Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2008 Mar;25(3):483-8.
doi: 10.1007/s11095-007-9523-x. Epub 2008 Jan 31.

The use of BDDCS in classifying the permeability of marketed drugs

Leslie Z Benet  1 , Gordon L Amidon, Dirk M Barends, Hans Lennernäs, James E Polli, Vinod P Shah, Salomon A Stavchansky, Lawrence X Yu
Affiliations

The use of BDDCS in classifying the permeability of marketed drugs

Leslie Z Benet et al. Pharm Res. 2008 Mar.

Abstract

We recommend that regulatory agencies add the extent of drug metabolism (i.e., >or=90% metabolized) as an alternate method in defining Class 1 marketed drugs suitable for a waiver of in vivo studies of bioequivalence. That is, >or=90% metabolized is an additional methodology that may be substituted for >or=90% absorbed. We propose that the following criteria be used to define>or=90% metabolized for marketed drugs: Following a single oral dose to humans, administered at the highest dose strength, mass balance of the Phase 1 oxidative and Phase 2 conjugative drug metabolites in the urine and feces, measured either as unlabeled, radioactive labeled or nonradioactive labeled substances, account for >or=90% of the drug dosed. This is the strictest definition for a waiver based on metabolism. For an orally administered drug to be >or=90% metabolized by Phase 1 oxidative and Phase 2 conjugative processes, it is obvious that the drug must be absorbed. This proposal, which strictly conforms to the present>or=90% criteria, is a suggested modification to facilitate a number of marketed drugs being appropriately assigned to Class 1.

PubMed Disclaimer

References

    1. Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutics drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 1995;12:413–420. - PubMed
    1. Food and Drug Administration. Classification System. Food and Drug Administration; Rockville, MD: 2000. Guidance for Industry: Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics. Retrieved from www.fda.gov/cder/guidance/index.htm.
    1. Polli JE, Yu LX, Cook JA, Amidon GL, Borchardt RT, Burnside BA, Burton PS, Chen M-L, Conner DP, Faustino J, Hawi AA, Hussain AS, Joshi HN, Kwei G, Lee VHL, Lesko LJ, Lipper RA, Loper AE, Nerurkar SG, Polli JW, Sanvordeker DR, Taneja R, Uppoor RS, Vattikonda CS, Wilding I, Zhang G. Summary Workshop Report: Biopharmaceutics Classification System – Implementation Challenges and Extension Opportunities. J Pharm Sci. 2004;93:1375–1381. - PubMed
    1. Lennernäs H, Ahrenstedt Ö, Hällgren R, Knutson L, Ryde M, Paalzow L. Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man. Pharm Res. 1992;9:1243–1251. - PubMed
    1. Lennernäs H, Knutson L, Knutson T, Lesko L, Salomonson T, Amidon GL. Human effective permeability data for atenolol, metoprolol and carbamazepine to be used in the proposed biopharmaceutical classification for IR-products. Pharm Res. 1995;12:S295.

Publication types

Substances