JP2015533134A5 - - Google Patents
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- Publication number
- JP2015533134A5 JP2015533134A5 JP2015536105A JP2015536105A JP2015533134A5 JP 2015533134 A5 JP2015533134 A5 JP 2015533134A5 JP 2015536105 A JP2015536105 A JP 2015536105A JP 2015536105 A JP2015536105 A JP 2015536105A JP 2015533134 A5 JP2015533134 A5 JP 2015533134A5
- Authority
- JP
- Japan
- Prior art keywords
- arginine
- composition
- moisture
- tablet
- active substances
- 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.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims description 70
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims description 61
- 229930064664 L-arginine Natural products 0.000 claims description 58
- 235000014852 L-arginine Nutrition 0.000 claims description 58
- 239000002671 adjuvant Substances 0.000 claims description 38
- 239000013543 active substance Substances 0.000 claims description 34
- 239000003826 tablet Substances 0.000 claims description 33
- 238000000034 method Methods 0.000 claims description 32
- 239000000463 material Substances 0.000 claims description 29
- 238000002360 preparation method Methods 0.000 claims description 26
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 26
- 238000001035 drying Methods 0.000 claims description 17
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 239000007787 solid Substances 0.000 claims description 17
- 238000009472 formulation Methods 0.000 claims description 16
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 13
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 10
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims description 9
- 229960003105 metformin Drugs 0.000 claims description 8
- 238000003860 storage Methods 0.000 claims description 8
- 230000009897 systematic effect Effects 0.000 claims description 8
- 239000004475 Arginine Substances 0.000 claims description 7
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 7
- 235000009697 arginine Nutrition 0.000 claims description 7
- 238000002156 mixing Methods 0.000 claims description 7
- 238000005550 wet granulation Methods 0.000 claims description 7
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims description 6
- 229960002397 linagliptin Drugs 0.000 claims description 6
- 229960005095 pioglitazone Drugs 0.000 claims description 6
- JVDHWXLTNDKLIZ-WCCKRBBISA-N (2s)-2-amino-5-(diaminomethylideneamino)pentanoic acid;hydrate Chemical compound O.OC(=O)[C@@H](N)CCCNC(N)=N JVDHWXLTNDKLIZ-WCCKRBBISA-N 0.000 claims description 4
- 239000011230 binding agent Substances 0.000 claims description 4
- 239000000945 filler Substances 0.000 claims description 4
- 239000000314 lubricant Substances 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 230000001105 regulatory effect Effects 0.000 claims description 4
- 229920002261 Corn starch Polymers 0.000 claims description 2
- 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 description 2
- 150000008535 L-arginines Chemical class 0.000 claims description 2
- 125000002059 L-arginyl group Chemical group O=C([*])[C@](N([H])[H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=N[H])N([H])[H] 0.000 claims description 2
- 229930195725 Mannitol Natural products 0.000 claims description 2
- 229920000881 Modified starch Polymers 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 2
- 229920001531 copovidone Polymers 0.000 claims description 2
- 239000008120 corn starch Substances 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 235000019359 magnesium stearate Nutrition 0.000 claims description 2
- 239000000594 mannitol Substances 0.000 claims description 2
- 235000010355 mannitol Nutrition 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 238000004806 packaging method and process Methods 0.000 claims 2
- 238000007906 compression Methods 0.000 description 3
- 230000006835 compression Effects 0.000 description 3
- 238000007908 dry granulation Methods 0.000 description 3
- 230000036571 hydration Effects 0.000 description 3
- 238000006703 hydration reaction Methods 0.000 description 3
- 230000007704 transition Effects 0.000 description 3
- 230000018044 dehydration Effects 0.000 description 2
- 238000006297 dehydration reaction Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000001179 sorption measurement Methods 0.000 description 2
