CA2479638A1 - Hfa-suspension formulations of crystalline tiotropium bromide anhydrate - Google Patents
Hfa-suspension formulations of crystalline tiotropium bromide anhydrate Download PDFInfo
- Publication number
- CA2479638A1 CA2479638A1 CA002479638A CA2479638A CA2479638A1 CA 2479638 A1 CA2479638 A1 CA 2479638A1 CA 002479638 A CA002479638 A CA 002479638A CA 2479638 A CA2479638 A CA 2479638A CA 2479638 A1 CA2479638 A1 CA 2479638A1
- Authority
- CA
- Canada
- Prior art keywords
- acid
- contain
- glyceryl
- suspensions according
- group
- 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.)
- Granted
Links
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
- A61K9/10—Dispersions; Emulsions
-
- 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
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
Abstract
The invention relates to propellant formulations containing suspensions of a crystalline anhydrate of (1.alpha.,2.beta.,4.beta.,5.alpha.,7.beta.)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide.
Claims (9)
1) Suspensions of crystalline tiotropium bromide anhydrate in the propellant gases HFA 227 and/or HFA 134a, optionally in admixture with one or more other propellant gases selected from the group consisting of propane, butane, pentane, dimethylether, CHClF2, CH2F2, CF3CH3, isobutane, isopentane and neopentane.
2) Suspensions according to claim 1, characterised in that they contain between 0.001 and 0.8% tiotropium.
3) Suspensions according to claim 1 or 2, characterised in that they contain as other ingredients surface-active agents (surfactants), adjuvants, antioxidants and/or flavourings.
4) Suspensions according to claim 3, characterised in that they contain as surface-active agents (surfactants) one or more compounds selected from the group consisting of Polysorbate 20, Polysorbate 80, Myvacet 9-45, Myvacet 9-08, isopropylmyristate, oleic acid, propyleneglycol, polyethyleneglycol, Brij, ethyl oleate, glyceryl trioleate, glyceryl monolaurate, glyceryl monooleate, glyceryl monosterate, glyceryl monoricinoleate, cetylalcohol, sterylalcohol, cetylpyridinium chloride, block polymers, natural oil, ethanol and isopropanol .
5) Suspensions according to claim 3, characterised in that they contain as adjuvants one or more compounds selected from the group consisting of alanine, albumin, ascorbic acid, aspartame, betaine, cysteine, phosphoric acid, nitric acid, hydrochloric acid, sulphuric acid and citric acid.
6) Suspensions according to claim 3, characterised in that they contain as antioxidants one or more compounds selected from the group consisting of ascorbic acid, citric acid, sodium edetate, editic acid, tocopherols, butylhydroxytoluene, butylhydroxyanisol and ascorbyl palmitate.
7) Suspensions according to claim 1 or 2, characterised in that they contain no other ingredients apart from the active substance and the propellant gas or gases.
8) Use of a suspension according to one of claims 1 to 7 for preparing a pharmaceutical composition, preferably for preparing a pharmaceutical composition for the treatment by inhalation or nasal route of diseases in which anticholinergics may confer a therapeutic benefit.
