辣椒素理化性质及体外透皮性能的研究

Physical and Chemical Properties and Percutaneous Permeation of Capsaicin

目的研究辣椒素的理化性质及体外透皮性能。方法采用平衡溶解度法、紫外分光光度法、摇瓶法、差示扫描量热法和体外扩散池法,分别测定辣椒素的表观溶解度、解离常数、表观油/水分配系数、熔点和体外经皮渗透参数,并采用滞留时间法评价其经皮渗透特性。结果辣椒素极微溶于水,表观溶解度为(22.85±0.06)mg.L-1;为弱碱,解离常数为(10.25±0.11);表观油/水分配系数随pH的增加而变化,当pH>8时lg P增加;熔点为60.20℃。辣椒素的滞留时间(tlag)为(2.437±0.273)h,体外经皮渗透参数(P)为(7.012±0.341)×10-2cm.h-1,渗透速率(Js)为(4.647±0.226)μg.cm-2.h-1。结论辣椒素具有适宜经皮渗透的理化性质及较好的经皮渗透性能。

OBJECTIVE To study the physical and chemical properties and transdermal delivery characteristics of capsaicin. METHODS Equilibrium solubility method, ultraviolet spectrophotometry, bottle-shaking method, differential scanning calorimetry （DSC） and in vitro diffusion eel1 method were used to determine the apparent solubility, dissociation constant, apparent oil/water partition coefficient, melting point and percutaneous penetration of capsaicin, respectively. And the permeation characteristics were evaluated by lag time method. RESULTS Capsaicin was slightly dissolved in water, and the apparent solubility was （22. 85 ± 0. 06 ） mg· L^-1. It was a weak base with a dissociation constant of（ 10. 25 ±0. 11 ）. The apparent oil/water partition coefficient of capsaiein changed with the pH value, and increased when pH was greater than 8. Its melting point was 60. 20 ℃. The residence time（ tlag） was （2. 437 ± 0. 273 ） h, the permeability coefficient （P） （7. 012 ± 0. 341 ） ·10^ -2 cm· h ^-1, and the pereutaneous penetration rate （ Js ） （4. 647 ±0. 226） μg ·cm^-2 ·h^-1. CONCLUSION Capsaiein possesses appropriate physical and chemical properties for percutaneous penetration and exhibits excellent percutaneous penetration.