EP2833874A1 - Capsule formulations comprising ceftibuten - Google Patents

Capsule formulations comprising ceftibuten

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Publication number
EP2833874A1
EP2833874A1 EP13724914.0A EP13724914A EP2833874A1 EP 2833874 A1 EP2833874 A1 EP 2833874A1 EP 13724914 A EP13724914 A EP 13724914A EP 2833874 A1 EP2833874 A1 EP 2833874A1
Authority
EP
European Patent Office
Prior art keywords
formulation
formulation according
ceftibuten
agent
range
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP13724914.0A
Other languages
German (de)
French (fr)
Inventor
Mahmut Bilgic
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of EP2833874A1 publication Critical patent/EP2833874A1/en
Withdrawn legal-status Critical Current

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular 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
    • A61K9/16—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
    • A61K9/14—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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin

Definitions

  • the present invention relates to pharmaceutical formulations comprising ceftibuten for use in treatment of upper and lower respiratory tract and urinary system infections. Said formulations are characterized in being in capsule form. Ceftibuten was first disclosed in the application numbered US 4634697.
  • ceftibuten is indicated for infections such as abscesses caused by susceptible bacteria, bronchitis, dermatitis, otitis, empyema, enteritis, gastroenteritis, nasopharyngitis, osteomyelitis, pneumonia, pneumonitis, pustulosis, pyelonephritis, respiratory tract infections, rhinitis, septicemia, tonsillitis, ulcer, urinary system infections, wound and soft tissue infections.
  • infections such as abscesses caused by susceptible bacteria, bronchitis, dermatitis, otitis, empyema, enteritis, gastroenteritis, nasopharyngitis, osteomyelitis, pneumonia, pneumonitis, pustulosis, pyelonephritis, respiratory tract infections, rhinitis, septicemia, tonsillitis, ulcer, urinary system infections, wound and soft tissue infections.
  • Ceftibuten is present in 200 and 400 mg tablet forms on the market.
  • ceftibuten is stabile in dihydrate and trihydrate forms. Furtermore, it is also disclosed in said patents that dihydrate and trihydrate forms of ceftibuten can be filled into hard gelatin capsules for oral administration.
  • ceftibuten formulations are formulated in capsule form, low solubility of the capsules in gastro-intestinal liquid in body and difficulties of dissolution of ceftibuten decreases absorption of the medicine and leads to loss of effectiveness of the treatment. Therefore, there is still need for new approaches in order to develop ceftibuten formulations produced in capsule form which can disperse easily and fast in body, have high absorption and bioavailability during oral use.
  • ceftibuten capsule forms which comprise a composition of at least two different pH agents having high water solubility as pH agent wherein the ratio of the first pH agent to the second pH agent composing this composition is in the range of 1 :5 to 5: 1 by weight disperse easily and fast in body and absorption and thus bioavailability of the drug is high.
  • the present invention relates to capsule formulations comprising ceftibuten and is characterized in that said formulations comprise a composition of at least two different pH agents having high solubility in aqueous solutions and the ratio of the first pH agent to the second pH agent composing this composition is in the range of 1 :5 to 5:1 by weight.
  • the ratio of the first pH agent to the second pH agent in the composition comprising at least two different pH agents is preferably in the range of 1 :3 to 5: 1 , more preferably in the range of 1 :2 to 4: 1 by weight.
  • the first and the second pH agents composing the composition comprising at least two different pH agents having high solubility in aqueous solutions to be used in the formulations of the present invention can be selected from a group comprising tribasic calcium phosphate, monosodium glutamate, potassium citrate, trisodium citrate, sodium hydroxide, dibasic sodium phosphate, monobasic sodium phosphate, disodium hydrogen phosphate, sodium bicarbonate or combinations thereof.
  • the first pH agent in the composition comprising at least two different pH agents having high solubility in aqueous solutions that shall be used in the formulations of the present invention can be disodium hydrogen phosphate.
  • the second pH agent in the composition comprising at least two different pH agents having high solubility in aqueous solutions that shall be used in the formulations of the present invention can be sodium bicarbonate.
  • the ratio of the two different pH agents disodium hydrogen phosphate and disodium sodium bicarbonate having high solubility in aqueous solutions to be used in the formulations of the present invention to each other can be in the range of 1 :5 to 5: 1 , preferably in the range of 1 :3 to 5 : 1 , more preferably in the range of 1 :2 to 4: 1 by weight.
