WO2013109228A1 - Formulations comprenant du céfixime utilisé comme agent actif - Google Patents

Formulations comprenant du céfixime utilisé comme agent actif Download PDF

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Publication number
WO2013109228A1
WO2013109228A1 PCT/TR2013/000041 TR2013000041W WO2013109228A1 WO 2013109228 A1 WO2013109228 A1 WO 2013109228A1 TR 2013000041 W TR2013000041 W TR 2013000041W WO 2013109228 A1 WO2013109228 A1 WO 2013109228A1
Authority
WO
WIPO (PCT)
Prior art keywords
tablet
cefixime
tablet formulation
pharmaceutical
formulation according
Prior art date
Application number
PCT/TR2013/000041
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 WO2013109228A1 publication Critical patent/WO2013109228A1/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
    • 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 cefixime to be used in the treatment of infectious diseases caused by gram positive and gram negative bacteria.
  • Cefixime was first disclosed in the patent application numbered EP0030630 (Bl). In said document, cefixime was indicated to be effective in the treatment of infectious diseases caused by gram positive and gram negative bacteria.
  • Cefixime is available in the form of 200 and 400 mg oral tablets or oral suspension on the market.
  • physical properties of the 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.
  • the inventors have found that the most perfect mechanical tablet resistance, the most appropriate dissolution rate and accordingly the highest bioavailability are attained with the tablet formulations that have a tablet hardness value between 3 kP and 50 kP.
  • another characteristic of the tablet formulations of the present invention is that said tablet formulations comprise cefixime as active agent and at least one pharmaceutically acceptable excipient, and the value of tablet hardness is between 3 kP and 50 kP.
  • Another characteristic of the tablet formulations of the present invention is that said tablet formulations comprise cefixime 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 of the present invention comprise cefixime as active agent and at least one pharmaceutically acceptable excipient, and the value of tablet hardness is between 5 kP and 30 kP.
  • tablette used throughout the text 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.
  • the tablet forms to be used in a preferred embodiment of the invention are film tablet, effervescent tablet and/or orodispersible tablet forms.
  • Cefixime 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.
  • Cefixime is preferably in the form of hydrate, more preferably in the form of cefixime trihydrate.
  • the pharmaceutical formulations of the present invention comprise at least one pharmaceutically acceptable excipient selected from a 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.
  • a pharmaceutically acceptable excipient selected from a 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 cefixime as active agent comprise cefixime 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 cefixime as active agent can optionally comprise a second active agent in addition to cefixime.
  • 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, immunosup
  • the pharmaceutical tablet formulations of the invention comprising cefixime as active agent preferably comprise clavulanic acid as an optional second active agent in addition to cefixime.
  • 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.
  • sugar-based coating agent 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.
  • 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
  • a characteristic of the tablet formulations of the present invention is that said tablet formulations comprise cefixime 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 cefixime 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 cefixime 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 5 kN and 40 kN.
  • the tablet formulations of the invention can be produced in accordance with any of the production methods given below;
  • cefixime 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 in the prevention and treatment of the infectious diseases caused by gram positive and gram negative bacteria.

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

Abstract

La présente invention concerne des formulations pharmaceutiques en comprimés comprenant du céfixime, utilisables dans le traitement de maladies infectieuses provoquées par des bactéries gram positif ou gram négatif.
PCT/TR2013/000041 2012-01-18 2013-01-18 Formulations comprenant du céfixime utilisé comme agent actif WO2013109228A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR201200594 2012-01-18
TR2012/00594 2012-01-18

Publications (1)

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WO2013109228A1 true WO2013109228A1 (fr) 2013-07-25

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PCT/TR2013/000042 WO2013109229A1 (fr) 2012-01-18 2013-01-18 Formulations en comprimés comprenant du céfixime utilisé comme agent actif
PCT/TR2013/000041 WO2013109228A1 (fr) 2012-01-18 2013-01-18 Formulations comprenant du céfixime utilisé comme agent actif

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0030630B1 (fr) 1979-11-19 1987-04-01 Fujisawa Pharmaceutical Co., Ltd. Dérivés de l'acide 7-acylamino-3-vinyl céphalosporanique, procédé pour leur préparation, compositions pharmaceutiques les contenant; leurs produits de départ et leur préparation
US20040005361A1 (en) * 2002-07-06 2004-01-08 Sanjeev Khandelwal Pharmaceutical preparations
US20050181051A1 (en) * 2004-02-16 2005-08-18 Sanjeev Khandelwal Synergistic antibacterial formulation and to a method of making the same
CN1803138A (zh) * 2006-01-09 2006-07-19 深圳市制药厂 头孢克肟口腔崩解片及其制备方法
CN1850087A (zh) * 2006-03-07 2006-10-25 中国药科大学 一种含有头孢克肟的泡腾片及制法
CN101606913A (zh) * 2009-07-16 2009-12-23 广州白云山制药股份有限公司广州白云山制药总厂 头孢克肟分散片及其制备方法
WO2011093822A1 (fr) * 2010-01-29 2011-08-04 Mahmut Bilgic Formulations effervescentes comprenant de la céfixime et de l'acide clavulanique comme agents actifs

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0030630B1 (fr) 1979-11-19 1987-04-01 Fujisawa Pharmaceutical Co., Ltd. Dérivés de l'acide 7-acylamino-3-vinyl céphalosporanique, procédé pour leur préparation, compositions pharmaceutiques les contenant; leurs produits de départ et leur préparation
US20040005361A1 (en) * 2002-07-06 2004-01-08 Sanjeev Khandelwal Pharmaceutical preparations
US20050181051A1 (en) * 2004-02-16 2005-08-18 Sanjeev Khandelwal Synergistic antibacterial formulation and to a method of making the same
CN1803138A (zh) * 2006-01-09 2006-07-19 深圳市制药厂 头孢克肟口腔崩解片及其制备方法
CN1850087A (zh) * 2006-03-07 2006-10-25 中国药科大学 一种含有头孢克肟的泡腾片及制法
CN101606913A (zh) * 2009-07-16 2009-12-23 广州白云山制药股份有限公司广州白云山制药总厂 头孢克肟分散片及其制备方法
WO2011093822A1 (fr) * 2010-01-29 2011-08-04 Mahmut Bilgic Formulations effervescentes comprenant de la céfixime et de l'acide clavulanique comme agents actifs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
G. VINOTH KUMAR; K. ANAND BABU, C. RAMASAMY: "Formulation and evaluation of bilayered tablets of cefixime trihydrate and dicloxacillin sodium", INTERNATIONAL JOURNAL OF PHARMTECH RESEARCH, vol. 3, no. 2, April 2011 (2011-04-01), pages 613 - 618, XP002698643, ISSN: 0974-4304 *
SANDIP KUMER MANGAL BHAI PATEL ET AL.: "Formulation, development and evaluation of film coated tablet containing Cefixime and Potassium clavulanate", JOURNAL OF PHARMACY RESEARCH, vol. 4, no. 6, 11 June 2011 (2011-06-11), pages 1861 - 1863, XP002698642, ISSN: 0974-6943 *

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Publication number Publication date
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