Definition of the right excipients in a formulation for active pharmaceutical ingredients (APIs) stability


Physical and chemical instability of APIs is the reason of many market recalls of products, due to unacceptable levels of their decomposition, which alter content uniformity of the final formulation. Excipients’ properties, such as hygroscopicity and microenvironmental acidity, can have a significant impact on API stability in a drug product. Incompatibility or interaction between API and excipients, during manufacture or shelf storage, need detailed investigation.
Elettra’s contribution:
Synchrotron X-ray diffractioncan be used to assess the physical stability of an API in powder blends, tablets (even in blister), gel capsules, and creams providing information on the presence of API different physical forms. API quantification can be accomplished based on the intensities of one or more of its characteristic peaks. By quantifying the API in the dosage form, it is possible to readily assess the influence of formulation composition on API stability.   

Facility: XRD1 Beamline.

Bibliography: Most of these studies have been performed with companies under non-disclosure agreements. However, an example of a similar study can be found here: N. Kaur et al., “Investigating the Influence of Excipients on the Stability of Levothyroxine Sodium Pentahydrate”, Mol. Pharmaceutics, 2021, 18, 2683. 


Last Updated on Monday, 20 June 2022 16:34