYSA-N 0.000 description 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 description 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
- 229920001661 Chitosan Polymers 0.000 description 1
- 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 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-M L-tartrate(1-) Chemical class OC(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-M 0.000 description 1
- 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 description 1
- 239000005913 Maltodextrin Substances 0.000 description 1
- 229920002774 Maltodextrin Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- ZKLXUUYLEHCAMF-UUWFMWQGSA-N Oripavine Chemical class C([C@@H](N(CC1)C)C2=CC=C3OC)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 ZKLXUUYLEHCAMF-UUWFMWQGSA-N 0.000 description 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 description 1
- 244000025272 Persea americana Species 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 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 description 1
- 150000001242 acetic acid derivatives Chemical class 0.000 description 1
- 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 description 1
- 150000001252 acrylic acid derivatives Chemical class 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 150000003931 anilides Chemical class 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000021302 avocado oil Nutrition 0.000 description 1
- 239000008163 avocado oil Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229930003827 cannabinoid Natural products 0.000 description 1
- 239000003557 cannabinoid Substances 0.000 description 1
- 229940065144 cannabinoids Drugs 0.000 description 1
- 239000001913 cellulose Chemical class 0.000 description 1
- 229920002678 cellulose Chemical class 0.000 description 1
- 235000010980 cellulose Nutrition 0.000 description 1
- 229920003086 cellulose ether Polymers 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000003246 corticosteroid Chemical class 0.000 description 1
- 229960005168 croscarmellose Drugs 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 229960004590 diacerein Drugs 0.000 description 1
- 235000019700 dicalcium phosphate Nutrition 0.000 description 1
- 235000013681 dietary sucrose Nutrition 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 150000004676 glycans Chemical class 0.000 description 1
- 229940111120 gold preparations Drugs 0.000 description 1
- 238000009474 hot melt extrusion Methods 0.000 description 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 description 1
- 229960001410 hydromorphone Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 229940053326 magnesium salt Drugs 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 235000019426 modified starch Nutrition 0.000 description 1
- INAXVFBXDYWQFN-XHSDSOJGSA-N morphinan Chemical class C1C2=CC=CC=C2[C@]23CCCC[C@H]3[C@@H]1NCC2 INAXVFBXDYWQFN-XHSDSOJGSA-N 0.000 description 1
- 229960005181 morphine Drugs 0.000 description 1
- 229940121367 non-opioid analgesics Drugs 0.000 description 1
- 238000010943 off-gassing Methods 0.000 description 1
- 229960005118 oxymorphone Drugs 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920005606 polypropylene copolymer Polymers 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 150000005599 propionic acid derivatives Chemical class 0.000 description 1
- JEXVQSWXXUJEMA-UHFFFAOYSA-N pyrazol-3-one Chemical compound O=C1C=CN=N1 JEXVQSWXXUJEMA-UHFFFAOYSA-N 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 229940076279 serotonin Drugs 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 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 description 1
- 229960005126 tapentadol Drugs 0.000 description 1
- 229960003676 tenidap Drugs 0.000 description 1
- 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 description 1
- 229960004380 tramadol Drugs 0.000 description 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 description 1
- 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 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15165065 | 2015-04-24 | ||
| EP15165065.2 | 2015-04-24 | ||
