Category | Small Molecule
As active pharmaceutical ingredients (APIs) become increasingly complex, they pose potential formulation problems that can extend timelines and explode budgets. Certain physiochemical characteristics, such as melting points, density, flowability, and compressibility, may be manageable at a smaller scale, but production at greater volumes can present a completely different story. The last thing any developer should have to do is repeat early-development stages when many of these challenges can be anticipated and mitigated with proper expertise and understanding of the formulation space.
Complex molecules react more sensitively to changes in conditions and can have a greater variety of side reactions than simpler APIs. To anticipate these circumstances, API and drug product development teams can work together during phase I and phase II trials to understand critical physical properties and determine the target characteristics of the API at scale-up. These characteristics should be adopted as the formal specification for future production. Some tools to support this approach include:
Every day, our teams work to improve existing tools or develop new strategies to address formulation challenges. Some areas of formulation innovation that Thermo Fisher finds particularly exciting include:
Trends such as these bring great promise for new treatment options and subsequent improvements in patients’ health care overall.
As molecule complexity continues to increase and options for formulations continue to expand, the importance of early collaboration between API and drug product development teams becomes even more critical. These early conversations between groups require minimal resources from companies, especially in contrast to the immense costs of encountering formulation challenges at scale-up. Early investments to more deeply understand the critical attributes of the API can yield great savings throughout the development process.