  • the present invention relates to capsule formulations comprising ceftibuten and another characteristic feature of said formulations is that the capsule formulations in which the ceftibuten formulation is filled is prepared from titanium dioxide, gelatin or a combination thereof.
  • Solid dosage forms of the molecule ceftibuten having low water solubility present weak dispersibility and solubility characteristics and this results in decrease in absorption of the drug and thus effectiveness of the treatment.
  • the inventors have observed that capsule formulations comprising ceftibuten present optimum dispersibility and solubility in the case that the ratio of ceftibuten to the pH agent composition comprising at least two different pH agents having high solubility in aqueous solutions is in the range of 1 : 1 to 15:1, preferably in the range of 3: 1 to 10:1.
  • capsule formulations of the present invention comprise at least one pharmaceutically acceptable excipient in addition to ceftibuten and pH agent composition.
  • the pharmaceutically acceptable excipients that can be used in the formulations of the present invention can be selected from a group comprising disintegrant, glidant, lubricant and binder.
  • the disintegrant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, microcrystalline cellulose, silicon dioxide, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, methylcellulose, povidone, magnesium aluminium silicate, starch.
  • croscarmellose sodium can be used as the disintegrant in the capsule formulations of the present invention comprising ceftibuten.
  • the glidant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising magnesium silicate, silicon dioxide, colloidal silicon dioxide, starch, talc, tribasic calcium phosphate or a combination thereof.
  • the lubricant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected form a group comprising calcium stearate, magnesium stearate, sodium stearyl fumarate, polyethylene glycol, PEG 6000, polyvinyl alcohol, potassium benzoate, sodium benzoate.
  • the binder that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising ethyl cellulose, gelatin, hydroxyl ethyl cellulose, hydroxyl methyl cellulose, hydroxyl propyl cellulose, hypromellose, magnesium aluminium silicate, methyl cellulose, povidone.
  • capsule formulations of the present invention comprising ceftibuten
  • said formulations comprise ceftibuten in the range of 5-99%, preferably in the range of 10-95%, more preferably in the range of 30-90% by weight in proportion to total weight of the unit dose amount.
  • ceftibuten in the form of its pharmaceutically acceptable solvates, monohydrate form, dihydrate form, trihydrate form, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms.
  • ceftibuten in the capsule formulations of the present invention comprising ceftibuten, can preferably be in hydrate form, more preferably in dihydrate form.
  • the formulations prepared according to the present invention can comprise 5-25% pH agent, 1-15% binder, 0.5-5% disintegrant, 0.01-0.5% glidant, 0.1-1.5% lubricant by weight in proportion to total weight of the unit dose amount.
  • wet granulation method is used for preparation of the formulation of the present invention.
  • ceftibuten is granulated with the granulation solution and the obtained granules are dried.
  • the pH agent, disintegrant and glidant are added to the sieved granules and they are mixed together.
  • the mixture is sieved again, lubricated adding the lubricant and then filled into capsules.
  • the capsules are blistered and put into cartons.
  • capsule formulations of the present invention comprising ceftibuten are used for production of a medicament effective in treatment of pharyngitis in children and/or adults; tonsillitis, sinusitis, red fever; upper respiratory tract infections such as otitis media in children, acute bronchitis, acute exacerbations of chronic bronchitis in adults; and lower respiratory tract infections such as pneumonia in patients suitable for oral treatment; urinary system infections such as acute and chronic pyelitis, cystopyelitis, cystitis, urethritis in adults and children.
  • the examples below are given in order to explain the pharmaceutical compositions of the present invention and their preparation methods, yet the invention cannot be limited to these.
  • the formulation given above is prepared by using wet granulation method. According to this, ceftibuten dihydrate is granulated with a granulation solution comprising binder. The obtained granules are dried, sieved and mixed with the pH agents, disintegrant and glidant. At the last phase, lubrication is applied with the lubricant and mixture is filled into capsules. Capsules are blistered and put into cartons.

Abstract

The present invention relates to pharmaceutical formulations comprising ceftibuten for use in treatment of upper and lower respiratory tract and urinary system infections. Said formulations are characterized in being in capsule form.

