RU2014152320A - PHARMACEUTICAL COMPOSITIONS CONTAINING GLUCAGON-LIKE PEPTIDE 1 (GLP-1) - Google Patents

PHARMACEUTICAL COMPOSITIONS CONTAINING GLUCAGON-LIKE PEPTIDE 1 (GLP-1) Download PDF

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RU2014152320A
RU2014152320A RU2014152320A RU2014152320A RU2014152320A RU 2014152320 A RU2014152320 A RU 2014152320A RU 2014152320 A RU2014152320 A RU 2014152320A RU 2014152320 A RU2014152320 A RU 2014152320A RU 2014152320 A RU2014152320 A RU 2014152320A
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glp
diketopiperazine
dry powder
powder composition
composition according
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RU2014152320A
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Стефани ГРИН
Дэвид БРАНДТ
Кохава ГЕЛЬБЕР
Марк КИНГ
Вэйман Вэнделл ЧИЗАМ
Кит ОБЕРГ
Андреа ЛЕОНЕ-БЭЙ
Марк Дж. ХОУКЕНСОН
Мэри Фейрис
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Маннкайнд Корпорейшн
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Abstract

1. Сухая порошкообразная композиция, содержащая микрочастицы, включающие дикетопиперазин и гликагон-подобный пептид GLP-1.2. Сухая порошкообразная композиция по п. 1, где указанный GLP-1 выбран из группы, состоящей из нативных GLP-1, метаболитов GLP-1, аналогов GLP-1, производных GLP-1, GLP-1, защищенных от действия дипептидил-пептидазы-IV (DPP-IV), миметиков GLP-1, аналогов пептида GLP-1 или биосинтетических аналогов GLP-1.3. Сухая порошкообразная композиция по п. 1, где указанным дикетопиперазином является дикетопиперазин 2,5-дикето-3,6-ди(4-X-аминобутил)пиперазин, где X выбран из группы, состоящей из сукцинила, глутарила, малеила и фумарила.4. Сухая порошкообразная композиция по п. 3, где указанным дикетопиперазином является 2,5-дикето-3,6-ди-(4-фумарил- аминобутил)пиперазин.5. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является нативный GLP-1.6. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является амидированный GLP-1.7. Сухая порошкообразная композиция по п. 6, где указанным амидированным GLP-1 является GLP-1(7-36)амид.8. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является GLP-1, защищенный от действия DPP-IV.9. Способ образования частицы, включающей GLP-1 и дикетопиперазин, включающий стадии:обеспечения GLP-1;обеспечения дикетопиперазина в форме, выбранной из дикетопиперазина образующего частицы, частиц дикетопиперазина, и их комбинаций; иобъединения указанного GLP-1 и указанного дикетопиперазина в форме сорастворителя, где образуется частица, включающая GLP-1 и дикетопиперазин.10. Способ по п. 9, дополнительно включающий удаление растворителя из указанного сорастворителя лиофилизацией, фильтрацией или сушкой распылением.11. Способ по п. 10, где указанная частица, включающая GLP-1 и дикетопиперазин образуется удалением указанного раство1. A dry powder composition containing microparticles, including diketopiperazine and glycagon-like peptide GLP-1.2. The dry powder composition according to claim 1, wherein said GLP-1 is selected from the group consisting of native GLP-1, GLP-1 metabolites, GLP-1 analogs, GLP-1 derivatives, GLP-1, protected against dipeptidyl peptidase- IV (DPP-IV), GLP-1 mimetics, GLP-1 peptide analogues or GLP-1.3 biosynthetic analogues. The dry powder composition according to claim 1, wherein said diketopiperazine is 2,5-diketo-3,6-di (4-X-aminobutyl) piperazine diketopiperazine, wherein X is selected from the group consisting of succinyl, glutaryl, maleyl and fumaril. . The dry powder composition according to claim 3, wherein said diketopiperazine is 2,5-diketo-3,6-di- (4-fumaryl-aminobutyl) piperazine. 5. The dry powder composition according to claim 1, wherein said GLP-1 is native GLP-1.6. The dry powder composition according to claim 1, wherein said GLP-1 is amidated GLP-1.7. The dry powder composition according to claim 6, wherein said amidated GLP-1 is GLP-1 (7-36) amide. The dry powder composition according to claim 1, wherein said GLP-1 is GLP-1 protected against the action of DPP-IV.9. A method of forming a particle comprising GLP-1 and diketopiperazine, comprising the steps of: providing GLP-1; providing diketopiperazine in a form selected from diketopiperazine-forming particles, diketopiperazine particles, and combinations thereof; and combining said GLP-1 and said diketopiperazine in the form of a co-solvent, where a particle is formed comprising GLP-1 and diketopiperazine. 10. The method of claim 9, further comprising removing the solvent from said co-solvent by lyophilization, filtration, or spray drying. The method of claim 10, wherein said particle comprising GLP-1 and diketopiperazine is formed by removing said solution

Claims (32)

1. Сухая порошкообразная композиция, содержащая микрочастицы, включающие дикетопиперазин и гликагон-подобный пептид GLP-1.1. A dry powder composition containing microparticles, including diketopiperazine and glycagon-like peptide GLP-1. 2. Сухая порошкообразная композиция по п. 1, где указанный GLP-1 выбран из группы, состоящей из нативных GLP-1, метаболитов GLP-1, аналогов GLP-1, производных GLP-1, GLP-1, защищенных от действия дипептидил-пептидазы-IV (DPP-IV), миметиков GLP-1, аналогов пептида GLP-1 или биосинтетических аналогов GLP-1.2. The dry powder composition according to claim 1, wherein said GLP-1 is selected from the group consisting of native GLP-1, GLP-1 metabolites, GLP-1 analogs, GLP-1, GLP-1 derivatives protected against dipeptidyl- peptidase-IV (DPP-IV), GLP-1 mimetics, GLP-1 peptide analogues, or GLP-1 biosynthetic analogues. 3. Сухая порошкообразная композиция по п. 1, где указанным дикетопиперазином является дикетопиперазин 2,5-дикето-3,6-ди(4-X-аминобутил)пиперазин, где X выбран из группы, состоящей из сукцинила, глутарила, малеила и фумарила.3. The dry powder composition according to claim 1, wherein said diketopiperazine is diketopiperazine 2,5-diketo-3,6-di (4-X-aminobutyl) piperazine, where X is selected from the group consisting of succinyl, glutaryl, maleyl and fumaril . 4. Сухая порошкообразная композиция по п. 3, где указанным дикетопиперазином является 2,5-дикето-3,6-ди-(4-фумарил- аминобутил)пиперазин.4. The dry powder composition according to claim 3, wherein said diketopiperazine is 2,5-diketo-3,6-di- (4-fumaryl-aminobutyl) piperazine. 5. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является нативный GLP-1.5. The dry powder composition according to claim 1, wherein said GLP-1 is native GLP-1. 6. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является амидированный GLP-1.6. The dry powder composition according to claim 1, wherein said GLP-1 is amidated GLP-1. 7. Сухая порошкообразная композиция по п. 6, где указанным амидированным GLP-1 является GLP-1(7-36)амид.7. The dry powder composition according to claim 6, wherein said amidated GLP-1 is GLP-1 (7-36) amide. 8. Сухая порошкообразная композиция по п. 1, где указанным GLP-1 является GLP-1, защищенный от действия DPP-IV.8. The dry powder composition according to claim 1, wherein said GLP-1 is GLP-1 protected against DPP-IV. 9. Способ образования частицы, включающей GLP-1 и дикетопиперазин, включающий стадии: 9. A method of forming a particle comprising GLP-1 and diketopiperazine, comprising the steps of: обеспечения GLP-1; providing GLP-1; обеспечения дикетопиперазина в форме, выбранной из дикетопиперазина образующего частицы, частиц дикетопиперазина, и их комбинаций; и providing diketopiperazine in a form selected from diketopiperazine forming particles, diketopiperazine particles, and combinations thereof; and объединения указанного GLP-1 и указанного дикетопиперазина в форме сорастворителя, где образуется частица, включающая GLP-1 и дикетопиперазин. combining said GLP-1 and said diketopiperazine in the form of a co-solvent, where a particle is formed comprising GLP-1 and diketopiperazine. 