Title of Invention	EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF
Abstract	The present invention relates to extended release oral pharmaceutical composition comprising Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixture thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating systems releases the drug over a period of time using drug release-retarding agents. This matrix dosage form designed to float in the taken in the acidic medium without using any gas generarating agent. This composition shall be taken once daily through oral administration for the treatment of benign prostatic hyperplasia (BPH).

Title of Invention

EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF

Abstract

The present invention relates to extended release oral pharmaceutical composition comprising Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixture thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating systems releases the drug over a period of time using drug release-retarding agents. This matrix dosage form designed to float in the taken in the acidic medium without using any gas generarating agent. This composition shall be taken once daily through oral administration for the treatment of benign prostatic hyperplasia (BPH).

Full Text	FORM 2 THE PATENTS ACT 1970 (39 OF 1970) PROVISOINAL SPECIFICATION (SECTION 10) "EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF" UNICHEM LABORATORIES LIMITED, A COMPANY REGISTERED UNDER THE INDIAN COMPANY ACT, 1956, HAVING ITS REGISTERED OFFICE LOCATED AT MAHALAXMI CHAMBERS, 2nd FLOOR, 22, BHULABHAIDESAI ROAD, MUMBAI-400 026. MAHARASTRA, INDIA The following specification describes the invention. "EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF" FIELD OF INVENTION The present invention relates to an extended release oral pharmaceutical composition comprising alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof, an µ1 -Adrenoceptor antagonist for the treatment of urinary disorders associated with benign prostatic hyperplasia, and method of preparing the same. BACKGROUND OF THE INVENTION Alfuzosin hydrochloride is a quinazoline derivative, selective and competitive alpha-adrenoreceptor antagonist that belongs to the chemical class of 4-amino-6, 7-dimethoxy quinazol-2-yl-alkylene diamines. It distributes preferentially in the prostate compared with plasma, and decreases the sympathetically controlled tone of prostatic smooth muscle. As a result lower urinary tract symptoms suggestive of benign prostatic hyperplasia (BPH) are improved. Alfuzosin has a short -half life about 3 to 5 hours and is more intensely absorbed at the duodenum and jejunum than in subsequent portions of the GI tract. This means, most of the release of drug is required in the stomach or at the upper parts of intestine and therefore gastro retentive or floating in the acidic medium or contents is a suitable dosage form to achieve required release of the drug over a period of time. The extended release formulation of alfuzosin hydrochloride controls the symptoms associated with the BPH as effectively as immediate release and have additional advantages, better patient compliance, reduced fluctuations of plasma drug levels and reduced toxicity. Presently alfuzosin controlled release tablets are available in the market (UROXATRAL in USA-triple layer tablet). However there are no floating dosage forms are available which are more suitable for such drugs. The technology of floating systems, particularly suitable for controlled delivery of drugs that are absorbed greatly in upper parts of the gastrointestinal tract with a specific absorption window. The US 20060062846 (Mathias S. et al, 2006) discloses the controlled release of Alfiizosin in the monolithic polymeric matrix which releases the drug over a period of time but does not float in the gastric fluids. US 20040115259 (Frederique B. et al, 2004) discloses a method for producing a tablet containing alfiizosin, which comprises where the quantity of active principle is homogeneously mixed with a quantity of carrier of between 50 and 99.9% of the total weight, the carrier being chosen from among at least one compound from the family of cellulose derivatives and/or Povidone derivatives and/or polyvinyl acetate derivatives ; the mixture is compressed to produce a homogeneous monolithic tablet that floats immediately , in the gastric medium. The invention also covers on the tablets obtained. In the present invention polymeric systems are different and easy to implement and cost effective process for commercial preparation(is this statement and the final system produced floats on to the acidic medium. The floating dosage form finally obtained floats on to the aqueous medium independent of pH, which is advantageous as GIT pH varies. Abstract of WO/2006/021692 which describes about pharmaceutical composition in the form of a gastric resident matrix tablet, comprising an active principle, characterized in that when contacted with an environment representing a gastric fluid, it increases after fifteen minutes in volume by swelling rate of at least 200%. The drawback of this could be rate of swelling is much more where dose dumping can be expected accidentally