WO2013109206A1 - Formulations en comprimés comprenant du céfuroxime - Google Patents

Formulations en comprimés comprenant du céfuroxime Download PDF

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Publication number
WO2013109206A1
WO2013109206A1 PCT/TR2013/000018 TR2013000018W WO2013109206A1 WO 2013109206 A1 WO2013109206 A1 WO 2013109206A1 TR 2013000018 W TR2013000018 W TR 2013000018W WO 2013109206 A1 WO2013109206 A1 WO 2013109206A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
cefuroxime
tablet formulation
pharmaceutical
formulation according
Prior art date
Application number
PCT/TR2013/000018
Other languages
English (en)
Inventor
Mahmut Bilgic
Original Assignee
Mahmut Bilgic
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 Mahmut Bilgic filed Critical Mahmut Bilgic
Publication of WO2013109206A1 publication Critical patent/WO2013109206A1/fr

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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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
    • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Definitions

  • the present invention relates to pharmaceutical tablet formulations comprising cefuroxime to be used in the treatment of upper respiratory tract infections such as otorhinolaryngological infections, otitis media, sinusitis, tonsillitis, pharyngitis; lower respiratory tract infections such as cystitis and urethritis; and skin and soft tissue infections such as furuncle, pyoderma, impetigo; gonorrhea and lyme diseases caused by gram positive and gram negative bacteria.
  • upper respiratory tract infections such as otorhinolaryngological infections, otitis media, sinusitis, tonsillitis, pharyngitis
  • lower respiratory tract infections such as cystitis and urethritis
  • skin and soft tissue infections such as furuncle, pyoderma, impetigo; gonorrhea and lyme diseases caused by gram positive and gram negative bacteria.
  • Cefuroxime was first disclosed with the patent application numbered US3974153.
  • cefuroxime was indicated to be effective in use for upper respiratory tract infections such as otorhinolaryngological infections, otitis media, sinusitis, tonsillitis, pharyngitis; lower respiratory tract infections such as cystitis and urethritis; and skin and soft tissue infections such as furuncle, pyoderma, impetigo; in the treatment of gonorrhea and lyme diseases caused by gram positive and gram negative bacteria.
  • Cefuroxime physically appears in the forms of suspension and 100-5000 mg tablets on the market.
  • physical properties of dosage form for every type of tablet dosage form are directly related to durability in storage conditions; dissolution and bioavailability of the dosage form obtained.
  • Tablet hardness is an important physical parameter in pharmaceutical tablet formulations and is related to resistance of tablets to storage, transport, coating and erosion-breakage before usage. Tablets with low hardness are more exposed to erosion, friability or breakage and this case leads;
  • Tablets that are too hard do not disperse or dissolve adequately; in this case, bioavailability of said dosage forms will decrease and therefore the time for desired biological response to occur will extend.
  • bioavailability of said dosage forms will decrease and therefore the time for desired biological response to occur will extend.
  • all types of tablets such as effervescent, film-coated, soluble, extended-release, modified-release, delayed-release tablets etc.
  • Attaining appropriate tablet hardness is influenced by many parameters such as the types of active agents and excipients used, particle sizes thereof, flowability of the powder or granules prepared for tablet compressing and tablet compression force.
  • hardness value of tablets are aimed to be so low as to quickly disintegrate in the stomach but so high as to preserve tablet uniformity during packaging, carrying and storing phases from the time of production until used by patient.
  • tablet formulations of the present invention comprise cefuroxime as active agent and at least one pharmaceutically acceptable excipient, and the value of tablet hardness is between 3 kP and 50 kP.
  • tablet formulations of the present invention comprise cefuroxime as active agent and at least one pharmaceutically acceptable excipient, and the value of tablet hardness is between 4 kP and 40 kP.
  • tablet formulations comprise cefuroxime as active agent and at least one pharmaceutically acceptable excipient, and the value of tablet hardness is between 5 kP and 30 kP.
  • tablette refers to tablet types such as tablet, effervescent tablet, film-coated tablet, enteric-coated tablet, orodispersible tablet, water-soluble tablet, extended-release tablet, modified-release tablet, delayed-release tablet.