- 230000001364 causal effect Effects 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000003795 desorption Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12187796 | 2012-10-09 | ||
| EP12187796.3 | 2012-10-09 | ||
| PCT/EP2013/070979 WO2014056942A1 (en) | 2012-10-09 | 2013-10-08 | Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015533134A JP2015533134A (ja) | 2015-11-19 |
| JP2015533134A5 true JP2015533134A5 (enExample) | 2016-12-01 |
Family
ID=47010364
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015536105A Pending JP2015533134A (ja) | 2012-10-09 | 2013-10-08 | 錠剤の機械的安定性に適切な少なくとも１種の水和物形成活性物質及び／又はアジュバントを含有する機械的に安定な錠剤、特にアルギニン含有錠剤の製造における選択的に水分調整された打錠材料の使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20140100236A1 (enExample) |
| EP (1) | EP2908806A1 (enExample) |
| JP (1) | JP2015533134A (enExample) |
| WO (1) | WO2014056942A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| BRPI0711558A2 (pt) | 2006-05-04 | 2011-11-08 | Boeringer Ingelheim Internat Gmbh | polimorfos |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| PH12012501037A1 (en) | 2009-11-27 | 2013-01-14 | Boehringer Ingelheim Int | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| CA2797310C (en) | 2010-05-05 | 2020-03-31 | Boehringer Ingelheim International Gmbh | Glp-1 receptor agonist and dpp-4 inhibitor combination therapy |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| EP4151218A1 (en) | 2012-05-14 | 2023-03-22 | Boehringer Ingelheim International GmbH | Linagliptin, a xanthine derivative as dpp-4 inhibitor, for use in the treatment of sirs and/or sepsis |
| US20130303462A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| DK2970283T3 (da) | 2013-03-14 | 2021-01-25 | Boehringer Ingelheim Int | Substituerede 2-aza-bicyclo[2.2.1]heptan-3-carboxylsyre-(benzyl-cyano-methyl)-amider som inhibitorer af cathepsin-c |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| KR102510588B1 (ko) * | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
| WO2017211979A1 (en) | 2016-06-10 | 2017-12-14 | Boehringer Ingelheim International Gmbh | Combinations of linagliptin and metformin |
| TR201720515A2 (tr) * | 2017-12-15 | 2019-07-22 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Li̇nagli̇pti̇n i̇çeren bi̇r kati oral dozaj formu |
| EP3801539A4 (en) * | 2018-06-01 | 2022-02-23 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | SOLID ORAL PHARMACEUTICAL COMPOSITIONS OF LINAGLIPTIN |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003231252A1 (en) * | 2002-05-09 | 2003-11-11 | Enos Pharmaceuticals, Inc. | Methods and compositions for the treatment and prevention of intermittent claudication or alzheimer's disease |
| US20080145424A1 (en) | 2002-10-24 | 2008-06-19 | Enos Phramaceuticals, Inc. | Sustained release L-arginine formulations and methods of manufacture and use |
| MXPA05004290A (es) * | 2002-10-24 | 2005-11-23 | Enos Pharmaceuticals Inc | Formulaciones de l-arginina de liberacion sostenida, y metodos para su fabricacion y uso. |
| JP2005298373A (ja) | 2004-04-08 | 2005-10-27 | Kyowa Hakko Kogyo Co Ltd | 吸水性アミノ酸含有糖衣錠剤 |
| EP2022497B1 (en) * | 2006-05-26 | 2014-04-30 | Toyama Chemical Co., Ltd. | Oral composition comprising 3-[5-[4-(cyclopentyloxy) -2-hydroxybenzoyl]-2-](3-hydroxy-1,2-benzisoxazol-6- yl)methoxy¨phenyl¨propionic acid or salt thereof |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| JP2010027011A (ja) | 2008-07-17 | 2010-02-04 | Alios:Kk | ネイルサロンスペース貸しシステム及びネイルサロン運営システム |
| 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 |
| JP5476782B2 (ja) | 2009-04-21 | 2014-04-23 | 大正製薬株式会社 | アルギニン含有錠剤の製造方法 |
| JP5446716B2 (ja) * | 2009-10-21 | 2014-03-19 | 大正製薬株式会社 | アルギニン及びカルニチン含有錠剤の製造方法 |
| UY33937A (es) | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
-
2013
- 2013-10-08 WO PCT/EP2013/070979 patent/WO2014056942A1/en not_active Ceased
- 2013-10-08 JP JP2015536105A patent/JP2015533134A/ja active Pending
- 2013-10-08 US US14/048,445 patent/US20140100236A1/en not_active Abandoned
- 2013-10-08 EP EP13776453.6A patent/EP2908806A1/en not_active Withdrawn
-
2016
- 2016-12-15 US US15/379,584 patent/US20170095423A1/en not_active Abandoned
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