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1.
China Journal of Chinese Materia Medica ; (24): 1130-1132, 2008.
Article in Chinese | WPRIM | ID: wpr-295397

ABSTRACT

<p><b>OBJECTIVE</b>To investigate penetration characteristics of artemether and the effect of different permeation enhancer on transdermal permeation of artemether through rat skin.</p><p><b>METHOD</b>The permeation experiments were performed using rat skin on modified Franz diffusion cells in vitro. The concentrations of artemether in receptor compartment at specified time points were determined by HPLC.</p><p><b>RESULT</b>The permeating ratio through human skin of artemether solution was Js (2.78 +/- 0.78) microg x cm(-2) x h(-1), the quantity of drug penetrated through and accumulated in the skin by the end of the experiment were (69.07 +/- 3.01) microg x cm(-2), (58.93 +/- 3.56) microg x cm(-2) respectively. Four different permeation enhancers can improve the transdermal permeation of artemether.</p><p><b>CONCLUSION</b>Artemether have the potential to be developed to new transdermal preparation.</p>


Subject(s)
Animals , Male , Rats , Adjuvants, Pharmaceutic , Chemistry , Artemisinins , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , In Vitro Techniques , Permeability , Rats, Wistar , Skin , Metabolism
2.
China Journal of Chinese Materia Medica ; (24): 46-50, 2008.
Article in Chinese | WPRIM | ID: wpr-324301

ABSTRACT

<p><b>OBJECTIVE</b>To compare the pharmacokinetics and tissue distribution of alpha-asarone in lipid emulsion and aqueous solution for injection and study the feasibility of lipid emulsion of alpha-asarone as the parenteral drug delivery system.</p><p><b>METHOD</b>HPLC was used to determine the drug concentration in rat plasma and mice tissues after intravenous (i.v.) administration of lipid emulsion and aqueous solution of alpha-asarone at a single dose (40 mg x kg(-1)), respectively.</p><p><b>RESULT</b>The plasma concentration-time profiles of lipid emulsion and aqueous solution of alpha-asarone after intravenous administration of them are similar and the drug concentration-time data were fitted to a two-compartment open model. The results of tissues distribution showed that distribution contents of alpha-asarone from lipid emulsion and aqueous solution in vivo are similar in lungs but lipid emulsion increased the uptake in livers and spleens, and decreased the uptake in hearts and kidneys for alpha-asarone.</p><p><b>CONCLUSION</b>The plasma concentration-time profiles of alpha-asarone in lipid emulsion and aqueous solution are similar, but lipid emulsion significantly altered the tissue distribution of alpha-asarone, which may be beneficial to decrease its potential toxicity to heart and kidney.</p>


Subject(s)
Animals , Female , Male , Mice , Rats , Anisoles , Blood , Pharmacokinetics , Chromatography, High Pressure Liquid , Emulsions , Chemistry , Injections, Intravenous , Kinetics , Lipids , Chemistry , Rats, Sprague-Dawley , Tissue Distribution
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