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Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs
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1  Department of Analytical Chemistry, Medical University of Lodz, Poland

Abstract:

The dermal permeability coefficient (log Kp) of 14 drugs (temazepam, alprazolam, bromazepam, elenium, oxazepam, lorazepam, lormetazepam, clotrazepate, ranitidine, methyldopa, piroxicam, amizepine, paracetamol, aspirin) was estimated in silico using DERMWIN v. 2.0 software. RP-18 thin layer chromatographic retention data were collected using methanol-water mobile phases containing between 50 and 90% (v/v) of methanol. The retention factor (Rf) values were converted to RM values following the equation: RM = log (1/Rf -1).

RM values were plotted against the concentration of methanol in the mobile phase (cMeOH) and extrapolated to zero concentration of methanol following the linear equation: RM = RM0 + S cMeOH.

RM0 and S chromatographic parameters were found to be connected with log Kp via reversed parabolic relationships explaining over 93% of total variability.

This research was supported by an internal grant of the Medical University of Łódź no. 503/3-016-03/503-31-001

Keywords: drugs, RP-18 TLC, transdermal absorption
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