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 90
- Downloads 0
2005 AAPS Biotechnology Conference Open Forum on Aggregation of Protein Therapeutics — Panel Discussion June 5–8, 2005 San Francisco, CA
Erratum to: In Vitro Considerations to Support Bioequivalence of Locally Acting Drugs in Dry Powder Inhalers for Lung Diseases
The online version of the original article can be found at 10.1208/s12248-009-9121-4.
Mechanistic Modeling of Monocarboxylate Transporter-Mediated Toxicokinetic/Toxicodynamic Interactions Between γ-Hydroxybutyrate and l -Lactate
Overdose of γ-hydroxybutyrate (GHB) can result in severe respiratory depression. Monocarboxylate transporter (MCT) inhibitors, including l -lactate, increase GHB clearance and represent a potential treatment for...
Autoradiography, MALDI-MS, and SIMS-MS Imaging in Pharmaceutical Discovery and Development
Whole-body autoradiography ((WBA) or quantitative WBA (QWBA)), microautoradiography (MARG), matrix-assisted laser desorption/ionization mass spectrometric imaging (MALDI-MSI), and secondary ion mass spectrometric imaging...
Percutaneous Permeation Enhancement by Terpenes: Mechanistic View
A popular approach for improving transdermal drug delivery involves the use of penetration enhancers (sorption promoters or accelerants) which penetrate into skin to reversibly reduce the barrier resistance. The potentia...