JP2012512147A5 - - Google Patents

Info

Publication number

JP2012512147A5

JP2012512147A5 JP2011540134A JP2011540134A JP2012512147A5 JP 2012512147 A5 JP2012512147 A5 JP 2012512147A5 JP 2011540134 A JP2011540134 A JP 2011540134A JP 2011540134 A JP2011540134 A JP 2011540134A JP 2012512147 A5 JP2012512147 A5 JP 2012512147A5

Authority

JP

Japan

Prior art keywords

preparation according

depot preparation

depot

polymer

microparticles

Prior art date

2009-12-14

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

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• Global Dossier
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• 239000010419 fine particle Substances 0.000 claims description 10
• 229920000642 polymer Polymers 0.000 claims description 10
• 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 8
• 206010028980 Neoplasm Diseases 0.000 claims description 6
• 239000004480 active ingredient Substances 0.000 claims description 6
• DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims description 5
• 108010016076 Octreotide Proteins 0.000 claims description 5
• 239000011859 microparticle Substances 0.000 claims description 5
• 229960002700 octreotide Drugs 0.000 claims description 5
• 150000003839 salts Chemical class 0.000 claims description 5
• 206010000599 Acromegaly Diseases 0.000 claims description 3
• 102000055135 Vasoactive Intestinal Peptide Human genes 0.000 claims description 3
• 108010003205 Vasoactive Intestinal Peptide Proteins 0.000 claims description 3
• 208000019493 atypical carcinoid tumor Diseases 0.000 claims description 3
• 238000011010 flushing procedure Methods 0.000 claims description 3
• VBUWHHLIZKOSMS-RIWXPGAOSA-N invicorp Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 VBUWHHLIZKOSMS-RIWXPGAOSA-N 0.000 claims description 3
• 230000007774 longterm Effects 0.000 claims description 3
• 238000009115 maintenance therapy Methods 0.000 claims description 3
• 208000026775 severe diarrhea Diseases 0.000 claims description 3
• 230000002378 acidificating effect Effects 0.000 claims description 2
• 230000002744 anti-aggregatory effect Effects 0.000 claims description 2
• 239000008135 aqueous vehicle Substances 0.000 claims description 2
• 239000003795 chemical substances by application Substances 0.000 claims description 2
• 150000002148 esters Chemical class 0.000 claims description 2
• 239000007943 implant Substances 0.000 claims description 2
• 239000007787 solid Substances 0.000 claims description 2
• 239000003981 vehicle Substances 0.000 claims description 2
• 239000003405 delayed action preparation Substances 0.000 claims 9
• 238000009472 formulation Methods 0.000 claims 3
• 239000000203 mixture Substances 0.000 claims 3
• KFWJVABDRRDUHY-XJQYZYIXSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical group C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1.C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 KFWJVABDRRDUHY-XJQYZYIXSA-N 0.000 claims 1
• 229920001577 copolymer Polymers 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000013022 formulation composition Substances 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 description 23
• 238000013268 sustained release Methods 0.000 description 6
• 239000012730 sustained-release form Substances 0.000 description 6
• 238000000034 method Methods 0.000 description 4
• 230000036470 plasma concentration Effects 0.000 description 3
• 239000008346 aqueous phase Substances 0.000 description 2
• 239000012074 organic phase Substances 0.000 description 2
• 239000003791 organic solvent mixture Substances 0.000 description 2
• RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 description 1
• 241000283973 Oryctolagus cuniculus Species 0.000 description 1
• 239000008186 active pharmaceutical agent Substances 0.000 description 1
• 239000003708 ampul Substances 0.000 description 1
• 229940088679 drug related substance Drugs 0.000 description 1
• 238000001035 drying Methods 0.000 description 1
• 230000001804 emulsifying effect Effects 0.000 description 1
• 239000000839 emulsion Substances 0.000 description 1
• JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 description 1
• 238000002156 mixing Methods 0.000 description 1
• 229920002959 polymer blend Polymers 0.000 description 1
• 229940071643 prefilled syringe Drugs 0.000 description 1
• 238000000935 solvent evaporation Methods 0.000 description 1
• 238000000638 solvent extraction Methods 0.000 description 1
• 239000003381 stabilizer Substances 0.000 description 1
• 230000001225 therapeutic effect Effects 0.000 description 1
• 238000005406 washing Methods 0.000 description 1