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Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs

Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs - PowerPoint Presentation

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Uploaded On 2022-08-04

Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs - PPT Presentation

Anna W Sobańska Elżbieta Brzezińska Department of Analytical ID: 935763

retention methanol drugs rm0 methanol retention rm0 drugs log permeability skin layer thin parameters chromatographic values research cmeoh

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Application of RP-18 TLC retention data to prediction of transdermal absorption of drugs

Anna W. Sobańska*, Elżbieta Brzezińska

Department of Analytical ChemistryMedical University of Lodz, PolandMuszyńskiego 1, 90-151 Łódź, Polandanna.sobanska@umed.lodz.pl

ObjectiveThe objective of this research was to evaluate the retention parameters (RM0, S) obtained via RP-18 Thin Layer Chromatography as predictors of the skin permeability of selected drugs (mainly benzodiazepines). Material and methodThe 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 [1] (Table 1). 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) [2].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. The relationships between the chromatographic parameters RM0 (intercept) or S (slope) obtained in this manner and the computed dermal permeability coefficient (log Kp) are presented in Figures 1 and 2. ResultsRM0 and S chromatographic parameters were found to be connected with log Kp via reversed parabolic relationships explaining over 93% of total variability. The maximum skin permeation was observed for RM0 ≈ 2 and S ≈ -3, respectively. Conclusion RP-18 Thin Layer Chromatography was found to be a suitable tool to estimate the skin permeability of studied drugs.References1.EPI SuiteTM, www.epa.gov2. Bate-Smith E.C., Westall R.G. Biochim. Biophys. Acta 1950, 4, 427-440AcknowlegementsThis research was supported by an internal grant of the Medical University of Łódź no. 503/3-016-03/503-31-001

Table

1SRM0log KpTemazepam-3.7983.050-3.037Alprazolam-3.8773.254-3.129Bromazepam-3.2692.496-3.217Elenium-2.5512.131-2.866Oxazepam-3.7522.864-2.924Lorazepam-4.0373.031-3.019Lormetazepam-4.2073.303-3.201Clorazepate-3.8403.117-3.206Ranitidine-0.518-0.073-4.390Methyldopa-0.197-0.805-5.180Piroxicam-3.1932.598-2.631Amizepine-3.2212.484-2.503Paracetamol-1.5000.459-3.348Aspirin-2.2041.301-3.025