JP2018514534A5 - - Google Patents

Info

Publication number

JP2018514534A5

JP2018514534A5 JP2017555791A JP2017555791A JP2018514534A5 JP 2018514534 A5 JP2018514534 A5 JP 2018514534A5 JP 2017555791 A JP2017555791 A JP 2017555791A JP 2017555791 A JP2017555791 A JP 2017555791A JP 2018514534 A5 JP2018514534 A5 JP 2018514534A5

Authority

JP

Japan

Prior art keywords

composition

particles

pharmaceutically acceptable

less

diameter

Prior art date

2016-04-26

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 73
• 239000002245 particle Substances 0.000 claims description 36
• 229960001601 obeticholic acid Drugs 0.000 claims description 32
• ZXERDUOLZKYMJM-ZWECCWDJSA-N obeticholic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)CCC(O)=O)CC[C@H]21 ZXERDUOLZKYMJM-ZWECCWDJSA-N 0.000 claims description 32
• 150000001413 amino acids Chemical class 0.000 claims description 23
• 150000002148 esters Chemical class 0.000 claims description 23
• 150000003839 salts Chemical class 0.000 claims description 23
• 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 11
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 8
• 208000019423 liver disease Diseases 0.000 claims description 7
• 238000000034 method Methods 0.000 claims description 7
• 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 6
• 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 6
• 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 6
• 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 6
• 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 5
• 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 5
• 239000008108 microcrystalline cellulose Substances 0.000 claims description 5
• 229940016286 microcrystalline cellulose Drugs 0.000 claims description 5
• 229920000080 bile acid sequestrant Polymers 0.000 claims description 4
• 239000003814 drug Substances 0.000 claims description 4
• 238000004519 manufacturing process Methods 0.000 claims description 4
• 229940124531 pharmaceutical excipient Drugs 0.000 claims description 4
• RUDATBOHQWOJDD-UHFFFAOYSA-N (3beta,5beta,7alpha)-3,7-Dihydroxycholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RUDATBOHQWOJDD-UHFFFAOYSA-N 0.000 claims description 3
• 208000022309 Alcoholic Liver disease Diseases 0.000 claims description 3
• 208000005176 Hepatitis C Diseases 0.000 claims description 3
• 208000019425 cirrhosis of liver Diseases 0.000 claims description 3
• 239000000835 fiber Substances 0.000 claims description 3
• 208000010710 hepatitis C virus infection Diseases 0.000 claims description 3
• 238000010902 jet-milling Methods 0.000 claims description 3
• 230000000750 progressive effect Effects 0.000 claims description 3
• 208000010157 sclerosing cholangitis Diseases 0.000 claims description 3
• RUDATBOHQWOJDD-UZVSRGJWSA-N ursodeoxycholic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-UZVSRGJWSA-N 0.000 claims description 3
• 229960001661 ursodiol Drugs 0.000 claims description 3
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
• 206010067125 Liver injury Diseases 0.000 claims description 2
• 239000003795 chemical substances by application Substances 0.000 claims description 2
• 231100000234 hepatic damage Toxicity 0.000 claims description 2
• 230000008818 liver damage Effects 0.000 claims description 2
• 229940079832 sodium starch glycolate Drugs 0.000 claims description 2
• 229920003109 sodium starch glycolate Polymers 0.000 claims description 2
• 239000008109 sodium starch glycolate Substances 0.000 claims description 2
• 239000002552 dosage form Substances 0.000 claims 2
• 229940009976 deoxycholate Drugs 0.000 claims 1
• KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 claims 1
• MXBCYQUALCBQIJ-RYVPXURESA-N (8s,9s,10r,13s,14s,17r)-13-ethyl-17-ethynyl-11-methylidene-1,2,3,6,7,8,9,10,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-ol;(8r,9s,13s,14s,17r)-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1.C1CC[C@@H]2[C@H]3C(=C)C[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 MXBCYQUALCBQIJ-RYVPXURESA-N 0.000 description 1
• 206010016654 Fibrosis Diseases 0.000 description 1
• 201000010099 disease Diseases 0.000 description 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
• 230000004761 fibrosis Effects 0.000 description 1
• 210000004185 liver Anatomy 0.000 description 1
• 238000005259 measurement Methods 0.000 description 1
• 230000002459 sustained effect Effects 0.000 description 1