(158b) Modeling of Disintegration and Dissolution of Formulated API

Authors: 
Zaborenko, N. - Presenter, Eli Lilly and Company
Sperry, D. C., Eli Lilly & Co.

The absorption rate and extent of absorption of an active pharmaceutical ingredient (API) in patients often depends strongly on the mechanisms of the API release from the formulation into absorbable form.  These mechanisms include coating dissolution, tablet mechanical disintegration into granules or aggregates, granule disintegration into component powder particles, and API dissolution from available surfaces.  These phenomena can occur simultaneously and can affect each other.  Additionally, each of these phenomena is affected by a number of chemical and physical parameters stemming from the molecular properties of the API and excipients, the nature of the dissolution medium, and the processing parameters for tablet formation such as compaction force and blending shear.  In this work, a mathematical model is derived to relate API tablet dissolution profile to API and medium properties, tablet preparation parameters, and measurable tablet properties.  Case studies are presented illustrating the application and utility of  this model for formulations.