Please use this identifier to cite or link to this item: https://doi.org/10.1248/cpb.49.1395
Title: Effect of cetrimide and ascorbic acid on in vitro human skin permeation of haloperidol
Authors: Vaddi, H.K.
Wang, L.Z. 
Ho, P.C.-L. 
Chan, Y.W.
Chan, S.Y. 
Keywords: Ascorbic acid
Cetrimide
Fourier transform infrared spectroscopy
Haloperidol
Transdermal
Issue Date: 2001
Citation: Vaddi, H.K., Wang, L.Z., Ho, P.C.-L., Chan, Y.W., Chan, S.Y. (2001). Effect of cetrimide and ascorbic acid on in vitro human skin permeation of haloperidol. Chemical and Pharmaceutical Bulletin 49 (11) : 1395-1400. ScholarBank@NUS Repository. https://doi.org/10.1248/cpb.49.1395
Abstract: Permeation of haloperidol through the human skin in vitro was studied with two enhancers, cetrimide and ascorbic 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 36 h at 32 °C 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.
Source Title: Chemical and Pharmaceutical Bulletin
URI: http://scholarbank.nus.edu.sg/handle/10635/105868
ISSN: 00092363
DOI: 10.1248/cpb.49.1395
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