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Process For Preparation Of Amorphous Carvedilol Dihydrogen Phosphate

Abstract: The present invention relates to a process for the preparation of amorphous carvedilol phosphate comprising; adding carvedilol base or carvedilol phosphate to a solvent consisting of water miscible cyclic ether(s) or aliphatic nitrile(s) or a mixture thereof and optionally adding water; optionally. adding orthophosphoric acid or its diluted solution to the preceeding; and spray drying the solution thus obtained to afford amorphous carvedilol phosphate.

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
26 May 2008
Publication Number
49/2009
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
Parent Application

Applicants

ALKEM LABORATORIES LTD.
DEVASHISH, ALKEM HOUSE, SENAPATI BAPAT MARG, LOWER PAREL, MUMBAI 400013 MAHARASHTRA, INDIA.

Inventors

1. JITENDRA KOUNDINYA
ALKEM LABORATORIES LTD.C-6/1, MIDC INDUSTRIAL AREA, TALOJA. TALUKA-PANVEL, DISTT.-RAIGAD-410208.INDIA
2. RAJIV KUMAR
ALKEM LABORATORIES LTD. C-6/1, MIDC INDUSTRIAL AREA, TALOJA. TALUKA-PANVEL, DISTT.-RAIGAD-410208. INDIA
3. ASHOK RAMPAL
C-943, SUSHANT LOK-I, GURGAON-122002, HARYANA, INDIA.

Specification

FORM 2 THE PATENTS ACT, 1970 (39 OF 1970) & PATENTS RULES, 2006 PROVISIONAL SPECIFICATION (SECTION 10; RULE 13) "PROCESS FOR PREPARATION OF AMORPHOUS CARVEDBLOL DIHYDROGEN PHOSPHATE" ALKEM LABORATORIES LIMITED, A COMPANY INCORPORATED UNDER THE COMPANIES ACT, 1956, HAVING ITS CORPORATE. OFFICE AT ALKEM HOUSE, DEVASHISH, ADJACENT TO MATULYA CENTRE, S.B.MARG, LOWER PAREL, MUMBAI - 400013, MAHARASHTRA, INDIA THE FOLLOWING SPECIFICATION DESCRIBES THE NATURE OF THE INVENTION AND THE MANNER IN WHICH IT IS TO BE PERFORMED FIELD OF THE INVENTION The present invention relates to a process for preparation of amorphous carvedilol dihydrogen phosphate. BACKGROUND OF THE INVENTION Carvedilol, (±)-l-(Carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy) ethyl] amino]-2-propanol, is a nonselective B-adrenergic blocker with a i-blocking activity. Carvedilol is a racemic mixture having the following structural formula (I): Carvedilol is the active ingredient in COREG®, which is indicated for the treatment of congestive heart failure and for the management of hypertension. Since carvedilol is a multiple-action drug, its beta-blocking activity affects the response to certain nerve impulses in parts of the body. As a result, beta-blockers decrease the heart's need for blood and oxygen by reducing its workload. Carvedilol is also known to be a vasodilator resulting primarily from alpha-adrenoceptor blockade. The multiple actions of carvedilol are responsible for the antihypertensive efficacy of the drug and for its effectiveness in managing congestive heart failure. Carvedilol contains an a-hydroxyl secondary amine functional group, which has a pKa of 7.8. Carvedilol exhibits predictable solubility behaviour in neutral or alkaline media, i.e. above a pH of 9.0, the solubility of carvedilol is relatively low (

