EP2608776A2 - Cefpodoxime proxetil formulations - Google Patents

Cefpodoxime proxetil formulations

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Publication number
EP2608776A2
EP2608776A2 EP11782258.5A EP11782258A EP2608776A2 EP 2608776 A2 EP2608776 A2 EP 2608776A2 EP 11782258 A EP11782258 A EP 11782258A EP 2608776 A2 EP2608776 A2 EP 2608776A2
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EP
European Patent Office
Prior art keywords
pharmaceutical composition
composition according
range
agent
cefpodoxime
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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Withdrawn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
EP11782258.5A
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German (de)
French (fr)
Inventor
Mahmut Bilgic
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Bilgic Mahmut
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Individual
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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

Definitions

  • Water dispersible tablets of the present invention can be prepared as specified below, yet the invention is not restricted to these examples.
  • EXAMPLE 1 Formulation and process for preparation of water dispersible granule

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Medicinal Preparation (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

The present invention relates to pharmaceutical formulations comprising cefpodoxime proxetil.

Description

CEFPODOXIME PROXETIL FORMULATIONS
The present invention relates to pharmaceutical compositions comprising cefpodoxime and optionally clavulanic acid or derivatives thereof.
Background of the Invention:
Cefpodoxime proxetil (figure I), chemical name of which is pivaloyloxymethyl 7-[2-(2- amino-thiazole-4-yl]-2-(syn)-methoxyimino-acetamido]-3-methoxymethyl-3-cefem-4- carboxylate, was first disclosed in the patent numbered EP0049118.
Figure 1
Cefpodoxime proxetil is a third generation cephalosporin. Due to this feature, it is indicated in the treatment of infections caused by gram positive and gram negative bacteria.
Clavulanic acid and derivatives thereof (for instance its salts such as potassium clavulanate) are known as the beta-lactamase inhibitors which withstand the beta-lactamase-originated resistance mechanism by suppressing the activity of beta-lactamase enzymes. Clavulanic acid and derivatives thereof can optionally be formulated as combined with antibiotics in order to increase efficiency of beta-lactam derivative antibiotics.
Tablets which contain 100 mg and 200 mg of cefpodoxime are available on the market. When these tablets containing 100 or 200 mg of active agent are formulated with excipients, they become too large in size and this makes the use of this dosage form inconvenient for patients who have swallowing difficulties, especially for pediatric and geriatric patients.
The molecule cefpodoxime proxetil has quite low water solubility; therefore bioavailability of tablet forms is rather low. It is known that efficiency of a drug depends on the design of the formulation to a great extent. When highly hydrophobic nature of cephalosporins, especially cefpodoxime, are taken into consideration, it is seen that selecting each agent to be used in the formulation carefully is significant to attain to the desired level of bioavailability in the dosage forms constituted.
In order to overcome the problems that solid dosage forms pose, water dispersible dosage forms have been developed. However, the fact that cefpodoxime has rather low water solubility makes development of water dispersible cefpodoxime formulations difficult.
At this point, there is need for formulations comprising cefpodoxime and optionally clavulanic acid or derivatives thereof which have higher bioavailability than solid oral dosage forms; can dissolve in water; have no gelling problem in order to meet the needs of patients with swallowing difficulties.
Description of the invention:
The subject matter of the present invention is formulations comprising water dispersible cefpodoxime and optionally clavulanic acid or derivatives thereof which comprise at least 35% of diluent. Surprisingly, it has been seen that powder, tablet and/or granules comprising the active agent cefpodoxime that has a rather low water solubility which are formulated with at least 35% of lactose constitute a suspension which disperses in water without gelling.
According to this, pharmaceutical dosage forms in the form of water dispersible powder, tablet and/or granule; a) can be taken by the patients more comfortably as they disperse in water homogeneously prior to use and their bioavailability is superior to said solid dosage forms; b) thus, the problem of gelling which is frequently encountered in cefpodoxime formulations is overcome.
Cefpodoxime that can be used in the water dispersible powder, tablet and/or granule formulations of the present invention can be in the form of its esters, solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms or free form and/or a combination thereof. In the present invention, cefpodoxime proxetil is preferably used. The term "water dispersible powder, tablet and/or granule" used in the text comprises single dose effervescent powder, tablets and/or granules; single dose water dispersible powders, tablets and granules; multiple dose powder, tablet and granules which are as dispersed in water to form suspension; single dose water soluble powder, tablet and granules; multiple dose water soluble powder, tablet and granules.
