CA2531832A1 - Powdery formulations for inhalation, containing a novel anticholinergic agent - Google Patents
Powdery formulations for inhalation, containing a novel anticholinergic agent Download PDFInfo
- Publication number
- CA2531832A1 CA2531832A1 CA002531832A CA2531832A CA2531832A1 CA 2531832 A1 CA2531832 A1 CA 2531832A1 CA 002531832 A CA002531832 A CA 002531832A CA 2531832 A CA2531832 A CA 2531832A CA 2531832 A1 CA2531832 A1 CA 2531832A1
- Authority
- CA
- Canada
- Prior art keywords
- inhalable powder
- powder according
- excipient
- inhalable
- inhalation
- 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
- 0 C*1(*)C(C2)[C@]3OC3C1C[C@]2(*)OC(C(*)(c1ccccc1)c1ccccc1)=O Chemical compound C*1(*)C(C2)[C@]3OC3C1C[C@]2(*)OC(C(*)(c1ccccc1)c1ccccc1)=O 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pulmonology (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Otolaryngology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
The invention relates to powdery formulations for inhalation, containing an anticholinergic agent of formula (I), wherein X represents an anion which ca n have meanings cited in the description and in the claims, a method for the production thereof and the use thereof in the production of a medicament for treating respiratory tract diseases, especially for treating COPD (chronic obstructive pulmonary disease) and asthma.
Claims (12)
1) Inhalable powder, containing as sole active substance a compound of formula 1 wherein X- denotes a pharmaceutically acceptable anion, in admixture with a physiologically acceptable excipient, characterised in that the excipient has an average particle size of 10 - 50 µm.
2) Inhalable powder according to claim 1, characterised in that the anion X-is selected from the group consisting of chloride, bromide, iodide, sulphate, phosphate, methanesulphonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate and p-toluenesulphonate.
3) Inhalable powder according to claim 1 or 2, characterised in that the content of active substance based on the pharmacologically active cation of formula 1' is between 0.0008 and 33 %.
4) Inhalable powder according to claim 1, 2 or 3, characterised in that the physiologically acceptable excipient is selected from among the monosaccharides, disaccharides, oligo- and polysaccharides, the polyalcohols, cyclodextrins, amino acids or the salts thereof.
5) Inhalable powder according to one of claims 1 to 4, characterised in that the excipient has an average particle size of 12 to 35 µm.
6) Inhalable powder according to one of claims 1 to 5, characterised in that the excipient has a 10% fine content of 0.5 to 6 µm.
7) Inhalable powder according to one of claims 1 to 6, characterised in that the excipient has a specific surface area of 0.1 to 2 m2/g.
8) Use of an inhalable powder according to one of claims 1 to 7 for preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD and/or asthma.
9) Capsule containing an inhalable powder according to one of claims 1 to 7.
10) Capsule according to claim 9, characterised in that the capsule material consists of synthetic plastics.
11) Inhalation kit consisting of a capsule according to one of claims 9 or 10 and an inhaler which may be used for administering inhalable powders from powder-filled capsules.
12) Inhalation kit according to claim 11, characterised by a housing 1 containing two windows 2, a deck 3 in which there are air inlet ports and which is provided with a screen 5 secured via a screen housing 4, an inhalation chamber 6 connected to the deck 3 on which there is a push button 9 provided with two sharpened pins 7 and movable counter to a spring 8, and a mouthpiece 12 which is connected to the housing 1, the deck 3 and a cover 11 via a spindle 10 to enable it to be flipped open or shut, as well as air through-holes 13 for adjusting the flow resistance.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10331350.8 | 2003-07-11 | ||
| DE10331350A DE10331350A1 (en) | 2003-07-11 | 2003-07-11 | Inhalation powder useful for treating respiratory diseases comprises a 9,9-dimethyl-7-(2,2-diphenylpropionyloxy)-3-oxa-9-azatricyclononane salt and a finely divided excipient |
| PCT/EP2004/007357 WO2005007134A1 (en) | 2003-07-11 | 2004-07-06 | Powdery formulations for inhalation, containing a novel anticholinergic agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2531832A1 true CA2531832A1 (en) | 2005-01-27 |
| CA2531832C CA2531832C (en) | 2012-09-18 |
Family
ID=33546971
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2531832A Expired - Lifetime CA2531832C (en) | 2003-07-11 | 2004-07-06 | Powdery formulations for inhalation, containing a novel anticholinergic agent |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1646365B1 (en) |
| JP (1) | JP2009514778A (en) |
| AT (1) | ATE420627T1 (en) |
| CA (1) | CA2531832C (en) |
| DE (2) | DE10331350A1 (en) |
| ES (1) | ES2318298T3 (en) |
| WO (1) | WO2005007134A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1925295A1 (en) * | 2006-11-22 | 2008-05-28 | Boehringer Ingelheim Pharma GmbH & Co. KG | Stable powder formulation containing a new antichinolinergic agent |
| EP1925296A1 (en) * | 2006-11-22 | 2008-05-28 | Boehringer Ingelheim Pharma GmbH & Co. KG | Stable powder formulation containing a new antichinolinergic agent |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA75375C2 (en) * | 2000-10-12 | 2006-04-17 | Boehringer Ingelheim Pharma | Method for producing powdery preparations for inhaling |
| DE10050994A1 (en) * | 2000-10-14 | 2002-04-18 | Boehringer Ingelheim Pharma | New diphenylalkanoic acid azabicyclooctane ester quaternary salts useful as anticholinergic agents, especially in treatment of asthma and chronic obstructive pulmonary disease |
-
2003
- 2003-07-11 DE DE10331350A patent/DE10331350A1/en not_active Withdrawn
-
2004
- 2004-07-06 ES ES04740685T patent/ES2318298T3/en not_active Expired - Lifetime
- 2004-07-06 EP EP04740685A patent/EP1646365B1/en not_active Expired - Lifetime
- 2004-07-06 CA CA2531832A patent/CA2531832C/en not_active Expired - Lifetime
- 2004-07-06 AT AT04740685T patent/ATE420627T1/en active
- 2004-07-06 WO PCT/EP2004/007357 patent/WO2005007134A1/en active Application Filing
- 2004-07-06 JP JP2006518121A patent/JP2009514778A/en active Pending
- 2004-07-06 DE DE502004008877T patent/DE502004008877D1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CA2531832C (en) | 2012-09-18 |
| DE502004008877D1 (en) | 2009-03-05 |
| ES2318298T3 (en) | 2009-05-01 |
| EP1646365B1 (en) | 2009-01-14 |
| ATE420627T1 (en) | 2009-01-15 |
| JP2009514778A (en) | 2009-04-09 |
| WO2005007134A1 (en) | 2005-01-27 |
| WO2005007134A8 (en) | 2006-06-15 |
| EP1646365A1 (en) | 2006-04-19 |
| DE10331350A1 (en) | 2005-01-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |