丹皮酚理化性质及体外经皮渗透性的研究

Physical and Chemical Properties and Percutaneous Penetration of Paeonol

目的研究丹皮酚与经皮吸收相关的理化性质以及体外经皮渗透性能。方法采用紫外分光光度法、平衡溶解度法、摇瓶法、差示扫描量热法和体外扩散池法,分别测定丹皮酚的解离常数、表观溶解度、表观油/水分配系数、熔点和体外经皮渗透参数。结果丹皮酚极微溶解于水,表观溶解度为(0.386±0.010)mg.mL-1;为一元弱酸,解离常数为10.47±0.10;表观油/水分配系数为2.054±0.043,随pH的增加,表观油/水分配系数降低;熔点为51.27℃;体外经皮渗透速率(Js)为41.05μg.cm-2.h-1,渗透系数(Ps)为0.03μm.s-1。结论丹皮酚具有适宜经皮渗透的理化性质及显著的经皮渗透性能。

Objective To study the physical and chemical properties associated with percutaneous absorption and percutaneous penetration of paeonol.Methods Ultraviolet spectrophotometry,equilibrium solubility method,shaking method,differential scanning calorimetry（DSC） and in-vitro diffusion cell method wee used to determine the dissociation constant,apparent solubility,apparent oil / water partition coefficient,melting point and percutaneous penetration of paeonol,respectively.Results The results showed that paeonol was mildly dissolved in water with a apparent solubility of（0.386±0.010）mg·mL-1.It was an acid with weak polarity,and the dissociation constant was 10.47±0.10.The apparent oil/water partition coefficient of paeonol was 2.054 ± 0.043,and increased with the pH value.The melting point of paeonol was 51.27 ℃,the percutaneous penetration rate（Js） was 41.05 μg·cm-2·h-1,and the permeability coefficient（Ps） was 0.03 μm·s-1.Conclusion Paeonol exerts appropriate physical and chemical properties and is easy for percutaneous penetration.