WO2015163832A1 - Composition combinée d'ibuprofène et de famotidine ayant une stabilité améliorée - Google Patents

Composition combinée d'ibuprofène et de famotidine ayant une stabilité améliorée Download PDF

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Publication number
WO2015163832A1
WO2015163832A1 PCT/TR2015/000153 TR2015000153W WO2015163832A1 WO 2015163832 A1 WO2015163832 A1 WO 2015163832A1 TR 2015000153 W TR2015000153 W TR 2015000153W WO 2015163832 A1 WO2015163832 A1 WO 2015163832A1
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Prior art keywords
ibuprofen
famotidine
pharmaceutical composition
composition according
unit dose
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PCT/TR2015/000153
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English (en)
Inventor
Ersin Yildirim
Fatih Cengiz AYGÜL
Başak Acar KARAKÖY
Kerim AKKAYA
Pradeep Kumar VISHWAKARMA
Derya AKSU
Original Assignee
Pharmacti̇ve İlaç Sanayi̇ Ve Ti̇caret A.Ş.
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Publication of WO2015163832A1 publication Critical patent/WO2015163832A1/fr

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    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles

Definitions

  • the present invention relates to the preperation of stable pharmaceutical compositions containing the active ingredients; ibuprofen and famotidine.
  • ibuprofen chemical name is 2-(4-isobutylphenyl) propionic acid, is a well-known antiinflammatory drug having a molecular weight of 206.28. Ibuprofen is now marketed generically and is patented in the 60's.
  • Ibuprofen has been used in humans for many years. It is a member of nonsteroidal antiinflammatory drugs (NSAID). In general, NSAlDs are used for the treatment of acute/chronic conditions attached with pain and inflammation. NSAIDs are generally used for the symptomatic relief of the following conditions; osteoarthritis, rheumatoid arthritis, mild- to-moderate pain due to inflammation and tissue injury, low back pain, inflammatory arthropathies, tennis elbow, headache, migraine, acute gout, Dysmenorrhoea, metastatic bone pain, postoperative pain, muscle stiffness and pain due to Parkinson's disease, pyrexia (fever), ileus, renal colic and etc. Ibuprofen is used for relieving pain, alleviating fever and reducing inflammation.
  • Famotidine is a member of H 2 -receptor antagonist group.
  • the most known 3 ⁇ 4 receptor antagonists are cimetidine, lafutidine, nizatidine, ranitidine, roxatidine and famotidine.
  • H 2 antagonists are used in the treatment of dyspepsia.
  • Pepcidtwo chewable tablet belongs to McNeil Products that comprising famotidine. This tablet is used for the short-term symptomatic relief of heartburn, indigestion, acid indigestion, and hyperacidity.
  • WO 1998025595 A2 relates to drinkable ibuprofen composition containing the ibuprofen active ingredient comprises ibuprofen or S(+)-ibuprofen.
  • WO 2003039532 relates to a pharmaceutical composition
  • a pharmaceutical composition comprising an aqueous solution of arginine and ibuprofen, wherein the molar ratio of arginine to ibuprofen is certain (less than EP0474509 relates to a method for purifying ibuprofen-comprising mixtures of the kind which are typically produced during a reaction process in which ibuprofen (2-(4'- isobutylphenyl)propionic acid) is formed.
  • WO2008011426 relates to a stable pharmaceutical composition in a single unit dosage form comprising: a core comprising from 775 mg to 825 mg of ibuprofen or salt thereof and a surrounding portion comprising from 24 mg to 28 mg of famotidine or salt thereof in a weight ratio in the range 29: 1 to 31 : 1.
  • WO 2007012022 relates to an oral dosage form for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine, in admixture with one or more excipients.
  • US8449910 relates to with two layers in the form of a single tablet unit dosage form comprising a first layer; 800 mg ibuprofen as an active pharmaceutical ingredient and second layer; famotidine as an active pharmaceutical ingredient.
  • US 20050020671 relates to a pharmaceutical formulation which comprises a core comprising a first active ingredient, a coating comprising a second active ingredient which is incompatible with the first active ingredient and a barrier between the core and the coating which prevents physical contact between the core and the coating.
  • EP0256747 relates to polymorph form A of famotidine and its characteristics in DSC and IR spectrum.
  • US5120850 refers to polymorph form B of famotidine.
  • US5650421 relates to pharmaceutical compositions, and more specifically to an aqueous- based, premix formulation of famotidine.
