FORM 2
THE PATENT ACT, 1970
(39 of 1970)
&
The Patents Rules, 2003
COMPLETE SPECIFICATION
(See section 10 and rule 13)
Title of the invention "SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION OF IBUPROFEN "
Centaur Pharmaceutical Pvt. Ltd. an Indian Company, having its Registered Office at Centaur House, Near Grand Hyatt, Vakola, Santacruz (East) Mumbai -400055
1. The following specification particularly describes the invention and the manner in which it is to be performed.

SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION OF IBUPROFEN
FIELD OF INVENTION:
The present invention relates to sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar.
BACKGROUND OF THE INVENTION:
Ibuprofen is chemically (RS)-2-(4-(2-methyIpropyl) phenyl) propanoic acid and it is belonging to the chemical class of a propionic acid derivative NSAID and is represented by structural formula I:

Ibuprofen is approved in USA as oral suspension and it has been marketed under the name Ibuprofen by actavis mid atlantic. Ibuprofen is nonsteroidal anti-inflammatory drug [NSAID] and approved in USA for the treatment of fever, aches and pains.
U.S Patent No. 5,292,518 describes prolonged release drug tablet formulations of Ibuprofen wherein gel-forming dietary fiber such as guar gum fiber is being used along with citric acid, dextrose and calcium carbonate excipients. The citric acid and calcium carbonate act to mechanically disintegrate the guar gum fiber so that it forms a sphere or plug of hydrated gel which coats the Ibuprofen and from which the Ibuprofen slowly leaches as the gel hydrates and passes through the gastrointestinal tract and dextrose assist tablet disintegration upon ingestion.

The PCT Publication No. 2010017358 describes sustained release compositions of highly soluble active pharmaceutical ingredients (API), such as tramadol hydrochloride (Example 9) and venlafaxine hydrochloride (Example 7) and sparingly soluble API such as guaiphenesin (Example 8) and diclofenac sodium (Examples 6 and 10.) wherein at least one polysaccharide gum and at least one polyhydric sugar alcohol in a solvent was dissolved to form a solution/suspension; followed by spray drying the solution/suspension to form particles of a sustained release composition; mixing the sustained release composition with at least one filler and at least one active pharmaceutical ingredient to form a tabletting mixture; and compressing the tabletting mixture to form the sustained release pharmaceutical dosage form.
Accordingly the present invention provides sustained release pharmaceutical composition of ibuprofen.
SUMMARY OF THE INVENTION:
A first aspect of the present invention is to provide sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar.
A second aspect of the present invention is to provide a method of treating fever, aches and pains comprising administering sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar as a medicament in human being.
Another aspect of the present invention is to provide method of preparing sustained release pharmaceutical composition of Ibuprofen comprising coprocessed guar gum and sugar.
Another aspect of the present invention is to provide sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum with sugar and pharmaceutically acceptable excipients.

Another aspect of the present invention is to provide sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum; sugar and pharmaceutically acceptable excipients such as fillers, granulating agent/binders, glident and lubricant.
Another aspect of the present invention is to provide a method of preparing sustained release pharmaceutical composition of Ibuprofen comprising but not limited to:
a) mixing coprocessed guar gum and sugar with Ibuprofen, at least one filler, granulating agent/binder, glident and one lubricant to form tabletting mixture;
b) compressing tabletting mixture into tablets and
c) coating of tablets to obtain sustained release pharmaceutical dosage form.
DETAILED DESCRIPTION OF THE INVENTION:
It has been unexpectedly discovered that a composition produced by spray drying a solution/suspension including guar gum and at least one sugar results in a product that provides a sustained release profile when formulated with an Ibuprofen. Physical mixing or wet granulation of guar gum and sugar components does not provide a composition suitable for sustained release applications, although limited release retardation may be observed.
The sustained release pharmaceutical composition of the present invention may be in the form of granules, powder, tablet, capsule or tablet in capsule.
The pharmaceutical composition of the present invention preferably may be in the form of tablet.
The examples of sugar may include but not limited to monosaccharide or disaccharides, for example dextrose, ribose, mannose, galactose, fructose, xylose, maltose or sucrose; polyols, such as glycerol, dulcitol, mannitol, sorbitol or xylitol.
The examples of pharmaceutically acceptable excipients may include fillers such as microcrystalline cellulose (MCC), lactose, calcium carbonate, calcium phosphate dicalcium

