JPWO2021224901A5 - - Google Patents

Info

Publication number

JPWO2021224901A5

JPWO2021224901A5 JP2024509421A JP2024509421A JPWO2021224901A5 JP WO2021224901 A5 JPWO2021224901 A5 JP WO2021224901A5 JP 2024509421 A JP2024509421 A JP 2024509421A JP 2024509421 A JP2024509421 A JP 2024509421A JP WO2021224901 A5 JPWO2021224901 A5 JP WO2021224901A5

Authority

JP

Japan

Prior art keywords

formulation

cyclosporine

weight

stable

nanomicelle

Prior art date

2024-10-16

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.)

Pending

Links

• Espacenet
• Global Dossier
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• 239000000203 mixture Substances 0.000 claims 47
• 238000009472 formulation Methods 0.000 claims 33
• PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 21
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 18
• 108010036949 Cyclosporine Proteins 0.000 claims 15
• 229960001265 ciclosporin Drugs 0.000 claims 15
• 229930182912 cyclosporin Natural products 0.000 claims 15
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 12
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 12
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 12
• 239000008215 water for injection Substances 0.000 claims 12
• 238000000034 method Methods 0.000 claims 10
• WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 6
• 229920002675 Polyoxyl Polymers 0.000 claims 6
• 239000008186 active pharmaceutical agent Substances 0.000 claims 6
• 239000004359 castor oil Substances 0.000 claims 6
• 235000019438 castor oil Nutrition 0.000 claims 6
• BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims 6
• ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 6
• 229920004914 octoxynol-40 Polymers 0.000 claims 6
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 6
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 6
• 229940069328 povidone Drugs 0.000 claims 6
• 239000011780 sodium chloride Substances 0.000 claims 6
• AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims 6
• 229940061607 dibasic sodium phosphate Drugs 0.000 claims 4
• 238000004090 dissolution Methods 0.000 claims 3
• 229910000397 disodium phosphate Inorganic materials 0.000 claims 2
• 235000019800 disodium phosphate Nutrition 0.000 claims 2
• -1 The formulation Chemical compound 0.000 claims 1
• 229940045641 monobasic sodium phosphate Drugs 0.000 claims 1
• 229910000403 monosodium phosphate Inorganic materials 0.000 claims 1
• 235000019799 monosodium phosphate Nutrition 0.000 claims 1
• 238000003756 stirring Methods 0.000 claims 1