CA2536053A1 - Powder formulation comprising the cgrp antagonist 1-(n2-(3,5-dibromo-n-(4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazine - Google Patents
Powder formulation comprising the cgrp antagonist 1-(n2-(3,5-dibromo-n-(4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazine Download PDFInfo
- Publication number
- CA2536053A1 CA2536053A1 CA002536053A CA2536053A CA2536053A1 CA 2536053 A1 CA2536053 A1 CA 2536053A1 CA 002536053 A CA002536053 A CA 002536053A CA 2536053 A CA2536053 A CA 2536053A CA 2536053 A1 CA2536053 A1 CA 2536053A1
- Authority
- CA
- Canada
- Prior art keywords
- active substance
- particularly preferably
- powder
- drying gas
- organic
- 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.)
- Abandoned
Links
- 239000000843 powder Substances 0.000 title claims abstract description 76
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 title claims abstract description 9
- 239000000203 mixture Substances 0.000 title claims description 29
- 229940127597 CGRP antagonist Drugs 0.000 title abstract description 8
- 239000003735 calcitonin gene related peptide receptor antagonist Substances 0.000 title abstract description 8
- 238000009472 formulation Methods 0.000 title description 18
- 239000011859 microparticle Substances 0.000 claims abstract description 21
- 238000004519 manufacturing process Methods 0.000 claims abstract description 14
- 230000002685 pulmonary effect Effects 0.000 claims abstract description 6
- 239000013543 active substance Substances 0.000 claims description 68
- 239000002245 particle Substances 0.000 claims description 68
- 238000000034 method Methods 0.000 claims description 37
- 238000001035 drying Methods 0.000 claims description 34
- 239000007921 spray Substances 0.000 claims description 26
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 12
- 239000003125 aqueous solvent Substances 0.000 claims description 10
- 239000007787 solid Substances 0.000 claims description 10
- 239000010419 fine particle Substances 0.000 claims description 9
- 239000003595 mist Substances 0.000 claims description 8
- 238000005507 spraying Methods 0.000 claims description 8
- 239000002775 capsule Substances 0.000 claims description 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 239000003960 organic solvent Substances 0.000 claims description 5
- 239000002904 solvent Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 abstract description 5
- 238000011282 treatment Methods 0.000 abstract description 5
- 208000006561 Cluster Headache Diseases 0.000 abstract description 3
- 206010019233 Headaches Diseases 0.000 abstract description 3
- 231100000869 headache Toxicity 0.000 abstract description 3
- 239000007789 gas Substances 0.000 description 22
- 239000000126 substance Substances 0.000 description 16
- 238000002360 preparation method Methods 0.000 description 14
- 210000004072 lung Anatomy 0.000 description 12
- 239000000243 solution Substances 0.000 description 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- 238000001694 spray drying Methods 0.000 description 6
- 239000012876 carrier material Substances 0.000 description 5
- 238000009826 distribution Methods 0.000 description 5
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 4
- 206010027599 migraine Diseases 0.000 description 4
- 230000008021 deposition Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000000227 grinding Methods 0.000 description 3
- 238000005259 measurement Methods 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 230000036470 plasma concentration Effects 0.000 description 3
- 239000011877 solvent mixture Substances 0.000 description 3
- 208000002193 Pain Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 208000005298 acute pain Diseases 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 208000018912 cluster headache syndrome Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 238000009516 primary packaging Methods 0.000 description 2
- 239000007858 starting material Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000007910 systemic administration Methods 0.000 description 2
- 230000009885 systemic effect Effects 0.000 description 2
- 238000009827 uniform distribution Methods 0.000 description 2
- YFMFNYKEUDLDTL-UHFFFAOYSA-N 1,1,1,2,3,3,3-heptafluoropropane Chemical compound FC(F)(F)C(F)C(F)(F)F YFMFNYKEUDLDTL-UHFFFAOYSA-N 0.000 description 1
- QGZKDVFQNNGYKY-OUBTZVSYSA-N Ammonia-15N Chemical compound [15NH3] QGZKDVFQNNGYKY-OUBTZVSYSA-N 0.000 description 1
- 241000276498 Pollachius virens Species 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000274 adsorptive effect Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000011067 equilibration Methods 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 230000009246 food effect Effects 0.000 description 1
- 235000021471 food effect Nutrition 0.000 description 1
- 230000005484 gravity Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000000877 morphologic effect Effects 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical class C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 description 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 239000012088 reference solution Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000013557 residual solvent Substances 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000004441 surface measurement Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DEDE10338403.0 | 2003-08-18 | ||