phosphate, tribasic calcium sulfate, calcium carboxymethylcellulose, hydroxypropyl methyl cellulose (HPMC), starch or mixture(s) thereof.
The examples of pharmaceutically acceptable excipients may include granulating agent/binder selected from the group comprising of hydroxypropyl methyl cellulose (HPMC), polyvinylpyrrolidone (PVP), hydroxypropylcellulose (HPC), starch, carmellose sodium or mixture thereof
The examples of pharmaceutically acceptable excipients may include glidant selected from the group comprising of hydrophilic/hydrophobic colloidal silicon dioxide, talc, silicon dioxide.
The examples of pharmaceutically acceptable excipients may include lubricants such as agar, calcium stearate, ethyl oleate, ethyl laureate, glycerin, glyceryl palmitostearate, hydrogenated vegetable oil, magnesium oxide, magnesium stearate, poloxamer, glycols, sodium benzoate, sodium lauryl sulfate, sodium stearyl, sorbitol, stearic acid, talc, zinc stearate or mixture(s) thereof.
The guar gum may be combined in various proportions with at least one sugar. The combination reduced the viscosity of the guar gum adequately to result in excellent spray characteristics and ease in spray drying, resulting in coprocessed guar gum.
The co-processed guar gum and sugar may contain guar gum and sugar in the range of 1: 0.1 to 1: 10.
The co-processed guar gum and sugar may be present in an amount of 5% to 75% of the formulation.
The co-processing of guar gum with sugar may be carried out by methods known in the art such as spray-drying.
The co-processed guar gum and sugar may be mixed with pharmaceutically acceptable excipients to form tabletting mixture.

The co-processed guar gum and sugar may be mixed with pharmaceutically acceptable excipients either by dry mix or by wet granulation process to form tabletting mixture.
The resulting tabletting mixture may be converted into dosage form such as granules, powder, tablets, capsules or tablets in capsules by methods known in the art.
DESCRIPTION OF FIGURE
FIGURE NO.l: Dissolution profile of Ibuprofen SR Tablets obtained from example no 1 and example no 2
The following examples are provided for illustrative purposes only and are not limiting of the present invention disclosed and claimed herein.
Examples no.l: Direct Compression

Sr.No. Name of material Quantity (nig) per Tablets
Blending
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 240
3 Microcrystalline Cellulose 49
Lubrication
4 Magnesium Stearate 11
Procedure:
Blending: Ibuprofen, Spray Dried Guar Gum: Mannitol [Brand Name: PanExcea CR, Grade: MC15G alone or in combination with MC13G, Supplied by Aventor Performance Material], Microcrystalline Cellulose sifted and blended.
Lubrication: Blended material lubricated using sifted magnesium stearate.
Compression: Lubricated blend compressed into tablets.

Examples no.2: Direct Compression

Sr.No. Name of material Quantity(mg) per Tablets
Blending
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 300
3 Microcrystalline Cellulose 300
Lubrication
4 Magnesium Stearate 10
Procedure:
Blending: Ibuprofen, Spray Dried Guar Gum: Mannitol (PanExcea CR), Microcrystalline
Cellulose sifted and blended. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets
Examples no.3: Wet Granulation

Sr.No. Name of material Quantity(mg) per Tablets
Intragranular
1 Ibuprofen 800
Granula ting Fluid
2 Povidone 25
3 Purified Water q.s
Extragranular
4 Spray Dried Guar Gum: Mannitol (PanExcea CR) 300
5 Colloidal Silica anhydrous 11.5
Lubrication
6 Magnesium Stearate 13.5
Procedure:
Granulation: Ibuprofen granules prepared using granulating fluid of Povidone in purified water.
Blending: Sized granules blended with sifted spray dried guar gum: mannitol (PanExcea
CR) and colloidal silica anhydrous. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets.

Examples no.4: Wet Granulation

Sr.No. Name of material Quantity(mg) per Tablets
Intragranular
1 Ibuprofen 800
Granulai ting Fluid
2 Povidone 50
3 Purified Water q.S
Extragranular
4 Spray Dried Guar Gum: Mannitol (PanExcea CR) 430
5 Colloidal Silica anhydrous 5
Lubrication
6 Magnesium Stearate 15
Coating
7 Opadry 03B28796 White 26
Procedure:
Granulation: Ibuprofen granules prepared using granulating fluid of Povidone solution in
Purified water. Blending: Sized granules blended with sifted spray dried guar gum: mannitol (PanExcea
CR) and colloidal silica anhydrous.
Lubrication: Blended material lubricated using sifted magnesium stearate.
Compression: Lubricated blend compressed into tablets.
Coating: Compressed Tablets coated with Opadry 03B28796 White coating dispersion in
water comprising hypromellose, polyethylene glycol, titanium dioxide, talc. Examples no.5: Wet Granulation

Sr.No. Name of material Quantity(mg) per Tablets
Intragranular
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 200
Granula ting Fluid
3 Povidone 50
4 Purified Water q.s
Extragranular
5 Spray Dried Guar Gum: Mannitol (PanExcea CR) 230
6 Colloidal Silica anhydrous 5
Lubrication
7 Magnesium Stearate 15

Procedure;
Granulation: Granules of Ibuprofen & Spray Dried Guar Gum: Mannitol (PanExcea CR)
prepared using granulating fluid of Povidone solution in purified water. Blending: Sized granules blended with sifted spray dried guar gum: mannitol (PanExcea CR)
and colloidal silica anhydrous. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets.
Examples no.6: Wet Granulation

Sr.No. Name of material Quantity(mg) per Tablets
Intragranular
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 430
Granula ting Fluid
3 Povidone 50
4 Purified Water q.s
Extragranular
5 Colloidal Silica anhydrous 5
Lubrication
6 Magnesium Stearate 15
Procedure:
Granulation: Granules of Ibuprofen & Spray Dried Guar Gum: Mannitol (PanExcea CR)
prepared using granulating fluid of Povidone solution in purified water. Blending: Sized granules blended with sifted spray dried guar gum: mannitol (PanExcea
CR) and colloidal silica anhydrous. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets. Examples no.7: Direct Compression

Sr.No. Name of material Quantity(mg) per Tablets
Blending
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 480
3 Microcrystalline Cellulose 100
4 Povidone 30

5 Colloidal Silica anhydrous 5
Lubrication
6 Magnesium Stearate 15
Procedure:
Blending: Ibuprofen , Spray Dried Guar Gum: Mannitol (PanExcea CR), Microcrystalline
Cellulose, Povidone and Colloidal Silica anhydrous sifted and blended. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets Examples no.8: Direct Compression

Sr.No. Name of material Quantiry(mg) per Tabiets
Blending
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 460
3 Microcrystalline Cellulose 100
4 Hydroxypropyl cellulose 50
5 Colloidal Silica anhydrous 5
Lubrication
6 Magnesium Stearate 15
Procedure:
Blending: Ibuprofen, Spray Dried Guar Gum: Mannitol (PanExcea CR), Microcrystalline
Cellulose, Hydroxypropyl cellulose and Colloidal Silica anhydrous sifted and
blended. Lubrication: Blended material lubricated using sifted magnesium stearate. Compression: Lubricated blend compressed into tablets.
Examples no.9: Direct Compression

Sr.No. Name of material Quantity(mg) per Tablets
Blending
1 Ibuprofen 800
2 Spray Dried Guar Gum: Mannitol (PanExcea CR) 460
3 Microcrystalline Cellulose 100
4 Hydroxypropyl cellulose 50
5 Colloidal Silica anhydrous 5
Lubrication
6 Stearic Acid 15

Procedure:
Blending: Jbuprofen, Spray Dried Guar Gum: Mannitol (PanExcea CR), Microcrystalline
Cellulose, Hydroxypropyl cellulose and Colloidal Silica anhydrous sifted and
blended. Lubrication: Sifted Stearic Acid used to lubricate blended material. Compression: Lubricated blend compressed into tablets.

WE CLAIM:
1. A sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar.
2. The sustained release pharmaceutical composition according to claim no. 1, wherein sustained pharmaceutical composition is in the form of granules, powder, tablet, capsule or tablet in capsule.
3. The sustained release pharmaceutical composition according to claim no. 1, wherein sugar is selected from the group comprising of dextrose, ribose, mannose, galactose, fructose, xylose, maltose, sucrose, glycerol, dulcitol, mannitol, sorbitol, xylitol or mixture(s) thereof.
4. The sustained release pharmaceutical composition according to claim no. 1, wherein co-processed guar gum and sugar contain guar gum and sugar in the range of 1: 0.1 to 1: 10.
5. The sustained release pharmaceutical composition according to claim no. 1, wherein co-processed guar gum and sugar is present in the range of 5% to 75% weight / weight of the formulation.
6. A sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar and pharmaceutically acceptable excipients such as fillers, granulating agent/binders, glident and lubricant.
7. The sustained release pharmaceutical composition according to claim no. 6, wherein fillers is selected from the group comprising of microcrystalline cellulose (MCC), lactose, calcium carbonate, calcium phosphate dicalcium phosphate, tribasic calcium sulfate, calcium carboxymethylcellulose, hydroxypropyl methyl cellulose (HPMC), starch or mixture(s) thereof; wherein granulating agent/binder is selected from the group comprising of hydroxypropyl methyl cellulose (HPMC), polyvinylpyrrolidone (PVP), hydroxypropylcellulose(HPC), starch,

carmellose sodium or mixture thereof and glidant is selected from the group comprising of hydrophilic/hydrophobic colloidal silicon dioxide, talc, silicon dioxide.
8. The sustained release pharmaceutical composition according to claim no. 6, wherein lubricants is selected from the group comprising of agar, calcium stearate, ethyl oleate, ethyl laureate, glycerin, glyceryl palmitostearate, hydrogenated vegetable oil, magnesium oxide, magnesium stearate, poloxamer, glycols, sodium benzoate, sodium lauryl sulfate, sodium stearyl, sorbitol, stearic acid, talc, zinc stearate or mixture(s) thereof.
9. A method of treating fever, aches and pains comprising administering sustained release pharmaceutical composition of ibuprofen comprising coprocessed guar gum and sugar as a medicament in human being.
10. A method of preparing sustained release pharmaceutical composition of Ibuprofen
comprising but not limited to:
a) mixing coprocessed guar gum and sugar with Ibuprofen, at least one filler, granulating agent/binder, glident and one lubricant to form tabletting mixture and
b) compressing tabletting mixture into tablets and
c) coating of tablets to obtain sustained release pharmaceutical dosage form.