JP2002512946A5 - - Google Patents
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- Publication number
- JP2002512946A5 JP2002512946A5 JP2000545505A JP2000545505A JP2002512946A5 JP 2002512946 A5 JP2002512946 A5 JP 2002512946A5 JP 2000545505 A JP2000545505 A JP 2000545505A JP 2000545505 A JP2000545505 A JP 2000545505A JP 2002512946 A5 JP2002512946 A5 JP 2002512946A5
- Authority
- JP
- Japan
- Prior art keywords
- levosimendan
- controlled release
- composition
- release
- forming 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.)
- Granted
Links
- WHXMKTBCFHIYNQ-SECBINFHSA-N Levosimendan Chemical compound C[C@@H]1CC(=O)NN=C1C1=CC=C(NN=C(C#N)C#N)C=C1 WHXMKTBCFHIYNQ-SECBINFHSA-N 0.000 description 11
- 229960000692 levosimendan Drugs 0.000 description 11
- 239000000203 mixture Substances 0.000 description 11
- 239000003814 drug Substances 0.000 description 4
- 229940079593 drugs Drugs 0.000 description 4
- 229920000642 polymer Polymers 0.000 description 4
- 239000000843 powder Substances 0.000 description 3
- 239000002775 capsule Substances 0.000 description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- PUSNGFYSTWMJSK-GSZQVNRLSA-N (2R,3R,4S,5R,6R)-2,3,4-trimethoxy-6-(methoxymethyl)-5-[(2S,3R,4S,5R,6R)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxyoxane;1-[[(2R,3R,4S,5R,6S)-3,4,5-tris(2-hydroxypropoxy)-6-[(2R,3R,4S,5R,6R)-4,5,6-tris(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)oxan- 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](OC)O[C@@H]1COC.CC(O)CO[C@@H]1[C@@H](OCC(C)O)[C@H](OCC(C)O)[C@@H](COCC(O)C)O[C@H]1O[C@H]1[C@H](OCC(C)O)[C@@H](OCC(C)O)[C@H](OCC(C)O)O[C@@H]1COCC(C)O PUSNGFYSTWMJSK-GSZQVNRLSA-N 0.000 description 1
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical group COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 description 1
- XJKJWTWGDGIQRH-BFIDDRIFSA-N Alginic acid Chemical compound O1[C@@H](C(O)=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](C)[C@@H](O)[C@H]1O XJKJWTWGDGIQRH-BFIDDRIFSA-N 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 230000001747 exhibiting Effects 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
Description
【特許請求の範囲】
【請求項1】 (a)レボシメンダンおよび微結晶性セルロースを含有する粉末形態の急速放出部分、ならびに
(b)レボシメンダンおよび放出制御親水性ゲル形成ポリマーを含有する顆粒形態の制御放出部分
を含有する経口投与用制御放出組成物であって、全レボシメンダンの重量に対して40〜60%が制御放出部分にあり、かつ親水性ゲル形成ポリマーの量が、組成物の重量に対して30〜70%である組成物。
【請求項2】 放出制御親水性ゲル形成ポリマーが、ヒドロキシプロピルメチルセルロース、アルギン酸またはそれらの混合物である請求項1記載の組成物。
【請求項1】 (a)レボシメンダンおよび微結晶性セルロースを含有する粉末形態の急速放出部分、ならびに
(b)レボシメンダンおよび放出制御親水性ゲル形成ポリマーを含有する顆粒形態の制御放出部分
を含有する経口投与用制御放出組成物であって、全レボシメンダンの重量に対して40〜60%が制御放出部分にあり、かつ親水性ゲル形成ポリマーの量が、組成物の重量に対して30〜70%である組成物。
【請求項2】 放出制御親水性ゲル形成ポリマーが、ヒドロキシプロピルメチルセルロース、アルギン酸またはそれらの混合物である請求項1記載の組成物。
利点が本発明にもとづいて、a)治療に効果的な量のレボシメンダン、ならびにb)レボシメンダンの放出を長期間にわたって提供するため、および代謝産物(II)に対する20ng/ml未満、好ましくは10ng/ml未満の定常状態プラズマレベルを提供するための薬剤放出制御成分を含有する組成物の制御された放出によって提供される。
とくに、本発明は、a)治療に効果的な量のレボシメンダン、およびb)レボシメンダンの放出を長期間にわたって提供するための薬剤放出制御成分を含有する、経口投与のための制御放出組成物であって、その組成物が、少なくとも90パーセントのレボシメンダン含有量に対し、リン酸緩衝液pH5.8(50または100rpmで)における米国薬局方XXIIかご集合法(basket assembly method)にもとづいて決定された、実質的に1時間から4時間のあいだの全インビトロ溶解時間を示すことができる組成物に関する。
本発明のとくに好ましい実施態様は、レボシメンダンと場合により少なくとも1つの賦形剤とを含有する急速放出部分を、レボシメンダンおよび薬剤放出制御成分を含有する制御放出部分と組合せることにより得られる。薬剤放出制御成分は前述の通り選択できるが、親水性ゲル形成ポリマーであることが好ましい。とくに好ましいものは、(a)少なくとも1つの賦形剤と共にレボシメンダンを含有する粉末形態の急速放出部分、ならびに(b)レボシメンダンおよび放出制御親水性ゲル形成ポリマーを含有する顆粒形態の制御放出部分を含有する組成物である。粉末形態の急速放出部分および顆粒形態の制御放出部分は、好ましくは、ゼラチンカプセルまたはHPMCカプセルのようなカプセルに充填できる自由流動性の混合物とする。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FI980901 | 1998-04-23 | ||
