WO2014125504A2 - Pharmaceutical compositions of febuxostat - Google Patents
Pharmaceutical compositions of febuxostat Download PDFInfo
- Publication number
- WO2014125504A2 WO2014125504A2 PCT/IN2014/000092 IN2014000092W WO2014125504A2 WO 2014125504 A2 WO2014125504 A2 WO 2014125504A2 IN 2014000092 W IN2014000092 W IN 2014000092W WO 2014125504 A2 WO2014125504 A2 WO 2014125504A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- tablet
- febuxostat
- acid
- weight
- immediate release
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
Definitions
- the invention relates to pharmaceutical compositions comprising febuxostat or a pharmaceutically acceptable salt thereof.
- Febuxostat is a xanthine oxidase inhibitor indicated for the chronic management of hyperuricemia in patients with gout, disclosed in U.S. Patent No. 5,614,520 assigned to Teijin. Its chemical name is 2-[3-cyano4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid, having the following structure:
- Febuxostat is marketed by Takeda under the trade name of ULORIC . It is available as oral tablets in strengths of 40mg and 80mg.
- U.S. Patent No. 6,225,474 assigned to Teijin disclose crystalline form A, B, C, D, G and an amorphous form of febuxostat.
- U.S. Patent No. 7,361 ,676 assigned to Teijin disclose tablet comprising crystal A of febuxostat having average particle diameter from 12.9 ⁇ to 26.2 ⁇ , and a disintegrating agent.
- the object of the present invention is to provide a solid oral dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof.
- the present invention provides an immediate release tablet comprising febuxostat, and an acid component in an amount of from 0.05% to 2% by weight of the tablet.
- the present invention provides an immediate release tablet dosage form comprising febuxostat crystalline Form H I , characterized by peaks in the powder x-ray diffraction spectrum having 2 ⁇ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ⁇ 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients.
- crystalline form H I of febuxostat having average particle diameter from 2 ⁇ to 10 ⁇ is used for preparing pharmaceutical composition.
- Tablet dosage form of the present invention is indicated for the chronic management of hyperuricemia in patients with gout.
- the present invention provides a solid dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof.
- solid dosage form includes tablets, capsules, granules, pills and lozenges meant for immediate release. Of these, tablets are most preferred.
- febuxostat as used herein according to the present invention includes febuxostat in the form of free base, in the form of a pharmaceutically acceptable salt thereof, amorphous febuxostat, crystalline febuxostat or any isomer, derivative, hydrate, solvate, or prodrug or combinations thereof.
- febuxostat is in crystalline Form HI , characterized by peaks in the powder x-ray diffraction spectrum having 2 ⁇ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ⁇ 0.2 degrees.
- the present invention provides an immediate release tablet comprising febuxostat, and an acid component and one or more pharmaceutically acceptable excipients.
- excipient means a pharmacologically inactive component such as a diluent, disintegrant, carrier, etc of a pharmaceutical product.
- the excipients that are useful in preparing a pharmaceutical composition are generally safe and non-toxic.
- Suitable "diluents” include, but are not limited to, either individually or in combination, lactose, microcrystalline cellulose, starch, corn starch, pregelatinized starch, maize starch, potato starch, powdered celluloses, sorbitol, xylitol, dibasic calcium phosphate, calcium phosphate, calcium carbonate, magnesium carbonate and the like. Of these, lactose and microcrystalline cellulose are preferably used. According to present invention lactose is used in an amount of more than 25% by
- Suitable "binders” include, but are not limited to, either individually or in combination, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, copovidone, pregelatinized starch, powdered acacia, gelatin, guar gum, carbomers and the like.
- Suitable "disintegrants” include, but are not limited to, either individually or in combination, croscarmellose sodium, polacrilin potassium, sodium starch glycolate, crospovidone, pregelatinized starch and the like.
- Suitable “acid components” include, but are not limited to, either individually or in combination, citric acid, fumaric acid, tartaric acid, ascorbic acid and the like.
