WO2010131265A1 - Novel pharmaceutical compositions of choline fenofibrate - Google Patents
Novel pharmaceutical compositions of choline fenofibrate Download PDFInfo
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- WO2010131265A1 WO2010131265A1 PCT/IN2010/000298 IN2010000298W WO2010131265A1 WO 2010131265 A1 WO2010131265 A1 WO 2010131265A1 IN 2010000298 W IN2010000298 W IN 2010000298W WO 2010131265 A1 WO2010131265 A1 WO 2010131265A1
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- choline fenofibrate
- controlled release
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- pharmaceutical composition
- fenofibrate
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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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
- A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
- A61K9/2846—Poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
Abstract
A controlled release pharmaceutical composition(s) comprising choline fenofibrate wherein the core comprises choline fenofibrate and auxiliary excipient and a coating layer comprising rate controlling agent(s). A controlled release pharmaceutical composition(s) comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agent(s). A controlled release pharmaceutical composition(s) comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s) which is bioequivalent to commercially available choline fenofibrate (Trilipix®) formulations.
Description
NOVEL PHARMACEUTICAL COMPOSITIONS OF CHOLINE FENOFIBRATE
FIELD OF THE INVENTION
The present invention relates to novel solid oral pharmaceutical compositions of choline fenofibrate. The invention also relates to a process for the preparation of said compositions of choline fenofibrate.
BACKGROUND OF THE INVENTION
Fenofibrate is a well-known lipid-regulating agent, which has been commercially available for a long time. Fenofibrate is usually orally administered. After its absorption, which is known to take place in the duodenum and other parts of the gastrointestinal tract, fenofibrate is metabolized in the body to fenofibric acid. Fenofibric acid represents the active ingredient of fenofibrate, which is a prodrug and which is converted in vivo to the active molecule. After oral administration of fenofibrate, fenofibric acid is found in plasma.
The fenofibrate products currently on the market involve a formulation comprising a micronized drug substance in capsules and/or tablets. Fenofibrate is known to be nearly insoluble in water.
However the salts of fenofibric acid are highly soluble in water and are more bioavailable as compared to the fenofibrate.
Choline fenofibrate is marketed under the brand name Trilipix ©delayed release oral capsules containing 45mg or 135 mg of fenofibric acid.
US 7,259,186 disclose various salts of fenofibrate and pharmaceutical formulations, which essentially have an enteric binder.
US 2008/0095851 A1 discloses nanoparticulate compositions of fenofibrate salts.
US 2008/0152714 A1 discloses modified release formulation comprising an active agent in a hydrophilic polymer matrix.
US 2007/0026062 A1 discloses solid dosage form comprising a solid dispersion or solid solution of fibrate.
Although above mentioned patents and patent applications provide various dosage forms, but production of dosage forms of these references is a lengthy, expensive process or requires specialized equipments or techniques.
There exists a need to develop a controlled release pharmaceutical composition comprising choline fenofibrate, which offers advantages like simple manufacturing process, compact dosage form, use of conventional manufacturing equipment, high throughput, easy scale-up, economic, etc.
Thus there still exists a need to develop a novel controlled release pharmaceutical composition comprising choline fenofibrate, wherein the release rate controlling agent is in the coating.
OBJECT OF THE INVENTION
The first object of the present invention provides controlled release pharmaceutical compositions comprising choline fenofibrate wherein the core comprises choline fenofibrate and auxiliary excipient and a coating layer comprising rate controlling agent(s).
Yet another object of the invention provides controlled release pharmaceutical compositions comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s).
Yet another object of the invention provides controlled release pharmaceutical compositions comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic
agents(s) and the core is devoid of hydrophilic polymers which are capable of forming a matrix.
Yet another object of the invention provides controlled release pharmaceutical compositions comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s) and the core is devoid of any enteric binder.
Yet another object of the invention provides controlled release pharmaceutical compositions comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s) and further an additional enteric coating.
Yet another object of the invention provides controlled release pharmaceutical compositions comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s) which is bioequivalent to commercially available choline fenofibrate (Trilipix®) formulations.
BRIEF DESCRIPTION OF THE DRAWINGS
Fig 1 (a) shows a release profile of controlled release dosage forms of choline fenofibrate of example 1 B, in pH 3.5 buffer followed by pH 6.8 Phosphate buffer, 50 rpm, USP Paddle.
Fig 1 (b) shows a release profile of controlled release dosage forms of choline fenofibrate of example 1 B, in pH 4.5 buffer followed by pH 6.8 Phosphate buffer, 50 rpm, USP paddle.
