ZA200104361B - Micronized eplerenone compositions. - Google Patents
Micronized eplerenone compositions. Download PDFInfo
- Publication number
- ZA200104361B ZA200104361B ZA200104361A ZA200104361A ZA200104361B ZA 200104361 B ZA200104361 B ZA 200104361B ZA 200104361 A ZA200104361 A ZA 200104361A ZA 200104361 A ZA200104361 A ZA 200104361A ZA 200104361 B ZA200104361 B ZA 200104361B
- Authority
- ZA
- South Africa
- Prior art keywords
- pharmaceutical composition
- eplerenone
- weight percent
- composition according
- micronized
- Prior art date
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- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
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Landscapes
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EP (1) | EP1135139B1 (de) |
JP (1) | JP2002531508A (de) |
KR (1) | KR100671275B1 (de) |
CN (1) | CN1230179C (de) |
AR (1) | AR028982A1 (de) |
AT (1) | ATE249223T1 (de) |
AU (1) | AU763166B2 (de) |
BR (1) | BR9915964A (de) |
CA (1) | CA2326842A1 (de) |
CZ (1) | CZ20011942A3 (de) |
DE (1) | DE69911240T2 (de) |
DK (1) | DK1135139T3 (de) |
EA (1) | EA003266B1 (de) |
ES (1) | ES2207977T3 (de) |
HK (1) | HK1041641B (de) |
HU (1) | HU224428B1 (de) |
ID (1) | ID30115A (de) |
IL (1) | IL143301A0 (de) |
IS (1) | IS2325B (de) |
MY (1) | MY125651A (de) |
NO (1) | NO20012782L (de) |
NZ (1) | NZ511869A (de) |
PL (1) | PL198425B1 (de) |
PT (1) | PT1135139E (de) |
TR (1) | TR200101643T2 (de) |
TW (1) | TWI234459B (de) |
UA (1) | UA74141C2 (de) |
WO (1) | WO2000033847A1 (de) |
ZA (1) | ZA200104361B (de) |
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UA74141C2 (uk) * | 1998-12-09 | 2005-11-15 | Дж.Д. Сірл Енд Ко. | Фармацевтична композиція на основі тонкоподрібненого еплеренону (варіанти), спосіб її одержання та спосіб лікування розладів, опосередкованих альдостероном (варіанти) |
EP1527782A1 (de) * | 1999-12-08 | 2005-05-04 | Pharmacia Corporation | Nanopartikelzusammensetzungen enthaltend Eplerenon |
DK1175220T3 (da) * | 1999-12-08 | 2005-08-29 | Pharmacia Corp | Nanopartikulære eplerenonkompositioner |
CA2409437A1 (en) * | 2000-05-11 | 2001-11-22 | Pharmacia Corporation | Aldosterone antagonist composition for release during aldosterone acrophase |
AU2001279050B2 (en) * | 2000-07-27 | 2006-10-19 | Pharmacia Corporation | Epoxy-steroidal aldosterone antagonist and beta-adrenergic antagonist combination therapy for treatment of congestive heart failure |
JP2004518611A (ja) * | 2000-07-27 | 2004-06-24 | ファルマシア・コーポレーション | 炎症関連障害を予防するか又は治療するためのアルドステロン遮断薬療法 |
US20020111337A1 (en) * | 2000-08-28 | 2002-08-15 | Fedde Kenton N. | Use of an aldosterone receptor antagonist to improve cognitive function |
US8168616B1 (en) * | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
IL157816A0 (en) | 2001-03-12 | 2004-03-28 | Roberto Pellicciari | Steroids as agonists for fxr |
US6962715B2 (en) * | 2001-10-24 | 2005-11-08 | Hewlett-Packard Development Company, L.P. | Method and dosage form for dispensing a bioactive substance |
US20040173146A1 (en) * | 2001-06-07 | 2004-09-09 | Figueroa Iddys D. | Application of a bioactive agent to a delivery substrate |
US20040173147A1 (en) * | 2001-06-07 | 2004-09-09 | Figueroa Iddys D. | Application of a bioactive agent to a delivery substrate |
GB0114532D0 (en) * | 2001-06-14 | 2001-08-08 | Jagotec Ag | Novel compositions |
CN1537019A (zh) * | 2001-07-19 | 2004-10-13 | �ź㴫 | 醛固酮受体拮抗剂和HMG CoA还原酶抑制剂的药物组合 |