- Puipose of adding an acid component is to impart acidic nature to the composition which consequently improves the bioavailability of febuxostat.
- An acid component of the present invention is used in an amount of 0.05% to 2% by weight of the tablet.
- Suitable “glidants” include, but are not limited to, either individually or in combination, colloidal silicon dioxide, magnesium silicate, magnesium trisilicate, talc, and other forms of silicon dioxide, such as aggregated silicates and hydrated silica. Of these, colloidal silicon dioxide is preferably used.
- Suitable "lubricants” include, but are not limited to, either individually or in combination, magnesium stearate, stearic acid, talc, fumaric acid, palmitic acid, sodium stearyl fumarate, carnauba wax, hydrogenated vegetable oils, mineral oil, polyethylene glycols. Of these, magnesium stearate is preferably used.
- One aspect of the present invention provides an immediate release tablet comprising febuxostat, and an acid component in an amount of from 0.05%> to 2% by weight of the tablet.
- Another aspect of the present invention provides an immediate release tablet dosage form comprising febuxostat, citric acid in an amount of 0.05% to 2% by weight, and lactose in an amount of more than 25% by weight of the tablet.
- a tablet of the present invention is provided with a film coating.
- the film coating composition comprises a film forming polymer and one or more excipients.
- film coating bases include polyvinyl alcohol (e.g., Opadry® II, commercially available from Colorcon, Inc.); polyvinylpyrrolidone, polyvinylalcol-polyethylene glycol graft-copolymers; cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose. Of these, polyvinyl alcohol base is preferably used.
- polyvinyl alcohol e.g., Opadry® II, commercially available from Colorcon, Inc.
- polyvinylpyrrolidone polyvinylalcol-polyethylene glycol graft-copolymers
- cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose.
- polyvinyl alcohol base is preferably used.
- the present invention provides tablet dosage form comprising febuxostat crystalline Form HI, characterized by peaks in the powder x-ray diffraction spectrum having 2 ⁇ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ⁇ 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients.
- particle size can affect the solubility properties of a pharmaceutical compound. Particle size reduction can increase a compound's dissolution rate and consequently its bioavailability.
- the present invention utilizes febuxostat of fine particle size, which has good solubility and is well suited for preparing pharmaceutical products.
- febuxostat has an average particle diameter from 1 ⁇ to 25 ⁇ . Particularly, the average particle diameter of febuxostat ranges from 2 ⁇ to 10 ⁇ .
- the drug particles of the desired particle size may be obtained by any of the conventional size reduction processes known in the art.
- the present invention also teaches method of preparing tablets by direct compression which involves sifting and blending the febuxostat and one or more excipients, followed by lubrication, and finally compressing into tablets.
- the present invention provides an immediate release tablet dosage form comprising febuxostat crystalline Form HI , characterized by peaks in the powder x-ray diffraction spectrum having 2 ⁇ angle positions at about 5.7, 7.9, 11.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ⁇ 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients; wherein febuxostat crystalline Form HI having average particle diameter from 2 ⁇ to 10 ⁇ ; and wherein the tablet is prepared by direct compression process.
- Tablet dosage form of the present invention is indicated for the chronic management of hyperuricemia in patients with gout.
- Table 1 Composition of Febuxostat prepared by direct compression process.
- microcrystalline cellulose, croscarmellose sodium, citric acid and colloidal silicon dioxide were sifted together through mesh #40, 3. materials of step no, 1 and 2 were sifted and blended,
- magnesium stearate was sifted through mesh #60
- step no. 3 was lubricated with magnesium stearate of step no. 4,
- step no. 6 tablets of step no. 6 were film coated with Opadry® II green.
- Dissolution Medium 0.05 M Potassium phosphate buffer pH 6.8 at 37 °C ⁇ 0.5°C
- Table 2 Composition of Febuxostat prepared by direct compression process.