According to this, one aspect of the present invention is water dispersible powder, tablet and/or granule formulations comprising cefpodoxime as the active agent and at least 35% of diluent.
Another aspect of the present invention is water dispersible powder, tablet and/or granule formulations comprising cefpodoxime as the active agent, at least 35% of diluent and additionally other pharmaceutically acceptable excipients.
Apart from cefpodoxime and the diluent; the water dispersible powder, tablet and/or granule formulation can comprise various excipients such as, but not limited to, binders, glidants, diluents, lubricants, humectants, disintegrants, basic agents, acidic agents, taste regulating agents, viscosity agents, flavoring agents, preservative agents and optionally effervescent couple.
The binder that can be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising ethyl cellulose, gelatine, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hypromellose, magnesium aluminum silicate, methyl cellulose, povidone or combinations thereof.
The lubricant that can be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising calcium stearate, magnesium stearate, polyethylene glycol, PEG 6000, polyvinyl alcohol, potassium benzoate, talc, sodium benzoate or a combination thereof. Preferably, talc is used as lubricant in the formulation of the present invention.
The glidant that can be used in the water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising magnesium silicate, silicon dioxide, starch, talc, tribasic calcium phosphate or combinations thereof. Preferably, silicon dioxide is used as glidant in the formulation of the present invention. The humectant that can be used in the water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising anhydrous sodium sulphate, silica gel and potassium carbonate or a combination thereof.
The disintegrant that can be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, microcrystalline cellulose, silicon dioxide, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, methyl cellulose, povidone, magnesium aluminum silicate and starch or combinations thereof.
The diluent that can be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising calcium carbonate, calcium sulphate, dibasic calcium phosphate, tribasic calcium phosphate, calcium phosphate, calcium sulphate, microcrystalline cellulose, lactose, magnesium carbonate, magnesium oxide, maltodextrin, maltose, mannitol, sodium chloride, sorbitol, starch, xylitol or combinations thereof. Preferably, a disaccharide, more preferably lactose is used in the formulation of the present invention as diluent.
In another aspect, percentage of the diluent used in the present invention is at least 35%, preferably in the range of 40-65%, more preferably in the range of 45-60%.
The basic agent that can be used in the water dispersible powder, tablet and/or granule formulation of the present invention can be selected from a group comprising potassium carbonate, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium carbonate, sodium bicarbonate or combinations thereof.
The acidic agent that can be used in the water dispersible powder, tablet and/or granule formulation of the present invention can be selected from a group comprising acetic acid, citric acid, lactic acid, malic acid, phosphoric acid, propionic acid, tartaric acid or combinations thereof. Preferably, citric acid is used in the formulation of the present invention as acidic agent.
The taste regulating agent that can be used in water dispersible powder, tablet and/or granule formulation of the present invention can be selected from a group comprising acesulfame, aspartame, dextrose, fructose, glucose, lactitol, maltitol, maltose, sorbitol, saccharine, saccharine sodium, sodium cyclamate, sucralose, sodium chloride, potassium chloride, sucrose, xylitol or combinations thereof. It is known that cefpodoxime has bitter taste. In the formulation of the present invention, percentage of the taste regulation agent used is in the range of 5-30%, preferably in the range of 10-28%, more preferably in the range of 15-25%.
According to this, another aspect of the present invention is water dispersible cefpodoxime formulations comprising 5-30% of taste regulating agent.
The viscosity agent that can be used in water dispersible powder, tablet and/or granule formulation of the present invention can be selected from a group comprising carboxy methyl cellulose sodium, carboxy methyl cellulose calcium, colloidal silicone dioxide, ethyl cellulose, hydroxyl ethyl cellulose, hydroxypropyl cellulose, hydroxyl methyl cellulose, hypromellose or a combination thereof.
The preservative agent that can be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from a group comprising methylparaben, ethylparaben, butylparaben, sorbic acid, tertiary ammonium salts, potassium sorbate, benzoic acid and/or salts thereof (sodium benzoate) and benzyl alcohol or a combination thereof.
