DESC:TECHNICAL FIELD OF THE INVENTION
The present invention relates to an extended release pharmaceutical composition of Oxcarbazepine, wherein said composition does not contain pH-dependent soluble polymer. Particularly, the present invention relates to an extended release pharmaceutical composition of Oxcarbazepine comprising hydrophilic polymer and/or hydrophobic material and a process for preparing the same, wherein said composition does not contain pH-dependent soluble polymer.
BACKGROUND OF THE INVENTION
Oxcarbazepine is an anticonvulsant agent. Its chemical name is 10,11-Dihydro-10-oxo-5H-dibenz[b,f]-azepine-5-carboxamide. Oxcarbazepine has a molecular weight of 252.27 with the following structural formula:

The pharmacological activity of Oxcarbazepine is primarily exerted through the 10-monohydroxy metabolite (MHD) of Oxcarbazepine. The precise mechanism by which Oxcarbazepine and MHD exert their anti-seizure effect is unknown; however, in vitro electrophysiological studies indicate that they produce blockade of voltage-sensitive sodium channels, resulting in stabilization of hyperexcited neural membranes, inhibition of repetitive neuronal firing, and diminution of propagation of synaptic impulses. These actions are thought to be important in the prevention of seizure spread in the intact brain. In addition, increased potassium conductance and modulation of high-voltage activated calcium channels contribute to the anticonvulsant effects of the drug.
Oxcarbazepine and its pharmaceutically acceptable salts are described in German patent DE 2011087 which is incorporated herein by reference.
The Oxcarbazepine has been commercialized for over 15 years as an immediate release formulation, e.g. under the registered trademark Trileptal® and as an extended release formulation, e.g. under the registered trademark Oxtellar XR®. Oxcarbazepine is indicated for the treatment of partial-onset seizures with or without secondarily generalized tonic-clonic seizures, in both adults and children aged over 6 years, as monotherapy or adjunctive therapy.
U.S. Patent No. 7,722,898, discloses controlled release preparations of Oxcarbazepine and derivatives thereof comprising matrix of Oxcarbazepine, a matrix-forming polymer, a solubility enhancer and a release promoting agent comprising a polymer having pH-dependent solubility rate.
U.S. Patent No. 7,037,525 discloses Oxcarbazepine composition having improved bioavailability with a hydrophilic permeable outer coating.
U.S. Patent No. 6,296,873 discloses sustained-release delivery systems for carbamazepine and its derivatives like Oxcarbazepine.
PCT. Publication. No. 2015/063670 A1 discloses a solid oral modified-release composition comprising Oxcarbazepine by using a functional coating of rate-controlling excipient having pH-dependent solubility over the matrix core of Oxcarbazepine or salt thereof.
The inventors of the present invention have surprisingly found that an extended release pharmaceutical composition Oxcarbazepine composition formed by using hydrophilic polymer and/or hydrophobic material, the composition exhibiting improved bioavailability of Oxcarbazepine without using pH dependent soluble polymer. Further, the inventors of the present invention have also found that such composition of Oxcarbazepine has excellent storage stability and the process is cost effective.
SUMMARY OF THE INVENTION
The present invention provides an extended release pharmaceutical composition of Oxcarbazepine, wherein said composition does not contain pH-dependent soluble polymer.
