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Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.
Hofsäss, Martin A Souza, Jacqueline de Silva-Barcellos, Neila M Bellavinha, Karime R Abrahamsson, Bertil Cristofoletti, Rodrigo Groot, D W Parr, Alan Langguth, Peter Polli, James E
Hofsäss, Martin A
Souza, Jacqueline de
Silva-Barcellos, Neila M
Bellavinha, Karime R
Abrahamsson, Bertil
Cristofoletti, Rodrigo
Groot, D W
Parr, Alan
Langguth, Peter
Polli, James E
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Series / Report no.
Open Access
Type
Article
Language
en
Date of publication
2017-12
Year of publication
Research Projects
Organizational Units
Journal Issue
Title
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.
Translated Title
Published in
J Pharm Sci 2017, 106(12):3421-430
Abstract
This work presents a review of literature and experimental data relevant to the possibility of waiving pharmacokinetic bioequivalence studies in human volunteers for approval of immediate-release solid oral pharmaceutical forms containing folic acid as the single active pharmaceutical ingredient. For dosage forms containing 5 mg folic acid, the highest dose strength on the World Health Organization Essential Medicines List, the dose/solubility ratio calculated from solubility studies was higher than 250 mL, corresponding to a classification as "not highly soluble." Small, physiological doses of folic acid (≤320 μg) seem to be absorbed completely via active transport, but permeability data for higher doses of 1-5 mg are inconclusive. Following a conservative approach, folic acid is classified as a Biopharmaceutics Classification System class IV compound until more reliable data become available. Commensurate with its solubility characteristics, the results of dissolution studies indicated that none of the folic acid products evaluated showed rapid dissolution in media at pH 1.2 or 4.5. Therefore, according to the current criteria of the Biopharmaceutics Classification System, the biowaiver approval procedure cannot be recommended for immediate-release solid oral dosage forms containing folic acid.