不同溶剂对扑热息痛体外透皮吸收的影响

The effect of percutaneous absorption of paracetamol across the excised rat's skin in different dissolvant

【目的】研究不同溶剂组成对扑热息痛体外经皮渗透的影响。【方法】采用Franz扩散池,用离体大鼠皮肤考察乙醇、丙二醇、甘油及聚乙二醇4种溶剂单用与合用对扑热息痛体外经皮透过性影响的研究。【结果】单用乙醇、丙二醇、甘油及聚乙二醇4种溶剂时扑热息痛体外经皮累积透过量不同,其中乙醇为溶剂的累积释放量最大,甘油及聚乙二醇的累积释放量最小。而采用不同比例乙醇水(5%、10%、15%)做溶剂时,随乙醇比例增大,扑热息痛的累积释放量增加。而分别采用混合溶剂15%乙醇水中加入10%丙二醇、甘油、聚乙二醇,扑热息痛的累积释放量无明显增加,而15%乙醇水混合溶剂中,扑热息痛的累积释放量明显增加。【结论】在4种不同溶剂,15%的乙醇水做溶剂时,扑热息痛经皮透过量最大,说明乙醇作为溶剂对扑热息痛有一定的促透作用。

[Objective] To study the effects of different dissolvant on percutaneous absorption of paracetamol through rat＇ s skin. [Methods] Using the improved Franz diffusion cells, to investigate the effect of Ethanol, PF, Glycerine, PEG in the experiment of percutaneous of paracetamol through rat＇s skin in vitro. [Results] Accumulated transit dose in Ethanol is maximum, accumulated transit dose in PF and Glycerine is minemum. Using Ethanol in different concentration as dissolvant, accumulated transit dose of paracetamol increasing accompany with the concentration of Ethanol increased. Add the PF, Glycerine, PEG into the Ethanol at the concentrations of 15%, accumulated transit dose of paracetamol has no signifficant increase, however, accumulated transit dose of paracetamol has signifficantly increase in Ethanol at the concentrations of 15%. [Conclusions] In four different dissolvants, accumulated transit dose of paracetamol in Ethanol at the concentrations of 15 % is maximum. It is shown that Ethanol can enhance the percutaneous absorption of paracetamol through rat＇ s skin.