Description

CAPSULE FORMULATIONS COMPRISING CEFTIBUTEN
The present invention relates to pharmaceutical formulations comprising ceftibuten for use in treatment of upper and lower respiratory tract and urinary system infections. Said formulations are characterized in being in capsule form. Ceftibuten was first disclosed in the application numbered US 4634697. It has been disclosed in said document that ceftibuten is indicated for infections such as abscesses caused by susceptible bacteria, bronchitis, dermatitis, otitis, empyema, enteritis, gastroenteritis, nasopharyngitis, osteomyelitis, pneumonia, pneumonitis, pustulosis, pyelonephritis, respiratory tract infections, rhinitis, septicemia, tonsillitis, ulcer, urinary system infections, wound and soft tissue infections.
Ceftibuten is present in 200 and 400 mg tablet forms on the market.
It is disclosed in the patents numbered US 4933443 and US 4812561 that ceftibuten is stabile in dihydrate and trihydrate forms. Furtermore, it is also disclosed in said patents that dihydrate and trihydrate forms of ceftibuten can be filled into hard gelatin capsules for oral administration.
However, low solubility of the molecule ceftibuten in aqueous solutions due to its hygroscopic nature leads to dispersibility and solubility problems during use of solid dosage forms of formulations comprising ceftibuten. In the case that ceftibuten formulations are formulated in capsule form, low solubility of the capsules in gastro-intestinal liquid in body and difficulties of dissolution of ceftibuten decreases absorption of the medicine and leads to loss of effectiveness of the treatment. Therefore, there is still need for new approaches in order to develop ceftibuten formulations produced in capsule form which can disperse easily and fast in body, have high absorption and bioavailability during oral use. The inventors have surprisingly observed that ceftibuten capsule forms which comprise a composition of at least two different pH agents having high water solubility as pH agent wherein the ratio of the first pH agent to the second pH agent composing this composition is in the range of 1 :5 to 5: 1 by weight disperse easily and fast in body and absorption and thus bioavailability of the drug is high.
Description of the Invention
The present invention relates to capsule formulations comprising ceftibuten and is characterized in that said formulations comprise a composition of at least two different pH agents having high solubility in aqueous solutions and the ratio of the first pH agent to the second pH agent composing this composition is in the range of 1 :5 to 5:1 by weight.
Another characteristic of the formulations prepared according to the present invention is that the ratio of the first pH agent to the second pH agent in the composition comprising at least two different pH agents is preferably in the range of 1 :3 to 5: 1 , more preferably in the range of 1 :2 to 4: 1 by weight. The first and the second pH agents composing the composition comprising at least two different pH agents having high solubility in aqueous solutions to be used in the formulations of the present invention can be selected from a group comprising tribasic calcium phosphate, monosodium glutamate, potassium citrate, trisodium citrate, sodium hydroxide, dibasic sodium phosphate, monobasic sodium phosphate, disodium hydrogen phosphate, sodium bicarbonate or combinations thereof.
Preferably, the first pH agent in the composition comprising at least two different pH agents having high solubility in aqueous solutions that shall be used in the formulations of the present invention can be disodium hydrogen phosphate.
Preferably, the second pH agent in the composition comprising at least two different pH agents having high solubility in aqueous solutions that shall be used in the formulations of the present invention can be sodium bicarbonate.
The ratio of the two different pH agents disodium hydrogen phosphate and disodium sodium bicarbonate having high solubility in aqueous solutions to be used in the formulations of the present invention to each other can be in the range of 1 :5 to 5: 1 , preferably in the range of 1 :3 to 5 : 1 , more preferably in the range of 1 :2 to 4: 1 by weight. The present invention relates to capsule formulations comprising ceftibuten and another characteristic feature of said formulations is that the capsule formulations in which the ceftibuten formulation is filled is prepared from titanium dioxide, gelatin or a combination thereof. Solid dosage forms of the molecule ceftibuten having low water solubility present weak dispersibility and solubility characteristics and this results in decrease in absorption of the drug and thus effectiveness of the treatment. The inventors have observed that capsule formulations comprising ceftibuten present optimum dispersibility and solubility in the case that the ratio of ceftibuten to the pH agent composition comprising at least two different pH agents having high solubility in aqueous solutions is in the range of 1 : 1 to 15:1, preferably in the range of 3: 1 to 10:1.
