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.read more
Citations
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Drug-polymer solubility and miscibility: Stability consideration and practical challenges in amorphous solid dispersion development.
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References
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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.
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Pharmaceutical Applications of Hot-Melt Extrusion: Part I
Michael M. Crowley,Feng Zhang,Michael A. Repka,Sridhar Thumma,Sampada B. Upadhye,Sunil Kumar Battu,James W. McGinity,Charles R. Martin +7 more
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.
Journal ArticleDOI
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.