JP2005535730A5 - - Google Patents

Info

Publication number

JP2005535730A5

JP2005535730A5 JP2004548888A JP2004548888A JP2005535730A5 JP 2005535730 A5 JP2005535730 A5 JP 2005535730A5 JP 2004548888 A JP2004548888 A JP 2004548888A JP 2004548888 A JP2004548888 A JP 2004548888A JP 2005535730 A5 JP2005535730 A5 JP 2005535730A5

Authority

JP

Japan

Prior art keywords

formulation

cationic

mol

stabilizer

cationic liposome

Prior art date

2003-06-26

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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• 239000000203 mixture Substances 0.000 claims description 57
• 238000009472 formulation Methods 0.000 claims description 56
• 239000002502 liposome Substances 0.000 claims description 50
• 125000002091 cationic group Chemical group 0.000 claims description 46
• 238000000034 method Methods 0.000 claims description 20
• 239000003381 stabilizer Substances 0.000 claims description 20
• OGQYPPBGSLZBEG-UHFFFAOYSA-N dimethyl(dioctadecyl)azanium Chemical compound CCCCCCCCCCCCCCCCCC[N+](C)(C)CCCCCCCCCCCCCCCCCC OGQYPPBGSLZBEG-UHFFFAOYSA-N 0.000 claims description 16
• 229940123237 Taxane Drugs 0.000 claims description 14
• 229960001592 paclitaxel Drugs 0.000 claims description 14
• 239000007864 aqueous solution Substances 0.000 claims description 13
• 239000000243 solution Substances 0.000 claims description 13
• DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims description 12
• 239000012736 aqueous medium Substances 0.000 claims description 11
• -1 cationic lipid Chemical class 0.000 claims description 11
• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 9
• 229930012538 Paclitaxel Natural products 0.000 claims description 9
• 229960003668 docetaxel Drugs 0.000 claims description 9
• RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 9
• 150000001875 compounds Chemical class 0.000 claims description 7
• 239000003960 organic solvent Substances 0.000 claims description 6
• 238000000108 ultra-filtration Methods 0.000 claims description 4
• 239000002245 particle Substances 0.000 claims description 3
• 238000002360 preparation method Methods 0.000 claims 15
• 238000004519 manufacturing process Methods 0.000 claims 9
• 229930013356 epothilone Natural products 0.000 claims 2
• 239000002671 adjuvant Substances 0.000 claims 1
• 150000001720 carbohydrates Chemical class 0.000 claims 1
• 150000001768 cations Chemical class 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 claims 1
• 150000003883 epothilone derivatives Chemical class 0.000 claims 1
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 150000002632 lipids Chemical class 0.000 claims 1
• 239000012528 membrane Substances 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 239000002904 solvent Substances 0.000 claims 1
• 125000002730 succinyl group Chemical group C(CCC(=O)*)(=O)* 0.000 claims 1
• 230000001172 regenerating effect Effects 0.000 description 2
• 238000011146 sterile filtration Methods 0.000 description 2
• KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 description 1
• 229940127093 camptothecin Drugs 0.000 description 1
• VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 description 1