Abstract：
:The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro potential of these formulations, permeation studies were performed with Franz diffusion cells using excised dorsal rat skin. To investigate their in vivo performance, a carrageenan-induced rat paw edema model was used. The commercial formulation of DS (C) was used as a reference formulation. The results of the in vitro permeation studies and the paw edema tests were analyzed by repeated-measures analysis of variance. The in vitro permeation studies found that M was superior to G and C and that adding DMSO to M increased the permeation rate. The permeability coefficients (Kp) of DS from M and M+DMSO were higher (Kp = 4.9 x 10(-3) +/- 3.6 x 10(-4) cm/h and 5.3 x 10(-3) +/- 1.2 x 10(-3) cm/h, respectively) than the Kp of DS from C (Kp = 2.7 x 10(-3) +/- 7.3 x 10(-4) cm/h) and G (Kp = 4.5 x 10(-3) +/- 4.5 x 10(-5) cm/h). In the paw edema test, M showed the best permeation and effectiveness, and M+DMSO had nearly the same effect as M. The in vitro and in vivo studies showed that M could be a new, alternative dosage form for effective therapy.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Sarigüllü Ozgüney I,Yeşim Karasulu H,Kantarci G,Sözer S,Güneri T,Ertan Gdoi
10.1208/pt070488subject
Has Abstractpub_date
2006-10-20 00:00:00pages
88issue
4issn
1530-9932journal_volume
7pub_type
杂志文章abstract：:Gliclazide (GLI), a poorly water-soluble antidiabetic, was transformed into a glassy state by melt quench technique in order to improve its physicochemical properties. Chemical stability of GLI during formation of glass was assessed by monitoring thin-layer chromatography, and an existence of amorphous form was confir...
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journal_title：AAPS PharmSciTech
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pub_type： 杂志文章,评审
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
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journal_title：AAPS PharmSciTech
pub_type： 杂志文章
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journal_title：AAPS PharmSciTech
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更新日期：2006-01-01 00:00:00