and or swelling is too much where stomach fullness can be felt all the time by patients. WO2006063858 (Grenier P. et al, 2006) describes pharmaceutical composition containing coated floating particles. The dosage form comprises these particles comprising an inner drug containing core, an intermediate layer surrounding said core and a release rate-controlling outer coating. This product contains more manufacturing steps and commercially tedious. Therefore there exist a need in order to get improved, simple and cost effective composition which eliminates the disadvantages of the prior art reported compositions of Alfuzosin. OBJECT OF THE INVENTION The object of the present invention is to provide an improved, simple and cost effective composition and process of preparation of the extended release floating system, comprising alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof, by using drug release retarding agents without using any gas generating excipients. SUMMARY OF THE INVENTION The present invention relates to the composition and process of preparation of an extended release oral pharmaceutical composition comprising, Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating system releases the drug over a period of time using drug release-retarding agents. The present invention provides a cost effective and simple manufacturing composition process. In another aspect of the present invention involves the direct compression method to manufacture of tablets. Tablets prepared by this method are easy to manufacture, involves less processing steps, and more economical and cheap as it involves the use of conventional equipments. Another aspect of the present invention is to provide the matrix tablet which is designed to float in the acidic medium without using any gas generating agents. An extended release pharmaceutical composition is in the form of floating system, containing active ingredient, along with one or more of release retarding agents. Release retarding agents may comprises one or more of cellulose derivatives, gums, carboxyvinyl polymers, chitosans, carrageenans, methacrylates and copolymers, polyanhydrides, polyvinyl alcohol, glucans, dextran, waxes and vegetable oils. The cellulose derivative may be one or more of ethyl cellulose, hydroxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropylcellulose, carboxy methylcellulose, and methylcellulose. Gum comprises one or more of xanthan gum, veegum, guar gum, karaya gum, locust bean gum, gellan gum, hupu gum, carob gum, caramania, sodium alginate and alginic acid. Glucans may be one or more of lichenin, nigeran and glycogens. The extended release floating system further includes one or more pharmaceutically acceptable excipients. The one or more pharmaceutically acceptable excipients may include matrix ballooning inducers, diluents, glidants, lubricants and optionally binders. The ballooning inducers may be one or more of crosslinked povidone, sodium starch glycolate, cross carmellose sodium, pregelatinized starch, carboxymethyl cellulose sodium and carboxymethyl cellulose calcium. The binder may be one or more of povidone, magnesium aluminum silicate, co-povidone, acacia, sorbitol and gelatin. The diluent may be one or more of lactose, starch, dibasic calcium phosphate dihydrate, mannitol, sorbitol, calcium sulphate dihydrate, dextrose and microcrystalline cellulose. The lubricants may be one or more of magnesium stearate, talc, stearic acid, wax, sodium stearyl fumerate, polyethylene glycol and calcium stearate. The glidants may be one or more colloidal silicon dioxide, talc and starch. The extended release formulation may contain 1-10% of Alfuzosin hydrochloride, 10-60% of xanthan gum, 1-65% of crosslinked povidone, 10-90% of microcrystalline cellulose, 0.1-5% of the magnesium stearate, 0.1-5% of the colloidal silicon dioxide. The matrix composition of the present invention may include the active ingredient in a range of about 1 mg to about 20 mg. Preferred dosage form contain either 5 mg or 10 mg of the active ingredient. The term 'active ingredient' refers to alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. The formulation may contain 1-10% of the active ingredient. Preferably formulation may contain 1-5% of the active ingredient. The active ingredient may be alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. The formulation may contain 1-80% of the release modifying agents. Preferably formulation may contain in between 10-50% of the release modifying agents. The formulation may contain 1-80% of the matrix ballooning inducers. Preferably formulation may contain in between 10-65% of the matrix ballooning inducers. The formulation may contain 5-90% of the diluents. Preferably formulation may contain 10-85% of the diluents. The formulation may contain 0.1-5% of the lubricants. Preferably formulation may contain 0.1-3% of the lubricants. Another aspect of the invention is to provide a formulation comprising active ingredients particle size is of 1 to 100 microns. In one preferred embodiment, the extended release floating system may include Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof in amounts ranging from about 1% to about 