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Effect of the unstirred water layer on permeability enhancement by hydrophilic cyclodextrins
Ist Teil von
International journal of pharmaceutics, 2007-09, Vol.342 (1), p.250-253
Ort / Verlag
Amsterdam: Elsevier B.V
Erscheinungsjahr
2007
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
Saturated solutions of three test compounds, carbamazepine, griseofulvin and hydrocortisone, were prepared in aqueous buffer (pH 7.4) containing 0, 1, 5 and 10% HPβCD. The permeability and flux of the drugs though a PAMPA membrane at different unstirred water layer (UWL) thicknesses was determined. In absence of HPβCD, permeability coefficients increased two- to three-fold with decreasing UWL thickness to a certain minimum values of about 40
μm. Addition of HPβCD to systems exhibiting larger UWL thicknesses significantly increased compound flux. The effect of HPβCD was linked to its association constant (
K
1:1) with the model drugs and decreased with decreasing UWL thickness to a certain minimum value. This suggests that hydrophilic cyclodextrins enhance flux when the UWL resistance significantly contributes to the overall barrier resistance.