K. Yu et al., Optimization of sustained-release diltiazem formulations in man by use of an in-vitro/in-vivo correlation, J PHARM PHA, 50(8), 1998, pp. 845-850
In-vitro/in-vivo correlations (IVIVC) are useful for predicting in-vivo res
ults from in-vitro data. An IVIVC has been used to optimize a hydrocolloida
l-based matrix tablet designed to be bioequivalent to an existing once-dail
y diltiazem HCl product (Dilacor XR 240 mg; Rhone-Poulenc Rorer).
Data from a preliminary formulation dosed to fasted and fed subjects were u
sed to establish the IVIVC. The correlation was then used during reformulat
ion of the dosage forms to predict changes in the maximum plasma concentrat
ion (C-max) and the area under the plasma-concentration-time curve (AUC) fo
r fasted and fed subjects using in-vitro dissolution data.
The IVIVC adequately predicted plasma profiles of two optimized formulation
s in studies with fasted and fed subjects.