Preparation and pharmaceutical evaluation of new tacrolimus-loaded solid self-emulsifying drug delivery system

Title
Preparation and pharmaceutical evaluation of new tacrolimus-loaded solid self-emulsifying drug delivery system
Author(s)
김종오서윤기김동욱[김동욱]조관형[조관형]Yousaf[Yousaf]김동식[김동식]김정훈[김정훈]용철순최한곤[최한곤]
Keywords
ENHANCED ORAL BIOAVAILABILITY; DISPERSION; PHARMACOKINETICS
Issue Date
201502
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.38, no.2, pp.223 - 228
Abstract
The purpose of this study was to develop a novel tacrolimus-loaded solid self-emulsifying drug delivery system (SEDDS) using Labrafac as an oil phase. The ternary phase diagram was plotted with Labrafac, Labrasol and Lauroglycol used as an oil, surfactant and co-surfactant, respectively. The liquid SEDDS formulated with Labrasol, Lauroglycol and Labrafac (70:15:15, volume ratio) furnished the smallest emulsion globule size. The solid SEDDS was obtained by spray-drying the liquid mixture containing the liquid SEDDS with 5 % tacrolimus and silicon dioxide. Furthermore, dissolution of tacrolimus from the solid SEDDS and pharmacokinetics in rats was studied compared to the commercial product. The solid SEDDS produced relatively larger emulsion globule size than that exhibited by the corresponding liquid SEDDS. However, this size variation was not significantly different. The solid SEDDS with approximately 280 nm emulsion droplet size improved the dissolution of the drug compared to drug power and the commercial product. It resulted in significantly higher plasma concentration, AUC and C-max, and shorter T-max values than did the commercial product (p < 0.05). The enormously enhanced oral bioavailability of tacrolimus in rats was attributed to relatively faster absorption due to accelerated dissolution of the drug from the solid SEDDS. Therefore, this novel solid SEDDS prepared with Labrafac as an oil phase is an excellent way to achieve better bioavailability of tacrolimus given via the oral route.
URI
http://hdl.handle.net/YU.REPOSITORY/33498http://dx.doi.org/10.1007/s12272-014-0459-5
ISSN
0253-6269
Appears in Collections:
약학대학 > 약학부 > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE