D-最优混料设计结合多种力学指标优化柴栀凝胶贴膏的基质处方及其体外释放透皮研究

Matrix formulation of chaizhi cataplasma optimized by D-optimal mixture design combined with multiple mechanical indicators and its in vitro evaluation

该研究旨在优化柴栀凝胶贴膏的基质配方以及评价其体外释放与透皮行为。采用D-最优混料设计,通过探子初黏力试验,180度剥离强度试验和胶强度试验测定凝胶贴膏的黏性指标,包括初黏力,黏接力和内聚力,确定最优基质处方。采用改良Franz扩散池法,以有效成分栀子苷为指标,研究凝胶贴膏的体外释放和经皮渗透性能。柴栀凝胶贴膏的基质配方为NP700,甘羟铝,酒石酸,甘油,PVP K90,蒸馏水(9∶0.7∶0.8∶30∶5∶30.5)。凝胶贴膏中栀子苷24 h体外释放(77.02±3.73)%,经皮渗透速率为7.25μg·cm^(-2)·h^(-1),24 h累积渗透量为(156.22±4.90)μg·cm^(-2)。最优基质处方下制备的柴栀凝胶贴膏具有良好的黏性,栀子苷体外释放符合一级方程,体外透皮接近零级方程。

To optimize the matrix formulation of Chaizhi cataplasma（ CC） and investigate its release and transdermal absorption properties in vitro. The optimized matrix formulation of cataplasma containing liquid herbal extract is determined by using D-optimal mixture design,with initial bonding strength,endurance bonding strength and gel strength as the evaluating indicators. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of geniposide in CC. The optimized matrix formulation of CC contained NP700,aluminum glycinate,tartaric acid,glycerin,PVPK90 and water（ 9∶ 0. 7 ∶ 0. 8 ∶ 30 ∶ 5 ∶ 30. 5）. Cumulative release rate of geniposide in CC was（ 77. 02 ± 3. 73） % in 24 h. The percutaneous penetration rate of geniposide was 7. 25 μg·cm^（-2）·h^（-1）and the 24 h permeated amount was（ 156. 22 ± 4. 90） μg·cm^（-2）. The optimized CC prepared by the D-optimal mixture design showed a good adhesion and formability. The in vitro release of the geniposide in CC was in accordance with the first order equation,while its in vitro transdermal absorption was close to the zero order equation.