JP2007502296A5 - - Google Patents

Info

Publication number

JP2007502296A5

JP2007502296A5 JP2006523385A JP2006523385A JP2007502296A5 JP 2007502296 A5 JP2007502296 A5 JP 2007502296A5 JP 2006523385 A JP2006523385 A JP 2006523385A JP 2006523385 A JP2006523385 A JP 2006523385A JP 2007502296 A5 JP2007502296 A5 JP 2007502296A5

Authority

JP

Japan

Prior art keywords

robust

group

active ingredient

weight

pharmacologically acceptable

Prior art date

2004-08-11

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.)

Pending

Links

• Espacenet
• Global Dossier
• Discuss

• 239000008188 pellet Substances 0.000 claims 39
• 239000004480 active ingredient Substances 0.000 claims 21
• 239000002552 dosage form Substances 0.000 claims 16
• 229940079593 drug Drugs 0.000 claims 15
• 239000003814 drug Substances 0.000 claims 15
• 239000003623 enhancer Substances 0.000 claims 12
• 238000010521 absorption reaction Methods 0.000 claims 10
• 239000003795 chemical substances by application Substances 0.000 claims 10
• 238000011143 downstream manufacturing Methods 0.000 claims 10
• 238000000034 method Methods 0.000 claims 10
• 239000000825 pharmaceutical preparation Substances 0.000 claims 8
• 238000007906 compression Methods 0.000 claims 7
• 230000006835 compression Effects 0.000 claims 7
• 238000004519 manufacturing process Methods 0.000 claims 7
• 239000004094 surface-active agent Substances 0.000 claims 7
• 229930182555 Penicillin Natural products 0.000 claims 6
• LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin 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=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 claims 6
• 229960003022 amoxicillin Drugs 0.000 claims 6
• 229940126534 drug product Drugs 0.000 claims 6
• LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims 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 5
• -1 compression Substances 0.000 claims 5
• 229940049954 penicillin Drugs 0.000 claims 5
• 229930186147 Cephalosporin Natural products 0.000 claims 4
• ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin 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)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 claims 4
• 229940124587 cephalosporin Drugs 0.000 claims 4
• 150000001780 cephalosporins Chemical class 0.000 claims 4
• MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 claims 4
• 239000011248 coating agent Substances 0.000 claims 4
• 238000000576 coating method Methods 0.000 claims 4
• XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims 4
• 238000001035 drying Methods 0.000 claims 4
• 238000001125 extrusion Methods 0.000 claims 4
• 239000012530 fluid Substances 0.000 claims 4
• 229940124307 fluoroquinolone Drugs 0.000 claims 4
• 239000003120 macrolide antibiotic agent Substances 0.000 claims 4
• 238000005563 spheronization Methods 0.000 claims 4
• 229940124530 sulfonamide Drugs 0.000 claims 4
• 150000003456 sulfonamides Chemical class 0.000 claims 4
• UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 4
• 238000005550 wet granulation Methods 0.000 claims 4
• SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims 3
• 239000004098 Tetracycline Substances 0.000 claims 3
• 239000008137 solubility enhancer Substances 0.000 claims 3
• 239000002904 solvent Substances 0.000 claims 3
• 235000019364 tetracycline Nutrition 0.000 claims 3
• 229930101283 tetracycline Natural products 0.000 claims 3
• 150000003522 tetracyclines Chemical class 0.000 claims 3
• 150000003952 β-lactams Chemical class 0.000 claims 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 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 2
