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Solvent-Assisted Hot Melt Extrusion of a Thermally Labile, High Melting Point Compound.
C Lagan1,2, J E Huckle3, J M Katz1
1Drug Product Technologies, Amgen Inc., Thousand Oaks, California, 91320, USA.
AAPS Pharmscitech
|September 9, 2021
Summary
A novel solvent-assisted hot melt extrusion (HME) method enables processing of thermally labile active pharmaceutical ingredients (APIs). This technique overcomes melting point limitations, creating amorphous solid dispersions for enhanced bioavailability.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Molecular dispersions enhance bioavailability of poorly soluble active pharmaceutical ingredients (APIs).
- Hot melt extrusion (HME) is a scalable technique for preparing molecular dispersions.
- Processing thermally labile APIs via HME is challenging due to degradation at high temperatures.
Purpose of the Study:
- To develop a modified HME method for preparing amorphous solid dispersions of thermally labile APIs.
- To overcome the limitation of API melting point in HME processing.
- To demonstrate the feasibility of processing meloxicam (MEL), a model thermally labile API, using the modified HME technique.
Main Methods:
- A solvent-assisted hot melt extrusion (HME) process was developed.
- Dimethylformamide (DMF) was incorporated into the formulation blend during extrusion.
- Extrusion was performed below the melting point of meloxicam (MEL) using a twin-screw extruder.
- A secondary vacuum drying step was employed to remove the incorporated solvent.
Main Results:
- The solvent-assisted HME method successfully prepared amorphous solid dispersions of meloxicam (MEL).
- Processing temperatures were significantly reduced, allowing for the incorporation of thermally labile APIs.
- Higher conversion of MEL to its amorphous form was achieved compared to traditional HME.
- The incorporated solvent was effectively removed post-processing.
Conclusions:
- Solvent-assisted HME is a viable technique for processing thermally labile APIs.
- This advancement expands the applicability of HME technology for drug formulation.
- The method facilitates the creation of amorphous solid dispersions, potentially improving drug bioavailability.
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