Dec 11, 20 hot melt extrusion hme as a technique for producing amorphous solid dispersion asd has been widely used in pharmaceutical research. Extruders provide extensive mixing and agitation that causes deaggregation of the suspended particles in the molten polymer resulting in a uniform dispersion. The sulindacpolymerplasticizer combination that was stable with good film forming properties was processed by hot melt mixing, a technique close to hot melt extrusion, to predict its behavior in a hot. Writers aliaune thiam, gwen stefani, giorgio tuinfort, akon. Hot melt extrusion manufacturing process melt extrusion is an excellen t process to formulate poorly soluble drugs and to improve bioavailability advantages vs spray drying continuous process choice of an appropriate polymer is crucial for the formulation and the process most important polymer features aretg and melt viscosity. Hot melt extruder pharmaceutical machine manufacturers and. Oct 20, 2015 hot melt extrusion hme is a wellknown process in plastic industry to produce products of uniform shape and density and its application dates back to the 1930s. In the 1980s, basf became the first company to apply it to the production of pharmaceuticals for enhancing the solubility. Abstract the objective of this doctoral thesis was to evaluate the use of several nonconventional polymers as matrix excipients for hot melt extruded oralrelease formulations. Solid dispersions can be obtained using different processes. Hot melt extrusion hme is a proven technology for bioavailability enhancement of poorly soluble apis. Basf publishes first hot melt extrusion compendium plastics. Hot melt extrusion system for pharmaceutical applications.
Pharmaceutical applications is an essential multidisciplinary guide to the emerging pharmaceutical uses of this processing technology for researchers in academia and industry working in drug formulation and delivery, pharmaceutical engineering and processing, and polymers and materials science. Hme has already been demonstrated as a robust, novel technique to make solid dispersions in order to provide time controlled, modified, extended, and. Hme is recently being used in healthcare industry to manufacture medical devices, amorphous solid dispersion asd to enhance bioavailability of poorly soluble api, targeted release drug delivery systems, implants, bioadhesive. Dec 11, 2010 basf has now published the first compendium on hot melt extrusion, a method that is being increasingly used in the pharmaceutical industry to help an active drug substance to dissolve properly in the stomach and provide more effective treatment. Since then we have continuously expanded our solution offer. Interactions between drugs and polymers influencing hot melt. Hot melt extrusion is the upgraded version of twin screw extruder with heating as an element, the whole process involves hopper for feeding the raw material along with waxes which is pre. Pharmaceutical applications is an essential multidisciplinary guide to the emerging pharmaceutical uses of this processing technology for researchers in academia and industry working.
The temperatures of the individual barrels were in a range of 100150c. Basf publishes first hot melt extrusion compendium. Leveraging hot melt extrusion for solubility and continuous. Williams iii 1, 1 molecular pharmaceutics and drug delivery, college of pharmacy, the university of texas at austin, 2409 university avenue, austin, tx. You can find detailed information on our product range by looking up your industry or using our product finder. Hot melt extrusion with basf pharma polymers extrusion compendium 2nd revised and enlarged edition k. The barrel had ten sections barrel zones, which were individually heated with electric heaters. The new edition provides readers with an even better understanding of solid dispersions and the hotmelt extrusion process. A systematic stepbystep approach is presented, where thermodynamics, polymer screening, multivariate statistics and process optimization are combined, to increase the success of hmebased drug product development. Improved mesalamine release by hotmelt extrusion hme technique could be utilized for better management of inflammatory bowel disease ibd. Three dimensional 3d printing as an advanced manufacturing technology is progressing to be established in the pharmaceutical industry to overcome the traditional manufacturing regime of one size fits for all. The extrudability of a polymer is mainly determined by t g or t m and melt viscosity. Unlike other formulation options, hot melt extrusion technology is solventfree.
Basf has been committed to the pharmaceutical industry since we introduced our original kollidon in the early 20th century. Hot melt extruded filaments based on pharmaceutical grade polymers for 3d printing by fused deposition modeling. 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. Pdf pharmaceutical applications of hotmelt extrusion. Hotmelt extrusion resulted in an even higher mixing capability. Useful for understanding hotmelt extrusion technology and principles. Hotmelt extrusion is a sophisticated technology used to develop solid dispersion dosage forms for improved drug solubility and bioavailability, a common challenge for formulation scientists in the. Pharmaceutics free fulltext polymers for extrusion. Hot melt extrusion hme is a wellknown process in plastic industry to produce products of uniform shape and density and its application dates back to the 1930s. Hotmelt extrusion hme is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market.
The interest in hotmelt extrusion has increased rapidly in the pharmaceutical industry during the last years which has led to a demand in. The role of polymer excipients in hot melt extrusion a. It offers an overview of basf s polymers, more realworld application data and factors to consider in the formulation process. Melt extrusion materials, technology and drug product. Products made from melt extruded polymers range from. Here the use of the spraydried copolymer did not show any benefit concerning the kinetic miscibility of the drug and copolymer, but it resulted in a remarkable decrease in the torque experienced by the extruder allowing extrusion at lower temperature and torque. In the 1980s, basf became the first company to apply it to the production of pharmaceuticals for enhancing the solubility and bioavailability of poorly soluble actives. Three dimensional 3d printing as an advanced manufacturing technology is progressing to be established in the pharmaceutical industry to overcome the traditional manufacturing regime of one.
Overallapplicationsofhme extrusion technology is one of the most important fabrication processes in the plastic and rubber industries. It offers an overview of basf s polymers, more realworld application. Hotmelt extrusion with basf pharma polymers extrusion compendium 2nd revised and enlarged edition k. Provide on the one hand an efficient screening tool for hotmelt extrusion hme formulation development and make available on the other. Polymers for hotmelt extrusion must exhibit thermoplastic characteristics and must be thermally stable at the proper extrusion temperature. Today we solve unmet formulation needs and offer intelligent solutions for today and tomorrows challenges in drug formulation. Hot melt extrusion hme technology has become a key solution to adding absorption for enhanced solubility. The biggest challenge for the application of hme is. We produce excipients and active ingredients of outstanding quality and performance. Nonconventional polymers as matrix excipients for hot melt.
Solid dispersions by hotmelt extrusion pharmaceutical. Hotmelt extruded filaments based on pharmaceutical grade polymers for 3d printing by fused deposition modeling. Nov 23, 2010 hot melt extrusion resulted in an even higher mixing capability. Hot melt extrusion is the upgraded version of twin screw extruder with heating as an element, the whole process involves hopper for feeding the raw material along with waxes which is pre mixed in solid form. Effective delivery of many of bcs class ii compounds with low solubility can be enabled with amorphous dispersions made by hotmelt extrusion hme. Compared with other pharmaceutical technologies, such as granulation and compression, hot melt extrusion is still an emerging method, and its potential has not been explored fully yet. Formulation and characterization of solid dispersion. Suitability of pure and plasticized polymers for hot melt.
Polymers are the key materials that are necessary for 3d. Hot melt extrusion is the new mixer extrusion range that builds on the proven umang technology and its benefits. Here the use of the spraydried copolymer did not show any benefit concerning the kinetic miscibility of the drug and copolymer. This paper presents a novel onestep process for converting a liquid stabilized nanosuspension into a solid formulation via hotmelt extrusion combined with an internal devolatilization. Bioavailability enhancement using hot melt extrusion basf. Polymeric formulations for drug release prepared by hot melt extrusion 1. In developing an hme drug system, the glass transition and melting temperatures are critical factors. Mes and hydrophilic polymers like eudragit epo, kollidonva64 and peg 6000 were hot melt extruded using a corotating twinscrew laboratory extruder. Hot melt extrusion hotmelt extrusion hme is used for blending, melting, extrusion and shaping in a single step process. One major advantage is the fact that no solvents are required.
Polymeric formulations for drug release prepared by hot melt. Hot melt extrusion for amorphous solid dispersions. Polymeric formulations for drug release prepared by hot. Polymers for hot melt extrusion must exhibit thermoplastic characteristics and must be thermally stable at the proper extrusion temperature. The objective of this doctoral thesis was to evaluate the use of several nonconventional polymers as matrix excipients for hot melt extruded oralrelease formulations.
Extrusion compendium 2nd revised and enlarged edition 2012. Jul 10, 2015 hot melt extrusion hme is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. Pharmaceutics free fulltext polymers for extrusionbased. A systematic stepbystep approach is presented, where thermodynamics, polymer. Interactions between drugs and polymers influencing hot. Investigation of pharmaceutical hotmelts via simultaneous. Over the last three decades industrial adaptability has allowed hot melt extrusion hme to gain wide acceptance and has already established its place in the broad spectrum of manufacturing operations and pharmaceutical research developments. Interest in hotmelt extrusion techniques for pharmaceutical applications is growing rapidly with well over 100 papers published in the pharmaceutical scientific literature in the last 12 years. Nir and raman for hme lien saerens seps pharma, gent, belgium workshop explanation and group assignment workshops session ii. Through science and innovation we provide our customers with products to meet the current and future needs of business and society.
In drug discovery and development, industry estimates that more than 50% of. Our affinisol polymers are specifically tailored to address the solubilization performance requirements of your apis, whether you have chosen to formulate via spraydried dispersion sdd or hot melt extrusion hme. In developing an hme drug system, the glass transition and. Author bart claeys ugent promoter chris vervaet ugent and jean paul remon ugent organization.
Improved mesalamine release by hot melt extrusion hme technique could be utilized for better management of inflammatory bowel disease ibd. University of groningen innovative platform technologies. Scale up of a hot melt extrusion process andreas gryczke basf. However, as with other innovations, numerous obstacles have to be overcome before the technology and resulting dosage forms can be exploited commercially. Hot melt extrusion is a sophisticated technology used to develop solid dispersion dosage forms for improved drug solubility and bioavailability, a common challenge for formulation scientists in the development of drug products today. Over the last three decades industrial adaptability has allowed hotmelt extrusion hme to gain wide acceptance and has already established its place in the broad spectrum of manufacturing operations.
By drawing on continuous processing, hot melt extrusion is more economical and can be used for abuse deference and taste masking applications. Prior to joining basf he worked for croda international in uk, japan and usa. Comparison between hotmelt extrusion and spraydrying for. It offers an overview of basf s polymers, more realworld application data and. Hot melt extrusion hot melt extrusion hme is used for blending, melting, extrusion and shaping in a single step process. One major advantage is the fact that no solvents are. Hotmelt extruded filaments based on pharmaceutical grade. Our affinisol polymers are specifically tailored to address the solubilization performance requirements of your apis. Hot melt extrusion hme as a technique for producing amorphous solid dispersion asd has been widely used in pharmaceutical research. Introduction since the 1930s, hot melt extrusion hme has found its place as an established process in the plastic and food. Temperature and moisture activated drugpolymer interactions for enhanced stability. Today, hme is an accepted process for creating solid dispersions of apis. You can find detailed information on our product range by looking up. Hme is also a continuous process, which has been encouraged by the fda.
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