AU2009245294B2 - Methods and compositions for oral administration of exenatide - Google Patents
Methods and compositions for oral administration of exenatide Download PDFInfo
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- AU2009245294B2 AU2009245294B2 AU2009245294A AU2009245294A AU2009245294B2 AU 2009245294 B2 AU2009245294 B2 AU 2009245294B2 AU 2009245294 A AU2009245294 A AU 2009245294A AU 2009245294 A AU2009245294 A AU 2009245294A AU 2009245294 B2 AU2009245294 B2 AU 2009245294B2
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- exenatide
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| US9259456B2 (en) * | 2005-09-06 | 2016-02-16 | Oramed Pharmaceuticals Inc. | Methods and compositions for oral administration of proteins |
| US10058593B2 (en) | 2008-03-26 | 2018-08-28 | Oramed Ltd. | Methods and compositions for oral administration of proteins |
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| CN109157742B (zh) | 2009-08-03 | 2022-04-05 | 因卡伯实验室有限责任公司 | 用于刺激肠道内肠促胰岛素产生的吞咽式囊和方法 |
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| US8562589B2 (en) | 2009-12-24 | 2013-10-22 | Rani Therapeutics, Llc | Swallowable drug delivery device and method of delivery |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US9283179B2 (en) | 2010-12-23 | 2016-03-15 | Rani Therapeutics, Llc | GnRH preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8734429B2 (en) | 2010-12-23 | 2014-05-27 | Rani Therapeutics, Llc | Device, system and methods for the oral delivery of therapeutic compounds |
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| US10639272B2 (en) | 2010-12-23 | 2020-05-05 | Rani Therapeutics, Llc | Methods for delivering etanercept preparations into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9149617B2 (en) | 2010-12-23 | 2015-10-06 | Rani Therapeutics, Llc | Device, system and methods for the oral delivery of therapeutic compounds |
| US8846040B2 (en) | 2010-12-23 | 2014-09-30 | Rani Therapeutics, Llc | Therapeutic agent preparations comprising etanercept for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9629799B2 (en) | 2010-12-23 | 2017-04-25 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9284367B2 (en) | 2010-12-23 | 2016-03-15 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8969293B2 (en) | 2010-12-23 | 2015-03-03 | Rani Therapeutics, Llc | Therapeutic agent preparations comprising exenatide for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9861683B2 (en) | 2010-12-23 | 2018-01-09 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8764733B2 (en) | 2010-12-23 | 2014-07-01 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8809271B2 (en) | 2010-12-23 | 2014-08-19 | Rani Therapeutics, Llc | Therapeutic agent preparations comprising liraglutide for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9415004B2 (en) | 2010-12-23 | 2016-08-16 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8980822B2 (en) | 2010-12-23 | 2015-03-17 | Rani Therapeutics, Llc | Therapeutic agent preparations comprising pramlintide for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8809269B2 (en) | 2010-12-23 | 2014-08-19 | Rani Therapeutics, Llc | Therapeutic agent preparations comprising insulin for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9402807B2 (en) | 2010-12-23 | 2016-08-02 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US9259386B2 (en) | 2010-12-23 | 2016-02-16 | Rani Therapeutics, Llc | Therapeutic preparation comprising somatostatin or somatostatin analogoue for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| CA2814763C (en) | 2011-01-11 | 2019-05-28 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| US20120178813A1 (en) | 2011-01-12 | 2012-07-12 | Thetis Pharmaceuticals Llc | Lipid-lowering antidiabetic agent |
