Injection moulded controlled release amorphous solid dispersions: Synchronized drug and polymer release for robust...

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery Systems

Background:

• Conventional extended release (ER) tablets often face challenges with incomplete drug release and stability.
• Amorphous solid dispersions (ASD) offer potential for improved drug solubility and bioavailability.
• Polyethylene oxide (PEO) is a widely used polymer in hydrophilic matrix systems for controlled drug release.

Purpose of the Study:

• To evaluate the controlled release performance of injection moulded (IM) ASD tablets containing AZD0837 and PEO.
• To compare the stability and release robustness of IM ASD tablets against conventional direct compressed (DC) ER tablets.
• To elucidate the drug and polymer release mechanisms from both tablet formulations.

Main Methods:

• Fabrication of caplet-shaped IM ASD tablets and DC ER tablets using AZD0837 and PEO.
• Characterization of physical/chemical storage stability and release profiles under varying hydrodynamic conditions.
• Dissolution studies to analyze synchronized release of drug and polymer.

Main Results:

• IM ASD tablets exhibited complete and synchronized release of AZD0837 and PEO, even in limited dissolution media.
• Conventional DC ER tablets showed slower and incomplete AZD0837 release.
• AZD0837 remained amorphous and stable in a supersaturated state throughout dissolution from IM ASD tablets.
• IM tablets demonstrated robustness against variations in dissolution environment hydrodynamics and PEO molecular weight.

Conclusions:

• Injection moulding of ASD tablets with PEO provides a superior controlled release system for AZD0837.
• Synchronized release from IM ASD tablets ensures drug stability and maintains supersaturation, enhancing bioavailability.
• IM ASD technology offers a robust and reliable alternative to conventional ER tablet manufacturing.