WO2010046933A3 - Pharmaceutical compositions of taste-masked linezolid - Google Patents

Pharmaceutical compositions of taste-masked linezolid Download PDF

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Publication number
WO2010046933A3
WO2010046933A3 PCT/IN2009/000597 IN2009000597W WO2010046933A3 WO 2010046933 A3 WO2010046933 A3 WO 2010046933A3 IN 2009000597 W IN2009000597 W IN 2009000597W WO 2010046933 A3 WO2010046933 A3 WO 2010046933A3
Authority
WO
WIPO (PCT)
Prior art keywords
linezolid
taste
masked
pharmaceutical compositions
tablets
Prior art date
Application number
PCT/IN2009/000597
Other languages
French (fr)
Other versions
WO2010046933A2 (en
Inventor
Pratibha Sudhir Pilgaonkar
Maharukh Tehmasp Rustomjee
Anilkumar Surendrakumar Gandhi
Atul A. Kelkar
Original Assignee
Rubicon Research Private Limited
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 Rubicon Research Private Limited filed Critical Rubicon Research Private Limited
Publication of WO2010046933A2 publication Critical patent/WO2010046933A2/en
Publication of WO2010046933A3 publication Critical patent/WO2010046933A3/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
    • A61K9/48—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
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • 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
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • 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
    • A61K9/0087—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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds

Abstract

The present invention relates to a pharmaceutical composition of linezolid for oral administration, comprising taste-masked linezolid and at least one pharmaceutically acceptable excipient. The taste-masked linezolid comprises linezolid and at least one taste-masking agent. The invention further relates to methods for masking the objectionable taste of linezolid by using at least one taste-masking agent and its incorporation into such palatable formulations. The pharmaceutical compositions of taste-masked linezolid are suitable for oral administration as suspensions, powders for suspensions, dispersible tablets, orally disintegrating tablets, chewable tablets, effervescent tablets and the like.
PCT/IN2009/000597 2008-10-22 2009-10-22 Pharmaceutical compositions of taste-masked linezolid WO2010046933A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2277/MUM/2008 2008-10-22
IN2277MU2008 2008-10-22

Publications (2)

Publication Number Publication Date
WO2010046933A2 WO2010046933A2 (en) 2010-04-29
WO2010046933A3 true WO2010046933A3 (en) 2010-07-01

Family

ID=42076966

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000597 WO2010046933A2 (en) 2008-10-22 2009-10-22 Pharmaceutical compositions of taste-masked linezolid

Country Status (1)

Country Link
WO (1) WO2010046933A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2635307T (en) * 2010-11-01 2020-11-03 Melinta Subsidiary Corp Pharmaceutical compositions
CN103099792B (en) * 2012-12-10 2014-11-26 成都欣捷高新技术开发有限公司 Preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving
WO2014118809A1 (en) * 2013-01-29 2014-08-07 Actavis Group Ptc Ehf. Pharmaceutical composition with linezolid
EP2801349A1 (en) 2013-05-06 2014-11-12 Siegfried AG Oral Pharmaceutical Formulation
RU2015156033A (en) * 2013-06-03 2017-07-13 Макнейл Аб A SOLID PHARMACEUTICAL MEDICINAL FOR USE TO RELEASE, AT LEAST, ONE ACTIVE PHARMACEUTICAL INGREDIENT IN THE ORAL CAVITY
CN104622831B (en) * 2013-11-06 2018-06-22 江苏豪森药业集团有限公司 A kind of oral tablet and preparation method thereof
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
CN113995726A (en) * 2021-11-26 2022-02-01 深圳万乐药业有限公司 Linezolid II crystal form tablet and preparation method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0239542A2 (en) * 1986-03-27 1987-09-30 Warner-Lambert Company Medicament adsorbates with complex magnesium aluminum silicate and their preparation
WO2001052848A2 (en) * 2000-01-20 2001-07-26 Eurand Pharmaceuticals Ltd. Functional coating of linezolid microcapsules for oral administration
US20040191326A1 (en) * 2003-03-31 2004-09-30 Reo Joseph P. Taste-masking vehicle for coated oxazolidinone particles

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5688792A (en) 1994-08-16 1997-11-18 Pharmacia & Upjohn Company Substituted oxazine and thiazine oxazolidinone antimicrobials
US6514529B2 (en) 2000-03-22 2003-02-04 Pharmacia & Upjohn Company Oxazolidinone tablet formulation
US20040170686A1 (en) 2003-01-31 2004-09-02 Fredrickson Jennifer K. Suspension vehicle for coated drug particles
US9198862B2 (en) 2005-07-22 2015-12-01 Rubicon Research Private Limited Dispersible tablet composition

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0239542A2 (en) * 1986-03-27 1987-09-30 Warner-Lambert Company Medicament adsorbates with complex magnesium aluminum silicate and their preparation
WO2001052848A2 (en) * 2000-01-20 2001-07-26 Eurand Pharmaceuticals Ltd. Functional coating of linezolid microcapsules for oral administration
US20040191326A1 (en) * 2003-03-31 2004-09-30 Reo Joseph P. Taste-masking vehicle for coated oxazolidinone particles
WO2004087108A1 (en) * 2003-03-31 2004-10-14 Pharmacia Corporation Taste-masking vehicle for coated oxazolidinone particles

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JANNIN V ET AL: "Comparative study of the lubricant performance of Compritol(R) 888 ATO either used by blending or by hot melt coating.", INTERNATIONAL JOURNAL OF PHARMACEUTICS (KIDLINGTON), vol. 262, no. 1-2, 27 August 2003 (2003-08-27), pages 39 - 45, XP002579756, ISSN: 0378-5173 *
MOU-YING FU LU ET AL: "A POLYMER CARRIER SYSTEM FOR TASTE MASKING OF MACROLIDE ANTIBIOTICS", PHARMACEUTICAL RESEARCH, KLUWER ACADEMIC PUBLISHERS, NEW YORK, NY, US LNKD- DOI:10.1023/A:1015889631314, vol. 8, no. 6, 1 June 1991 (1991-06-01), pages 706 - 712, XP000645421, ISSN: 0724-8741 *
NANDA A ET AL: "AN UPDATE ON TASTE MASKING TECHNOLOGIES FOR ORAL PHARMACEUTICALS", JOURNAL OF THE INDIAN CHEMICAL SOCIETY, THE INDIAN CHEMICAL SOCIETY, CALCUTTA; IN, vol. 64, no. 1, 1 January 2002 (2002-01-01), pages 10 - 17, XP008043034, ISSN: 0019-4522 *

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Publication number Publication date
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