Acta Pharmaceutica, Vol. 66 No. 4, 2016.
Short communication, Note
https://doi.org/10.1515/acph-2016-0047
Preparation and in vivo evaluation of gel-based nasal delivery system for risperidone
FUGEN GU
; Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, China
WEINA MA
; School of Pharmacy, Inner Mongolia Medical University, Hohhot 010110, China
GENDALAI MENG
; Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, China
CHUNZHI WU
; Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, China
YI WANG
; Department of Pharmaceutics, Affiliated Hospital, Inner Mongolia Medical University, Hohhot 010050, China
Abstract
The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax ) and the time to reach cmax (tmax) were 15.2 µg mL–1 and 5min for the nasal gel, 3.6 µg mL–1and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax, cmax and AUC between oral and nasal routes were significantly different (p ＜ 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0%. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.
Keywords
risperidone; nasal gel; formulation; pharmacokinetics; bioavailability; ciliotoxicity
Hrčak ID:
165024
URI
Publication date:
31.12.2016.
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