| KR20200006177A (ko) | 2011-03-02 | 2020-01-17 | 제롬 쉔타그 | 단독으로 또는 c형 간염 바이러스 감염과 결합되는 간 지방증의 치료를 위한 조성물, 방법 및 진단 |
| CA3070695C (en) * | 2011-06-29 | 2024-01-23 | Rani Therapeutics, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| DK2800579T3 (da) * | 2012-01-03 | 2017-11-13 | Oramed Ltd | Kapsler indeholdende olie-baserede flydende sammensætninger af kombinerede terapeutiske stoffer til behandling af diabetes |
| JP6567827B2 (ja) | 2012-02-01 | 2019-08-28 | オラムド エルティーディー． | プロテアーゼ阻害剤を含有する組成物、該組成物を含む組成物、および、該組成物を製造および使用する方法 |
| US9382187B2 (en) | 2012-07-10 | 2016-07-05 | Thetis Pharmaceuticals Llc | Tri-salt form of metformin |
| US8765811B2 (en) | 2012-07-10 | 2014-07-01 | Thetis Pharmaceuticals Llc | Tri-salt form of metformin |
| ITFI20120259A1 (it) * | 2012-11-27 | 2014-05-28 | Stefano Bacci | Analoghi del glucagon-like peptide (glp-1) per uso topico. |
| WO2014106846A2 (en) * | 2013-01-03 | 2014-07-10 | Oramed Ltd. | Methods and compositions for treating nafld, hepatic steatosis, and sequelae thereof |
| WO2014152795A2 (en) * | 2013-03-14 | 2014-09-25 | Schentag Jerome J | Cholestosome vesicles for incorporation of molecules into chylomicrons |
| EP2799062A1 (en) * | 2013-05-03 | 2014-11-05 | Gilberto Borges de Brito | Pharmaceutical product for inducing magnified release of endogenous gut hormones, pyy and glp-1, to a therapeutic effect on obesity and dm2 |
| CA2947741A1 (en) | 2014-05-05 | 2015-11-12 | Thetis Pharmaceuticals Llc | Compositions and methods relating to ionic salts of peptides |
| CN113368233A (zh) | 2014-05-15 | 2021-09-10 | 拉尼医疗有限公司 | 包含多肽和/或蛋白质的固体块的药物组合物和该固体块的制备方法 |
| US9242008B2 (en) | 2014-06-18 | 2016-01-26 | Thetis Pharmaceuticals Llc | Mineral amino-acid complexes of fatty acids |
| EA201692548A1 (ru) | 2014-06-18 | 2017-10-31 | ТЕТИС ФАРМАСЬЮТИКАЛЗ ЭлЭлСи | Минеральные аминокислотные комплексы активных веществ |
| US10265384B2 (en) | 2015-01-29 | 2019-04-23 | Novo Nordisk A/S | Tablets comprising GLP-1 agonist and enteric coating |
| CN104740647A (zh) * | 2015-04-08 | 2015-07-01 | 东莞市麦亘生物科技有限公司 | 一种艾塞那肽口服制剂及其制备方法 |
| LT3297653T (lt) | 2015-05-22 | 2022-01-10 | The Board Of Trustees Of The Leland Stanford Junior University | Postbariatrinės hipoglikemijos gydymas glp-1 antagonistais |
| RU2702690C2 (ru) * | 2015-08-13 | 2019-10-09 | БИОЛИНГУС АйПи ЛЛСи | Способ получения продуктов, содержащих стабилизированные активные вещества, и композиций, содержащих таковые |
| US10653753B2 (en) | 2016-03-04 | 2020-05-19 | Eiger Biopharmaceuticals, Inc. | Treatment of hyperinsulinemic hypoglycemia with exendin-4 derivatives |
| JP6906047B2 (ja) | 2016-06-03 | 2021-07-21 | テティス・ファーマシューティカルズ・エルエルシー | 特異的炎症収束性メディエーターの塩に関連する組成物及び方法 |
| HRP20250278T1 (hr) | 2016-11-21 | 2025-04-25 | Amylyx Pharmaceuticals, Inc. | Puferovane formulacije eksendina (9-39) |
