EP2120880A2 - Pellets mit magensaftresistenter wirkstoff-matrix - Google Patents

Pellets mit magensaftresistenter wirkstoff-matrix

Info

Publication number
EP2120880A2
EP2120880A2 EP08701298A EP08701298A EP2120880A2 EP 2120880 A2 EP2120880 A2 EP 2120880A2 EP 08701298 A EP08701298 A EP 08701298A EP 08701298 A EP08701298 A EP 08701298A EP 2120880 A2 EP2120880 A2 EP 2120880A2
Authority
EP
European Patent Office
Prior art keywords
acid
polymer
pellets
pellets according
acrylate
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.)
Ceased
Application number
EP08701298A
Other languages
German (de)
English (en)
French (fr)
Inventor
Andreas Gryczke
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.)
Evonik Roehm GmbH
Original Assignee
Evonik Roehm GmbH
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.)
Filing date
Publication date
Application filed by Evonik Roehm GmbH filed Critical Evonik Roehm GmbH
Publication of EP2120880A2 publication Critical patent/EP2120880A2/de
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Definitions

  • the invention is drug forms with gastric juice-resistant coatings, as z. B. from WO 01/68058 are known.
  • the dosage form described in WO 01/68058 is expensive to manufacture because of its layer structure. It should be provided enteric drug forms or their precursors, which are provided easier and less expensive to produce technical alternative.
  • the water-insoluble polymer may be a mixture of Eudragit® RS and Eudragit® RL type polymers in a 20 to 1 to 1 to 20 ratio.
  • a (meth) acrylate monomer having an anionic group may e.g. As acrylic acid, but preferably be methacrylic acid. Also suitable are anionic (meth) acrylate copolymers of 40 to 60, wt .-% methacrylic acid and 60 to 40 wt .-% methyl methacrylate or 60 to 40 wt .-% ethyl acrylate (types EUDRAGIT® L or EUDRAGIT® L100-55).
  • the glass transition temperature of the copolymers (measurement without addition of plasticizer at a residual monomer content (REMO) of less than 100 ppm, heating rate 10 ° C / min, nitrogen atmosphere) according to ISO 11357-2, point 3.3.3 (T mg ), at most 60, preferably 40 to 60, particularly preferably 45 to 55 0 C.
  • REMO residual monomer content
  • Example V1 contain the water-insoluble polymer Eudragit® RS and no water-soluble polymer.
  • the formulation shows a delayed release of active ingredient, but is not enteric, since after 120 min at pH 1.2, already 19.8% of the initially contained active ingredient are released.

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
EP08701298A 2007-02-22 2008-01-08 Pellets mit magensaftresistenter wirkstoff-matrix Ceased EP2120880A2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102007009242A DE102007009242A1 (de) 2007-02-22 2007-02-22 Pellets mit magensaftresistenter Wirkstoff-Matix
PCT/EP2008/050124 WO2008101743A2 (de) 2007-02-22 2008-01-08 Pellets mit magensaftresistenter wirkstoff-matrix

Publications (1)

Publication Number Publication Date
EP2120880A2 true EP2120880A2 (de) 2009-11-25

Family

ID=39687953

Family Applications (1)

Application Number Title Priority Date Filing Date
EP08701298A Ceased EP2120880A2 (de) 2007-02-22 2008-01-08 Pellets mit magensaftresistenter wirkstoff-matrix

Country Status (12)

Country Link
US (1) US8216613B2 (ja)
EP (1) EP2120880A2 (ja)
JP (1) JP2010519236A (ja)
KR (1) KR101500769B1 (ja)
CN (2) CN101610755A (ja)
BR (1) BRPI0807569A8 (ja)
CA (1) CA2679010C (ja)
DE (1) DE102007009242A1 (ja)
HK (1) HK1205684A1 (ja)
IL (1) IL199637B (ja)
MX (1) MX2009008952A (ja)
WO (1) WO2008101743A2 (ja)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8476425B1 (en) 2012-09-27 2013-07-02 Cubist Pharmaceuticals, Inc. Tazobactam arginine compositions
US8809314B1 (en) 2012-09-07 2014-08-19 Cubist Pharmacueticals, Inc. Cephalosporin compound
US9724353B2 (en) 2011-09-09 2017-08-08 Merck Sharp & Dohme Corp. Methods for treating intrapulmonary infections