EP1453522A1 (de) * | 2001-12-13 | 2004-09-08 | Pharmacia Corporation | Behandlung- oder vorbeugungsmethoden von aldosteronbedingten pathogenen wirkungen durch epoxysteroidaldosteronantagonisten |
KR20040078683A (ko) * | 2002-01-30 | 2004-09-10 | 파마시아 코포레이션 | 심혈관 질환의 예방 또는 치료를 위한 알도스테론 길항제및 비스테로이드 소염제의 조합 치료법 |
PT1480679E (pt) * | 2002-02-26 | 2007-07-18 | Astrazeneca Ab | Fórmulação farmacêutica de iressa compreendendo um derivado de celulose solúvel em água |
WO2003080181A2 (en) * | 2002-03-20 | 2003-10-02 | Pharmacia Corporation | Storage stable eplerenone formulation |
US7235655B2 (en) * | 2002-03-22 | 2007-06-26 | Pharmacia & Upjohn Company | Processes to prepare eplerenone |
MXPA04010682A (es) * | 2002-04-26 | 2004-12-13 | Schering Ag | Tratamiento contra la hipertension en mujeres quienes reciben tratamiento restitutivo hormonal. |
US20040048840A1 (en) * | 2002-08-23 | 2004-03-11 | Pharmacia Corporation | Modulation of matrix metalloproteinase (MMP) activity with aldosterone blocker(s) |
CN1694689A (zh) * | 2002-09-30 | 2005-11-09 | 阿库斯菲尔公司 | 供吸入的缓释多孔微粒 |
PT1558265E (pt) * | 2002-11-05 | 2010-03-22 | Bayer Schering Pharma Ag | Utilização da drospirenona para o tratamento da hipertensão |
AU2002368326A1 (en) * | 2002-11-05 | 2004-06-07 | Schering Aktiengesellschaft | Hormone replacement therapy with drospirenone |
US7786101B2 (en) * | 2002-11-05 | 2010-08-31 | Bayer Schering Pharma Ag | Cardiovascular protection using anti-aldosteronic progestins |
CN1310648C (zh) * | 2002-12-13 | 2007-04-18 | 佳高泰克有限公司 | 局部纳米颗粒螺甾内酯制剂 |
DE10335027A1 (de) | 2003-07-31 | 2005-02-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von Angiotensin II Rezeptor Antagonisten |
US20040229901A1 (en) * | 2003-02-24 | 2004-11-18 | Lauren Otsuki | Method of treatment of disease using an adenosine A1 receptor antagonist |
US20060293312A1 (en) * | 2003-04-25 | 2006-12-28 | Howard Dittrich | Method of improved diuresis in individuals with impaired renal function |
NZ543109A (en) * | 2003-04-25 | 2008-06-30 | Novacardia Inc | Method of improved diuresis in individuals with impaired renal function |
KR100473422B1 (ko) * | 2003-06-12 | 2005-03-14 | 박원봉 | 렉틴 함유 천연물의 장용성 코팅용 조성물 |
EP2535042A1 (de) * | 2003-06-16 | 2012-12-19 | ANDRX Pharmaceuticals LLC. | Orale Makrolidusammensetzung mit erweiterter Freisetzung |
US7198653B2 (en) | 2003-07-31 | 2007-04-03 | Delavau Llc | Calcium carbonate granulation |
US20050031683A1 (en) * | 2003-08-04 | 2005-02-10 | Ashish Kapoor | Solid pharmaceutical composition |
US7390503B1 (en) | 2003-08-22 | 2008-06-24 | Barr Laboratories, Inc. | Ondansetron orally disintegrating tablets |
US7282217B1 (en) * | 2003-08-29 | 2007-10-16 | Kv Pharmaceutical Company | Rapidly disintegrable tablets |
TR201910177T4 (tr) * | 2003-09-12 | 2019-08-21 | Amgen Inc | Bir sinakalset HCl içeren hızlı çözünme formülasyonu. |
CA2533887A1 (en) * | 2003-09-30 | 2005-04-14 | Acusphere, Inc. | Injectable, oral, or topical sustained release pharmaceutical formulations |
US20050203482A1 (en) * | 2004-03-15 | 2005-09-15 | Chinea Vanessa I. | Pharmaceutical dispensing apparatus and method |
US20070196471A1 (en) * | 2004-04-02 | 2007-08-23 | Thosar Shilpa S | Micronized Eplerenone Compositions |
US20050232957A1 (en) * | 2004-04-14 | 2005-10-20 | Katz Kenneth A | Compositions and methods for moisturizing skin |
