Melt-extruded orally administrable opioid formulations
AssigneeEuro-Celtique S.A.
InventorsBenjamin Oshlack, Mark Chasin, Hua-Pin Huang, David Sackler
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Abstract
Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques disclosed.
Claims27
A method of controlling the release characteristics of a therapeutically active agent from sustained-release pharmaceutical extrudate suitable for oral administration, the sustained-release pharmaceutical extrudate being prepared by blending a therapeutically active agent together with (1) a hydrophobic material selected from the group consisting of alkylcelluloses, acrylic and methacrylic acid polymers and copolymers, shellac, zein, hydrogenated castor oil, hydrogenated vegetable oil, and mixtures thereof and (2) an optional hydrophobic fusible carrier retardant material selected from the group consisting of natural or synthetic waxes, fatty acids, fatty alcohols, and mixtures thereof;
- said optional hydrophobic fusible carrier having a melting point between 30-200° C.;
- heating said blend to a temperature sufficient to soften the mixture sufficiently to extrude the same;
- extruding said heated mixture as a strand having a diameter of from 0.1-3 mm;
- cooling said strand;
- and optionally dividing said strand to form multiparticulates of said extrudate;
- the method comprising controlling the amount of air present during said extrusion phase and thereby controlling the porosity of the extrudate thereby obtained.
A method of controlling the release characteristics of a therapeutically active agent from a sustained-release pharmaceutical extrudate suitable for oral administration, the sustained-release pharmaceutical extrudate being prepared by blending in an extruder, a therapeutically active agent together with one or more hydrophobic materials selected from the group consisting of alkylcelluloses, acrylic and methacrylic acid polymers and copolymers, shellac, zein hydrogenated castor oil, hydrogenated vegetable oil, and mixtures thereof, heating said blend to a temperature sufficient to soften the mixture sufficiently to extrude the same;
- extruding said heated mixture as a strand;
- and cooling said strand;
- the method comprising controlling the amount of air present during said extrusion phase and thereby controlling the porosity of the extrudate thereby obtained.
Dependencies are inferred from the claim text.