JP2013518870A5 - - Google Patents
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- JP2013518870A5 JP2013518870A5 JP2012551732A JP2012551732A JP2013518870A5 JP 2013518870 A5 JP2013518870 A5 JP 2013518870A5 JP 2012551732 A JP2012551732 A JP 2012551732A JP 2012551732 A JP2012551732 A JP 2012551732A JP 2013518870 A5 JP2013518870 A5 JP 2013518870A5
- Authority
- JP
- Japan
- Prior art keywords
- total weight
- pellets
- sustained release
- layer
- polymer
- 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.)
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- 239000008188 pellet Substances 0.000 claims 27
- 239000010410 layer Substances 0.000 claims 18
- 229920000642 polymer Polymers 0.000 claims 18
- 238000013268 sustained release Methods 0.000 claims 18
- 239000012730 sustained-release form Substances 0.000 claims 18
- 239000013543 active substance Substances 0.000 claims 12
- 239000011247 coating layer Substances 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 11
- 239000000314 lubricant Substances 0.000 claims 11
- 238000013265 extended release Methods 0.000 claims 9
- RUOKEQAAGRXIBM-UHFFFAOYSA-N n-prop-2-ynyl-2,3-dihydro-1h-inden-1-amine Chemical compound C1=CC=C2C(NCC#C)CCC2=C1 RUOKEQAAGRXIBM-UHFFFAOYSA-N 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 8
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 8
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 8
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 7
- 239000011230 binding agent Substances 0.000 claims 7
- 239000003826 tablet Substances 0.000 claims 7
- 239000011248 coating agent Substances 0.000 claims 6
- 238000000576 coating method Methods 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 238000009498 subcoating Methods 0.000 claims 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 5
- 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 5
- 229920001223 polyethylene glycol Polymers 0.000 claims 5
- 239000000454 talc Substances 0.000 claims 5
- 229910052623 talc Inorganic materials 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 239000011148 porous material Substances 0.000 claims 4
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical group CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 3
- 239000002775 capsule Substances 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
- 238000009472 formulation Methods 0.000 claims 3
- 238000002955 isolation Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 2
- 239000001856 Ethyl cellulose Substances 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 229920001244 Poly(D,L-lactide) Polymers 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- 229920001688 coating polymer Polymers 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- DOIRQSBPFJWKBE-UHFFFAOYSA-N dibutyl phthalate Chemical compound CCCCOC(=O)C1=CC=CC=C1C(=O)OCCCC DOIRQSBPFJWKBE-UHFFFAOYSA-N 0.000 claims 2
- 239000002702 enteric coating Substances 0.000 claims 2
- 238000009505 enteric coating Methods 0.000 claims 2
- 229920001249 ethyl cellulose Polymers 0.000 claims 2
- 235000019325 ethyl cellulose Nutrition 0.000 claims 2
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims 2
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 239000011159 matrix material Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 239000008203 oral pharmaceutical composition Substances 0.000 claims 2
- 239000004014 plasticizer Substances 0.000 claims 2
- 239000000725 suspension Substances 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
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims 2
- 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
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 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 1
- 208000024827 Alzheimer disease Diseases 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
