CA2481268A1 - Medicaments comprising steroids and a novel anticholinergic - Google Patents
Medicaments comprising steroids and a novel anticholinergic Download PDFInfo
- Publication number
- CA2481268A1 CA2481268A1 CA002481268A CA2481268A CA2481268A1 CA 2481268 A1 CA2481268 A1 CA 2481268A1 CA 002481268 A CA002481268 A CA 002481268A CA 2481268 A CA2481268 A CA 2481268A CA 2481268 A1 CA2481268 A1 CA 2481268A1
- Authority
- CA
- Canada
- Prior art keywords
- composition according
- pharmaceutical composition
- inhalable
- propellant
- contain
- 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
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Classifications
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, ***e
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
-
- 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
- A61P11/08—Bronchodilators
-
- 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
- A61P11/16—Central respiratory analeptics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Dispersion Chemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
The invention relates to novel medicament compositions based on long-acting steroids and salts of a novel anticholinesterase drug, to methods for the production of these compositions and their use in treating respiratory tract diseases.
Claims (20)
1) Pharmaceutical compositions, characterised in that they contain one or more, preferably one, salt of formula 1 wherein X - denotes an anion with a single negative charge, preferably an anion selected from the group consisting of chloride, bromide, iodide, sulphate, phosphate, methanesulphonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate and p-toluenesulphonate, combined with one or more, preferably one, steroid 2, optionally in the form of the diastereomers, mixtures of the diastereomers or in the form of the racemates thereof, optionally in the form of the solvates or hydrates and optionally together with a pharmaceutically acceptable excipient.
2) Pharmaceutical composition according to claim 1, characterised in that the active substances 1 and 2 are present either together in a single formulation or in two separate formulations.
3) Pharmaceutical composition according to claim 1 or 2, characterised in that the steroids 2 are flunisolide, beclomethasone, triamcinolone, budesonide, fluticasone, mometasone, ciclesonide, rofleponide, ST-126 or dexamethasone.
4) Pharmaceutical composition according to claim 3, characterised in that the steroids 2 are budesonide, fluticasone, mometasone, ciclesonide or ST-126.
5) Pharmaceutical composition according to one of claims 1 to 4, characterised in that the weight ratios of 1' to steroid 2 are in the range from about 1:250 to 250:1, preferably in the range from 1:150 to 150:1.
6) Pharmaceutical composition according to one of claims 1 to 5, characterised in that it is in the form of a preparation suitable for inhalation.
7) Pharmaceutical composition according to claim 6, characterised in that it is a preparation selected from among the inhalable powders, propellant-containing metered-dose aerosols and propellant-free inhalable solutions or suspensions.
8) Pharmaceutical composition according to claim 7, characterised in that it is an inhalable powder which contains 1 and 2 in admixture with suitable physiologically acceptable excipients selected from among the monosaccharides, disaccharides, oligo- and polysaccharides, polyalcohols, salts, or mixtures of these excipients with one another.
9) Inhalable powder according to claim 8, characterised in that the excipient has a maximum average particle size of up to 250µm, preferably between 10 and 150µm.
10) Pharmaceutical composition according to claim 7, characterised in that it is an inhalable powder which contains only the active substances 1 and 2 as its ingredients.
11) Pharmaceutical composition according to claim 7, characterised in that it is a propellant-containing inhalable aerosol which contains 1 and 2 in dissolved or dispersed form.
12) Propellant-containing inhalable aerosol according to claim 11, characterised in that it contains, as propellant gas, hydrocarbons such as n-propane, n-butane or isobutane or halohydrocarbons such as chlorinated and/or fluorinated derivatives of methane, ethane, propane, butane, cyclopropane or cyclobutane.
13) Propellant-containing inhalable aerosol according to claim 12, characterised in that the propellant gas is TG11, TG12, TG134a, TG227 or mixtures thereof, preferably TG134a, TG227 or a mixture thereof.
14) Propellant-containing inhalable aerosol according to claim 11, 12 or 13, characterised in that it may contain up to 5% by weight of active substance 1 and/or 2.
15) Pharmaceutical composition according to claim 7, characterised in that it is a propellant-free inhalable solution which contains water, ethanol or a mixture of water and ethanol as solvent.
16) Inhalable solution according to claim 15, characterised in that it optionally contains other co-solvents and/or excipients.
17) Inhalable solution according to claim 16, characterised in that it contains as co-solvents ingredients which contain hydroxyl groups or other polar groups, e.g.
alcohols - particularly isopropyl alcohol, glycols - particularly propyleneglycol, polyethyleneglycol, polypropyleneglycol, glycolether, glycerol, polyoxyethylene alcohols and polyoxyethylene fatty acid esters.
alcohols - particularly isopropyl alcohol, glycols - particularly propyleneglycol, polyethyleneglycol, polypropyleneglycol, glycolether, glycerol, polyoxyethylene alcohols and polyoxyethylene fatty acid esters.
