论文部分内容阅读
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 physicochemical properties of percutaneous absorption of paeonol and its transdermal permeability in vitro. Methods The dissociation constants, apparent solubility, apparent oil / water partition coefficients, melting points of paeonol were determined by ultraviolet spectrophotometry, equilibrium solubility method, shake flask method, differential scanning calorimetry and in vitro diffusion cell. And in vitro transdermal penetration parameters. Results Paeonol was very slightly soluble in water with an apparent solubility of (0.386 ± 0.010) mg.mL-1, a simple weak acid with a dissociation constant of 10.47 ± 0.10 and an apparent oil / water partition coefficient of 2.054 ± 0.043. , The apparent oil / water partition coefficient decreased, the melting point was 51.27 ℃, the transdermal penetration rate (Js) was 41.05μg.cm-2.h-1 and the permeability coefficient (Ps) was 0.03μm.s-1. Conclusion Paeonol has the best physico-chemical properties and significant transdermal permeability.