RDD 2020: Development of an X-ray Diffraction Method for the Quantification of API Recrystallized API

Typically, in the development of dry powder inhaler (DPI) formulations the use of a stable crystalline form of the active pharmaceutical ingredient (API) is desired. However, often in order to produce crystalline particles of suitable size for inhalation, micronization processes will be required, resulting in surface amorphous material which may affect the efficacy of the product.

If required, additional conditioning/processing steps may then be applied to the API (or to ensure drug product stability under use) without requiring any additional solid state characterization of the API in the drug product. 

Increasingly, formulations are now being developed with non-crystalline engineered API particles. These amorphous APIs are thermodynamically unstable and may be prone to recrystallization over time or upon exposure to humidity, with such recrystallization having potentially dramatic effects on the efficacy and performance of the product.