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical group CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 claims 1
- 241000255925 Diptera Species 0.000 claims 1
- 229920003153 Eudragit® NE polymer Polymers 0.000 claims 1
- 229920003151 Eudragit® RL polymer Polymers 0.000 claims 1
- 229920003152 Eudragit® RS polymer Polymers 0.000 claims 1
- 229920003137 Eudragit® S polymer Polymers 0.000 claims 1
- 229920003134 Eudragit® polymer Polymers 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 1
- -1 Kollicoat® Polymers 0.000 claims 1
- 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 1
- 208000001738 Nervous System Trauma Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical class CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims 1
- 239000000783 alginic acid Substances 0.000 claims 1
- 235000010443 alginic acid Nutrition 0.000 claims 1
- 229920000615 alginic acid Polymers 0.000 claims 1
- 229960001126 alginic acid Drugs 0.000 claims 1
- 150000004781 alginic acids Chemical class 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 229920002988 biodegradable polymer Polymers 0.000 claims 1
- 239000004621 biodegradable polymer Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 235000010980 cellulose Nutrition 0.000 claims 1
- 239000007910 chewable tablet Substances 0.000 claims 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000010828 elution Methods 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- HQQADJVZYDDRJT-UHFFFAOYSA-N ethene;prop-1-ene Chemical group C=C.CC=C HQQADJVZYDDRJT-UHFFFAOYSA-N 0.000 claims 1
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- 239000001087 glyceryl triacetate Substances 0.000 claims 1
- 235000013773 glyceryl triacetate Nutrition 0.000 claims 1
- 230000002209 hydrophobic effect Effects 0.000 claims 1
- 239000008101 lactose 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
- JDBJJCWRXSVHOQ-UHFFFAOYSA-N methanesulfonic acid;n-prop-2-ynyl-2,3-dihydro-1h-inden-1-amine Chemical compound CS(O)(=O)=O.C1=CC=C2C(NCC#C)CCC2=C1 JDBJJCWRXSVHOQ-UHFFFAOYSA-N 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
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000028412 nervous system injury Diseases 0.000 claims 1
- 235000021317 phosphate Nutrition 0.000 claims 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 1
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims 1
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims 1
- 229920002643 polyglutamic acid Polymers 0.000 claims 1
- 229920002959 polymer blend Polymers 0.000 claims 1
- 229920001451 polypropylene glycol Polymers 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000000541 pulsatile effect Effects 0.000 claims 1
- RUOKEQAAGRXIBM-GFCCVEGCSA-N rasagiline Chemical compound C1=CC=C2[C@H](NCC#C)CCC2=C1 RUOKEQAAGRXIBM-GFCCVEGCSA-N 0.000 claims 1
- 229960000245 rasagiline Drugs 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 claims 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 1
- 229940033134 talc Drugs 0.000 claims 1
- 229940095064 tartrate Drugs 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 229960002622 triacetin Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30101910P | 2010-02-03 | 2010-02-03 | |
| US61/301,019 | 2010-02-03 | ||
| PCT/IL2011/000126 WO2011095973A1 (en) | 2010-02-03 | 2011-02-03 | Extended release formulations of rasagiline and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016186945A Division JP6440662B2 (ja) | 2010-02-03 | 2016-09-26 | ラサギリンの持続放出性製剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013518870A JP2013518870A (ja) | 2013-05-23 |
| JP2013518870A5 true JP2013518870A5 (https=) | 2014-03-20 |
| JP6045347B2 JP6045347B2 (ja) | 2016-12-14 |
Family
ID=43896855
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551732A Active JP6045347B2 (ja) | 2010-02-03 | 2011-02-03 | ラサギリンの持続放出性製剤およびその使用 |
| JP2016186945A Active JP6440662B2 (ja) | 2010-02-03 | 2016-09-26 | ラサギリンの持続放出性製剤およびその使用 |
