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Applications of hot-melt extrusion for drug delivery.

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TLDR
The range of HME applications for pharmaceutical dosage forms, such as tablets, capsules, films and implants for drug delivery through oral, transdermal, transmucosal, transungual, as well as other routes of administration are reviewed.
Abstract
In today's pharmaceutical arena, it is estimated that more than 40% of new chemical entities produced during drug discovery efforts exhibit poor solubility characteristics. However, over the last decade hot-melt extrusion (HME) has emerged as a powerful processing technology for drug delivery and has opened the door to a host of molecules previously considered unviable as drugs. HME is considered to be an efficient technique in developing solid molecular dispersions and has been demonstrated to provide sustained, modified and targeted drug delivery resulting in improved bioavailability. This article reviews the range of HME applications for pharmaceutical dosage forms, such as tablets, capsules, films and implants for drug delivery through oral, transdermal, transmucosal, transungual, as well as other routes of administration. Interest in HME as a pharmaceutical process continues to grow and the potential of automation and reduction of capital investment and labor costs have made this technique worthy of consideration as a drug delivery solution.

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Journal ArticleDOI

Drug-polymer solubility and miscibility: Stability consideration and practical challenges in amorphous solid dispersion development.

TL;DR: This commentary attempts to discuss the concepts and implications of the drug-polymer solubility and miscibility on the stabilization of solid dispersions, review recent literatures, and propose some practical strategies for the evaluation and development of such systems utilizing a working diagram.
Journal ArticleDOI

Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

TL;DR: This review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology.
Journal ArticleDOI

A Review of Hot-Melt Extrusion: Process Technology to Pharmaceutical Products

TL;DR: This paper reviews the innumerable benefits of HME, based on a holistic perspective of the equipment, processing technologies to the materials, novel formulation design and developments, and its varied applications in oral drug delivery systems.
Journal ArticleDOI

Hot melt extrusion (HME) for amorphous solid dispersions: Predictive tools for processing and impact of drug–polymer interactions on supersaturation

TL;DR: The highest dissolution rate and supersaturation of poorly water soluble drugs could be attributed to drug-polymer interactions occurred during HME.
References
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Journal ArticleDOI

Melt extrusion: from process to drug delivery technology

TL;DR: Improved bioavailability was achieved again demonstrating the value of the technology as a drug delivery tool, with particular advantages over solvent processes like co-precipitation.
Journal ArticleDOI

Pharmaceutical Applications of Hot-Melt Extrusion: Part I

TL;DR: The pharmaceutical applications of hot-melt extrusion, including equipment, principles of operation, and process technology, are reviewed and the physicochemical properties of the resultant dosage forms are described.
Journal ArticleDOI

Solubility parameters as predictors of miscibility in solid dispersions

TL;DR: It was concluded that Hildebrand parameters give an indication of possible incompatibilities between drugs and carriers in solid dispersions, but that the use of partial solubility parameters may provide a more accurate prediction of interactions in and between materials and could provide more accurate indications of potential incomp atibilities.
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Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis

TL;DR: Combining calculation of Hansen solubility parameters with thermal analysis of drug/excipient miscibility can be successfully applied to predict formation of glass solutions with melt extrusion.
Journal ArticleDOI

High throughput physicochemical profiling for drug discovery

TL;DR: High throughput methods to measure the properties: solubility, permeability, lipophilicity, pKa, stability and integrity are described and compared and the underlying discovery requirements, needs and application strategies are discussed.
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