| US20220233487A1 (en) | 2019-05-06 | 2022-07-28 | Evonik Operations Gmbh | Preparation for use in weight management comprising omega-3 fatty acid salts and basic amino acids |
| CN112057619A (zh) | 2019-06-10 | 2020-12-11 | 苏州兰鼎生物制药有限公司 | 一种具有降血糖作用的药物组合物 |
| AU2021211236B2 (en) * | 2020-01-23 | 2025-12-18 | Axcess (UK) Ltd | Cellular uptake |
| WO2021166899A1 (ja) * | 2020-02-17 | 2021-08-26 | 宇部興産株式会社 | インクレチン様物質と組み合わせて使用するための消化管プロテアーゼ阻害剤を含む薬剤 |
| FR3120189B1 (fr) | 2021-03-01 | 2024-11-29 | Farid Bennis | Composition pharmaceutique pour une administration par voie orale d’un agoniste du récepteur du GLP-1 |
| US12384744B2 (en) | 2021-09-29 | 2025-08-12 | Ensysce Biosciences Inc. | Enzyme-cleavable methadone prodrugs and methods of use thereof |
| EP4545069A1 (en) * | 2022-06-24 | 2025-04-30 | Sunsho Pharmaceutical Co., Ltd. | Pharmaceutical composition and method for producing same |
| WO2025090920A1 (en) * | 2023-10-25 | 2025-05-01 | Piton Therapeutics, Inc. | Compositions and methods for treating dysfunction of glucose metabolism and/or regulation |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009118722A2 (en) * | 2008-03-26 | 2009-10-01 | Oramed Pharmaceuticals, Inc. | Methods and compositions for oral administration of proteins |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL68769A (en) * | 1983-05-23 | 1986-02-28 | Hadassah Med Org | Pharmaceutical compositions containing insulin for oral administration |
| JPS6350793A (ja) | 1986-08-20 | 1988-03-03 | 株式会社東芝 | 高速増殖炉の崩壊熱除去システム |
| US5034415A (en) | 1987-08-07 | 1991-07-23 | Century Laboratories, Inc. | Treatment of diabetes mellitus |
| ES2045276T3 (es) | 1988-07-21 | 1994-01-16 | Hoffmann La Roche | Preparacion de insulina |
| JPH02250823A (ja) * | 1989-03-24 | 1990-10-08 | Tsumura & Co | マイクロカプセル剤およびその製造方法 |
| GB9007052D0 (en) | 1990-03-29 | 1990-05-30 | Skua Investments Ltd | Pharmaceutical formulations |
| US5206219A (en) * | 1991-11-25 | 1993-04-27 | Applied Analytical Industries, Inc. | Oral compositions of proteinaceous medicaments |
| US6692766B1 (en) * | 1994-06-15 | 2004-02-17 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Controlled release oral drug delivery system |
| US5824638A (en) * | 1995-05-22 | 1998-10-20 | Shire Laboratories, Inc. | Oral insulin delivery |
| IL114673A (en) | 1995-07-19 | 2000-12-06 | Hadasit Med Res Service | Pharmaceutical compositions containing protein for oral administration |
| JPH09208485A (ja) * | 1996-01-31 | 1997-08-12 | Teijin Ltd | ペプチド・蛋白質性薬物の水難溶性組成物 |
| US6858576B1 (en) * | 1996-08-08 | 2005-02-22 | Amylin Pharmaceuticals, Inc. | Methods for regulating gastrointestinal motility |
| JPH10330287A (ja) * | 1997-03-31 | 1998-12-15 | Nippon Suisan Kaisha Ltd | 多価不飽和脂肪酸からなる消化管吸収促進剤およびそれを含有する薬剤 |
| US5975893A (en) | 1997-06-20 | 1999-11-02 | Align Technology, Inc. | Method and system for incrementally moving teeth |
| JP2000050793A (ja) * | 1998-08-07 | 2000-02-22 | Meiji Milk Prod Co Ltd | 人工乳組成物 |
| JP2000128805A (ja) | 1998-10-27 | 2000-05-09 | Nippon Suisan Kaisha Ltd | 多価不飽和脂肪酸および高分子ゲルからなる経粘膜吸収促進剤及びそれを含有する薬剤 |
| US6761903B2 (en) | 1999-06-30 | 2004-07-13 | Lipocine, Inc. | Clear oil-containing pharmaceutical compositions containing a therapeutic agent |