Documents

Application Documents

# Name Date
1 1100-MUM-2008- OTHER DOCUMENTS.pdf 2022-05-04
1 1100-MUM-2008-FORM 26(24-11-2011).pdf 2011-11-24
2 1100-MUM-2008--ASSIGNMENT(9-4-2012).pdf 2018-08-09
2 1100-MUM-2008-FORM 18(24-11-2011).pdf 2011-11-24
3 1100-MUM-2008-CORRESPONDENCE(24-11-2011).pdf 2011-11-24
3 1100-MUM-2008--CORRESPONDENCE(9-4-2012).pdf 2018-08-09
4 1100-MUM-2008-CORRESPONDENCE(IPO)-(FER)-(21-10-2014).pdf 2014-10-21
4 1100-MUM-2008-ABSTRACT(26-5-2009).pdf 2018-08-09
5 1100-MUM-2008_EXAMREPORT.pdf 2018-08-09
5 1100-MUM-2008-ASSIGNMENT(9-4-2012).pdf 2018-08-09
6 1100-MUM-2008-FORM 5(26-5-2009).pdf 2018-08-09
6 1100-MUM-2008-CLAIMS(26-5-2009).pdf 2018-08-09
7 1100-mum-2008-form 3.pdf 2018-08-09
7 1100-MUM-2008-CORRESPONDENCE(26-5-2009).pdf 2018-08-09
8 1100-MUM-2008-CORRESPONDENCE(9-4-2012).pdf 2018-08-09
8 1100-mum-2008-form 2.pdf 2018-08-09
9 1100-MUM-2008-CORRESPONDENCE(IPO)-(22-7-2008).pdf 2018-08-09
10 1100-MUM-2008-CORRESPONDENCE(IPO)-(AB21)-(3-12-2015).pdf 2018-08-09
10 1100-mum-2008-form 2(title page).pdf 2018-08-09
11 1100-mum-2008-correspondence.pdf 2018-08-09
11 1100-MUM-2008-FORM 2(TITLE PAGE)-(26-5-2009).pdf 2018-08-09
12 1100-MUM-2008-DESCRIPTION(COMPLETE)-(26-5-2009).pdf 2018-08-09
12 1100-mum-2008-form 2(26-5-2009).pdf 2018-08-09
13 1100-mum-2008-form 1.pdf 2018-08-09
14 1100-mum-2008-description(provisional).pdf 2018-08-09
15 1100-mum-2008-form 1.pdf 2018-08-09
16 1100-MUM-2008-DESCRIPTION(COMPLETE)-(26-5-2009).pdf 2018-08-09
16 1100-mum-2008-form 2(26-5-2009).pdf 2018-08-09
17 1100-mum-2008-correspondence.pdf 2018-08-09
17 1100-MUM-2008-FORM 2(TITLE PAGE)-(26-5-2009).pdf 2018-08-09
18 1100-mum-2008-form 2(title page).pdf 2018-08-09
18 1100-MUM-2008-CORRESPONDENCE(IPO)-(AB21)-(3-12-2015).pdf 2018-08-09
19 1100-MUM-2008-CORRESPONDENCE(IPO)-(22-7-2008).pdf 2018-08-09
20 1100-MUM-2008-CORRESPONDENCE(9-4-2012).pdf 2018-08-09
20 1100-mum-2008-form 2.pdf 2018-08-09
21 1100-MUM-2008-CORRESPONDENCE(26-5-2009).pdf 2018-08-09
21 1100-mum-2008-form 3.pdf 2018-08-09
22 1100-MUM-2008-CLAIMS(26-5-2009).pdf 2018-08-09
22 1100-MUM-2008-FORM 5(26-5-2009).pdf 2018-08-09
23 1100-MUM-2008-ASSIGNMENT(9-4-2012).pdf 2018-08-09
23 1100-MUM-2008_EXAMREPORT.pdf 2018-08-09
24 1100-MUM-2008-ABSTRACT(26-5-2009).pdf 2018-08-09
24 1100-MUM-2008-CORRESPONDENCE(IPO)-(FER)-(21-10-2014).pdf 2014-10-21
25 1100-MUM-2008--CORRESPONDENCE(9-4-2012).pdf 2018-08-09
25 1100-MUM-2008-CORRESPONDENCE(24-11-2011).pdf 2011-11-24
26 1100-MUM-2008-FORM 18(24-11-2011).pdf 2011-11-24
26 1100-MUM-2008--ASSIGNMENT(9-4-2012).pdf 2018-08-09
27 1100-MUM-2008-FORM 26(24-11-2011).pdf 2011-11-24
27 1100-MUM-2008- OTHER DOCUMENTS.pdf 2022-05-04