JP2015044823A5 - - Google Patents

Info

Publication number

JP2015044823A5

JP2015044823A5 JP2014207464A JP2014207464A JP2015044823A5 JP 2015044823 A5 JP2015044823 A5 JP 2015044823A5 JP 2014207464 A JP2014207464 A JP 2014207464A JP 2014207464 A JP2014207464 A JP 2014207464A JP 2015044823 A5 JP2015044823 A5 JP 2015044823A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

microparticles

composition according

plga

aggregating agent

Prior art date

2014-10-08

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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• 239000008194 pharmaceutical composition Substances 0.000 claims description 16
• 239000011859 microparticle Substances 0.000 claims description 14
• 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims description 13
• 239000000203 mixture Substances 0.000 claims description 7
• 229920000642 polymer Polymers 0.000 claims description 7
• 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 3
• 108010016076 Octreotide Proteins 0.000 claims description 3
• 239000010419 fine particle Substances 0.000 claims description 3
• 229960002700 octreotide Drugs 0.000 claims description 3
• 239000003795 chemical substances by application Substances 0.000 claims 7
• 230000002744 anti-aggregatory effect Effects 0.000 claims 6
• HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 4
• RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims 3
• JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims 3
• 238000004519 manufacturing process Methods 0.000 claims 3
• 239000000178 monomer Substances 0.000 claims 3
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 239000004480 active ingredient Substances 0.000 claims 2
• 239000008346 aqueous phase Substances 0.000 claims 2
• 238000002156 mixing Methods 0.000 claims 2
• 239000012074 organic phase Substances 0.000 claims 2
• 239000003791 organic solvent mixture Substances 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• 206010000599 Acromegaly Diseases 0.000 claims 1
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
• 206010012735 Diarrhoea Diseases 0.000 claims 1
• 229930195725 Mannitol Natural products 0.000 claims 1
• 102000055135 Vasoactive Intestinal Peptide Human genes 0.000 claims 1
• 108010003205 Vasoactive Intestinal Peptide Proteins 0.000 claims 1
• 239000003708 ampul Substances 0.000 claims 1
• 239000008135 aqueous vehicle Substances 0.000 claims 1
• 208000019493 atypical carcinoid tumor Diseases 0.000 claims 1
• 238000001035 drying Methods 0.000 claims 1
• 230000009977 dual effect Effects 0.000 claims 1
• 239000000839 emulsion Substances 0.000 claims 1
• 238000011010 flushing procedure Methods 0.000 claims 1
• 238000005469 granulation Methods 0.000 claims 1
• 230000003179 granulation Effects 0.000 claims 1
• 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 1
• 230000007774 longterm Effects 0.000 claims 1
• 238000009115 maintenance therapy Methods 0.000 claims 1
• 239000000594 mannitol Substances 0.000 claims 1
• 235000010355 mannitol Nutrition 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 229920000747 poly(lactic acid) Polymers 0.000 claims 1
• 230000005855 radiation Effects 0.000 claims 1
• 238000000935 solvent evaporation Methods 0.000 claims 1
• 238000000638 solvent extraction Methods 0.000 claims 1
• 239000003381 stabilizer Substances 0.000 claims 1
• 238000013268 sustained release Methods 0.000 claims 1
• 239000012730 sustained-release form Substances 0.000 claims 1
• 239000003981 vehicle Substances 0.000 claims 1
• 238000005406 washing Methods 0.000 claims 1
• 229920002959 polymer blend Polymers 0.000 description 3
• 239000007943 implant Substances 0.000 description 2
• 238000009472 formulation Methods 0.000 description 1
• 239000006104 solid solution Substances 0.000 description 1
• 239000000725 suspension Substances 0.000 description 1