Stable pharmaceutical formulation of paroxetine hydrochloride anhydrous and a process for preparation thereof

a technology of paroxetine hydrochloride and pharmaceutical formulation, which is applied in the field of stable pharmaceutical formulation of paroxetine hydrochloride anhydrous and its preparation, can solve the problems of microcrystalline cellulose not being such a perfect excipient, and the hygroscopic nature of the anhydrous form

Inactive Publication Date: 2005-09-01
FOX MICHAEL +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A potential problem with paroxetine hydrochloride anhydrous tablets is the hygroscopic nature of the anhydrous form.
According to WO 02 / 069969, “[I]t is surprising that in the present invention microcrystalline cellulose acts as a perfect [excipient].” However, microcrystalline cellulose may not be such a perfect excipient.

Method used

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  • Stable pharmaceutical formulation of paroxetine hydrochloride anhydrous and a process for preparation thereof
  • Stable pharmaceutical formulation of paroxetine hydrochloride anhydrous and a process for preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

example

Example 1

[0048] Composition of Stable Tablets of Paroxetine Hydrochloride:

[0049] A paroxetine hydrochloride tablet was made which was of anhydrous form despite use of wet granulation. A tablet composition of paroxetine hydrochloride anhydrous, as made, is provided in Table 1. The manufacturing process is provided after the table.

TABLE 1Tablet Composition of Paroxetine Hydrochloride Anhydrous [Includesextra-granular excipients]Mg perINGREDIENTStabletFUNCTIONCoresParoxetine Hydrochloride22.21Active IngredientAnhydrousPovidone K-308binderDibasic Calcium Phosphate160.79FillerAnhydrousSodium starch Glycolate6.0DisintegrantMagnesium Stearate3.0LubricantPurified waterQ.S.Processing solvent (wetgranulation)Coating Suspension:*Opadry ®6.0*Composition of the Opadry ®% W / WTitanium Dioxide31.250Hydroxypropylmethylcellulose29.875(Methocel E3 Premium)Hydroxypropylmethylcellulose29.875(Methocel E5 Premium)Polyethylene Glycol 4008.000Polysorbate 80 (Tween)1.000

[0050] Manufacturing Process of St...

example 2

Paroxetine Anhydrous Tablet with Hydroxypropyl Methylcellulose as a Binder (Prepared Generally by the Same Process Disclosed in Example 1):

[0068] Paroxetine HCl Anhydrous (app. 11% w / w). [0069] Dibasic Calcium Phosphate Anhydrous (app. 82% w / w). [0070] Hydroxypropyl Methylcellulose, Grade E-5 (app. 2% w / w). [0071] Sodium Starch Glycolate (app. 3% w / w). [0072] Magnesium Stearate (app. 1.5% w / w). [0073] Purified Water (processing solvent only).

example 3

Prophetic Example

[0074] The paroxetine hydrochloride tablet prepared in Example 1 is subjected to a mechanical test-(Kraemer® Tablets Test System)

HARDNESS OF THE TABLETS, SCUHARDNESS OF THEAFTER 24 HOURS, 80° C., 75%TABLETS, SCU INITIALRELATIVE HUMIDITY1616

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PUM

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Abstract

Provided are formulations of a stable commercial paroxetine tablet comprising paroxetine hydrochloride anhydrous, povidone, copovidone or HPMC as a binder, and an HCl free / non-hygroscopic filler, prepared by the wet granulation method.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of provisional application Ser. No. 60 / 344,120, filed Dec. 28, 2001 and provisional application Ser. No. 60 / 366,351, filed Mar. 21, 2002, both of which are incorporated herein by reference.FIELD OF THE INVENTION [0002] The present invention relates to pharmaceutical formulations of paroxetine hydrochloride anhydrous and their preparation. BACKGROUND OF THE INVENTION [0003] Paroxetine, trans (−)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl) piperidine, is a serotonin re-uptake inhibitor, and has the following molecular formula: [0004] Paroxetine, disclosed in U.S. Pat. No. 4,007,196 (incorporated herein by reference), is an orally administered antidepressant for the treatment of depression, social anxiety disorders, obsessive compulsive disorder, panic disorder, generalized anxiety disorder and posttraumatic stress disorder. Other syndromes such as pre-menstrual syndrome (PMS) and male sexual...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K9/28A61K31/4525
CPCA61K9/2009A61K9/2027A61K9/2054A61K9/2059A61K31/4525A61K9/2095A61K9/2866A61K9/2886A61K9/2077
Inventor FOX, MICHAELCOHEN, RAKEFETBRAUNSTEIN, ANNELEIBOVICI, MINUTZA
Owner FOX MICHAEL
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