Komada F, Imanidis G, Miyajima M, Okano T, Durrani M J, Higuchi W I, Kim S W, Shannon W M, Baker D C
University of Utah, Salt Lake City, 84112.
J Pharm Sci. 1991 Oct;80(10):935-41. doi: 10.1002/jps.2600801007.
Transdermal delivery systems of 9-beta-D-arabinofuranosyladenine (ara-A), having controlling membranes of various permeabilities, were developed and applied to Azone-pretreated hairless mouse abdominal skin. It was confirmed that the blood concentrations of ara-A and its metabolite 9-beta-D-arabinofuranosylhypoxanthine (ara-H) in hairless mice are controlled by the permeability of the controlling membrane in the transdermal patch. Furthermore, these blood concentrations were found to closely agree with the values obtained from theoretical model calculations. Finally, but importantly, the "micropharmacokinetic" behavior of ara-A in cutaneous tissue could also be predicted. These results suggest that the transdermal patch may be employed in dermal and transdermal ara-A efficacy studies in the treatment of cutaneous herpes virus infections in hairless mice.
开发了具有不同渗透性控制膜的9-β-D-阿拉伯呋喃糖基腺嘌呤（ara-A）透皮给药系统，并将其应用于用氮酮预处理的无毛小鼠腹部皮肤。结果证实，无毛小鼠体内ara-A及其代谢产物9-β-D-阿拉伯呋喃糖基次黄嘌呤（ara-H）的血药浓度受透皮贴剂中控制膜的渗透性控制。此外，发现这些血药浓度与理论模型计算得到的值非常吻合。最后但同样重要的是，还可以预测ara-A在皮肤组织中的“微观药代动力学”行为。这些结果表明，透皮贴剂可用于无毛小鼠皮肤疱疹病毒感染治疗中ara-A的皮肤和透皮疗效研究。
