微透析采样进行蛇床子软膏的皮肤局部药动学研究(1)
[摘要] 目的 建立蛇床子素在体皮肤微透析采样方法,研究蛇床子软膏在SD大鼠体内的局部药动学。 方法 采用浓差法考察浓度、流速对探针体外回收率的影响;减量法研究探针的体内回收率稳定性。SD大鼠植入皮肤探针后将蛇床子软膏涂敷于探针所在皮肤表面,测定微透析液中蛇床子素浓度,绘制药时曲线,计算药动学参数。 结果 随着灌流速度的增大,探针体外回收率有所下降,且回收率大小與蛇床子素的浓度无关;探针体内回收率为(44.29±1.28)%,体内12 h基本保持稳定;蛇床子软膏给药后,蛇床子素在皮肤组织内的透皮速率约为9.3402 μg/min,AUC0-t为8105.4 μg/(mL·min),平均滞留时间为979.8 min,能较长时间维持在较高水平。 结论 在体皮肤微透析法可用于蛇床子软膏局部药动学研究。[关键词] 蛇床子软膏;皮肤微透析;局部药动学;经皮给药
[中图分类号] R285.5 [文献标识码] A [文章编号] 1673-7210(2017)04(c)-0021-05
[Abstract] Objective To establish a method of skin microdialysis technology in vivo in order to study the local pharmacokinetics of Fructus Cnidii Ointments in rats. Methods The effect of different flow rate and concentration on the probe recovery in vitro were investigated by gain and loss method. Recovery by loss was used to study the stability of the probe recovery in vivo. The Fructus Cnidii Ointments was applied to the skin surface where the skin probe was implanted. The osthole concentration of skin microdialysates was determined ......
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