Sustained drug release composition
Inventors
Gervais, Sonia • Smith, Damon • Contamin, Pauline • Ouzerourou, Rachid • Ma, My Linh
Assignees
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Publication Number
US-8414919-B2
Publication Date
2013-04-09
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 is directed to a solid, monolithic sustained release pharmaceutical composition having an outer surface. The composition includes a sustained release matrix having a solvent accessible surface, where the matrix comprises from about 20% to about 60% by weight of cross-linked high amylose starch, and an effective amount of at least one pharmaceutically active agent disposed within the matrix. The composition is characterized by a hardness in the range of from about 100 N to about 350 N.
The outer surface defines a score that permits the composition to be fractured along the score to produce at least two subunits. At least one of the subunits and the composition from which it is derived have substantially the same release kinetics of the active agent disposed therein. At least one of the subunits created by fracturing has a new solvent accessible surface capable of forming a barrier upon contact with a solvent.
The background problem described is that subdivision of a solid, monolithic sustained release dosage form can affect release kinetics and dissolution profiles, and therefore can affect performance such as sustained release behavior. The invention addresses this by providing a scored, fracture-permitting monolithic sustained release composition whose subunits preserve substantially the same release kinetics while introducing a new solvent accessible surface that forms a barrier upon contact with a solvent.
Claims Coverage
The partial content identifies one independent claim. It contains about five core inventive requirements spanning the sustained release matrix composition, mechanical hardness and scoring for fracturing, preservation of release kinetics in subunits, and the barrier-forming capability of a new solvent accessible surface created upon fracturing.
Solvent accessible sustained release matrix with cross-linked high amylose starch
A sustained release matrix having a solvent accessible surface comprising from about 20% to about 60% by weight of cross-linked high amylose starch, with an effective amount of at least one pharmaceutically active agent disposed within the matrix.
Hardness enabling scored fracturing into subunits
The composition having a hardness in the range of from about 100 N to about 350 N, wherein the outer surface defines a score that permits fracturing along the score to produce at least two subunits.
Subunits with substantially the same release kinetics
At least one of the subunits and the composition from which it was derived have substantially the same release kinetics of the active agent disposed therein.
New solvent accessible surface that forms a barrier
At least one of the subunits created by fracturing has a new solvent accessible surface that is capable of forming a barrier upon contact with a solvent.
Across the independent claim and its dependents, the invention centers on a scored, hardness-bounded monolithic sustained release tablet using cross-linked high amylose starch as the matrix, preserving substantially the same release kinetics after fracturing into subunits, and providing a new solvent accessible surface in at least one subunit that can form a barrier upon solvent contact.
Stated Advantages
Subunits and the intact composition have substantially the same release kinetics of the active agent disposed therein.
At least one subunit has a new solvent accessible surface capable of forming a barrier upon contact with a solvent.
Documented Applications
A sustained release pharmaceutical composition intended to provide sustained release behavior over a period extending to about 24 hours after administration, including examples discussed in connection with plasma concentration timing (up to about 24 hours).
Administration producing an effective plasma concentration of an active agent spanning from about 1 hour to about 24 hours after initial administration.
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