Developing in vitro-in vivo correlation of risperidone immediate release tablet.
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.
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
Yardi
Y
Saibi
Hitoshi
H
Sato
Hidehisa
H
Tachiki
D002626:Chemistry, Pharmaceutical / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D018967:Risperidone / Q000138:chemical synthesis* / Q000378:metabolism*; D013607:Tablets
D013607:Tablets; D018967:Risperidone