18) Inhalable solutions according to one of claims 16 or 17, characterised in that they contain as excipients surfactants, stabilisers, complexing agents, antioxidants and/or preservatives, flavourings and/or vitamins.
19) Inhalable solutions according to claim 18, characterised in that they contain as complexing agents editic acid or a salt of editic acid, preferably sodium edetate.
20) Use of a composition according to one of claims 1 to 19 for preparing a medicament for the treatment of inflammatory and/or obstructive respiratory complaints, particularly asthma or COPD.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10216429.0 | 2002-04-12 | ||
DE10216429A DE10216429A1 (en) | 2002-04-12 | 2002-04-12 | Synergistic medicaments for treating inflammatory or obstructive respiratory tract diseases, containing quaternized scopine ester anticholinergic agent and steroid, e.g. budesonide |
PCT/EP2003/003668 WO2003086399A1 (en) | 2002-04-12 | 2003-04-09 | Medicaments containing steroids and a novel anticholinesterase drug |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2481268A1 true CA2481268A1 (en) | 2003-10-23 |
CA2481268C CA2481268C (en) | 2011-07-12 |
Family
ID=28458802
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA2481268A Expired - Lifetime CA2481268C (en) | 2002-04-12 | 2003-04-09 | Medicaments comprising steroids and a novel anticholinergic |
Country Status (29)
Country | Link |
---|---|
EP (2) | EP1621197A3 (en) |
JP (1) | JP4559086B2 (en) |
KR (1) | KR101010869B1 (en) |
CN (1) | CN1646126A (en) |
AR (1) | AR039275A1 (en) |
AT (1) | ATE312607T1 (en) |
AU (1) | AU2003216921B2 (en) |
BR (1) | BR0309085A (en) |
CA (1) | CA2481268C (en) |
DE (2) | DE10216429A1 (en) |
DK (1) | DK1496902T3 (en) |
EA (1) | EA008386B1 (en) |
EC (1) | ECSP045355A (en) |
ES (1) | ES2254917T3 (en) |
HR (1) | HRP20040943B1 (en) |
IL (2) | IL164391A0 (en) |
ME (1) | MEP54208A (en) |
MX (1) | MXPA04009917A (en) |
MY (1) | MY137045A (en) |
NO (1) | NO20044097L (en) |
NZ (1) | NZ536284A (en) |
PE (1) | PE20040326A1 (en) |
PL (1) | PL211227B1 (en) |
RS (1) | RS50776B (en) |
TW (1) | TWI311055B (en) |
UA (1) | UA80125C2 (en) |
UY (1) | UY27758A1 (en) |
WO (1) | WO2003086399A1 (en) |
ZA (1) | ZA200406751B (en) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2165768B1 (en) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | NEW DERIVATIVES OF QUINUCLIDINE AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM. |
GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
WO2005074918A1 (en) * | 2004-02-06 | 2005-08-18 | Benzstrasse 1 D-61352 Bad Homburd | The combination of anticholinergics and glucocorticoids for the long-term treatment of asthma and copd |
EP2100598A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
EP2100599A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
CA2763939A1 (en) | 2009-05-29 | 2010-12-02 | Pearl Therapeutics, Inc. | Compositions for pulmonary delivery of long-acting muscarinic antagonists and long-acting b2 adrenergic receptor agonists and associated methods and systems |
US8815258B2 (en) | 2009-05-29 | 2014-08-26 | Pearl Therapeutics, Inc. | Compositions, methods and systems for respiratory delivery of two or more active agents |
EP2510928A1 (en) | 2011-04-15 | 2012-10-17 | Almirall, S.A. | Aclidinium for use in improving the quality of sleep in respiratory patients |
KR102391332B1 (en) | 2013-03-15 | 2022-04-26 | 펄 테라퓨틱스 인코포레이티드 | Methods and systems for conditioning of particulate crystalline materials |
CN115282411A (en) * | 2022-01-14 | 2022-11-04 | 温州医科大学 | Delivery system for delivering drugs into the brain using the nasal olfactory region and method of use thereof |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4570630A (en) | 1983-08-03 | 1986-02-18 | Miles Laboratories, Inc. | Medicament inhalation device |
