Exploring Hot-Melt Extrusion
When it comes to developing a viable formulation for an API with poor solubility and poor bioavailability, manufacturers should look to hot-melt extrusion (HME) – a well-established process that is easy to scale up with the right mathematical models
Sampada Upadhye | | Longer Read
This article was published in our sister publication, The Small Molecule Manufacturer, which celebrates the field of small molecule drug development and manufacturing with interviews and articles focusing on success stories, equipment, and new processing techniques. Read more about The Small Molecule Manufacturer here https://themedicinemaker.com/manufacture/small-but-never-forgotten
First developed for polymer processing in the plastics industry in the 1930s, hot-melt extrusion (HME) is a well-established and flexible technology in the pharma industry. HME facilitates the formulation of low-solubility, low-permeability drugs into a number of patient-friendly dose forms, including tablets, capsules or free-flowing granules.
HME uses heat and pressure to melt a polymer before it is forced at constant pressure through an orifice (see sidebar: “How HME Works”). The resulting “extrudate” is then further processed into products that display uniform API particle distribution and density. HME has become widely used in drug product development, because of the added flexibility it offers; by selecting suitable polymeric matrix excipients, formulators can create products that achieve higher bioavailability (than traditional formulations) as well as targeted delivery into the upper regions of the intestine, when drugs have poor solubility and/or poor permeability.
Poorly-soluble APIs are a key challenge for the development of solid dosage forms. The more efficiently the active ingredient can be released from a specific delivery system into the bloodstream, the better its bioavailability. It is estimated that up to 90 percent of all newly-synthesized APIs are poorly soluble and almost half of drug development project failures are due to a lack of API solubility and the resulting poor drug bioavailability and/or variable pharmacological behavior (1).
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