- microcrystalline cellulose, crospovidone, fumaric acid and colloidal silicon dioxide were sifted together through mesh #40,
- step no. 1 and 2 materials of step no. 1 and 2 were sifted and blended
- magnesium stearate was sifted through mesh #60
- step no. 3 was lubricated with magnesium stearate of step no. 4, 6. lubricated blend of step no. 5 was compressed into tablets.
- step no. 6 tablets of step no. 6 were film coated with Opadry® II.
- Table 3 Composition of Febuxostat prepared by direct compression process.
- magnesium stearate was sifted through mesh #60
- step no. 3 was lubricated with magnesium stearate of step no. 4,
- step no. 5 lubricated blend of step no. 5 was compressed into tablets.
- step no. 6 tablets of step no. 6 were film coated with Opadry® II green. -
Abstract
The present invention relates to solid dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof. Particularly, the present invention relates to tablet compositions of febuxostat and process for their preparation.
Description
PHARMACEUTICAL COMPOSITIONS OF FEBUXOSTAT
PRIORITY
This patent application claims priority to Indian patent application number 703/CHE/2013, filed on February 18, 2013, the contents of which are incorporated by reference herein in their entirety.
FIELD OF THE DISCLOSURE
The invention relates to pharmaceutical compositions comprising febuxostat or a pharmaceutically acceptable salt thereof.
BACKGROUND
Febuxostat is a xanthine oxidase inhibitor indicated for the chronic management of hyperuricemia in patients with gout, disclosed in U.S. Patent No. 5,614,520 assigned to Teijin. Its chemical name is 2-[3-cyano4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid, having the following structure:
Febuxostat is marketed by Takeda under the trade name of ULORIC . It is available as oral tablets in strengths of 40mg and 80mg.
U.S. Patent No. 6,225,474 assigned to Teijin disclose crystalline form A, B, C, D, G and an amorphous form of febuxostat.
U.S. Patent No. 7,361 ,676 assigned to Teijin disclose tablet comprising crystal A of febuxostat having average particle diameter from 12.9 μηι to 26.2 μπι, and a disintegrating agent.
International publication No. WO 2012/038971 A l assigned to Hetero Research Foundation disclose febuxostat crystalline Form H 1 .
There is a need to develop tablet compositions comprising crystalline form of febuxostat using simplified process that were comparable with marketed ULORIC® tablets.
SUMMARY
The object of the present invention is to provide a solid oral dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof.
The present invention provides an immediate release tablet comprising febuxostat, and an acid component in an amount of from 0.05% to 2% by weight of the tablet.
Specifically, the present invention provides an immediate release tablet dosage form comprising febuxostat crystalline Form H I , characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ± 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients.
In one aspect, crystalline form H I of febuxostat having average particle diameter from 2μ to 10μ is used for preparing pharmaceutical composition.
Tablet dosage form of the present invention is indicated for the chronic management of hyperuricemia in patients with gout.
DETAILED DESCRIPTION
The present invention provides a solid dosage form comprising febuxostat or a pharmaceutically acceptable salt thereof.
The "solid dosage form" of the present disclosure includes tablets, capsules, granules, pills and lozenges meant for immediate release. Of these, tablets are most preferred.
The term "febuxostat" as used herein according to the present invention includes febuxostat in the form of free base, in the form of a pharmaceutically acceptable salt thereof, amorphous febuxostat, crystalline febuxostat or any isomer, derivative, hydrate, solvate, or prodrug or combinations thereof.
In a preferred aspect, febuxostat is in crystalline Form HI , characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ± 0.2 degrees.
The present invention provides an immediate release tablet comprising febuxostat, and an acid component and one or more pharmaceutically acceptable excipients.
The term "excipient" means a pharmacologically inactive component such as a diluent, disintegrant, carrier, etc of a pharmaceutical product. The excipients that are useful in preparing a pharmaceutical composition are generally safe and non-toxic. Suitable "diluents" include, but are not limited to, either individually or in combination, lactose, microcrystalline cellulose, starch, corn starch, pregelatinized starch, maize starch, potato starch, powdered celluloses, sorbitol, xylitol, dibasic calcium phosphate, calcium phosphate, calcium carbonate, magnesium carbonate and the like. Of these, lactose and microcrystalline cellulose are preferably used. According to present invention lactose is used in an amount of more than 25% by
Weight, preferably in the range of from 25% to 75% by weight, more preferably 35% to 65% by weight of the tablet.
