Benzonatate modified release solid tablets and capsules

摘要

A 12-hour anti-tussive modified release solid tablet or capsule is described which comprises a benzonatate adsorbate in a matrix with a sufficient amount of one or more pharmaceutically acceptable modified release pH-independent, substances to provide a 12-hour modified release profile to the benzonatate, wherein there is substantially no benzonatate release from the tablet or capsule in the buccal cavity and no more than about 25% release of the benzonatate within 1 hour as determined in an in vitro dissolution assay.

主权项

1. A modified release benzonatate solid oral composition comprising (a) a homogenous solid dispersion comprising (i) benzonatate adsorbed onto one or more of a silica, silicon dioxide or silicate to form a benzonatate adsorbate and (ii) at least one pharmaceutically acceptable modified release pH-independent, hydrophilic or hydrophobic matrix-forming substance in an amount effective to provide a modified release profile to the benzonatate, and (b) a coating over said homogenous solid dispersion,
wherein there is substantially no benzonatate release from the composition in the buccal cavity, and wherein the composition provides a pharmacokinetic profile for benzonatate, based on an equivalent of about a 300 mg dose of benzonatate administered at 12 hour intervals in a 24 hour period, of one or more of: a geometric mean area under the curve (AUC)inf of about 110 ng-h/mL to about 170 ng-h/mL, a geometric mean maximum plasma concentration (Cmax) of about 28 ng/mL to about 34 ng/mL and/or a Tmax of about 12 hours to 20 hours.