9) Use according to claim 8, characterised in that the diseases are respiratory complaints, preferably asthma or COPD.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10214264.5 | 2002-03-28 | ||
DE10214264A DE10214264A1 (en) | 2002-03-28 | 2002-03-28 | HFA suspension formulations of an anhydrate |
PCT/EP2003/002899 WO2003082244A2 (en) | 2002-03-28 | 2003-03-20 | Hfa-suspension formulation of an anhydrate |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2479638A1 true CA2479638A1 (en) | 2003-10-09 |
CA2479638C CA2479638C (en) | 2011-01-04 |
Family
ID=28050990
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2479638A Expired - Fee Related CA2479638C (en) | 2002-03-28 | 2003-03-20 | Hfa-suspension formulations of crystalline tiotropium bromide anhydrate |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP1492498A2 (en) |
JP (1) | JP5147158B2 (en) |
KR (1) | KR101005717B1 (en) |
CN (1) | CN1642525A (en) |
AU (1) | AU2003221509B2 (en) |
BR (1) | BR0308709A (en) |
CA (1) | CA2479638C (en) |
DE (1) | DE10214264A1 (en) |
EA (1) | EA008610B1 (en) |
EC (1) | ECSP045322A (en) |
HR (1) | HRP20040890A2 (en) |
IL (1) | IL163696A0 (en) |
ME (1) | ME00246B (en) |
MX (1) | MXPA04009338A (en) |
NO (1) | NO20044004L (en) |
NZ (1) | NZ536030A (en) |
PL (1) | PL371295A1 (en) |
RS (1) | RS52481B (en) |
UA (1) | UA79776C2 (en) |
WO (1) | WO2003082244A2 (en) |
ZA (1) | ZA200405637B (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110135737A1 (en) * | 2009-05-29 | 2011-06-09 | Pearl Therapeutics, Inc. | Compositions for respiratory delivery of active agents and associated methods and systems |
US9415009B2 (en) | 2009-05-29 | 2016-08-16 | Pearl Therapeutics, Inc. | Compositions, methods and systems for respiratory delivery of two or more active agents |
US11471468B2 (en) | 2013-03-15 | 2022-10-18 | Pearl Therapeutics, Inc. | Methods and systems for conditioning of particulate crystalline materials |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2606549A1 (en) * | 2005-05-02 | 2006-11-09 | Boehringer Ingelheim International Gmbh | Crystalline forms of tiotropium bromide |
KR20080007656A (en) * | 2005-05-02 | 2008-01-22 | 베링거 인겔하임 인터내셔날 게엠베하 | Novel crystalline forms of tiotropium bromide |
AU2015201037C1 (en) * | 2009-05-29 | 2017-07-27 | Pearl Therapeutics, Inc. | Respiratory delivery of active agents |
EP3515439B1 (en) * | 2016-09-19 | 2021-12-15 | Mexichem Fluor S.A. de C.V. | Pharmaceutical composition comprising tiotropium bromide |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3931041C2 (en) * | 1989-09-16 | 2000-04-06 | Boehringer Ingelheim Kg | Esters of thienyl carboxylic acids with amino alcohols, their quaternization products, processes for their preparation and medicaments containing them |
CN1150890C (en) * | 1998-08-04 | 2004-05-26 | 杰格研究股份公司 | Medicinal aerosol formulations |
GB0009605D0 (en) * | 2000-04-18 | 2000-06-07 | Glaxo Group Ltd | Medicaments |
GB0009606D0 (en) * | 2000-04-18 | 2000-06-07 | Glaxo Group Ltd | Therapeutic combinations |
GB0009592D0 (en) * | 2000-04-18 | 2000-06-07 | Glaxo Group Ltd | Respiratory combinations |
GB0009583D0 (en) * | 2000-04-18 | 2000-06-07 | Glaxo Group Ltd | Respiratory formulations |
DE10111058A1 (en) * | 2001-03-08 | 2002-09-12 | Boehringer Ingelheim Pharma | New drug compositions based on anticholinergics and NK¶1¶ receptor antagonists |
CA2436537C (en) * | 2000-10-31 | 2009-05-26 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical compositions comprising tiotropium salts and antihistamines |
DE10113366A1 (en) * | 2001-03-20 | 2002-09-26 | Boehringer Ingelheim Pharma | Medicament for treating inflammatory or obstructive respiratory diseases, e.g. asthma or chronic obstructive pulmonary disease, containing synergistic combination of anticholinergic agent and endothelin antagonist |