The effervescent couple that can optionally be used in water dispersible powder, tablet and granule formulation of the present invention can be selected from organic acids such as citric acid, tartaric acid, malic acid, fumaric acid etc. and basic agents such as sodium hydrogen carbonate, sodium carbonate, potassium carbonate and potassium hydrogen carbonate etc.
The water dispersible powder, tablet and granule formulation of the present invention can comprise cefpodoxime in the range of 20-800 mg or its pharmaceutically acceptable esters, salts, hydrates, solvates or a combination thereof in an equal amount.
The water dispersible powder, tablet and granule formulation of the present invention can comprise 5-60% of cefpodoxime or its pharmaceutically acceptable esters, solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms in proportion to total weight of unit dose.
The water dispersible powder, tablet and granule formulation of the present invention can comprise 5-60 % of cefpodoxime and at least one; binder in the range of 0-40%; glidant in the range of 0.5-5%; lubricant in the range of 1-10%; humectant in the range of 0-40%; disintegrant and/or disintegrants in the range of 0-20%; diluent in the range of 35-65%; basic agent in the range of 0-40%; acidic agent in the range of 0.1-40%; taste regulating agent in the range of 5-30%; viscosity agent in the range of 2-15%; flavoring agent in the range of 0.1-5%; preservative agent in the range of 0-5% and optionally effervescent couple in the range of 0- 85% in proportion to the total weight of unit dose amount.
If required, the formulation of the present invention can be used for pharmaceutical compositions comprising clavulanic acid or derivatives thereof along with cefpodoxime.
According to this, the present invention relates to pharmaceutical compositions comprising cefpodoxime and clavulanic acid or derivatives thereof, at least 35% of diluent and optionally pharmaceutically acceptable excipients in addition.
Clavulanic acid that can optionally be used in the pharmaceutical composition of the present invention can be in the form of solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms or in free form and/or a combination thereof. Preferably, potassium clavulanate is used in the present invention.
The pharmaceutical composition of the present invention can comprise clavulanic acid in the range of 50-500 mg or its pharmaceutically acceptable salts, hydrates, solvates or a combination thereof in an equal amount.
Clavulanic acid and its derivatives (e.g. potassium clavulanate) are extremely susceptible to moisture. To this respect, potassium clavulanate in the pharmaceutical composition of the present invention is preferably used with a humectant in the ratio of 1 : 1.
One or more of the substances comprising silica; colloidal silica, for instance colloidal silica anhydrous, for example Aerosil® 200, magnesium trisilicate, cellulose powder, Cabosil®, magnesium oxide, calcium silicate, Syloid®, starch, microcrystalline cellulose, talc can be used as the humectant.
In the pharmaceutical composition of the present invention, potassium clavulanate is preferably used with syloid in the ratio of 1 : 1.
The pharmaceutical composition of the present invention can comprise 5-50% of clavulanic acid in proportion to total weight of unit dose amount or pharmaceutically acceptable salts, hydrates, solvates or combinations thereof in an equal amount. In another aspect, the present invention relates to processes that can be used for preparation of water dispersible powder, tablet and/or granule formulations comprising pharmaceutically acceptable excipients in addition to cefpodoxime as active agent.
According to this, the process of the present invention comprises granulation of the active agent cefpodoxime proxetil by conventional wet and/or dry granulation methods; or powdering ceipodoxime proxetil and other excipients after mixing them by dry blending method and optionally compressing tablets.
The powder, tablet and/or granules obtained are dispersed in water before use by patients and taken in liquid form.
Another aspect of the present invention is that the formulation prepared according to said invention is used in the treatment of diseases related with infections caused by gram negative and gram positive bacteria.
Water dispersible tablets of the present invention can be prepared as specified below, yet the invention is not restricted to these examples.
EXAMPLE 1: Formulation and process for preparation of water dispersible granule
A method for preparation of water dispersible granule given in this example comprises, but not limited to, dissolving cefpodoxime proxetil in a suitable solvent; and granulating the diluent with this solution; and drying and then mixing the granules obtained with the other excipients. EXAMPLE 2: Formulation and process for preparation of water dispersible granule
A method for preparation of water dispersible granule given in this example comprises, but not limited to, dissolving cefpodoxime proxetil in a suitable solvent; and granulating the diluent with this solution; and drying and then mixing the granules obtained with the potassium clavylanate-syloid (1:1) and the other excipients.

