Pharmacoscintigraphic evaluation of riboflavin-containing microballoons for a floating controlled drug delivery system in healthy humans

Journal of Controlled Release : Official Journal of the Controlled Release Society
Yasunori SatoYasuhisa Fujibayashi

Abstract

Hollow microspheres (microballoons) floating on artificial gastric juice were developed as a floating controlled drug delivery system in the stomach. The intragastric behavior of 99mTc labelled microballoons (MB) and nonfloating microspheres (NF) (control) following oral administration in fasted and fed humans was investigated by gamma scintigraphy. Simultaneously, pharmacokinetic examination of riboflavin released from MB and NF was conducted in fasted and fed human subjects. In the fed state, MB were dispersed in the upper portion of the stomach; moreover, MB were retained in the stomach up to 300 min compared with NF, which descended gradually into the lower part of stomach within 90 min. In the fasted state, MB floated for approximately 60 min, after which it was removed rapidly via the cyclic activity referred to as the interdigestive migrating motor complex (IMMC). NF were removed more rapidly, i.e., within 60 min. Pharmacokinetic parameters, e.g., excretion half-life time (t1/2) and total urinary excretion, were well correlated with the gastric residence time (GRT) determined by the gamma scintigraphy analysis. The present investigation suggests that MB are very useful for improving drug bioavailability, resulting in a m...Continue Reading

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Citations

Mar 2, 2006·Expert Opinion on Drug Delivery·Alexander StreubelRoland Bodmeier
Feb 2, 2016·Expert Opinion on Drug Delivery·Janki V Andhariya, Diane J Burgess
Aug 30, 2008·Expert Opinion on Drug Delivery·Dhaivat C Parikh, Avani F Amin
Apr 18, 2015·Expert Opinion on Drug Delivery·Božena BürmenMarija Bogataj
Sep 7, 2007·Journal of Pharmaceutical Sciences·Hao ZouShen Gao
Mar 2, 2016·Journal of Research in Medical Sciences : the Official Journal of Isfahan University of Medical Sciences·Maha A KhalilMohamed Z Hussein
Jun 10, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Orazio Luca StrusiPaolo Colombo
Mar 17, 2012·The Journal of Pharmacy and Pharmacology·Sumalee Thitinan, Jason T McConville
Sep 9, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Mamoru FukudaJames W McGinity
Jan 13, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·P L BardonnetF Falson
Jul 11, 2012·Biomacromolecules·Remya P NarayananArtem Melman
Feb 28, 2013·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Wei Li LeeSay Chye Joachim Loo
Oct 21, 2014·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Jingxian HuangJianhua Zhou

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