White Paper on Aspirin
Seqen’s survey used control parameters on the Rondol vertical extruder such as drug loading, screw configuration and process temperature to demonstrate that for a 45% AcetylSalicylic Acid (ASA) – 55% water soluble polymer Soluplus® extruded at 130°C, Aspirin is completely amorphous with no tendency to recrystallize after 6 weeks.
In vitro pharmacokinetic studies would now need to be performed to validate the impact of ASA amorphization and understand the interaction between ASA and the Soluplus® polymer and its impact on bioavailability and release profile.
AcetylSalicylic Acid (ASA better known as Aspirin) is one of the most popular Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) in the world. First used as a pain killer, Aspirin also brings lesser-known benefits that can be essential to prevent cardiovascular events. Further applications are currently being developed to prevent certain forms of cancer as well as cognitive decline.
Aspirin formulation is very well documented but has not really been changed for decades. In our collaboration with Seqens, we decided to investigate a possible improvement in bioavailability in order to foster both its known usages and its repurposing for cancer or cardiovascular applications.
A recent survey done in Brazil with a similar model drug confirmed hot melt extrusion (HME) as a technology that can bring important benefits by obtaining formulations with improved characteristics, such as faster disintegration, higher drug solubilization, and better stability. In the case of Aspirin, HME could therefore help to reduce some of its well-known secondary effects on the digestive system.