FR2585563B1 (en) | 1985-07-30 | 1993-11-12 | Glaxo Group Ltd | DEVICE FOR ADMINISTERING MEDICINES TO PATIENTS |
SG45171A1 (en) | 1990-03-21 | 1998-01-16 | Boehringer Ingelheim Int | Atomising devices and methods |
DE4108393A1 (en) | 1991-03-15 | 1992-09-17 | Boehringer Ingelheim Kg | NEW ESTERS BI-AND TRICYCLIC AMINO ALCOHOLS, THEIR PREPARATION AND THEIR USE IN MEDICINAL PRODUCTS |
IL107120A (en) | 1992-09-29 | 1997-09-30 | Boehringer Ingelheim Int | Atomising nozzle and filter and spray generating device |
DE4318455A1 (en) | 1993-06-03 | 1994-12-08 | Boehringer Ingelheim Kg | Capsule holder |
AU700837B2 (en) * | 1995-04-28 | 1999-01-14 | Banyu Pharmaceutical Co., Ltd. | 1,4-di-substituted piperidine derivatives |
DE19536902A1 (en) | 1995-10-04 | 1997-04-10 | Boehringer Ingelheim Int | Miniature fluid pressure generating device |
DE19536903C2 (en) | 1995-10-04 | 1998-09-10 | Boehringer Ingelheim Int | Device for holding a fluidic component |
DE19545226C1 (en) | 1995-12-05 | 1997-06-19 | Boehringer Ingelheim Int | Locking mechanism for a spring-operated output |
GB0009591D0 (en) * | 2000-04-18 | 2000-06-07 | Glaxo Group Ltd | Medical combinations |
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 |
CA2733294C (en) * | 2000-10-31 | 2011-12-20 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmaceutical combination of a tiotropium salt and ciclesonide |
-
2002
- 2002-04-12 DE DE10216429A patent/DE10216429A1/en not_active Withdrawn
-
2003
- 2003-04-09 AR ARP030101241A patent/AR039275A1/en active Pending
- 2003-04-09 ES ES03712137T patent/ES2254917T3/en not_active Expired - Lifetime
- 2003-04-09 DE DE50301934T patent/DE50301934D1/en not_active Expired - Lifetime
- 2003-04-09 EA EA200401303A patent/EA008386B1/en not_active IP Right Cessation
- 2003-04-09 ME MEP-542/08A patent/MEP54208A/en unknown
- 2003-04-09 DK DK03712137T patent/DK1496902T3/en active
- 2003-04-09 EP EP05109887A patent/EP1621197A3/en not_active Withdrawn
- 2003-04-09 AU AU2003216921A patent/AU2003216921B2/en not_active Expired
- 2003-04-09 JP JP2003583418A patent/JP4559086B2/en not_active Expired - Lifetime
- 2003-04-09 BR BR0309085-0A patent/BR0309085A/en not_active Expired - Fee Related
- 2003-04-09 PL PL371561A patent/PL211227B1/en not_active IP Right Cessation
- 2003-04-09 RS YUP-899/04A patent/RS50776B/en unknown
- 2003-04-09 CN CNA038083299A patent/CN1646126A/en active Pending
- 2003-04-09 AT AT03712137T patent/ATE312607T1/en active
- 2003-04-09 WO PCT/EP2003/003668 patent/WO2003086399A1/en active IP Right Grant
- 2003-04-09 IL IL16439103A patent/IL164391A0/en unknown
- 2003-04-09 MX MXPA04009917A patent/MXPA04009917A/en active IP Right Grant
- 2003-04-09 CA CA2481268A patent/CA2481268C/en not_active Expired - Lifetime
- 2003-04-09 EP EP03712137A patent/EP1496902B1/en not_active Expired - Lifetime
- 2003-04-09 NZ NZ536284A patent/NZ536284A/en not_active IP Right Cessation
- 2003-04-09 KR KR1020047016335A patent/KR101010869B1/en not_active IP Right Cessation
- 2003-04-10 UY UY27758A patent/UY27758A1/en not_active Application Discontinuation
- 2003-04-10 TW TW092108227A patent/TWI311055B/en not_active IP Right Cessation
- 2003-04-10 MY MYPI20031320A patent/MY137045A/en unknown
- 2003-04-10 PE PE2003000365A patent/PE20040326A1/en not_active Application Discontinuation
- 2003-09-04 UA UA20041109192A patent/UA80125C2/en unknown
-
2004
- 2004-08-25 ZA ZA200406751A patent/ZA200406751B/en unknown
- 2004-09-27 NO NO20044097A patent/NO20044097L/en not_active Application Discontinuation
- 2004-10-04 IL IL164391A patent/IL164391A/en not_active IP Right Cessation
- 2004-10-11 EC EC2004005355A patent/ECSP045355A/en unknown
- 2004-10-11 HR HRP20040943AA patent/HRP20040943B1/en not_active IP Right Cessation
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request | ||
MKEX | Expiry |
Effective date: 20230411 |