Effect of Formulation on Adinazolam Pharmacokinetics and Pharmacodynamics

Conference: CRS
Division: PBPK


Adinazolam has been reported to have anxiolytic and antidepressant properties [1]. Numerous pharmacokinetic (PK) and pharmacodynamic (PD) studies of immediate release as well as sustained release formulations have been reported in the literature [2-9]. Some of the studies report PK parameters fitted to intravenous or oral doses. One provides an in vivo-in vitro correlation relating the % of drug dissolved in vitro to the % of drug absorbed in vivo [10]. Some PD relationships between the plasma concentration (Cp) and PD effect have been reported as well [9]. However, these models are mostly descriptive in nature and can only be used with difficulties to predict the PK or PD profiles after oral administration of new controlled release formulations. The current study was performed in order to create a comprehensive model for the simulation of the Adinazolam Cp-time profile as well as its therapeutic PD profile as a function of drug release from the formulation, taking into account the physiological parameters of the in vivo system. Such a model can be useful in predicting the PD effect of various Adinazolam formulations or to help in design of formulations with desired strengths and durations of PD effect.

Controlled Release Society (CRS) Annual Meeting and Exposition, July 7-11, 2007, Long Beach, California

By Viera Lukacova, Grazyna Fraczkiewicz, Anand Prabhakaran, Michael B.Bolger, Walter S. Woltosz