EA027685B1 - Фармацевтическая композиция с покрытием, содержащая регорафениб - Google Patents

Info

Publication number

EA027685B1

EA027685B1 EA201590520A EA201590520A EA027685B1 EA 027685 B1 EA027685 B1 EA 027685B1 EA 201590520 A EA201590520 A EA 201590520A EA 201590520 A EA201590520 A EA 201590520A EA 027685 B1 EA027685 B1 EA 027685B1

Authority

EA

Eurasian Patent Office

Prior art keywords

regorafenib

dosage form

form according

pharmaceutical composition

polyvinyl alcohol

Prior art date

2012-09-06

Links

• Espacenet
• Global Dossier
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• 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 78
• 239000002138 L01XE21 - Regorafenib Substances 0.000 title claims abstract description 65
• 229960004836 regorafenib Drugs 0.000 title claims abstract description 65
• FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 title claims abstract description 65
• 239000011248 coating agent Substances 0.000 claims abstract description 54
• 238000000576 coating method Methods 0.000 claims abstract description 53
• 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 35
• 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 34
• 229920000642 polymer Polymers 0.000 claims abstract description 30
• 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 26
• 239000002552 dosage form Substances 0.000 claims abstract description 22
• 150000003839 salts Chemical class 0.000 claims abstract description 22
• 239000002207 metabolite Substances 0.000 claims abstract description 9
• 239000012453 solvate Substances 0.000 claims abstract description 9
• -1 hydrate Substances 0.000 claims description 33
• 239000007962 solid dispersion Substances 0.000 claims description 32
• 239000000203 mixture Substances 0.000 claims description 30
• 239000011159 matrix material Substances 0.000 claims description 16
• 239000000126 substance Substances 0.000 claims description 14
• 239000002202 Polyethylene glycol Substances 0.000 claims description 12
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 12
• DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 11
• 229920001223 polyethylene glycol Polymers 0.000 claims description 11
• 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 11
• 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 11
• 239000004480 active ingredient Substances 0.000 claims description 10
• 229920002785 Croscarmellose sodium Polymers 0.000 claims description 9
• 229920001577 copolymer Polymers 0.000 claims description 9
• 229960001681 croscarmellose sodium Drugs 0.000 claims description 9
• 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 9
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• 239000004014 plasticizer Substances 0.000 claims description 8
• 229920000858 Cyclodextrin Polymers 0.000 claims description 6
• DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 6
• FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
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• ZFOZVQLOBQUTQQ-UHFFFAOYSA-N Tributyl citrate Chemical compound CCCCOC(=O)CC(O)(C(=O)OCCCC)CC(=O)OCCCC ZFOZVQLOBQUTQQ-UHFFFAOYSA-N 0.000 claims description 4
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• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
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• 229930091371 Fructose Natural products 0.000 claims description 2
• 239000005715 Fructose Substances 0.000 claims description 2
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• SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims description 2
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• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
• 239000005913 Maltodextrin Substances 0.000 claims description 2
• 229920002774 Maltodextrin Polymers 0.000 claims description 2
• GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims description 2
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