JP2008543942A

JP2008543942A - ホップ酸の無機塩を含有する組成物、及び該組成物の製造方法

ホップ酸の無機塩を含有する組成物、及び該組成物の製造方法 Download PDF

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Publication number: JP2008543942A
Authority: JP; Japan
Prior art keywords: acid; slurry; composition; salt; calcium
Prior art date: 2005-06-21
Legal status : Pending

Application number

JP2008518335A

Other languages

English (en)

Japanese (ja)

Other versions

JP2008543942A5 (https=

Inventor

ケー．ケビン，マドセン

エム．マーク，ボッサート

オノミツノリ

Original Assignee

ジョンアイ．ハース，インク

Priority date

2005-06-21

Filing date

2006-06-21

Publication date

2008-12-04

2006-06-21 Application filed by ジョンアイ．ハース，インク filed Critical ジョンアイ．ハース，インク

2008-12-04 Publication of JP2008543942A publication Critical patent/JP2008543942A/ja

2009-08-06 Publication of JP2008543942A5 publication Critical patent/JP2008543942A5/ja

Status Pending legal-status Critical Current

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239000002253 acid Substances 0.000 title claims abstract description 208
239000000203 mixture Substances 0.000 title claims abstract description 165
229910017053 inorganic salt Inorganic materials 0.000 title claims description 29
238000004519 manufacturing process Methods 0.000 title claims description 24
238000000034 method Methods 0.000 claims abstract description 131
239000003814 drug Substances 0.000 claims abstract description 18
QRDZSRWEULKVNW-UHFFFAOYSA-N 6-hydroxy-2-oxo-1h-quinoline-4-carboxylic acid Chemical compound C1=C(O)C=C2C(C(=O)O)=CC(=O)NC2=C1 QRDZSRWEULKVNW-UHFFFAOYSA-N 0.000 claims description 119
150000001875 compounds Chemical class 0.000 claims description 100
239000002002 slurry Substances 0.000 claims description 75
150000007513 acids Chemical class 0.000 claims description 59
239000007864 aqueous solution Substances 0.000 claims description 51
-1 aminoglycoside Substances 0.000 claims description 43
150000003839 salts Chemical class 0.000 claims description 41
239000000243 solution Substances 0.000 claims description 40
238000001035 drying Methods 0.000 claims description 38
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 37
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 36
229910052791 calcium Inorganic materials 0.000 claims description 36
239000011575 calcium Substances 0.000 claims description 36
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 34
229910052749 magnesium Inorganic materials 0.000 claims description 34
239000011777 magnesium Substances 0.000 claims description 34
XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 32
230000002829 reductive effect Effects 0.000 claims description 29
RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims description 26
PXHVJJICTQNCMI-UHFFFAOYSA-N Nickel Chemical compound [Ni] PXHVJJICTQNCMI-UHFFFAOYSA-N 0.000 claims description 26
229910052802 copper Inorganic materials 0.000 claims description 26
239000010949 copper Substances 0.000 claims description 26
229910052700 potassium Inorganic materials 0.000 claims description 24
159000000003 magnesium salts Chemical class 0.000 claims description 23
229910052708 sodium Inorganic materials 0.000 claims description 23
239000011734 sodium Substances 0.000 claims description 23
159000000007 calcium salts Chemical class 0.000 claims description 22
229910052744 lithium Inorganic materials 0.000 claims description 22
BQCADISMDOOEFD-UHFFFAOYSA-N Silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 claims description 21
229910052709 silver Inorganic materials 0.000 claims description 21
239000004332 silver Substances 0.000 claims description 21
125000000217 alkyl group Chemical group 0.000 claims description 20
238000011282 treatment Methods 0.000 claims description 19
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 18
239000011591 potassium Substances 0.000 claims description 18
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 17
206010061218 Inflammation Diseases 0.000 claims description 16
WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims description 16
208000001145 Metabolic Syndrome Diseases 0.000 claims description 16
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229910052794 bromium Inorganic materials 0.000 claims description 14
239000000460 chlorine Substances 0.000 claims description 14
VYZAMTAEIAYCRO-UHFFFAOYSA-N Chromium Chemical compound [Cr] VYZAMTAEIAYCRO-UHFFFAOYSA-N 0.000 claims description 13
229910052788 barium Inorganic materials 0.000 claims description 13
DSAJWYNOEDNPEQ-UHFFFAOYSA-N barium atom Chemical compound [Ba] DSAJWYNOEDNPEQ-UHFFFAOYSA-N 0.000 claims description 13
150000001768 cations Chemical class 0.000 claims description 13
229910052804 chromium Inorganic materials 0.000 claims description 13
239000011651 chromium Substances 0.000 claims description 13
229910017052 cobalt Inorganic materials 0.000 claims description 13
239000010941 cobalt Substances 0.000 claims description 13
GUTLYIVDDKVIGB-UHFFFAOYSA-N cobalt atom Chemical compound [Co] GUTLYIVDDKVIGB-UHFFFAOYSA-N 0.000 claims description 13
WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 claims description 13
229910052759 nickel Inorganic materials 0.000 claims description 13
CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical group [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims description 12
229910052793 cadmium Inorganic materials 0.000 claims description 12
BDOSMKKIYDKNTQ-UHFFFAOYSA-N cadmium atom Chemical compound [Cd] BDOSMKKIYDKNTQ-UHFFFAOYSA-N 0.000 claims description 12
229910052740 iodine Inorganic materials 0.000 claims description 12
238000002156 mixing Methods 0.000 claims description 12
230000008569 process Effects 0.000 claims description 11
229940124597 therapeutic agent Drugs 0.000 claims description 11
150000003751 zinc Chemical class 0.000 claims description 9
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 8
230000003110 anti-inflammatory effect Effects 0.000 claims description 8
238000001914 filtration Methods 0.000 claims description 8
229910052739 hydrogen Inorganic materials 0.000 claims description 8
108010000817 Leuprolide Proteins 0.000 claims description 7
206010012601 diabetes mellitus Diseases 0.000 claims description 7
RGLRXNKKBLIBQS-XNHQSDQCSA-N leuprolide acetate Chemical compound CC(O)=O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 RGLRXNKKBLIBQS-XNHQSDQCSA-N 0.000 claims description 7
229940087857 lupron Drugs 0.000 claims description 7
208000035143 Bacterial infection Diseases 0.000 claims description 6
JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 claims description 6
208000022362 bacterial infectious disease Diseases 0.000 claims description 6
239000003937 drug carrier Substances 0.000 claims description 6
238000004108 freeze drying Methods 0.000 claims description 6
229910052943 magnesium sulfate Inorganic materials 0.000 claims description 6
235000019341 magnesium sulphate Nutrition 0.000 claims description 6
238000001694 spray drying Methods 0.000 claims description 6
208000002874 Acne Vulgaris Diseases 0.000 claims description 5
241000894006 Bacteria Species 0.000 claims description 5
206010000496 acne Diseases 0.000 claims description 5
238000002036 drum drying Methods 0.000 claims description 5
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UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 4
206010020751 Hypersensitivity Diseases 0.000 claims description 4
206010039085 Rhinitis allergic Diseases 0.000 claims description 4
201000010105 allergic rhinitis Diseases 0.000 claims description 4
208000006673 asthma Diseases 0.000 claims description 4
229910000019 calcium carbonate Inorganic materials 0.000 claims description 4
239000001110 calcium chloride Substances 0.000 claims description 4
229910001628 calcium chloride Inorganic materials 0.000 claims description 4
AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims description 4
239000000920 calcium hydroxide Substances 0.000 claims description 4