In another embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine comprising hydrophilic polymer and/or hydrophobic material, wherein said composition does not contain pH-dependent soluble polymer.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine comprising hydrophilic polymer and/or hydrophobic material and one or more other excipients.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine comprising one or more excipients selected from group consisting of hydrophilic polymers, hydrophobic materials, diluents, binders, disintegrating agents, glidants and lubricants.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition comprising;
40% to 65% by weight of Oxcarbazepine,
5% to 40% by weight of hydrophilic polymers and/or hydrophobic material, and
10% to 40% by weight of one or more other excipients.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition comprising;
40% to 65% by weight of Oxcarbazepine,
2% to 40% by weight of hydrophilic polymers and/or
2% to 30% hydrophobic material, and
10% to 40% by weight of one or more other excipients.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition comprising;
40% to 65% by weight of Oxcarbazepine,
2% to 10% by weight of Hydroxypropyl methylcellulose,
2% to 5% by weight of Glyceryl dibehenate,
10% to 40% by weight of Silicified microcrystalline cellulose,
0.1% to 2% by weight of Colloidal silicon dioxide, and
0.1% to 2% by weight of Magnesium stearate.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition comprising;
40% to 65% by weight of Oxcarbazepine,
20% to 30% by weight of Vinyl pyrollidon vinyl acetate,
2% to 10% by weight of Hydroxypropyl methylcellulose,
10% to 30% by weight of Silicified microcrystalline cellulose,
0.1% to 2% by weight of Colloidal silicon dioxide, and
0.1% to 2% by weight of Magnesium stearate.
In yet another embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine and a process for preparing the same by using wet granulation or melt extrusion process.
In yet another embodiment, the present invention provides a process for the preparation of extended release pharmaceutical composition of Oxcarbazepine comprising;
a. Sifting and mixing Oxcarbazepine, hydrophilic polymer and/or hydrophobic material and other excipients,
b. Preparing granules or extrudates using wet granulation or melt extrusion, and
c. Adding other excipients and compressing into tablet.
In yet another embodiment, the present invention provides a process for the preparation of extended release pharmaceutical composition of Oxcarbazepine comprising;
a. Sifting the Oxcarbazepine, hydrophilic polymer and/or hydrophobic material and other excipients,
b. Preparing binder solution by dissolving binder in the water,
c. Granulating the mixture of step (a) with binder solution of step (b),
d. Drying the granules of step (c),
e. Pre-lubricating the granules of step (d),
f. Adding the lubricant to blend of step (e) and compressing into tablet, and
g. Coating the tablet with suitable coating material.
In yet another embodiment, the present invention provides a process for the preparation of extended release pharmaceutical composition of Oxcarbazepine comprising;
a. Passing the blend of Oxcarbazepine and hydrophilic polymer and/or hydrophobic material through hot melt extruder,
b. Milling the extrudates of step (a),
c. Adding other excipients to extrudates of step (b),
d. Adding the lubricant to blend of step (c) and compressing into tablet, and
e. Coating the tablet with suitable coating material.
BRIEF DESCRIPTION OF THE DRAWINGS
Figure 01: Comparative dissolution data of Oxtellar XR® and Oxcarbazepine tablet prepared as per the compositions of example 1.
Figure 02: Comparative dissolution data of Oxtellar XR® and Oxcarbazepine tablet prepared as per the compositions of example 2.
Figure 03: Comparative dissolution data of Oxtellar XR® and Oxcarbazepine tablet prepared as per the compositions of example 3.
DETAILED DESCRIPTION OF THE INVENTION
The present invention provides an extended release pharmaceutical composition of Oxcarbazepine, wherein the said composition does not contain pH-dependent soluble polymer.
The compositions described herein may be prepared by techniques using wet granulation, direct compression and hot melt extrusion process.
In one embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine and a process for the preparing the same by using wet granulation process.
In one embodiment, the present invention provides an extended release pharmaceutical composition of Oxcarbazepine and a process for the preparing the same by using hot melt extrusion.
The term “hot melt extrusion” (HME) is the process of applying heat and pressure to melt a excipient and force it though an orifice in a continuous process.
As used herein, the term "comprising" means that the various components, ingredients, or steps, conjointly employed in practicing the present invention. Accordingly, the term "comprising" encompasses the more restrictive terms "consisting essentially of" and "consisting of"
The term “Oxcarbazepine” as used herein refers to 10,11-Dihydro-10-oxo-5H-dibenz[b,f]-azepine-5-carboxamide or its salts, solvates, prodrugs, hydrates, enantiomers or polymorphs thereof.
