The Progress on the In Vivo-In Vitro Correlation (IVIVC) for Immediate Release Dosage Form as an Alternative to Bioavailability Studies

Michal      Ostrowski; Tomasz      Baczek

Abstract

Currently, in vivo-in vitro correlation (IVIVC) has become an effective tool to predict absorption behaviour of various pharmaceutical dosage forms. IVIVC in conjunction along with biopharmaceutical classification system (BCS) is considered to be a more effective alternative tool in view of the classical bioavailability studies. The most popular and recognized type of IVIVC are studies related to prolonged release oral dosage forms. The methodology for these tests is widely defined by FDA guidelines.

Examples of IVIVCs for other pharmaceutical dosage forms like immediate release oral or parenteral prolonged release preparations are still limited. Especially, in the case of immediate release oral forms it seems to be such because of the lack of criteria, defined methodology, technical difficulties as well as troubles to find immediate release formulations comprising different extent of absorption. First, the examples of IVIVC for variable immediate release oral dosage forms were discussed along with the appropriate biopharmaceutical class and pharmacokinetic profile of an individual active substance. Proposed approaches were also analyzed in view of the estimation of their reliability. Moreover, some technical aspects of the building of IVIVC were discussed with the emphasis on the tools, which were applied to establish a correlation (e.g., time scaling factor, kind of pharmacokinetic analysis, medium, type of apparatus, dissolution procedure). Finally, the perspectives of IVIVC application for immediate release dosage forms as an alternative strategy to the bioavailability studies were estimated and then a proposal for the reliability criteria of IVIVC in the case of immediate release oral dosage forms was done.

Keywords: Bioavailability, Biopharmaceutical classification system (BCS) studies, Immediate release (IR) dosage forms, In vivo-in vitro correlation (IVIVC), Review, In Vivo-In Vitro Correlation, biopharmaceutical classification system, Bioavailabilit, GI tract, AUC, correlation coefficient, Wagner-Nelson, Loo-Riegelmann method, BCS class 4, coefficient of variation, beta-lactam antibiotics, zero-order process, glyburide, gastrointestinal simulation, GastroPlus, L-thyroxine, BioDis apparatus, artificial digestive system, paracetamol, gemfibrozil, BCS class 2, Carbmazepine, amoxicillin, glibenclamide/metformin, Flutamide, sodium lauryl sulfate, ketoconazole, deramiciclane fumarate, AUC cumulative ratio, clarithromycin, macrolide