Suitable "binders" include, but are not limited to, either individually or in combination, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, copovidone, pregelatinized starch, powdered acacia, gelatin, guar gum, carbomers and the like. Suitable "disintegrants" include, but are not limited to, either individually or in combination, croscarmellose sodium, polacrilin potassium, sodium starch glycolate, crospovidone, pregelatinized starch and the like.
Suitable "acid components" include, but are not limited to, either individually or in combination, citric acid, fumaric acid, tartaric acid, ascorbic acid and the like. Puipose of adding an acid component is to impart acidic nature to the composition which consequently improves the bioavailability of febuxostat.
An acid component of the present invention is used in an amount of 0.05% to 2% by weight of the tablet.
Suitable "glidants" include, but are not limited to, either individually or in combination, colloidal silicon dioxide, magnesium silicate, magnesium trisilicate, talc, and other forms of silicon dioxide, such as aggregated silicates and hydrated silica. Of these, colloidal silicon dioxide is preferably used.
Suitable "lubricants" include, but are not limited to, either individually or in combination, magnesium stearate, stearic acid, talc, fumaric acid, palmitic acid, sodium stearyl fumarate, carnauba wax, hydrogenated vegetable oils, mineral oil, polyethylene glycols. Of these, magnesium stearate is preferably used.
One aspect of the present invention provides an immediate release tablet comprising febuxostat, and an acid component in an amount of from 0.05%> to 2% by weight of the tablet. Another aspect of the present invention provides an immediate release tablet dosage form comprising febuxostat, citric acid in an amount of 0.05% to 2% by weight, and lactose in an amount of more than 25% by weight of the tablet.
In addition, a tablet of the present invention is provided with a film coating. The film coating composition comprises a film forming polymer and one or more excipients.
Suitable examples of film coating bases include polyvinyl alcohol (e.g., Opadry® II, commercially available from Colorcon, Inc.); polyvinylpyrrolidone, polyvinylalcol-polyethylene glycol graft-copolymers; cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose. Of these, polyvinyl alcohol base is preferably used.
In particular, the present invention provides tablet dosage form comprising febuxostat crystalline Form HI, characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ± 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients.
Further, it is well known that particle size can affect the solubility properties of a pharmaceutical compound. Particle size reduction can increase a compound's dissolution rate and consequently its bioavailability. The present invention utilizes febuxostat of fine particle size, which has good solubility and is well suited for preparing pharmaceutical products.
In one aspect, febuxostat has an average particle diameter from 1μ to 25μ. Particularly, the average particle diameter of febuxostat ranges from 2μ to 10μ. The drug particles of the desired particle size may be obtained by any of the conventional size reduction processes known in the art.
The present invention also teaches method of preparing tablets by direct compression which involves sifting and blending the febuxostat and one or more excipients, followed by lubrication, and finally compressing into tablets.
In particular, the present invention provides an immediate release tablet dosage form comprising febuxostat crystalline Form HI , characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 11.4, 12.6, 17.7,
20.4, 24.6 and 25.7 ± 0.2 degrees, citric acid in an amount of 0.05% to 2% by weight of the tablet and one or more pharmaceutically acceptable excipients; wherein febuxostat crystalline Form HI having average particle diameter from 2μ to 10μ; and wherein the tablet is prepared by direct compression process. Tablet dosage form of the present invention is indicated for the chronic management of hyperuricemia in patients with gout.
EXAMPLES
The following examples further describe and demonstrate particular embodiments within the scope of the present invention. The examples are given solely for illustration and are not to be constmed as limitations as many variations are possible without departing from spirit and scope of the invention.
Example 1 :
Table 1 : Composition of Febuxostat prepared by direct compression process.