10% w/w, xanthan gum in amounts ranging from about 10% to about 60% w/w, crosslinked povidone in amounts ranging from about 1% to about 65% w/w, microcrystalline cellulose in amounts ranging from about 10% to about 85% w/w, magnesium stearate in amounts ranging from about 0.1% to about 3% w/w, and colloidal silicon dioxide in amounts ranging from about 0.1% to about 3% w/w. The extended release floating system may be in the form of one or more of tablets, capsules, pellets, granules and other dosage forms suitable for oral administration. The extended release floating system release the drug less than about 18% in about 1 hour, less than about 62 % in about 8 hours, as measured in 0.0IN HCL using USP type II apparatus, at 37±2°C. The extended release floating system release the drug less than about 28% in about 2 hours, less than about 75% in about 12 hours, more than about 90% in about 24 hours, as measured in 0.0IN HCL using USP type II apparatus, at 37±2°C. The extended release floating system release the drug less than about 45% in about 4 hours, less than about 85% in about 16 hours, as measured in a 0.01N HCL using USP type II apparatus, at 37±2°C. The extended release pharmaceutical composition may be used for the treatment of benign prostatic hyperplasia (BPH). The extended release pharmaceutical composition may be administered orally either twice daily or once daily. In another aspect there is provided a process for forming an extended release floating system in oral dosage form. The process includes. Sift all the materials; forming a mixture of alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof and one or more release retarding agents; forming a floating system. The floating system may include cosmetic coating. The cosmetic coating may include a colorant. The extended release floating system may be prepared by direct compression, dry granulation, or wet granulation, preferably direct compression. Forming floating system may be in the form of tablets, capsules, pellets, granules or other dosage forms suitable for oral administration. According to the present invention provides a pharmaceutical composition is in the form of tablets or capsules, which relates to extended release floating system of Alfuzosin that may substantially reduce the adverse events, which are present in the art of conventional tablets. Alfuzosin absorbed greatly in upper parts of the GI tract, especially absorbed in duodenum and jejunum. The present composition is a floating system containing Alfuzosin, permits guaranteeing optimum dwell time in the stomach of the individual by floating sufficiently, a controlled release of the active drug in an extended period of time. Although the invention has been described with reference to specific embodiments, this description is not meant to be construed in a limiting sense. Various modifications of the disclosed embodiments, as well as alternate embodiments of the invention, will become apparent to persons skilled in the art upon reference to the description of the invention. It is therefore contemplated that such modifications can be made without departing from the spirit or scope of the present invention as defined. EXAMPLES The following examples are presented for illustration only, and are not intended to limit the scope of the invention or appended claims. Example 1 Table 1 SNO Ingredient Mg/tab %W/W 1 Alfuzosin hydrochloride IH 10 3.33 2 Xanthan gum NF 90 . 30 3 Crospovidone NF 90 30 4 Microcrystalline cellulose NF 104 34.66 5 Colloidal silicon dioxide NF 3 1 6 Magnesium stearate NF 3 1 Alfuzosin hydrochloride and all other ingredients, namely xanthan gum, crospovidone, microcrystalline cellulose and colloidal silicon dioxide were sifted through ASTM # 40 mesh twice and mixed for 5 minutes using double cone blender. Blend was lubricated with presifted magnesium stearate (#40 mesh) and mixed for 3 minutes using double cone blender. The above mixture was compressed into tablets by using 8.5 mm round flat face beveled edge punches. Example 2 Table 2: formulation of example 2 S.NO Ingredients Mg/tab %W/w 1 Alfuzosin hydrochloride IH 10 3.33 2 Xanthan gum NF 90 30 3 Crospovidone NF 110 30 4 Microcrystalline cellulose NF 84 36.66 5 Colloidal silicon dioxide NF 3 1 6 Magnesium stearate NF 3 1 Alfuzosin hydrochloride and all other ingredients, namely xanthan gum, crospovidone, microcrystalline cellulose and colloidal silicon dioxide were sifted through ASTM # 40 mesh twice and mixed for 5 minutes using double cone blender. Blend was lubricated with presifted magnesium stearate (#40 mesh) and mixed for 3 minutes using double cone blender. The above mixture was compressed into tablets by using 8.5 mm round flat face beveled edge punches. ABSTRACT The present invention relates to extended release oral pharmaceutical composition comprising Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating system releases the drug over a period of time using drug release-retarding agents. This matrix dosage form designed to float in the acidic medium without using any gas generating agents. This composition shall be taken once daily through oral administration for the treatment of benign prostatic hyperplasia (BPH).

