US 8,105,627 B2Granted

Extended release venlafaxine tablet formulation

AssigneeDexcel Ltd.

InventorsSima Volpert, Avi Avramoff

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Abstract

An extended release formulation for administration of venlafaxine in an oral tablet dosage form. The formulation preferably features a core, over which an outer coating is layered. The core preferably contains venlafaxine, a filler, and a water soluble cellulosic polymer, optionally and more preferably with a water insoluble cellulosic polymer. The core is preferably coated with a coating material. The coating preferably contains a mixture of water soluble cellulosic polymer and a water insoluble cellulosic polymer. According to a first embodiment of the present invention, the filler is preferably present in an amount of at least about 40% weight per weight of the total formulation. More preferably, the filler comprises microcrystalline cellulose. Most preferably, the filler solely comprises microcrystalline cellulose. Also most preferably, microcrystalline cellulose is present in the core in a range of from about 45% to about 65% weight per weight of the total formulation.

Claims27

Dependent claims

An extended release coated tablet formulation for venlafaxine, comprising a tablet which consists of:

(a) a core comprising a pharmaceutically effective amount of venlafaxine or a pharmaceutically acceptable salt thereof, said core being in a form of a tablet, and said core further comprising:
(i) at least 40% of a filler, weight per weight of the entire formulation;
(ii) at least 5% of a water soluble cellulosic polymer selected from the group consisting of hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose, hydroxyethyl cellulose, methyl cellulose and carboxymethyl cellulose, weight per weight of the entire formulation;
(iii) at least 5% of ethyl cellulose, weight per weight of the entire formulation;
(b) a coating for said core, said coating comprising:
(i) a water soluble cellulosic polymer that is hydroxypropyl methylcellulose (HPMC);
and
(ii) a water insoluble cellulosic polymer that is ethyl cellulose,
the tablet formulation having a dissolution profile in USP Apparatus 1 (basket) at 100 rpm in phosphate buffer at pH 6.8 according to a table:
Time (hours)
Average % Venlafaxine released
2
<30
4
25- 45
8
55- 75
12
75- 95
24
>80

18 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/555,310Filed 11 Dec 2003
Priority: EP 031012162 May 2003
Published: US 2007/0082049 A112 Apr 2007
Granted: 31 Jan 2012
Term ends: Not estimatedThe source records don’t support an estimate.

Classification4 codes

A61K 9/2866
Polysaccharides, e.g. gums; Cyclodextrin: cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
A61K 31/137
Having aromatic rings , e.g. ketamine, nortriptyline: arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
A61K 9/2054
Polysaccharides, e.g. alginate, gums; Cyclodextrin: cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
A61K
Medicines and medical preparations