WO2001052848A3 - Functional coating of linezolid microcapsules for oral administration - Google Patents

Functional coating of linezolid microcapsules for oral administration Download PDF

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Publication number
WO2001052848A3
WO2001052848A3 PCT/US2001/001414 US0101414W WO0152848A3 WO 2001052848 A3 WO2001052848 A3 WO 2001052848A3 US 0101414 W US0101414 W US 0101414W WO 0152848 A3 WO0152848 A3 WO 0152848A3
Authority
WO
WIPO (PCT)
Prior art keywords
linezolid
taste
masked
microcapsules
fast
Prior art date
Application number
PCT/US2001/001414
Other languages
French (fr)
Other versions
WO2001052848A2 (en
Inventor
Phillip J Percel
Gopi M Venkatesh
Krishna S Vishnupad
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
Priority to EP01902073A priority Critical patent/EP1248616B1/en
Priority to DE60127379T priority patent/DE60127379D1/en
Priority to AU2001227915A priority patent/AU2001227915A1/en
Publication of WO2001052848A2 publication Critical patent/WO2001052848A2/en
Publication of WO2001052848A3 publication Critical patent/WO2001052848A3/en

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

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.
PCT/US2001/001414 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for oral administration WO2001052848A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP01902073A EP1248616B1 (en) 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for oral administration
DE60127379T DE60127379D1 (en) 2000-01-20 2001-01-16 FUNCTIONAL COATING OF LINEZOLID MICROPHONES FOR TASTE MASKING AND ASSOCIATED ORAL DRUG PREPARATION
AU2001227915A AU2001227915A1 (en) 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules for taste-masking and associated formulation for oral administration

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US17723300P 2000-01-20 2000-01-20
US60/177,233 2000-01-20
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
US09/506,051 2000-02-17

Publications (2)

Publication Number Publication Date
WO2001052848A2 WO2001052848A2 (en) 2001-07-26
WO2001052848A3 true WO2001052848A3 (en) 2001-12-13

Family

ID=26873062

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/001414 WO2001052848A2 (en) 2000-01-20 2001-01-16 Functional coating of linezolid microcapsules 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)

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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
AU2002368090A1 (en) * 2002-07-17 2004-02-09 Eurand Pharmaceuticals Ltd Process for the preparation of pharmaceutical microcapsules with enhanced tastemasking and high dissolution rate
CA2492874C (en) * 2002-07-19 2011-09-20 Aventis Pharma S.A. Taste masked oral composition of telithromycin
US20040013737A1 (en) * 2002-07-19 2004-01-22 Philippe Becourt Taste masked oral composition 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
US20040265372A1 (en) * 2003-06-27 2004-12-30 David Wynn Soft tablet containing high molecular weight cellulosics
US20040265373A1 (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
TW200938186A (en) * 2008-02-13 2009-09-16 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
CA2750059C (en) 2009-01-30 2014-11-18 Sunovion Pharmaceuticals Inc. Coated tablets of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5h-pyrrolo[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
CA2802994A1 (en) 2010-06-17 2011-12-22 The United States Of America As Represented By The Secretary, National I Nstitutes Of Health Compositions and methods for treating inflammatory conditions
KR101944124B1 (en) * 2010-11-24 2019-01-30 멜린타 서브시디어리 코프. Pharmaceutical compositions
CA2778748A1 (en) * 2011-06-01 2012-12-01 Nitto Denko Corporation Particulate preparation and method for producing the same
EP2719377B1 (en) * 2011-06-10 2018-04-18 Nipro Corporation 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
EP3110403B1 (en) * 2014-02-25 2019-11-06 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

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WO1988003795A1 (en) * 1986-11-24 1988-06-02 Nortec Development Associates, Inc. Taste-masked pharmaceutical compositions
EP0352781A2 (en) * 1988-07-29 1990-01-31 The Du Pont Merck Pharmaceutical Company Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents
US5084278A (en) * 1989-06-02 1992-01-28 Nortec Development Associates, Inc. Taste-masked pharmaceutical compositions
WO1999025344A1 (en) * 1997-11-18 1999-05-27 Pharmacia & Upjohn Company Use of oxazolidinone derivatives for treating psoriasis, arthritis and reducing the toxicity of cancer chemotherapy
WO1999037630A1 (en) * 1998-01-23 1999-07-29 Versicor, Inc. Oxazolidinone combinatorial libraries, compositions and methods of preparation

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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
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Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988003795A1 (en) * 1986-11-24 1988-06-02 Nortec Development Associates, Inc. Taste-masked pharmaceutical compositions
EP0352781A2 (en) * 1988-07-29 1990-01-31 The Du Pont Merck Pharmaceutical Company Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents
US5084278A (en) * 1989-06-02 1992-01-28 Nortec Development Associates, Inc. Taste-masked pharmaceutical compositions
WO1999025344A1 (en) * 1997-11-18 1999-05-27 Pharmacia & Upjohn Company Use of oxazolidinone derivatives for treating psoriasis, arthritis and reducing the toxicity of cancer chemotherapy
WO1999037630A1 (en) * 1998-01-23 1999-07-29 Versicor, Inc. Oxazolidinone combinatorial libraries, compositions and methods of preparation

Also Published As

Publication number Publication date
EP1248616B1 (en) 2007-03-21
US6451345B1 (en) 2002-09-17
EP1248616A2 (en) 2002-10-16
ATE357231T1 (en) 2007-04-15
DE60127379D1 (en) 2007-05-03
AU2001227915A1 (en) 2001-07-31
WO2001052848A2 (en) 2001-07-26

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