The extended release composition comprises Oxcarbazepine in an amount of about 10% to about 80% by weight; specifically in an amount of about 20% to 70% by weight; more specifically about 40% to about 65% by weight.
Hydrophilic polymers include, but are not limited to hydroxypropyl methylcellulose, hydroxypropyl cellulose, a polyethylene glycol, polyvinyl acetate and polyvinylcaprolactame-based graft copolymer (Soluplus®), vinylpyrrolidone-vinyl acetate copolymer (Kollidon® VA 64), Polyvinylpyrrolidone (Kollidon®), poly ethylene-co-vinyl acetate, homopolymers and co-polymers of N-vinyl lactams, dextrins, carboxymethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, sodium carboxymethylcellulose and carboxymethylcellulose calcium.
The extended release composition comprise Hydrophilic polymers an amount of about 2% to about 80% by weight; specifically in an amount of about 2% to 50% by weight; more specifically 2% to 40% by weight.
Hydrophobic material include, but are not limited to ethyl cellulose, polyvinyl acetate, waxes, such as, beeswax, carnauba wax, microcrystalline wax, candelilla wax, spermaceti, montan wax, hydrogenated vegetable oil, hydrogenated castor powder (Kolliwax® HCO), lecithin, hydrogenated cottonseed oil, hydrogenated tallow, paraffin wax, shellac wax, petrolatum, ozokerite, synthetic waxes, fatty acids, fatty alcohols, fatty acid esters, glyceryl monostearate, glycerol monooleate, acetylated monoglycerides, tristearin, tripalmitm, cetyl esters wax, glyceryl palmitostearate and glyceryl dibehenate (Compritol® 888 ATO); vegetable oil, such as, hydrogenated castor oil and mineral oil.
The extended release composition comprise hydrophobic materials, an amount of about 2% to about 50% by weight; specifically in an amount of about 2% to about 40% by weight; more specifically 2% to 30% by weight.
The pharmaceutical composition further comprise one or more pharmaceutically acceptable excipients selected from a group consisting of diluents, binders, disintegrants, glidants and lubricants or any other excipients known in the art.
Diluents include, but are not limited to corn starch, lactose, sucrose, sugar compressible, glucose, sorbitol, calcium carbonate, calcium phosphate-dibasic, calcium phosphate-tribasic, calcium sulfate, microcrystalline cellulose, silicified microcrystalline cellulose, cellulose powdered, hydroxypropyl methylcellulose, hydroxypropyl cellulose, dextrates, dextrins, dextrose, fructose, kaolin, lactitol, mannitol, starch and pregelatinized starch.
The extended release composition comprise diluents, an amount of about 10% to about 50% by weight; specifically in an amount of about 10% to about 40% by weight; more specifically 10% to 30% by weight.
Binders include, but are not limited to polyvinylpyrrolidone, starch mucilage, pregelatinized starch, sodium alginate, alginic acid, acacia mucilage, tragacanth, hydroxypropyl methylcellulose, carboxymethylcellulose sodium, carboxymethylcellulose calcium, cellulose, ethyl cellulose, polyethylene glycol, hydroxyethyl cellulose, hydroxy propyl cellulose, methyl cellulose, polymethacrylates, carboxyvinyl polymers and carbopols.
The extended release composition comprise binders, an amount of about 0.1% to about 5% by weight; specifically in an amount of about 0.1% to about 4% by weight; more specifically 0.1% to 3% by weight.
Disintegrants include, but are not limited to cross-linked polyvinylpyrrolidone, sodium starch glycolate, cross-linked sodium carboxymethyl cellulose (croscarmellose sodium), silicified microcrystalline cellulose, microcrystalline cellulose, calcium carboxymethyl cellulose, alginic acid and alginates, pregelatinised starch, starch and starch derivatives, hydroxypropyl methylcellulose and hydroxypropyl cellulose.
