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使用四氢香叶醇(THG)作为母体,采用格式反应制备4,8二甲基1壬醇(DIMNOL)。研究DIMNOL对5氟脲嘧啶和盐酸曲马多渗透离体鼠皮的促进作用。以阿佐恩(Azone)和四氢香叶醇(THG)为对照,DIMNOL,THG和Azone对5氟脲嘧啶,分别可使药物渗透系数增加3678,4830,8272倍。而对盐酸曲马多,则分别增加11325,10969,9304倍。这些促进剂能增加药物的分配系数的扩散系数值。可以认为这些促进剂的作用方式是影响分配和扩散过程,其中扩散过程是主要因素。
Tetrahydro geraniol (THG) was used as the precursor to prepare 4, 8-dimethyl-1-nonyl alcohol (DIMNOL) by the format reaction. To investigate the promoting effect of DIMNOL on 5fluorouracil and tramadol hydrochloride isolated rat skin. With Azone and THG, DIMNOL, THG and Azone could increase the drug permeation coefficient by 36.78, 4830 and 8272 times for 5fluorouracil, respectively. Tramadol hydrochloride, respectively, an increase of 113.25, 109.69, 93.04 times. These enhancers increase the diffusion coefficient value of the drug’s partition coefficient. It can be considered that the mode of action of these accelerators is to influence the distribution and diffusion processes, of which the diffusion process is the major factor.