Stable pharmaceutical formulation of paroxetine hydrochloride anhydrous and a process for preparation thereof
AssigneeTeva Pharmaceutical Industries Ltd.
InventorsMichael Fox, Rakefet Cohen, Anne Braunstein, Minutza Leibovici
Life of this patent
Estimating the term…
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.
Claims92
An oral pharmaceutical dosage form comprising paroxetine hydrochloride anhydrous, a binder selected from the group consisting of povidone and copovidone, and a filler that is HCl free or non-hygroscopic, wherein the pharmaceutical dosage form is prepared by wet granulating paroxetine hydrochloride in the presence of a binder grade of povidone or copovidone, and the filler, to obtain an intra-granular portion of a granulate, and converting the granulate to the oral pharmaceutical dosage form.
A process for preparing an oral pharmaceutical dosage form, comprising the steps of:
- a) wet granulating paroxetine hydrochloride anhydrous in the presence of a binder grade of a binder selected from the group consisting of povidone or copovidone, and an HCl free or a non-hygroscopic filler, to obtain an intra-granular portion of a granulate;
- b) drying the granulate;
- c) preparing a final blend from the granulate;
- and
- d) converting the final blend to an oral pharmaceutical dosage form.
A tablet comprising of the following active ingredient and excipients, in weight to weight percentages:
- a) about 10% to about 12.5% of paroxetine hydrochloride anhydrous;
- b) about 70% to about 90% of dibasic calcium phosphate anhydrous;
- c) about 1.5% to about 5% of sodium starch glycolate;
- d) about 0.5% to about 3% of magnesium stearate;
- and
- e) about 2.5% to about 7.5% of povidone,
- wherein the tablet is prepared by wet granulating paroxetine hydrochloride anhydrous in the presence of povidone, dibasic calcium phosphate anhydrous and sodium starch
- glycolate to obtain a granulate, and converting the granulate to the tablet.
A process for preparing a paroxetine hydrochloride anhydrous tablet comprising the steps of:
- a) wet granulating with water as a processing solvent paroxetine hydrochloride anhydrous in the presence of sodium starch glycolate, Grade 29 to Grade 32 povidone and dibasic calcium phosphate anhydrous to obtain a granulate;
- b) drying the granulate to obtain LOD-NMT of about 1%;
- c) milling the granulate;
- d) mixing the granulate with an additional amount of sodium starch glycolate and calcium phosphate dibasic anhydrous;
- e) adding magnesium stearate to obtain a final blend;
- and
- f) compressing the final blend to obtain the tablet.
An oral pharmaceutical dosage form comprising paroxetine hydrochloride anhydrous, a binder grade of HPMC as a binder, and a filler that is HCl free or non-hygroscopic, wherein the pharmaceutical dosage form is prepared by wet granulating paroxetine hydrochloride in the presence of a binder grade of HPMC, and the filler, to obtain an intra-granular portion of a granulate, and converting the granulate to the oral pharmaceutical dosage form.
A process for preparing an oral pharmaceutical dosage form comprising the steps of:
- a) wet granulating paroxetine hydrochloride anhydrous in the presence of a binder grade of HPMC and an HCl free or a non-hygroscopic filler to obtain an intra-granular portion of a granulate;
- b) drying the granulate;
- c) preparing a final blend from the granulate;
- and
- d) converting the final blend to an oral pharmaceutical dosage form.
A tablet comprising of the following active ingredient and excipients, in weight to weight percentages:
- a) about 10% to about 12.5% of paroxetine hydrochloride anhydrous as an active ingredient;
- b) about 70% to about 90% of dibasic calcium phosphate anhydrous;
- c) about 1.5% to about 5% of sodium starch glycolate;
- d) about 0.5% to about 3% of magnesium stearate;
- and
- e) about 1% to about 4% of HPMC,
- wherein the tablet is prepared by wet granulating paroxetine hydrochloride anhydrous in the presence of HPMC, dibasic calcium phosphate anhydrous and sodium starch glycolate to obtain a granulate, and converting the granulate to the tablet.
A process for preparing a paroxetine hydrochloride anhydrous tablet comprising the steps of:
- a) wet granulating with water as a processing solvent paroxetine hydrochloride anhydrous in the presence of sodium starch glycolate, HPMC with a viscosity of about 2 mPa*s to about 20 mPa*s for about a 2% solution in water at about 20° C. and dibasic calcium phosphate anhydrous to obtain a granulate;
- b) drying the granulate to obtain LOD-NMT of about 1%;
- c) milling the granulate;
- d) mixing the granulate with an additional amount of sodium starch glycolate and calcium phosphate dibasic anhydrous;
- e) adding magnesium stearate to obtain a final blend;
- and
- f) compressing the final blend to obtain the tablet.
Dependencies are inferred from the claim text.