WO2004087111A1 - Compositions pharmaceutiques orales a gout masque - Google Patents

Compositions pharmaceutiques orales a gout masque Download PDF

Info

Publication number
WO2004087111A1
WO2004087111A1 PCT/IB2004/001036 IB2004001036W WO2004087111A1 WO 2004087111 A1 WO2004087111 A1 WO 2004087111A1 IB 2004001036 W IB2004001036 W IB 2004001036W WO 2004087111 A1 WO2004087111 A1 WO 2004087111A1
Authority
WO
WIPO (PCT)
Prior art keywords
inorganic carrier
film forming
polymeric film
process according
pharmaceutical ingredient
Prior art date
Application number
PCT/IB2004/001036
Other languages
English (en)
Inventor
Harvinder Popli
Pradeep Bhadauria
Sudhir Verma
Original Assignee
Ranbaxy Laboratories 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 Ranbaxy Laboratories Limited filed Critical Ranbaxy Laboratories Limited
Publication of WO2004087111A1 publication Critical patent/WO2004087111A1/fr

Links

Classifications

    • 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
    • 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
    • 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
    • A61K9/20—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
    • A61K9/501—Inorganic compounds

Definitions

  • the present invention relates to oral taste masked pharmaceutical compositions that include a core having an active ingredient coated with a mixture of polymeric film fonning binders and inorganic carriers. Also provided are processes for preparing the oral taste masked pharmaceutical composition.
  • compositions intended for oral use are usually administered either in the form of liquid dosage forms, such as a syrup, suspension, or emulsion, or solid dosage forms, such as a capsule, compressed tablet, granule, etc.
  • liquid dosage forms such as a syrup, suspension, or emulsion
  • solid dosage forms such as a capsule, compressed tablet, granule, etc.
  • U.S. Patent No. 6,197,348 describes a dosage form that utilizes encapsulated particles coated with polymers, such as Eudragit RS and Eudragit RL.
  • Taste masking is achieved as a result of the polymer coatings and a liquid suspending medium having a pH that is adjusted to a point where the active ingredient is insoluble.
  • the thickness and type of coating is not sufficient for taste masking.
  • U.S. Patent No. 6,106,861 discloses a multiparticulate disintegrating tablet which includes excipients and an active ingredient in the form of microcrystals. Only a limited number of active ingredients can be commercially made in the form of microcrystals, and specifically, amorphous powders cannot be utilized in this process.
  • the inorganic carrier may be one or more of calcium carbonate, dibasic calcium phosphate, calcium silicate, magnesium carbonate, magnesium silicate, calcium oxide and magnesium oxide.
  • the inorganic carrier may be present at a concentration ranging from about 1% w/w to about 90% w/w.
  • the ratio of the film forming binder to the inorganic carrier may range from about 10:90 to about 90:10.
  • the ratio of polymeric film forming binder to inorganic carrier may further range from about 40:60 to about 50:50.
  • the taste masking coating may be about 10% w/w to about 100% w/w of the core.
  • Suitable active phannaceutical ingredients include one or more of antiallergic, anti- inflammatory, antibacterial, antiasthmatics, nonsteroidal anti-inflammatory, antiarthritic, antipsychotics, tranquillizers, antidiabetics, antipyretics, antiulcerants, prokinetics, antihypertensives, antianxiety, and nonsteroidal anti-inflammatory active pharmaceutical ingredients and the like.
  • the ratio of the polymeric film forming binder and inorganic carrier may be varied depending on the type of release profile desired.
  • the polymeric film forming binder and inorganic carrier may have a weight ratio in the range of about 10:90 to about 90:10, preferably from about 70:30 to about 30:70, and even more preferably from about 40:60 to about 50:50.
  • the blend of the polymeric film forming binder and inorganic carrier renders the taste masking coating completely insoluble and non-swellable in a neutral pH. This characteristic makes them more suitable for use in an aqueous suspension and overcomes the inconvenience of supplying a special vehicle for reconstitution, such as in an oil.
  • the present inventions specifically make use of the aqueous-based coating systems that are safe and make environmental regulatory compliance (e.g., EPA) relatively easy compared to non-aqueous based coating systems.
  • the neutral methacrylic acid ester copolymers were found especially suitable because of their balanced permeability characteristics and hydophilicity.
  • the coating composition is the same as described above in Example 1.
  • Ciprofloxacin base cores (#40/60) 150 gm
  • Ciprofloxacin for oral suspension Ciprofloxacin for oral suspension
  • Ciprofloxacin base (below # 60) 125 mg
  • Titanium dioxide 10.0 mg
  • the suspension was reconstituted with boiled and cooled water and evaluated for taste and physical changes; the data is depicted in Table 8.
  • Example 1 The cores of Example 1 were used for the controlled release coating of the following composition. Significant sustained effect was achieved at,a coating build up of approximately 60%. Ciprofloxacin base cores 150.0 gm (As per Example 1) Aquacoat ECD 30% 200 gm
  • the active ingredient suspension was layered on the microcrystalline cellulose spheres using a fluidized bed coating. Then the active ingredient-layered microcapsules were further coated with the taste masking coating as described above. Complete taste masking was achieved at approximately 50% to 60% build up. The process used was the same as described above with respect to Example 1.