  • Cefuroxime comprised in the pharmaceutical formulations of the present invention can be in the form of its pharmaceutically acceptable salts, hydrates, solvates, esters, enantiomers, diastereomers or combinations thereof in terms of chemical structure; and in crystalline, amorphous forms or combinations thereof in terms of polymorphic structure.
  • the active agent cefuroxime is preferably in the form of cefuroxime axetil.
  • the pharmaceutical formulations of the present invention comprise at least one pharmaceutically acceptable excipient selected from the group comprising disintegrant, diluent, lubricant, glidant, binder, effervescent couple composed of at least one effervescent acid and at least one effervescent base, coloring agent, pH regulating agent, surfactant, stabilizing agent, sweetener and/or taste regulating agent, flavoring agent.
  • the diluent that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising calcium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, microcrystalline cellulose, dextrose, fructose, lactitol, lactose, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, mannitol, simethicone, sorbitol, starch, sodium chloride, sucrose, talc, xylitol or combinations thereof.
  • the lubricant that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising calcium stearate, magnesium stearate, polythylene glycol, sodium benzoate, potassium benzoate, sodium lauryl sulphate, talc, stearic acid, zinc stearate or combinations thereof.
  • the glidant that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising tribasic calcium phosphate, colloidal silicon dioxide, magnesium silicate, magnesium trisilicate, talc or combinations thereof.
  • the binder that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising carboxymethyl cellulose sodium, ethyl cellulose, gelatin, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hypromellose, magnesium aluminum silicate, maltodextrin, methyl cellulose, povidone, starch or combinations thereof.
  • the effervescent acids that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising organic acids such as malic acid, citric acid, tartaric acid, fumaric acid; and said effervescent bases can selected from a group comprising agents such as sodium carbonate, potassium carbonate, sodium hydrogen carbonate, potassium hydrogen carbonate or combinations thereof.
  • the pH regulating agent that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising citrate, phosphate, carbonate, tartrate, fumarate, acetate and amino acid salts or combinations thereof.
  • the surfactant that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising sodium lauryl sulphate, polysorbate, polyoxyethylene, polyoxypropylene glycol or combinations thereof.
  • the sweetener and/or the taste regulating agent that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising acesulfame, aspartame, dextrose, fructose, maltitol, maltose, mannitol, saccharine, saccharine sodium, sodium cyclamate, sorbitol, sucralose, sucrose, xylitol, sodium chloride or combinations thereof.
  • the flavoring agent that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising flavors such as menthol, lemon, orange, vanilla, strawberry, raspberry, caramel, and the like or combinations thereof.
  • the solvents that can be used in the pharmaceutical formulations of the invention can be selected from a group comprising ethyl alcohol, methyl alcohol, propyl alcohol, benzene, toluene, acetone, deionized water or combinations thereof.
  • the pharmaceutical formulations of the invention comprising cefuroxime as active agent comprise cefuroxime in the range of 0.1-99.9%, preferably in the range of 1-99%, more preferably in the range of 5-95% by weight.
  • the pharmaceutical formulations of the invention comprising cefuroxime as active agent can optionally comprise a second active agent in addition to cefuroxime.
  • the second active agent can be selected from a group comprising antacid, anticholinergic, antispazmodic, antiemetic, antidiabetic, antipropulsive, antiallergic, antidiarrheal, antiobesity, antithrombotic, antifibrinolytic, antianemic, antihypertensive, antifungal, antipruritic, antipsoriatic, antibiotic, antiseptic, antiacne, antibacterial, antimycotic, antiviral, antineoplastic, antiarithmic, antiadrenergic, antiepileptic, anti-parkinson, antiprotozoal, anthelmintic, anti-inflammatory, diuretic, laxative, sulphonamide, imidazole, corticosteroid, tiazolidinedione, biguanide, immunostimulant, immuno
  • Said tablet formulations can optionally be treated with film-coating agents, for instance sugar- based coating agents, water-soluble film-coating agents, enteric coating agents, coating agents prepared to provide various release properties (such as fast release, slow release, controlled release) or coating compositions comprising any combination thereof.