-
2002
- 2002-03-28 DE DE10214264A patent/DE10214264A1/en not_active Withdrawn
-
2003
- 2003-03-20 ME MEP-2008-473A patent/ME00246B/en unknown
- 2003-03-20 KR KR1020047015174A patent/KR101005717B1/en active IP Right Grant
- 2003-03-20 CN CNA038072475A patent/CN1642525A/en active Pending
- 2003-03-20 UA UA20041008758A patent/UA79776C2/en unknown
- 2003-03-20 RS YU86004A patent/RS52481B/en unknown
- 2003-03-20 EA EA200401159A patent/EA008610B1/en unknown
- 2003-03-20 IL IL16369603A patent/IL163696A0/en unknown
- 2003-03-20 NZ NZ536030A patent/NZ536030A/en not_active IP Right Cessation
- 2003-03-20 BR BR0308709-3A patent/BR0308709A/en active Pending
- 2003-03-20 MX MXPA04009338A patent/MXPA04009338A/en active IP Right Grant
- 2003-03-20 AU AU2003221509A patent/AU2003221509B2/en not_active Expired
- 2003-03-20 WO PCT/EP2003/002899 patent/WO2003082244A2/en active Application Filing
- 2003-03-20 CA CA2479638A patent/CA2479638C/en not_active Expired - Fee Related
- 2003-03-20 JP JP2003579782A patent/JP5147158B2/en not_active Expired - Lifetime
- 2003-03-20 EP EP03717219A patent/EP1492498A2/en not_active Withdrawn
- 2003-03-20 PL PL03371295A patent/PL371295A1/en not_active Application Discontinuation
-
2004
- 2004-07-15 ZA ZA2004/05637A patent/ZA200405637B/en unknown
- 2004-09-23 NO NO20044004A patent/NO20044004L/en not_active Application Discontinuation
- 2004-09-27 HR HR20040890A patent/HRP20040890A2/en not_active Application Discontinuation
- 2004-09-28 EC EC2004005322A patent/ECSP045322A/en unknown
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20110135737A1 (en) * | 2009-05-29 | 2011-06-09 | Pearl Therapeutics, Inc. | Compositions for respiratory delivery of active agents and associated methods and systems |
AU2010253770B2 (en) * | 2009-05-29 | 2014-12-11 | Pearl Therapeutics, Inc. | Compositions for respiratory delivery of active agents and associated methods and systems |
US9415009B2 (en) | 2009-05-29 | 2016-08-16 | Pearl Therapeutics, Inc. | Compositions, methods and systems for respiratory delivery of two or more active agents |
US10716753B2 (en) | 2009-05-29 | 2020-07-21 | Pearl Therapeutics, Inc. | Compositions for pulmonary delivery of long-acting muscarinic antagonists or long-acting B2 adrenergic receptor agonists and associated methods and systems |
US11471468B2 (en) | 2013-03-15 | 2022-10-18 | Pearl Therapeutics, Inc. | Methods and systems for conditioning of particulate crystalline materials |
Also Published As
Publication number | Publication date |
---|---|
IL163696A0 (en) | 2005-12-18 |
AU2003221509A1 (en) | 2003-10-13 |
BR0308709A (en) | 2005-01-04 |
MXPA04009338A (en) | 2005-01-25 |
NO20044004L (en) | 2004-10-05 |
UA79776C2 (en) | 2007-07-25 |
EP1492498A2 (en) | 2005-01-05 |
NZ536030A (en) | 2006-07-28 |
KR20040098022A (en) | 2004-11-18 |
AU2003221509B2 (en) | 2008-01-24 |
JP2005527550A (en) | 2005-09-15 |
WO2003082244A2 (en) | 2003-10-09 |
CA2479638C (en) | 2011-01-04 |
EA008610B1 (en) | 2007-06-29 |
MEP47308A (en) | 2011-02-10 |
KR101005717B1 (en) | 2011-01-05 |
JP5147158B2 (en) | 2013-02-20 |
RS52481B (en) | 2013-02-28 |
EA200401159A1 (en) | 2005-04-28 |
ZA200405637B (en) | 2005-07-27 |
YU86004A (en) | 2006-08-17 |
DE10214264A1 (en) | 2003-10-16 |
CN1642525A (en) | 2005-07-20 |
WO2003082244A3 (en) | 2004-02-05 |
HRP20040890A2 (en) | 2005-06-30 |
PL371295A1 (en) | 2005-06-13 |
ECSP045322A (en) | 2005-01-28 |
ME00246B (en) | 2011-05-10 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request | ||
MKLA | Lapsed |
Effective date: 20220301 |
|
MKLA | Lapsed |
Effective date: 20200831 |