NO328889B1 - Faste lipid-formuleringer, fremstilling av slike samt anvendelse av slike for fremstilling av medikament for forebygging og behandling av fedme. - Google Patents

Faste lipid-formuleringer, fremstilling av slike samt anvendelse av slike for fremstilling av medikament for forebygging og behandling av fedme. Download PDF

Info

Publication number: NO328889B1
Authority: NO; Norway
Prior art keywords: pharmaceutical preparation; preparation according; fatty acid; mixtures; group
Prior art date: 1999-09-13

Application number

NO20021205A

Other languages

English (en)

Norwegian (no)

Other versions

NO20021205L (no

NO20021205D0 (no

Inventor

Paul Hadvary

Passchier Christiaan De Smidt

Hans Lengsfeld

Hans Steffen

Joseph Tardio

Marcel Schmid

David Macfarland Small

Original Assignee

Hoffmann La Roche

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.)

1999-09-13

Filing date

2002-03-12

Publication date

2010-06-07

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8238989&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO328889(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2002-03-12 Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche

2002-03-12 Publication of NO20021205L publication Critical patent/NO20021205L/no

2002-03-12 Publication of NO20021205D0 publication Critical patent/NO20021205D0/no

2010-06-07 Publication of NO328889B1 publication Critical patent/NO328889B1/no

Links

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Classifications

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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic 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
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- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- 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
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- A—HUMAN NECESSITIES
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- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- 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
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics

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Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
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Biophysics (AREA)
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Chemical Kinetics & Catalysis (AREA)
Diabetes (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Zoology (AREA)
Nutrition Science (AREA)
Physiology (AREA)
Obesity (AREA)
Hematology (AREA)
Child & Adolescent Psychology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicinal Preparation (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicines Containing Plant Substances (AREA)

NO20021205A 1999-09-13 2002-03-12 Faste lipid-formuleringer, fremstilling av slike samt anvendelse av slike for fremstilling av medikament for forebygging og behandling av fedme. NO328889B1 (no)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP99118179		1999-09-13
PCT/EP2000/008857 WO2001019378A2 (fr)	1999-09-13	2000-09-11	Formulations lipidiques solides

Publications (3)

Publication Number	Publication Date
NO20021205L NO20021205L (no)	2002-03-12
NO20021205D0 NO20021205D0 (no)	2002-03-12
NO328889B1 true NO328889B1 (no)	2010-06-07

Family

ID=8238989

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO20021205A NO328889B1 (no)	1999-09-13	2002-03-12	Faste lipid-formuleringer, fremstilling av slike samt anvendelse av slike for fremstilling av medikament for forebygging og behandling av fedme.

Country Status (36)

