Thermo-kinetic mixing for pharmaceutical applications
Inventors
Brough, Chris • McGinity, James W. • Miller, Dave A. • DiNunzio, James C. • Williams, III, Robert O.
Assignees
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Publication Number
US-12023343-B2
Publication Date
2024-07-02
Expiration Date
Abstract
Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
Core Innovation
The invention relates to a method of making a pharmaceutical composition by making a melt blended pharmaceutical composite comprising processing one or more active pharmaceutical ingredients (APIs) with one or more pharmaceutically acceptable excipients by thermokinetic compounding for less than 300 seconds, wherein the thermokinetic compounding forms a melt blended pharmaceutical composite. The thermokinetic compounding is characterized as processing that forms melt blended pharmaceutical composite under a brief thermokinetic compounding time.
The melt blended pharmaceutical composite is then processed into a pharmaceutical composition by hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding. The composite is described as including melt blended pharmaceutical composites that can be amorphous and single-phase, and may correspond to amorphous solid dispersions and miscible/heterogeneous composites produced via thermokinetic processing.
The disclosures further associate the thermokinetic compounding approach with controlling solid-state properties such as glass transition temperature and stability, and with limiting degradation of the API while retaining drug potency. The documented composite outcomes include lower degradation products and retained potency thresholds, with morphology constraints such as a single-phase amorphous composite.
Claims Coverage
The document provides one independent claim method and multiple dependent refinements that collectively specify the thermokinetic compounding conditions, the resulting composite attributes, optional excipient/API selections, and performance/safety thresholds. The independent claim covers the overall workflow: thermokinetic compounding to form a melt blended pharmaceutical composite for less than 300 seconds, followed by conversion to a final pharmaceutical composition via one of multiple downstream processing routes.
Thermokinetic compounding to form a melt blended pharmaceutical composite in less than 300 seconds
Making a melt blended pharmaceutical composite comprising processing one or more active pharmaceutical ingredients (APIs) with one or more pharmaceutically acceptable excipients by thermokinetic compounding for less than 300 seconds, wherein the thermokinetic compounding of the one or more active pharmaceutical ingredients and the one or more pharmaceutically acceptable excipients forms a melt blended pharmaceutical composite.
Convert the melt blended pharmaceutical composite into a pharmaceutical composition by selected downstream processing
Processing the melt blended pharmaceutical composite by hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding to make the pharmaceutical composition.
Overall, claim coverage centers on brief thermokinetic compounding (<300 seconds) that forms a melt blended pharmaceutical composite from APIs and pharmaceutically acceptable excipients, and on subsequent conversion of that composite into a pharmaceutical composition using conventional downstream manufacturing processing options listed in the claim.
Stated Advantages
Less than 300 seconds thermokinetic compounding time.
Limitation of API degradation products by defining a composite containing less than about 1.0% degradation products of the at least one API.
Retention of drug potency by requiring at least about 94% drug potency after thermokinetic compounding.
Control of composite solid-state form by specifying a single-phase amorphous composite.
Documented Applications
Making pharmaceutical compositions from melt blended pharmaceutical composites produced by thermokinetic compounding, followed by conversion to compositions using hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
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