Abstract

La présente invention se rapporte à des compositions pharmaceutiques orales à goût masqué comportant un noyau composé d'un ingrédient actif enrobé d'un mélange de liants polymères filmogènes et d'excipients inorganiques. On a également prévu des procédés de préparation d'une composition pharmaceutique orale à goût masqué de ce type.
PCT/IB2004/001036 2003-04-04 2004-04-05 Compositions pharmaceutiques orales a gout masque WO2004087111A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN569/DEL/2003 2003-04-04
IN569DE2003 2003-04-04

Publications (1)

Publication Number Publication Date
WO2004087111A1 true WO2004087111A1 (fr) 2004-10-14

Family

ID=33104993

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2004/001036 WO2004087111A1 (fr) 2003-04-04 2004-04-05 Compositions pharmaceutiques orales a gout masque

Country Status (1)

Country Link
WO (1) WO2004087111A1 (fr)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008000040A1 (fr) * 2006-06-30 2008-01-03 Alphapharm Pty Ltd Composition stabilisée comprenant des inhibiteurs de l'eca
WO2011030351A3 (fr) * 2009-09-03 2011-06-30 Rubicon Research Private Limited Compositions pharmaceutiques au goût masqué
WO2011128906A1 (fr) * 2010-04-12 2011-10-20 S. Zhaveri Pharmakem Pvt. Ltd. Composition sèche de ciprofloxacine pour suspension buvable
US8071128B2 (en) 1996-06-14 2011-12-06 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
AU2005307052B2 (en) * 2004-11-12 2012-01-12 Aptalis Pharma Limited Taste-masked multiparticulate pharmaceutical compositions comprising a drug-containing core particle and a solvent-coacervated membrane
US8367111B2 (en) 2002-12-31 2013-02-05 Aptalis Pharmatech, Inc. Extended release dosage forms of propranolol hydrochloride
US8580313B2 (en) 2009-12-02 2013-11-12 Aptalis Pharma Limited Fexofenadine microcapsules and compositions containing them
US8747895B2 (en) 2004-09-13 2014-06-10 Aptalis Pharmatech, Inc. Orally disintegrating tablets of atomoxetine
US9040086B2 (en) 2001-10-04 2015-05-26 Aptalis Pharmatech, Inc. Timed, sustained release systems for propranolol
US9161918B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
WO2016024928A1 (fr) 2014-08-14 2016-02-18 Bi̇ofarma İlaç Sanayi̇ Ve Ti̇caret A.Ş. Formulations de paracétamol au goût masqué
WO2017221268A1 (fr) * 2016-06-21 2017-12-28 Laila Nutraceuticals Formulation masquant le goût de composés naturels amers
US9884014B2 (en) 2004-10-12 2018-02-06 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
EP3248595A4 (fr) * 2015-01-22 2018-07-11 Nipro Corporation Préparation de film
US10471017B2 (en) 2004-10-21 2019-11-12 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
US11179331B1 (en) 2020-04-21 2021-11-23 Cure Pharmaceutcai Holding Corp Oral soluble film containing sildenafil citrate

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670459A (en) * 1984-10-03 1987-06-02 Merrell Dow Pharmaceuticals Inc. Method of alleviating withdrawal symptoms
EP0914823A1 (fr) * 1997-11-06 1999-05-12 Lannacher Heilmittel Ges.m.b.H. Préparation orale à effet retard comprenant Tramadol et son procédé de fabrication
WO2001080829A2 (fr) * 2000-04-20 2001-11-01 Bristol-Myers Squibb Company Composition de revetement masquant le gout
EP1157690A1 (fr) * 2000-05-26 2001-11-28 Pharma Pass LLC Composition pharmaceutique à libération prolongée

