Solventless mixing process for coating pharmaceutical ingredients

摘要

The present invention is a solventless method of producing polymer coated active pharmaceutical ingredient that is taste-masked and may be released in relatively short time. It employs high energy vibrations or acoustic mixing of API particles, water soluble coating material particles and hydrophobic polymer particles, with or without use of other pharmaceutically relevant powders as media. Additionally the method is capable of producing individually coated drug particles without agglomeration or the long drying times associated with solvent based coating methods.

主权项

1. A process for preparing a particulate pharmaceutical formulation from core particles comprising an active pharmaceutical ingredient, comprising the step of:
mixing the core particles, water soluble and/or water swellable coating material particles, and substantially water insoluble polymer particles, to produce the particulate pharmaceutical formulation comprising coated core particles; and subjecting the coated core particles to mechanical stress to deform a coating on the coated core particles into a substantially continuous or continuous film; wherein a volume averaged median particle size of the core particles is at least three times greater than a median particle size of both the water soluble and/or water swellable coating material particles and the substantially water insoluble polymer particles; less than 0.1% of the active pharmaceutical ingredient dissolves in a dissolution test indicative of taste-release in the mouth in 60 seconds; and at least 90% of an amount of the API that would have been released from uncoated core particles of a same composition and size in a United States Pharmacopeia dissolution test indicative of dissolution in the gastrointestinal tract is released within 30 minutes.