US20050239759A1 (en) * | 2004-04-16 | 2005-10-27 | Lauren Otsuki | Method of treatment of disease using an adenosine A1 receptor antagonist and an aldosterone inhibitor |
US8075910B2 (en) * | 2004-05-20 | 2011-12-13 | Pbm Pharmaceuticals, Inc. | Oral compositions comprising edible oils and vitamins and/or minerals and methods for making oral compositions |
US7846466B2 (en) * | 2004-06-10 | 2010-12-07 | Northwestern University | Biodegradable scaffolds and uses thereof |
US20060134212A1 (en) * | 2004-09-02 | 2006-06-22 | Forest Laboratories, Inc. | Lercanidipine immediate release compositions |
US20060165788A1 (en) * | 2004-09-09 | 2006-07-27 | Wattanaporn Abramowitz | Lercanidipine pH dependent pulsatile release compositions |
US20060165789A1 (en) * | 2004-09-09 | 2006-07-27 | Forest Laboratories, Inc. | Lercanidipine modified release compositions |
US8022053B2 (en) * | 2004-11-02 | 2011-09-20 | Bayer Schering Pharma Aktiengesellschaft | Oral solid dosage forms containing a low dose of estradiol |
CA2552766C (en) * | 2004-11-23 | 2010-08-17 | Dong Wha Pharmaceutical Ind. Co., Ltd. | N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine bis(methanesulfonate) |
WO2006097342A1 (en) * | 2005-03-17 | 2006-09-21 | Synthon B.V. | Process for making steroidal compounds |
US20060252738A1 (en) * | 2005-05-06 | 2006-11-09 | Phero Tech Inc. | Method for preparing and using water-based steroid pheromone compositions |
WO2006125304A1 (en) * | 2005-05-25 | 2006-11-30 | Liponex, Inc. | Pharmaceutical compositions for treating or preventing coronary artery disease |
WO2007012960A1 (en) * | 2005-07-29 | 2007-02-01 | Glenmark Pharmaceuticals Limited | Pharmaceutical compositions of eplerenone |
US20070095705A1 (en) * | 2005-10-31 | 2007-05-03 | Legault Dennis X | Array of packages |
JP5030973B2 (ja) * | 2006-01-13 | 2012-09-19 | インディアナ・ユニバーシティ・リサーチ・アンド・テクノロジー・コーポレーション | あるipf(特発性肺線維症)患者が、v型コラーゲンによる経口寛容治療の候補であるかを決定するための方法 |
US20070184163A1 (en) * | 2006-02-07 | 2007-08-09 | International Flavors, & Fragrances Inc. | Non-hygroscopic flavor particles |
WO2007102169A1 (en) * | 2006-03-08 | 2007-09-13 | Jubilant Organosys Limited | Extended release pharmaceutical formulation of venlafaxine and method of manufacturing the same |
US20070248665A1 (en) * | 2006-04-24 | 2007-10-25 | Sherman Bernard C | Compositions comprising co-precipitate of eplerenone and a water-soluble excipient |
DE602007009230D1 (de) * | 2006-05-31 | 2010-10-28 | Vertex Pharma | Orale formulierungen mit kontrollierter freisetzung eines interleukin-1-beta-converting-enzyme inhibitors |
CN101466383A (zh) * | 2006-06-16 | 2009-06-24 | 美国诺华卡迪亚公司 | 包含低频率投与aa1ra的肾功能延长改善 |
DE102006033723A1 (de) * | 2006-07-21 | 2008-01-24 | Bayer Technology Services Gmbh | Formulierungen von Multikompartimenten-Granulaten für Wirkstoffe |
EP2051696A2 (de) * | 2006-08-18 | 2009-04-29 | Morton Grove Pharmaceuticals, Inc. | Stabile flüssige levetiracetam-zusammensetzungen und verfahren |
US9138414B1 (en) | 2006-09-15 | 2015-09-22 | Delavau Llc | Calcium supplement having enhanced absorption |
JP2010513325A (ja) * | 2006-12-21 | 2010-04-30 | アルファファーム ピーティーワイ リミテッド | 医薬組成物 |
US20100137424A1 (en) * | 2007-01-22 | 2010-06-03 | Mostafa Akbarieh | Pharmaceutical compositions comprising nebivolol or a nebivolol analogue |
TW200836774A (en) * | 2007-02-01 | 2008-09-16 | Takeda Pharmaceutical | Solid preparation |
