OBJECTIVE To study the skin permeation of Huperzine A (Hup-A) in vitro transdermal patches in mouse,dog and human skins,and provide data for the formulation screening,pharmacodynamic and pharmacokinetics studies.METHODS In vitro permeation studies were conducted using two-chambered Valia-Chien glass diffusion cell assembly in three different skin species. Hup-A concentrations were determined by HPLC method,and permeation rates of Hup-A were calculated and compared.RESULTS The penetration of Hup-A through mouse skin was quicker and permeation rate was higher than that through dog and human skins. The permeation rate-time profiles of Hup-A through dog and human skins were similar.Hup-A permeation rate reached the maximum approximately 12~24 h following the application of the patch,and then maintained for up to 84 h.CONCLUSION The Hup-A permeation rates of mouse and human skins were greatly different. So,the mouse-based pharmacodynamics should be designed according to the in vitro Hup-A skin permeation study. In addition,the similarity of Hup-A skin permeation between dog and human skin supports the use of the dog as a species for evaluating the pharmacokinetics of transdermally-administered Hup-A.
YE Jin-cui;CHEN Guo-shen.
Skin Permeation of Huperzine A in Different Skin Species [J]. Chinese Pharmaceutical Journal, 2007, 42(14): 1095-1097
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参考文献
[1] LEE W R,SHEN S C,LAI H H,et al. Transdermal drug delivery enhanced and controlled by erbium:YAG laser:a comparative study of lipophilic and hydrophilic drugs [J] . J Controlled Release,2001,75(1-2):155-160.
[2] TANG X C. Huperzine A (shueng yiping):a promising drug for Alzheimer’s disease [J] .Acta Pharmacol Sin,1996,17(6):481-484.
[3] XU S S,CAI Z Y,QU Z W,et al. Huperzine-A in capsules and tablets for treating patients with Alzheimer's disease [J] . Acta Pharmacol Sin(中国药理学报),1999,20(6):601-603.
[4] YE J C,ZENG S,ZHANG W G,et al. Ion-pair RP-HPLC method for determination of Huperzine A in beagle dog serum [J] . J Chromatography B,2005,817(2):187-191.
[5] SHI H,YE J C,QIAN B C,et al. Improvement function of huperzine-A transdermal drug delivery system administration at Governor Vessel acu-points on memory disorders induced by scopolamine in mice[J] . Chin J Clinical Pharmacol Ther(中国临床药理学与治疗学),2002,7(6):489-492.
[6] SHI H,YE J C,ZHANG W G,et al. The improvement Function of huperzine-A transdermal drug delivery system on learning and memory in mice [J] . Chin J Mod Appl Pharm,2002,19(4):276-277.