CONTROLLED RELEASE AND TASTE MASKING ORAL PHARMACEUTICAL COMPOSITION

摘要

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

主权项

1. A solid oral formulation for enhancing release of budesonide in the colon, comprising:
an extended release core comprising 9 mg of budesonide, hydroxypropyl cellulose and optionally other excipients; and a gastro-resistant coating comprising a copolymer of methacrylic acid and methyl methacrylate in 1:1 ratio, a copolymer of methacrylic acid and methyl methacrylate in 1:2 ratio, and optionally other excipients to control the release of said budesonide from the solid oral formulation, wherein following oral administration of a single dose to a human, the formulation provides a mean AUC0-t of said budesonide in said human of about 13555.9±7816.9 (pg)(hr)/mL in 36 hours.