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目的:考察不同pH值对马钱子碱油水分配系数和体外经皮渗透性的影响。方法:采用恒温水浴磁力搅拌法,测定马钱子碱的油水分配系数;改良的Franz扩散池进行体外经皮吸收实验,选择离体大鼠腹部皮肤为渗透屏障,HPLC测定马钱子碱的浓度。结果:pH值为5,6,7.4,8,9时,油水分配系数分别为:0.04,0.25,3.59,11.02,26.05;累积透过百分率为:(56.785±27.825)%,(71.258±5.46)%,(63.760±8.176)%,(70.232±5.72)%,(75.551±2.48)%,油水分配系数随着pH的升高而增大,而经皮渗透速率不随pH的增大规律性升高,在pH值为9时,渗透速率最大。结论:本研究为马钱子碱贴剂制备提供实验依据。
OBJECTIVE: To investigate the effects of different pH values on the distribution coefficient of strychnine oil and water and the transdermal permeability in vitro. Methods: The oil-water partition coefficient of brucine was determined by a magnetic stirring method in a constant temperature water bath. The percutaneous absorption test was carried out in a modified Franz diffusion cell. The abdominal skin of isolated rat was used as the permeation barrier. The concentration of brucine . Results: The partition coefficients of oil and water were 0.04, 0.25, 3.59, 11.02 and 26.05 respectively at the pH values of 5, 6, 7, 8, 8 and 9; the cumulative percentages of permeation were (56.785 ± 27.825)% and (71.258 ± 5.46) %, (63.760 ± 8.176)%, (70.232 ± 5.72)% and (75.551 ± 2.48)%, respectively. The oil-water partition coefficient increased with the increase of pH, while the transdermal permeation rate did not increase with the increase of pH At pH 9, the permeation rate was the highest. Conclusion: This study provides experimental evidence for the preparation of brucine patches.