SK6942003A3 - Oral extended release formulation of gepirone - Google Patents

Oral extended release formulation of gepirone Download PDF

Info

Publication number: SK6942003A3
Authority: SK; Slovakia
Prior art keywords: amount; gepirone; pharmaceutical composition; tablets; polymer matrix
Prior art date: 2000-12-08

Application number

SK694-2003A

Other languages

English (en)

Slovak (sk)

Inventor

Johannes Gerardus Jos Egberink

John Francis Engelhart

Original Assignee

Akzo Nobel Nv

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.)

2000-12-08

Filing date

2001-11-30

Publication date

2003-10-07

2001-11-30 Application filed by Akzo Nobel Nv filed Critical Akzo Nobel Nv

2003-10-07 Publication of SK6942003A3 publication Critical patent/SK6942003A3/sk

Links

QOIGKGMMAGJZNZ-UHFFFAOYSA-N gepirone Chemical compound O=C1CC(C)(C)CC(=O)N1CCCCN1CCN(C=2N=CC=CN=2)CC1 QOIGKGMMAGJZNZ-UHFFFAOYSA-N 0.000 title claims abstract description 28
229960000647 gepirone Drugs 0.000 title claims abstract description 28
239000000203 mixture Substances 0.000 title abstract description 25
238000009472 formulation Methods 0.000 title abstract description 6
238000013265 extended release Methods 0.000 title abstract 3
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 20
229920000642 polymer Polymers 0.000 claims abstract description 11
239000011159 matrix material Substances 0.000 claims abstract description 10
229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 9
235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 9
239000008108 microcrystalline cellulose Substances 0.000 claims abstract description 9
229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 9
239000011230 binding agent Substances 0.000 claims abstract description 7
238000011282 treatment Methods 0.000 claims abstract description 4
238000013268 sustained release Methods 0.000 claims description 10
239000012730 sustained-release form Substances 0.000 claims description 10
235000010980 cellulose Nutrition 0.000 claims description 5
229920002678 cellulose Polymers 0.000 claims description 5
239000001913 cellulose Substances 0.000 claims description 5
108010038196 saccharide-binding proteins Proteins 0.000 claims description 3
208000020401 Depressive disease Diseases 0.000 claims 1
210000003169 central nervous system Anatomy 0.000 claims 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
208000015114 central nervous system disease Diseases 0.000 abstract description 3
208000012902 Nervous system disease Diseases 0.000 abstract 1
150000001720 carbohydrates Chemical class 0.000 abstract 1
238000000034 method Methods 0.000 description 9
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
238000004519 manufacturing process Methods 0.000 description 6
229940079593 drug Drugs 0.000 description 5
239000003814 drug Substances 0.000 description 5
239000004615 ingredient Substances 0.000 description 5
239000000546 pharmaceutical excipient Substances 0.000 description 5
239000000314 lubricant Substances 0.000 description 4
235000019359 magnesium stearate Nutrition 0.000 description 4
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
229940075614 colloidal silicon dioxide Drugs 0.000 description 3
238000007906 compression Methods 0.000 description 3
230000006835 compression Effects 0.000 description 3
-1 glidants Substances 0.000 description 3
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 3
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 3
238000002156 mixing Methods 0.000 description 3
238000003825 pressing Methods 0.000 description 3
UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 2
125000000217 alkyl group Chemical group 0.000 description 2
239000003086 colorant Substances 0.000 description 2
238000004040 coloring Methods 0.000 description 2
238000004090 dissolution Methods 0.000 description 2
239000000975 dye Substances 0.000 description 2
230000000694 effects Effects 0.000 description 2
239000000945 filler Substances 0.000 description 2
