JP2015522001A5 - - Google Patents

Info

Publication number

JP2015522001A5

JP2015522001A5 JP2015519379A JP2015519379A JP2015522001A5 JP 2015522001 A5 JP2015522001 A5 JP 2015522001A5 JP 2015519379 A JP2015519379 A JP 2015519379A JP 2015519379 A JP2015519379 A JP 2015519379A JP 2015522001 A5 JP2015522001 A5 JP 2015522001A5

Authority

JP

Japan

Prior art keywords

poly

repeating units

biodegradable

drug delivery

ethylene glycol

Prior art date

2013-06-27

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
• Discuss

• 239000000203 mixture Substances 0.000 claims description 49
• 239000004480 active ingredient Substances 0.000 claims description 25
• RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims description 16
• LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 claims description 8
• 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 description 8
• 108010036949 Cyclosporine Proteins 0.000 claims description 8
• 229960001265 ciclosporin Drugs 0.000 claims description 8
• 229930182912 cyclosporin Natural products 0.000 claims description 8
• PSGAAPLEWMOORI-PEINSRQWSA-N medroxyprogesterone acetate Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2CC[C@]2(C)[C@@](OC(C)=O)(C(C)=O)CC[C@H]21 PSGAAPLEWMOORI-PEINSRQWSA-N 0.000 claims description 8
• 229960002985 medroxyprogesterone acetate Drugs 0.000 claims description 8
• 229960003387 progesterone Drugs 0.000 claims description 8
• 239000000186 progesterone Substances 0.000 claims description 8
• 239000002904 solvent Substances 0.000 claims description 7
• 229920000747 poly(lactic acid) Polymers 0.000 claims 39
• 238000012377 drug delivery Methods 0.000 claims 29
• 230000002209 hydrophobic effect Effects 0.000 claims 20
• 229920000428 triblock copolymer Polymers 0.000 claims 17
• 229920001427 mPEG Polymers 0.000 claims 13
• 229920001223 polyethylene glycol Polymers 0.000 claims 13
• 239000004626 polylactic acid Substances 0.000 claims 13
• 229920000359 diblock copolymer Polymers 0.000 claims 11
• 238000000034 method Methods 0.000 claims 11
• WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 claims 7
• AZSNMRSAGSSBNP-UHFFFAOYSA-N 22,23-dihydroavermectin B1a Natural products C1CC(C)C(C(C)CC)OC21OC(CC=C(C)C(OC1OC(C)C(OC3OC(C)C(O)C(OC)C3)C(OC)C1)C(C)C=CC=C1C3(C(C(=O)O4)C=C(C)C(O)C3OC1)O)CC4C2 AZSNMRSAGSSBNP-UHFFFAOYSA-N 0.000 claims 7
• SPBDXSGPUHCETR-JFUDTMANSA-N 8883yp2r6d Chemical compound O1[C@@H](C)[C@H](O)[C@@H](OC)C[C@@H]1O[C@@H]1[C@@H](OC)C[C@H](O[C@@H]2C(=C/C[C@@H]3C[C@@H](C[C@@]4(O[C@@H]([C@@H](C)CC4)C(C)C)O3)OC(=O)[C@@H]3C=C(C)[C@@H](O)[C@H]4OC\C([C@@]34O)=C/C=C/[C@@H]2C)/C)O[C@H]1C.C1C[C@H](C)[C@@H]([C@@H](C)CC)O[C@@]21O[C@H](C\C=C(C)\[C@@H](O[C@@H]1O[C@@H](C)[C@H](O[C@@H]3O[C@@H](C)[C@H](O)[C@@H](OC)C3)[C@@H](OC)C1)[C@@H](C)\C=C\C=C/1[C@]3([C@H](C(=O)O4)C=C(C)[C@@H](O)[C@H]3OC\1)O)C[C@H]4C2 SPBDXSGPUHCETR-JFUDTMANSA-N 0.000 claims 7
• 229960002418 ivermectin Drugs 0.000 claims 7
• 229960004400 levonorgestrel Drugs 0.000 claims 7
• 229920002959 polymer blend Polymers 0.000 claims 7
• RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims 7
• 229960001534 risperidone Drugs 0.000 claims 7
• 229940079593 drug Drugs 0.000 claims 6
• 239000003814 drug Substances 0.000 claims 6
• 239000003960 organic solvent Substances 0.000 claims 6
• 229960003150 bupivacaine Drugs 0.000 claims 5
• LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 4
• IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 4
• JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 4
• -1 lactyl Chemical group 0.000 claims 4
• 229920001400 block copolymer Polymers 0.000 claims 2
• 150000002148 esters Chemical class 0.000 claims 2
• 238000001704 evaporation Methods 0.000 claims 2
• 235000014655 lactic acid Nutrition 0.000 claims 2
• 239000004310 lactic acid Substances 0.000 claims 2
• 239000000725 suspension Substances 0.000 claims 2
• 239000007943 implant Substances 0.000 claims 1
• 238000002347 injection Methods 0.000 claims 1
• 239000007924 injection Substances 0.000 claims 1
• 239000000243 solution Substances 0.000 claims 1
• 229930105110 Cyclosporin A Natural products 0.000 description 1