Evaluation of pantoprazole formulations in different dissolution apparatus using biorelevant medium

Abstract

Purpose:

The study was developed to compare the in vitro dissolution profile of pantoprazole (CAS 102625-70-7) formulations in both The United State Pharmacopeia (USP) apparatus 2 and by applying biorelevant medium. Moreover, an in vitro – in vivo relationship was proposed considering in vivo data from previously published study

Methods:

In vitro dissolution profile were evaluated in biorelevant medium in USP apparatus 2 and 3 and the dissolution curves were either compared by the similarity factor (f₂) or a model-independent approach. The fraction of drug dissolved in vitro in apparatus 2 was compared with the fraction of drug absorbed in vivo, which was obtained from a retro-spective in vivo study. An in vitro – in vivo relationship analysis was then applied to elucidate the overall absorption characteristics of formulations

Results:

The dissolution profiles of formulations demonstrated similar disposition in biorelevant medium in both USP apparatus 2 and 3. The dissolution profiles were described by f₂ model in apparatus 2 and Weibull's function in apparatus 3. The vitro–in vivo relationship analysis showed that the formulation exhibited permeability rate-limiting absorption.

Conclusion:

Biorelevant medium in both USP apparatus 2 and 3 may be used as a tool to predict in vivo disposition of formulations of pantoprazole. Furthermore, it can be argued that biowaiver can be granted for enteric coated formulations of pantoprazole on the basis of in vitro dissolution profile.

Key word

Biopharmaceutics classification system - Biorelevant dissolution testing - CAS 102625-70-7 - In vitro–in vivo correlation - Pantoprazole

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