  • US4283408 describes to a process for preparing famotidine, or guanidinothiazole compounds, and medical compositions containing such compounds.
  • Famotidine is used in many combination pharmaceutical formulation.
  • WO2012173581 relates to composition useful for treating muscular and skeletal system diseases, inflammation and pain, comprises thiocolchicoside, etodolac and famotidine.
  • Famotidine is used for many treatments like the treatment to depression, depressive disorders and symtopms suggesting depression as mentioned in EP 1289520 adding to dyspepsia.
  • the present invention relates to administration of solid oral dosage form comprising ibuprofen, famotidine, and one or more pharmaceutically acceptable excipients, to a patient in need of ibuprofen treatment having a gastroesophageal disorder and/or prone to that and/or only for protection aim.
  • the present invention provides a pharmaceutical composition
  • a pharmaceutical composition comprising: famotidine that is a histamin H2 blocker, ibuprofen that is an antiinflammatory agent and relevant excipients.
  • present invention has the advantage to provide a stable combination product providing superior analgesic, anti inflammatory and gastro-protection compared to plain ibuprofen or famotidine tablets. It furthers provides a combination product with reduced and controlled impurities.
  • present invention is a pharmaceutical composition containing a combination of a ibuprofen and famotidine, both active ingredients being present in the free state or in the form of a salt, solvate, enantiomer.
  • Another object of the present invention is a pharmaceutical composition in a form being able to be administered by the oral route.
  • pharmaceutical composition may be formulated, for example, in the form of pharmaceutical compositions for oral administration such as granules, fine granules, powders, hard capsules, soft capsules, syrups, emulsions, suspensions, solutions and the like, or in the, form for sublingual a buccal administration, or in the form of pharmaceutical compositions for parenteral administrations such as injections for intravenous, intramuscular, or subcutaneous administration, drip infusions, transdermal preparations, transmucosal preparations, nasal drops, inhalants, suppositories and the like, injections or drip infusions may be prepared as powdery preparations such as in the form of lyophilized preparations, and may be used by dissolving just before use in an appropriate aqueous medium such as physiological saline.
  • parenteral administrations such as injections for intravenous, intramuscular, or subcutaneous administration, drip infusions, transdermal preparations, transmucosal preparations, nasal drops, inhalants,
  • composition of invention is solid dosage form.
  • the solid dosage form for the present invention includes sprinkles, capsules, caplets, powders and preferably monolayer tablets.
  • Tablet may include multiple layer-compressed tablets, bilayer tablets, mouth dissolving tablets or orally disintegrating tablets, water dispersible tablets, and chewable tablets. More preferably tablets are multiple layer-compressed tablets. It is also desirable for tablets and pills to be formulated into prolonged release preparations.
  • pharmaceutical composition may developed in the form of a unit dosage form, such as tablet, minitablet, bilayer tablet, caplet, granules/pellets, and in the form of capsule or sachet filled with tablets, minitablets, granules/pellets., wherein tablet is scored or unscored.
  • a unit dosage form such as tablet, minitablet, bilayer tablet, caplet, granules/pellets, and in the form of capsule or sachet filled with tablets, minitablets, granules/pellets., wherein tablet is scored or unscored.
  • composition and its formulation process involve avoiding chemical interaction of famotidine with ibuprofen, using pharmaceutically acceptable excipients in the dosage form.
  • the impurity data profile reveals that when ibuprofen and famotidine are mixed in intimate contact with each other using pharmaceutically acceptable excipients, there is a significant increase in the level of degradation products as compared to, when they are separated in the dosage form.
  • An object of the invention is a pharmaceutical composition containing ibuprofen and famotidine, being present in the free state or in the form of a salt, and not being intimately mixed in the composition.
  • pharmaceutical composition can be prepared by various formulation techniques known to the person skilled in the art, such as, but not limited to direct compression, wet or dry granulation, slugging, hot melt granulation, extrusion-spheronization, hot melt extrusion, fluidized bed granulation, extrusion, spray drying spray coating, and solvent evaporation and the like.
  • the process of preparing the stable pharmaceutical composition comprises steps of preparing a core comprising ibuprofen or salt, solvate, enantiomer thereof, coating the core at least partially by famotidine or salt, solvate, enantiomer thereof.
  • step (d) optionally, coating a protective layer over the core prepared in step (c).
  • pharmaceutical composition may comprise single or plurality of multiple-compression tablets which are formed by two or more compression cycles.