Fig 1 (c) shows a release profile of controlled release dosage forms of choline fenofibrate of example 1 B, in pH 6.8 buffer, 900 ml, USP paddle, 50 rpm.
DETAIL DESCRIPTION OF THE INVENTION
The dosage forms of the invention typically contain 25 to 200 mg equivalent to fenofibric acid.
The term "immediate release core" herein refers to core comprising choline fenofibrate thereof devoid of any release-controlling agent(s).
The term "controlled release compositions" herein refers to any composition or dosage form which comprises an active drug and which is formulated to provide a longer duration of pharmacological response after administration of the dosage form than is ordinarily experienced after administration of a corresponding immediate release composition comprising the same drug in the same amount. Controlled release compositions include, inter alia, those compositions described elsewhere as "extended release", "delayed release", "sustained release", "prolonged release", "programmed release", "time release" and/or "rate controlled" compositions or dosage forms.
The hydrophobic release controlling agents are selected from but are not limited to polyvinyl acetate dispersion, ethyl cellulose, cellulose acetate, cellulose propionate (lower, medium or higher molecular weight), cellulose acetate propionate, cellulose acetate butyrate, cellulose acetate phthalate, cellulose triacetate, poly (methyl methacrylate), poly (ethyl methacrylate), poly (butyl methacrylate), poly (isobutyl methacrylate), and poly (hexyl methacrylate), poly (isodecyl methacrylate), poly (lauryl methacrylate), poly (phenyl methacrylate), poly (methyl acrylate), poly (isopropyl acrylate), poly (isobutyl acrylate), poly (octadecyl acrylate), waxes such as beeswax, carnauba wax, paraffin wax, microcrystalline wax, and. ozokerite; fatty alcohols such as cetostearyl alcohol, stearyl alcohol, cetyl alcohol and myristyl alcohol, and fatty acid esters such as glyceryl monostearate; glycerol monooleate, acetylated monoglycerides, tristearin, tripalmitin, cetyl esters wax, glyceryl palmitostearate, glyceryl behenate, and hydrogenated vegetable oils.
The term "controlled release pharmaceutical compositions" includes a pharmaceutical composition that encompasses one or more individual coated units. The coated units may be a capsule or tablet or may be in form of granules, pellets, minitablets or beads.
The compositions of the present invention can also include other materials such as dissolution enhancing agents, binders, diluents, anti-adherents, glidants and lubricants.
Diluents may be, for example, any pharmaceutically acceptable, non-toxic diluent. Particular examples include lactose, dextrose, sucrose, maltose, starch, calcium hydrogen phosphate, mannitol and the like.
Binders may be, for example, starch, sugars, gums, low molecular weight hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose or the like.
Lubricants may be, for example, talc, magnesium stearate, calcium stearate, stearic acid, sodium stearyl fumarate, sodium benzoate or the like.
Antiadherents and Glidants may be, for example, colloidal silicon dioxide, talc or the like.
Solid oral dosage forms of the present invention may be prepared by any conventional techniques for example dry granulation, direct compression, wet granulation, and extrusion- spheronization. Wet granulation and extrusion-spheronization are the preferred techniques.
In the wet granulation method, choline fenofibrate and other auxiliary pharmaceutical ingredients are granulated with a granulating fluid (e.g., isopropyl alcohol, ethyl alcohol, and water) in a planetary mixer, high shear mixer, or fluidized bed granulator. The binder and organic acid solution is prepared in suitable vehicles, both can be mixed. Only binder or mixed solution of binder and organic acid can be used to granulate the powder mass. The wet granules are dried in an oven or fluidized bed dryer, and then sieved through a suitable screen to obtain free flowing granules. The resulting granules are blended with a suitable lubricant and glidant. These granules are compressed into solid dosage from of suitable size. These are further coated with the one or more hydrophobic controlling agent(s) effective for the controlled release of choline fenofibrate.
In extrusion-spheronization method, choline fenofibrate is geometrically mixed with water soluble inert material. The binder and organic acid solution is prepared in suitable vehicles, both can be mixed. Only binder or mixed solution of binder and organic acid is used to
granulate the blend of active material with water insoluble inert material. Then wet mass is extrudated using suitable extruder and spheronized using spheronizer. Pellets or spheroids thus obtained are dried and coated with release controlling hydrophobic controlling agent(s). The so-formed multiple units may be filled into hard shell capsules or compressed into a tablet.
