JP2020523335A5 - - Google Patents
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- Publication number
- JP2020523335A5 JP2020523335A5 JP2019568138A JP2019568138A JP2020523335A5 JP 2020523335 A5 JP2020523335 A5 JP 2020523335A5 JP 2019568138 A JP2019568138 A JP 2019568138A JP 2019568138 A JP2019568138 A JP 2019568138A JP 2020523335 A5 JP2020523335 A5 JP 2020523335A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- acid
- solid pharmaceutical
- composition according
- caliprazin
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 239000007787 solid Substances 0.000 claims 18
- 239000003795 chemical substances by application Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- KPWSJANDNDDRMB-QAQDUYKDSA-N cariprazine Chemical compound C1C[C@@H](NC(=O)N(C)C)CC[C@@H]1CCN1CCN(C=2C(=C(Cl)C=CC=2)Cl)CC1 KPWSJANDNDDRMB-QAQDUYKDSA-N 0.000 claims 2
- 229920001477 hydrophilic polymer Polymers 0.000 claims 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- 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 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 2
- 239000000314 lubricant Substances 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- QBYIENPQHBMVBV-HFEGYEGKSA-N (2R)-2-hydroxy-2-phenylacetic acid Chemical compound O[C@@H](C(O)=O)c1ccccc1.O[C@@H](C(O)=O)c1ccccc1 QBYIENPQHBMVBV-HFEGYEGKSA-N 0.000 claims 1
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims 1
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 claims 1
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- IWYDHOAUDWTVEP-UHFFFAOYSA-N R-2-phenyl-2-hydroxyacetic acid Natural products OC(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-N 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-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
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 150000004649 carbonic acid derivatives Chemical class 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 229960005123 cariprazine Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000002474 experimental method Methods 0.000 claims 1
- 238000005187 foaming Methods 0.000 claims 1
- 235000019253 formic acid Nutrition 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000001530 fumaric acid Substances 0.000 claims 1
- 229960002598 fumaric acid Drugs 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 238000005469 granulation Methods 0.000 claims 1
- 230000003179 granulation Effects 0.000 claims 1
- 229920001600 hydrophobic polymer Polymers 0.000 claims 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- 229960002510 mandelic acid Drugs 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 235000010981 methylcellulose Nutrition 0.000 claims 1
- 235000006408 oxalic acid Nutrition 0.000 claims 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000036470 plasma concentration Effects 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 229960004889 salicylic acid Drugs 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- 230000002459 sustained effect Effects 0.000 claims 1
- 229940095064 tartrate Drugs 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HUP1700253 HUP1700253A1 (hu) | 2017-06-13 | 2017-06-13 | Szilárd orális gyógyszerkészítmények |
| HUP1700253 | 2017-06-13 | ||
| PCT/IB2018/054227 WO2018229641A1 (en) | 2017-06-13 | 2018-06-12 | Solid preparation of cariprazine for oral administration |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020523335A JP2020523335A (ja) | 2020-08-06 |
| JP2020523335A5 true JP2020523335A5 (https=) | 2021-07-26 |
Family
ID=89992469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019568138A Pending JP2020523335A (ja) | 2017-06-13 | 2018-06-12 | 経口投与用固形製剤 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20200222391A1 (https=) |
| EP (1) | EP3638210A1 (https=) |
| JP (1) | JP2020523335A (https=) |
| KR (1) | KR20200016378A (https=) |
| CN (1) | CN110769815A (https=) |
| AR (1) | AR112137A1 (https=) |
| AU (1) | AU2018284138A1 (https=) |
| BR (1) | BR112019025214A2 (https=) |
| CA (1) | CA3064694A1 (https=) |
| CL (1) | CL2019003619A1 (https=) |
| CO (1) | CO2020000168A2 (https=) |
| EA (1) | EA202090029A1 (https=) |
| HU (1) | HUP1700253A1 (https=) |
| IL (1) | IL271108A (https=) |