The extended release composition comprise disintegrants, an amount of about 1% to about 10% by weight; specifically in an amount of about 1% to about 7% by weight; more specifically 1% to 5% by weight.
Lubricants and glidants include, but are not limited to colloidal silicon dioxide, anhydrous silica, stearic acid, magnesium stearate, calcium stearate, talc or mixtures thereof.
The extended release composition comprise lubricants and glidants, an amount of about 0.1% to about 5% by weight; specifically in an amount of about 0.1% to about 4% by weight; more specifically 0.5% to 4% by weight.
The present invention further provides pharmaceutical composition that includes therapeutically effective amount of Oxcarbazepine, wherein the composition is in the form of tablets, dispersible tablets, capsules, granules, beads and pellets. Particularly, the compositions of the present invention are formulated into tablets, capsules or dispersible tablets. Further, the tablets are film-coated.
The tablets are coated using a sugar-based agent, an agent for water-soluble film-coating base, enteric film-coating agent or a modified release film-coating agent, preferably film coating.
The film coating comprises coating materials which include polymers such as hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, ethyl cellulose, povidone and copovidone, graft copolymers of polyethylene glycol and polyvinyl alcohol, shellac, polymers of methacrylic acid or methacrylic acid esters, methacrylic acid- methyl acrylate copolymers, plasticizers such as propylene glycols, polyethylene glycols, glycerol triacetate, triethyl citrate, antitacking agents such as talc, glycerol monostearate , magnesium stearate and colorants or pigments such as titanium dioxide and/or iron oxides such as yellow iron oxide, red iron oxide and black iron oxide.
Preferred coatings are Opadry® II Brown (Polyvinyl Alcohol; Polyethylene Glycol, Titanium Dioxide; Talc, Yellow Iron Oxide and Red Iron Oxide), Opadry® White (Hypromellose, Talc & Titanium dioxide), Opadry® Yellow (Hypromellose, Talc, Titanium dioxide & Iron oxide yellow), Opadry® Pink (Hypromellose, Titanium dioxide, Talc, Iron oxide red and Iron oxide yellow), Opadry® II pink (Polyvinyl alcohol, Polyethylene glycol, Titanium dioxide, Talc, Red iron oxide and Yellow iron oxide), WincoatTM WT-19012P Brown (Polyvinyl alcohol, Polyethylene glycol 3350, Titanium dioxide, Talcum, Red iron oxide, Black Iron Oxide and Yellow iron oxide), WincoatTM WT-19049P Brown (Polyvinyl alcohol, Polyethylene glycol 3350, Titanium dioxide, Talcum and Red iron oxide), WincoatTM WT-18033P Yellow (Polyvinyl alcohol, Polyethylene glycol 3350, Titanium dioxide, Talcum and Yellow iron oxide).
In an embodiment, the present invention provides an extended release pharmaceutical composition comprising Oxcarbazepine in an amount of about 40% to about 65% by weight, hydroxypropyl methylcellulose in an amount of about 2% to about 10% by weight, glyceryl dibehenate in an amount of about 2% to about 5% by weight, silicified microcrystalline cellulose in an amount of about 10 % to about 40% by weight, colloidal silicon dioxide in an amount of about 0.1 % to about 2% by weight, and magnesium stearate in an amount of about 0.1% to about 2% by weight.
In another embodiment, the present invention provides an extended release pharmaceutical composition comprising Oxcarbazepine in an amount of about 40% to about 65% by weight, vinyl pyrollidon vinyl acetate in an amount of about 20% to about 30% by weight, hydroxypropyl methylcellulose in an amount of about 2% to about 10% by weight, silicified microcrystalline cellulose in an amount of about 10 % to about 30% by weight, colloidal silicon dioxide in an amount of about 0.1 % to about 2% by weight, and magnesium stearate in an amount of about 0.1% to about 2% by weight.