  • Each compression cycle uses, alternatively, separate portions of each of ibuprofen and famotidine. This results in a multiple-compression tablet which has at least two discrete layers defined by the presence of the said parts in the layer.
  • a multiple-compression tablet can exist as, for example, a layered tablet, as a compression-coated tablet, or as an inlay tablet.
  • a layered tablet is a tablet which is made up of two or more distinct cores of granulation compressed together with the individual layers lying one on top of another.
  • Layered tablets are generally prepared by compressing a granulation onto a previously compressed granulation. The operation may be repeated to produce multilayered tablets of more than two layers.
  • a compression-coated tablet is a tablet which is made up of an inner core and one or more outer core or coats wherein the inner core is completely surrounded by the outer coat or coats. These tablets have at least three discrete zones of components compressed together, i.e., an inner core, middle core, and an outermost coat. Such tablets also referred to as press-coat or dry-coated tablets are prepared by feeding a previously compressed inner core into a special tableting machine and compressing one or more other granulation coats around the preformed inner core.
  • inlay tablets instead of an inner core being completely surrounded by an outer coat, one surface of the inner core is exposed.
  • These tablets have at least two cores of components compressed together, i.e., an inlay core and a base core.
  • the preparation of inlay tablets is similar to the preparation of compression-coated tablets except that a surface of coating is eliminated. It will be within the pursuit of the skilled artisan to select any component or mixture thereof for preparing inlay core and base core.
  • the barrier layer may be formed by any method, including compression, molding, dipping, or spray coating.
  • the famotidine layer is applied over the barrier coat.
  • the famotidine layer can be applied by compression, spray coating, or other methods.
  • the famotidine layer is applied by spray coating a formulation containing famotidine and excipients such as polymers, plasticizers, and the like.
  • administration of the pharmaceutical composition vary from patient to patient according to type of the disease.
  • Oral daily dose of famotidine is changing from 10 mg to 120 mg.
  • Approved dose regimen of famotidine administration includes 10 mg orally once or twice daily for Dyspepsia, 40 mg orally once a day at bedtime or 20 mg orally twice a day for Duodenal Ulcer, 40 mg orally once a day at bedtime or 20 mg orally twice a day for Peptic Ulcer, 20 mg orally once a day for Duodenal Ulcer Prophylaxis, 40 mg orally once a day at bedtime or 20 mg orally twice a day for Gastric Ulcer, 20 mg orally twice a day for Gastroesophageal Reflux Disease, 20 mg to 40 mg orally twice a day for Erosive Esophagitis, 20 mg orally every 6 hours for Zollinger-EUison Syndrome, 20 mg orally every 6 hours for Pathological Hypersecretory Conditions.
  • Oral daily dose of ibuprofen is varying from 600 mg to 3200 mg.
  • Approved dose regimen of ibuprofen administration includes 200 to 400 mg orally every 4 to 6 hours for dysmenorrhea, 400 to 800 mg orally every 6 to 8 hours for Osteoarthritis, for Rheumatoid Arthritis, 200 to 400 mg orally every 4 to 6 hours for Pain, 200 to 400 mg orally every 4 to 6 hours for Fever.
  • pharmaceutical compositions of the present invention enable versatile administration of combination mentioned herein to different patients' group being in need of different treatment regimen.
  • compositions of the present invention are generally formulated in dosage units containing from 200 to 800mg of ibuprofen and 10 to 40 mg of famotidine per unit dosage.
  • Another object of the present invention is a pharmaceutical composition containing 800mg of ibuprofen and 40 mg of famotidine or 800 mg of ibuprofen and 20 mg of famotidine or 400mg of ibuprofen and 20 mg of famotidine or 200mg of ibuprofen and 10 mg of famotidine.
  • composition of the present invention comprises ibuprofen and famotidine, in combination with at least one pharmaceutically acceptable excipient, wherein ratio of ibuprofen to famotidine is in the range of 10: 1 to 41 : 1 , preferably in the range of 1 : 1 to 22 : 1 , more preferably in the range of 19: 1 to 21 : 1.
  • pharmaceutical composition characterized in that it comprises ibuprofen and famotidine, in combination with at least one pharmaceutically acceptable excipient, wherein ratio of ibuprofen to famotidine is in the range of 19: 1 to 21 :1 or 39: 1 to 41 : 1 , preferably in the range of 20:1 or 40: 1 the said pharmaceutical composition being provided in the solid form, which are stable over time.