| MX (1) | MX2019015206A (https=) |
| PE (1) | PE20200334A1 (https=) |
| PH (1) | PH12019502566A1 (https=) |
| TW (1) | TW201906608A (https=) |
| WO (1) | WO2018229641A1 (https=) |
| ZA (1) | ZA201908454B (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS53866B1 (sr) | 2008-07-16 | 2015-08-31 | Richter Gedeon Nyrt. | Farmaceutske formulacije koje sadrže ligande dopaminskih receptora |
| US11274087B2 (en) | 2016-07-08 | 2022-03-15 | Richter Gedeon Nyrt. | Industrial process for the preparation of cariprazine |
| US11547707B2 (en) | 2019-04-10 | 2023-01-10 | Richter Gedeon Nyrt. | Carbamoyl cyclohexane derivatives for treating autism spectrum disorder |
| US11344503B2 (en) * | 2019-12-13 | 2022-05-31 | Halo Science LLC | Cariprazine release formulations |
| US20230355612A1 (en) * | 2020-08-26 | 2023-11-09 | Shanghai Bocimed Pharmaceutical Co., Ltd. | Pharmaceutically acceptable salt of cariprazine and crystal form thereof, and preparation method therefor and use thereof |
| CN114748428B (zh) * | 2020-12-25 | 2023-05-23 | 上海京新生物医药有限公司 | 一种高载药量的盐酸卡利拉嗪长效缓释微球及其制备方法 |
| CN114681406B (zh) * | 2020-12-25 | 2023-10-13 | 上海京新生物医药有限公司 | 一种卡利拉嗪长效缓释微球及其制备方法 |
| WO2023160583A1 (zh) * | 2022-02-22 | 2023-08-31 | 上海云晟研新生物科技有限公司 | 卡利拉嗪药用盐及其晶型、药物组合物、制备方法和用途 |
| AU2023234747A1 (en) | 2022-03-17 | 2024-09-12 | Mapi Pharma Ltd. | Depot systems comprising cariprazine or salts thereof |
| HU231682B1 (hu) * | 2022-08-05 | 2025-10-28 | Richter Gedeon Nyrt. | Kariprazin tartalmú szájban diszpergálódó tabletta |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6248618A (ja) * | 1985-08-27 | 1987-03-03 | Zeria Shinyaku Kogyo Kk | 徐放性製剤およびその製造法 |
| US5910319A (en) | 1997-05-29 | 1999-06-08 | Eli Lilly And Company | Fluoxetine enteric pellets and methods for their preparation and use |
| HU227534B1 (en) | 2003-08-04 | 2011-08-29 | Richter Gedeon Nyrt | (thio)carbamoyl-cyclohexane derivatives, process for producing them and pharmaceutical compositions containing them |
| GB0618879D0 (en) | 2006-09-26 | 2006-11-01 | Zysis Ltd | Pharmaceutical compositions |
| US20090036468A1 (en) * | 2007-08-03 | 2009-02-05 | Forest Laboratories Holdings Limited | Pharmaceutical compositions containing dopamine receptor ligands and methods of treatment using dopamine receptor ligands |
| CA2715760C (en) * | 2008-02-21 | 2017-06-13 | Mitsubishi Tanabe Pharma Corporation | Solid preparation for oral administration of cariprazine hydrochloride |
| RS53866B1 (sr) | 2008-07-16 | 2015-08-31 | Richter Gedeon Nyrt. | Farmaceutske formulacije koje sadrže ligande dopaminskih receptora |
| KR20160117596A (ko) * | 2014-02-07 | 2016-10-10 | 오스펙스 파마슈티칼스, 인코포레이티드 | 신규 제약 제제 |
| CN106692149A (zh) * | 2015-11-13 | 2017-05-24 | 天津市汉康医药生物技术有限公司 | 一种卡利拉嗪药物口服制剂及其制备方法 |
-
2017
- 2017-06-13 HU HUP1700253 patent/HUP1700253A1/hu unknown
-
2018
- 2018-05-30 TW TW107118464A patent/TW201906608A/zh unknown
- 2018-06-12 EP EP18734306.6A patent/EP3638210A1/en not_active Withdrawn
- 2018-06-12 BR BR112019025214-2A patent/BR112019025214A2/pt not_active Application Discontinuation
- 2018-06-12 EA EA202090029A patent/EA202090029A1/ru unknown
- 2018-06-12 KR KR1020207001040A patent/KR20200016378A/ko not_active Ceased
- 2018-06-12 MX MX2019015206A patent/MX2019015206A/es unknown
- 2018-06-12 JP JP2019568138A patent/JP2020523335A/ja active Pending
- 2018-06-12 WO PCT/IB2018/054227 patent/WO2018229641A1/en not_active Ceased
- 2018-06-12 PE PE2019002491A patent/PE20200334A1/es unknown
- 2018-06-12 AU AU2018284138A patent/AU2018284138A1/en not_active Abandoned
- 2018-06-12 AR ARP180101591A patent/AR112137A1/es unknown
- 2018-06-12 CN CN201880040070.6A patent/CN110769815A/zh active Pending
- 2018-06-12 CA CA3064694A patent/CA3064694A1/en not_active Abandoned
- 2018-06-12 US US16/622,020 patent/US20200222391A1/en not_active Abandoned
-
2019
- 2019-11-15 PH PH12019502566A patent/PH12019502566A1/en unknown
- 2019-12-02 IL IL271108A patent/IL271108A/en unknown
- 2019-12-11 CL CL2019003619A patent/CL2019003619A1/es unknown
- 2019-12-18 ZA ZA2019/08454A patent/ZA201908454B/en unknown
-
2020
- 2020-01-09 CO CONC2020/0000168A patent/CO2020000168A2/es unknown
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