Abstract

The present study was aimed to predict the absorption profile of a risperidone immediate release tablet (IR) and to develop the level A in vitro-in vivo correlation (IVIVC) of the drug using the gastrointestinal simulation based on the advanced compartmental absorption and transit model implemented in GastroPlus™. Plasma concentration data, physicochemical, and pharmacokinetic properties of the drug were used in building its absorption profile in the gastrointestinal tract. Since the fraction absorbed of risperidone in simulation was more than 90% with low water solubility, the drug met the criteria of class II of the Biopharmaceutics Classification System. The IVIVC was developed based on the model built using the plasma data and the in vitro dissolution data in several dissolution media based on the Japanese Guideline for Bioequivalence Studies of Generic Products. The gastrointestinal absorption profile of risperidone was successfully predicted. A level A IVIVC was also successfully developed in all dissolution media with percent prediction error for Cmax and the area under the curve less than 10% for both reference and test drug.

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Authors

Saibi Y, Sato H, Tachiki H

Institution

Department of Clinical and Molecular Pharmacokinetics/Pharmacodynamics, Faculty of Pharmaceutical Science, Showa University, 1-5-8 Hatanodai, Shinagawaku, Tokyo, 142-8555, Japan. yardilaili@yahoo.com

Source

AAPS PharmSciTech 13:3 2012 Sep pg 890-5

MeSH

Chemistry, Pharmaceutical
Drug Discovery
Humans
Risperidone
Tablets

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22696224