  • the pharmaceutical composition of the invention is suitable for BID,TID or QID administrations.
  • BID,TID,QID refer to two times a day, three times a day, four times a day respectively.
  • pharmaceutical composition of the present invention may further comprise diluents, binders, dispersing agents, disintegrants, stabilizing agents, surfactants, lubricants, glidants, flavoring agents, sweeteners and other pharmaceutical additives or excipient to facilitate the physical formulation of various dosage forms like orally disintegrating tablets, chewable tablets and suspensions (including dry powders or granules for suspension).
  • Binders can be selected from the group, but are not limited to, methylcellulose, sodium carboxymethycellulose, calcium carboxymethycellulose, ethyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, silicified microcrystalline cellulose(SMCC), polyvinyl pyrrolidone, gelatine, polyvinyl alcohol, acacia, tragacanth, guar, pectin, starch paste, pre-gelatinized starch, alginic acid, compressible sugar, liquid glucose, dextrates, dextrin, dextrose, maltodextrin, guar gum, magnesium aluminium silicate, polymethacrylates, sorbitol and other materials known to one of ordinary skill in the art.
  • a preferred binder is polyvinylpyrrolidone.
  • a mixture of binders may also be used. The binder is preferably used in an amount of from about 2 to about 15% by weight.
  • Diluents may be water-soluble or water insoluble. Diluents can be selected from the group, but are not limited to, spray-dried or anhydrous lactose, sucrose, dextrose, starch, pre- gelatinized starch, mannitol, maltitol, sorbitol, xylitol, dextrin, cellulose derivatives including powdered cellulose, microcrystalline cellulose, dibasic calcium phosphate, tribasic calcium phosphate and calcium sulphate, kaolin, precipitated calcium carbonate, maltodextrin and other materials known to one of ordinary skill in the art.
  • a preferred diluent is mannitol.
  • a mixture of diluents may also be used. Mannitol is commercially available from under the brand name Pearlitol®. The diluent is preferably used in an amount of from about 10% to about 70% by weight.
  • Disintegrants can be selected from the group, but are not limited to, alginic acid, carboxymethylcellulose calcium, carboxymethyl cellulose, carboxymethylcellulose sodium, cross-linked sodium carboxymethylcellulose, low substituted hydroxypropyl cellulose, colloidal silicon dioxide, croscarmellose sodium, crospovidone, guar gum, magnesium aluminium silicate, microcrystalline cellulose, methyl cellulose, polyvinylpyrrolidone, cross- linked polyvinylpyrrolidones, polacrilin potassium, starch, pregelatinised starch, sodium alginate, sodium lauryl sulphate, sodium starch glycollate, crystalline cellulose, hydroxypropyl starch and other materials known to one of ordinary skill in the art.
  • the combination of above-mentioned disintegrants can also be used.
  • the preferred disintegrant is low substituted hydroxypropyl cellulose.
  • the disintegrant is preferably used in an amount of from about 5% to about 50% by weight.
  • Stabilizing agent can be selected from the group, but are not limited to, consisting of polysorbates, cellulose derivatives such as hydroxylpropylcellulose, hydroxylpropylmethylcellulose, poloxamers, carbomers, silicon dioxide, carbonates, sulfates phosphates, hydroxides of alkali and/o alkaline earth metals, sodium carboxymethyl cellulose, polyvinylpyrrolidone, Labrasol®, Gelucire®.
  • lecithin phosphatides
  • gum acacia cholesterol, tragacanth, carotenoids
  • polyoxyethylene alkyl ethers polyoxyethylene castor oil derivatives
  • polyoxyethylene sorbitan fatty acid esters polyoxyethylene stearates
  • mono and diglycerides colloidal silicon dioxide, sodium dodecylsulfate, magnesium aluminum silicate, triethanolamine, stearic acid, calcium stearate, glycerol monostearate, cetostearyl alcohol, cetomacrogol emulsifying wax, short and medium chain alcohols, Labrafil®, Purol-oleique®, polyvinyl alcohol and combinations thereof.
  • Lubricants can be selected from the group, but are not limited to, vegetable oils, such as hydrogenated vegetable oil or hydrogenated castor oil; polyethylene glycols, such as polyethylene glycol (PEG)-4000 and PEG-6000; stearic acid; derivatives of stearic acid, such as magnesium stearate, sodium stearate, calcium stearate, zinc stearate, glyceryl monostearate, glyceryl palmitostearate and sodium stearyl fumarate; mineral salts, such as talc; inorganic salts; organic salts, such as sodium benzoate, sodium acetate, sodium chloride and sodium oleate; and polyvinyl alcohols, microcrystalline cellulose, sodium lauryl sulphate, silica, colloidal silica, cornstarch, calcium silicate, magnesium silicate, silicon hydrogel and other materials known to one of ordinary skill in the art.