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670459A (en) * 1984-10-03 1987-06-02 Merrell Dow Pharmaceuticals Inc. Method of alleviating withdrawal symptoms
EP0914823A1 (fr) * 1997-11-06 1999-05-12 Lannacher Heilmittel Ges.m.b.H. Préparation orale à effet retard comprenant Tramadol et son procédé de fabrication
WO2001080829A2 (fr) * 2000-04-20 2001-11-01 Bristol-Myers Squibb Company Composition de revetement masquant le gout
EP1157690A1 (fr) * 2000-05-26 2001-11-28 Pharma Pass LLC Composition pharmaceutique à libération prolongée

Cited By (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8945618B2 (en) 1996-06-14 2015-02-03 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8071128B2 (en) 1996-06-14 2011-12-06 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8956650B2 (en) 1996-06-14 2015-02-17 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US8357396B2 (en) 1996-06-14 2013-01-22 Kyowa Hakko Kirin Co., Ltd. Intrabuccally rapidly disintegrating tablet and a production method of the tablets
US9358214B2 (en) 2001-10-04 2016-06-07 Adare Pharmaceuticals, Inc. Timed, sustained release systems for propranolol
US9040086B2 (en) 2001-10-04 2015-05-26 Aptalis Pharmatech, Inc. Timed, sustained release systems for propranolol
US8367111B2 (en) 2002-12-31 2013-02-05 Aptalis Pharmatech, Inc. Extended release dosage forms of propranolol hydrochloride
US8747895B2 (en) 2004-09-13 2014-06-10 Aptalis Pharmatech, Inc. Orally disintegrating tablets of atomoxetine
US9884014B2 (en) 2004-10-12 2018-02-06 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US11452689B2 (en) 2004-10-12 2022-09-27 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10568832B2 (en) 2004-10-12 2020-02-25 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10130580B2 (en) 2004-10-12 2018-11-20 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions
US10952971B2 (en) 2004-10-21 2021-03-23 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
US10471017B2 (en) 2004-10-21 2019-11-12 Adare Pharmaceuticals, Inc. Taste-masked pharmaceutical compositions with gastrosoluble pore-formers
AU2005307052B2 (en) * 2004-11-12 2012-01-12 Aptalis Pharma Limited Taste-masked multiparticulate pharmaceutical compositions comprising a drug-containing core particle and a solvent-coacervated membrane
US10500161B2 (en) 2005-05-02 2019-12-10 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9161919B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9566249B2 (en) 2005-05-02 2017-02-14 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9579293B2 (en) 2005-05-02 2017-02-28 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US11147772B2 (en) 2005-05-02 2021-10-19 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US9161918B2 (en) 2005-05-02 2015-10-20 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
US10045946B2 (en) 2005-05-02 2018-08-14 Adare Pharmaceuticals, Inc. Timed, pulsatile release systems
WO2008000040A1 (fr) * 2006-06-30 2008-01-03 Alphapharm Pty Ltd Composition stabilisée comprenant des inhibiteurs de l'eca
WO2011030351A3 (fr) * 2009-09-03 2011-06-30 Rubicon Research Private Limited Compositions pharmaceutiques au goût masqué
US10729682B2 (en) 2009-12-02 2020-08-04 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US10166220B2 (en) 2009-12-02 2019-01-01 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US9233105B2 (en) 2009-12-02 2016-01-12 Adare Pharmaceuticals S.R.L. Fexofenadine microcapsules and compositions containing them
US8580313B2 (en) 2009-12-02 2013-11-12 Aptalis Pharma Limited Fexofenadine microcapsules and compositions containing them
WO2011128906A1 (fr) * 2010-04-12 2011-10-20 S. Zhaveri Pharmakem Pvt. Ltd. Composition sèche de ciprofloxacine pour suspension buvable
WO2016024928A1 (fr) 2014-08-14 2016-02-18 Bi̇ofarma İlaç Sanayi̇ Ve Ti̇caret A.Ş. Formulations de paracétamol au goût masqué
EP3248595A4 (fr) * 2015-01-22 2018-07-11 Nipro Corporation Préparation de film
WO2017221268A1 (fr) * 2016-06-21 2017-12-28 Laila Nutraceuticals Formulation masquant le goût de composés naturels amers
US11576941B2 (en) 2016-06-21 2023-02-14 Laila Nutraceuticals Taste masking formulation for bitter natural compounds
US11179331B1 (en) 2020-04-21 2021-11-23 Cure Pharmaceutcai Holding Corp Oral soluble film containing sildenafil citrate

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