JP2014181234A5 - - Google Patents
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- Publication number
- JP2014181234A5 JP2014181234A5 JP2014045951A JP2014045951A JP2014181234A5 JP 2014181234 A5 JP2014181234 A5 JP 2014181234A5 JP 2014045951 A JP2014045951 A JP 2014045951A JP 2014045951 A JP2014045951 A JP 2014045951A JP 2014181234 A5 JP2014181234 A5 JP 2014181234A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- pharmaceutical dosage
- sustained release
- tofacitinib
- pharmaceutically acceptable
- Prior art date
- 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
- 239000002552 dosage form Substances 0.000 claims 84
- 238000013268 sustained release Methods 0.000 claims 42
- 239000012730 sustained-release form Substances 0.000 claims 42
- 239000004012 Tofacitinib Substances 0.000 claims 34
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims 34
- 229960001350 tofacitinib Drugs 0.000 claims 34
- 239000011159 matrix material Substances 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 7
- 230000036470 plasma concentration Effects 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000011248 coating agent Substances 0.000 claims 6
- 238000000576 coating method Methods 0.000 claims 6
- 239000003937 drug carrier Substances 0.000 claims 6
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 5
- 239000001913 cellulose Substances 0.000 claims 4
- 229920002678 cellulose Polymers 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 239000012528 membrane Substances 0.000 claims 4
- 239000003826 tablet Substances 0.000 claims 4
- 238000009792 diffusion process Methods 0.000 claims 3
- -1 fatty acid ester Chemical class 0.000 claims 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 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
- 208000026278 immune system disease Diseases 0.000 claims 3
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 claims 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 2
- 229960000485 methotrexate Drugs 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 229920003176 water-insoluble polymer Polymers 0.000 claims 2
- 229920003169 water-soluble polymer Polymers 0.000 claims 2
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims 1
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 239000004375 Dextrin Substances 0.000 claims 1
- 229920001353 Dextrin Polymers 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 229920002907 Guar gum Polymers 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- UETNIIAIRMUTSM-UHFFFAOYSA-N Jacareubin Natural products CC1(C)OC2=CC3Oc4c(O)c(O)ccc4C(=O)C3C(=C2C=C1)O UETNIIAIRMUTSM-UHFFFAOYSA-N 0.000 claims 1
- 240000007472 Leucaena leucocephala Species 0.000 claims 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 claims 1
- 239000005913 Maltodextrin Substances 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 229920002125 Sokalan® Polymers 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 150000005215 alkyl ethers Chemical class 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 229960005370 atorvastatin Drugs 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 claims 1
- 229960002170 azathioprine Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 229920002301 cellulose acetate Polymers 0.000 claims 1
- 235000019425 dextrin Nutrition 0.000 claims 1
- 239000002702 enteric coating Substances 0.000 claims 1
- 238000009505 enteric coating Methods 0.000 claims 1
- 230000003628 erosive effect Effects 0.000 claims 1
- 239000007941 film coated tablet Substances 0.000 claims 1
- 239000003862 glucocorticoid Substances 0.000 claims 1
- 150000002327 glycerophospholipids Chemical class 0.000 claims 1
- 239000000665 guar gum Substances 0.000 claims 1
- 235000010417 guar gum Nutrition 0.000 claims 1
- 229960002154 guar gum Drugs 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 229940035034 maltodextrin Drugs 0.000 claims 1
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- KBOPZPXVLCULAV-UHFFFAOYSA-N mesalamine Chemical compound NC1=CC=C(O)C(C(O)=O)=C1 KBOPZPXVLCULAV-UHFFFAOYSA-N 0.000 claims 1