10. Способ по п. 9, дополнительно включающий удаление растворителя из указанного сорастворителя лиофилизацией, фильтрацией или сушкой распылением. 10. The method of claim 9, further comprising removing the solvent from said co-solvent by lyophilization, filtration, or spray drying. 11. Способ по п. 10, где указанная частица, включающая GLP-1 и дикетопиперазин образуется удалением указанного растворителя. 11. The method of claim 10, wherein said particle comprising GLP-1 and diketopiperazine is formed by removing said solvent. 12. Способ по п. 10, где указанная частица, включающая GLP-1 и дикетопиперазин образуется до удаления указанного растворителя. 12. The method of claim 10, wherein said particle comprising GLP-1 and diketopiperazine is formed prior to removal of said solvent. 13. Способ по п. 9, где указанный GLP-1 выбран из группы, состоящей из нативного GLP-1, аналога GLP-1, производного GLP-1, GLP-1, защищенного от действия дипептидил-пептидазы IV (DPP-IV), GLP-1-миметика, аналога пептида GLP-1 или биосинтетического аналога GLP-1.13. The method according to p. 9, where the specified GLP-1 is selected from the group consisting of native GLP-1, an analog of GLP-1, a derivative of GLP-1, GLP-1, protected from the action of dipeptidyl peptidase IV (DPP-IV) , GLP-1 mimetic, GLP-1 peptide analog, or GLP-1 biosynthetic analog. 14. Способ по п. 9, где указанный GLP-1 обеспечивают в форме раствора, содержащего GLP-1 в концентрации, составляющей 1 мкг/мл - 50 мг/мл.14. The method of claim 9, wherein said GLP-1 is provided in the form of a solution containing GLP-1 at a concentration of 1 μg / ml to 50 mg / ml. 15. Способ по п. 9, где указанный GLP-1 обеспечивают в форме раствора, содержащего GLP-1 в концентрации, составляющей 0,1 мг/мл - 10 мг/мл.15. The method of claim 9, wherein said GLP-1 is provided in the form of a solution containing GLP-1 at a concentration of 0.1 mg / ml to 10 mg / ml. 16. Способ по п. 9, где указанный GLP-1 обеспечивают в форме раствора, содержащего GLP-1 в концентрации, составляющей 0,25 мг/мл.16. The method of claim 9, wherein said GLP-1 is provided in the form of a solution containing GLP-1 at a concentration of 0.25 mg / ml. 17. Способ по п. 9, где указанный дикетопиперазин обеспечивают в форме суспензии частиц дикетопиперазина. 17. The method of claim 9, wherein said diketopiperazine is provided in the form of a suspension of diketopiperazine particles. 18. Способ по п. 9, где указанный дикетопиперазин обеспечивают в форме раствора, включающего дикетопиперазин, образующий частицы, где указанный способ дополнительно включает доведение pH указанного раствора до образования частиц дикетопиперазина. 18. The method of claim 9, wherein said diketopiperazine is provided in the form of a solution comprising particles forming diketopiperazine, wherein said method further comprises adjusting the pH of said solution to form diketopiperazine particles. 19. Способ по п. 17 или 18, дополнительно включающий добавление агента к указанному раствору или суспензии, где средство выбрано из группы, состоящей из солей, поверхностно-активных веществ, ионов, осмолитов, хаотропов и лиотропов, кислот, оснований и органических растворителей. 19. The method according to p. 17 or 18, further comprising adding an agent to the specified solution or suspension, where the agent is selected from the group consisting of salts, surfactants, ions, osmolytes, chaotropes and lyotropes, acids, bases and organic solvents. 20. Способ по п. 19, где указанный агент способствует ассоциации указанного GLP-1 с указанными частицами дикетопиперазина или указанным дикетопиперазином, образующим частицы. 20. The method of claim 19, wherein said agent facilitates the association of said GLP-1 with said particles of diketopiperazine or said diketopiperazine forming particles. 