AU2001227915A1 - Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration - Google Patents

Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration

Info

Publication number
AU2001227915A1
AU2001227915A1 AU2001227915A AU2791501A AU2001227915A1 AU 2001227915 A1 AU2001227915 A1 AU 2001227915A1 AU 2001227915 A AU2001227915 A AU 2001227915A AU 2791501 A AU2791501 A AU 2791501A AU 2001227915 A1 AU2001227915 A1 AU 2001227915A1
Authority
AU
Australia
Prior art keywords
taste
linezolid
masked
microcapsules
oral administration
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.)
Abandoned
Application number
AU2001227915A
Inventor
Phillip J. Percel
Gopi M. Venkatesh
Krishna S. Vishnupad
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.)
Allergan Pharmaceuticals Holdings Ireland ULC
Original Assignee
Eurand America Inc
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 Eurand America Inc filed Critical Eurand America Inc
Publication of AU2001227915A1 publication Critical patent/AU2001227915A1/en
Abandoned 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K9/0012—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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5%, most preferably less than 3%, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets. The contents of the Linezolid unit dose containers are suspended in an aqueous medium prior to oral administration to pediatric and geriatric patients, who are unwilling and/or find it difficult to swallow Linezolid tablets. In contrast, fast-disintegrating tablets on administration without water rapidly disperse into taste masked granules in the mouth.
AU2001227915A 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration Abandoned AU2001227915A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US17723300P 2000-01-20 2000-01-20
US60177233 2000-01-20
US09506051 2000-02-17
US09/506,051 US6451345B1 (en) 2000-01-20 2000-02-17 Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration
PCT/US2001/001414 WO2001052848A2 (en) 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for oral administration

Publications (1)

Publication Number Publication Date
AU2001227915A1 true AU2001227915A1 (en) 2001-07-31

Family

ID=26873062

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001227915A Abandoned AU2001227915A1 (en) 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration

Country Status (6)

