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Developing in vitro-in vivo correlation of risperidone immediate release tablet.
Yardi Saibi1, Hitoshi Sato, Hidehisa Tachiki
1Department of Clinical and Molecular Pharmacokinetics/Pharmacodynamics, Faculty of Pharmaceutical Science, Showa University, 1-5-8 Hatanodai, Shinagawaku, Tokyo, 142-8555, Japan. yardilaili@yahoo.com
AAPS Pharmscitech
|June 15, 2012
Summary
This study successfully predicted risperidone absorption and developed a Level A in vitro-in vivo correlation (IVIVC) using gastrointestinal simulation. The model accurately correlated in vitro dissolution with in vivo performance for risperidone immediate release tablets.
Area of Science:
- Pharmaceutical Sciences
- Biopharmaceutics
- Pharmacokinetics
Background:
- Risperidone immediate release (IR) tablets require accurate absorption prediction.
- Developing in vitro-in vivo correlation (IVIVC) is crucial for generic drug development.
- Biopharmaceutics Classification System (BCS) aids in understanding drug absorption characteristics.
Purpose of the Study:
- To predict the gastrointestinal absorption profile of risperidone IR tablets.
- To develop a Level A IVIVC for risperidone using gastrointestinal simulation.
- To validate the developed IVIVC against Japanese bioequivalence guidelines.
Main Methods:
- Utilized GastroPlus™ software with an advanced compartmental absorption and transit model.
- Integrated plasma concentration, physicochemical, and pharmacokinetic data.
- Employed in vitro dissolution data in multiple media and plasma data to build the IVIVC model.
Main Results:
- Risperidone was identified as a BCS Class II drug, indicating low solubility and high permeability.
- The gastrointestinal absorption profile of risperidone was accurately predicted.
- A robust Level A IVIVC was successfully established with prediction errors below 10% for Cmax and AUC.
Conclusions:
- The advanced compartmental absorption and transit model effectively predicts risperidone absorption.
- The developed Level A IVIVC provides a reliable tool for risperidone IR tablet development and quality control.
- This simulation-based approach supports regulatory requirements for generic drug bioequivalence studies.
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