Pharmaceutical Applications of Hot-Melt Extrusion: Part I

Abstract

Interest in hot-melt extrusion techniques for pharmaceutical applications is growing rapidly with well over 100 papers published in the pharmaceutical scientific literature in the last 12 years. Hot-melt extrusion (HME) has been a widely applied technique in the plastics industry and has been demonstrated recently to be a viable method to prepare several types of dosage forms and drug delivery systems. Hot-melt extruded dosage forms are complex mixtures of active medicaments, functional excipients, and processing aids. HME also offers several advantages over traditional pharmaceutical processing techniques including the absence of solvents, few processing steps, continuous operation, and the possibility of the formation of solid dispersions and improved bioavailability. This article, Part I, reviews the pharmaceutical applications of hot-melt extrusion, including equipment, principles of operation, and process technology. The raw materials processed using this technique are also detailed and the physicochemical properties of the resultant dosage forms are described. Part II of this review will focus on various applications of HME in drug delivery such as granules, pellets, immediate and modified release tablets, transmucosal and transdermal systems, and implants.

Hot-Melt Extrusion (HME): From Process to Pharmaceutical Applications

“…HME has now provided opportunity for use of materials in order to mask the bitter taste of active substances. Since industrial application of the extrusion process back in the 1930's HME has received considerable attention from both the pharmaceutical industry and academia in a range of applications for pharmaceutical dosage forms, such as tablets, capsules, films and implants for drug delivery through oral, transdermal and transmucosal routes [5]. This makes HME an excellent alternative to other conventionally available techniques such as roll spinning and spray drying.…”

“…So far, the USA and Germany hold approximately more than half (56%) of all issued patents for HME in the market [69]. Despite this increased interest, only a handful of commercialized HME pharmaceutical products are currently marketed.…”

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

“…Several water-soluble polymeric carriers suitable for HME applications have been identified (e.g. hydroxypropyl cellulose, polyethylene oxide, poly(vinyl pyrrolidone) (Crowley et al, 2007), polyvinyl alcohol (Dawson and Stevens, 2002)). …”

Taste Masking of Griseofulvin and Caffeine Anhydrous Using Kleptose Linecaps DE17 by Hot Melt Extrusion

“…However, there is an imperative need for more robust, costeffective, and easy to scale-up taste masking technologies. Hot melt extrusion (HME) initially used in the plastic industry has attracted significant interest in the pharmaceutical industry over the last decade as a continuous, one-step process for solid dispersions development with considerable advantages over solvent-based processes such as spray drying and coprecipitation techniques (4,5). Additionally, it can be used to develop various formulations such as controlled release matrices, sustained release matrices, topical films, etc.…”