Ingredients mg/ tab
Febuxostat (Form HI) 80.00
Lactose monohydrate 290.00
Microcrystalline cellulose 89.00
Croscarmellose sodium 25.00
Citric acid 1.00
Collodial sillicon dioxide 6.00
Magnesium stearate 9.00
Film coating
' Opadry® II green 85F510039 15.000
Purified water q.s.
Total tablet weight 515.000
Brief manufacturing process :
1. Febuxostat and lactose monohydrate were sifted together through mesh #40,
2. microcrystalline cellulose, croscarmellose sodium, citric acid and colloidal silicon dioxide were sifted together through mesh #40, 3. materials of step no, 1 and 2 were sifted and blended,
4. magnesium stearate was sifted through mesh #60,
5. blend of step no. 3 was lubricated with magnesium stearate of step no. 4,
6. lubricated blend of step no. 5 was compressed into tablets,
7. tablets of step no. 6 were film coated with Opadry® II green.
Study on dissolution time:
Dissolution Medium : 0.05 M Potassium phosphate buffer pH 6.8 at 37 °C±0.5°C
Volume 900 ml
Apparatus USP II (Paddle)
Speed 75 PM
% drug release at different time intervals
Time in minutes ULORIC® tablets Example- 1
5 89 83
10 99 94
15 100 96
30 100 98
45 101 98
Example 2:
Table 2: Composition of Febuxostat prepared by direct compression process.
Ingredients mg/ tab
Febuxostat (Form HI) 80.00
Lactose monohydrate 215.00
Microcrystalline cellulose 159.00
Crospovidone 25.00
Fumaric acid 1.00
Collodial sillicon dioxide 6.00
Magnesium stearate 9.00
Film coating
Opadry® II 15.000
Purified water q.s.
Total tablet weight 510.000
Brief manufacturing process:
1. Febuxostat and lactose monohydrate were sifted together through mesh #40,
2. microcrystalline cellulose, crospovidone, fumaric acid and colloidal silicon dioxide were sifted together through mesh #40,
3. materials of step no. 1 and 2 were sifted and blended,
4. magnesium stearate was sifted through mesh #60,
5. blend of step no. 3 was lubricated with magnesium stearate of step no. 4,
6. lubricated blend of step no. 5 was compressed into tablets.
7. tablets of step no. 6 were film coated with Opadry® II.
Example 3:
Table 3 : Composition of Febuxostat prepared by direct compression process.
Ingredients mg/ tab
Febuxostat 80.00
Lactose monohydrate 310.00
Microcrystalline cellulose 74.00
Sodium starch glycolate 25.00
Citric acid monohydrate 1.00
Collodial Sillicon Dioxide 6.00
Magnesium stearate 9.00
Film coating
Opadry® II green 85F510039, IH 15.000
Purified water , q.s.
Total tablet weight 520.00
Brief manufacturing process:
1. Febuxostat and lactose monohydrate were sifted together through mesh #40,
2. macrocrystalline cellulose, sodium starch glycolate, citric acid monohydrate and colloidal silicon dioxide were sifted together through mesh #40, 3. materials of step no. 1 and 2 were sifted and blended,
4. magnesium stearate was sifted through mesh #60,
5. blend of step no. 3 was lubricated with magnesium stearate of step no. 4,
6. lubricated blend of step no. 5 was compressed into tablets.
7. tablets of step no. 6 were film coated with Opadry® II green. -
Claims
WE CLAIM:
1. An immediate release tablet comprising febuxostat, and an acid component in an amount of from 0.05% to 2% by weight of the tablet.
2. The tablet of claim 1 , wherein said febuxostat is in the form of crystalline Form HI , characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 11.4, 12.6, 17.7, 20.4, 24.6 and 25.7 ± 0.2 degrees.
3. The tablet according to claim 1 , wherein said febuxostat is a crystalline polymorph having average particle diameter from 1 μ to 25μ, preferably 2μ to 10μ.
