SOLID TABLETS AND CAPSULES OF MODIFIED RELEASE OF BENZONATATE Russian patent published in 2018 - IPC A61K31/137 A61K31/216 A61K9/22 A61K47/04 A61P11/14 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: group of inventions relates to the chemical-pharmaceutical industry and is an antitussive solid oral modified release formulation, in particular a 12-hour release, which is a tablet or capsule containing (a) benzonatate in a matrix, wherein said matrix is a homogeneous solid dispersion comprising (I) adsorbate containing benzonatate adsorbed on an adsorbent containing non-metallic silica, and (II) at least one pharmaceutically acceptable pH-independent, hydrophilic or hydrophobic matrix-forming modified release agent in an amount effective to provide a modified release profile for the benzonatate, where no more than about 55 % of the benzonatate is released from the composition within 1 hour as determined in the dissolution test in vitro, and there is no release of benzonatate from the composition in the buccal cavity. Hydrophilic matrix-forming agent in these tablets comprises a hydrophilic polymer or a mixture of low viscosity polymers, and the hydrophobic matrix-forming material contains glyceryl behenate, stearyl alcohol and/or cetyl alcohol. Tablets of the present invention may consist of a core, the composition of which is described above, and a reversible enteric coating.

EFFECT: group of inventions makes it possible to provide a modified release profile of a benzonatate, where there is practically no release of benzonatate from a tablet or capsule in the oral cavity and no more than 25 % of the release of benzonatate for 1 hour, without undesirable side effects.

26 cl, 1 dwg, 64 tbl, 18 ex