JP2014501781A5 - - Google Patents

Info

Publication number

JP2014501781A5

JP2014501781A5 JP2013548475A JP2013548475A JP2014501781A5 JP 2014501781 A5 JP2014501781 A5 JP 2014501781A5 JP 2013548475 A JP2013548475 A JP 2013548475A JP 2013548475 A JP2013548475 A JP 2013548475A JP 2014501781 A5 JP2014501781 A5 JP 2014501781A5

Authority

JP

Japan

Prior art keywords

solution

vancomycin

peg

mannitol

weight

Prior art date

2012-01-04

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
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• 238000000034 method Methods 0.000 claims description 26
• 108010059993 Vancomycin Proteins 0.000 claims description 23
• 239000000243 solution Substances 0.000 claims description 23
• 239000002202 Polyethylene glycol Substances 0.000 claims description 19
• 229920001223 polyethylene glycol Polymers 0.000 claims description 19
• 229960001572 vancomycin hydrochloride Drugs 0.000 claims description 14
• LCTORFDMHNKUSG-XTTLPDOESA-N vancomycin monohydrochloride Chemical compound Cl.O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)[C@H](O)[C@H](C)O1 LCTORFDMHNKUSG-XTTLPDOESA-N 0.000 claims description 14
• 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 claims description 11
• 229930195725 Mannitol Natural products 0.000 claims description 11
• 235000010355 mannitol Nutrition 0.000 claims description 11
• 239000000594 mannitol Substances 0.000 claims description 11
• 239000000843 powder Substances 0.000 claims description 10
• 229960003165 vancomycin Drugs 0.000 claims description 9
• MYPYJXKWCTUITO-LYRMYLQWSA-N vancomycin Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-N 0.000 claims description 9
• MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims description 9
• 238000001694 spray drying Methods 0.000 claims description 8
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
• 238000010253 intravenous injection Methods 0.000 claims description 6
• 239000007979 citrate buffer Substances 0.000 claims description 5
• 239000008194 pharmaceutical composition Substances 0.000 claims description 4
• 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims description 2
• MYPYJXKWCTUITO-KIIOPKALSA-N chembl3301825 Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)C(O)[C@H](C)O1 MYPYJXKWCTUITO-KIIOPKALSA-N 0.000 claims description 2
• 239000007864 aqueous solution Substances 0.000 claims 2
• 238000005507 spraying Methods 0.000 claims 2
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 239000000203 mixture Substances 0.000 description 14
• 238000009472 formulation Methods 0.000 description 13
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
• 239000008215 water for injection Substances 0.000 description 6
• 239000007921 spray Substances 0.000 description 4
• 239000008186 active pharmaceutical agent Substances 0.000 description 3
• 230000002349 favourable effect Effects 0.000 description 1
• 238000004128 high performance liquid chromatography Methods 0.000 description 1
• 238000004806 packaging method and process Methods 0.000 description 1
• 239000000546 pharmaceutical excipient Substances 0.000 description 1
• 239000002798 polar solvent Substances 0.000 description 1
• 238000012430 stability testing Methods 0.000 description 1
• 230000001954 sterilising effect Effects 0.000 description 1
• 238000004659 sterilization and disinfection Methods 0.000 description 1
• 238000012360 testing method Methods 0.000 description 1