US20090197900A1 (en) * | 2007-03-29 | 2009-08-06 | Howard Dittrich | Methods of treating heart failure and renal dysfunction in individuals with an adenosine a1 receptor antagonist |
US20080242684A1 (en) * | 2007-03-29 | 2008-10-02 | Howard Dittrich | Methods of administration of adenosine a1 receptor antagonists |
US8372431B2 (en) * | 2007-10-26 | 2013-02-12 | Bial-Portela & C.A., S.A. | Pharmaceutical composition comprising licarbazepine acetate |
EP2249813A1 (de) * | 2008-03-11 | 2010-11-17 | Mallinckrodt Inc. | Verwendung von magnesiumstearat-dihydrat zur befeuchtung fester pharmazeutischer zusammensetzungen |
US8343524B2 (en) * | 2008-07-31 | 2013-01-01 | Clarke Mosquito Control Products, Inc. | Extended release tablet and method for making and using same |
GB0814953D0 (en) * | 2008-08-18 | 2008-09-24 | Unilever Plc | Improvements relating to nanodisperse compositions |
US8545892B2 (en) | 2009-06-26 | 2013-10-01 | Nano Pharmaceutical Laboratories, Llc | Sustained release beads and suspensions including the same for sustained delivery of active ingredients |
ES2670808T3 (es) * | 2009-08-28 | 2018-06-01 | Hercules Llc | Composición para revestimiento de película a partir de compuestos en polvo sólido |
US9345848B2 (en) | 2009-10-20 | 2016-05-24 | Sima Patent Ve Lisanslama Hizmetleri Ltd. Sti. | Dry powder inhaler |
ES2550033T3 (es) | 2009-12-23 | 2015-11-04 | Ratiopharm Gmbh | Forma de dosificación farmacéutica sólida de ticagrelor |
EA201290556A1 (ru) * | 2009-12-23 | 2013-01-30 | Рациофарм Гмбх | Оральная лекарственная форма, включающая энтекавир |
AR081935A1 (es) * | 2010-06-16 | 2012-10-31 | Teijin Pharma Ltd | Tableta con nucleo recubierto de liberacion controlada |
TR201007653A2 (tr) * | 2010-09-20 | 2012-04-24 | Bi̇lgi̇ç Mahmut | Eplerenon içeren farmasötik kompozisyon |
KR20120093461A (ko) * | 2011-01-27 | 2012-08-23 | 양지화학 주식회사 | 정제형 감미료 조성물 및 그 제조방법 |
US9849255B2 (en) | 2011-11-25 | 2017-12-26 | Mahmut Bilgic | Inhalation device |
US9682093B2 (en) | 2012-03-30 | 2017-06-20 | Charles R. Drew University Of Medicine And Science | Compositions and methods for treating or preventing metabolic syndrome disorders |
CN104736178A (zh) | 2012-06-04 | 2015-06-24 | 药品循环公司 | 布鲁顿酪氨酸激酶抑制剂的晶形 |
FR3001890B1 (fr) * | 2013-02-08 | 2015-08-07 | Greenpharma Sas | Composition dermatologique pour repousse des poils ou des cheveux |
US20140271923A1 (en) | 2013-03-14 | 2014-09-18 | Christopher Brian Reid | Compositions & formulations for preventing and treating chronic diseases that cluster in patients such as cardiovascular disease, diabetes, obesity, polycystic ovary syndrome, hyperlipidemia and hypertension, as well as for preventing and treating other diseases and conditions |
USD744087S1 (en) | 2013-10-01 | 2015-11-24 | Mahmut Bilgic | Dry powder inhaler |
US11007203B2 (en) * | 2013-10-06 | 2021-05-18 | Salim Shah | Formulations comprising aldosterone receptor antagonists and treatments using same |
US10716783B2 (en) | 2013-12-12 | 2020-07-21 | Cornell University | Prolylhydroxylase/ATF4 inhibitors and methods of use for treating neural cell injury or death and conditions resulting therefrom |
FR3019045A1 (fr) * | 2014-03-26 | 2015-10-02 | Greenpharma Sas | Composition dermatologique pour la repousse des poils ou des cheveux |
MX2017001671A (es) | 2014-08-07 | 2017-07-04 | Pharmacyclics Llc | Formulaciones novedosas de un inhibidor de la tirosina cinasa de bruton. |
