不同结构萜类对盐酸普萘洛尔透皮活化能的影响

目的 研究不同结构萜类对盐酸普萘洛尔透皮活化能的影响.方法 测定不同温度下盐酸普萘洛尔透过离体鼠皮的渗透系数,根据Arrhenius方程计算透皮活化能.结果 由计算公式得到不同条件下的Arrhenius方程,方程变量间相关系数良好(r>0.97).由方程斜率计算得到,对照溶液中盐酸普萘洛尔的活化能为90.06 kJ/mol,而薄荷醇、薄荷酮和红没药醇存在下的活化能分别为69.42、106.14、124.39 kJ/mol.结论 盐酸普萘洛尔透过鼠皮需要较高活化能,除薄荷醇外,薄荷酮和红没药醇不能降低其透皮活化能.推断其原因可能为盐酸普萘洛尔与萜之间形成分子间氢键.

Effect of terpenes of different structure on transdermal activation energy of propranolol hydrochloride

Objective To investigate the effect of terpenes of different structure on the transdermal activation energy of propranolol hydrochloride.Methods The permeability coefficients of propranolol hydrochloride through the rat skin were determined in vitro at different temperatures and the transdermal activation energy was calculated from Arrhenius relationship.Results The Arrhenius equations under different conditions were calculated,in which there was good coefficient relationship（r0.97）between the varieties.The transdermal activation energy of propranolol hydrochloride calculated from the slope of Arrhenius equations was 90.06 kJ/mol in the control solution,69.42 kJ/mol in menthol solution,106.14 kJ/mol in menthone solution,and 124.39 kJ/mol in bisabolol solution.Conclusions A strong transdermal activation energy of propranolol hydrochloride is required to pass through the rat skin.Terpenes except menthol cannot decrease the energy significantly.The possible mechanism might be the formation of molecular hrdrogen bonds between propranolol hydrochloride and terpenes.