药物经离体角质层渗透的非平衡态特性药物经离体角质层渗透的非平衡态特性

目的阐述药物在经角质层渗透过程中的非平衡态特性,为经皮给药技术提供理论和方法。方法把离体扩散池系统设定为孤立系统,建立系统达到平衡态的条件和网络热力学模型。以替硝唑为模式药物,进行非平衡态实验和漏糟实验。结果非平衡态包括:达到平衡态的长时程性;渗透启动的延迟性;初始通量的不确定性。漏糟包括:渗透通量递减性;渗透时间常数的可变性。结论扩散池药物经角质层渗透系统是一个非线性时变系统。

Non-equilibrium properties of drug permeation through stratum corneum in vitro

AimTo illustrate the non-equilibrium properties of drug permeation through stratum corneum (SC) to provide theory and method for transdermal drug delivery. MethodsThe system of side-by-side permeation chambers in vitro was isolated, thus conditions for equilibrium state were decided. And a network thermodynamic model was established. Non-equilibrium and leakage experiments were completed with which tinidazole was pattern drug. ResultsThe properties of non-equilibrium including: long term to reach equilibrium state; delay-start of the permeation; uncertainty of initial drug permeable flux. The properties of leakage including: degression of drug permeable flux; changeability of permeation time constant. Conclusion The permeation cell is believed to be a non-linear and time variable system.