The following examples illustrate various aspects of the present invention. These examples should not be construed as limiting the scope of the invention. Example 1 A
Brief Manufacturing Process Sifting & Dry mixing
Sift together choline fenofibrate, lactose and colloidal silicon dioxide through #30 mesh and mix in RMG
Granulation
Dissolve Hypromellose in water and add to the above dry mix under mixing, and continue mixing till granular mass of desired consistency is obtained
Drying
Dry the wet mass at a suitable temperature to get desired L.O.D.
Sizing
Mill the dried granules through #30 mesh.
Blending
Blend the dried granules with Lactose (extra granular), Colloidal silicon dioxide (extra granular) for 10 min and finally lubricate with Sodium stearyl fumarate for 5 min
Compression
Compress the above lubricated blend into mini tablets using suitable tooling.
Ethyl cellulose and PVP coating
Coat the mini tablets with the solution of Ethyl cellulose and PVP to a desired weight gain.
Example 1 B
The mini tablets can be prepared as per example 1A and can additionally have an enteric coating.
Eudragit coating: Above ethyl cellulose and PVP coated tablets were coated with Eudragit dispersion to give a 14 % w/w by preparing 20 % w/w dispersion in purified water.
Example 2A
Brief Manufacturing Process Sifting & Dry mixing
Sift together choline fenofibrate, lactose and colloidal silicon dioxide through #30 mesh and mix in RMG
Granulation
Dissolve PVP in water and add to the above dry mix under mixing, and continue mixing till granular mass of desired consistency is obtained
Drying Dry the wet mass at a suitable temperature to get desired L. O. D.
Sizing
Mill the dried granules through #30 mesh.
Blending
Blend the dried granules with Lactose (extra granular), Colloidal silicon dioxide (extra granular) for 10 min and finally lubricate with Sodium stearyl fumarate for 5 min
Compression
Compress the above lubricated blend into mini tablets using suitable tooling.
Ethyl cellulose and Lactose coating
Coat the mini tablets with the solution of Ethyl cellulose and Lactose to a desired weight gain.
Example 2 B
The mini tablets can be prepared as per Example 2A and can have an additional enteric coating.
Brief Manufacturing Process Sifting & Dry mixing
Sift together choline fenofibrate, lactose and colloidal silicon dioxide through #30 mesh and mix in RMG
Granulation Prepare Starch paste in water and add to the above dry mix under mixing, and continue mixing till granular mass of desired consistency is obtained
Drying
Dry the wet mass at a suitable temperature to get desired L. O. D.
Sizing Mill the dried granules through #30 mesh.
Blending
Blend the dried granules with Lactose (extra granular), Colloidal silicon dioxide (extra granular) for 10 min and finally lubricate with Sodium stearyl fumarate for 5 min
Compression
Compress the Above lubricated blend into mini tablets using suitable tooling.
Ethyl cellulose and PVP coating
Coat the mini tablets with the solution of Ethyl cellulose and PVP to a desired weight gain.
Example 3B
The mini tablets can be prepared as per example 3A and can have an additional enteric coating.
Sift together choline fenofibrate, lactose and colloidal silicon dioxide through #30 mesh and mix in RMG
Granulation
Prepare Starch paste in water and add to the above dry mix under mixing, and continue mixing till granular mass of desired consistency is obtained
Drying
Dry the wet mass at a suitable temperature to get desired L. O. D.
Sizing
Mill the dried granules through #30 mesh.
Blending
Blend the dried granules with Lactose (extra granular), Colloidal silicon dioxide (extra granular) for 10 min and finally lubricate with Sodium Stearyl Fumarate for 5 min
Compression
Compress the above lubricated blend into mini tablets using suitable tooling.
Coat the mini tablets with the solution of Ethyl acrylate methyl ethacrylate copolymer aqueous dispersion and HPMC coating to a desired weight gain.
Example 4B
The mini tablets can be prepared as per example 4A and can have an additional enteric coating.
Brief Manufacturing Process Sifting & Dry mixing
Sift together choline fenofibrate, dibasic calcium phosphate and colloidal silicon dioxide through #30 mesh and mix in RMG
Granulation
Dissolve PVP in water and add to the above dry mix under mixing, and continue mixing till granular mass of desired consistency is obtained
Drying Dry the wet mass at a suitable temperature to get desired L.O.D.
Sizing
Mill the dried granules through #30 mesh.
