SK7292002A3 - Pharmaceutical composition with controlled release for increasing the dose or system exposure of a medicament inhibiting pde4 - Google Patents

Pharmaceutical composition with controlled release for increasing the dose or system exposure of a medicament inhibiting pde4 Download PDF

Info

Publication number: SK7292002A3
Authority: SK; Slovakia
Prior art keywords: drug; dose; pharmaceutical composition; controlled release; pde4
Prior art date: 1999-10-29

Application number

SK729-2002A

Other languages

English (en)

Slovak (sk)

Inventor

Robert D Murdoch

Theodore J Torphy

Barry D Zussman

Original Assignee

Smithkline Beecham Corp

Smithkline Beecham Plc

Priority date (The priority date 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 date listed.)

1999-10-29

Filing date

2000-10-26

Publication date

2002-12-03

2000-10-26 Application filed by Smithkline Beecham Corp, Smithkline Beecham Plc filed Critical Smithkline Beecham Corp

2002-12-03 Publication of SK7292002A3 publication Critical patent/SK7292002A3/sk

Links

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238000013270 controlled release Methods 0.000 title claims description 47
239000008194 pharmaceutical composition Substances 0.000 title claims description 23
230000002401 inhibitory effect Effects 0.000 title claims description 12
101100296719 Caenorhabditis elegans pde-4 gene Proteins 0.000 title 1
230000036470 plasma concentration Effects 0.000 claims abstract description 27
229940079593 drug Drugs 0.000 claims description 81
239000000203 mixture Substances 0.000 claims description 60
230000000694 effects Effects 0.000 claims description 53
239000012729 immediate-release (IR) formulation Substances 0.000 claims description 48
229920002125 Sokalan® Polymers 0.000 claims description 29
239000000546 pharmaceutical excipient Substances 0.000 claims description 13
230000009885 systemic effect Effects 0.000 claims description 7
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239000000651 prodrug Substances 0.000 claims description 4
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MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical compound FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 claims description 4
150000003839 salts Chemical class 0.000 claims description 4
JVTIXNMXDLQEJE-UHFFFAOYSA-N 2-decanoyloxypropyl decanoate 2-octanoyloxypropyl octanoate Chemical compound C(CCCCCCC)(=O)OCC(C)OC(CCCCCCC)=O.C(=O)(CCCCCCCCC)OCC(C)OC(=O)CCCCCCCCC JVTIXNMXDLQEJE-UHFFFAOYSA-N 0.000 claims description 3
150000002148 esters Chemical class 0.000 claims description 3
229960002586 roflumilast Drugs 0.000 claims description 3
101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 claims 1
101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 claims 1
238000010521 absorption reaction Methods 0.000 abstract description 22
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HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 12
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QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 3
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229960000278 theophylline Drugs 0.000 description 2
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HJPRDDKCXVCFOH-UHFFFAOYSA-N 1,3-dibutyl-7-(2-oxopropyl)purine-2,6-dione Chemical compound O=C1N(CCCC)C(=O)N(CCCC)C2=C1N(CC(C)=O)C=N2 HJPRDDKCXVCFOH-UHFFFAOYSA-N 0.000 description 1
SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
MRHCSNNEUHXNIC-UHFFFAOYSA-N 9-benzylpurin-6-amine Chemical class C1=NC=2C(N)=NC=NC=2N1CC1=CC=CC=C1 MRHCSNNEUHXNIC-UHFFFAOYSA-N 0.000 description 1
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WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
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IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 description 1
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101000909851 Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv) cAMP/cGMP dual specificity phosphodiesterase Rv0805 Proteins 0.000 description 1
BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 description 1
229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 1
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239000007933 dermal patch Substances 0.000 description 1
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DPHDSIQHVGSITN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-2-[1-[(4-fluorophenyl)methyl]-5-hydroxyindol-3-yl]-2-oxoacetamide Chemical compound C1=C(C(=O)C(=O)NC=2C(=CN=CC=2Cl)Cl)C2=CC(O)=CC=C2N1CC1=CC=C(F)C=C1 DPHDSIQHVGSITN-UHFFFAOYSA-N 0.000 description 1
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230000003204 osmotic effect Effects 0.000 description 1
WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
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239000006187 pill Substances 0.000 description 1
239000002243 precursor Substances 0.000 description 1
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HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 description 1
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- 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
- A61K31/74—Synthetic polymeric materials
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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
- A61P35/00—Antineoplastic agents
- 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)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Epidemiology (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pulmonology (AREA)
Inorganic Chemistry (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Hospice & Palliative Care (AREA)
Rheumatology (AREA)
Pain & Pain Management (AREA)
Psychiatry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Enzymes And Modification Thereof (AREA)