Country Link
US (1) US6451345B1 (en)
EP (1) EP1248616B1 (en)
AT (1) ATE357231T1 (en)
AU (1) AU2001227915A1 (en)
DE (1) DE60127379D1 (en)
WO (1) WO2001052848A2 (en)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2795962B1 (en) * 1999-07-08 2003-05-09 Prographarm Laboratoires PROCESS FOR THE MANUFACTURE OF MASK TASTE COATED GRANULES AND IMMEDIATE RELEASE OF THE ACTIVE INGREDIENT
US20030091634A1 (en) * 2001-09-14 2003-05-15 Pawan Seth Delayed release tablet of venlafaxin
US7488496B2 (en) 2002-03-06 2009-02-10 Christer Rosen Effervescent compositions comprising bisphosphonates and methods related thereto
US20050269722A1 (en) * 2002-07-17 2005-12-08 Stefano De Luigi Brushci Process for the preparation of pharmaceutical microcapsules with enhanced taste-masking and high dissolution rate
US20040013737A1 (en) * 2002-07-19 2004-01-22 Philippe Becourt Taste masked oral composition of telithromycin
DE60234539D1 (en) * 2002-07-19 2010-01-07 Aventis Pharma Sa TASTE-MASKED ORAL PREPARATION OF TELITHROMYCIN
US20040208936A1 (en) * 2002-07-22 2004-10-21 Roland Chorin Novel compositions
US6875784B2 (en) * 2002-10-09 2005-04-05 Pharmacia & Upjohn Company Antimibicrobial [3.1.0.] bicyclic oxazolidinone derivatives
US20040191326A1 (en) * 2003-03-31 2004-09-30 Reo Joseph P. Taste-masking vehicle for coated oxazolidinone particles
US20040265373A1 (en) * 2003-06-27 2004-12-30 David Wynn Soft tablet containing high molecular weight cellulosics
US20040265372A1 (en) * 2003-06-27 2004-12-30 David Wynn Soft tablet containing high molecular weight cellulosics
US7632521B2 (en) * 2003-07-15 2009-12-15 Eurand, Inc. Controlled release potassium chloride tablets
US8168228B2 (en) * 2003-10-17 2012-05-01 Sandoz Ag Antibiotic clarithromycin micropellet compositions
US7387793B2 (en) * 2003-11-14 2008-06-17 Eurand, Inc. Modified release dosage forms of skeletal muscle relaxants
US8545881B2 (en) 2004-04-19 2013-10-01 Eurand Pharmaceuticals, Ltd. Orally disintegrating tablets and methods of manufacture
IS7724A (en) * 2005-03-02 2006-09-03 Actavis Group Composition of tablets with rapid decomposition containing heavy magnesium carbonate
US20070098746A1 (en) * 2005-11-02 2007-05-03 Nichols William M Multi-layered coating technology for taste masking
US20080014257A1 (en) * 2006-07-14 2008-01-17 Par Pharmaceutical, Inc. Oral dosage forms
JP5228359B2 (en) * 2007-04-12 2013-07-03 ニプロ株式会社 Active ingredient particles, process for producing the same and orally disintegrating tablets
FR2918296B1 (en) 2007-07-05 2009-09-18 Oreal CORE / BARK TYPE CAPSULES AND PROCESS FOR PREPARING THE SAME
WO2009102830A1 (en) * 2008-02-13 2009-08-20 Eurand Inc Orally disintegrating tablet compositions of ranitidine and methods of manufacture
WO2010046933A2 (en) 2008-10-22 2010-04-29 Rubicon Research Private Limited Pharmaceutical compositions of taste-masked linezolid
AU2010208240A1 (en) 2009-01-30 2011-09-22 Sunovion Pharmaceuticals Inc Coated tablets of 6-(5-chloro-2-pyridyl) -5-[ (4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6, 7-dihydro-5H-pyrrol o [3,4-b] pyrazine and methods for measuring effectiveness of coating
WO2011080570A2 (en) * 2009-12-29 2011-07-07 Micro Labs Limited Extended release pharmaceutical composition comprising linezolid and process for preparing the same
WO2011160062A2 (en) 2010-06-17 2011-12-22 The Usa As Represented By The Secretary, National Institutes Of Health Compositions and methods for treating inflammatory conditions
BR112013012833A8 (en) * 2010-11-24 2018-01-02 Melinta Subsidiary Corp PHARMACEUTICAL COMPOSITION AND USE OF AN ANTIMICROBIAL OXAZOLIDINONE AGENT
CA2778748A1 (en) * 2011-06-01 2012-12-01 Nitto Denko Corporation Particulate preparation and method for producing the same
WO2012169614A1 (en) 2011-06-10 2012-12-13 ニプロ株式会社 Method for producing orodispersible tablets
WO2013088389A1 (en) * 2011-12-14 2013-06-20 Alembic Pharmaceuticals Limited Linezolid premix
GR1008143B (en) 2013-03-11 2014-03-14 "Φαρματεν Α.Β.Ε.Ε.", Pharmaceutical preparation containing one oxazolidinonic antibacterial factor-preparation method of the same
CN104739788B (en) * 2013-12-27 2018-02-16 桂林南药股份有限公司 A kind of children's Linezolid composition freeze-drying oral disnitegration tablet and preparation method thereof
WO2015130760A1 (en) * 2014-02-25 2015-09-03 Orbis Biosciences, Inc. Taste masking drug formulations
CN105055354B (en) * 2015-09-08 2017-11-21 深圳万乐药业有限公司 A kind of Linezolid piece and preparation method thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4800087A (en) 1986-11-24 1989-01-24 Mehta Atul M Taste-masked pharmaceutical compositions
US4948801A (en) 1988-07-29 1990-08-14 E. I. Du Pont De Nemours And Company Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents
US5084278A (en) * 1989-06-02 1992-01-28 Nortec Development Associates, Inc. Taste-masked pharmaceutical compositions
US5082669A (en) 1989-07-20 1992-01-21 Dainippon Pharmaceutical Co., Ltd. Rapid-releasing oral particle pharmaceutical preparation with unpleasant taste masked
IT1246382B (en) 1990-04-17 1994-11-18 Eurand Int METHOD FOR THE TARGETED AND CONTROLLED DELIVERY OF DRUGS IN THE INTESTINE AND PARTICULARLY IN THE COLON
US5075114A (en) 1990-05-23 1991-12-24 Mcneil-Ppc, Inc. Taste masking and sustained release coatings for pharmaceuticals
DE69419281T2 (en) * 1993-04-28 2000-03-23 Takeda Chemical Industries Ltd Flavor-masked solid preparation and manufacturing method
US5840332A (en) * 1996-01-18 1998-11-24 Perio Products Ltd. Gastrointestinal drug delivery system
ES2193592T3 (en) 1997-11-18 2003-11-01 Upjohn Co USE OF OXAZOLIDINONE DERIVATIVES FOR THE TREATMENT OF ARTHRITIS.
KR20010015910A (en) 1998-01-23 2001-02-26 로렌스 티. 마이젠헬더 Oxazolidinone Combinatorial Libraries, Compositions and Methods of Preparation

Also Published As

Publication number Publication date
WO2001052848A2 (en) 2001-07-26
US6451345B1 (en) 2002-09-17
EP1248616A2 (en) 2002-10-16
WO2001052848A3 (en) 2001-12-13
ATE357231T1 (en) 2007-04-15
DE60127379D1 (en) 2007-05-03
EP1248616B1 (en) 2007-03-21

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