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US 5,965,161 AGranted
Extruded multi-particulates
AssigneeEuro-Celtique S.A.
InventorsBenjamin Oshlack, Mark Chasin, Hua-Pin Huang
Life of this patent
Estimating the term…
Abstract
A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.
Claims66
A unit dose sustained-release oral dosage form comprising a plurality of extruded particles, each of said particles consisting essentially of
- an opioid analgesic dispersed in a matrix comprising
- one or more retardants;
- and
- a water insoluble binder;
- said particles being non-spheroidal and having a length from about 0.1 mm to about 12 mm and a diameter from about 0.1 mm to about 5 mm, said unit dose providing a release of said opioid analgesic over at least about 6 hours, said particles being formed by mixing the opioid analgesic, the one or more retardants, and the water insoluble binder in an extruder to form said matrix, extruding the matrix in the extruder to form strands, and cutting said strands into said extruded particles.
2 more elements
A sustained-release particle comprising
- an active agent selected from the group consisting of disinfecting agents, chemical impregnants, cleansing agents, deodorants, fragrances, dyes, animal repellants, insect repellents, fertilizing agents, pesticides, herbicides, fungicides and plant growth stimulants dispersed in a matrix comprising
- at least one retardant;
- and
- a water insoluble binder selected from the group consisting of fatty alcohols, hydrogenated fats, fatty acid glycerides, hydrocarbons, waxes, hydrophobic and hydrophilic polymers having hydrocarbon backbones, fatty acid esters and mixtures thereof;
- said particle being non-spheroidal and having a length from about 0.1 mm to about 12 mm and a diameter from about 0.1 mm to about 5 mm and providing sustained release of said active agent, said particle being formed by mixing the active agent, the at least one retardant, and the water insoluble binder in an extruder to form said matrix, extruding the matrix in the extruder to form strands, and cutting said strands into said extruded particles.
2 more elements
A sustained-release formulation comprising
- a plurality of extruded particles, each of said particles comprising
- an opioid analgesic dispersed in a matrix comprising
- one or more retardants selected from the group consisting of ethylcellulose and acrylic polymers;
- and
- a water insoluble binder selected from the group consisting of fatty alcohols, hydrogenated fats, fatty acid glycerides, hydrocarbons, waxes, hydrophobic and hydrophilic polymers having hydrocarbon backbones, fatty acid esters and mixtures thereof;
- said particles being non-spheroidal and having a length from about 0.1 mm to about 12 mm and a diameter from about 0.1 mm to about 5 mm and providing sustained release of the opioid analgesic over at least about 6 hours, said particles being formed by mixing the opioid analgesic, the one or more retardants, and the water insoluble binder in an extruder to form said matrix, extruding the matrix in the extruder to form strands, and cutting said strands into said extruded particles.
3 more elements
A unit dose comprising
- a gelatin capsule containing a plurality of extruded particles, each of said particles comprising
- an opioid analgesic dispersed in a matrix comprising
- one or more retardants selected from the group consisting of ethylcellulose, acrylic polymers and mixtures thereof;
- a water insoluble binder selected from the group consisting of stearic acid;
- and
- a hydroxyalkycellulose;
- said particles being non-spheroidal and having a length from about 0.1 mm to about 12 mm and a diameter from about 0.1 mm to about 5 mm, said formulation providing sustained release of the olpioid analgesic over at least about 6 hours, said particles being formed by mixing the opioid analgesic, the one or more retardants, and the water insoluble binder in an extruder to form said matrix, extruding the matrix in the extruder to form strands, and cutting said strands into said extruded particles.
4 more elements
A method of preparing a multiparticulate sustained release oral dosage form, comprising the steps of:
- (a) feeding, in powder form, a therapeutically active agent, and a waterinsoluble retardant into an extruder;
- (b) mixing together the therapeutically active agent and the water-insoluble retardant in the extruder to obtain a homogeneous mixture;
- (c) heating said homogeneous mixture in the extruder;
- (d) extruding said homogeneous mixture with the extruder to thereby form strands;
- (e) cooling said strands containing said homogeneous mixture;
- (f) cutting said strands into generally cylindrically-shaped particles having a length from about 0.1 mm to about 12 mm and a diameter of from about 0.1 mm to about 5 mm;
- and
- (g) dividing said generally cylindrically-shaped particles into unit doses, the ratio of said water insoluble retardant to said therapeutically active agent in said mixture being sufficient to impart a release of said therapeutically active agent from said particles over a time period of at least about 6 hours when said particles are exposed to an aqueous fluid.
5 more elements
A method of treating a patient with a sustained release multiparticulate formulation of a therapeutically active agent, comprising the steps of:
- (a) feeding in powder form, a therapeutically active agent, and a waterinsoluble retardant into an extruder;
- (b) mixing together the therapeutically active agent and the water-insoluble retardant in the extruder to obtain a homogeneous mixture;
- (c) heating said homogeneous mixture in the extruder;
- (d) extruding said homogeneous mixture with the extruder to thereby form strands;
- (e) cooling said strands containing said homogeneous mixture;
- (f) cutting said strands into generally cylindrically-shaped particles having a length of from about 0.1 mm to about 12 mm and a diameter of from about 0.1 mm to about 3 mm;
- (g) dividing said generally cylindrically-shaped particles into unit doses;
- and
- (h) administering said unit dose to a patient, the ratio of said water insoluble retardant to said therapeutically active agent in said mixture being sufficient to impart a release of said therapeutically active agent from said particles over a time period of at least about 6 hours when said unit dose is administered to said patient.
6 more elements
A method of preparing a multiparticulate sustained release oral dosage form, comprising the steps of:
- (a) directly metering into an extruder a water-insoluble retardant and a therapeutically active agent to obtain a homogeneous mixture;
- (b) heating said homogeneous mixture;
- (c) extruding said homogeneous mixture to thereby form strands;
- (d) cooling said strands containing said homogeneous mixture;
- (e) cutting said strands into generally cylindrically-shaped particles having a length of from about 0.1 mm to about 12 mm and a diameter of from about 0.1 mm to about 3 mm;
- and
- (f) dividing said generally cylindrically-shaped particles into unit doses.
4 more elements
An opioid unit dose sustained-release oral dosage form having substantially no feeding-fasting effect, comprising a plurality of extruded particles, each of said particles comprising a matrix consisting essentially of
- an opioid analgesic;
- one or more retardants;
- said particles having a length from about 0.1 mm to about 12 mm and a diameter of from about 0.1 mm to about 3 mm, said unit dose providing a release of said opioid analgesic over at least about 12-24 hours, said particles being formed by mixing the opioid analgesic, the one or more retardants, an optional water insoluble binder, and optional excipients in an extruder to form said matrix, extruding the matrix in the extruder to form strands, and cutting said strands into said extruded particles.
Dependencies are inferred from the claim text.