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以?-萜品醇为先导化合物合成其脂肪酸酯衍生物[丁酸萜品醇酯(T-BUT)和己酸萜品醇酯(T-HEX)]。采用卧式双室扩散池,以离体兔皮为屏障进行体外渗透试验,考察了合成得到的萜品醇酯、?-萜品醇、月桂氮酮(azone)和N-甲基吡咯烷酮(NMP)在肉豆蔻酸异丙酯(IPM)系统中对硝酸异山梨酯(1)渗透行为的影响。结果表明,与不加促渗剂(空白)相比,浓度为5%的萜品醇、T-BUT、T-HEX、azone及NMP对1均有显著的促透作用(P<0.05);与萜品醇相比,NMP、T-BUT和T-HEX的促渗作用均显著提高(P<0.05)。可见,萜品醇脂肪酸酯能显著提高萜品醇的促透能力。当5%NMP与5%T-HEX联用时,1的8 h累积透过量是空白组的11.24倍。
The fatty acid ester derivatives (T-BUT and T-HEX) were synthesized from? -terpineol as the lead compound. In vitro two-compartment diffusion cells were used to in vitro rabbit skin as a barrier for in vitro penetration tests were investigated, the synthesis of terpineol esters,? -terpineol, azone and N-methylpyrrolidone (NMP ) On permeation behavior of isosorbide dinitrate (1) in isopropyl myristate (IPM) system. The results showed that 5% terpineol, T-BUT, T-HEX, azone and NMP could significantly promote the permeation of 1 (P <0.05) compared with those without permeation enhancer (blank) Compared with terpineol, the promoting effect of NMP, T-BUT and T-HEX significantly increased (P <0.05). It can be seen that terpineol fatty acid ester can significantly enhance the permeability of terpineol. When 5% NMP combined with 5% T-HEX, the cumulative transmission of 1 at 8 h was 11.24 times that of the blank group.