The majority (approximately 90%) of new chemical entities (NCEs) discovered by the pharmaceutical industry today are poorly soluble or lipophilic compounds; as are about 40% of existing drugs in the market. Consequently, this can create major challenges in drug development due to poor solubility, short biological half-life, poor bioavailability, prominent adverse effects, and stability of NCE’s.
Challenges with Suspension Dosing
To evaluate these compounds at the preclinical stage, the compound is often dosed orally as an aqueous-based suspension, because a solution formulation may not easily be obtained without either toxic levels of excipients and/or considerable resources (i.e., impractical at an early stage when evaluating a high number of compounds). A potential downside to this approach is that dosing a suspension may have detrimental in vivo consequences such as decreased bioavailability and higher inter-subject variability when compared to dosing a solution formulation.
Micronization Improves Solubility
Reducing a suspensions particle size with micronization can help mitigate these effects. Adaptive Focused AcousticsTM can be used for particle size in a controlled manner to make uniform suspensions with low micron or nano-scale particle sizes.
Eliminates molecular thermal damage by maintaining isothermal sample temperatures during the process
Scales from bench-top screens through clinical studies (micro-liters to 1,000+ liters) Compatible with Quality By Design and Process Analytical Technology
Enables sterile, closed, single-use fluid circuits which eliminate carryover Enables disposable wetted surfaces which minimizes impurities
Standardizes the process application of industry-proven AFA technology Automated process by minimizing subjective operator influence
Improves processing performance (from 2 days to 2 minutes); increases solubility and stability
Interested in a micronization technology project with Covaris?