目的 优化寒痹舒凝胶膏剂的基质配方并研究其体外释放和透皮吸收行为。方法 采用D-最优混料设计, 以含药凝胶膏剂的初黏力、持黏力和胶强度3个指标对基质组成进行优化, 确定最优基质配方并进行验证试验;采用改良Franz扩散池法, 以蛇床子素为指标进行体外释放和经皮渗透性能的研究。结果 寒痹舒凝胶膏剂的基质配方为NP700 6.97 g、甘羟铝0.30 g、酒石酸0.25 g、甘油35.00 g、PVP K90 3.87 g、蒸馏水43.61 g;寒痹舒流浸膏10 g。凝胶膏中蛇床子素24 h体外释放达到(63.30±0.05)%, 经皮渗透速率为0.16 μg/(cm²·h), 24 h累积渗透量为(3.61±0.32)μg/cm²。结论 D-最优混料设计优化出的寒痹舒凝胶膏剂具有良好的黏附性和成型性。蛇床子素体外释放符合一级方程模型, 体外透皮符合零级方程模型。

Objective To optimize the matrix formulation of Hanbishu Cataplasma (HC) and to investigate its realease and transdermal absorption properties in vitro. Methods To optimize the cataplasma with liquid extract by D-optimal mixture design, using initial bonding strength, endurance bonding strength, and gel strength as evaluating indicators, and to validate the optimal formulation. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of osthole in the HC. Results The matrix formulation of HC was as follows: NP700 6.97 g, aluminum glycinate 0.30 g, tartaric acid 0.25 g, glycerin 35.00 g, PVP K90 3.87 g, water 43.61 g, and Hanbishu liquid extract 10 g. Cumulative release rate of osthole in HC was (63.30 ± 0.05)% in 24 h. The percutaneous penetration rate of osthole was 0.16 μg/(cm²·h) and the 24 h permeated amount was (3.61 ± 0.32) μg/cm². Conclusion The optimal prescription of HC optimized by D-optimal mixture design has good adhesion and formability. In vitro release characteriistics of osthole in HC conform to the first dynamical equation, and the transdermal absorption behavior is a zero-order kinetics.