Another characteristic feature of the capsule formulations of the present invention is that said formulations comprise at least one pharmaceutically acceptable excipient in addition to ceftibuten and pH agent composition. The pharmaceutically acceptable excipients that can be used in the formulations of the present invention can be selected from a group comprising disintegrant, glidant, lubricant and binder.
The disintegrant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, microcrystalline cellulose, silicon dioxide, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, methylcellulose, povidone, magnesium aluminium silicate, starch.
Preferably, croscarmellose sodium can be used as the disintegrant in the capsule formulations of the present invention comprising ceftibuten.
The glidant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising magnesium silicate, silicon dioxide, colloidal silicon dioxide, starch, talc, tribasic calcium phosphate or a combination thereof.
The lubricant that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected form a group comprising calcium stearate, magnesium stearate, sodium stearyl fumarate, polyethylene glycol, PEG 6000, polyvinyl alcohol, potassium benzoate, sodium benzoate. The binder that can be used in the capsule formulations of the present invention comprising ceftibuten can be selected from a group comprising ethyl cellulose, gelatin, hydroxyl ethyl cellulose, hydroxyl methyl cellulose, hydroxyl propyl cellulose, hypromellose, magnesium aluminium silicate, methyl cellulose, povidone. Another characteristic of the capsule formulations of the present invention comprising ceftibuten is that said formulations comprise ceftibuten in the range of 5-99%, preferably in the range of 10-95%, more preferably in the range of 30-90% by weight in proportion to total weight of the unit dose amount.
In the capsule formulations of the present invention comprising ceftibuten, ceftibuten can be in the form of its pharmaceutically acceptable solvates, monohydrate form, dihydrate form, trihydrate form, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms.
In the capsule formulations of the present invention comprising ceftibuten, ceftibuten can preferably be in hydrate form, more preferably in dihydrate form. The formulations prepared according to the present invention can comprise 5-25% pH agent, 1-15% binder, 0.5-5% disintegrant, 0.01-0.5% glidant, 0.1-1.5% lubricant by weight in proportion to total weight of the unit dose amount.
Preferably, wet granulation method is used for preparation of the formulation of the present invention. According to this method, ceftibuten is granulated with the granulation solution and the obtained granules are dried. The pH agent, disintegrant and glidant are added to the sieved granules and they are mixed together. The mixture is sieved again, lubricated adding the lubricant and then filled into capsules. The capsules are blistered and put into cartons.
Another characteristic feature of the capsule formulations of the present invention comprising ceftibuten is that they are used for production of a medicament effective in treatment of pharyngitis in children and/or adults; tonsillitis, sinusitis, red fever; upper respiratory tract infections such as otitis media in children, acute bronchitis, acute exacerbations of chronic bronchitis in adults; and lower respiratory tract infections such as pneumonia in patients suitable for oral treatment; urinary system infections such as acute and chronic pyelitis, cystopyelitis, cystitis, urethritis in adults and children. The examples below are given in order to explain the pharmaceutical compositions of the present invention and their preparation methods, yet the invention cannot be limited to these.
EXAMPLE I. Capsule formulations comprising ceftibuten
The formulation given above is prepared by using wet granulation method. According to this, ceftibuten dihydrate is granulated with a granulation solution comprising binder. The obtained granules are dried, sieved and mixed with the pH agents, disintegrant and glidant. At the last phase, lubrication is applied with the lubricant and mixture is filled into capsules. Capsules are blistered and put into cartons.

