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Extended release tablet formulations of venlafaxine

A technology of delayed release and tablet, applied in the field of preparation of the formulation, delayed or slow release tablet formulation, and can solve the problems of difficult preparation, time-consuming preparation, etc.

Inactive Publication Date: 2007-01-03
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, such encapsulated formulations are more difficult and time-consuming to manufacture than delayed-release tablets, which require less complex machinery

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0040] ingredients

[0041] * Equivalent to 75mg base

[0042] ** Carboxyvinyl polymers are commercially available from BF Goodrich, Pharmaceuticals Division

[0043] Dissolution test

[0044] Dissolution tests were carried out over a 24 hour time course using USP type 2 apparatus in 900 ml water at 100 rpm or in 900 ml simulated medium at 50 rpm. As for the simulated liquid, it was first dissolved in 900ml simulated gastric juice USP (without enzyme) for 2 hours, and then the medium was replaced with 900ml simulated intestinal fluid USP (without enzyme). Dissolution tests were performed at 37°C. 5 ml samples were withdrawn from the dissolution vessel at the required time intervals and the venlafaxine hydrochloride content and thus its dissolution rate were determined by UV spectroscopy. The dissolution data shown are the average of at least 3 tablets.

[0045] result

[0046] The results obtained from the dissolution tests are shown in Table 1 below.

[0047...

example 2

[0065] * Equivalent to 75mg base

[0066] Dissolution test / results

[0067] Dissolution tests were carried out as described in Example 1 and the results shown in Table 4 were obtained:

[0068] time

example 3

[0071] * Equivalent to 75mg base

[0072] Dissolution test / results

[0073] Dissolution tests were carried out as described in Example 1 and the results shown in Table 5 were obtained:

[0074] time

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PUM

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Abstract

This invention relates to an extended release tableted dosage formulation of the antidepressant venlafaxine hydrochloride or an optical form thereof having improved bioavailability.

Description

technical field [0001] The present invention relates to the use of delayed-release tablet formulations of venlafaxine in medicine and veterinary medicine, more specifically, the present invention relates to venlafaxine and venlafaxine enantiomers (R or S) Delayed or slow release tablet formulations in the form of , the invention also relates to methods for the preparation of said formulations and their use. Background technique [0002] Neuropharmacology of venlafaxine, 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-cyclohexanol, in the treatment of depression and common anxiety disorders It is an important drug in therapy (armentarium). Venlafaxine and its acid addition salts are disclosed in US Patent No. 4,535,186. Currently, adults are orally administered venlafaxine hydrochloride in the form of compressed tablets, taken 2 or 3 times a day, in doses ranging from 75 to 350 mg / day. European Patent No. 0639374 discloses that venlafaxine is effective in the treatment of o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61K9/22A61K9/20
CPCA61K9/2013A61K9/2054A61K9/2027A61K31/137A61K9/20
Inventor 迈克尔·罗利安杰拉·波茨爱德华·希姆斯
Owner WYETH LLC