Sustained drug release composition
Inventors
Gervais, Sonia • Smith, Damon • Contamin, Pauline • Ouzerourou, Rachid • Ma, My Linh
Assignees
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Publication Number
US-8962019-B2
Publication Date
2015-02-24
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
A solid, monolithic sustained release pharmaceutical composition has an outer surface and includes a sustained release matrix having a solvent accessible surface. The matrix comprises from about 15% to about 85% by weight of a controlled release excipient selected from the group consisting of cross-linked high amylose starch, hydroxypropylmethylcellulose, and a combination thereof, and an effective amount of at least one pharmaceutically active agent is disposed within the matrix. The composition has a hardness of greater than 100 N.
The outer surface defines at least one score that permits the composition to be fractured along the score to produce at least two subunits. At least one of the subunits and an intact form of the composition have substantially the same release kinetics of the active agent disposed within the matrix, and their dissolution profiles have a similarity factor of at least 60%.
When an outer surface comprises a coating surrounding the matrix, the coating does not affect the release kinetics of the active agent disposed within the matrix. The fracture-related behavior is attributed to a newly exposed solvent-accessible surface that acts as a membrane-like barrier. Example sustained release compositions are described in tablet and caplet forms, including subdivision by scoring while maintaining substantially similar release kinetics and dissolution profiles.
Claims Coverage
The document centers on one independent claim, which defines a scored, fractured solid monolithic sustained release composition with solvent-accessible surface behavior and maintained release kinetics upon subdivision. The key inventive concept is supported by dependent claims that further constrain hardness, formulation ranges, excipient details, and forms.
Scored monolithic sustained release matrix with solvent accessible surface
A solid, monolithic sustained release pharmaceutical composition having an outer surface, the composition comprising a sustained release matrix having a solvent accessible surface, wherein the matrix comprises from about 15% to about 85% by weight of a controlled release excipient selected from the group consisting of cross-linked high amylose starch, hydroxypropylmethylcellulose and a combination thereof, and an effective amount of at least one pharmaceutically active agent disposed within the matrix, wherein the composition has hardness of greater than 100 N.
Fracturable outer surface producing subunits with substantially same release kinetics
The outer surface of the composition defining at least one score that permits the composition to be fractured along the score to produce at least two subunits, wherein at least one of the subunits and an intact form of the composition have substantially the same release kinetics of the active agent disposed therein and their dissolution profiles have a similarity factor of at least 60%.
Coating does not affect release kinetics
Wherein, if the outer surface comprises a coating surrounding the matrix, the coating does not affect the release kinetics of the active agent disposed within the matrix.
Overall claim coverage is focused on maintaining substantially the same release kinetics after fracturing along a score, using a sustained release matrix with a solvent accessible surface and ensuring dissolution profile similarity, while optionally preventing any coating from affecting release kinetics.
Stated Advantages
Subunits produced by fracturing along the score have substantially the same release kinetics as an intact form of the composition.
Subunits and an intact form have dissolution profiles with a similarity factor of at least 60%.
If an outer surface comprises a coating surrounding the matrix, the coating does not affect the release kinetics of the active agent.
Documented Applications
In vitro dissolution comparisons are described for intact versus bisected tablets, including scoring-depth effects.
Sustained release pharmaceutical compositions are described with active agents including trazodone, tramadol, acetaminophen, and betahistine.
Tablet and caplet forms are described in connection with scoring and subdivision into subunits.
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