SK729-2002A 1999-10-29 2000-10-26 Pharmaceutical composition with controlled release for increasing the dose or system exposure of a medicament inhibiting pde4 SK7292002A3 (en)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date	Title
US16247799P	1999-10-29	1999-10-29
US16264199P	1999-11-01	1999-11-01
US17981700P	2000-02-02	2000-02-02
PCT/US2000/029453 WO2001032165A1 (en)	1999-10-29	2000-10-26	Method for administering a phosphodiesterase 4 inhibitor

Publications (1)

Publication Number	Publication Date
SK7292002A3 true SK7292002A3 (en)	2002-12-03

Family

ID=27388757

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK729-2002A SK7292002A3 (en)	1999-10-29	2000-10-26	Pharmaceutical composition with controlled release for increasing the dose or system exposure of a medicament inhibiting pde4

Country Status (29)

Country	Link
US (1)	US20030212112A1 (pl)
EP (1)	EP1225884A4 (pl)
JP (1)	JP2003513038A (pl)
KR (1)	KR20020050249A (pl)
CN (1)	CN1387433A (pl)
AP (1)	AP2002002446A0 (pl)
AR (1)	AR026254A1 (pl)
AU (1)	AU772909B2 (pl)
BG (1)	BG106623A (pl)
BR (1)	BR0015039A (pl)
CA (1)	CA2389293A1 (pl)
CO (1)	CO5271676A1 (pl)
CZ (1)	CZ20021443A3 (pl)
DZ (1)	DZ3249A1 (pl)
EA (1)	EA200200502A1 (pl)
HK (1)	HK1049105A1 (pl)
HU (1)	HUP0203682A3 (pl)
IL (1)	IL148813A0 (pl)
MA (1)	MA25562A1 (pl)
MX (1)	MXPA02004220A (pl)
NO (1)	NO20021937L (pl)
NZ (1)	NZ518002A (pl)
OA (1)	OA12078A (pl)
PE (1)	PE20011004A1 (pl)
PL (1)	PL355262A1 (pl)
SK (1)	SK7292002A3 (pl)
TR (1)	TR200201150T2 (pl)
UY (1)	UY26422A1 (pl)
WO (1)	WO2001032165A1 (pl)

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DE10207160A1 (de) *	2002-02-20	2003-12-18	Altana Pharma Ag	Darreichungsform enthaltend PDE 4-Hemmer als Wirkstoff
ME00565A (en) *	2002-05-28	2011-12-20		Topically applicable pharmaceutical preparation
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PT1606261E (pt)	2003-03-10	2010-01-11	Nycomed Gmbh	Novo processo para a preparação de roflumilast
WO2004096274A1 (ja) *	2003-03-31	2004-11-11	Kyowa Hakko Kogyo Co., Ltd.	気道内投与剤
US20050026883A1 (en) *	2003-07-31	2005-02-03	Robinson Cynthia B.	Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a PDE-4 inhibitor for treatment of asthma or chronic obstructive pulmonary disease
US8663694B2 (en)	2005-03-16	2014-03-04	Takeda Gmbh	Taste masked dosage form containing roflumilast
CN102711463B (zh) *	2009-12-03	2015-05-13	Opko健康公司	超硫酸化双糖制剂
RS60415B1 (sr) *	2011-12-27	2020-07-31	Amgen (Europe) GmbH	Formulacije (+)-2-[1-(3-etoksi-4-metoksi-fenil)-2-metansulfonil-etil]-4-acetil aminoizoindolin-1,3-diona
CN103536582A (zh) *	2013-10-12	2014-01-29	云南龙海天然植物药业有限公司	罗氟司特干粉吸入剂
US12582809B2 (en)	2018-01-26	2026-03-24	Bt Bidco, Inc.	Treatment of a disease of the gastrointestinal tract with a PDE4 inhibitor
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CN121197633A (zh)	2019-12-13	2025-12-26	比特比德科有限责任公司	用于将治疗剂递送至胃肠道的可摄取装置

