Melt-extrusion multiparticulates
OwnerBenjamin Oshlack, Hua-Pin Huang +1inventors
InventorsBENJAMIN OSHLACK, HUA-PIN HUANG, MARK CHASIN
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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.
Claims38
A unit dose sustained-release oral dosage form comprising a plurality of melt extruded particles, each of said particles comprising:
- (a) a therapeutically active agent;
- (b) one or more retardants;
- and
- (c) an optional water insoluble binder;
- said particles having a (length) size from about 0.1 mm to about 12 mm, said unit dose providing a release of said therapeutically active agent over at least about 6 hours.
A method of preparing a multiparticulate sustained release oral dosage form, comprising:
- (a) mixing together a therapeutically active agent, a water-insoluble retardant, and an optional binder to obtain a homogeneous mixture, 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 4 hours when said particle is exposed to an aqueous fluid;
- (b) heating said homogenous mixture;
- (c) extruding said homogenous mixture to thereby form strands;
- (d) cooling said strands containing said homogeneous mixture;
- and
- (e) cutting said strands into particles having a size from about 0.1 mm to about 12 mm;
- and
- (f) dividing said particles into unit doses.
A method of treating a patient with a sustained release multiparticulate formulation of a therapeutically active agent, comprising:
- (a) mixing together a therapeutically active agent, a water-insoluble retardant, and an optional binder to obtain a homogeneous mixture, 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 4 hours when said particle is exposed to an aqueous fluid;
- (b) heating said homogenous mixture;
- (c) extruding said homogenous mixture to thereby form strands;
- (d) cooling said strands containing said homogeneous mixture;
- and
- (e) cutting said strands into particles having a size from about 0.1 mm to about 12 mm;
- (f) dividing said particles into unit doses;
- and
- (g) administering said unit dose to a patient.
A method of preparing a multiparticulate sustained release oral dosage form, comprising:
- (a) directly metering into an extruder a water-insoluble retardant, a therapeutically active agent, and an optional binder;
- (b) heating said homogenous mixture;
- (c) extruding said homogenous mixture to thereby form strands;
- (d) cooling said strands containing said homogeneous mixture;
- and
- (e) cutting said strands into particles having a size from about 0.1 mm to about 12 mm;
- and
- (f) dividing said particles into unit doses.
An opioid unit dose sustained-release oral dosage form having substantially no feeding-fasting effect, comprising a plurality of melt extruded particles, each of said particles comprising:
- (a) a therapeutically active agent;
- (b) one or more retardants;
- and
- (c) an optional water insoluble binder;
- said particles having a (length) size from about 0.1 mm to about 12 mm, said unit dose providing a release of said therapeutically active agent over at least about 12-24 hours.
An opioid unit dose sustained-release oral dosage form having substantially no feeding-fasting effect, comprising a plurality of melt extruded particles, each of said particles comprising:
- (a) a therapeutically active agent;
- (b) one or more retardants;
- and
- (c) an optional water insoluble binder;
- said particles having a (length) size from about 0.1 mm to about 12 mm, said unit dose providing a release of said therapeutically active agent over at least about 6 hours.
Dependencies are inferred from the claim text.