CA2593432A1 - Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene - Google Patents

Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene Download PDF

Info

Publication number: CA2593432A1
Authority: CA; Canada
Prior art keywords: varenicline; dosage form; fast disintegrating; disintegrating dosage; fast
Prior art date: 2005-01-07
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.): Abandoned

Application number

CA002593432A

Other languages

English (en)

Inventor

Barbara Alice Johnson

Carl Bernard Ziegler Jr.

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Pfizer Products Inc

Original Assignee

Individual

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.)

2005-01-07

Filing date

2005-12-22

Publication date

2006-07-13

2005-12-22 Application filed by Individual filed Critical Individual

2006-07-13 Publication of CA2593432A1 publication Critical patent/CA2593432A1/fr

Status Abandoned legal-status Critical Current

Links

239000002552 dosage form Substances 0.000 title claims abstract description 109
JQSHBVHOMNKWFT-UHFFFAOYSA-N varenicline Chemical compound C12=CC3=NC=CN=C3C=C2C2CC1CNC2 JQSHBVHOMNKWFT-UHFFFAOYSA-N 0.000 title description 2
229960004751 varenicline Drugs 0.000 claims abstract description 130
JQSHBVHOMNKWFT-DTORHVGOSA-N varenicline Chemical compound C12=CC3=NC=CN=C3C=C2[C@H]2C[C@@H]1CNC2 JQSHBVHOMNKWFT-DTORHVGOSA-N 0.000 claims abstract description 130
238000000034 method Methods 0.000 claims abstract description 60
239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 42
150000003839 salts Chemical class 0.000 claims abstract description 29
210000000214 mouth Anatomy 0.000 claims abstract description 24
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 6
235000002637 Nicotiana tabacum Nutrition 0.000 claims abstract description 5
206010057852 Nicotine dependence Diseases 0.000 claims abstract description 5
208000025569 Tobacco Use disease Diseases 0.000 claims abstract description 5
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 33
-1 Brij.TM.35 Polymers 0.000 claims description 32
FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 29
229930195725 Mannitol Natural products 0.000 claims description 29
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239000000594 mannitol Substances 0.000 claims description 29
239000003795 chemical substances by application Substances 0.000 claims description 28
239000011230 binding agent Substances 0.000 claims description 27
150000001720 carbohydrates Chemical class 0.000 claims description 24
235000014633 carbohydrates Nutrition 0.000 claims description 24
235000003599 food sweetener Nutrition 0.000 claims description 22
239000003765 sweetening agent Substances 0.000 claims description 22
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 21
FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 20
FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 19
235000010356 sorbitol Nutrition 0.000 claims description 19
239000000600 sorbitol Substances 0.000 claims description 19
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 18
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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 claims description 10
HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 10
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235000010447 xylitol Nutrition 0.000 claims description 10
HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 10
229960002675 xylitol Drugs 0.000 claims description 10
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 8
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239000000126 substance Substances 0.000 claims description 8
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CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 7
235000010418 carrageenan Nutrition 0.000 claims description 7
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235000010420 locust bean gum Nutrition 0.000 claims description 7
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UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 claims description 7
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 6
WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical class [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 claims description 6
NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 6
206010012335 Dependence Diseases 0.000 claims description 6
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239000002202 Polyethylene glycol Substances 0.000 claims description 6
208000030886 Traumatic Brain injury Diseases 0.000 claims description 6
206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 6
OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 6
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ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims description 6
235000010445 lecithin Nutrition 0.000 claims description 6
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230000009529 traumatic brain injury Effects 0.000 claims description 6
FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical class OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 5
150000001860 citric acid derivatives Chemical class 0.000 claims description 5
235000019868 cocoa butter Nutrition 0.000 claims description 5
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235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 5
239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims description 5
229940068968 polysorbate 80 Drugs 0.000 claims description 5
229920000053 polysorbate 80 Polymers 0.000 claims description 5
229960002920 sorbitol Drugs 0.000 claims description 5
BLILOGGUTRWFNI-UHFFFAOYSA-N Monomenthyl succinate Chemical compound CC(C)C1CCC(C)CC1OC(=O)CCC(O)=O BLILOGGUTRWFNI-UHFFFAOYSA-N 0.000 claims description 4
244000061176 Nicotiana tabacum Species 0.000 claims description 4
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HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims description 3
SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 3
CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 3
GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims description 3
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UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
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HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims description 3
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Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Pain & Pain Management (AREA)
Heart & Thoracic Surgery (AREA)
Psychiatry (AREA)
Cardiology (AREA)
Epidemiology (AREA)
Psychology (AREA)
Obesity (AREA)
Anesthesiology (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Hematology (AREA)
Diabetes (AREA)
Hospice & Palliative Care (AREA)
Rheumatology (AREA)
Child & Adolescent Psychology (AREA)
Zoology (AREA)
Nutrition Science (AREA)
Physiology (AREA)
Dermatology (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