Claims

CLAIMS:
1. A pharmaceutical composition comprising cefpodoxime characterized in that said composition is water dispersible cefpodoxime formulation comprising at least 35% of diluent.
2. The pharmaceutical composition according to claim 1, wherein cefpodoxime that is used as active agent can be in the form of its esters, solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms or in free form and/or a combination thereof.
3. The pharmaceutical composition according to claim 2, wherein cefpodoxime proxetil is used as the active agent.
4. The pharmaceutical composition according to claim 1, wherein said composition can be in the form of single dose effervescent powder, tablets and/or granules; single dose water dispersible powders, tablets and granules; multiple dose powder, tablet and granules which are as dispersed in water to form suspension; single dose water soluble powder, tablet and granules; multiple dose water soluble powder, tablet and granules.
5. The pharmaceutical composition according to claim 1, wherein said composition further comprises pharmaceutically acceptable excipients in addition to cefpodoxime as the active agent and at least 35% of diluent.
6. The pharmaceutical composition according to claim 5, wherein said composition can comprise binder, glidant, lubricant, humectant, disintegrant, diluent, basic agent, acidic agent, sweetener, viscosity agent, flavoring agent, preservative agent and/or effervescent couple in addition to cefpodoxime as the active agent and at least 35% of diluent.
7. The pharmaceutical composition according to claim 6, wherein the binder can be selected from a group comprising ethyl cellulose, gelatine, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hypromellose, magnesium aluminum silicate, methyl cellulose, povidone or a combination thereof.
8. The pharmaceutical composition according to claim 6, wherein the lubricant can be selected from a group comprising calcium stearate, magnesium stearate, polyethylene glycol, PEG 6000, polyvinyl alcohol, potassium benzoate, talc, sodium benzoate or a combination thereof.
9. The pharmaceutical composition according to claim 8, wherein talc is preferably used as lubricant.
10. The pharmaceutical composition according to claim 6, wherein the glidant can be selected from a group comprising magnesium silicate, silicon dioxide, starch, talc, tribasic calcium phosphate or combinations thereof.
11. The pharmaceutical composition according to claim 10, wherein silicon dioxide is preferably used as glidant.
12. The pharmaceutical composition according to claim 6, wherein the humectant can be selected from a group comprising anhydrous sodium sulphate, silica gel and potassium carbonate or a combination thereof.
13. The pharmaceutical composition according to claim 6, wherein the disintegrant can be selected from a group comprising carboxymethyl cellulose calcium, carboxymethylcellulose sodium, microcrystalline cellulose, silicon dioxide, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, methyl cellulose, povidone, magnesium aluminum silicate, starch or combinations thereof.
14. The pharmaceutical composition according to claim 6, wherein the diluent can be selected from a group comprising calcium carbonate, calcium sulphate, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulphate, microcrystalline cellulose, lactose, magnesium carbonate, magnesium oxide, maltodextrin, maltose, mannitol, sodium chloride, sorbitol, starch, xylitol or combinations thereof.
15. The pharmaceutical composition according to claim 14, wherein a disaccharide is preferably used as diluent.
16. The pharmaceutical composition according to claim 15, wherein lactose is preferably used as diluent.
17. The pharmaceutical composition according to claim 14, wherein the amount of the diluent used is at least 35%.
18. The pharmaceutical composition according to claim 17, wherein the percentage of the diluent used is in the range of 40% to 65%.
19. The pharmaceutical composition according to claim 18, wherein the percentage of the diluent used is in the range of 45% to 60%.
20. The pharmaceutical composition according to claim 6, wherein the basic agent can be selected from a group comprising potassium carbonate, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium carbonate, sodium bicarbonate or combinations thereof.
21. The pharmaceutical composition according to claim 6, wherein the acidic agent can be selected from a group comprising acetic acid, citric acid, lactic acid, malic acid, phosphoric acid, propionic acid, tartaric acid or combinations thereof.
22. The pharmaceutical composition according to claim 21, wherein citric acid is preferably used as acidic agent.
