~3H-氮酮透皮吸收示踪研究

  • 摘要: 氮酮(Azone)是目前应用最好的药物皮肤渗透促渗剂之一。用 ̄3H-Azone作示踪剂,研究了透皮吸收后,Azone在小鼠体内的分布、离体皮肤的渗透速率和透皮吸收后Azone在大鼠血液中的浓度和时间的关系。实验结果表明,Azone能迅速透过皮肤进入血液循环,分布到各脏器中。体外法(invitro)测定表明,它的平均渗透率为1.00μg/h·cm ̄2,在8h内总渗透率为0.70%。Azone透皮吸收后,在大鼠血液中的浓度先上升,在2h时达最大;然后下降,峰值浓度为2.70μg/ml,到24h时仍高达1.6μg/ml。由此证明Azone在皮肤上既能迅速被吸收又有持续作用。

     

    Abstract: A STUDY ON PERCUTANEOUS ABSORPTION OF AZONE WITH ~3H TRACER Shen Zilong; Lin Song (China Pharmaceutical University, Research Center, Nanjing 210009)ABSTRACT Azone is one of the best enhancer of cutaneous Penetration. The distribution of Azone in mice af-ter percutaneous absorption and in vitro diffusion of Azone through excised mice skins using tracer ~3H-Azone are studied. The concentration of Azone in rat’ s blood after percutaneous absorption is studiedalso. The ~3H-Azone is found widely distributed in lung , liver. kidney , fat , heart , brain and spleen af-ter percutaneous absorption. The total diffusion ratio of ~3H-Azone is 0. 70 per cent in 8 h. The peakconcentration(2.7μg/ml) of Azone in rat’ s blood appears at 2 h after percutaneous absorption, but re-mains l.6μg/ml at 24 h. Key words azone~3H-azone distribution percutaneous absorption

     

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