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去甲斑蝥素在人工胃液及人工肠液中均以去甲斑蝥酸的形式存在。该化合物为二元酸,有二步解离,按Noyes法计算,其pKa_1=4.02±0.02、pKa_2=5.86±0.02。去甲斑蝥酸为弱有机酸,在人体液中有解离型及分子型两种形式存在,而分子型在胃中易于吸收。按照Handerson-Hasselpha-lch方程计算,口服去甲斑蝥素后在血液中几全部以解离型存在,在胃中约99%以分子型存在,因而预示口服吸收良好,与静脉给药将有同样效果。通过药物的PKa及所在人体部位的pH测定、计算,可初步预示其存在形式及吸收情况。本实验预示的结果,与动物实验及临床观察结果基本一致。
Norcantharidin in artificial gastric juice and artificial intestinal fluid are in the form of norcantharidinic acid. The compound is a dibasic acid with two steps of dissociation. According to the Noyes method, its pKa_1 = 4.02 ± 0.02 and pKa_2 = 5.86 ± 0.02. To cantharidate acid as a weak organic acids, there is dissociation in human body fluids and molecular forms exist in two forms, while the molecular type in the stomach is easy to absorb. Calculated in accordance with the Handerson-Hasselpha-lch equation, almost all of the blood in the presence of norcantharidin exists as a dissociated form, with about 99% being present in the stomach as a molecular pattern, thus indicating a good oral absorption and will be the same as intravenous administration effect. Through the drug PKa and where the human body parts of the pH determination, calculation, can be preliminarily predicted its existence and absorption. The results predicted by this experiment are basically consistent with the results of animal experiments and clinical observations.