Claims

1. Capsule formulations comprising ceftibuten, characterized in that said formulations comprise a composition comprising at least two different pH agents having high water solubility and the ratio of the first pH agent to the second pH agent composing this composition is in the range of 1 :5 to 5:1 by weight.
2. The formulation according to claim 1 , characterized in that the ratio of the first pH agent to the second pH agent composing the pH agent composition in said formulations is in the range of 1 :3 to 5: 1 by weight.
3. The formulation according to claim 2, characterized in that the ratio of the first pH agent to the second pH agent composing the pH agent composition in said formulations is in the range of 1 :2 to 4: 1 by weight.
4. The formulation according to claims 1-3, characterized in that the first and the second pH agents composing the pH agent composition in said formulations are selected from a group comprising tribasic calcium phosphate, monosodium glutamate, potassium citrate, trisodium citrate, sodium hydroxide, dibasic sodium phosphate, monobasic sodium phosphate, disodium hydrogen phosphate, sodium bicarbonate or combinations thereof.
5. The formulation according to claim 4, characterized in that disodium hydrogen phosphate is used as the first pH agent composing the pH agent composition in said formulation.
6. The formulation according to claim 4, characterized in that sodium bicarbonate is used as the second pH agent composing the pH agent composition in said formulation.
7. The formulation according to claims 1-6, characterized in that the ratio of the pH agents disodium hydrogen phosphate: sodium bicarbonate composing the pH composition to each other is in the range of 1 :5 to 5: 1 by weight.
8. The formulation according to claim 7, characterized in that the ratio of the pH agents disodium hydrogen phosphate: sodium bicarbonate composing the pH composition to each other is in the range of 1 :3 to 5:1 by weight.
9. The formulation according to claim 8, characterized in that the ratio of the pH agents disodium hydrogen phosphate: sodium bicarbonate composing the pH composition to each other is in the range of 1 :2 to 4: 1 by weight.
10. The formulation according to claims 1-9, characterized in that the ratio of ceftibuten-.pH agent composition is in the range of 1 : 1 to 15: 1 by weight.
1 1. The formulation according to claim 10, characterized in that the ratio of ceftibutenrpH agent composition is in the range of 3: 1 to 10: 1 by weight.
12. The formulation according to claims 1-1 1 , characterized in that said formulation comprises at least one pharmaceutically acceptable excipient in addition to ceftibuten and the pH agent composition.
13. The formulation according to claim 12, characterized in that the excipients that can be used in said formulation are selected from a group comprising disintegrant, glidant, lubricant and binder.
14. The formulation according to claim 13, characterized in that the disintegrant that can be used in said formulation is selected from a group comprising carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, microcrystalline cellulose, silicon dioxide, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, methylcellulose, povidone, magnesium aluminium silicate, starch or combinations thereof.
15. The formulation according to claim 14, characterized in that croscarmellose sodium is preferably used as the disintegrant that can be used in said formulation.
16. The formulation according to claim 13, characterized in that the glidant that can be used in said formulation is selected from a group comprising magnesium silicate, silicon dioxide, colloidal silicon dioxide, starch, talc, tribasic calcium phosphate or a combination thereof.
17. The formulation according to claim 13, characterized in that the lubricant that can be used in said formulation is selected from a group comprising calcium stearate, magnesium stearate, sodium stearyl fumarate, polyethylene glycol, PEG 6000, polyvinyl alcohol, potassium benzoate, sodium benzoate.
18. The formulation according to claim 13, characterized in that the binder that can be used in said formulation is selected from a group comprising ethyl cellulose, gelatin, hydroxyl ethyl cellulose, hydroxyl methyl cellulose, hydroxyl propyl cellulose, hypromellose, magnesium aluminium silicate, methyl cellulose, povidone.
19. The formulation according to any preceding claims, characterized in that the capsule formulation used in the capsule wherein ceftibuten formulation is filled is prepared from titanium dioxide, gelatin or a combination thereof.
20. The formulation according to any preceding claims, characterized in that said formulation comprises ceftibuten in the range of 5-99%.
21. The formulation according to claim 20, characterized in that said formulation comprises ceftibuten in the range of 10-95%.
22. The formulation according to claim 21, characterized in that said formulation comprises ceftibuten in the range of 30-90%.
23. The formulation according to any preceding claims, characterized in that ceftibuten comprised in said formulation is selected from a group comprising its pharmaceutically acceptable solvates, monohydrate form, dihydrate form, trihydrate form, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms.
24. The formulation according to claim 23, characterized in that ceftibuten in said formulation is in hydrate form.
25. The formulation according to claim 24, characterized in that ceftibuten in said formulation is in dihydrate form.
26. The formulation according to claim 24, characterized in that said formulation comprises 5-25% pH agent, 1-15% binder, 0.5-5% disintegrant, 0.01 -0.5% glidant, 0.1-1.5% lubricant by weight in proportion to total weight of unit dose amount.
27. A method for production of a formulation according to any preceding claims, characterized in that said method comprises the steps of granulating ceftibuten with the granulation solution, drying and sieving the obtained granules, adding pH agent, disintegrant and glidant to the granules and mixing them together, sieving the mixture again and lubricating it adding the lubricant, then filling the mixture into capsules.
28. The formulation according to any preceding claims, characterized in that said formulation is used for production of a medicament effective in treatment of pharyngitis in children and/or adults; tonsillitis, sinusitis, scarlet fever; upper respiratory tract infections such as otitis media in children, acute bronchitis, acute exacerbations of chronic bronchitis in adults; and lower respiratory tract infections such as pneumonia in patients suitable for oral treatment; urinary system infections such as acute and chronic pyelitis, cystopyelitis, cystitis, urethritis in adults and children.
EP13724914.0A 2012-04-04 2013-04-03 Capsule formulations comprising ceftibuten Withdrawn EP2833874A1 (en)

Applications Claiming Priority (2)

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TR201203836 2012-04-04
PCT/TR2013/000109 WO2013151518A1 (en) 2012-04-04 2013-04-03 Capsule formulations comprising ceftibuten

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