Research provides a data-driven foundation for excipient selection in drug formulation development, particularly solid dosage forms.
Excipient choice drives moisture-related degradation of sensitive active pharmaceutical ingredients (APIs), according to new research by a joint team of academics and experts at UCB.
The ratio of APIs and microcrystalline cellulose (MCC), not the MCC grade, “makes or breaks stability”. This is chiefly through governing water uptake and availability, according to Steeger et al.
Using acetylsalicylic acid (ASA) and MCC as a model, their results showed that a higher MCC content increased water uptake and reduced ASA stability.
Additionally, the authors accurately predicted the formulation’s real-time stability from short-term accelerated data, a valuable finding given the rising demand for real-time data in pharma.
Steeger et al. highlighted that as stability is a “critical attribute” for the safety and quality of APIs in solid dosage forms, moisture-induced degradation remains a major challenge during drug formulation.
As such, the study addressed “the lack of a systematic and quantitative understanding of how excipient properties, particularly MCC grade, excipient ratio, and resulting water content jointly influence the stability of moisture-sensitive APIs in solid dosage forms”.
Writing on LinkedIn, co-author Ghamdan Beshr, New Solutions & Clinical Stability Lead at UCB said: “controlling water availability is a powerful lever for stabilising moisture-sensitive formulations, whether the risk is chemical degradation or physical change. Predictive stability also lets us pick the right formulation early, straight from screening, so stability becomes something we design for from the start rather than test for at the end.”
Overall, the results underline the importance of optimising excipients and the value of predictive stability modelling for drug formulation development, specifically the link between excipient-driven water content and API degradation.
The paper was published in Journal of Drug Delivery Science and Technology.
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