| DE10338403A DE10338403A1 (de) | 2003-08-18 | 2003-08-18 | 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-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum |
| PCT/EP2004/009103 WO2005018614A1 (de) | 2003-08-18 | 2004-08-13 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2536053A1 true CA2536053A1 (en) | 2005-03-03 |
Family
ID=34201782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002536053A Abandoned CA2536053A1 (en) | 2003-08-18 | 2004-08-13 | Powder formulation comprising the cgrp antagonist 1-(n2-(3,5-dibromo-n-(4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazine |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1660046A1 (https=) |
| JP (1) | JP2007502792A (https=) |
| AR (1) | AR045461A1 (https=) |
| CA (1) | CA2536053A1 (https=) |
| DE (1) | DE10338403A1 (https=) |
| TW (1) | TW200516077A (https=) |
| WO (1) | WO2005018614A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10338402A1 (de) * | 2003-08-18 | 2005-03-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Sprühgetrocknetes, amorphes BIBN 4096, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum |
| 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 |
| GB0613925D0 (en) * | 2006-07-13 | 2006-08-23 | Unilever Plc | Improvements relating to nanodispersions |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1242211A (en) * | 1967-08-08 | 1971-08-11 | Fisons Pharmaceuticals Ltd | Pharmaceutical composition |
| MA25590A1 (fr) * | 1998-09-14 | 2002-12-31 | Inhale Therapeutic Syst | Agent actif de delivraison de poudre seche |
| DE10139410A1 (de) * | 2001-08-17 | 2003-02-27 | Boehringer Ingelheim Pharma | Verwendung von BIBN4096 in Kombination mit anderen Arzneistoffen gegen Migräne für die Behandlung von Migräne |
| DE10206770A1 (de) * | 2002-02-19 | 2003-08-28 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung eines Pulverinhalativums enthaltend ein Salz des CGRP-Antagonisten BIBN4096 |
| DE10207026A1 (de) * | 2002-02-20 | 2003-08-28 | Boehringer Ingelheim Kg | Pulverinhalativum, enthaltend den CGRP-Antagonisten BIBN4096 und Verfahren zu dessen Herstellung |
-
2003
- 2003-08-18 DE DE10338403A patent/DE10338403A1/de not_active Withdrawn
-
2004
- 2004-08-13 EP EP04764097A patent/EP1660046A1/de not_active Withdrawn
- 2004-08-13 WO PCT/EP2004/009103 patent/WO2005018614A1/de not_active Ceased
- 2004-08-13 JP JP2006523585A patent/JP2007502792A/ja active Pending
- 2004-08-13 CA CA002536053A patent/CA2536053A1/en not_active Abandoned
- 2004-08-17 TW TW093124725A patent/TW200516077A/zh unknown
- 2004-08-18 AR ARP040102955A patent/AR045461A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE10338403A1 (de) | 2005-03-17 |
| AR045461A1 (es) | 2005-10-26 |
| TW200516077A (en) | 2005-05-16 |
| WO2005018614A1 (de) | 2005-03-03 |
| EP1660046A1 (de) | 2006-05-31 |
| JP2007502792A (ja) | 2007-02-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20080038357A1 (en) | Inhalation Powder Containing the CGRP antagonist BIBN4096 and Process for the Preparation Thereof | |
| US6900317B2 (en) | Salts of the CGRP antagonist BIBN4096 and inhalable powdered medicaments containing them | |
| JP4085064B2 (ja) | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６の塩を含有する吸入粉末の調製方法 | |
| US20050043247A1 (en) | Spray-dried amorphous BIBN 4096, process for preparing and the use thereof as inhalative | |
| AU2020250195B2 (en) | Rapamycin Powders for Pulmonary Delivery | |
| CA2536047A1 (en) | Spray-dried amorphous bibn 4096 method for production and use thereof as inhalant | |
| TW581681B (en) | Liquid crystal forms of cyclosporin | |
| US20050042178A1 (en) | Microparticles containing the CGRP-antagonist 1-[N2-[3,5-dibrom-N-[[4-(3,4-dihydro-2(1H)-oxoquinazoline-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine, process for preparing and the use thereof as inhalation powder | |
| CA2536053A1 (en) | Powder formulation comprising the cgrp antagonist 1-(n2-(3,5-dibromo-n-(4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazine | |
| US20050042180A1 (en) | Powder formulation containing the CGRP antagonist 1 [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2 (1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin, process for preparing and the use thereof as inhalation powder | |
| JP4085063B2 (ja) | Ｃｇｒｐ拮抗剤ｂｉｂｎ４０９６を含有する吸入粉末及びその調製方法 | |
| JP2007502792A6 (ja) | Ｃｇｒｐアンタゴニスト１−［ｎ２−［３，５−ジブロモ−ｎ−［［４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル］カルボニル］−ｄ−チロシル］−ｌ−リシル］−４−（４−ピリジニル）−ピペラジンを含有する粉末製剤、その吸入粉末としての製造方法及び使用 | |
| CA2963666A1 (en) | Formulations containing tiotropium, amino acid and acid and methods thereof | |
| CA2536048A1 (en) | Microparticles comprising the cgrp antagonist 1-[n2-[3,5-dibromo-n-[[4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazine method for production and use thereof as inhalation powder | |
| JP2007502790A6 (ja) | Ｃｇｒｐアンタゴニスト１−〔ｎ２−〔３，５−ジブロモ−ｎ−〔〔４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル〕カルボニル〕−ｄ−チロシル〕−ｌ−リシル〕−４−（４−ピリジニル）−ピペラジンを含む微粒子、その調製方法及び吸入粉末としてのその使用 | |
| JP7439084B2 (ja) | 吸入用乾燥粉末製剤のための新規担体粒子 | |
| CA2536050A1 (en) | Novel inhalation powder comprising the cgrp antagonist 1-[n2-[3,5-dibromo-n-[[4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazine | |
| US20060222599A1 (en) | Inhalative powder formulations containing the CGRP-antagonist 1 [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazine | |
| EP3316865A1 (en) | Triptan powders for pulmonary delivery |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Dead |