JP2017002092A5 - - Google Patents
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- Publication number
- JP2017002092A5 JP2017002092A5 JP2016202730A JP2016202730A JP2017002092A5 JP 2017002092 A5 JP2017002092 A5 JP 2017002092A5 JP 2016202730 A JP2016202730 A JP 2016202730A JP 2016202730 A JP2016202730 A JP 2016202730A JP 2017002092 A5 JP2017002092 A5 JP 2017002092A5
- Authority
- JP
- Japan
- Prior art keywords
- starch
- pharmaceutically acceptable
- acceptable salt
- calcium
- canagliflozin
- 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
- 150000003839 salts Chemical class 0.000 claims 67
- 229920002678 cellulose Polymers 0.000 claims 38
- 239000001913 cellulose Substances 0.000 claims 38
- 235000010980 cellulose Nutrition 0.000 claims 38
- 238000002360 preparation method Methods 0.000 claims 38
- 239000007787 solid Substances 0.000 claims 37
- 229960001713 canagliflozin Drugs 0.000 claims 36
- VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 36
- 229920002472 Starch Polymers 0.000 claims 33
- 229930006000 Sucrose Natural products 0.000 claims 33
- 239000005720 sucrose Substances 0.000 claims 33
- 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 32
- 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 32
- 229920000881 Modified starch Polymers 0.000 claims 32
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 32
- 239000001506 calcium phosphate Substances 0.000 claims 32
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims 32
- 239000008101 lactose Substances 0.000 claims 32
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 30
- -1 dextrate Polymers 0.000 claims 22
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 17
- 235000019698 starch Nutrition 0.000 claims 17
- 239000008107 starch Substances 0.000 claims 17
- 229920002261 Corn starch Polymers 0.000 claims 16
- 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 16
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 16
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 16
- 229920001353 Dextrin Polymers 0.000 claims 16
- 239000004375 Dextrin Substances 0.000 claims 16
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims 16
- 239000004386 Erythritol Substances 0.000 claims 16
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims 16
- 229930091371 Fructose Natural products 0.000 claims 16
- 239000005715 Fructose Substances 0.000 claims 16
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims 16
- 229920002774 Maltodextrin Polymers 0.000 claims 16
- 239000005913 Maltodextrin Substances 0.000 claims 16
- 229930195725 Mannitol Natural products 0.000 claims 16
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims 16
- FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 claims 16
- 239000001354 calcium citrate Substances 0.000 claims 16
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 16
- 235000011010 calcium phosphates Nutrition 0.000 claims 16
- 238000007906 compression Methods 0.000 claims 16
- 230000006835 compression Effects 0.000 claims 16
- 239000008120 corn starch Substances 0.000 claims 16
- 235000019425 dextrin Nutrition 0.000 claims 16
- 239000008121 dextrose Substances 0.000 claims 16
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims 16
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims 16
- 229940038472 dicalcium phosphate Drugs 0.000 claims 16
- 235000019414 erythritol Nutrition 0.000 claims 16
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims 16
- 229940009714 erythritol Drugs 0.000 claims 16
- 239000000845 maltitol Substances 0.000 claims 16
- 235000010449 maltitol Nutrition 0.000 claims 16
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 claims 16
- 229940035436 maltitol Drugs 0.000 claims 16
- 229940035034 maltodextrin Drugs 0.000 claims 16
- 239000000594 mannitol Substances 0.000 claims 16
- 235000010355 mannitol Nutrition 0.000 claims 16
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims 16
- 229920001592 potato starch Polymers 0.000 claims 16
- 229940116317 potato starch Drugs 0.000 claims 16
- 229940100486 rice starch Drugs 0.000 claims 16
- 239000000600 sorbitol Substances 0.000 claims 16
- 235000010356 sorbitol Nutrition 0.000 claims 16
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 16
- 235000013337 tricalcium citrate Nutrition 0.000 claims 16
- 229940100445 wheat starch Drugs 0.000 claims 16
- 239000002023 wood Substances 0.000 claims 16
- 239000000811 xylitol Substances 0.000 claims 16
- 235000010447 xylitol Nutrition 0.000 claims 16
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims 16
- 229960002675 xylitol Drugs 0.000 claims 16
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 15
- XFWJKVMFIVXPKK-UHFFFAOYSA-N calcium;oxido(oxo)alumane Chemical compound [Ca+2].[O-][Al]=O.[O-][Al]=O XFWJKVMFIVXPKK-UHFFFAOYSA-N 0.000 claims 13
- 239000008187 granular material Substances 0.000 claims 7
- WGRQANOPCQRCME-PMACEKPBSA-N teneligliptin Chemical compound O=C([C@H]1NC[C@H](C1)N1CCN(CC1)C1=CC(=NN1C=1C=CC=CC=1)C)N1CCSC1 WGRQANOPCQRCME-PMACEKPBSA-N 0.000 claims 7
- 229950000034 teneligliptin Drugs 0.000 claims 7
- 244000215068 Acacia senegal Species 0.000 claims 6