  • film-coating agents for instance sugar- based coating agents, water-soluble film-coating agents, enteric coating agents, coating agents prepared to provide various release properties (such as fast release, slow release, controlled release) or coating compositions comprising any combination thereof.
  • saccharose can be used on its own or optionally with any of the agents such as talc, calcium carbonate, calcium phosphate, calcium sulphate, gelatin, gum arabic, polyvinylpyrrolidone and pullulan or any combination thereof.
  • the water-soluble film-coating agents can be selected from cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose; synthetic polymers such as polyvinyl acetal diethyl aminoacetate, aminoalkyl methacrylate copolymers and polyvinylpyrrolidone and polysaccharides such as pullulan; or combinations thereof.
  • the enteric coating agents can be selected from cellulose derivatives such as hydroxypropyl methyl cellulose phthalate, hydroxypropyl methyl cellulose acetate succinate, carboxymethyl ethyl cellulose, cellulose acetate phthalate; acrylic acid derivatives such as methacrylic acid copolymer L, methacrylic acid copolymer LD and methacrylic acid copolymer S; and natural substances such as shellac; or combinations thereof.
  • cellulose derivatives such as hydroxypropyl methyl cellulose phthalate, hydroxypropyl methyl cellulose acetate succinate, carboxymethyl ethyl cellulose, cellulose acetate phthalate
  • acrylic acid derivatives such as methacrylic acid copolymer L, methacrylic acid copolymer LD and methacrylic acid copolymer S
  • natural substances such as shellac; or combinations thereof.
  • release rate determining polymers that can be comprised in coating composition or pharmaceutical tablet composition can be selected from a group comprising pH dependent polymers, pH independent polymers, swellable polymers, non-swellable polymers, hydrophilic polymers, hydrophobic polymers, and/or one or more hydrophobic substances, sodium alginate, polyactides, polyglycolides, polyactide-co-glycolides, polyactic acids, polyglycolic acids, polyactic acid-co-glycolic acids, polycaprolactone, polycarbonates, polyesteramides, polyanhydrides, polyamino acids, polyorthoesters, polyacetyls, polycyanoacrylates, polyetheresters, polydioxanones, polyalkylene alkylates, polyethylene glycol and polyorthoester copolymers, biodegradable polyurethanes, hydrogels, mixture
  • the preparation method of the formulations of the invention comprises formulating the active agent with an appropriate excipient composition and compressing said formulation in the form of tablets under an appropriate compression force.
  • a characteristic of the tablet formulations of the present invention is that said tablet formulations comprise cefuroxime as active agent, at least one pharmaceutically acceptable excipient and the tablet compression force used for compressing said formulations in the form of tablets is between 3 kN and 50 kN.
  • a characteristic feature of the tablet formulations of the present invention is that said tablet formulations comprise cefuroxime as active agent, at least one pharmaceutically acceptable excipient and the tablet compression force used for compressing said formulations in the form of tablets is between 4 kN and 45 kN.
  • tablet formulations of the present invention comprise cefuroxime as active agent, at least one pharmaceutically acceptable excipient and the tablet compression power used for compressing said formulations in the form of tablets is between 5 kN and 40 kN.
  • the tablet formulations of the invention can be produced in accordance with any of the production methods given below;
  • cefuroxime as active agent with, if present, the second active agent homogenously and, when necessary, adding at least one of the excipients stated above, treating the mixture optionally with at least one pharmaceutically acceptable lubricant, compressing this mixture in the form of tablets under an appropriate compression force according to the invention
  • the production can be made through a method composed of using any of said methods above separately for active agent compositions and combining the obtained formulations together.
  • the pharmaceutical composition of the invention can be used for upper respiratory tract infections such as otorhinolaryngological infections, otitis media, sinusitis, tonsillitis, pharyngitis; lower respiratory tract infections such as pyelonephritis, cystitis and urethritis; skin and soft tissue infections such as furuncle, pyoderma, impetigo; in the prophylaxis and treatment of gonorrhea and lyme diseases caused by gram positive and gram negative bacteria.
  • upper respiratory tract infections such as otorhinolaryngological infections, otitis media, sinusitis, tonsillitis, pharyngitis
  • lower respiratory tract infections such as pyelonephritis, cystitis and urethritis
  • skin and soft tissue infections such as furuncle, pyoderma, impetigo
  • skin and soft tissue infections such as furuncle, pyoderma, impetigo

