title: In-vitro and in-vivo evaluation of taste-masked cetirizine hydrochloride formulated in oral lyophilisates.
abstract: The use of solid oral dosage forms is typically favored with regard to stability and ease of administration. The aim of this study was to investigate whether cyclodextrins (CD) or ion exchange resins (IER) could be used to taste-mask cetirizine HCl when formulated in a freeze-dried oral formulation. The oral lyophilisates were produced using the Zydis(®) technology that offer the opportunity to produce the dosage form directly in the aluminum laminate blister packs. This study confirmed that a pre-formed resinate of cetirizine HCl and various cyclodextrins can be successfully incorporated into the Zydis(®) oral lyophilisate. A chemically stable product with acceptable release profile was obtained in the case of cyclodextrin. This study has also demonstrated that the Insent(®) taste sensing system is a useful technique for predicting the taste-masking potential of Zydis(®) formulations. The electronic taste sensing system (e-tongue) data can be used to provide guidance on the selection of taste-masked formulations. Principal component analysis (PCA) of sensor data by plotting the PCA scores revealed the effects of used taste-masking techniques on the e-tongue sensors, indicating the successful taste improvement. The PCA plot of the taste sensor data revealed larger distances between the non-taste-masked sample and the CD- and IER-loaded samples, and the shift toward the drug-free formulations and excipient signals indicates a modification of the product taste. The human taste trial confirms the acceptability of the selected promising formulations. The taste evaluation results showed that an effectively taste-masked formulation has been achieved using β-cyclodextrin and cherry/sucralose flavor system with over 80% of volunteers finding the tablet to be acceptable.
authors.affiliation: Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Artillerigatan 6A, 20520 Turku, Finland; Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University of Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany. Electronic address: maren.preis@abo.fi.
authors.forename: Maren
authors.initials: M
authors.lastname: Preis
authors.affiliation: Catalent Pharma Solutions U.K. Swindon Zydis(®) Limited, Swindon SN5 8RU, United Kingdom.
authors.forename: Leon
authors.initials: L
authors.lastname: Grother
authors.affiliation: Catalent Pharma Solutions U.K. Swindon Zydis(®) Limited, Swindon SN5 8RU, United Kingdom.
authors.forename: Philip
authors.initials: P
authors.lastname: Axe
authors.affiliation: Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University of Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany.
authors.forename: Jörg
authors.initials: J
authors.lastname: Breitkreutz
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D017332:Cetirizine / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003505:Cyclodextrins / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D005260:Female; D005612:Freeze Drying / Q000379:methods; D006801:Humans; D007475:Ion Exchange Resins / Q000737:chemistry; D008297:Male; D008875:Middle Aged; D000068220:Prunus avium / Q000737:chemistry; D016037:Single-Blind Method; D012995:Solubility; D013395:Sucrose / Q000031:analogs & derivatives / Q000737:chemistry; D013607:Tablets / Q000737:chemistry; D013649:Taste / Q000502:physiology; D014059:Tongue / Q000502:physiology; D055815:Young Adult; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D003505:Cyclodextrins; D005079:Excipients; D007475:Ion Exchange Resins; D013607:Tablets; D047392:beta-Cyclodextrins; D013395:Sucrose; C026285:trichlorosucrose; C031215:betadex; D017332:Cetirizine
keywords: Electronic tongue; Oral lyophilisate; Orally disintegrating tablet; Orodispersible tablet; Taste trial; Taste-masking