- 229920000084 Gum arabic Polymers 0.000 claims 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 6
- 235000010489 acacia gum Nutrition 0.000 claims 6
- 239000000205 acacia gum Substances 0.000 claims 6
- 239000011248 coating agent Substances 0.000 claims 6
- 238000000576 coating method Methods 0.000 claims 6
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 6
- 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 6
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 6
- 239000008247 solid mixture Substances 0.000 claims 6
- 238000005469 granulation Methods 0.000 claims 4
- 230000003179 granulation Effects 0.000 claims 4
- 239000000654 additive Substances 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 235000012241 calcium silicate Nutrition 0.000 claims 3
- 229910052918 calcium silicate Inorganic materials 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 239000003086 colorant Substances 0.000 claims 3
- 239000007884 disintegrant Substances 0.000 claims 3
- 238000009472 formulation Methods 0.000 claims 3
- 239000000314 lubricant Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000002245 particle Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 239000003381 stabilizer Substances 0.000 claims 3
- 239000004094 surface-active agent Substances 0.000 claims 3
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 239000000796 flavoring agent Substances 0.000 claims 2
- 239000003205 fragrance Substances 0.000 claims 2
- 238000009775 high-speed stirring Methods 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000003002 pH adjusting agent Substances 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- PMVSDNDAUGGCCE-TYYBGVCCSA-L Ferrous fumarate Chemical compound [Fe+2].[O-]C(=O)\C=C\C([O-])=O PMVSDNDAUGGCCE-TYYBGVCCSA-L 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 239000002253 acid Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 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 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 229960005069 calcium Drugs 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 235000013539 calcium stearate Nutrition 0.000 claims 1
- 239000008116 calcium stearate Substances 0.000 claims 1
- FYHXNYLLNIKZMR-UHFFFAOYSA-N calcium;carbonic acid Chemical compound [Ca].OC(O)=O FYHXNYLLNIKZMR-UHFFFAOYSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 229940105329 carboxymethylcellulose Drugs 0.000 claims 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 claims 1
- 229960005168 croscarmellose Drugs 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000004503 fine granule Substances 0.000 claims 1
- 235000019634 flavors Nutrition 0.000 claims 1
- 235000013355 food flavoring agent Nutrition 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 235000001727 glucose Nutrition 0.000 claims 1
- 239000001341 hydroxy propyl starch Substances 0.000 claims 1
- 235000013828 hydroxypropyl starch Nutrition 0.000 claims 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014262702 | 2014-12-25 | ||
| JP2014262702 | 2014-12-25 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546861A Division JP6027710B1 (ja) | 2014-12-25 | 2015-12-24 | 糖尿病治療用固形製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017002092A JP2017002092A (ja) | 2017-01-05 |
| JP2017002092A5 true JP2017002092A5 (OSRAM) | 2019-01-31 |
| JP6639368B2 JP6639368B2 (ja) | 2020-02-05 |
Family
ID=56150656
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546861A Active JP6027710B1 (ja) | 2014-12-25 | 2015-12-24 | 糖尿病治療用固形製剤 |
| JP2016202730A Active JP6639368B2 (ja) | 2014-12-25 | 2016-10-14 | 糖尿病治療用固形製剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546861A Active JP6027710B1 (ja) | 2014-12-25 | 2015-12-24 | 糖尿病治療用固形製剤 |
Country Status (2)
| Country | Link |
|---|---|
| JP (2) | JP6027710B1 (OSRAM) |
| WO (1) | WO2016104643A1 (OSRAM) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018142334A1 (en) * | 2017-02-03 | 2018-08-09 | Glenmark Pharmaceuticals Limited | Formulations comprising oxalate salts of teneligliptin and solvates thereof |
| JPWO2020209350A1 (OSRAM) * | 2019-04-12 | 2020-10-15 | ||
| AU2020394498A1 (en) | 2019-11-28 | 2022-06-09 | Boehringer Ingelheim Vetmedica Gmbh | Use of SGLT-2 inhibitors in the drying-off of non-human mammals |
| JPWO2024053680A1 (OSRAM) * | 2022-09-07 | 2024-03-14 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY147596A (en) * | 2007-02-01 | 2012-12-31 | Takeda Pharmaceutical | Solid preparation comprising alogliptin and pioglitazone |
| CL2008003653A1 (es) * | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| UY32427A (es) * | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma |
| KR101479824B1 (ko) * | 2009-12-18 | 2015-01-06 | 미쓰비시 타나베 파마 코퍼레이션 | 용출 안정성 제제 |
| WO2011142478A1 (en) * | 2010-05-11 | 2011-11-17 | Mitsubishi Tanabe Pharma Corporation | Canagliflozin containing tablets |
-
2015
- 2015-12-24 JP JP2016546861A patent/JP6027710B1/ja active Active
- 2015-12-24 WO PCT/JP2015/086097 patent/WO2016104643A1/ja not_active Ceased
-
2016
- 2016-10-14 JP JP2016202730A patent/JP6639368B2/ja active Active
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