CA002593432A 2005-01-07 2005-12-22 Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene Abandoned CA2593432A1 (fr)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US64208305P	2005-01-07	2005-01-07
US60/642,083		2005-01-07
PCT/IB2005/003979 WO2006072832A1 (fr)	2005-01-07	2005-12-22	Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene

Publications (1)

Publication Number	Publication Date
CA2593432A1 true CA2593432A1 (fr)	2006-07-13

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ID=36129747

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CA002593432A Abandoned CA2593432A1 (fr)	2005-01-07	2005-12-22	Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene

Country Status (4)

Country	Link
EP (1)	EP1843769A1 (fr)
JP (1)	JP2008526827A (fr)
CA (1)	CA2593432A1 (fr)
WO (1)	WO2006072832A1 (fr)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20110086086A1 (en) *	2005-07-26	2011-04-14	Pfizer Inc	Transdermal system for varenicline
JP5228359B2 (ja) *	2007-04-12	2013-07-03	ニプロ株式会社	主薬粒子及びその製造方法ならびに口腔内崩壊錠
BRPI0811303A2 (pt) *	2007-05-08	2015-01-27	Hercules Inc	Formulação de comprimido de desintegranção rápida robusta
EP2262780A4 (fr) *	2008-03-06	2012-01-25	Reddys Lab Ltd Dr	Tartrate de varénicline amorphe
EP2370417A2 (fr) *	2008-11-21	2011-10-05	Millennium Pharmaceuticals, Inc.	Sel de lactate du (4-isopropoxyphényl)-amide de l acide 4-(6-méthoxy-7-(3-pipéridin-1-yl-propoxy)quinazolin-4-yl¨pipérazine-1-carboxylique et les compositions pharmaceutiques l incluant dans le traitement du cancer et d'autres pathologies ou troubles
WO2010061846A1 (fr) *	2008-11-25	2010-06-03	田辺三菱製薬株式会社	Comprimé à délitement oral rapide, et procédé pour produire celui-ci
EP2397161B1 (fr) *	2009-02-12	2019-09-25	Fuji Chemical Industry Co., Ltd.	Composition de particule se désintégrant et matériau moulé par compression se désintégrant rapidement comprenant celle-ci
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2005
- 2005-12-22 WO PCT/IB2005/003979 patent/WO2006072832A1/fr not_active Ceased
- 2005-12-22 CA CA002593432A patent/CA2593432A1/fr not_active Abandoned
- 2005-12-22 JP JP2007549963A patent/JP2008526827A/ja not_active Abandoned
- 2005-12-22 EP EP05826405A patent/EP1843769A1/fr not_active Withdrawn

Also Published As

Publication number	Publication date
EP1843769A1 (fr)	2007-10-17
JP2008526827A (ja)	2008-07-24
WO2006072832A1 (fr)	2006-07-13

Publication	Publication Date	Title
US20060057207A1 (en)	2006-03-16	Fast-disintegrating dosage forms of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene
CA2593432A1 (fr)	2006-07-13	Formes posologiques a desintegration rapide de 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene
AU2002300238C1 (en)	2004-03-04	Process for manufacturing bite-dispersion tablets
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JP6061924B2 (ja)	2017-01-18	口腔内分散性製剤
US20030165566A1 (en)	2003-09-04	Sedative non-benzodiazepine formulations
KR20050118775A (ko)	2005-12-20	당류의 재결정화 및 약물과의 가교형성을 이용한 구강내속붕해정
WO2013098399A1 (fr)	2013-07-04	Formulation de mozavaptan
EP1941878A1 (fr)	2008-07-09	Formules sédatives sans benzodiazépine
AU2003201155B2 (en)	2007-03-08	Sedative non-benzodiazepine formulations

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