title: Biowaiver monograph for immediate-release solid oral dosage forms: bisoprolol fumarate.
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 bisoprolol as the sole active pharmaceutical ingredient (API) are reviewed. Bisoprolol is classified as a Class I API according to the current Biopharmaceutics Classification System (BCS). In addition to the BCS class, its therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions, and reported BE/bioavailability problems are taken into consideration. Qualitative compositions of IR tablet dosage forms of bisoprolol with a marketing authorization (MA) in ICH (International Conference on Harmonisation) countries are tabulated. It was inferred that these tablets had been demonstrated to be bioequivalent to the innovator product. No reports of failure to meet BE standards have been made in the open literature. On the basis of all these pieces of evidence, a biowaiver can currently be recommended for bisoprolol fumarate IR dosage forms if (1) the test product contains only excipients that are well known, and used in normal amounts, for example, those tabulated for products with MA in ICH countries and (2) both the test and comparator dosage form are very rapidly dissolving, or, rapidly dissolving with similarity of the dissolution profiles demonstrated at pH 1.2, 4.5, and 6.8.
authors.affiliation: Xepa-Soul Pattinson (M) Sdn Bhd, Melaka, Malaysia.
authors.forename: Naseem A
authors.initials: NA
authors.lastname: Charoo
authors.forename: Areeg A A
authors.initials: AA
authors.lastname: Shamsher
authors.forename: Lai Y
authors.initials: LY
authors.lastname: Lian
authors.forename: Bertil
authors.initials: B
authors.lastname: Abrahamsson
authors.forename: Rodrigo
authors.initials: R
authors.lastname: Cristofoletti
authors.forename: D W
authors.initials: DW
authors.lastname: Groot
authors.forename: Sabine
authors.initials: S
authors.lastname: Kopp
authors.forename: Peter
authors.initials: P
authors.lastname: Langguth
authors.forename: James
authors.initials: J
authors.lastname: Polli
authors.forename: Vinod P
authors.initials: VP
authors.lastname: Shah
authors.forename: Jennifer
authors.initials: J
authors.lastname: Dressman
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000737:chemistry* / Q000627:therapeutic use; D001682:Biological Availability; D001702:Biopharmaceutics; D001711:Biotransformation; D017298:Bisoprolol / Q000008:administration & dosage* / Q000737:chemistry* / Q000627:therapeutic use; D002463:Cell Membrane Permeability; D002851:Chromatography, High Pressure Liquid; D005079:Excipients; D006333:Heart Failure / Q000188:drug therapy; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D012995:Solubility; D013237:Stereoisomerism; D013810:Therapeutic Equivalency; D014018:Tissue Distribution
chemical_list: D000319:Adrenergic beta-Antagonists; D005079:Excipients; D017298:Bisoprolol
keywords: absorption; bioequivalence; biopharmaceutics classification system (BCS); bisoprolol; dissolution; permeability; solubility