JP2011511012A5 - - Google Patents

Info

Publication number

JP2011511012A5

JP2011511012A5 JP2010545328A JP2010545328A JP2011511012A5 JP 2011511012 A5 JP2011511012 A5 JP 2011511012A5 JP 2010545328 A JP2010545328 A JP 2010545328A JP 2010545328 A JP2010545328 A JP 2010545328A JP 2011511012 A5 JP2011511012 A5 JP 2011511012A5

Authority

JP

Japan

Prior art keywords

rifabutin

clofazimine

clarithromycin

medicament

patient

Prior art date

2009-02-05

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 229960000885 rifabutin Drugs 0.000 claims description 44
• ZWBTYMGEBZUQTK-PVLSIAFMSA-N [(7S,9E,11S,12R,13S,14R,15R,16R,17S,18S,19E,21Z)-2,15,17,32-tetrahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-1'-(2-methylpropyl)-6,23-dioxospiro[8,33-dioxa-24,27,29-triazapentacyclo[23.6.1.14,7.05,31.026,30]tritriaconta-1(32),2,4,9,19,21,24,26,30-nonaene-28,4'-piperidine]-13-yl] acetate Chemical compound CO[C@H]1\C=C\O[C@@]2(C)Oc3c(C2=O)c2c4NC5(CCN(CC(C)C)CC5)N=c4c(=NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)c(O)c2c(O)c3C ZWBTYMGEBZUQTK-PVLSIAFMSA-N 0.000 claims description 43
• WDQPAMHFFCXSNU-BGABXYSRSA-N clofazimine Chemical compound C12=CC=CC=C2N=C2C=C(NC=3C=CC(Cl)=CC=3)C(=N/C(C)C)/C=C2N1C1=CC=C(Cl)C=C1 WDQPAMHFFCXSNU-BGABXYSRSA-N 0.000 claims description 40
• 229960004287 clofazimine Drugs 0.000 claims description 40
• AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 claims description 35
• 229960002626 clarithromycin Drugs 0.000 claims description 35
• FZAPWRFYENETJG-FMPFFZOVSA-N (7S,9E,11S,12S,13S,14R,15R,16R,17S,18S,19E,21Z)-2,13,15,17,32-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-1'-(2-methylpropyl)spiro[8,33-dioxa-24,27,29-triazapentacyclo[23.6.1.14,7.05,31.026,30]tritriaconta-1(31),2,4,9,19,21,25(32),26,29-nonaene-28,4'-piperidine]-6,23-dione Chemical compound CO[C@H]1\C=C\O[C@@]2(C)Oc3c(C2=O)c2c(c(O)c3C)c(O)c(NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](O)[C@@H]1C)c1=NC3(CCN(CC(C)C)CC3)N=c21 FZAPWRFYENETJG-FMPFFZOVSA-N 0.000 claims description 9
• 239000003814 drug Substances 0.000 claims 36
• 238000010521 absorption reaction Methods 0.000 claims 9
• 239000003623 enhancer Substances 0.000 claims 9
• 239000000203 mixture Substances 0.000 claims 9
• 239000002202 Polyethylene glycol Substances 0.000 claims 8
• 229920001223 polyethylene glycol Polymers 0.000 claims 8
• 239000002552 dosage form Substances 0.000 claims 5
• 230000004060 metabolic process Effects 0.000 claims 4
• 210000002966 serum Anatomy 0.000 claims 4
• 208000015181 infectious disease Diseases 0.000 claims 3
• 208000011231 Crohn disease Diseases 0.000 claims 2
• 241000186359 Mycobacterium Species 0.000 claims 2
• 241000187644 Mycobacterium vaccae Species 0.000 claims 2
• 229940097933 clofazimine 100 mg Drugs 0.000 claims 2
• 229940084443 clofazimine 50 mg Drugs 0.000 claims 2
• 230000001717 pathogenic effect Effects 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 208000014997 Crohn colitis Diseases 0.000 claims 1
• 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
• 241000187482 Mycobacterium avium subsp. paratuberculosis Species 0.000 claims 1
• 241000187481 Mycobacterium phlei Species 0.000 claims 1
• XEOSKTHOPLADLN-QTJNJRLBSA-N acetyl (z,12r)-12-hydroxyoctadec-9-enoate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC(=O)OC(C)=O XEOSKTHOPLADLN-QTJNJRLBSA-N 0.000 claims 1
• 238000011260 co-administration Methods 0.000 claims 1
• 230000003247 decreasing effect Effects 0.000 claims 1
• 230000003053 immunization Effects 0.000 claims 1
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
• 229920000053 polysorbate 80 Polymers 0.000 claims 1
• 229940068968 polysorbate 80 Drugs 0.000 claims 1
• 201000000306 sarcoidosis Diseases 0.000 claims 1
• 241000701447 unidentified baculovirus Species 0.000 claims 1
• BLPFDXNVUDZBII-KNPZYKNQSA-N 14-hydroxyclarithromycin Chemical compound O1[C@@H](C)[C@H](O)[C@@](OC)(C)C[C@@H]1O[C@@H]1[C@@H](C)C(=O)O[C@H](C(C)O)[C@@](C)(O)[C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(OC)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C BLPFDXNVUDZBII-KNPZYKNQSA-N 0.000 description 2
• 238000005259 measurement Methods 0.000 description 2
• 230000036470 plasma concentration Effects 0.000 description 2
• 238000004458 analytical method Methods 0.000 description 1
• 238000003556 assay Methods 0.000 description 1
• 238000011088 calibration curve Methods 0.000 description 1
• 239000002775 capsule Substances 0.000 description 1
• 229940084436 clarithromycin 500 mg Drugs 0.000 description 1
• HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical compound C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 description 1
• 229960004166 diltiazem Drugs 0.000 description 1
• 238000011156 evaluation Methods 0.000 description 1
• 238000002474 experimental method Methods 0.000 description 1
• 238000004128 high performance liquid chromatography Methods 0.000 description 1
• 239000002207 metabolite Substances 0.000 description 1
• 238000002414 normal-phase solid-phase extraction Methods 0.000 description 1
• 238000004366 reverse phase liquid chromatography Methods 0.000 description 1