Blending
Lubricate the dried granules with Sodium Stearyl Fumarate and mix for 5 min. Compression
Compress the above lubricated blend into mini tablets using suitable tooling.
The mini tablets were coated with the solution of Ethyl cellulose and Lactose to a desired weight gain.
Example 5B
The mini tablets can be prepared as per example 5A and can have an additional enteric coating.
The term "bioequivalent" as used herein is intended to illustrate bioequivalence of the compositions of the present invention in comparison to the reference composition.
The term "reference composition" as used herein refers to the marketed preparation of
Choline fenofibrate which is sold under the trade name of Trilipix by Abbott.
Bioequivalence studies are conducted to demonstrate equivalence in the bioavailability of the active ingredient in different formulations.
The U.S. Food and Drug Administration (FDA) requires ANDA filers to show bioequivalence against the innovator's reference listed product before approval. Bioequivalence study involves statistical analysis for pharmacokinetic measures, such as area under the curve (AUC) and peak concentration (Cmax) for a test (T) and reference (R) drug product, where T and R can vary, depending on the comparison to be performed (e.g., to-be-marketed dosage form versus clinical trial material, generic drug versus reference listed drug, drug product changed after approval versus drug product before the change). Bioequivalence comparisons normally rely on (1) a criterion, (2) a confidence interval for the criterion, and (3) a predetermined bioequivalence limit. According to the FDA guidance, demonstration of bioequivalence involves the calculation of a 90% confidence interval for the ratio of the averages of the measures for the T and R products. To establish bioequivalence, the calculated confidence interval should fall within a limit of 80-125% for the ratio of the product averages. For a broad range of drugs, a bioequivalence limit of 80 to 125% for the ratio of the product averages has been adopted for use of a bioequivalence criterion. Generally, the bioequivalence limit of 80 to 125% is based on a clinical judgment that a test product with bioavailability measures outside this range should be denied market access.
In vivo test
A single dose, two way crossover bioequivalence studies was carried out and bioavailability of Example 1A of the present invention was compared with the bioavailability of the reference product (Trilipix 145 mg Capsule, Abbott) on 10 and 12 healthy subjects in standard fasting and fed conditions respectively.
Table 1 : Comparative pharmacokinetic data for composition of example 1A (T) and Trilipix ® under fasting conditions (n=10)
Table 2: Comparative pharmacokinetic data for composition of example 1A (T) and Trilipix ® under fed conditions (n=12)
Cmax= Maximum plasma concentration
AUCiast = Area under the plasma concentration vs. time curve from 0 hours to the time of last sample collected
AUC- = Area under the plasma concentration vs. time curve from 0 hours to infinity As is evident from Table 1 and Table 2, the composition of Example 1A is bioequivalent to the reference product under both fasting and fed conditions.
Claims
1. A controlled release pharmaceutical composition(s) comprising choline fenofibrate wherein the core comprises choline fenofibrate and auxiliary excipient and a coating layer comprising rate controlling agent(s).
2. A controlled release pharmaceutical composition(s) of claim 1 comprise(s) choline fenofibrate comprising an immediate release core, wherein the core is devoid of hydrophilic polymers which are capable of forming a matrix.
3. A controlled release pharmaceutical composition(s) of claim 1 comprise(s) choline fenofibrate comprising an immediate release core, wherein the core is devoid of any enteric binder.
4. A controlled release pharmaceutical composition(s) comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agent(s).
5. A controlled release pharmaceutical composition(s) comprising choline fenofibrate of claim 4, wherein the hydrophobic rate controlling agent(s) are selected from the group consisting of polyvinyl acetate dispersion, ethyl cellulose, cellulose acetate, cellulose propionate (lower, medium or higher molecular weight), cellulose acetate propionate, cellulose acetate butyrate, cellulose acetate phthalate, cellulose triacetate, poly (methyl methacrylate), poly (ethyl methacrylate), poly (butyl methacrylate), poly (isobutyl methacrylate), and poly (hexyl methacrylate), poly (isodecyl methacrylate), poly (lauryl methacrylate), poly (phenyl methacrylate), poly
(methyl acrylate), poly (isopropyl acrylate), poly (isobutyl acrylate), poly (octadecyl acrylate), waxes such as beeswax, carnauba wax, paraffin wax, microcrystalline wax, and. ozokerite; fatty alcohols such as cetostearyl alcohol, stearyl alcohol, cetyl alcohol and myristyl alcohol, and fatty acid esters such as glyceryl monostearate; glycerol monooleate, acetylated monoglycerides, tristearin, tripalmitin, cetyl esters wax, glyceryl palmitostearate, glyceryl behenate, and hydrogenated vegetable oils.
