CA2670153A1 - Stable powder formulation containing a novel anticholinergic agent - Google Patents
Stable powder formulation containing a novel anticholinergic agent Download PDFInfo
- Publication number
- CA2670153A1 CA2670153A1 CA002670153A CA2670153A CA2670153A1 CA 2670153 A1 CA2670153 A1 CA 2670153A1 CA 002670153 A CA002670153 A CA 002670153A CA 2670153 A CA2670153 A CA 2670153A CA 2670153 A1 CA2670153 A1 CA 2670153A1
- Authority
- CA
- Canada
- Prior art keywords
- acid
- spray
- powder formulation
- salt
- sterically demanding
- 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 108
- 239000000203 mixture Substances 0.000 title claims abstract description 107
- 238000009472 formulation Methods 0.000 title claims abstract description 95
- 239000000812 cholinergic antagonist Substances 0.000 title description 5
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 title description 2
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- 239000002253 acid Substances 0.000 claims abstract description 95
- 150000001875 compounds Chemical class 0.000 claims abstract description 66
- 235000015165 citric acid Nutrition 0.000 claims abstract description 59
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims abstract description 55
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims abstract description 51
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims abstract description 46
- 239000000463 material Substances 0.000 claims abstract description 43
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims abstract description 40
- 239000002245 particle Substances 0.000 claims abstract description 39
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims abstract description 34
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- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims abstract description 32
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- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 28
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- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 22
- 239000007787 solid Substances 0.000 claims description 22
- 230000001078 anti-cholinergic effect Effects 0.000 claims description 20
- 229940001468 citrate Drugs 0.000 claims description 18
- 238000001035 drying Methods 0.000 claims description 18
- -1 alkali metal salt Chemical class 0.000 claims description 17
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- WGIWBXUNRXCYRA-UHFFFAOYSA-H trizinc;2-hydroxypropane-1,2,3-tricarboxylate Chemical compound [Zn+2].[Zn+2].[Zn+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WGIWBXUNRXCYRA-UHFFFAOYSA-H 0.000 claims description 14
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- 239000002904 solvent Substances 0.000 claims description 11
- 239000001384 succinic acid Substances 0.000 claims description 11
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- 229920000858 Cyclodextrin Polymers 0.000 claims description 9
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- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims description 8
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Landscapes
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06124578.3 | 2006-11-22 | ||
| EP06124578A EP1925296A1 (de) | 2006-11-22 | 2006-11-22 | Stabile Pulverformulierung enthaltend ein neues Anticholinergikum |
| PCT/EP2007/061910 WO2008061873A2 (de) | 2006-11-22 | 2007-11-06 | Stabile pulverformulierung enthaltend ein neues anticholinergikum |
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| CA2670153A1 true CA2670153A1 (en) | 2008-05-29 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CA002670153A Abandoned CA2670153A1 (en) | 2006-11-22 | 2007-11-06 | Stable powder formulation containing a novel anticholinergic agent |
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| Country | Link |
|---|---|
| US (1) | US20100047359A1 (https=) |
| EP (2) | EP1925296A1 (https=) |
| JP (1) | JP2010510278A (https=) |
| CA (1) | CA2670153A1 (https=) |
| WO (1) | WO2008061873A2 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1925295A1 (de) * | 2006-11-22 | 2008-05-28 | Boehringer Ingelheim Pharma GmbH & Co. KG | Stabile Pulverformulierung enthaltend ein Anticholinergikum |
| PT107312B (pt) * | 2013-11-25 | 2022-05-10 | Advanced Cyclone Systems S A | Ciclone aglomerador de fluxo invertido e respectivo processo |
| CN111533959B (zh) * | 2020-05-25 | 2021-11-23 | 上海邦成生物工程有限公司 | 低聚壳聚糖/木薯淀粉复合丙酸锌固形物及其制备方法 |
Family Cites Families (9)
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| US6077543A (en) * | 1996-12-31 | 2000-06-20 | Inhale Therapeutic Systems | Systems and processes for spray drying hydrophobic drugs with hydrophilic excipients |
| US6667344B2 (en) * | 2001-04-17 | 2003-12-23 | Dey, L.P. | Bronchodilating compositions and methods |
| WO2003024396A2 (en) * | 2001-09-17 | 2003-03-27 | Glaxo Group Limited | Dry powder medicament formulations |
| DE10203741A1 (de) * | 2002-01-31 | 2003-08-14 | Boehringer Ingelheim Pharma | Neue Fluorencarbonsäureester, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel |
| US20050112087A1 (en) * | 2003-04-29 | 2005-05-26 | Musso Gary F. | Pharmaceutical formulations for sustained drug delivery |
| US7462367B2 (en) * | 2003-07-11 | 2008-12-09 | Boehringer Ingelheim International Gmbh | Anticholinergic powder formulations for inhalation |
| DE10331350A1 (de) * | 2003-07-11 | 2005-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pulverformulierungen für die Inhalation enthaltend ein neues Anticholinergikum |
| US20050186175A1 (en) * | 2004-02-20 | 2005-08-25 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions based on benzilic acid esters and soluble TNF receptor fusion proteins |
| WO2005079794A1 (en) * | 2004-02-20 | 2005-09-01 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions based on anticholinergics and pegsunercept |
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2006
- 2006-11-22 EP EP06124578A patent/EP1925296A1/de not_active Ceased
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2007
- 2007-11-06 US US12/515,564 patent/US20100047359A1/en not_active Abandoned
- 2007-11-06 JP JP2009537589A patent/JP2010510278A/ja active Pending
- 2007-11-06 EP EP07822237A patent/EP2094245A2/de not_active Withdrawn
- 2007-11-06 WO PCT/EP2007/061910 patent/WO2008061873A2/de not_active Ceased
- 2007-11-06 CA CA002670153A patent/CA2670153A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2094245A2 (de) | 2009-09-02 |
| EP1925296A1 (de) | 2008-05-28 |
| WO2008061873A3 (de) | 2008-07-10 |
| US20100047359A1 (en) | 2010-02-25 |
| WO2008061873A2 (de) | 2008-05-29 |
| JP2010510278A (ja) | 2010-04-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |
Effective date: 20141106 |