23. The pharmaceutical composition according to claim 6, wherein the taste regulating agent is selected from a group comprising acesulfame, aspartame, dextrose, fructose, glucose, lactitol, maltitol, sorbitol, saccharine sodium, sodium cyclamate, sucralose, sodium chloride, potassium chloride, sucrose, xylitol or combinations thereof.
24. The pharmaceutical composition according to claim 23, wherein the percentage of the taste regulating agent in said composition is in the range of 5-30%.
25. The pharmaceutical composition according to claim 24, wherein the percentage of the taste regulating agent in said composition is in the range of 10-28%.
26. The pharmaceutical composition according to claim 25, wherein the percentage of the taste regulating agent in said composition is in the range of 15-25%.
27. The pharmaceutical composition according to claim 6, wherein the viscosity agent can be selected from a group comprising carboxy methyl cellulose sodium, carboxy methyl cellulose calcium, colloidal silicone dioxide, ethyl cellulose, hydroxyl ethyl cellulose, hydroxypropyl cellulose, hydroxyl methyl cellulose, hypromellose or a combination thereof.
28. The pharmaceutical composition according to claim 6, wherein the preservative agent can be selected from a group comprising methylparaben, ethylparaben, butylparaben, sorbic acid, tertiary ammonium salts, potassium sorbate, benzoic acid and/or salts thereof (sodium benzoate) and benzyl alcohol or a combination thereof.
29. The pharmaceutical composition according to claim 6, wherein the effervescent couple can be selected from organic acids such as citric acid, tartaric acid, malic acid, fumaric acid etc. and basic agents such as sodium hydrogen carbonate, sodium carbonate, potassium carbonate and potassium hydrogen carbonate etc..
30. The pharmaceutical composition according to claim 1, wherein said composition can comprise cefpodoxime in the range of 20-800 mg or its pharmaceutically acceptable esters, salts, hydrates, solvates or a combination thereof in an equal amount.
31. The pharmaceutical composition according to claim 1 , wherein said composition can comprise 5-60% of cefpodoxime or its pharmaceutically acceptable esters, solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms in proportion to total amount of unit dose.
32. The pharmaceutical composition according to claim 1, wherein said composition can comprise 5-60 % of cefpodoxime; binder in the range of 0-40%; glidant in the range of 0.5-5%; lubricant in the range of 1-10%; humectant in the range of 0-40%; disintegrant and/or disintegrants in the range of 0-20%; diluent in the range of 35- 65%; basic agent in the range of 0-40%; acidic agent in the range of 0.1-40%; taste regulating agent in the range of 1 -25%; viscosity agent and/or agents in the range of 2- 15%; flavoring agent in the range of 0.1-5%; preservative agent in the range of 0-5% and optionally effervescent couple in the range of 0-85% in proportion to the total weight of unit dose amount.
33. The pharmaceutical composition claimed in any preceding claims, wherein said composition comprises clavulanic acid or derivatives thereof in addition to cefpodoxime it comprises as active agent.
34. The pharmaceutical composition according to claim 33, wherein clavulanic acid can be in the form of its solvates, hydrates, enantiomers, racemates, organic salts, inorganic salts, polymorphs, crystalline and amorphous forms or in free form and/or a combination thereof.
35. The pharmaceutical composition according to claim 34, wherein potassium clavulanate is used in said composition.
36. A method for preparation of the pharmaceutical composition as claimed in any of the claims above, wherein said method comprises granulation of the active agent cefpodoxime proxetil by conventional wet and/or dry granulation methods; or powdering cefpodoxime proxetil and other excipients after mixing them by dry blending method and optionally compressing tablets.
37. The pharmaceutical composition according to claim 1, wherein said composition is used in production of a drug prepared so as to be used in the treatment of diseases related with infections caused by gram negative and gram positive bacteria.
EP11782258.5A 2010-08-25 2011-08-24 Cefpodoxime proxetil formulations Withdrawn EP2608776A2 (en)

Applications Claiming Priority (2)

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TR2010/07106A TR201007106A1 (en) 2010-08-25 2010-08-25 Cefpodoxime proxetil formulations.
PCT/TR2011/000200 WO2012026907A2 (en) 2010-08-25 2011-08-24 Cefpodoxime proxetil formulations

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CN107693491B (en) * 2017-04-20 2020-06-30 广东金城金素制药有限公司 Pharmaceutical composition and preparation for children
CN108815130A (en) * 2018-08-27 2018-11-16 邓倩 A kind of Cefpodoxime Proxetil tablet and its production technology

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