Pharmaceutical composition containing high drug load and method for preparing same
First Claim
1. A method for preparing a pharmaceutical composition in the form of a bead having a diameter of 0.5 to 1.5 mm and containing more than about 80% by weight medicament, which comprises forming a wet mass of medicament, non-lipophilic binder-plasticizer which is a microcrystalline cellulose in an amount within the range of from about 1 to about 15% by weight of the final composition, starch-based excipient in an amount within the range of from about 0.5 to about 12% by weight of the final composition, wherein the starch-based excipient is sodium starch glycolate, corn starch, croscarmellose, pregelatinized starch or mixtures thereof, and optionally water-soluble binder with a granulating fluid, extruding said wet mass to form an extrudate and forming said extrudate into beads and drying said beads.
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Accused Products
Abstract
A pharmaceutical composition in the form of beads prepared by an extrusion-spheronization technique and containing more than 80% by weight drug, less than 15% by weight non-lipophilic binder-plasticizer, such as microcrystalline cellulose to achieve required plasticity for processing, a starch-based excipient such as sodium starch glycolate or pregelatinized starch to control water/fluid distribution and thereby inhibit agglomeration during processing, and water-soluble binder such as hydrolyzed gelatin to make the final beads less friable. During processing a granulating agent such as ethanol/water is added to improve blend properties and control during spheronization. A method for preparing the above beads is also provided.
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Citations
19 Claims
- 1. A method for preparing a pharmaceutical composition in the form of a bead having a diameter of 0.5 to 1.5 mm and containing more than about 80% by weight medicament, which comprises forming a wet mass of medicament, non-lipophilic binder-plasticizer which is a microcrystalline cellulose in an amount within the range of from about 1 to about 15% by weight of the final composition, starch-based excipient in an amount within the range of from about 0.5 to about 12% by weight of the final composition, wherein the starch-based excipient is sodium starch glycolate, corn starch, croscarmellose, pregelatinized starch or mixtures thereof, and optionally water-soluble binder with a granulating fluid, extruding said wet mass to form an extrudate and forming said extrudate into beads and drying said beads.
Specification