The invention now will be described in particularity with the following illustrative examples; however, the scope of the present invention is not intended to be, and shall not be, limited to the exemplified embodiments below:
Examples
Example 1
SR. NO Ingredients Quantity (mg/tablet)
01 Oxcarbazepine 600.00
02 Vinyl pyrollidon vinyl acetate 250.00
Pre-lubrication
03 Hydroxypropyl methylcellulose 25.00
04 Silicified microcrystalline cellulose 125.00
05 Colloidal silicon dioxide 5.00
Lubrication
06 Magnesium stearate 5.00
Tablet weight (Core) 1010.00
Coating
07 Opadry® II Brown 20.00
Tablet weight (Coated) 1030.00
Manufacturing procedure:
a. Oxcarbazepine and vinyl pyrollidon vinyl acetate were weighed and processed using hot melt extruder,
b. Extrudates obtained in step (a) were milled and sized which was followed by addition of hydroxypropyl methylcellulose, silicified microcrystalline cellulose and colloidal silicon dioxide,
c. Magnesium stearate was added to blend obtained in step (b) and compressed into a tablet, and
d. Tablets of step (c) were further coated.
Comparison of in-vitro dissolution profile of example 1 composition with reference product:
The tablets of Oxcarbazepine prepared as per the compositions of example 1 and reference product Oxtellar XR® were subjected to dissolution studies in 900 ml of water with 0.5% SLS at 37 °C ± 0.5 °C using USP apparatus II with paddle speed at 50 rpm and the data is shown in Table 1.
Table 1
Time Hrs Oxtellar XR® 600 mg (Percentage Drug Released) Oxcarbazepine tablets as per example 1 (Percentage Drug Released)
0 00 00
1 5.67 18.77
2 15.08 38.16
3 25.41 49.92
4 36.05 54.33
5 46.86 57.92
6 56.8 60.06
8 70.84 64.39
10 70.36 67.83
12 76.48 71.39
16 77.85 74.9

Example 2
SR. NO Ingredients Quantity (mg/tablet)
Dry Mix
01 Oxcarbazepine 600.00
02 Silicified microcrystalline cellulose 270.00
03 Hydroxypropyl methylcellulose 85.00
04 Glyceryl dibehenate 30.00
Binder
05 Hydroxypropyl methylcellulose 5.00
06 Purified water QS
Pre-lubrication
07 Hydroxypropyl methylcellulose 10.00
08 Colloidal silicon dioxide 5.00
Lubrication
09 Magnesium stearate 5.00
Tablet weight (Core) 1010.00
Coating
10 WincoatTM WT-19012P Brown 20.00
11 Purified water QS
Tablet weight (Coated) 1030.00
Manufacturing procedure:
a. Oxcarbazepine, silicified microcrystalline cellulose, glyceryl behnate and hydroxypropyl methylcellulose were mixed in rapid mixer granulator for 10 minutes,
b. Hydroxypropyl methylcellulose was dissolved in purified water,
c. The dry mix of step (a) was granulated using step (b) binder solution,
d. The granules of step (c) were dried and milled,
e. Hydroxypropyl methylcellulose and colloidal silicon dioxide were mixed with granules of step (d) for 10 minutes,
f. Magnesium stearate was then mixed with blend of step (e) for 5 minutes and compressed into a tablet, and.
g. Tablets of step (f) were further coated.
Comparison of in-vitro dissolution profile of example 2 composition with reference product:
The tablets of Oxcarbazepine prepared as per the compositions of example 2 and reference product Oxtellar XR® were subjected to dissolution studies in 900 ml of water with 1% SLS at 37 °C ± 0.5 °C using USP apparatus II with paddle speed at 50 rpm and the data is shown in Table 2.
