JP2011526288A5 - - Google Patents

Info

Publication number

JP2011526288A5

JP2011526288A5 JP2011516610A JP2011516610A JP2011526288A5 JP 2011526288 A5 JP2011526288 A5 JP 2011526288A5 JP 2011516610 A JP2011516610 A JP 2011516610A JP 2011516610 A JP2011516610 A JP 2011516610A JP 2011526288 A5 JP2011526288 A5 JP 2011526288A5

Authority

JP

Japan

Prior art keywords

implantable device

delivery

polypeptide

surface area

agent

Prior art date

2009-06-24

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 14
• 239000000203 mixture Substances 0.000 claims 14
• 229920001184 polypeptide Polymers 0.000 claims 13
• 102000004196 processed proteins & peptides Human genes 0.000 claims 13
• 108090000765 processed proteins & peptides Proteins 0.000 claims 13
• 239000003795 chemical substances by application Substances 0.000 claims 11
• 238000002716 delivery method Methods 0.000 claims 10
• KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 9
• 238000009472 formulation Methods 0.000 claims 9
• GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 8
• 239000007787 solid Substances 0.000 claims 7
• DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical class C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 6
• 238000004519 manufacturing process Methods 0.000 claims 6
• 230000001225 therapeutic effect Effects 0.000 claims 6
• BQZJOQXSCSZQPS-UHFFFAOYSA-N 2-methoxy-1,2-diphenylethanone Chemical compound C=1C=CC=CC=1C(OC)C(=O)C1=CC=CC=C1 BQZJOQXSCSZQPS-UHFFFAOYSA-N 0.000 claims 5
• DBCAQXHNJOFNGC-UHFFFAOYSA-N 4-bromo-1,1,1-trifluorobutane Chemical compound FC(F)(F)CCCBr DBCAQXHNJOFNGC-UHFFFAOYSA-N 0.000 claims 5
• WOBHKFSMXKNTIM-UHFFFAOYSA-N Hydroxyethyl methacrylate Chemical compound CC(=C)C(=O)OCCO WOBHKFSMXKNTIM-UHFFFAOYSA-N 0.000 claims 5
• 229920001577 copolymer Polymers 0.000 claims 5
• STVZJERGLQHEKB-UHFFFAOYSA-N ethylene glycol dimethacrylate Substances CC(=C)C(=O)OCCOC(=O)C(C)=C STVZJERGLQHEKB-UHFFFAOYSA-N 0.000 claims 5
• 229930003427 Vitamin E Natural products 0.000 claims 4
• WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 4
• 239000000463 material Substances 0.000 claims 4
• 239000011159 matrix material Substances 0.000 claims 4
• 239000000178 monomer Substances 0.000 claims 4
• 229940046009 vitamin E Drugs 0.000 claims 4
• 235000019165 vitamin E Nutrition 0.000 claims 4
• 239000011709 vitamin E Substances 0.000 claims 4
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
• NOBYOEQUFMGXBP-UHFFFAOYSA-N (4-tert-butylcyclohexyl) (4-tert-butylcyclohexyl)oxycarbonyloxy carbonate Chemical compound C1CC(C(C)(C)C)CCC1OC(=O)OOC(=O)OC1CCC(C(C)(C)C)CC1 NOBYOEQUFMGXBP-UHFFFAOYSA-N 0.000 claims 3
• HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 3
• 108010011459 Exenatide Proteins 0.000 claims 3
• 235000021355 Stearic acid Nutrition 0.000 claims 3
• 229960001519 exenatide Drugs 0.000 claims 3
• 239000002736 nonionic surfactant Substances 0.000 claims 3
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 3
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 3
• 239000008117 stearic acid Substances 0.000 claims 3
• 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
• 229920001213 Polysorbate 20 Polymers 0.000 claims 2
• 239000004147 Sorbitan trioleate Substances 0.000 claims 2
• PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 claims 2
• AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims 2
• SFNALCNOMXIBKG-UHFFFAOYSA-N ethylene glycol monododecyl ether Chemical compound CCCCCCCCCCCCOCCO SFNALCNOMXIBKG-UHFFFAOYSA-N 0.000 claims 2
• 238000006116 polymerization reaction Methods 0.000 claims 2
• -1 polyoxyethylene Polymers 0.000 claims 2
• 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 2
• 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 2
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 2
• 229920000053 polysorbate 80 Polymers 0.000 claims 2
• 235000019337 sorbitan trioleate Nutrition 0.000 claims 2
• 229960000391 sorbitan trioleate Drugs 0.000 claims 2
• 238000013268 sustained release Methods 0.000 claims 2
• 239000012730 sustained-release form Substances 0.000 claims 2
• 239000000080 wetting agent Substances 0.000 claims 2
• OKKRPWIIYQTPQF-UHFFFAOYSA-N Trimethylolpropane trimethacrylate Chemical compound CC(=C)C(=O)OCC(CC)(COC(=O)C(C)=C)COC(=O)C(C)=C OKKRPWIIYQTPQF-UHFFFAOYSA-N 0.000 claims 1
• 150000001298 alcohols Chemical class 0.000 claims 1
• 239000003125 aqueous solvent Substances 0.000 claims 1
• 239000003638 chemical reducing agent Substances 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 238000013270 controlled release Methods 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• 230000002641 glycemic effect Effects 0.000 claims 1
• 239000000017 hydrogel Substances 0.000 claims 1
• 239000003960 organic solvent Substances 0.000 claims 1
• 239000007800 oxidant agent Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 239000000126 substance Substances 0.000 claims 1