title: Biowaiver monographs for immediate release solid oral dosage forms: acetazolamide.
abstract: Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing acetazolamide are reviewed. Acetazolamide's solubility and permeability characteristics according to the Biopharmaceutics Classification System (BCS), as well as its therapeutic use and therapeutic index, its pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability (BA) problems are taken into consideration. The available data on solubility, on oral absorption and permeability are not sufficiently conclusive to classify acetazolamide with certainty. Taking a conservative approach, no biowaiver is considered justified for the registration of new multisource drug products. However, SUPAC level 1 and level 2 postapproval changes and most EU Type I variations can be approved waiving in vivo BE studies.
authors.affiliation: Pharmacy Department, Chemical Sciences Faculty, National University of Córdoba, Córdoba, Argentina.
authors.forename: G E
authors.initials: GE
authors.lastname: Granero
authors.forename: M R
authors.initials: MR
authors.lastname: Longhi
authors.forename: C
authors.initials: C
authors.lastname: Becker
authors.forename: H E
authors.initials: HE
authors.lastname: Junginger
authors.forename: S
authors.initials: S
authors.lastname: Kopp
authors.forename: K K
authors.initials: KK
authors.lastname: Midha
authors.forename: V P
authors.initials: VP
authors.lastname: Shah
authors.forename: S
authors.initials: S
authors.lastname: Stavchansky
authors.forename: J B
authors.initials: JB
authors.lastname: Dressman
authors.forename: D M
authors.initials: DM
authors.lastname: Barends
mesh_terms: D000086:Acetazolamide / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000284:Administration, Oral; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004304:Dosage Forms; D005079:Excipients; D006801:Humans; D012995:Solubility; D013810:Therapeutic Equivalency
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D004304:Dosage Forms; D005079:Excipients; D000086:Acetazolamide