Country	Link
US (1)	US6703369B1 (fr)
EP (1)	EP1216048B1 (fr)
JP (1)	JP4217017B2 (fr)
KR (1)	KR100523879B1 (fr)
CN (1)	CN1197554C (fr)
AR (1)	AR025609A1 (fr)
AT (1)	ATE285783T1 (fr)
AU (1)	AU769016B2 (fr)
BR (1)	BRPI0013940B1 (fr)
CA (1)	CA2383036C (fr)
CO (1)	CO5210857A1 (fr)
CZ (1)	CZ301844B6 (fr)
DE (1)	DE60017156T2 (fr)
EG (1)	EG24225A (fr)
ES (1)	ES2233444T3 (fr)
GC (1)	GC0000259A (fr)
HK (1)	HK1049798B (fr)
HR (1)	HRP20020206B1 (fr)
HU (1)	HU229037B1 (fr)
IL (2)	IL148570A0 (fr)
JO (1)	JO2300B1 (fr)
MA (1)	MA26817A1 (fr)
ME (1)	ME00675B (fr)
MX (1)	MXPA02002662A (fr)
MY (1)	MY127430A (fr)
NO (1)	NO328889B1 (fr)
NZ (1)	NZ517396A (fr)
PE (1)	PE20010661A1 (fr)
PL (1)	PL199869B1 (fr)
PT (1)	PT1216048E (fr)
RS (1)	RS50373B (fr)
RU (1)	RU2248218C2 (fr)
SI (1)	SI1216048T1 (fr)
TR (1)	TR200200605T2 (fr)
WO (1)	WO2001019378A2 (fr)
ZA (1)	ZA200201249B (fr)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
AR025609A1 (es) *	1999-09-13	2002-12-04	Hoffmann La Roche	Formulaciones lipidas solidas
CN100423715C (zh) *	2000-07-28	2008-10-08	霍夫曼-拉罗奇有限公司	新型药物组合物
US20030027786A1 (en) *	2001-06-06	2003-02-06	Karsten Maeder	Lipase inhibiting composition
US6730319B2 (en) *	2001-06-06	2004-05-04	Hoffmann-La Roche Inc.	Pharmaceutical compositions having depressed melting points
DE10251963A1 (de) *	2002-11-08	2004-05-19	Lts Lohmann Therapie-Systeme Ag	Transmucosale pharmazeutische Darreichungsform
US8372430B2 (en)	2002-12-17	2013-02-12	The Procter & Gamble Company	Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
WO2004078164A1 (fr) *	2003-03-04	2004-09-16	Nostrum Pharmaceuticals, Inc.	Formulation a liberation commandee renfermant une substance hydrophobe comme agent de liberation soutenue
FI20045076L (fi) *	2004-03-15	2005-09-16	Bioferme Oy	Funktionaalinen elintarvike
BRPI0516772A (pt) *	2004-10-25	2008-09-23	Japan Tobacco Inc	formulação sólida com solubilidade e estabilidade melhoradas e método para produção da referida formulação
KR100669497B1 (ko) *	2005-08-17	2007-01-16	보람제약주식회사	안정성과 용출률이 뛰어난 약리학적 조성물 및 그 제조방법
US20070148245A1 (en) *	2005-12-22	2007-06-28	Ilan Zalit	Compressed solid dosage forms with drugs of low solubility and process for making the same
WO2007073389A1 (fr) *	2005-12-22	2007-06-28	Teva Pharmaceutical Industries Ltd.	Formes de dosage solides comprimées comprenant des médicaments de faible solubilité et procédé servant à les fabriquer
EP1808163A1 (fr) *	2005-12-22	2007-07-18	Teva Pharmaceutical Industries Ltd.	Formes galéniques solides comprimées avec des principes actifs de faible solubilité et leur procédé de fabrication
KR101252635B1 (ko)	2006-04-20	2013-04-10	(주)아모레퍼시픽	리파아제 저해제 및 친유성 오일흡수제를 포함하는 약학조성물 및 이로부터 제조된 경구 투여용 제제
KR100903504B1 (ko) *	2007-05-18	2009-06-17	강태용	비라칸사스 열매 추출물질을 포함하는 기능식품 및 체중 감소제
JP2010536798A (ja) *	2007-08-17	2010-12-02	テバファーマシューティカルインダストリーズリミティド	難溶性薬物の生体利用率を制御するための方法及び組成物
ES2350798T3 (es) *	2007-09-12	2011-01-27	Mader S.R.L.	Composiciones farmacéuticas para uso oral para tratar a pacientes afectados por la obesidad.
PL216542B1 (pl)	2008-03-20	2014-04-30	Zakłady Farmaceutyczne POLPHARMA Spółka Akcyjna	Sposób wytwarzania stabilnej kompozycji orlistatu w postaci kapsułkowanego proszku
WO2010042499A1 (fr) *	2008-10-06	2010-04-15	Banner Pharmacaps, Inc.	Solutions stables d'orlistat pour formes galéniques pharmaceutiques
BRPI0901602B8 (pt)	2009-04-03	2021-05-25	Ems S/A	formulação farmacêuticas
UA107369C2 (en)	2010-02-01	2014-12-25	Lab Bago S A	Pharmaceutical composition with anti-obesity activity comprising a premixture of pure orlistat and preparation process
EP2486805A1 (fr) *	2011-02-11	2012-08-15	Puratos N.V.	Émulsion à fouettement à température ambiante
WO2012140937A1 (fr) *	2011-04-14	2012-10-18	株式会社Ｊ－オイルミルズ	Huile de palme fractionnée, composition d'huile et produit alimentaire la contenant
CN102552168B (zh) *	2012-01-31	2013-08-07	杭州华东医药集团生物工程研究所有限公司	一种含有奥利司他的药物组合物及其制备方法
GB2501535A (en)	2012-04-26	2013-10-30	Sony Corp	Chrominance Processing in High Efficiency Video Codecs
EP2854763B1 (fr) *	2012-05-31	2018-09-26	Repros Therapeutics Inc.	Formulations d'administration vaginale d'antiprogestines
WO2015063039A1 (fr)	2013-10-28	2015-05-07	Nestec S.A.	Monoacylglycérols destinés à être utilisés conjointement avec un inhibiteur de lipases et/ou des régimes faibles en matières grasses et/ou calories
CN115105476B (zh) *	2021-03-23	2023-11-14	山东新时代药业有限公司	一种奥利司他冻干口服制剂及其制备工艺

