title: In vivo evaluation of matrix pellets containing nanocrystalline ketoprofen.
abstract: The aim of this study was to evaluate the in-vivo behaviour of matrix pellets formulated with nanocrystalline ketoprofen after oral administration to dogs. No significant differences in AUC-values were seen between pellet formulations containing nanocrystalline or microcrystalline ketoprofen and a commercial ketoprofen formulation (reference: Rofenid 200 Long Acting). C(max) of the formulations containing nano- or microcrystalline ketoprofen was significantly higher compared to reference, whereas t(max) was significantly lower. The in-vivo burst release observed for the spray dried nanocrystalline ketoprofen matrix pellets was reduced following compression of the pellets in combination with placebo wax/starch pellets. These matrix tablets sustained the ketoprofen plasma concentrations during 5.6 and 5.4 h for formulations containing nano- and microcrystalline ketoprofen, respectively.
authors.affiliation: Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, 9000, Ghent, Belgium.
authors.forename: G J
authors.initials: GJ
authors.lastname: Vergote
authors.forename: C
authors.initials: C
authors.lastname: Vervaet
authors.forename: I
authors.initials: I
authors.lastname: Van Driessche
authors.forename: S
authors.initials: S
authors.lastname: Hoste
authors.forename: S
authors.initials: S
authors.lastname: De Smedt
authors.forename: J
authors.initials: J
authors.lastname: Demeester
authors.forename: R A
authors.initials: RA
authors.lastname: Jain
authors.forename: S
authors.initials: S
authors.lastname: Ruddy
authors.forename: J P
authors.initials: JP
authors.lastname: Remon
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D005260:Female; D007660:Ketoprofen / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D036103:Nanotechnology; D010316:Particle Size; D012995:Solubility; D013608:Tablets, Enteric-Coated; D013997:Time Factors
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D013608:Tablets, Enteric-Coated; D007660:Ketoprofen