FI980901A FI980901A (fi) | 1998-04-23 | 1998-04-23 | Levosimendaania säädellysti vapauttavia oraalisia koostumuksia |
PCT/FI1999/000329 WO1999055305A2 (en) | 1998-04-23 | 1999-04-23 | Controlled release peroral compositions of levosimendan |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010004367A Division JP2010083900A (ja) | 1998-04-23 | 2010-01-12 | レボシメンダンの制御放出経口用組成物 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2002512946A JP2002512946A (ja) | 2002-05-08 |
JP2002512946A5 true JP2002512946A5 (ja) | 2010-03-04 |
JP4566402B2 JP4566402B2 (ja) | 2010-10-20 |
Family
ID=8551575
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2000545505A Expired - Fee Related JP4566402B2 (ja) | 1998-04-23 | 1999-04-23 | レボシメンダンの制御放出経口用組成物 |
JP2010004367A Withdrawn JP2010083900A (ja) | 1998-04-23 | 2010-01-12 | レボシメンダンの制御放出経口用組成物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010004367A Withdrawn JP2010083900A (ja) | 1998-04-23 | 2010-01-12 | レボシメンダンの制御放出経口用組成物 |
Country Status (38)
Country | Link |
---|---|
US (1) | US7045147B1 (ja) |
EP (1) | EP1071397B1 (ja) |
JP (2) | JP4566402B2 (ja) |
KR (1) | KR100960597B1 (ja) |
CN (1) | CN1248691C (ja) |
AR (1) | AR019096A1 (ja) |
AT (1) | ATE258425T1 (ja) |
AU (1) | AU756641B2 (ja) |
BG (1) | BG64839B1 (ja) |
BR (1) | BR9909869A (ja) |
CA (1) | CA2329234C (ja) |
CO (1) | CO5070607A1 (ja) |
CZ (1) | CZ295194B6 (ja) |
DE (1) | DE69914472T2 (ja) |
DK (1) | DK1071397T3 (ja) |
EA (1) | EA002829B1 (ja) |
EE (1) | EE04220B1 (ja) |
ES (1) | ES2215379T3 (ja) |
FI (1) | FI980901A (ja) |
GE (1) | GEP20032906B (ja) |
HK (1) | HK1034032A1 (ja) |
HR (1) | HRP20000704B1 (ja) |
HU (1) | HUP0101458A3 (ja) |
ID (1) | ID27987A (ja) |
IL (2) | IL138951A0 (ja) |
MX (1) | MXPA00010367A (ja) |
NO (1) | NO329809B1 (ja) |
NZ (1) | NZ507453A (ja) |
PL (1) | PL197447B1 (ja) |
PT (1) | PT1071397E (ja) |
RS (1) | RS49962B (ja) |
SI (1) | SI1071397T1 (ja) |
SK (1) | SK285427B6 (ja) |
TR (1) | TR200003102T2 (ja) |
TW (1) | TWI224507B (ja) |
UA (1) | UA68376C2 (ja) |
WO (1) | WO1999055305A2 (ja) |
ZA (1) | ZA200005632B (ja) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FI20011465A0 (fi) * | 2001-07-04 | 2001-07-04 | Orion Corp | Pyridatsinonijohdannaisen uusi käyttö |
CA2518734A1 (en) * | 2003-03-14 | 2004-09-30 | Nirmal Mulye | A process for preparing sustained release tablets |
FI20070521L (fi) * | 2006-11-10 | 2008-05-11 | Atacama Labs Oy | Rakeita, tabletteja ja rakeistusmenetelmä |
AU2009267052B2 (en) | 2008-06-30 | 2013-07-11 | Tocagen Inc. | Formulations of 5-fluorocytosine and uses thereof |
JP2014172850A (ja) * | 2013-03-07 | 2014-09-22 | Capsugel Belgium Nv | ハードカプセル製剤 |
CN105784895B (zh) * | 2015-10-30 | 2018-05-22 | 成都欣捷高新技术开发有限公司 | 一种用高效液相色谱仪检测左西孟旦中杂质的方法 |
AU2020408323A1 (en) | 2019-12-16 | 2022-08-11 | Tenax Therapeutics, Inc. | Levosimendan for treating pulmonary hypertension with heart failure with preserved ejection fraction (PH-HF-pEF) |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ203684A (en) | 1982-04-05 | 1986-06-11 | Merck Sharp & Dohme | Granular formulation for the stabilization of unstable drugs or food supplements |
US4716042A (en) | 1986-06-16 | 1987-12-29 | American Home Products Corporation | Stabilized coated aspirin tablets |
GB8903130D0 (en) * | 1989-02-11 | 1989-03-30 | Orion Yhtymae Oy | Substituted pyridazinones |
GB2251615B (en) * | 1991-01-03 | 1995-02-08 | Orion Yhtymae Oy | (-)-[[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]hydrazono]pro panedinitrile |
US5213811A (en) * | 1991-09-13 | 1993-05-25 | Sterling Drug Inc. | Oral sustained-release drug compositions |
GB2266841A (en) * | 1992-05-06 | 1993-11-17 | Orion Yhtymae Oy | Compounds for use as anti-ischemic medicaments |
US5795909A (en) * | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
GB9614098D0 (en) | 1996-07-05 | 1996-09-04 | Orion Yhtymae Oy | Transdermal delivery of levosimendan |
FI973804A (fi) | 1997-09-26 | 1999-03-27 | Orion Yhtymae Oy | Levosimendaanin oraalisia koostumuksia |
FI974578A (fi) * | 1997-12-19 | 1999-06-20 | Orion Yhtymae Oyj | Menetelmä levosimendaanin antamiseksi |
FI980902A (fi) * | 1998-04-23 | 1999-10-24 | Orion Yhtymae Oyj | Levosimendaanin stabiileja koostumuksia |
-
1998
- 1998-04-23 FI FI980901A patent/FI980901A/fi unknown
-
1999
- 1999-03-26 CO CO99018533A patent/CO5070607A1/es unknown
- 1999-04-09 TW TW088105661A patent/TWI224507B/zh not_active IP Right Cessation
- 1999-04-22 AR ARP990101869A patent/AR019096A1/es active IP Right Grant
- 1999-04-23 RS YUP-639/00A patent/RS49962B/sr unknown
- 1999-04-23 WO PCT/FI1999/000329 patent/WO1999055305A2/en not_active Application Discontinuation
- 1999-04-23 ES ES99916941T patent/ES2215379T3/es not_active Expired - Lifetime
- 1999-04-23 EE EEP200000617A patent/EE04220B1/xx not_active IP Right Cessation
- 1999-04-23 DK DK99916941T patent/DK1071397T3/da active
- 1999-04-23 UA UA2000116616A patent/UA68376C2/uk unknown
- 1999-04-23 KR KR1020007011788A patent/KR100960597B1/ko not_active IP Right Cessation
- 1999-04-23 SK SK1554-2000A patent/SK285427B6/sk not_active IP Right Cessation
- 1999-04-23 PT PT99916941T patent/PT1071397E/pt unknown
- 1999-04-23 CZ CZ20003780A patent/CZ295194B6/cs not_active IP Right Cessation
- 1999-04-23 EP EP99916941A patent/EP1071397B1/en not_active Expired - Lifetime
- 1999-04-23 TR TR2000/03102T patent/TR200003102T2/xx unknown
- 1999-04-23 CN CNB998064181A patent/CN1248691C/zh not_active Expired - Fee Related
- 1999-04-23 NZ NZ507453A patent/NZ507453A/xx unknown
- 1999-04-23 BR BR9909869-5A patent/BR9909869A/pt not_active Application Discontinuation
- 1999-04-23 AU AU35246/99A patent/AU756641B2/en not_active Ceased
- 1999-04-23 EA EA200001098A patent/EA002829B1/ru not_active IP Right Cessation
- 1999-04-23 PL PL344078A patent/PL197447B1/pl not_active IP Right Cessation
- 1999-04-23 AT AT99916941T patent/ATE258425T1/de not_active IP Right Cessation
- 1999-04-23 JP JP2000545505A patent/JP4566402B2/ja not_active Expired - Fee Related
- 1999-04-23 SI SI9930536T patent/SI1071397T1/xx unknown
- 1999-04-23 CA CA002329234A patent/CA2329234C/en not_active Expired - Fee Related
- 1999-04-23 ID IDW20002367A patent/ID27987A/id unknown
- 1999-04-23 HU HU0101458A patent/HUP0101458A3/hu unknown
- 1999-04-23 MX MXPA00010367A patent/MXPA00010367A/es unknown
- 1999-04-23 IL IL13895199A patent/IL138951A0/xx active IP Right Grant
- 1999-04-23 GE GEAP19995639A patent/GEP20032906B/en unknown
- 1999-04-23 DE DE69914472T patent/DE69914472T2/de not_active Expired - Lifetime
- 1999-04-23 US US09/673,794 patent/US7045147B1/en not_active Expired - Fee Related
-
2000
- 2000-10-11 IL IL138951A patent/IL138951A/en not_active IP Right Cessation
- 2000-10-12 ZA ZA200005632A patent/ZA200005632B/en unknown
- 2000-10-19 HR HR20000704A patent/HRP20000704B1/xx not_active IP Right Cessation
- 2000-10-20 NO NO20005313A patent/NO329809B1/no not_active IP Right Cessation
- 2000-11-17 BG BG104959A patent/BG64839B1/bg unknown
-
2001
- 2001-02-14 HK HK01101050A patent/HK1034032A1/xx not_active IP Right Cessation
-
2010
- 2010-01-12 JP JP2010004367A patent/JP2010083900A/ja not_active Withdrawn
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