Integration of active pharmaceutical ingredient solid form selection and particle engineering into drug product design

Abstract

This review seeks to offer a broad perspective that encompasses an understanding of the drug product attributes affected by active pharmaceutical ingredient (API) physical properties, their link to solid form selection and the role of particle engineering. While the crucial role of active pharmaceutical ingredient (API) solid form selection is universally acknowledged in the pharmaceutical industry, the value of increasing effort to understanding the link between solid form, API physical properties and drug product formulation and manufacture is now also being recognised.A truly holistic strategy for drug product development should focus on connecting solid form selection, particle engineering and formulation design to both exploit opportunities to access simpler manufacturing operations and prevent failures. Modelling and predictive tools that assist in establishing these links early in product development are discussed. In addition, the potential for differences between the ingoing API physical properties and those in the final product caused by drug product processing is considered. The focus of this review is on oral solid dosage forms and dry powder inhaler products for lung delivery.

Effect of crystallization kinetics on the properties of spray dried microparticles

“…The dependence of the performance of pulmonary drugs on their solid phase highlights the need to understand particle formation and crystallization process. The main goal of particle engineering is to understand particle formation process in order to control the properties of the produced microparticles (Ticehurst and Marziano 2015). The particle formation process is the transition between solution droplets to dried particles (Vicente et al 2013).…”

Crystallization of Cephradine Polymorphs and Hydrates from Mixed Solvents of Methanol and Water

“…The solvent composition may also play a role in determining the crystal shape and size. The growth rates of the different faces of the particle may change due to interactions between the solvent and the surface , . Furthermore, the extent of agglomeration may also be affected by the physical and chemical characteristics of both solvent and solute .…”

“…Formation of agglomerates often occurs as a result of cohesive properties of the API. The agglomerated particles may cause a larger apparent particle size and inconsistent PSD influencing, e.g., dissolution . The effect of the operating conditions on agglomeration has been studied in both model‐free and model‐based work .…”

Predicting compressive strength of consolidated molecular solids using computer vision and deep learning

“…roughness), and density. In turn, these crystal characteristics influence the overall microstructures of the consolidated parts [21], [22]. Figure 1 shows typical SEM images of TATB crystals.…”