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CA1247547A (fr) *	1983-06-22	1988-12-28	Paul Hadvary	Derives de leucine
FR2710264B1 (fr) *	1993-09-21	1995-12-08	Rocher Yves Biolog Vegetale	Utilisation pour le traitement des peaux mixtes d'une quantité efficace de substances actives.
AU5185398A (en) *	1996-12-04	1998-06-29	James S Pincott	Process and apparatus for making crumb rubber from scrap tyres
BR9807655A (pt)	1997-02-05	2000-02-15	Hoffmann La Roche	Uso de inibidores de lipase gastrintestinal.
US6004996A (en) *	1997-02-05	1999-12-21	Hoffman-La Roche Inc.	Tetrahydrolipstatin containing compositions
US6267952B1 (en)	1998-01-09	2001-07-31	Geltex Pharmaceuticals, Inc.	Lipase inhibiting polymers
BR9912980B1 (pt)	1998-08-14	2013-10-22		Composição farmacêutica administrável oralmente, tablete de mascar contendo a mesma e utilização da mesma
DE69916288T2 (de) *	1998-08-14	2005-03-24	F. Hoffmann-La Roche Ag	Lipasehemmer und chitosan enthaltende arzneimittel
AR025609A1 (es) *	1999-09-13	2002-12-04	Hoffmann La Roche	Formulaciones lipidas solidas

2000
- 2000-09-08 AR ARP000104722A patent/AR025609A1/es active IP Right Grant
- 2000-09-11 TR TR2002/00605T patent/TR200200605T2/xx unknown
- 2000-09-11 JP JP2001523010A patent/JP4217017B2/ja not_active Expired - Lifetime
- 2000-09-11 AU AU75177/00A patent/AU769016B2/en not_active Expired
- 2000-09-11 AT AT00964158T patent/ATE285783T1/de active
- 2000-09-11 BR BRPI0013940A patent/BRPI0013940B1/pt not_active IP Right Cessation
- 2000-09-11 SI SI200030589T patent/SI1216048T1/xx unknown
- 2000-09-11 EP EP00964158A patent/EP1216048B1/fr not_active Expired - Lifetime
- 2000-09-11 JO JO2000156A patent/JO2300B1/en active
- 2000-09-11 NZ NZ517396A patent/NZ517396A/en not_active IP Right Cessation
- 2000-09-11 MY MYPI20004207 patent/MY127430A/en unknown
- 2000-09-11 HU HU0202762A patent/HU229037B1/hu unknown
- 2000-09-11 RU RU2002107450/15A patent/RU2248218C2/ru active
- 2000-09-11 PT PT00964158T patent/PT1216048E/pt unknown
- 2000-09-11 CZ CZ20021277A patent/CZ301844B6/cs not_active IP Right Cessation
- 2000-09-11 CA CA002383036A patent/CA2383036C/fr not_active Expired - Lifetime
- 2000-09-11 HR HR20020206A patent/HRP20020206B1/xx not_active IP Right Cessation
- 2000-09-11 HK HK03101988.9A patent/HK1049798B/zh not_active IP Right Cessation
- 2000-09-11 MX MXPA02002662A patent/MXPA02002662A/es active IP Right Grant
- 2000-09-11 WO PCT/EP2000/008857 patent/WO2001019378A2/fr not_active Ceased
- 2000-09-11 PL PL356154A patent/PL199869B1/pl unknown
- 2000-09-11 KR KR10-2002-7003247A patent/KR100523879B1/ko not_active Expired - Lifetime
- 2000-09-11 RS YUP-136/02A patent/RS50373B/sr unknown
- 2000-09-11 ME MEP-2008-909A patent/ME00675B/fr unknown
- 2000-09-11 CN CNB008126798A patent/CN1197554C/zh not_active Expired - Lifetime
- 2000-09-11 ES ES00964158T patent/ES2233444T3/es not_active Expired - Lifetime
- 2000-09-11 DE DE60017156T patent/DE60017156T2/de not_active Expired - Lifetime
- 2000-09-11 IL IL14857000A patent/IL148570A0/xx active IP Right Grant
- 2000-09-12 EG EG20001160A patent/EG24225A/xx active
- 2000-09-12 CO CO00068855A patent/CO5210857A1/es active IP Right Grant
- 2000-09-13 PE PE2000000950A patent/PE20010661A1/es not_active IP Right Cessation
- 2000-09-13 GC GCP2000906 patent/GC0000259A/en active
- 2000-09-13 US US09/660,700 patent/US6703369B1/en not_active Expired - Lifetime
2002
- 2002-02-13 ZA ZA200201249A patent/ZA200201249B/en unknown
- 2002-03-07 IL IL148570A patent/IL148570A/en unknown
- 2002-03-11 MA MA26544A patent/MA26817A1/fr unknown
- 2002-03-12 NO NO20021205A patent/NO328889B1/no not_active IP Right Cessation