  • the preferred lubricant is sodium stearyl fumarate.
  • lubricant is
  • Glidants can be selected from the group, but are not limited to, colloidal silicon dioxide, colloidal silica, cornstarch, talc, calcium silicate, magnesium silicate, magnesium trisilicate, amorphous silica, colloidal silicon, silicon hydrogel, powdered cellulose, silicon dioxide, talc, tribasic calcium phosphate and other materials known to one of ordinary skill in the art. Glidants are used in an amount from about 1 to about 30 percent by weight. Preferably, from about 5 to about 15 percent by weight.
  • Fillers can be selected from the group, but are not limited to, calcium carbonate, calcium phosphate, calcium sulphate, carboxymethylcellulose calcium, carboxymethylcellulose sodium, compressible sugar, confectioner's sugar, dextrates, dextrin, dextrose, dibasic calcium phosphate dihydrate, dibasic calcium phosphate, fructose, glyceryl palmitostearate, glycine, hydrogenated vegetable oil-type 1, kaolin, lactose, maize starch, magnesium carbonate, magnesium oxide, maltodextrin, mannitol, microcrystalline cellulose, polymethacrylates, potassium chloride, powdered cellulose, pregelatinised starch, sodium chloride, sorbitol, starch, sucrose, sugar spheres, talc, tribasic calcium phosphate, and xylitol and other materials known to one of ordinary skill in the art.
  • Polymers can be selected from the group, but are not limited to, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, ethyl cellulose, hydroxypropylmethyl cellulose phthalate, hydroxypropylmethyl cellulose acetate succinate, cellulose acetate phthalate; methacrylic polymers, aminoalkyl methacrylate copolymer, methacrylic acid copolymer (e.g. Eudragit®), polyvinyl acetate phthalate and polyvinyl alcohol (PVA)
  • Plasticizer can be selected from the group, but are not limited to, Acetylated monoglycerides, Triethyl citrate, Acetyl triethyl citrate, Tributyl citrate, Acetyl tributyl citrate, Trioctyl citrate, Acetyl trioctyl citrate, Trihexyl citrate, Acetyl trihexyl citrate, Butyryl trihexyl citrate, Trimethyl citrate, PEG, Epoxidized vegetable oils, Bis(2-ethylhexyl)adipate, Dimethyl adipate, Monomethyl adipate, Dioctyl adipate, Dibutyl sebacate, Tributyl sebacate, Dibutyl maleate, Diisobutyl maleate.
  • Surfactants can be selected from the group, but are not limited to,also polyoxyethylene hardened castor oil, glyceryl monostearate, sorbitan monostearate, sorbitan monopalmitate, sorbitan monolaurate, polyoxyethylene polyoxypropylene block copolymers, polysorbates 80, sodium laurylsulfate, macrogols, sucrose esters of fatty acids and other materials known to one of ordinary skill in the art.
  • the preferred surfactant is sodium laurylsulfate.
  • surfactant is used in an amount of from about 0.1% to about 5% weight. A mixture of surfactants may also be used.
  • Dispersing agents or dispersants can be selected from the group, but are not limited to, colloidal silicon dioxide, talc, magnesium stearate and titanium dioxide and other materials known to one of ordinary skill in the art.
  • the preferred dispersing agent is colloidal silicon dioxide.
  • Preferably dispersing agent is used in an amount of from about 1 to about 5 percent by weight.
  • flavoring agents for the composition of the present invention are black current, sodium chloride, strawberry flavor, and peppermint flavor.
  • sweetners for the composition of the present invention include sucralose, acesulfame potassium and aspartame.
  • a combination of sweeteners and flavoring agents can also be used.
  • flavoring agents are used in an amount of from about 0.5 to about 5 percent by weight.
  • sweeteners are used in an amount of from about 1 to about 5 percent by weight.
  • Ibuprofen, MCC and Sodium lauryl sulfate is granulated using aqueous dispersion of Polyvinylpyrrolidone. Granules are then blended with MCC, Croscarmellose sodium, Colloidal silicon dioxide, lubricated with Magnesium stearate and the resulting mixture is then blendedwith mixture of MCC and Lactose monohydrate.