21. Способ по п. 19, где указанный агент улучшает стабильность или фармакодинамику указанного GLP-1. 21. The method of claim 19, wherein said agent improves the stability or pharmacodynamics of said GLP-1. 22. Способ по п. 19, где указанным агентом является хлорид натрия. 22. The method according to p. 19, where the specified agent is sodium chloride. 23. Способ по п. 17 или 18, дополнительно включающий доведение pH указанной суспензии или раствора. 23. The method of claim 17 or 18, further comprising adjusting the pH of said suspension or solution. 24. Способ по п. 23, где pH доводят до 4 или выше. 24. The method of claim 23, wherein the pH is adjusted to 4 or higher. 25. Способ по п. 9, где указанный GLP-1 в указанной частице имеет большую стабильность. 25. The method of claim 9, wherein said GLP-1 in said particle has greater stability. 26. Способ по п. 9, где концентрация GLP-1 в указанном сорастворе составляет 1 мкг/мл - 50 мг/мл. 26. The method of claim 9, wherein the concentration of GLP-1 in said co-solution is 1 μg / ml to 50 mg / ml. 27. Способ по п. 9, где концентрация GLP-1 в указанном сорастворе составляет 0,1 мг/мл - 10 мг/мл. 27. The method of claim 9, wherein the concentration of GLP-1 in said co-solution is 0.1 mg / ml to 10 mg / ml. 28. Способ по п. 9, где концентрация GLP-1 в указанном сорастворе составляет 0,25 мг/мл. 28. The method of claim 9, wherein the concentration of GLP-1 in said co-solution is 0.25 mg / ml. 29. Способ по п. 9, дополнительно включающий добавление средства к указанному сораствору или суспензии, где средство выбрано из группы, состоящей из солей, поверхностно-активных веществ, ионов, осмолитов, хаотропов и лиотропов, кислот, оснований и органических растворителей. 29. The method of claim 9, further comprising adding the agent to said co-solution or suspension, wherein the agent is selected from the group consisting of salts, surfactants, ions, osmolytes, chaotropes and lyotropes, acids, bases and organic solvents. 30. Способ по п. 29, где указанный агент способствует ассоциации указанного GLP-1 с указанными частицами дикетопиперазина или указанным дикетопиперазином, образующим частицы. 30. The method of claim 29, wherein said agent promotes association of said GLP-1 with said diketopiperazine particles or said diketopiperazine forming particles. 31. Способ по п. 29, где указанный агент улучшает стабильность или фармакодинамику указанного GLP-1. 31. The method according to p. 29, where the specified agent improves the stability or pharmacodynamics of the specified GLP-1. 32. Способ по п. 29, где указанным агентом является хлорид натрия. 32. The method according to p. 29, where the specified agent is sodium chloride.
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Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9006175B2 (en) 1999-06-29 2015-04-14 Mannkind Corporation Potentiation of glucose elimination
PT1808438E (en) 1999-06-29 2015-01-14 Mannkind Corp Purification and stabilization of peptide and proteins in pharmaceutical agents
WO2003080149A2 (en) 2002-03-20 2003-10-02 Mannkind Corporation Inhalation apparatus
US8921311B2 (en) 2003-08-01 2014-12-30 Mannkind Corporation Method for treating hyperglycemia
JP5078014B2 (en) 2004-08-20 2012-11-21 マンカインド コーポレイション Catalytic reaction of diketopiperazine synthesis.
HUE026797T2 (en) 2004-08-23 2016-07-28 Mannkind Corp Diketopiperazine salts for drug delivery
KR20120060245A (en) 2005-09-14 2012-06-11 맨카인드 코포레이션 Method of drug formulation based on increasing the affinity of crystalline microparticle surfaces for active agents
EP2497484A3 (en) 2006-02-22 2012-11-07 MannKind Corporation A method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent
EP2010155A2 (en) * 2006-04-14 2009-01-07 MannKind Corporation Glucagon-like peptide 1(glp-1) pharmaceutical formulations
US8785396B2 (en) 2007-10-24 2014-07-22 Mannkind Corporation Method and composition for treating migraines
