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Highly bioavailable oral delayed release dosage forms of O-desmethylvenlafaxine succinate

A methyl venlafaxine, oral dosage technology, applied in the field of treating depression and reducing the side effects of O-desmethylvenlafaxine, can solve the problems of variable effects of hydrogel preparations

Inactive Publication Date: 2008-08-20
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, variable effects of hydrogel formulations were observed when ODV hydrogel tablets were taken with food

Method used

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  • Highly bioavailable oral delayed release dosage forms of O-desmethylvenlafaxine succinate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: 2% Surelease (Ethylcellulose Dispersion)

[0049] Element

[0050] * Not present in the final formulation

Embodiment 2

[0051] Example 2: 3% Surelease (Ethylcellulose Dispersion)

[0052] Element

[0053] Release coat:

[0054] * Not present in the final formulation

Embodiment 3

[0055] Example 3: Enteric Coated Capsules Containing Hypromellose / Microcrystalline Cellulose Spheroid Cores

[0056] Element

mg / capsule (150mgODV dose)

Small ball core:

DVS-233

227.62

microcrystalline cellulose

97.55

Hypromellose

65.0

Sealing layer:

Opadry Clear

6.50

Enteric coating:

Eudragit L30-D55

71.77

triethyl citrate

2.15

sodium hydroxide

3.23

Talc

10.64

water *

Not applicable

[0057] * Not present in the final formulation

[0058] This formulation is expected to release in vivo more than 85% of its content within 12 hours after a 2 hour lag period following oral administration of the product, and to have approximately 100% release within 20 hours.

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Abstract

An oral, highly bioavailable unit dosage form of O-desmethylvenlafaxine succinate (DVS) having a delayed release of at least about one hour and a sustained release over multiple hours to provide a total release of greater than about 85 % within about 12 to about 14 hours is described. In one embodiment, the superbioavailable DVS composition has a delayed release of about two hours and a total release of greater than about 95 % within about 12 to about 14 hours. Use of the formulation in treating depression and reducing the gastrointestinal side-effects of O-desmethylvenlafaxine (ODV) is also described.

Description

[0001] The invention relates to an oral highly bioavailable dosage form of O-desmethylvenlafaxine succinate and its use in treating depression and reducing side effects of O-desmethylvenlafaxine. Background of the invention [0002] O-desmethylvenlafaxine (ODV) is the main metabolite of venlafaxine, which selectively blocks the reabsorption of serotonin and norepinephrine. Klamerus, K.J., et al., "An introduction to the pharmacokinetic composition parameters of venlafaxine and its active O-desmethyl metabolite", J. Clin. Pharmacol. 32: 716-724 (1992). O-desmethylvenlafaxine, the chemical name is 1-[2-(dimethylamino)-1-(4-phenol)ethyl]cyclohexanol, and its fumarate is listed in US Patent No. 4,535,186. However, the physicochemical properties and permeability of the fumarate salt of O-desmethyl-venlafaxine are less suitable. The free base of O-desmethyl-venlafaxine is also listed in International Patent Application WO 00 / 32555. [0003] US Patent 6,673,838 describes the succin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/32A61K31/135A61K9/50
CPCA61K9/2054A61K9/2866A61K9/5073A61K31/135A61P25/24A61K31/137A61K9/48
Inventor S·M·沙M·B·法齐C·R·迪奥里奥
Owner WYETH LLC
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