WO2016063269A1 (en) | 2014-10-20 | 2016-04-28 | Prendergast Patrick T | Use of antagonists to the nuclear steroid receptor alone or in combination as direct antiviral agents to inhibit alphavirus, togaviridae, arenaviridae, filoviridae, bunyaviridae, flaviviridae and rhabdoviridae |
CA2978593A1 (en) | 2015-01-12 | 2016-07-21 | Nano Pharmaceutical Laboratories Llc | Layered sustained-release microbeads and methods of making the same |
IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of proton tyrosine kinase inhibitor |
Family Cites Families (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4082751A (en) * | 1976-02-13 | 1978-04-04 | Bristol-Myers Company | Therapeutic agents |
IT1130924B (it) * | 1980-03-06 | 1986-06-18 | Secifarma Spa | Procedimento per la preparazione di spironolattone micronizzato |
US4559332A (en) * | 1983-04-13 | 1985-12-17 | Ciba Geigy Corporation | 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof |
US5082668A (en) | 1983-05-11 | 1992-01-21 | Alza Corporation | Controlled-release system with constant pushing source |
IE58110B1 (en) * | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
US4753802A (en) | 1986-03-19 | 1988-06-28 | Alza Corporation | Verapamil dosage form |
GB8613689D0 (en) * | 1986-06-05 | 1986-07-09 | Euro Celtique Sa | Pharmaceutical composition |
US4847093A (en) | 1986-06-19 | 1989-07-11 | Alza Corporation | Dosage form with means for governing rate of gas formation |
US5057317A (en) | 1987-03-24 | 1991-10-15 | Chugai Seiyaku Kabushiki Kaisha | Slow-release pharmaceutical agent |
GB8717168D0 (en) | 1987-07-21 | 1987-08-26 | Roussel Lab Ltd | Controlled-release device |
NZ238867A (en) | 1990-07-12 | 1993-08-26 | Alza Corp | Dosage form for delayed release comprising pharmaceutically active substance and a drug-release hindering means and a second composition which imbibes fluid, expands, and ejects the active substance from the device |
WO1992013547A1 (en) | 1991-02-07 | 1992-08-20 | Alexander Mellon Eaton | Drug delivery composition and method of using the same |
US5190765A (en) | 1991-06-27 | 1993-03-02 | Alza Corporation | Therapy delayed |
US5160744A (en) | 1991-06-27 | 1992-11-03 | Alza Corporation | Verapmil therapy |
US5529992A (en) * | 1992-04-21 | 1996-06-25 | Curators Of The University Of Missouri | Method for inhibiting myocardial fibrosis by administering an aldosterone antagonist which suppresses aldoster one receptors |
IT1260505B (it) | 1992-06-01 | 1996-04-09 | Poli Ind Chimica Spa | Sistemi farmaceutici orali a cessione ritardata per il rilascio specifico nel colon |
US5324718A (en) * | 1992-07-14 | 1994-06-28 | Thorsteinn Loftsson | Cyclodextrin/drug complexation |
GB9311191D0 (en) | 1993-05-29 | 1993-07-14 | Danbiosyst Uk | Controlled release drug formulation |
WO1998025949A1 (en) | 1996-12-09 | 1998-06-18 | Proscript, Inc. | Substituted 5-amino-1,3,4-thiadiazole-2-thiones |
BR9714510A (pt) | 1996-12-11 | 2000-11-28 | Searle & Co | Processo e preparo de esteróides de 9,11-époxi e intermediários úteis dos mesmos |
UA74141C2 (uk) * | 1998-12-09 | 2005-11-15 | Дж.Д. Сірл Енд Ко. | Фармацевтична композиція на основі тонкоподрібненого еплеренону (варіанти), спосіб її одержання та спосіб лікування розладів, опосередкованих альдостероном (варіанти) |
DK1175220T3 (da) * | 1999-12-08 | 2005-08-29 | Pharmacia Corp | Nanopartikulære eplerenonkompositioner |
-
1999
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