4. The tablet of claim 1 , wherein said acid component selected from cit-rjc acid, tartaric acid, fumaric acid, ascorbic acid and combinations thereof.
5. The tablet of claim 1 , further comprise lactose in an amount of more than 25% by weight of the tablet.
6. The tablet according to claim 1 , wherein the tablet is prepared by direct compression process. 7. The immediate release tablet according to claim 1, further comprise one or more other pharmaceutically acceptable excipients selected from diluents, binders, disintegrants, glidants, lubricants or combinations thereof.
8. An immediate release tablet comprising:
(a) febuxostat crystalline Form H I , characterized by peaks in the powder x-ray diffraction spectrum having 2Θ angle positions at about 5.7, 7.9, 1 1.4, 12.6, 17.7, 20.4,
24.6 and 25.7 ± 0.2 degrees,
(b) citric acid in an amount of 0.05% to 2% by weight of the tablet, and
(c) one or more pharmaceutically acceptable excipients;
wherein febuxostat crystalline Form HI having average particle diameter from 2μ to 10μ.
9. The tablet according to claim 8, is prepared by direct compression process and is further coated with a film coating composition. 10. The tablet of claim 1 and 8, is indicated for the chronic management of hyperuricemia in patients with gout.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN703/CHE/2013 | 2013-02-18 | ||
| IN703CH2013 | 2013-02-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2014125504A2 true WO2014125504A2 (en) | 2014-08-21 |
| WO2014125504A3 WO2014125504A3 (en) | 2014-12-04 |
Family
ID=51354640
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IN2014/000092 WO2014125504A2 (en) | 2013-02-18 | 2014-02-12 | Pharmaceutical compositions of febuxostat |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2014125504A2 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523633A (en) * | 2015-02-08 | 2015-04-22 | 长沙佰顺生物科技有限公司 | Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets |
| WO2018001569A1 (en) | 2016-06-30 | 2018-01-04 | Pharmathen S.A. | Pharmaceutical composition comprising a non-purine selective inhibitor of xanthine oxidase and method for the preparation thereof |
| CN109985016A (en) * | 2017-12-29 | 2019-07-09 | 江苏恒瑞医药股份有限公司 | A kind of controlled release composition of Febustat and preparation method thereof |
| WO2020048641A1 (en) | 2018-09-07 | 2020-03-12 | Pharmathen S.A. | Pharmaceutical composition comprising a magnesium oxide salt complex of febuxostat and method for the preparation thereof |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050043375A1 (en) * | 2002-03-28 | 2005-02-24 | Michio Iwai | Solid preparation containing single crystal form |
| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| US20110311620A1 (en) * | 2010-06-16 | 2011-12-22 | Takeda Pharmaceuticals North America, Inc. | Novel modified release dosage forms of xanthine oxidoreductase inhibitor or xanthine oxidase inhibitors |
| WO2012038971A2 (en) * | 2010-09-24 | 2012-03-29 | Hetero Research Foundation | Novel polymorphs of febuxostat |
| WO2012153313A1 (en) * | 2011-05-11 | 2012-11-15 | Ranbaxy Laboratories Limited | Pharmaceutical composition of febuxostat |
| WO2012172461A1 (en) * | 2011-06-13 | 2012-12-20 | Ranbaxy Laboratories Limited | Pharmaceutical compositions of febuxostat |
-
2014
- 2014-02-12 WO PCT/IN2014/000092 patent/WO2014125504A2/en active Application Filing
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050043375A1 (en) * | 2002-03-28 | 2005-02-24 | Michio Iwai | Solid preparation containing single crystal form |
| CN101780073A (en) * | 2009-01-21 | 2010-07-21 | 重庆圣华曦药业有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
| US20110311620A1 (en) * | 2010-06-16 | 2011-12-22 | Takeda Pharmaceuticals North America, Inc. | Novel modified release dosage forms of xanthine oxidoreductase inhibitor or xanthine oxidase inhibitors |