| PCT/EP2016/058980 WO2016170096A1 (en) | 2015-04-24 | 2016-04-22 | Tamper-resistant fixed dose combination providing fast release of two drugs from different particles |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018513872A JP2018513872A (ja) | 2018-05-31 |
| JP2018513872A5 true JP2018513872A5 (enExample) | 2019-05-30 |
Family
ID=53015580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017555531A Withdrawn JP2018513872A (ja) | 2015-04-24 | 2016-04-22 | 異なる粒子から２種の薬物の急速放出をもたらすタンパレジスタントな固定用量組合せ |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20160310428A1 (enExample) |
| EP (1) | EP3285748A1 (enExample) |
| JP (1) | JP2018513872A (enExample) |
| AU (1) | AU2016251853A1 (enExample) |
| BR (1) | BR112017022846A2 (enExample) |
| CA (1) | CA2983640A1 (enExample) |
| MX (1) | MX2017013636A (enExample) |
| WO (1) | WO2016170096A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2451274B1 (en) | 2009-07-08 | 2017-10-04 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| US10179109B2 (en) | 2016-03-04 | 2019-01-15 | Charleston Laboratories, Inc. | Pharmaceutical compositions comprising 5HT receptor agonist and antiemetic particulates |
| US10736905B1 (en) * | 2016-09-09 | 2020-08-11 | Shahin Fatholahi | Nefopam dosage forms and methods of treatment |
| US11446311B2 (en) | 2017-09-08 | 2022-09-20 | Shahin Fatholahi | Methods for treating pain associated with sickle cell disease |
| EP3473246A1 (en) | 2017-10-19 | 2019-04-24 | Capsugel Belgium NV | Immediate release abuse deterrent formulations |
| US12161754B2 (en) | 2017-12-20 | 2024-12-10 | Purdue Pharma L.P. | Abuse deterrent morphine sulfate dosage forms |
| JP7458085B2 (ja) * | 2021-07-28 | 2024-03-29 | 株式会社三協 | 錠剤用崩壊剤及びこれを利用した錠剤 |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7141250B2 (en) | 2001-08-06 | 2006-11-28 | Euro-Celtique S.A. | Pharmaceutical formulation containing bittering agent |
| 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 |
| PT1842533E (pt) | 2003-08-06 | 2013-05-17 | Gruenenthal Gmbh | Forma de dosagem protegida contra abuso |
| 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 |
| AR053304A1 (es) | 2004-07-01 | 2007-05-02 | Gruenenthal Gmbh | Formas farmaceuticas orales protegidas frente al abuso con liberacion controlada de (1r,2r)-3-(3 dimetilamino-1-etil-2metil-propil)fenol y procedimiento para su produccion. |
| 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 |
| CA2572491A1 (en) | 2004-07-01 | 2006-01-12 | Gruenenthal Gmbh | Oral dosage form safeguarded against abuse |
| DE102005005449A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| NZ585116A (en) | 2005-05-10 | 2011-12-22 | 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 |
| TWI454288B (zh) | 2008-01-25 | 2014-10-01 | Gruenenthal Chemie | 藥物劑型 |
| ES2599031T3 (es) | 2008-05-09 | 2017-01-31 | Grünenthal GmbH | Proceso para la preparación de una formulación de polvo intermedia y una forma de dosificación solida final utilizando un paso de congelación por pulverización |
| GB0909680D0 (en) | 2009-06-05 | 2009-07-22 | Euro Celtique Sa | Dosage form |
| ES2534908T3 (es) | 2009-07-22 | 2015-04-30 | Grünenthal GmbH | Forma de dosificación de liberación controlada extruida por fusión en caliente |
| BR112012001466A2 (pt) | 2009-07-22 | 2020-08-11 | Grünenthal GmbH | forma de dosagem resistente à falsificação para opioides sensíveis à oxidação, seu processo de fabricação, e embalagem |
| US9579285B2 (en) | 2010-02-03 | 2017-02-28 | Gruenenthal Gmbh | Preparation of a powdery pharmaceutical composition by means of an extruder |
| CA2808219C (en) | 2010-09-02 | 2019-05-14 | Gruenenthal Gmbh | Tamper resistant dosage form comprising inorganic salt |
| WO2012028318A1 (en) | 2010-09-02 | 2012-03-08 | Grünenthal GmbH | Tamper resistant dosage form comprising an anionic polymer |
| ES2534847T3 (es) | 2010-09-02 | 2015-04-29 | Grünenthal GmbH | Forma de dosificación inviolable que comprende un polímero aniónico |
| WO2012061779A1 (en) * | 2010-11-04 | 2012-05-10 | Abbott Gmbh & Co. Kg | Drug formulations |
| 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 |
| JP6063462B2 (ja) | 2011-07-29 | 2017-01-18 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 即時薬剤放出を提供するタンパーレジスタント錠剤 |
| BR112014002022A2 (pt) | 2011-07-29 | 2017-02-21 | Gruenenthal Gmbh | comprimido resistente à violação proporcionando liberação de fármaco imediata |