Full Text

FORM 2
THE PATENTS ACT 1970
(39 OF 1970)
PROVISOINAL SPECIFICATION
(SECTION 10)
"EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF"
UNICHEM LABORATORIES LIMITED, A COMPANY
REGISTERED UNDER THE INDIAN COMPANY ACT, 1956,
HAVING ITS REGISTERED OFFICE LOCATED AT
MAHALAXMI CHAMBERS, 2nd FLOOR,
22, BHULABHAIDESAI ROAD, MUMBAI-400 026.
MAHARASTRA, INDIA
The following specification describes the invention.

"EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING ALFUZOSIN AND PROCESS FOR THE PREPARATION THEREOF"
FIELD OF INVENTION
The present invention relates to an extended release oral pharmaceutical composition comprising alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof, an µ1 -Adrenoceptor antagonist for the treatment of urinary disorders associated with benign prostatic hyperplasia, and method of preparing the same.
BACKGROUND OF THE INVENTION
Alfuzosin hydrochloride is a quinazoline derivative, selective and competitive alpha-adrenoreceptor antagonist that belongs to the chemical class of 4-amino-6, 7-dimethoxy quinazol-2-yl-alkylene diamines. It distributes preferentially in the prostate compared with plasma, and decreases the sympathetically controlled tone of prostatic smooth muscle. As a result lower urinary tract symptoms suggestive of benign prostatic hyperplasia (BPH) are improved.
Alfuzosin has a short -half life about 3 to 5 hours and is more intensely absorbed at the duodenum and jejunum than in subsequent portions of the GI tract. This means, most of the release of drug is required in the stomach or at the upper parts of intestine and therefore gastro retentive or floating in the acidic medium or contents is a suitable dosage form to achieve required release of the drug over a period of time. The extended release formulation of alfuzosin hydrochloride controls the symptoms associated with the BPH as effectively as immediate release and have additional advantages, better patient compliance, reduced fluctuations of plasma drug levels and reduced toxicity. Presently alfuzosin controlled release tablets are available in the market (UROXATRAL in USA-triple layer tablet). However there are no floating dosage forms are available

which are more suitable for such drugs. The technology of floating systems, particularly suitable for controlled delivery of drugs that are absorbed greatly in upper parts of the gastrointestinal tract with a specific absorption window.
The US 20060062846 (Mathias S. et al, 2006) discloses the controlled release of Alfiizosin in the monolithic polymeric matrix which releases the drug over a period of time but does not float in the gastric fluids.
US 20040115259 (Frederique B. et al, 2004) discloses a method for producing a tablet containing alfiizosin, which comprises where the quantity of active principle is homogeneously mixed with a quantity of carrier of between 50 and 99.9% of the total weight, the carrier being chosen from among at least one compound from the family of cellulose derivatives and/or Povidone derivatives and/or polyvinyl acetate derivatives ; the mixture is compressed to produce a homogeneous monolithic tablet that floats immediately , in the gastric medium. The invention also covers on the tablets obtained. In the present invention polymeric systems are different and easy to implement and cost effective process for commercial preparation(is this statement and the final system produced floats on to the acidic medium. The floating dosage form finally obtained floats on to the aqueous medium independent of pH, which is advantageous as GIT pH varies.
Abstract of WO/2006/021692 which describes about pharmaceutical composition in the form of a gastric resident matrix tablet, comprising an active principle, characterized in that when contacted with an environment representing a gastric fluid, it increases after fifteen minutes in volume by swelling rate of at least 200%. The drawback of this could be rate of swelling is much more where dose dumping can be expected accidentally and or swelling is too much where stomach fullness can be felt all the time by patients.
WO2006063858 (Grenier P. et al, 2006) describes pharmaceutical composition containing coated floating particles. The dosage form comprises these particles comprising an inner drug containing core, an intermediate layer surrounding said core

and a release rate-controlling outer coating. This product contains more manufacturing steps and commercially tedious.
Therefore there exist a need in order to get improved, simple and cost effective composition which eliminates the disadvantages of the prior art reported compositions of Alfuzosin.
OBJECT OF THE INVENTION
The object of the present invention is to provide an improved, simple and cost effective composition and process of preparation of the extended release floating system, comprising alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof, by using drug release retarding agents without using any gas generating excipients.
SUMMARY OF THE INVENTION
The present invention relates to the composition and process of preparation of an extended release oral pharmaceutical composition comprising, Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating system releases the drug over a period of time using drug release-retarding agents.
The present invention provides a cost effective and simple manufacturing composition process.
In another aspect of the present invention involves the direct compression method to manufacture of tablets. Tablets prepared by this method are easy to manufacture, involves less processing steps, and more economical and cheap as it involves the use of conventional equipments.