| WO2012038971A2 (en) * | 2010-09-24 | 2012-03-29 | Hetero Research Foundation | Novel polymorphs of febuxostat |
| WO2012153313A1 (en) * | 2011-05-11 | 2012-11-15 | Ranbaxy Laboratories Limited | Pharmaceutical composition of febuxostat |
| WO2012172461A1 (en) * | 2011-06-13 | 2012-12-20 | Ranbaxy Laboratories Limited | Pharmaceutical compositions of febuxostat |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523633A (en) * | 2015-02-08 | 2015-04-22 | 长沙佰顺生物科技有限公司 | Topiroxostat dispersible tablets and preparation method of topiroxostat dispersible tablets |
| WO2018001569A1 (en) | 2016-06-30 | 2018-01-04 | Pharmathen S.A. | Pharmaceutical composition comprising a non-purine selective inhibitor of xanthine oxidase and method for the preparation thereof |
| CN109985016A (en) * | 2017-12-29 | 2019-07-09 | 江苏恒瑞医药股份有限公司 | A kind of controlled release composition of Febustat and preparation method thereof |
| CN109985016B (en) * | 2017-12-29 | 2021-07-27 | 江苏恒瑞医药股份有限公司 | Controlled release composition of febuxostat and preparation method thereof |
| WO2020048641A1 (en) | 2018-09-07 | 2020-03-12 | Pharmathen S.A. | Pharmaceutical composition comprising a magnesium oxide salt complex of febuxostat and method for the preparation thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2014125504A3 (en) | 2014-12-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2744432C2 (en) | Pharmaceutical composition including janus kinase inhibitor or pharmaceutically acceptable salt thereof | |
| US9770437B2 (en) | Compositions of eltrombopag | |
| EP2051694B1 (en) | Pharmaceutical compositions comprising aripiprazole | |
| WO2015124995A1 (en) | Solid dosage forms of rivaroxaban | |
| WO2014125504A2 (en) | Pharmaceutical compositions of febuxostat | |
| WO2019073331A2 (en) | Pharmaceutical compositions of apremilast | |
| TW201442712A (en) | Formulations of organic compounds | |
| JP2013502452A (en) | Otyronium direct compression tablets | |
| JP2024009815A (en) | Pharmaceutical compositions comprising axitinib | |
| JP4870402B2 (en) | Method for producing pranlukast hydrate-containing tablets | |
| WO2019116386A1 (en) | Oral pharmaceutical compositions of amorphous apremilast and process for preparing thereof | |
| EP2780001A2 (en) | Fast release solid oral compositions of entecavir | |
| WO2014115082A1 (en) | Pharmaceutical formulations of imatinib | |
| WO2014122671A2 (en) | Solid oral compositions of saxagliptin | |
| EP3669867A1 (en) | Pharmaceutical composition comprising ibrutinib | |
| WO2017093890A1 (en) | Clobazam tablet formulation and process for its preparation | |
| JP5744412B2 (en) | Furosemide formulation | |
| WO2019206472A1 (en) | Tablet compositions comprising abiraterone acetate | |
| JP2020090484A (en) | Medicine tablet comprising erlotinib as active principle | |
| US20200171025A1 (en) | Pharmaceutical composition comprising brexpiprazole and process for preparation thereof | |
| JP2021518422A (en) | Pharmaceutical composition containing lenalidomide | |
| JP2019065006A (en) | Solid preparation containing tadalafil improved in productivity and uniformity, and production method thereof | |
| US20230073216A1 (en) | Pharmaceutical Compositions of Raltegravir | |
| US10688050B1 (en) | Pharmaceutical composition comprising ibrutinib | |
| KR20180063645A (en) | Tablet comprising Metformin and HMG-CoA reductase inhibitor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 121 | Ep: the epo has been informed by wipo that ep was designated in this application |
Ref document number: 14751443 Country of ref document: EP Kind code of ref document: A2 |
|
| 122 | Ep: pct application non-entry in european phase |
Ref document number: 14751443 Country of ref document: EP Kind code of ref document: A2 |