| FR2979242A1 (fr) | 2011-08-29 | 2013-03-01 | Sanofi Sa | Comprime contre l'usage abusif, a base de paracetamol et d'oxycodone |
| CA2850853A1 (en) | 2011-10-06 | 2013-04-11 | Grunenthal Gmbh | Tamper-resistant oral pharmaceutical dosage form comprising opioid agonist and opioid antagonist |
| KR20140096062A (ko) | 2011-11-17 | 2014-08-04 | 그뤼넨탈 게엠베하 | 약리학적 활성 성분, 오피오이드 길항제 및/또는 혐오제, 폴리알킬렌 옥사이드 및 음이온성 중합체를 포함하는 탬퍼-저항성 경구 약제학적 투여형 |
| BR112014019988A8 (pt) | 2012-02-28 | 2017-07-11 | Gruenenthal Gmbh | Forma de dosagem resistente a socamento compreendendo um composto farmacologicamente ativo e um polímero aniônico |
| EP2819657A1 (en) | 2012-02-28 | 2015-01-07 | Grünenthal GmbH | Tamper-resistant pharmaceutical dosage form comprising nonionic surfactant |
| TW201722406A (zh) * | 2012-03-02 | 2017-07-01 | 羅德製藥公司 | 抗破壞性立即釋出型調製劑類 |
| LT2838512T (lt) | 2012-04-18 | 2018-11-12 | GrĆ¼nenthal GmbH | Pažeidimui atspari ir dozės atpalaidavimo nuokrypiui atspari farmacinė vaisto forma |
| JP2015516406A (ja) | 2012-05-11 | 2015-06-11 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 亜鉛を含む熱成形された不正使用防止医薬剤形 |
| AU2014273227B2 (en) | 2013-05-29 | 2019-08-15 | Grunenthal Gmbh | Tamper-resistant dosage form containing one or more particles |
| MX2015016254A (es) | 2013-05-29 | 2016-04-20 | Gruenenthal Gmbh | Forma de dosificacion resistente al uso indebido con perfil de liberacion bimodal. |
| CA2817728A1 (en) | 2013-05-31 | 2014-11-30 | Pharmascience Inc. | Abuse deterrent immediate release formulation |
| AU2014289187B2 (en) | 2013-07-12 | 2019-07-11 | Grunenthal Gmbh | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
-
2016
- 2016-04-22 US US15/135,597 patent/US20160310428A1/en not_active Abandoned
- 2016-04-22 WO PCT/EP2016/058980 patent/WO2016170096A1/en not_active Ceased
- 2016-04-22 MX MX2017013636A patent/MX2017013636A/es unknown
- 2016-04-22 JP JP2017555531A patent/JP2018513872A/ja not_active Withdrawn
- 2016-04-22 EP EP16721717.3A patent/EP3285748A1/en not_active Withdrawn
- 2016-04-22 BR BR112017022846-7A patent/BR112017022846A2/en active Search and Examination
- 2016-04-22 CA CA2983640A patent/CA2983640A1/en not_active Abandoned
- 2016-04-22 AU AU2016251853A patent/AU2016251853A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN105491885B (zh) | 疼痛药物组合及其用途 | |
| JP2015044834A5 (enExample) | ||
| WO2007123865A3 (en) | Treatment of inflammatory and ulcerative diseases of the bowel with opioid antagonists | |
| CN106456550A (zh) | 避免乙醇剂量倾泻的多颗粒 | |
| NZ592673A (en) | Antisense compositions with enteric coating for treating crohn's disease, colitis and bowel disease | |
| JP2013151541A5 (enExample) | ||
| EP1135121A2 (en) | Combination of duloxetine with non-steroidal antiinflammatory drug for treating pain | |
| HU227517B1 (en) | Controlled release oxycodone compositions | |
| CN104684548A (zh) | 防止滥用的控释药物组合物 | |
| US9205081B2 (en) | Combinations of opiod/TLR4 antagonist and a cyclooxygenase (COX) inhibitor for use in the treatment of pain | |
| JP2011137020A5 (enExample) | ||
| RU2011104146A (ru) | Фармацевтическая композиция, содержащая опиоидный антагонист, для лечения задержки мочи | |
| JP2009540014A (ja) | 胃障害を処置または予防するためのテガセロドを単独でまたはプロトンポンプ阻害剤と組合せて含む組成物 | |
| Leppert | Oxycodone/naloxone in the management of patients with pain and opioid–induced bowel dysfunction | |
| JP2018515455A5 (enExample) | ||
| JP2018513864A5 (enExample) | ||
| US20140296274A1 (en) | Treatment of pain using a composition of opioid/Toll-like receptor 4 antagonists and dextro enantiomers thereof | |
| CN1691936A (zh) | 立即释放和延长释放组合的镇痛药组合物 | |
| HRP20100373T4 (hr) | Upotreba kombinacije morfina s najmanje jednim opijatnim antagonistom u liječenju ovisnosti o opijatima i u sprječavanju neoralne zloupotrebe opijata kod ovisnika opijatima | |
| JP2014515405A (ja) | オピオイド受容体アゴニストの逐次投与のための組成物 | |
| JP2018515456A5 (enExample) | ||
| EP2019586A2 (en) | Acute pain medications based on fast acting diclofenac-opioid combinations | |
| JP6433980B2 (ja) | Ｎｓａｉｄ投与並びに関連する組成物、方法及びシステム | |
| EP2714042A1 (en) | An analgesic pharmaceutical composition for oral administration | |
| JP2013505260A5 (enExample) |