Also Published As

Publication number	Publication date
KR100523879B1 (ko)	2005-10-26
TR200200605T2 (tr)	2002-08-21
JO2300B1 (en)	2005-09-12
RS50373B (sr)	2009-11-10
ES2233444T3 (es)	2005-06-16
ATE285783T1 (de)	2005-01-15
HU229037B1 (en)	2013-07-29
CN1373659A (zh)	2002-10-09
AR025609A1 (es)	2002-12-04
PE20010661A1 (es)	2001-06-25
JP4217017B2 (ja)	2009-01-28
HUP0202762A2 (hu)	2003-01-28
BR0013940A (pt)	2002-05-14
KR20020060177A (ko)	2002-07-16
CO5210857A1 (es)	2002-10-30
GC0000259A (en)	2006-11-01
CN1197554C (zh)	2005-04-20
IL148570A (en)	2007-03-08
MXPA02002662A (es)	2002-07-30
PT1216048E (pt)	2005-04-29
MEP90908A (en)	2011-12-20
HRP20020206B1 (en)	2011-02-28
AU7517700A (en)	2001-04-17
HK1049798B (zh)	2005-08-05
WO2001019378A2 (fr)	2001-03-22
MY127430A (en)	2006-11-30
RU2248218C2 (ru)	2005-03-20
CA2383036A1 (fr)	2001-03-22
AU769016B2 (en)	2004-01-15
DE60017156T2 (de)	2006-01-05
CA2383036C (fr)	2006-01-10
HK1049798A1 (en)	2003-05-30
EG24225A (en)	2008-11-10
MA26817A1 (fr)	2004-12-20
HUP0202762A3 (en)	2005-04-28
NZ517396A (en)	2003-10-31
IL148570A0 (en)	2002-09-12
WO2001019378A3 (fr)	2001-05-10
US6703369B1 (en)	2004-03-09
CZ20021277A3 (cs)	2003-04-16
EP1216048A2 (fr)	2002-06-26
PL356154A1 (en)	2004-06-14
DE60017156D1 (de)	2005-02-03
NO20021205L (no)	2002-03-12
BRPI0013940B1 (pt)	2016-06-21
RU2002107450A (ru)	2004-01-10
YU13602A (sh)	2006-01-16
SI1216048T1 (en)	2005-06-30
PL199869B1 (pl)	2008-11-28
CZ301844B6 (cs)	2010-07-07
JP2003509373A (ja)	2003-03-11
EP1216048B1 (fr)	2004-12-29
HRP20020206A2 (en)	2004-04-30
ZA200201249B (en)	2003-07-30
NO20021205D0 (no)	2002-03-12
ME00675B (fr)	2011-12-20

Legal Events

Date	Code	Title	Description
2020-04-27	MM1K	Lapsed by not paying the annual fees

Publication	Publication Date	Title
AU769016B2 (en)	2004-01-15	Solid lipid formulations comprising an inhibitor of lipases and a fatty acid ester of polyols
JP4217016B2 (ja)	2009-01-28	リパーゼ阻害剤を含有する分散処方物
JP2009108076A (ja)	2009-05-21	リパーゼ阻害剤とショ糖脂肪酸エステルとを含む医薬組成物
AU2002257817A1 (en)	2003-05-08	Pharmaceutical composition comprising a lipase inhibitor and a sucrose fatty acid ester
HK1067312B (en)	2010-08-06	Pharmaceutical composition comprising a lipase inhibitor and a sucrose fatty acid ester