Preparation of stable paroxetine HC1 ER tablets using a melt granulation process

• US 20050266082A1
• Filed: 05/13/2005
• Published: 12/01/2005
• Est. Priority Date: 05/26/2004
• Status: Abandoned Application

• Current Assignee: Pablo Davila, Satishkumar Ambalal Patel, Suresh Palaniswamy
• Original Assignee: Pablo Davila, Satishkumar Ambalal Patel, Suresh Palaniswamy
• Inventors: Davila, Pablo, Patel, Satishkumar Ambalal, Palaniswamy, Suresh
• Application Number:
  US11/129,451
• Publication Number:
  US 20050266082A1
• Time in Patent Office: Days
• US Class Current: 424/484
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61P 25/24 Antidepressants

Abstract

A pharmaceutical composition comprising a hydrophobic matrix comprised of paroxetine HCl and a lipid component is provided. The matrix also preferably contains hydrophilic polymers, e.g., hypromellose. This invention also relates to a method of making such a composition by melt granulating paroxetine HCl with a molten binder comprising a lipid component. This invention also relates to tablets which contain such a matrix as a core and which having an enteric coating surrounding said core.

Claims

1. A pharmaceutical composition comprising a hydrophobic matrix comprised of paroxetine hydrochloride and a lipid component.

2. The pharmaceutical composition of claim 1, wherein the lipid component comprises a water-insoluble material having a melting point from about 30°

C. to about 120°

C.

3. The pharmaceutical composition of claim 2, wherein the water-insoluble material has a melting point from about 40°

C. to about 90°

C.

4. The pharmaceutical composition of claim 1, wherein the water-insoluble material is selected from the group consisting of waxes, spermaceti, paraffin, lecithin, fatty acids and salts or glyceride esters thereof, C₁₂ to C₂₂ aliphatic alcohols, and mixtures thereof.

5. The pharmaceutical composition of claim 4, wherein the water-insoluble material is selected from the group consisting of beeswax, carnauba wax, microcrystalline wax, stearic acid, palmitic acid, stearyl alcohol, and cetyl alcohol.

6. The pharmaceutical composition of claim 5, wherein the water-insoluble material is stearyl alcohol.

7. The pharmaceutical composition of claim 1, wherein the hydrophobic matrix additionally comprises one or more hydrophilic polymer.

8. The pharmaceutical composition of claim 7, wherein the hydrophilic polymer is hydroxypropyl methyl cellulose having a viscosity of at least about 500 mPas when measured at 2% concentration in water at 20°

C., and hydroxypropyl methyl cellulose having a viscosity of less than about 500 mPas when measured at 2% concentration in water at 20°

C.

9. The pharmaceutical composition of claim 8, wherein the paroxetine HCl is present in an amount of from about 5% to about 25% by weight of the matrix, the amount of the lipid component is from about 10% to about 20% by weight of the matrix, and the amount of the hydroxypropyl methyl cellulose polymer is from about 5% to about 25% by weight of the matrix.

10. A method of making a pharmaceutical composition comprising melt granulating paroxetine HCl with a molten binder comprising a lipid component.