JITOKQVGRJSHHA-UHFFFAOYSA-M monosodium methyl arsenate Chemical compound [Na+].C[As](O)([O-])=O JITOKQVGRJSHHA-UHFFFAOYSA-M 0.000 description 2
229940124531 pharmaceutical excipient Drugs 0.000 description 2
230000002035 prolonged effect Effects 0.000 description 2
102220487426 Actin-related protein 2/3 complex subunit 3_K15M_mutation Human genes 0.000 description 1
229920000945 Amylopectin Polymers 0.000 description 1
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
229920001353 Dextrin Polymers 0.000 description 1
239000004375 Dextrin Substances 0.000 description 1
239000001856 Ethyl cellulose Substances 0.000 description 1
ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
229920002774 Maltodextrin Polymers 0.000 description 1
239000005913 Maltodextrin Substances 0.000 description 1
229920003091 Methocel™ Polymers 0.000 description 1
229920002472 Starch Polymers 0.000 description 1
238000010521 absorption reaction Methods 0.000 description 1
239000004480 active ingredient Substances 0.000 description 1
239000013543 active substance Substances 0.000 description 1
239000000654 additive Substances 0.000 description 1
235000010443 alginic acid Nutrition 0.000 description 1
229920000615 alginic acid Polymers 0.000 description 1
229920013820 alkyl cellulose Polymers 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000002775 capsule Substances 0.000 description 1
125000004432 carbon atom Chemical group C* 0.000 description 1
239000000969 carrier Substances 0.000 description 1
238000012512 characterization method Methods 0.000 description 1
239000003795 chemical substances by application Substances 0.000 description 1
UHZZMRAGKVHANO-UHFFFAOYSA-M chlormequat chloride Chemical compound [Cl-].C[N+](C)(C)CCCl UHZZMRAGKVHANO-UHFFFAOYSA-M 0.000 description 1
150000001875 compounds Chemical class 0.000 description 1
235000019425 dextrin Nutrition 0.000 description 1
238000009826 distribution Methods 0.000 description 1
239000002552 dosage form Substances 0.000 description 1
239000003937 drug carrier Substances 0.000 description 1
238000002651 drug therapy Methods 0.000 description 1
229920001249 ethyl cellulose Polymers 0.000 description 1
235000019325 ethyl cellulose Nutrition 0.000 description 1
238000001125 extrusion Methods 0.000 description 1
238000000227 grinding Methods 0.000 description 1
238000009775 high-speed stirring Methods 0.000 description 1
125000002768 hydroxyalkyl group Chemical group 0.000 description 1
239000001863 hydroxypropyl cellulose Substances 0.000 description 1
235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
208000024714 major depressive disease Diseases 0.000 description 1
229940035034 maltodextrin Drugs 0.000 description 1
239000000463 material Substances 0.000 description 1
229920000609 methyl cellulose Polymers 0.000 description 1
239000001923 methylcellulose Substances 0.000 description 1
235000010981 methylcellulose Nutrition 0.000 description 1
238000000465 moulding Methods 0.000 description 1
238000011369 optimal treatment Methods 0.000 description 1
239000008203 oral pharmaceutical composition Substances 0.000 description 1
208000019906 panic disease Diseases 0.000 description 1
239000000843 powder Substances 0.000 description 1
238000011084 recovery Methods 0.000 description 1
229920005989 resin Polymers 0.000 description 1
239000011347 resin Substances 0.000 description 1
229920006395 saturated elastomer Polymers 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
238000003756 stirring Methods 0.000 description 1
239000000126 substance Substances 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000007916 tablet composition Substances 0.000 description 1
238000011287 therapeutic dose Methods 0.000 description 1
238000011269 treatment regimen Methods 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
- 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
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
- 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
- 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
- A61P25/24—Antidepressants

