Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol

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Permeation of haloperidol through the human skin in vitro was studied with two enhancers, cetrimide and asscorbic acid, at various concentrations. Amber glass Franz-type diffusion cells were used for the permeation studies and haloperidol was made soluble in aqueous solution with the aid of lactic acid. Donor solutions were prepared by adding excess of haloperidol to 0.03% (v/v) lactic acid solution with or without enhancers at concentrations 0.1, 0.3 and 0.6% (w/v) and stirred for 36h at 32℃ before filtering. Ascorbic acid gradually increased the solubility of the haloperidol from that of the control where as cetrimide did not show any effect. Cetrimide concentration dependent increase in the permeability coefficient of haloperidol was observed. Mechanism of enhancement by cetrimide was probed with the diffusion profile kinetics and Fourier transform infrared (FT-IR) spectroscopy. Cetrimide was found to increase the thermodynamic activity of the drug in the skin. IR spectra of the stratum corneum treated with cetrimide showed time-dependent decrease in the intensity of the spectrum and dose-dependent decrease of lipid band but no change in the protein conformation. Cetrimide appears to interact with both the dermal keratin and lipids and this interaction was found to be irreversible. Ascorbic acid although increased the flux of haloperidol to the same extent at all concentrations from that of the control, decreased the permeability coefficient and enhancer index in a concentration dependent manner and this is due to the increased solubility of the drug in the vehicle. Both the enhancers did not change the lag time from that of the control.
公益社団法人日本薬学会の論文
2001-11-01

Effect of Cetrimide and Ascorbic Acid on in Vitro Human Skin Permeation of Haloperidol

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