• AVFZOVWCLRSYKC-UHFFFAOYSA-N 1-methylpyrrolidine Chemical group CN1CCCC1 AVFZOVWCLRSYKC-UHFFFAOYSA-N 0.000 claims 2
• 239000004215 Carbon black (E152) Substances 0.000 claims 2
• 239000004099 Chlortetracycline Substances 0.000 claims 2
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
• AHVYPIQETPWLSZ-UHFFFAOYSA-N N-methyl-pyrrolidine Natural products CN1CC=CC1 AHVYPIQETPWLSZ-UHFFFAOYSA-N 0.000 claims 2
• NHUHCSRWZMLRLA-UHFFFAOYSA-N Sulfisoxazole Chemical compound CC1=NOC(NS(=O)(=O)C=2C=CC(N)=CC=2)=C1C NHUHCSRWZMLRLA-UHFFFAOYSA-N 0.000 claims 2
• OKBVVJOGVLARMR-QSWIMTSFSA-N cefixime Chemical compound S1C(N)=NC(C(=N\OCC(O)=O)\C(=O)N[C@@H]2C(N3C(=C(C=C)CS[C@@H]32)C(O)=O)=O)=C1 OKBVVJOGVLARMR-QSWIMTSFSA-N 0.000 claims 2
• 229960002129 cefixime Drugs 0.000 claims 2
• WYUSVOMTXWRGEK-HBWVYFAYSA-N cefpodoxime Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC)C(O)=O)C(=O)C(=N/OC)\C1=CSC(N)=N1 WYUSVOMTXWRGEK-HBWVYFAYSA-N 0.000 claims 2
• 229960005090 cefpodoxime Drugs 0.000 claims 2
• CYDMQBQPVICBEU-UHFFFAOYSA-N chlorotetracycline Natural products C1=CC(Cl)=C2C(O)(C)C3CC4C(N(C)C)C(O)=C(C(N)=O)C(=O)C4(O)C(O)=C3C(=O)C2=C1O CYDMQBQPVICBEU-UHFFFAOYSA-N 0.000 claims 2
• 229960004475 chlortetracycline Drugs 0.000 claims 2
• CYDMQBQPVICBEU-XRNKAMNCSA-N chlortetracycline Chemical compound C1=CC(Cl)=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O CYDMQBQPVICBEU-XRNKAMNCSA-N 0.000 claims 2
• 235000019365 chlortetracycline Nutrition 0.000 claims 2
• 229960003405 ciprofloxacin Drugs 0.000 claims 2
• 229960002626 clarithromycin Drugs 0.000 claims 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 2
• 230000003111 delayed effect Effects 0.000 claims 2
• YFAGHNZHGGCZAX-JKIFEVAISA-N dicloxacillin 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=C(Cl)C=CC=C1Cl YFAGHNZHGGCZAX-JKIFEVAISA-N 0.000 claims 2
• 229960001585 dicloxacillin Drugs 0.000 claims 2
• 229940075557 diethylene glycol monoethyl ether Drugs 0.000 claims 2
• 229960003722 doxycycline Drugs 0.000 claims 2
• 230000002708 enhancing effect Effects 0.000 claims 2
• 229960003276 erythromycin Drugs 0.000 claims 2
• 229930195733 hydrocarbon Natural products 0.000 claims 2
• 150000002430 hydrocarbons Chemical class 0.000 claims 2
• 230000002209 hydrophobic effect Effects 0.000 claims 2
• 239000012729 immediate-release (IR) formulation Substances 0.000 claims 2
• 150000004668 long chain fatty acids Chemical class 0.000 claims 2
• 229960004023 minocycline Drugs 0.000 claims 2
• 239000002736 nonionic surfactant Substances 0.000 claims 2
• 229960001180 norfloxacin Drugs 0.000 claims 2
• OGJPXUAPXNRGGI-UHFFFAOYSA-N norfloxacin Chemical compound C1=C2N(CC)C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNCC1 OGJPXUAPXNRGGI-UHFFFAOYSA-N 0.000 claims 2
• 229940127557 pharmaceutical product Drugs 0.000 claims 2
• 238000002360 preparation method Methods 0.000 claims 2
• 239000012744 reinforcing agent Substances 0.000 claims 2
• 150000004666 short chain fatty acids Chemical class 0.000 claims 2
• SEEPANYCNGTZFQ-UHFFFAOYSA-N sulfadiazine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)NC1=NC=CC=N1 SEEPANYCNGTZFQ-UHFFFAOYSA-N 0.000 claims 2
• 229960004306 sulfadiazine Drugs 0.000 claims 2
• 229960000654 sulfafurazole Drugs 0.000 claims 2
• 229960002180 tetracycline Drugs 0.000 claims 2
• NWXMGUDVXFXRIG-WESIUVDSSA-N (4s,4as,5as,6s,12ar)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carboxamide Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]4(O)C(=O)C3=C(O)C2=C1O NWXMGUDVXFXRIG-WESIUVDSSA-N 0.000 claims 1
• 229940041033 macrolides Drugs 0.000 claims 1
• 239000002831 pharmacologic agent Substances 0.000 claims 1
• 238000009490 roller compaction Methods 0.000 claims 1
• 229940040944 tetracyclines Drugs 0.000 claims 1