JPWO2020115257A5 - - Google Patents

Info

Publication number

JPWO2020115257A5

JPWO2020115257A5 JP2021532415A JP2021532415A JPWO2020115257A5 JP WO2020115257 A5 JPWO2020115257 A5 JP WO2020115257A5 JP 2021532415 A JP2021532415 A JP 2021532415A JP 2021532415 A JP2021532415 A JP 2021532415A JP WO2020115257 A5 JPWO2020115257 A5 JP WO2020115257A5

Authority

JP

Japan

Prior art keywords

coating

core

copolymer

enteric

formulation

Prior art date

2023-10-06

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

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• 239000011248 coating agent Substances 0.000 claims description 14
• 238000000576 coating method Methods 0.000 claims description 14
• 238000005192 partition Methods 0.000 claims description 11
• 239000000203 mixture Substances 0.000 claims description 10
• 229920002472 Starch Polymers 0.000 claims description 7
• 235000019698 starch Nutrition 0.000 claims description 7
• 239000008107 starch Substances 0.000 claims description 7
• 239000008199 coating composition Substances 0.000 claims description 6
• 238000000034 method Methods 0.000 claims description 5
• 102000004190 Enzymes Human genes 0.000 claims description 3
• 108090000790 Enzymes Proteins 0.000 claims description 3
• 230000015556 catabolic process Effects 0.000 claims description 3
• 230000000112 colonic effect Effects 0.000 claims description 3
• 238000006731 degradation reaction Methods 0.000 claims description 3
• 238000002360 preparation method Methods 0.000 claims description 3
• 229920001577 copolymer Polymers 0.000 claims 14
• 238000009472 formulation Methods 0.000 claims 7
• 230000003111 delayed effect Effects 0.000 claims 6
• 229940121363 anti-inflammatory agent Drugs 0.000 claims 4
• 239000002260 anti-inflammatory agent Substances 0.000 claims 4
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 3
• UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 3
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 3
• VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims 2
• 229920002845 Poly(methacrylic acid) Polymers 0.000 claims 2
• 239000002253 acid Substances 0.000 claims 2
• 210000001072 colon Anatomy 0.000 claims 2
• 150000002148 esters Chemical class 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 1
• VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 6
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
• 150000004676 glycans Chemical class 0.000 description 3
• 229940075507 glyceryl monostearate Drugs 0.000 description 3
• 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 3
• 229920001282 polysaccharide Polymers 0.000 description 3
• 239000005017 polysaccharide Substances 0.000 description 3
• DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 2
• 229920000642 polymer Polymers 0.000 description 2
• 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
• 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
• 229920000053 polysorbate 80 Polymers 0.000 description 2
• 229940068968 polysorbate 80 Drugs 0.000 description 2
• 239000001069 triethyl citrate Substances 0.000 description 2
• VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 2
• 235000013769 triethyl citrate Nutrition 0.000 description 2
• FEBUJFMRSBAMES-UHFFFAOYSA-N 2-[(2-{[3,5-dihydroxy-2-(hydroxymethyl)-6-phosphanyloxan-4-yl]oxy}-3,5-dihydroxy-6-({[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}methyl)oxan-4-yl)oxy]-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl phosphinite Chemical compound OC1C(O)C(O)C(CO)OC1OCC1C(O)C(OC2C(C(OP)C(O)C(CO)O2)O)C(O)C(OC2C(C(CO)OC(P)C2O)O)O1 FEBUJFMRSBAMES-UHFFFAOYSA-N 0.000 description 1
• SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-UHFFFAOYSA-N 0.000 description 1
• 229920000945 Amylopectin Polymers 0.000 description 1
• 229920000856 Amylose Polymers 0.000 description 1
• 229920002101 Chitin Polymers 0.000 description 1
• 229920001661 Chitosan Polymers 0.000 description 1
• 229920001287 Chondroitin sulfate Polymers 0.000 description 1
• 229920002558 Curdlan Polymers 0.000 description 1
• 239000001879 Curdlan Substances 0.000 description 1
• 229920000858 Cyclodextrin Polymers 0.000 description 1
• 229920002307 Dextran Polymers 0.000 description 1
• 229920003141 Eudragit® S 100 Polymers 0.000 description 1
• 229920001218 Pullulan Polymers 0.000 description 1
• 239000004373 Pullulan Substances 0.000 description 1
• 229920002305 Schizophyllan Polymers 0.000 description 1
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
• 239000000679 carrageenan Substances 0.000 description 1
• 229920001525 carrageenan Polymers 0.000 description 1
• 235000010418 carrageenan Nutrition 0.000 description 1
• 229940113118 carrageenan Drugs 0.000 description 1
• 239000003795 chemical substances by application Substances 0.000 description 1
• 229940059329 chondroitin sulfate Drugs 0.000 description 1
• 235000019316 curdlan Nutrition 0.000 description 1
• 229940078035 curdlan Drugs 0.000 description 1
• 239000012153 distilled water Substances 0.000 description 1
• 229940079593 drug Drugs 0.000 description 1
• 239000003814 drug Substances 0.000 description 1
• 239000000839 emulsion Substances 0.000 description 1
• FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 1
• AIHDCSAXVMAMJH-GFBKWZILSA-N levan Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)OC[C@@H]1[C@@H](O)[C@H](O)[C@](CO)(CO[C@@H]2[C@H]([C@H](O)[C@@](O)(CO)O2)O)O1 AIHDCSAXVMAMJH-GFBKWZILSA-N 0.000 description 1
• 239000000546 pharmaceutical excipient Substances 0.000 description 1
• 239000004014 plasticizer Substances 0.000 description 1
• 235000019423 pullulan Nutrition 0.000 description 1
• HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
• 239000004094 surface-active agent Substances 0.000 description 1
• 239000000454 talc Substances 0.000 description 1
• 229910052623 talc Inorganic materials 0.000 description 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
• UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1