| JP2018216973A Active JP6770564B2 (ja) | 2010-02-03 | 2018-11-20 | ラサギリンの持続放出性製剤およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016186945A Active JP6440662B2 (ja) | 2010-02-03 | 2016-09-26 | ラサギリンの持続放出性製剤およびその使用 |
| JP2018216973A Active JP6770564B2 (ja) | 2010-02-03 | 2018-11-20 | ラサギリンの持続放出性製剤およびその使用 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US9943489B2 (https=) |
| EP (2) | EP3517103A1 (https=) |
| JP (3) | JP6045347B2 (https=) |
| KR (1) | KR101791715B1 (https=) |
| CN (1) | CN102791258B (https=) |
| AU (1) | AU2011212068B2 (https=) |
| BR (1) | BR112012019374B1 (https=) |
| CA (1) | CA2789006C (https=) |
| CL (1) | CL2012002175A1 (https=) |
| CY (1) | CY1121781T1 (https=) |
| DK (1) | DK2531181T3 (https=) |
| ES (1) | ES2733133T3 (https=) |
| HU (1) | HUE044221T2 (https=) |
| IL (1) | IL221274A (https=) |
| LT (1) | LT2531181T (https=) |
| MX (1) | MX354423B (https=) |
| NZ (1) | NZ602111A (https=) |
| PL (1) | PL2531181T3 (https=) |
| PT (1) | PT2531181T (https=) |
| RS (1) | RS58988B1 (https=) |
| RU (2) | RU2607595C2 (https=) |
| SG (1) | SG183150A1 (https=) |
| TR (1) | TR201909277T4 (https=) |
| WO (1) | WO2011095973A1 (https=) |
| ZA (1) | ZA201206462B (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2607595C2 (ru) * | 2010-02-03 | 2017-01-10 | Фарма Ту Б Лтд. | Составы разагилина с пролонгированным высвобождением и их применение |
| CA2758556A1 (en) * | 2011-11-17 | 2013-05-17 | Pharmascience Inc. | Pharmaceutical composition of amphetamine mixed salts |
| WO2013105092A1 (en) * | 2012-01-12 | 2013-07-18 | Pharma Two B Ltd. | Fixed dose combination therapy of parkinson's disease |
| US9504657B2 (en) * | 2012-01-12 | 2016-11-29 | Pharmatwob Ltd. | Fixed dose combination therapy of Parkinson's disease |
| CN102579367B (zh) * | 2012-03-23 | 2014-03-12 | 中国人民解放军军事医学科学院毒物药物研究所 | 托吡酯缓释药物组合物、其制备方法及用途 |
| CN103316026B (zh) | 2012-03-23 | 2016-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | 含芬特明和托吡酯的联合产品及其制备方法 |
| EP2829270B1 (en) | 2012-03-23 | 2020-11-11 | Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China | Joint product containing synephrine and topiramate |
| US9308182B2 (en) | 2012-08-17 | 2016-04-12 | Teva Pharmaceutical Industries, Ltd. | Parenteral formulations of rasagiline |
| IN2013MU01782A (https=) * | 2013-05-20 | 2015-06-26 | Cadila Healthcare Ltd | |
| US20150275167A1 (en) * | 2014-03-28 | 2015-10-01 | Corning Incorporated | Composition and method for cell culture sustained release |
| US10709700B2 (en) * | 2014-09-15 | 2020-07-14 | Orphazyme A/S | Arimoclomol formulation |
| WO2018213838A1 (en) * | 2017-05-19 | 2018-11-22 | Biscayne Neurotherapeutics, Inc. | Modified release pharmaceutical compositions of huperzine and methods of using the same |
| CN107049985B (zh) * | 2017-06-07 | 2020-06-19 | 广州帝奇医药技术有限公司 | 一种抗帕金森病药物的长效缓释制剂及其制备方法 |
| CN112384210A (zh) * | 2018-04-25 | 2021-02-19 | 纽罗森特里亚股份有限公司 | 苏糖酸镁组合物及其用途 |
| MX2021004586A (es) | 2018-11-19 | 2021-06-15 | Supernus Pharmaceuticals Inc | Uso de dosis mas altas de formulaciones de huperzina de liberacion modificada. |
| JP7714473B2 (ja) * | 2019-05-31 | 2025-07-29 | デナリ セラピューティクス インコーポレイテッド | ピリミジニルアミノピラゾール化合物の調節放出製剤および処置方法 |
| KR20210014289A (ko) | 2019-07-30 | 2021-02-09 | (주)비씨월드제약 | 라사길린을 함유하는 서방출성 미립구의 제조방법 |
| AR121619A1 (es) * | 2020-03-25 | 2022-06-22 | Inibsa Ginecologia S A | Una forma de dosificación oral de múltiples unidades de liberación modificada de succinato de doxilamina y clorhidrato de piridoxina y un procedimiento para su preparación |
| WO2022238401A1 (en) * | 2021-05-11 | 2022-11-17 | Advicenne | Prolonged-release pharmaceutical composition for oral administration of sultiame |
| CN117355296A (zh) * | 2021-05-11 | 2024-01-05 | 阿德维斯尼公司 | 用于口服施用舒噻美的延长释放药物组合物 |
| CN118680910B (zh) * | 2024-08-26 | 2024-12-03 | 山东齐都药业有限公司 | 用于缓释递送雷沙吉兰甲磺酸盐的药物组合物及其制备方法和应用 |
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