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MY121142A (en) *	1999-02-23	2005-12-30	Smithkline Beecham Corp	Controlled release formulation for treating copd
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2000
- 2000-10-26 CA CA002389293A patent/CA2389293A1/en not_active Abandoned
- 2000-10-26 IL IL14881300A patent/IL148813A0/xx unknown
- 2000-10-26 BR BR0015039-8A patent/BR0015039A/pt not_active IP Right Cessation
- 2000-10-26 AR ARP000105644A patent/AR026254A1/es not_active Application Discontinuation
- 2000-10-26 JP JP2001534370A patent/JP2003513038A/ja not_active Withdrawn
- 2000-10-26 PL PL00355262A patent/PL355262A1/pl unknown
- 2000-10-26 MX MXPA02004220A patent/MXPA02004220A/es unknown
- 2000-10-26 TR TR2002/01150T patent/TR200201150T2/xx unknown
- 2000-10-26 WO PCT/US2000/029453 patent/WO2001032165A1/en not_active Ceased
- 2000-10-26 AU AU13445/01A patent/AU772909B2/en not_active Ceased
- 2000-10-26 EA EA200200502A patent/EA200200502A1/ru unknown
- 2000-10-26 CN CN00815150A patent/CN1387433A/zh active Pending
- 2000-10-26 CZ CZ20021443A patent/CZ20021443A3/cs unknown
- 2000-10-26 SK SK729-2002A patent/SK7292002A3/sk unknown
- 2000-10-26 AP APAP/P/2002/002446A patent/AP2002002446A0/en unknown
- 2000-10-26 OA OA1200200126A patent/OA12078A/en unknown
- 2000-10-26 EP EP00975385A patent/EP1225884A4/en not_active Withdrawn
- 2000-10-26 HK HK02109231.8A patent/HK1049105A1/zh unknown
- 2000-10-26 KR KR1020027005448A patent/KR20020050249A/ko not_active Withdrawn
- 2000-10-26 CO CO00081570A patent/CO5271676A1/es not_active Application Discontinuation
- 2000-10-26 HU HU0203682A patent/HUP0203682A3/hu unknown
- 2000-10-26 NZ NZ518002A patent/NZ518002A/en unknown
- 2000-10-26 DZ DZ003249A patent/DZ3249A1/fr active
- 2000-10-27 PE PE2000001157A patent/PE20011004A1/es not_active Application Discontinuation
- 2000-10-30 UY UY26422A patent/UY26422A1/es not_active Application Discontinuation
2002
- 2002-04-17 BG BG106623A patent/BG106623A/bg unknown
- 2002-04-24 NO NO20021937A patent/NO20021937L/no not_active Application Discontinuation
- 2002-04-26 MA MA26618A patent/MA25562A1/fr unknown
2003
- 2003-05-02 US US10/429,666 patent/US20030212112A1/en not_active Abandoned

Also Published As

Publication number	Publication date
BR0015039A (pt)	2002-06-25
JP2003513038A (ja)	2003-04-08
HUP0203682A3 (en)	2003-10-28
WO2001032165A1 (en)	2001-05-10
NO20021937L (no)	2002-05-30
IL148813A0 (en)	2002-09-12
CA2389293A1 (en)	2001-05-10
MA25562A1 (fr)	2002-10-01
AR026254A1 (es)	2003-02-05
AP2002002446A0 (en)	2002-03-31
CO5271676A1 (es)	2003-04-30
BG106623A (bg)	2003-02-28
DZ3249A1 (fr)	2001-05-10
CN1387433A (zh)	2002-12-25
AU772909B2 (en)	2004-05-13
NZ518002A (en)	2004-01-30
TR200201150T2 (tr)	2002-09-23
PE20011004A1 (es)	2001-09-28
US20030212112A1 (en)	2003-11-13
EP1225884A4 (en)	2005-06-15
EP1225884A1 (en)	2002-07-31
HUP0203682A2 (hu)	2003-04-28
EA200200502A1 (ru)	2002-10-31
PL355262A1 (pl)	2004-04-05
MXPA02004220A (es)	2002-10-17
HK1049105A1 (zh)	2003-05-02
CZ20021443A3 (cs)	2003-01-15
KR20020050249A (ko)	2002-06-26
NO20021937D0 (no)	2002-04-24
UY26422A1 (es)	2001-07-31
OA12078A (en)	2003-05-28
AU1344501A (en)	2001-05-14

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