An Investigation into the Importance of “Very Rapid Dissolution” Criteria for Drug Bioequivalence Demonstration using Gastrointestinal Simulation Technology
Journal Title: The AAPS Journal - Year 2009, Vol 11, Issue 2
Abstract
The Biopharmaceutics Classification System (BCS) is based on the mechanistic assumptions that the rate and extent of oral drug absorption are governed by drug solubility, intestinal permeability, and dissolution rate from the dosage form administered. One of the goals of BCS is to identify classes of drugs for which bioequivalence may be established based solely on the in vitro dissolution data, i.e., which would be eligible for biowaiver. On the basis of BCS, currently, the biowaiver concept is adopted and recommended for immediate release of drug products containing highly soluble and highly permeable compounds (BCS class 1 drugs). Dissolution testing properties are proposed to be more stringent: very rapid dissolution is demanded when generic drug application is submitted with the exemption of in vivo bioequivalence study. In the present paper, Gastrointestinal Simulation Technology has been applied in order to evaluate the potential for different in vitro drug dissolution kinetics to influence dosage forms in vivo behavior and the relevance of “very rapid dissolution” criteria to be met (i.e., more than 85% of dose dissolved in 15 min).
Authors and Affiliations
Ivan Kovačevi, Jelena Parojči, Marija Tubi-Grozdanis, Peter Langguth
Keywords
Related Articles
- EP ID EP681470
- DOI 10.1208/s12248-009-9114-3
- Views 93
- Downloads 0
Method to Screen Substrates of Apical Sodium-Dependent Bile Acid Transporter
Human apical sodium-dependent bile acid transporter (hASBT) is a potential prodrug target under study. Development of prodrugs that target hASBT may yield compounds with low solubility and/or susceptibility to hydrolysis...
Bioequivalence studies for levothyroxine
The Food and Drug Administration (FDA) Guidance for Bioavailability and Bioequivalence Studies for Levothyroxine has been challenged by companies that manufacture brand-name products. Their contention is that the current...
Aggregation Kinetics for IgG1-Based Monoclonal Antibody Therapeutics
Monoclonal antibodies (mAbs) as a class of therapeutic molecules are finding an increasing demand in the biotechnology industry for the treatment of diseases like cancer and multiple sclerosis. A key challenge associated...
An Extended Minimal Physiologically Based Pharmacokinetic Model: Evaluation of Type II Diabetes Mellitus and Diabetic Nephropathy on Human IgG Pharmacokinetics in Rats
Although many studies have evaluated the effects of type 2 diabetes mellitus (T2DM) on the pharmacokinetics (PK) of low molecular weight molecules, there is limited information regarding effects on monoclonal antibodies....
Preparation and ocular pharmacokinetics of ganciclovir liposomes
Ophthalmic liposomes of ganciclovir (GCV) were prepared by the reverse phase evaporation method, and their ocular pharmacokinetics in albino rabbits were compared with those obtained after dosing with GCV solution. The i...