A method for drug formulation and a pharmaceutical composition

A - Human Necessities – 61 – K

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A61K 31/655 (2006.01) A61K 9/16 (2006.01) A61K 9/26 (2006.01) A61K 9/52 (2006.01) A61K 31/43 (2006.01) A61K 31/60 (2006.01) B01J 2/10 (2006.01)

Patent

CA 2094030

A melt granulating method for the production of pellets (spheres) which contain a therapeutically active substance of high- dosage type. The method is characterized by: (i) mechanically working a mixture which contains (a) the active substance in cohe- sive form and (b) a binder (melting point 40°C - 100°C) while supplying sufficient energy for the binder to melt and to form spherical overwetted pellets; (ii) adding further cohesive substance, while maintaining the mechanical working; (iii) interrupting the mechanical working and supply of energy and cohesive substance when the desired mean particle size of dry pellets (spheres) has been achieved; and (iv) removing the smallest and largest particles and dividing the remaining pellets into dosage batches. A novel pharmaceutical composition containing a dosage of 300 - 500 mg of pellets obtainable from the process.

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