Sustained drug release compositions
Inventors
Gervais, Sonia • Smith, Damon • Contamin, Pauline • Ouzerourou, Rachid • Ma, My Linh
Assignees
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Publication Number
US-8795723-B2
Publication Date
2014-08-05
Expiration Date
Abstract
The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent.
Core Innovation
The invention provides a solid, monolithic sustained release pharmaceutical composition in the form of a tablet. The composition includes a sustained release matrix comprising a score that permits the composition to be broken along the score into at least two subunits, and the breaking creates at least one new solvent accessible surface on the subunits. At least one subunit exhibits a dissolution profile with a similarity factor relative to an intact form of at least 50%.
The matrix comprises about 20% to about 60% by weight of cross-linked high amylose starch. An effective amount of trazodone or a pharmaceutically acceptable salt thereof is disposed within the cross-linked high amylose starch matrix. The solid composition has a hardness of about 100 N to about 350 N and displays substantially the same release kinetics when the composition is broken to create a new solvent accessible surface.
The scored solid monolithic sustained release tablet can be divided into at least two subunits where each subunit releases the active agent with substantially the same release profile as the composition from which it was derived. The intact form and the subunits maintain dissolution behavior similarity after subdivision while preserving mechanical hardness in the tablet.
Claims Coverage
The partial content identifies two independent claims. Each independent claim centers on a scored, monolithic sustained release matrix that creates new solvent accessible surface(s) on subunits and requires dissolution-profile similarity with a similarity factor of at least 50% together with tablet form and hardness.
Scored monolithic sustained release matrix with solvent accessible surfaces
A solid, monolithic sustained release matrix comprising a score that permits the composition to be broken along the score to produce at least two subunits each having a new solvent accessible surface, where at least one subunit and an intact form have dissolution profiles with a similarity factor of at least 50%, and where the matrix comprises from about 20% to about 60% by weight of cross-linked high amylose starch.
Trazodone disposed within cross-linked high amylose starch and matched hardness/release kinetics after breakage
An effective amount of trazodone or a pharmaceutically acceptable salt thereof disposed within the matrix, wherein the composition has a hardness of from about 100 N to about 350 N, displays substantially the same release kinetics when broken to create a new solvent accessible surface, and is in the form of a tablet.
Subunit-by-subunit release substantially the same as the derived composition
A solid, monolithic sustained release matrix comprising a score that permits the composition to be broken along the score to produce at least two subunits each having a new solvent accessible surface, where at least one subunit and an intact form have dissolution profiles with a similarity factor of at least 50%, and where the matrix comprises from about 20% to about 60% by weight of cross-linked high amylose starch; each subunit releases the active agent with substantially the same release profile as the composition from which it was derived.
The inventive coverage requires a scored monolithic sustained release tablet matrix that generates new solvent accessible surface(s) when broken into subunits, dissolution-profile similarity between intact and at least one subunit, cross-linked high amylose starch in the stated range, trazodone or a pharmaceutically acceptable salt thereof, and hardness of about 100 N to about 350 N.
Stated Advantages
Substantially the same release kinetics when the composition is broken to create a new solvent accessible surface.
Subunits have dissolution profiles similar to an intact form with a similarity factor of at least 50%.
Tablet hardness is maintained, having hardness of about 100 N to about 350 N.
Each subunit releases the active agent with substantially the same release profile as the composition from which it was derived.
Documented Applications
No documented applications found
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