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CA2359812C (en) 2000-11-20 2004-02-10 The Procter & Gamble Company Pharmaceutical dosage form with multiple coatings for reduced impact of coating fractures
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
US8377952B2 (en) 2003-08-28 2013-02-19 Abbott Laboratories Solid pharmaceutical dosage formulation
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GEP20135845B (en) * 2008-03-11 2013-06-10 Takeda Pharmaceutical Orally-disintegrating solid formulation
CA2729015A1 (en) * 2008-06-26 2009-12-30 Mcneil-Ppc, Inc. Coated particles containing pharmaceutically active agents
MX2011001864A (es) 2008-08-20 2011-06-20 Univ Texas Extrusion de fusion en caliente de multiples particulas de liberacion modificada.
KR20110103987A (ko) * 2008-12-01 2011-09-21 인베이스크 테라퓨틱, 인크. 레닌-안지오텐신 알도스테론계 억제제 및 리포산 화합물을 포함하는 조성물, 및 레닌-안지오텐신 알도스테론계 관련 질환의 치료를 위한 이의 용도
MX2011009548A (es) 2009-03-13 2011-12-14 Da Volterra Composiciones y metodos para la eliminacion de bacterias gram-negativas.
KR101820374B1 (ko) 2010-02-23 2018-01-19 다 볼떼라 장 내 흡착제의 경구 전달을 위한 제형
CA2850468C (en) 2010-09-28 2019-08-13 Depomed, Inc. Gastric retentive dosage forms for extended release of acamprosate into the upper gastrointestinal tract
US8597683B2 (en) 2010-11-30 2013-12-03 Watson Pharmaceuticals, Inc. Modified release tranexamic acid formulation
MX2014006574A (es) * 2011-12-02 2015-02-10 Synchroneuron Inc Formulaciones de acamprosato, metodos de uso de las mismas, y combinaciones que comprenden las mismas.
US20130143867A1 (en) 2011-12-02 2013-06-06 Sychroneuron Inc. Acamprosate formulations, methods of using the same, and combinations comprising the same
CN102552921B (zh) * 2012-02-28 2013-08-21 南京正科制药有限公司 一种孟鲁司特钠组合物
EP2641592A1 (en) * 2012-03-23 2013-09-25 Salmon Pharma GmbH Pharmaceutical formulation comprising bendamustine
US20140275000A1 (en) 2013-03-15 2014-09-18 Cubist Pharmaceuticals, Inc. Ceftolozane pharmaceutical compositions
US9872906B2 (en) 2013-03-15 2018-01-23 Merck Sharp & Dohme Corp. Ceftolozane antibiotic compositions
MX2020004205A (es) 2013-03-15 2021-11-16 Merck Sharp & Dohme Llc Composiciones antibioticas de ceftolozano.
JP2016520653A (ja) 2013-06-05 2016-07-14 シンクロニューロン インコーポレイテッド アカンプロサート製剤、それを用いる方法、およびそれを含む合剤
CN105491886B (zh) * 2013-08-27 2019-01-29 V·沃道里斯 苯达莫司汀医药组合物
WO2015035376A2 (en) 2013-09-09 2015-03-12 Calixa Therapeutics, Inc. Treating infections with ceftolozane/tazobactam in subjects having impaired renal function
US20150094293A1 (en) 2013-09-27 2015-04-02 Calixa Therapeutics, Inc. Solid forms of ceftolozane
PE20180690A1 (es) 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc Composiciones de acido obeticolico y metodos de uso
BR112017025148A2 (pt) 2015-06-05 2018-08-07 Evonik Röhm Gmbh composição farmacêutica ou nutracêutica com resistência contra a influência do etanol
CN109715156A (zh) 2016-07-14 2019-05-03 尔察祯有限公司 用于治疗细菌感染的头孢布烯和克拉维酸的组合
CN107811994B (zh) * 2016-09-12 2020-09-25 江苏艾立康药业股份有限公司 一种西里帕格pH依赖-时滞型结肠靶向微丸及其制备方法
WO2018087109A1 (de) 2016-11-08 2018-05-17 Grünenthal GmbH Multipartikuläre arzneiform mit kontrollierter freisetzung von metamizol
KR20210042412A (ko) 2018-09-06 2021-04-19 주식회사 이노파마스크린 천식 또는 파킨슨병 치료를 위한 방법 및 조성물
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9724353B2 (en) 2011-09-09 2017-08-08 Merck Sharp & Dohme Corp. Methods for treating intrapulmonary infections
US10028963B2 (en) 2011-09-09 2018-07-24 Merck Sharp & Dohme Corp. Methods for treating intrapulmonary infections
US8809314B1 (en) 2012-09-07 2014-08-19 Cubist Pharmacueticals, Inc. Cephalosporin compound
US8476425B1 (en) 2012-09-27 2013-07-02 Cubist Pharmaceuticals, Inc. Tazobactam arginine compositions
US8685957B1 (en) 2012-09-27 2014-04-01 Cubist Pharmaceuticals, Inc. Tazobactam arginine compositions

Also Published As

Publication number Publication date
WO2008101743A3 (de) 2008-10-09
JP2010519236A (ja) 2010-06-03
CN104490789A (zh) 2015-04-08
US8216613B2 (en) 2012-07-10
IL199637A0 (en) 2010-04-15
US20080206350A1 (en) 2008-08-28
DE102007009242A1 (de) 2008-09-18
HK1205684A1 (en) 2015-12-24
MX2009008952A (es) 2009-08-31
CA2679010A1 (en) 2008-08-28
IL199637B (en) 2018-01-31
KR101500769B1 (ko) 2015-03-17
BRPI0807569A8 (pt) 2022-07-05
CN101610755A (zh) 2009-12-23
KR20090112717A (ko) 2009-10-28
BRPI0807569A2 (pt) 2014-07-01
CA2679010C (en) 2014-09-09
WO2008101743A2 (de) 2008-08-28

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