6. A controlled release pharmaceutical composition(s) comprising choline fenofibrate comprising an immediate release core wherein said core comprises choline fenofibrate, water soluble inert material with one or more auxiliary pharmaceutical excipient and a coating layer comprising rate controlling hydrophobic agents(s) which is bioequivalent to commercially available choline fenofibrate (Trilipix®) formulations.
7. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fasting conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean Cmax from about 5062.392 to about 8258.804 ng/ml.
8. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fed conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean Cmax from about 4432.864 to about 7738.208 ng/ml.
9. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fasting conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean AUQast from about 73573.383 to about 170959.600 ng/ml_*h.
10. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fed conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean AUC|as,from about 70844.844 to about 168518.265 ng/mL*h.
11. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fasting conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean AUC0--. from about 78492.577 to about 198882.560 ng/ml_*h.
12. A controlled release pharmaceutical composition(s) of claim 6 comprising choline fenofibrate which is bioequivalent under fed conditions to the commercially available choline fenofibrate capsule formulation, marketed under the brand name Trilipix® and exhibits a mean AUC0--. from about 79225.257 to about 196085.664 ng/ml_*h.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN724/KOL/2009 | 2009-05-11 | ||
| IN724KO2009 | 2009-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2010131265A1 true WO2010131265A1 (en) | 2010-11-18 |
Family
ID=42732802
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IN2010/000298 WO2010131265A1 (en) | 2009-05-11 | 2010-05-10 | Novel pharmaceutical compositions of choline fenofibrate |
Country Status (2)
| Country | Link |
|---|---|
| TR (1) | TR201111143T1 (en) |
| WO (1) | WO2010131265A1 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473909A (en) * | 2014-11-21 | 2015-04-01 | 哈尔滨圣吉药业股份有限公司 | Choline fenofibric acid sustained release pellets and preparation method thereof |
| CN105748445A (en) * | 2016-03-31 | 2016-07-13 | 武汉药谷生物工程有限公司 | Preparation method of choline fenofibrate acid sustained release capsule |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040058009A1 (en) * | 2002-05-24 | 2004-03-25 | Elan Pharma International, Ltd. | Nanoparticulate fibrate formulations |
| WO2006135480A2 (en) * | 2005-04-08 | 2006-12-21 | Abbott Laboratories | Oral pharmaceutical formulations comprising fenofibric acid and/or its salts |
| US20080051411A1 (en) * | 2002-12-17 | 2008-02-28 | Cink Russell D | Salts of Fenofibric Acid and Pharmaceutical Formulations Thereof |
| US20080152714A1 (en) * | 2005-04-08 | 2008-06-26 | Yi Gao | Pharmaceutical Formulations |
| WO2009057138A2 (en) * | 2007-10-29 | 2009-05-07 | Lupin Limited | Controlled release pharmaceutical compositions of tolterodine |
-
2010
- 2010-05-10 TR TR2011/11143T patent/TR201111143T1/en unknown
- 2010-05-10 WO PCT/IN2010/000298 patent/WO2010131265A1/en active Application Filing
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040058009A1 (en) * | 2002-05-24 | 2004-03-25 | Elan Pharma International, Ltd. | Nanoparticulate fibrate formulations |
| US20080051411A1 (en) * | 2002-12-17 | 2008-02-28 | Cink Russell D | Salts of Fenofibric Acid and Pharmaceutical Formulations Thereof |
| WO2006135480A2 (en) * | 2005-04-08 | 2006-12-21 | Abbott Laboratories | Oral pharmaceutical formulations comprising fenofibric acid and/or its salts |
| US20080152714A1 (en) * | 2005-04-08 | 2008-06-26 | Yi Gao | Pharmaceutical Formulations |
| WO2009057138A2 (en) * | 2007-10-29 | 2009-05-07 | Lupin Limited | Controlled release pharmaceutical compositions of tolterodine |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473909A (en) * | 2014-11-21 | 2015-04-01 | 哈尔滨圣吉药业股份有限公司 | Choline fenofibric acid sustained release pellets and preparation method thereof |
| CN105748445A (en) * | 2016-03-31 | 2016-07-13 | 武汉药谷生物工程有限公司 | Preparation method of choline fenofibrate acid sustained release capsule |
Also Published As
| Publication number | Publication date |
|---|---|
| TR201111143T1 (en) | 2012-05-21 |
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