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Epidemiology (AREA)
Neurosurgery (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Biomedical Technology (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Neurology (AREA)
General Chemical & Material Sciences (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Inorganic Chemistry (AREA)
Medicinal Preparation (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

SK694-2003A 2000-12-08 2001-11-30 Oral extended release formulation of gepirone SK6942003A3 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP00204388		2000-12-08
PCT/EP2001/014189 WO2002045753A2 (en)	2000-12-08	2001-11-30	Oral extended release formulation of gepirone

Publications (1)

Publication Number	Publication Date
SK6942003A3 true SK6942003A3 (en)	2003-10-07

Family

ID=8172397

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK694-2003A SK6942003A3 (en)	2000-12-08	2001-11-30	Oral extended release formulation of gepirone

Country Status (19)

Country	Link
EP (1)	EP1343504A2 (no)
JP (1)	JP2004517083A (no)
KR (1)	KR20040018314A (no)
CN (1)	CN1479620A (no)
AR (1)	AR031461A1 (no)
AU (1)	AU2002226371A1 (no)
BR (1)	BR0115976A (no)
CA (1)	CA2436692A1 (no)
CZ (1)	CZ20031589A3 (no)
EC (1)	ECSP034627A (no)
HU (1)	HUP0401021A2 (no)
IL (1)	IL155855A0 (no)
MX (1)	MXPA03005099A (no)
NO (1)	NO20032581D0 (no)
PL (1)	PL362445A1 (no)
RU (1)	RU2003120446A (no)
SK (1)	SK6942003A3 (no)
WO (1)	WO2002045753A2 (no)
ZA (1)	ZA200303915B (no)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2004028507A1 (en) *	2002-09-24	2004-04-08	Akzo Nobel N.V.	Method to improve pharmaceutical tablets having a matrix of cellulose ether
CA2585606A1 (en) *	2004-11-05	2006-05-18	Fabre-Kramer Pharmaceuticals, Inc.	High-dosage extended-release formulation of gepirone
WO2019023250A1 (en) *	2017-07-26	2019-01-31	Abbott Laboratories	NUTRITIONAL TABLETS AND METHODS OF MAKING THE SAME
CN109745323A (zh) *	2017-11-01	2019-05-14	四川科瑞德制药股份有限公司	氮哌酮类化合物提高副交感神经活性的用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5478572A (en) *	1994-09-06	1995-12-26	Bristol-Myers Squibb Co.	Gepirone dosage form

2001
- 2001-11-30 RU RU2003120446/15A patent/RU2003120446A/ru not_active Application Discontinuation
- 2001-11-30 CN CNA018201792A patent/CN1479620A/zh active Pending
- 2001-11-30 BR BR0115976-3A patent/BR0115976A/pt not_active Application Discontinuation
- 2001-11-30 HU HU0401021A patent/HUP0401021A2/hu unknown
- 2001-11-30 AU AU2002226371A patent/AU2002226371A1/en not_active Abandoned
- 2001-11-30 KR KR10-2003-7007555A patent/KR20040018314A/ko not_active Withdrawn
- 2001-11-30 WO PCT/EP2001/014189 patent/WO2002045753A2/en not_active Ceased
- 2001-11-30 SK SK694-2003A patent/SK6942003A3/sk unknown
- 2001-11-30 PL PL01362445A patent/PL362445A1/xx not_active Application Discontinuation
- 2001-11-30 MX MXPA03005099A patent/MXPA03005099A/es unknown
- 2001-11-30 IL IL15585501A patent/IL155855A0/xx unknown
- 2001-11-30 CA CA002436692A patent/CA2436692A1/en not_active Abandoned
- 2001-11-30 JP JP2002547535A patent/JP2004517083A/ja not_active Withdrawn
- 2001-11-30 EP EP01995688A patent/EP1343504A2/en not_active Withdrawn
- 2001-11-30 CZ CZ20031589A patent/CZ20031589A3/cs unknown
- 2001-12-07 AR ARP010105683A patent/AR031461A1/es not_active Application Discontinuation
2003
- 2003-05-20 ZA ZA200303915A patent/ZA200303915B/en unknown
- 2003-05-28 EC EC2003004627A patent/ECSP034627A/es unknown
- 2003-06-06 NO NO20032581A patent/NO20032581D0/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
WO2002045753A3 (en)	2002-08-29
ECSP034627A (es)	2004-09-28
NO20032581L (no)	2003-06-06
PL362445A1 (en)	2004-11-02
HUP0401021A2 (hu)	2004-09-28
EP1343504A2 (en)	2003-09-17
WO2002045753A2 (en)	2002-06-13
ZA200303915B (en)	2004-08-20
NO20032581D0 (no)	2003-06-06
JP2004517083A (ja)	2004-06-10
AU2002226371A1 (en)	2002-06-18
BR0115976A (pt)	2003-12-30
KR20040018314A (ko)	2004-03-03
CZ20031589A3 (cs)	2003-11-12
CA2436692A1 (en)	2002-06-13
MXPA03005099A (es)	2004-02-12
AR031461A1 (es)	2003-09-24
RU2003120446A (ru)	2005-02-20
CN1479620A (zh)	2004-03-03
IL155855A0 (en)	2003-12-23

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