How High Drug Load Nanocrystalline Tablets Lower Pill Burden, Delivering Better Products For Patients

Enzalutamide and apalutamide are crucial treatments for advanced prostate cancer, but their crystalline forms suffer from poor water solubility, hindering effective drug absorption. Traditionally, this challenge is addressed by converting them into amorphous solid dispersions (ASDs) via spray drying. While ASDs improve apparent solubility, they typically contain a high proportion of polymers—often two-thirds or more—leading to lower drug loading. This results in larger pills and increased pill burden, impacting patient compliance.
This webinar presents a breakthrough: the successful nanoformation of enzalutamide and apalutamide using Controlled Expansion of Supercritical Solutions (CESS®) technology. We showcase the development of nanocrystal-based tablets with high drug loading, demonstrating that nanocrystals can achieve pharmacokinetic profiles equivalent to ASDs while significantly reducing pill size and overall pill burden. This advancement paves the way for single-pill formulations, enhancing patient convenience and adherence. For innovators, this technology can extend market exclusivity. For generics, it offers a unique IP position and the opportunity to introduce value-added products earlier, providing significant patient benefits.
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