Table 2
Time Hrs Oxtellar XR® 600 mg (Percentage Drug Release) Oxcarbazepine tablets as per example 2 (Percentage Drug Release)
0 0.0 0.0
1 13.9 10.3
2 29.6 21.6
3 46.6 32.7
4 62.8 42.9
5 77.6 52.2
6 89.4 60.7
8 96.1 75.1
10 97.0 84.8
12 98.5 92.1
16 99.2 99.2

Example 3
SR. NO Ingredients Quantity (mg/tablet)
Dry Mix
01 Oxcarbazepine 600.00
02 Silicified microcrystalline cellulose 305.00
03 Hydroxypropyl methylcellulose 50.00
04 Glyceryl dibehenate 30.00
Binder
05 Hydroxypropyl methylcellulose 5.00
06 Purified Water QS
Prelubrication
07 Hydroxypropyl methylcellulose 10.00
08 Colloidal silicon dioxide 5.00
Lubrication
09 Magnesium stearate 5.00
Tablet weight (Core) 1010.00
Coating
10 WincoatTM WT-19012P Brown 20.00
11 Purified water QS
Tablet weight (Coated) 1030.00
Manufacturing procedure:
a. Oxcarbazepine, silicified microcrystalline cellulose, glyceryl behnate and hydroxypropyl methylcellulose were mixed in rapid mixer granulator for 10 minutes,
b. Hydroxypropyl methylcellulose was dissolved in purified water,
c. The dry mix of step (a) was granulated using step (b) binder solution,
d. The granules of step (c) were dried and milled,
e. Hydroxypropyl methylcellulose and colloidal silicon dioxide were mixed with granules of step (d) for 10 Minutes,
f. Magnesium stearate was then mixed with blend of step (e) for 5 minutes and compressed into a tablet, and.
g. Tablets of step (f) were further coated.
Comparison of in-vitro dissolution profile of example 3 composition with reference product:
The tablets of Oxcarbazepine prepared as per the compositions of example 3 and reference product Oxtellar XR® were subjected to dissolution studies in 900 ml of water with 1% SLS at 37 °C ± 0.5 °C using USP apparatus II with paddle speed at 50 rpm and the data is shown in table 3
Table 3
Time Hrs Oxtellar XR® 600 mg (Percentage Drug Release) Oxcarbazepine tablets as per example 2 (Percentage Drug Release)
0 0.0 0.0
1 13.9 12.0
2 29.6 25.8
3 46.6 39.0
4 62.8 50.4
5 77.6 60.3
6 89.4 68.8
8 96.1 82.4
10 97.0 91.5
12 98.5 97.0
16 99.2 99.7

Example 4
SR. NO Ingredients Quantity (mg/tablet)
01 Oxcarbazepine 600.00
02 Hydrogenated castor powder 300.00
Pre-lubrication
03 Hydroxypropyl methylcellulose 25.00
04 Silicified microcrystalline cellulose 75.00
05 Colloidal silicon dioxide 5.00
Lubrication
06 Magnesium stearate 5.00
Tablet weight (Core) 1010.00
Coating
07 Opadry® II Brown 20.00
Tablet weight (Coated) 1030.00
Manufacturing procedure:
a. Oxcarbazepine and hydrogenated castor powder were weighed and processed using hot melt extruder,
b. Extrudates obtained in step (a) were milled and sized which was followed by addition of hydroxypropyl methylcellulose, silicified microcrystalline cellulose and colloidal silicon dioxide,
c. Magnesium stearate was added to blend obtained in step (b) and compressed into a tablet, and
d. Tablets of step (c) were further coated.