  • Famotidine Lactose monohydrate , MCC, Crosscarmellose sodium and Colloidal Silicondioxide is prepared and then lubricated with Magnesium stearate to form Famotidine part.
  • an aqueous dispersion of Famotidine containing Polysorbate 80, PEG 400, HPMC, Lactose monohydrate is prepared.
  • the aqueous dispersion of Famotidine is then coated over the Ibuprofen tablets and resulting tablets are finally coated with aqueous dispersion of Opadry Blue.
  • a mixture of Famotidine, MCC, Croscarmellose sodium and Lactose monohydrate is granulated using aqueous dispersion of Polyvinylpyrrolidone. Granules are then coated with OPADRY Clear.
  • mixture of Ibuprofen, MCC and Sodium lauryl sulfate is granulated using aqueous dispersion of Polyvinylpyrrolidone. Granules are then blended with MCC, Croscarmellose sodium, Colloidal silicon dioxide and lubricated with magnesium stearate to form ibuprofen part.
  • Ibuprofen DC 85 Colloidal Silicondioxideand Magnesiumstearateisblended to form
  • Ibuprofen part can be coated.
  • Famotidine, Lactose monohydrate, MCC,Crosscarmellose sodium and Colloidal Silicondioxide are blended thorougly and then lubricated with Magnesium stearate. Blend is compressed into tablet. The resulting tablets are coated with aqueous dispersion of a coating material to avoid physical contact.
  • Ibuprofen part and Famotidine tablets are filled into capsule.
  • Ibuprofen part can be coated.
  • mixture of Famotidine, Lactose monohydrate , MCC, Crosscarmellose sodium and Colloidal Silicondioxide is prepared and then lubricated with Magnesium stearate. Blend is compressed into tablet. The resulting tablets are coated with aqueous dispersion of a coating material to avoid physical contact.
  • Ibuprofen part and Famotidine tablets are filled into capsule.

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Abstract

La présente invention se rapporte à une forme galénique pharmaceutique orale comprenant un anti-inflammatoire non stéroïdien, notamment un dérivé de l'acide propionique comme l'ibuprofène, associé à un antagoniste du récepteur H2 de l'histamine, comme la famotidine, dans lequel le rapport ibuprofène/famotidine se situe dans la plage de 19/1 à 21/1 ou de 39/1 à 41/1, de préférence dans la plage de 20/1 à 40/1. La présente invention concerne la préparation de compositions pharmaceutiques stables contenant les principes actifs ibuprofène et famotidine.
PCT/TR2015/000153 2014-04-25 2015-04-16 Composition combinée d'ibuprofène et de famotidine ayant une stabilité améliorée WO2015163832A1 (fr)

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EP0474509A2 (fr) 1990-09-06 1992-03-11 Hoechst Celanese Corporation Méthode de purification de mélanges contenant l'ibuprofène
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WO1998025595A2 (fr) 1996-12-10 1998-06-18 The Boots Company Plc Agents therapeutiques
EP1289520A2 (fr) 2000-06-06 2003-03-12 Richter Gedeon Vegyeszeti Gyar R.T. Compositions pharmaceutique pour le traitement de la depression ou des symptomes de la depression
WO2003039532A1 (fr) 2001-11-02 2003-05-15 Cumberland Pharmaceuticals Inc. Composition pharmaceutique d'acide propionique 2-(4-isobutylphenyle)
US20050020671A1 (en) 2001-02-14 2005-01-27 Matilde Fernandez Ibanez Pharmaceutical formulation
WO2007012022A2 (fr) 2005-07-18 2007-01-25 Horizon Therapeutics, Inc. Forme posologique unitaire renfermant un melange d'ibuprofene et de famotidine
WO2008011426A2 (fr) 2006-07-18 2008-01-24 Horizon Therapeutics, Inc. Procédés et médicaments destinés à l'administration d'ibuprofène
WO2012173581A1 (fr) 2011-03-21 2012-12-20 Ak Kimya Ithalat-Ihracat Ve Sanayii A.S. Combinaisons de thiocolchicoside, étodolac et famotidine
WO2013054352A1 (fr) * 2011-08-17 2013-04-18 Cadila Healthcare Limited Compositions pharmaceutiques d'ibuprofène et de famotidine
US8449910B2 (en) 2007-11-30 2013-05-28 Horizon Pharma Usa, Inc. Stable compositions of famotidine and ibuprofen

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