| JP2001240558A (ja) | 2000-02-29 | 2001-09-04 | Nippon Suisan Kaisha Ltd | 多価不飽和脂肪酸を経粘膜吸収促進剤として含有する固形製剤。 |
| US6673574B2 (en) | 2000-11-30 | 2004-01-06 | Unigene Laboratories Inc. | Oral delivery of peptides using enzyme-cleavable membrane translocators |
| KR20010069322A (ko) | 2001-03-08 | 2001-07-25 | 서종수 | 휴대형정보단말기 또는 화상이동통신장치를 이용한전자경매방법 |
| CN1160122C (zh) | 2001-04-20 | 2004-08-04 | 清华大学 | 一种制备口服胰岛素油相制剂的方法 |
| MXPA04000521A (es) | 2001-07-18 | 2005-09-08 | Solae Llc | Concentrado inhibidor de bowman-birk, de alto contenido en proteinas y proceso para su manufactura. |
| US20030198666A1 (en) | 2002-01-07 | 2003-10-23 | Richat Abbas | Oral insulin therapy |
| US7767828B2 (en) | 2003-11-12 | 2010-08-03 | Phenomix Corporation | Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| US20060286129A1 (en) * | 2003-12-19 | 2006-12-21 | Emisphere Technologies, Inc. | Oral GLP-1 formulations |
| US20050143303A1 (en) * | 2003-12-26 | 2005-06-30 | Nastech Pharmaceutical Company Inc. | Intranasal administration of glucose-regulating peptides |
| US8076288B2 (en) | 2004-02-11 | 2011-12-13 | Amylin Pharmaceuticals, Inc. | Hybrid polypeptides having glucose lowering activity |
| AU2005329255B2 (en) | 2004-04-15 | 2010-09-30 | Chiasma, Inc. | Compositions capable of facilitating penetration across a biological barrier |
| KR101276754B1 (ko) | 2004-07-19 | 2013-06-19 | 바이오콘 리미티드 | 인슐린―올리고머 접합체，제형 및 이들의 용도 |
| US20060046962A1 (en) * | 2004-08-25 | 2006-03-02 | Aegis Therapeutics Llc | Absorption enhancers for drug administration |
| WO2006025882A2 (en) * | 2004-08-25 | 2006-03-09 | The Uab Research Foundation | Absorption enhancers for drug administration |
| US9259456B2 (en) * | 2005-09-06 | 2016-02-16 | Oramed Pharmaceuticals Inc. | Methods and compositions for oral administration of proteins |
| US20070086972A1 (en) | 2005-09-12 | 2007-04-19 | Jacob Birnbaum | Hair growth compositions and methods for treating hair loss or related conditions |
| US20070077283A1 (en) * | 2005-09-30 | 2007-04-05 | Nastech Pharmaceutical Company Inc. | Method of enhancing transmucosal delivery of therapeutic compounds |
| CN101095942B (zh) * | 2006-06-30 | 2011-11-16 | 北京民海生物科技有限公司 | 一种包含稳定剂的Exendin-4注射剂药物配方 |
| NO2300031T3 (enExample) | 2008-05-05 | 2018-02-17 | ||
| CL2009001425A1 (es) | 2008-06-17 | 2010-04-30 | Univ Indiana Res & Tech Corp | Analogos de glucagon con un aminoacido aromatico grande que carece de cadena lateral de imidazol que le confiere actividad agonista del receptor gip; composiciones farmaceutica; kit que los contiene y uso para reducir el aumento de peso, tratar la diabetes o inducir paralisis del tracto intestinal. |
| ES2823233T3 (es) | 2008-08-18 | 2021-05-06 | Entera Bio Ltd | Métodos y composiciones para la administración oral de proteínas |
| DK2800579T3 (da) | 2012-01-03 | 2017-11-13 | Oramed Ltd | Kapsler indeholdende olie-baserede flydende sammensætninger af kombinerede terapeutiske stoffer til behandling af diabetes |
| JP6567827B2 (ja) | 2012-02-01 | 2019-08-28 | オラムド エルティーディー． | プロテアーゼ阻害剤を含有する組成物、該組成物を含む組成物、および、該組成物を製造および使用する方法 |
| WO2014106846A2 (en) | 2013-01-03 | 2014-07-10 | Oramed Ltd. | Methods and compositions for treating nafld, hepatic steatosis, and sequelae thereof |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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