- 229960004963 mesalazine Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 230000003204 osmotic effect Effects 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 229920000058 polyacrylate Polymers 0.000 claims 1
- 229940070721 polyacrylate Drugs 0.000 claims 1
- 239000004584 polyacrylic acid Substances 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 229940068984 polyvinyl alcohol Drugs 0.000 claims 1
- 239000008057 potassium phosphate buffer Substances 0.000 claims 1
- 239000000661 sodium alginate Substances 0.000 claims 1
- 235000010413 sodium alginate Nutrition 0.000 claims 1
- 229940005550 sodium alginate Drugs 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 229940032147 starch Drugs 0.000 claims 1
- 150000005846 sugar alcohols Chemical class 0.000 claims 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 claims 1
- 229960001940 sulfasalazine Drugs 0.000 claims 1
- NCEXYHBECQHGNR-UHFFFAOYSA-N sulfasalazine Natural products C1=C(O)C(C(=O)O)=CC(N=NC=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-UHFFFAOYSA-N 0.000 claims 1
- 229940037128 systemic glucocorticoids Drugs 0.000 claims 1
- 238000002689 xenotransplantation Methods 0.000 claims 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361802479P | 2013-03-16 | 2013-03-16 | |
| US61/802,479 | 2013-03-16 | ||
| US201361864059P | 2013-08-09 | 2013-08-09 | |
| US61/864,059 | 2013-08-09 | ||
| US201461934428P | 2014-01-31 | 2014-01-31 | |
| US61/934,428 | 2014-01-31 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016174293A Division JP6314188B2 (ja) | 2013-03-16 | 2016-09-07 | トファシチニブの経口持続放出剤形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014181234A JP2014181234A (ja) | 2014-09-29 |
| JP2014181234A5 true JP2014181234A5 (cg-RX-API-DMAC7.html) | 2015-09-17 |
| JP6041823B2 JP6041823B2 (ja) | 2016-12-14 |
Family
ID=50819757
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014045951A Active JP6041823B2 (ja) | 2013-03-16 | 2014-03-10 | トファシチニブの経口持続放出剤形 |
| JP2016174293A Active JP6314188B2 (ja) | 2013-03-16 | 2016-09-07 | トファシチニブの経口持続放出剤形 |
| JP2018058176A Pending JP2018100300A (ja) | 2013-03-16 | 2018-03-26 | トファシチニブの経口持続放出剤形 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016174293A Active JP6314188B2 (ja) | 2013-03-16 | 2016-09-07 | トファシチニブの経口持続放出剤形 |
| JP2018058176A Pending JP2018100300A (ja) | 2013-03-16 | 2018-03-26 | トファシチニブの経口持続放出剤形 |
Country Status (22)
Families Citing this family (60)
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| JP2759924B2 (ja) | 1995-08-11 | 1998-05-28 | 株式会社ゼクセル | 燃料噴射装置の噴射時期検出装置 |
| JP6041823B2 (ja) | 2013-03-16 | 2016-12-14 | ファイザー・インク | トファシチニブの経口持続放出剤形 |
| GB201402070D0 (en) * | 2014-02-07 | 2014-03-26 | Galapagos Nv | Pharmaceutical compositions for the treatment of inflammatory disorders |
| US20170151244A1 (en) * | 2014-06-23 | 2017-06-01 | Sun Pharmaceutical Industries Limited | Oral pharmaceutical composition of tofacitinib |
| AR101476A1 (es) | 2014-08-07 | 2016-12-21 | Acerta Pharma Bv | Métodos para tratar cánceres, enfermedades inmunes y autoinmunes, y enfermedades inflamatorias en base a la tasa de ocupación de la tirosin quinasa de bruton (btk) y a la tasa de resíntesis de la tirosin quinasa de bruton (btk) |
| CN104622827A (zh) * | 2015-03-05 | 2015-05-20 | 重庆华邦制药有限公司 | 托法替布片剂及其制备方法 |
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| CN120478294A (zh) | 2015-10-16 | 2025-08-15 | 艾伯维公司 | 制备咪唑并[1,2-a]吡咯并[2,3-e]吡嗪类化合物及其固态形式的方法 |
| US11524964B2 (en) | 2015-10-16 | 2022-12-13 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| WO2017185038A1 (en) | 2016-04-22 | 2017-10-26 | Receptor Life Sciences | Fast-acting plant-based medicinal compounds and nutritional supplements |
| CN108066319B (zh) * | 2016-11-10 | 2022-01-14 | 江苏先声药业有限公司 | 一种枸橼酸托法替布肠溶缓释微丸及其制备方法 |
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| KR20180066296A (ko) * | 2016-12-07 | 2018-06-19 | 서울대학교산학협력단 | 토파시티닙을 포함하는 고염증 증상의 예방 또는 치료용 약학적 조성물 및 토파시티닙을 포함하는 고염증 증상의 예방 또는 개선용 건강기능식품 조성물 |
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