KR20100090692A (en) 2007-10-24 2010-08-16 맨카인드 코포레이션 Delivery of active agents
WO2009055740A2 (en) 2007-10-24 2009-04-30 Mannkind Corporation Method of preventing adverse effects by glp-1
EP2300011A4 (en) 2008-05-27 2012-06-20 Dmi Life Sciences Inc Therapeutic methods and compounds
US8485180B2 (en) 2008-06-13 2013-07-16 Mannkind Corporation Dry powder drug delivery system
EP3281663B8 (en) 2008-06-13 2022-09-21 MannKind Corporation Breath powered dry powder inhaler for drug delivery
US9364619B2 (en) 2008-06-20 2016-06-14 Mannkind Corporation Interactive apparatus and method for real-time profiling of inhalation efforts
TWI494123B (en) 2008-08-11 2015-08-01 Mannkind Corp Use of ultrarapid acting insulin
US8314106B2 (en) 2008-12-29 2012-11-20 Mannkind Corporation Substituted diketopiperazine analogs for use as drug delivery agents
AU2010203573A1 (en) 2009-01-08 2011-06-30 Mannkind Corporation Method for treating hyperglycemia with GLP-1
TWI528982B (en) * 2009-03-04 2016-04-11 曼凱公司 An improved dry powder drug delivery system
CA2754595C (en) 2009-03-11 2017-06-27 Mannkind Corporation Apparatus, system and method for measuring resistance of an inhaler
EP3556356B1 (en) 2009-06-12 2021-05-05 MannKind Corporation Diketopiperazine microparticles with defined isomer content
WO2010144789A2 (en) 2009-06-12 2010-12-16 Mannkind Corporation Diketopiperazine microparticles with defined specific surface areas
US8642548B2 (en) * 2009-08-07 2014-02-04 Mannkind Corporation Val (8) GLP-1 composition and method for treating functional dyspepsia and/or irritable bowel syndrome
CA2778698A1 (en) 2009-11-03 2011-05-12 Mannkind Corporation An apparatus and method for simulating inhalation efforts
AU2011271097B2 (en) 2010-06-21 2014-11-27 Mannkind Corporation Dry powder drug delivery system and methods
WO2012033792A2 (en) 2010-09-07 2012-03-15 Dmi Acquisition Corp. Treatment of diseases
CN105667994B (en) 2011-04-01 2018-04-06 曼金德公司 Blister package for pharmaceutical kit
WO2012174472A1 (en) 2011-06-17 2012-12-20 Mannkind Corporation High capacity diketopiperazine microparticles
US8980834B2 (en) 2011-10-10 2015-03-17 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
WO2013055749A1 (en) 2011-10-10 2013-04-18 Ampio Pharmaceuticals, Inc. Implantable medical devices with increased immune tolerance, and methods for making and implanting
KR20140095483A (en) 2011-10-24 2014-08-01 맨카인드 코포레이션 Methods and compositions for treating pain
BR112014008036A2 (en) 2011-10-28 2017-04-11 Ampio Pharmaceuticals Inc rhinitis treatment
BR112014032938A2 (en) 2012-07-01 2017-08-01 Novo Nordisk As use of long-acting glp-1 peptides
DK2872205T3 (en) 2012-07-12 2017-02-27 Mannkind Corp DRY POWDER FORMAL ADMINISTRATION SYSTEM
JP2015526523A (en) * 2012-08-29 2015-09-10 マンカインド コーポレイション Methods and compositions for the treatment of hyperglycemia
UA116217C2 (en) 2012-10-09 2018-02-26 Санофі Exendin-4 derivatives as dual glp1/glucagon agonists
WO2014066856A1 (en) 2012-10-26 2014-05-01 Mannkind Corporation Inhalable influenza vaccine compositions and methods
AU2013366691A1 (en) 2012-12-21 2015-07-09 Sanofi Exendin-4 derivatives
KR102499439B1 (en) * 2013-03-15 2023-02-13 맨카인드 코포레이션 Microcrystalline diketopiperazine compositions and methods
SG10201707619RA (en) 2013-03-15 2017-10-30 Ampio Pharmaceuticals Inc Compositions for the mobilization, homing, expansion and differentiation of stem cells and methods of using the same
WO2015010092A1 (en) 2013-07-18 2015-01-22 Mannkind Corporation Heat-stable dry powder pharmaceutical compositions and methods
JP2016530930A (en) 2013-08-05 2016-10-06 マンカインド コーポレイション Ventilation device and method
US9782344B2 (en) 2013-08-22 2017-10-10 Zp Opco, Inc. Stable glucagon peptide formulations
WO2015027173A1 (en) * 2013-08-22 2015-02-26 Zp Opco, Inc. Stable glucagon peptide formulations
TW201609799A (en) 2013-12-13 2016-03-16 賽諾菲公司 Dual GLP-1/GIP receptor agonists
TW201609797A (en) 2013-12-13 2016-03-16 賽諾菲公司 Dual GLP-1/glucagon receptor agonists
EP3080150B1 (en) 2013-12-13 2018-08-01 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
TW201609796A (en) 2013-12-13 2016-03-16 賽諾菲公司 Non-acylated EXENDIN-4 peptide analogues
AU2015233635B2 (en) 2014-03-18 2019-07-25 Apeptico Forschung Und Entwicklung Gmbh Dry-powder peptide medicament
WO2015148905A1 (en) 2014-03-28 2015-10-01 Mannkind Corporation Use of ultrarapid acting insulin
TW201625669A (en) 2014-04-07 2016-07-16 賽諾菲公司 Peptidic dual GLP-1/glucagon receptor agonists derived from Exendin-4
TW201625668A (en) 2014-04-07 2016-07-16 賽諾菲公司 Exendin-4 derivatives as peptidic dual GLP-1/glucagon receptor agonists
TW201625670A (en) 2014-04-07 2016-07-16 賽諾菲公司 Dual GLP-1/glucagon receptor agonists derived from EXENDIN-4
US9932381B2 (en) 2014-06-18 2018-04-03 Sanofi Exendin-4 derivatives as selective glucagon receptor agonists
EP4066836A1 (en) 2014-08-18 2022-10-05 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
US10561806B2 (en) 2014-10-02 2020-02-18 Mannkind Corporation Mouthpiece cover for an inhaler
AR105319A1 (en) 2015-06-05 2017-09-27 Sanofi Sa PROPHARMS THAT INCLUDE A DUAL AGONIST GLU-1 / GLUCAGON CONJUGATE HIALURONIC ACID CONNECTOR
WO2016209969A1 (en) 2015-06-22 2016-12-29 Ampio Pharmaceuticals, Inc. Use of low molecular weight fractions of human serum albumin in treating diseases
TW201706291A (en) 2015-07-10 2017-02-16 賽諾菲公司 New EXENDIN-4 derivatives as selective peptidic dual GLP-1/glucagon receptor agonists
CN108066762B (en) * 2016-11-07 2022-04-01 赫兰 Application of GLP-1 receptor agonist drugs
TWI705820B (en) * 2018-06-22 2020-10-01 美商美國禮來大藥廠 Gip/glp1 agonist compositions
CN109827875A (en) * 2019-04-10 2019-05-31 上海市食品药品检验所 A kind of device and method for measuring sucking preparation dissolution rate
KR20210062509A (en) 2019-11-21 2021-05-31 대한민국(전북기계공업고등학교장) filterless dynamic fine dust air purifier
CN115192554A (en) * 2022-08-08 2022-10-18 浙江仙琚萃泽医药科技有限公司 Propellant-free peptide-containing inhalation solution and preparation method thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5352461A (en) * 1992-03-11 1994-10-04 Pharmaceutical Discovery Corporation Self assembling diketopiperazine drug delivery system
DE4242863A1 (en) * 1992-12-18 1994-06-23 Boehringer Mannheim Gmbh Stable lyophilized pharmaceutical preparations of G-CSF
ATE273996T1 (en) * 1997-09-12 2004-09-15 Pharis Biotec Gmbh COMPOSITION FOR THE THERAPY OF DIABETES MELLITUS AND OBESITY
PT1808438E (en) * 1999-06-29 2015-01-14 Mannkind Corp Purification and stabilization of peptide and proteins in pharmaceutical agents
JP2005506956A (en) * 2001-06-01 2005-03-10 イーライ・リリー・アンド・カンパニー Long-acting GLP-1 formulation
RU2332229C2 (en) * 2002-02-20 2008-08-27 Эмисфире Текнолоджис Инк. Method of glp-1 molecules introduction
WO2003075834A2 (en) * 2002-03-08 2003-09-18 Eli Lilly And Company Activated protein c formulations
US20040038865A1 (en) * 2002-08-01 2004-02-26 Mannkind Corporation Cell transport compositions and uses thereof
EP1545457A4 (en) * 2002-08-01 2009-07-01 Mannkind Corp Cell transport compositions and uses thereof
CA2528007C (en) * 2003-06-02 2012-03-27 Chiron Corporation Immunogenic compositions based on microparticles comprising adsorbed toxoid and a polysaccharide-containing antigen
HUE026797T2 (en) * 2004-08-23 2016-07-28 Mannkind Corp Diketopiperazine salts for drug delivery
KR20120060245A (en) * 2005-09-14 2012-06-11 맨카인드 코포레이션 Method of drug formulation based on increasing the affinity of crystalline microparticle surfaces for active agents
EP2497484A3 (en) * 2006-02-22 2012-11-07 MannKind Corporation A method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent
EP2010155A2 (en) * 2006-04-14 2009-01-07 MannKind Corporation Glucagon-like peptide 1(glp-1) pharmaceutical formulations

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