Another aspect of the present invention is to provide the matrix tablet which is designed to float in the acidic medium without using any gas generating agents.
An extended release pharmaceutical composition is in the form of floating system, containing active ingredient, along with one or more of release retarding agents. Release retarding agents may comprises one or more of cellulose derivatives, gums, carboxyvinyl polymers, chitosans, carrageenans, methacrylates and copolymers, polyanhydrides, polyvinyl alcohol, glucans, dextran, waxes and vegetable oils. The cellulose derivative may be one or more of ethyl cellulose, hydroxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropylcellulose, carboxy methylcellulose, and methylcellulose. Gum comprises one or more of xanthan gum, veegum, guar gum, karaya gum, locust bean gum, gellan gum, hupu gum, carob gum, caramania, sodium alginate and alginic acid. Glucans may be one or more of lichenin, nigeran and glycogens.
The extended release floating system further includes one or more pharmaceutically acceptable excipients. The one or more pharmaceutically acceptable excipients may include matrix ballooning inducers, diluents, glidants, lubricants and optionally binders. The ballooning inducers may be one or more of crosslinked povidone, sodium starch glycolate, cross carmellose sodium, pregelatinized starch, carboxymethyl cellulose sodium and carboxymethyl cellulose calcium. The binder may be one or more of povidone, magnesium aluminum silicate, co-povidone, acacia, sorbitol and gelatin. The diluent may be one or more of lactose, starch, dibasic calcium phosphate dihydrate, mannitol, sorbitol, calcium sulphate dihydrate, dextrose and microcrystalline cellulose. The lubricants may be one or more of magnesium stearate, talc, stearic acid, wax, sodium stearyl fumerate, polyethylene glycol and calcium stearate. The glidants may be one or more colloidal silicon dioxide, talc and starch.
The extended release formulation may contain 1-10% of Alfuzosin hydrochloride, 10-60% of xanthan gum, 1-65% of crosslinked povidone, 10-90% of microcrystalline cellulose, 0.1-5% of the magnesium stearate, 0.1-5% of the colloidal silicon dioxide. The matrix composition of the present invention may include the active ingredient in a range of about 1 mg to about 20 mg. Preferred dosage form contain either 5 mg or 10 mg

of the active ingredient. The term 'active ingredient' refers to alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof.
The formulation may contain 1-10% of the active ingredient. Preferably formulation may
contain 1-5% of the active ingredient. The active ingredient may be alfuzosin or
pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof.
The formulation may contain 1-80% of the release modifying agents. Preferably
formulation may contain in between 10-50% of the release modifying agents.
The formulation may contain 1-80% of the matrix ballooning inducers. Preferably
formulation may contain in between 10-65% of the matrix ballooning inducers.
The formulation may contain 5-90% of the diluents. Preferably formulation may contain
10-85% of the diluents.
The formulation may contain 0.1-5% of the lubricants. Preferably formulation may
contain 0.1-3% of the lubricants.
Another aspect of the invention is to provide a formulation comprising active ingredients
particle size is of 1 to 100 microns.
In one preferred embodiment, the extended release floating system may include
Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof in
amounts ranging from about 1% to about 10% w/w, xanthan gum in amounts ranging
from about 10% to about 60% w/w, crosslinked povidone in amounts ranging from about
1% to about 65% w/w, microcrystalline cellulose in amounts ranging from about 10% to
about 85% w/w, magnesium stearate in amounts ranging from about 0.1% to about 3%
w/w, and colloidal silicon dioxide in amounts ranging from about 0.1% to about 3% w/w.
The extended release floating system may be in the form of one or more of tablets, capsules, pellets, granules and other dosage forms suitable for oral administration.
The extended release floating system release the drug less than about 18% in about 1 hour, less than about 62 % in about 8 hours, as measured in 0.0IN HCL using USP type II apparatus, at 37±2°C.

The extended release floating system release the drug less than about 28% in about 2 hours, less than about 75% in about 12 hours, more than about 90% in about 24 hours, as measured in 0.0IN HCL using USP type II apparatus, at 37±2°C.
The extended release floating system release the drug less than about 45% in about 4 hours, less than about 85% in about 16 hours, as measured in a 0.01N HCL using USP type II apparatus, at 37±2°C.
The extended release pharmaceutical composition may be used for the treatment of benign prostatic hyperplasia (BPH).
The extended release pharmaceutical composition may be administered orally either twice daily or once daily.
In another aspect there is provided a process for forming an extended release floating system in oral dosage form. The process includes.
Sift all the materials; forming a mixture of alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof and one or more release retarding agents; forming a floating system.
The floating system may include cosmetic coating. The cosmetic coating may include a colorant.
The extended release floating system may be prepared by direct compression, dry granulation, or wet granulation, preferably direct compression.
Forming floating system may be in the form of tablets, capsules, pellets, granules or other dosage forms suitable for oral administration.
According to the present invention provides a pharmaceutical composition is in the form of tablets or capsules, which relates to extended release floating system of Alfuzosin that may substantially reduce the adverse events, which are present in the art of conventional