Example 5
SR. NO Ingredients Quantity (mg/tablet)
01 Oxcarbazepine 600.00
02 Glyceryl dibehenate 300.00
Pre-lubrication
03 Hydroxypropyl methylcellulose 25.00
04 Silicified microcrystalline cellulose 75.00
05 Colloidal silicon dioxide 5.00
Lubrication
06 Magnesium stearate 5.00
Tablet weight (Core) 1010.00
Coating
07 Opadry® II Brown 20.00
Tablet weight (Coated) 1030.00
Manufacturing procedure:
a. Oxcarbazepine and glyceryl dibehenate were weighed and processed using hot melt extruder,
b. Extrudates obtained in step (a) were milled and sized which was followed by addition of hydroxypropyl methylcellulose, silicified microcrystalline cellulose and colloidal silicon dioxide,
c. Magnesium stearate was added to blend obtained in step (b) and compressed into a tablet, and
d. Tablets of step (c) were further coated. ,CLAIMS:We Claim:
1. An extended release pharmaceutical composition of Oxcarbazepine, wherein said composition does not contain pH-dependent soluble polymer.
2. The composition as claimed in claim 1, wherein said composition further comprising hydrophilic polymer and/or hydrophobic material.
3. The composition as claimed in claim 2, wherein said hydrophilic polymers are selected from group consisting of hydroxypropyl methylcellulose, hydroxypropyl cellulose, a polyethylene glycol, polyvinyl acetate and polyvinylcaprolactame-based graft copolymer, vinylpyrrolidone-vinyl acetate copolymer, Polyvinylpyrrolidone, poly ethylene-co-vinyl acetate, homopolymers and co-polymers of N-vinyl lactams, dextrins, carboxymethylcellulose, hydroxyethylcellulose, hydroxy methylcellulose, sodium carboxymethylcellulose and carboxymethylcellulose calcium.
4. The composition as claimed in claim 2, wherein said hydrophobic materials are selected from group consisting of ethyl cellulose, polyvinyl acetate, waxes, such as, beeswax, carnauba wax, microcrystalline wax, candelilla wax, spermaceti, montan wax, hydrogenated vegetable oil, hydrogenated castor powder, lecithin, hydrogenated cottonseed oil, hydrogenated tallow, paraffin wax, shellac wax, petrolatum, ozokerite, synthetic waxes, fatty acids, fatty alcohols, fatty acid esters, glyceryl monostearate, glycerol monooleate, acetylated monoglycerides, tristearin, tripalmitm, cetyl esters wax, glyceryl palmitostearate and glyceryl dibehenate, vegetable oil, such as, hydrogenated castor oil, mineral oil.
5. An extended release pharmaceutical composition comprising;
40% to 65% by weight of Oxcarbazepine,
2% to 40% by weight of hydrophilic polymers and/or
2% to 30% hydrophobic material, and
10% to 40% by weight of other excipients,
wherein the composition is prepared by using wet granulation or melt extrusion process.
6. The composition as claimed in claim 5, wherein said excipients comprise diluents from about 10% to about 30% % by weight, binders from about 0.1% to about 3% % by weight, disintegrants from about 0.1% to about 3% % by weight, glidants and lubricants from about 0.5 % to about 5% by weight of the total weight of the composition.
7. The composition as claimed in claim 6, wherein said diluents are selected from group consisting of microcrystalline cellulose, silicified microcrystalline cellulose, corn starch, lactose, sucrose, sugar compressible, glucose, sorbitol, calcium carbonate, calcium phosphate-dibasic, calcium phosphate-tribasic and calcium sulfate.
8. The composition as claimed in claim 6, wherein said binders are selected from group consisting of hydroxypropyl methylcellulose, polyvinylpyrrolidone, pregelatinized starch, carboxymethylcellulose sodium, carboxymethylcellulose calcium, ethyl cellulose, hydroxyethyl cellulose and hydroxy propyl cellulose.
9. The composition as claimed in claim 6, wherein said disintegrants are selected from group consisting of silicified microcrystalline cellulose, microcrystalline cellulose, cross-linked polyvinylpyrrolidone, croscarmellose sodium, calcium carboxymethyl cellulose, hydroxypropyl methylcellulose and hydroxypropyl cellulose.
10. The composition as claimed in claim 6, wherein said lubricants and glidants are selected from group consisting of colloidal silicon dioxide, anhydrous silica, stearic acid, magnesium stearate, calcium stearate and talc.