229910001861 calcium hydroxide Inorganic materials 0.000 claims description 4
208000019622 heart disease Diseases 0.000 claims description 4
229930186147 Cephalosporin Natural products 0.000 claims description 3
230000007815 allergy Effects 0.000 claims description 3
239000003242 anti bacterial agent Substances 0.000 claims description 3
229940124587 cephalosporin Drugs 0.000 claims description 3
150000001780 cephalosporins Chemical class 0.000 claims description 3
SGKRLCUYIXIAHR-AKNGSSGZSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O SGKRLCUYIXIAHR-AKNGSSGZSA-N 0.000 claims description 2
FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 claims description 2
HZZVJAQRINQKSD-UHFFFAOYSA-N Clavulanic acid Natural products OC(=O)C1C(=CCO)OC2CC(=O)N21 HZZVJAQRINQKSD-UHFFFAOYSA-N 0.000 claims description 2
JWCSIUVGFCSJCK-CAVRMKNVSA-N Disodium Moxalactam Chemical compound N([C@]1(OC)C(N2C(=C(CSC=3N(N=NN=3)C)CO[C@@H]21)C(O)=O)=O)C(=O)C(C(O)=O)C1=CC=C(O)C=C1 JWCSIUVGFCSJCK-CAVRMKNVSA-N 0.000 claims description 2
241000590002 Helicobacter pylori Species 0.000 claims description 2
OJMMVQQUTAEWLP-UHFFFAOYSA-N Lincomycin Natural products CN1CC(CCC)CC1C(=O)NC(C(C)O)C1C(O)C(O)C(O)C(SC)O1 OJMMVQQUTAEWLP-UHFFFAOYSA-N 0.000 claims description 2
RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims description 2
241000187479 Mycobacterium tuberculosis Species 0.000 claims description 2
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229930195708 Penicillin V Natural products 0.000 claims description 2
108010040201 Polymyxins Proteins 0.000 claims description 2
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AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 claims description 2
229940098164 augmentin Drugs 0.000 claims description 2
WZPBZJONDBGPKJ-VEHQQRBSSA-N aztreonam Chemical compound O=C1N(S([O-])(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(=N/OC(C)(C)C(O)=O)\C1=CSC([NH3+])=N1 WZPBZJONDBGPKJ-VEHQQRBSSA-N 0.000 claims description 2
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YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims description 2
229960003669 carbenicillin Drugs 0.000 claims description 2
FPPNZSSZRUTDAP-UWFZAAFLSA-N carbenicillin Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)C(C(O)=O)C1=CC=CC=C1 FPPNZSSZRUTDAP-UWFZAAFLSA-N 0.000 claims description 2
229960001668 cefuroxime Drugs 0.000 claims description 2
JFPVXVDWJQMJEE-IZRZKJBUSA-N cefuroxime Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 JFPVXVDWJQMJEE-IZRZKJBUSA-N 0.000 claims description 2
229960002626 clarithromycin Drugs 0.000 claims description 2
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 2
229960003722 doxycycline Drugs 0.000 claims description 2
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OJMMVQQUTAEWLP-KIDUDLJLSA-N lincomycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@@H](C)O)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 OJMMVQQUTAEWLP-KIDUDLJLSA-N 0.000 claims description 2
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VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 claims description 2
229960004023 minocycline Drugs 0.000 claims description 2
GPXLMGHLHQJAGZ-JTDSTZFVSA-N nafcillin Chemical compound C1=CC=CC2=C(C(=O)N[C@@H]3C(N4[C@H](C(C)(C)S[C@@H]43)C(O)=O)=O)C(OCC)=CC=C21 GPXLMGHLHQJAGZ-JTDSTZFVSA-N 0.000 claims description 2
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UWYHMGVUTGAWSP-JKIFEVAISA-N oxacillin Chemical compound N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=CC=CC=C1 UWYHMGVUTGAWSP-JKIFEVAISA-N 0.000 claims description 2
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BPLBGHOLXOTWMN-MBNYWOFBSA-N phenoxymethylpenicillin Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)COC1=CC=CC=C1 BPLBGHOLXOTWMN-MBNYWOFBSA-N 0.000 claims description 2
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LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 claims description 2
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