tablets. Alfuzosin absorbed greatly in upper parts of the GI tract, especially absorbed in duodenum and jejunum. The present composition is a floating system containing Alfuzosin, permits guaranteeing optimum dwell time in the stomach of the individual by floating sufficiently, a controlled release of the active drug in an extended period of time.
Although the invention has been described with reference to specific embodiments, this description is not meant to be construed in a limiting sense. Various modifications of the disclosed embodiments, as well as alternate embodiments of the invention, will become apparent to persons skilled in the art upon reference to the description of the invention. It is therefore contemplated that such modifications can be made without departing from the spirit or scope of the present invention as defined.
EXAMPLES
The following examples are presented for illustration only, and are not intended to limit the scope of the invention or appended claims.
Example 1
Table 1
SNO Ingredient Mg/tab %W/W
1 Alfuzosin hydrochloride IH 10 3.33
2 Xanthan gum NF 90 . 30
3 Crospovidone NF 90 30
4 Microcrystalline cellulose NF 104 34.66
5 Colloidal silicon dioxide NF 3 1
6 Magnesium stearate NF 3 1

Alfuzosin hydrochloride and all other ingredients, namely xanthan gum, crospovidone, microcrystalline cellulose and colloidal silicon dioxide were sifted through ASTM # 40 mesh twice and mixed for 5 minutes using double cone blender. Blend was lubricated

with presifted magnesium stearate (#40 mesh) and mixed for 3 minutes using double cone blender. The above mixture was compressed into tablets by using 8.5 mm round flat face beveled edge punches.
Example 2
Table 2: formulation of example 2
S.NO Ingredients Mg/tab %W/w
1 Alfuzosin hydrochloride IH 10 3.33
2 Xanthan gum NF 90 30
3 Crospovidone NF 110 30
4 Microcrystalline cellulose NF 84 36.66
5 Colloidal silicon dioxide NF 3 1
6 Magnesium stearate NF 3 1

Alfuzosin hydrochloride and all other ingredients, namely xanthan gum, crospovidone, microcrystalline cellulose and colloidal silicon dioxide were sifted through ASTM # 40 mesh twice and mixed for 5 minutes using double cone blender. Blend was lubricated with presifted magnesium stearate (#40 mesh) and mixed for 3 minutes using double cone blender. The above mixture was compressed into tablets by using 8.5 mm round flat face beveled edge punches.

ABSTRACT
The present invention relates to extended release oral pharmaceutical composition comprising Alfuzosin or pharmaceutically acceptable salt, solvate, enantiomers or mixtures thereof. This pharmaceutical composition can be an extended release floating system or dosage form containing Alfuzosin and or its salt and the floating system releases the drug over a period of time using drug release-retarding agents. This matrix dosage form designed to float in the acidic medium without using any gas generating agents. This composition shall be taken once daily through oral administration for the treatment of benign prostatic hyperplasia (BPH).

Documents:

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Patent Number

271893

Indian Patent Application Number

1922/MUM/2007

PG Journal Number

11/2016

Publication Date

11-Mar-2016

Grant Date

09-Mar-2016

Date of Filing

28-Sep-2007

Name of Patentee

UNICHEM LABORATORIES LIMITED

Applicant Address

UNICHEM BHAVAN, PRABJHAT ESTATE, S.V.ROAD, JOGESHWARI WEST MUMBAI

Inventors:

#	Inventor's Name	Inventor's Address
1	ARAVIND VISHWESHWAR KERUDI	UNICHEM LABORATORIES LIMITED PLOT NOS 17 & 18, PILERNE INDUSTRIAL ESTATE, PILERNE, BARDEZ 403511
2	GEDALA VENKATA MURALI MOHAN BABU	UNICHEM LABORATORIES LIMITED PLOT NOS 17 & 18, PILERNE INDUSTRIAL ESTATE, PILERNE, BARDEZ 403511
3	MEKA VENAKTA SRIKANTH	UNICHEM LABORATORIES LIMITED PLOT NOS 17 & 18, PILERNE INDUSTRIAL ESTATE, PILERNE, BARDEZ 403511

PCT International Classification Number

C07D405/12; C07D405/00

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA