WO2005018603A3 - Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen herstellung sowie dessen verwendung als inhalativum - Google Patents

Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen herstellung sowie dessen verwendung als inhalativum Download PDF

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Publication number
WO2005018603A3
WO2005018603A3 PCT/EP2004/009012 EP2004009012W WO2005018603A3 WO 2005018603 A3 WO2005018603 A3 WO 2005018603A3 EP 2004009012 W EP2004009012 W EP 2004009012W WO 2005018603 A3 WO2005018603 A3 WO 2005018603A3
Authority
WO
WIPO (PCT)
Prior art keywords
production
microparticles
inhalant
bibn
spray
Prior art date
Application number
PCT/EP2004/009012
Other languages
English (en)
French (fr)
Other versions
WO2005018603A2 (de
Inventor
Michael Trunk
Claudius Weiler
Original Assignee
Boehringer Ingelheim Int
Boehringer Ingelheim Pharma
Michael Trunk
Claudius Weiler
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int, Boehringer Ingelheim Pharma, Michael Trunk, Claudius Weiler filed Critical Boehringer Ingelheim Int
Priority to EP04764016A priority Critical patent/EP1663149A2/de
Priority to JP2006523576A priority patent/JP2007502789A/ja
Priority to CA002536047A priority patent/CA2536047A1/en
Publication of WO2005018603A2 publication Critical patent/WO2005018603A2/de
Publication of WO2005018603A3 publication Critical patent/WO2005018603A3/de

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine

Abstract

Die Erfindung betrifft den CGRP-Antagonisten 1 [N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin (A) oder dessen physiologisch verträgliche Salze, die in amorphem Zustand unter Normalbedingungen (T < 50°C, relative Feuchte < 75%) stabil und in Form von Mikropartikeln vorliegen, Verfahren zur Herstellung von Mikropartikeln aus diesen Substanzen sowie die Verwendung dieser Partikel zur Herstellung eines Arzneimittels der Applikationsform Pulverinhalativum zur pulmonalen und nasalen Inhalation, insbesondere zur Herstellung eines Arzneimittels zur Behandlung von Kopfschmerzen, Migräne und Cluster Headache.
PCT/EP2004/009012 2003-08-18 2004-08-12 Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen herstellung sowie dessen verwendung als inhalativum WO2005018603A2 (de)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP04764016A EP1663149A2 (de) 2003-08-18 2004-08-12 Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen h erstellung sowie dessen verwendung als inhalativum
JP2006523576A JP2007502789A (ja) 2003-08-18 2004-08-12 噴霧乾燥された無定形ｂｉｂｎ４０９６、その調製方法及び吸入剤としてのその使用
CA002536047A CA2536047A1 (en) 2003-08-18 2004-08-12 Spray-dried amorphous bibn 4096 method for production and use thereof as inhalant

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEDE10338402.2 2003-08-18
DE2003138402 DE10338402A1 (de) 2003-08-18 2003-08-18 Sprühgetrocknetes, amorphes BIBN 4096, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum

Publications (2)

Publication Number Publication Date
WO2005018603A2 WO2005018603A2 (de) 2005-03-03
WO2005018603A3 true WO2005018603A3 (de) 2005-07-21

Family

ID=34201781

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/009012 WO2005018603A2 (de) 2003-08-18 2004-08-12 Sprühgetrocknetes, amorphes bibn 4096, verfahren zu dessen herstellung sowie dessen verwendung als inhalativum

Country Status (5)

Country Link
EP (1) EP1663149A2 (de)
JP (1) JP2007502789A (de)
CA (1) CA2536047A1 (de)
DE (1) DE10338402A1 (de)
WO (1) WO2005018603A2 (de)

Families Citing this family (29)

* 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
ES2425392T3 (es) 2002-03-20 2013-10-15 Mannkind Corporation Cartucho para un aparato de inhalación
DE10338407A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Inhalationspulver enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin
DE10338399A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Mikropartikel, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-Iysyl]-4-(4-pyridinyl)-piperazin, Verfahren zu deren Herstellung sowie deren Verwendung als Inhalaltionspulver
ATE486064T1 (de) 2004-08-20 2010-11-15 Mannkind Corp Katalyse der diketopiperazinsynthese
PL1791542T3 (pl) 2004-08-23 2015-11-30 Mannkind Corp Sole diketopiperazyny do dostarczania leków
AU2006290870B2 (en) 2005-09-14 2013-02-28 Mannkind Corporation Method of drug formulation based on increasing the affinity of active agents for crystalline microparticle surfaces
EP2497484A3 (de) 2006-02-22 2012-11-07 MannKind Corporation Verfahren zur Verbesserung der pharmazeutischen Eigenschaften von Mikropartikeln mit Diketopiperazin und einem Wirkstoff
US8485180B2 (en) 2008-06-13 2013-07-16 Mannkind Corporation Dry powder drug delivery system
DK2570147T3 (da) 2008-06-13 2018-01-29 Mannkind Corp Tørpulverinhalator og system til lægemiddelindgivelse
KR101628410B1 (ko) 2008-06-20 2016-06-08 맨카인드 코포레이션 흡입 활동에 관한 실시간 프로파일링을 위한 대화형 장치 및 방법
TWI532497B (zh) 2008-08-11 2016-05-11 曼凱公司 超快起作用胰島素之用途
US8314106B2 (en) 2008-12-29 2012-11-20 Mannkind Corporation Substituted diketopiperazine analogs for use as drug delivery agents
CA2754595C (en) 2009-03-11 2017-06-27 Mannkind Corporation Apparatus, system and method for measuring resistance of an inhaler
US8734845B2 (en) * 2009-06-12 2014-05-27 Mannkind Corporation Diketopiperazine microparticles with defined specific surface areas
CA2778698A1 (en) 2009-11-03 2011-05-12 Mannkind Corporation An apparatus and method for simulating inhalation efforts
RU2531455C2 (ru) 2010-06-21 2014-10-20 Маннкайнд Корпорейшн Системы и способы доставки сухих порошковых лекарств
MY180552A (en) 2011-04-01 2020-12-02 Mannkind Corp Blister package for pharmaceutical cartridges
WO2012174472A1 (en) 2011-06-17 2012-12-20 Mannkind Corporation High capacity diketopiperazine microparticles
WO2013063160A1 (en) 2011-10-24 2013-05-02 Mannkind Corporation Methods and compositions for treating pain
EP2836204B1 (de) 2012-04-13 2020-07-08 GlaxoSmithKline Intellectual Property Development Limited Aggregatteilchen
CA2878457C (en) 2012-07-12 2021-01-19 Mannkind Corporation Dry powder drug delivery systems and methods
WO2014066856A1 (en) 2012-10-26 2014-05-01 Mannkind Corporation Inhalable influenza vaccine compositions and methods
BR112015023168B1 (pt) 2013-03-15 2021-08-10 Mannkind Corporation Composição de 3,6-bis(n-fumaril-4-aminobutil)-2,5-dicetopiperazina cristalina, método de produção de partículas de 3,6-bis(n-fumaril-4-aminobutil)-2,5-dicetopiperazina e uso de uma composição de dicetopiperazina cristalina
RS58882B1 (sr) * 2013-06-19 2019-08-30 Aicuris Anti Infective Cures Gmbh Amorfni letermovir i njegove čvrste farmaceutske formulacije za oralno davanje
CN114848614A (zh) 2013-07-18 2022-08-05 曼金德公司 热稳定性干粉药物组合物和方法
CA2920488C (en) 2013-08-05 2022-04-26 Mannkind Corporation Insufflation apparatus and methods
US10307464B2 (en) 2014-03-28 2019-06-04 Mannkind Corporation Use of ultrarapid acting insulin
US10561806B2 (en) 2014-10-02 2020-02-18 Mannkind Corporation Mouthpiece cover for an inhaler

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003015787A1 (en) * 2001-08-17 2003-02-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of bibn4096 in combination with other antimigraine drugs for the treatment of migraine
WO2003070753A1 (de) * 2002-02-19 2003-08-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur herstellung eines pulverinhalativums enthaltend ein salz des cgrp-antagonisten bibn4096
WO2003070215A1 (de) * 2002-02-20 2003-08-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pulverinhalativum, enthaltend den cgrp-antagonisten bibn4096 und verfahren zu dessen herstellung
WO2005018614A1 (de) * 2003-08-18 2005-03-03 Boehringer Ingelheim International Gmbh Pulverformulierung, enthaltend den cgrp-antagonisten 1- (n2-(3,5-dibrom-n-(4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazin
WO2005018609A1 (de) * 2003-08-18 2005-03-03 Boehringer Ingelheim International Gmbh Mikropartikel, enthaltend den cgrp-antagonisten 1- [n2-[3,5-dibrom-n-[[4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazin, verfahren zu deren herstellung sowie deren verwendung als inhalationspulver

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1242211A (en) * 1967-08-08 1971-08-11 Fisons Pharmaceuticals Ltd Pharmaceutical composition
WO2001056581A1 (fr) * 2000-02-04 2001-08-09 Kissei Pharmaceutical Co., Ltd. Preparation en poudre pour inhalation et inhalateur de poudre contenant cette preparation
GB0014851D0 (en) * 2000-06-16 2000-08-09 Glaxo Group Ltd Novel pharmaceutical formulation
DE10338407A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Inhalationspulver enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003015787A1 (en) * 2001-08-17 2003-02-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of bibn4096 in combination with other antimigraine drugs for the treatment of migraine
WO2003070753A1 (de) * 2002-02-19 2003-08-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur herstellung eines pulverinhalativums enthaltend ein salz des cgrp-antagonisten bibn4096
WO2003070215A1 (de) * 2002-02-20 2003-08-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pulverinhalativum, enthaltend den cgrp-antagonisten bibn4096 und verfahren zu dessen herstellung
WO2005018614A1 (de) * 2003-08-18 2005-03-03 Boehringer Ingelheim International Gmbh Pulverformulierung, enthaltend den cgrp-antagonisten 1- (n2-(3,5-dibrom-n-(4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazin
WO2005018609A1 (de) * 2003-08-18 2005-03-03 Boehringer Ingelheim International Gmbh Mikropartikel, enthaltend den cgrp-antagonisten 1- [n2-[3,5-dibrom-n-[[4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazin, verfahren zu deren herstellung sowie deren verwendung als inhalationspulver

Also Published As

Publication number Publication date
WO2005018603A2 (de) 2005-03-03
EP1663149A2 (de) 2006-06-07
JP2007502789A (ja) 2007-02-15
DE10338402A1 (de) 2005-03-17
CA2536047A1 (en) 2005-03-03

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