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne des formulations pharmaceutiques en comprimés comprenant du céfuroxime, utilisables dans le traitement des infections des voies respiratoires supérieures telles que les infections otorhinolaryngologiques, l'otite moyenne, la sinusite, l'amygdalite, la pharyngite; dans le traitement des infections des voies respiratoires inférieures telles que la cystite et l'urétrite; des infections cutanées et des tissus mous telles que le furoncle, la pyodermite, l'impétigo. Ces formulations sont également utilisables dans le traitement de la gonorrhée et des maladies de Lyme provoquées par des bactéries gram positif et gram négatif.S
PCT/TR2013/000018 2012-01-18 2013-01-16 Formulations en comprimés comprenant du céfuroxime WO2013109206A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR201200595 2012-01-18
TR2012/00595 2012-01-18

Publications (1)

Publication Number Publication Date
WO2013109206A1 true WO2013109206A1 (fr) 2013-07-25

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Application Number Title Priority Date Filing Date
PCT/TR2013/000018 WO2013109206A1 (fr) 2012-01-18 2013-01-16 Formulations en comprimés comprenant du céfuroxime
PCT/TR2013/000039 WO2013109226A1 (fr) 2012-01-18 2013-01-18 Formulations pharmaceutiques en comprimés comprenant du céfuroxime

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Application Number Title Priority Date Filing Date
PCT/TR2013/000039 WO2013109226A1 (fr) 2012-01-18 2013-01-18 Formulations pharmaceutiques en comprimés comprenant du céfuroxime

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103505434A (zh) * 2013-09-16 2014-01-15 江苏正大清江制药有限公司 一种头孢呋辛酯片及其制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974153A (en) 1971-05-14 1976-08-10 Glaxo Laboratories Limited 7-Hydrocarbonoxy imino-acetamido-3-carbamoyloxy methylceph-3-em-4 carboxylic acids
EP1342470A1 (fr) * 2002-03-04 2003-09-10 Pharmathen S.A. Compositions à libération rapide de Cefuroxime Axetil
WO2005018618A1 (fr) * 2003-08-23 2005-03-03 Korea United Pharm, Inc Preparation d'un comprime stable a l'absorption de l'humidite et a dissolution rapide contenant du cefuroxime axetil et procede de fabrication correspondant
US20050079213A1 (en) * 2003-06-06 2005-04-14 Unilab Pharmatech Ltd Pharmaceutical compositions
EP2510922A1 (fr) * 2011-04-14 2012-10-17 Sanovel Ilaç Sanayi Ve Ticaret Anonim Sirketi Procès de manufacture pour des comprimés comprenant de céfuroxime

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8900637B2 (en) * 2005-12-02 2014-12-02 Lupin Limited Stable taste masked formulations of cephalosporins

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974153A (en) 1971-05-14 1976-08-10 Glaxo Laboratories Limited 7-Hydrocarbonoxy imino-acetamido-3-carbamoyloxy methylceph-3-em-4 carboxylic acids
EP1342470A1 (fr) * 2002-03-04 2003-09-10 Pharmathen S.A. Compositions à libération rapide de Cefuroxime Axetil
US20050079213A1 (en) * 2003-06-06 2005-04-14 Unilab Pharmatech Ltd Pharmaceutical compositions
WO2005018618A1 (fr) * 2003-08-23 2005-03-03 Korea United Pharm, Inc Preparation d'un comprime stable a l'absorption de l'humidite et a dissolution rapide contenant du cefuroxime axetil et procede de fabrication correspondant
EP2510922A1 (fr) * 2011-04-14 2012-10-17 Sanovel Ilaç Sanayi Ve Ticaret Anonim Sirketi Procès de manufacture pour des comprimés comprenant de céfuroxime

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Publication number Publication date
WO2013109226A1 (fr) 2013-07-25

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