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大黄的主要有效成分是大多以苷形式存在的蒽醌类化合物。我们采用高效液相色谱法来测定组织和血浆中蒽醌类化合物(芦荟大黄素、大黄素、大黄酸、大黄酚和大黄素甲醚)的浓度。对家兔和大鼠灌胃给予不同制剂后大黄蒽醌类化合物的药代动力学参数和分布特征进行了研究,结果发现其在家兔和大鼠体内的消除过程满足二室模型,在大鼠体内的过程用大黄酸以及总蒽醌的量来计算出的主要药代动力学参数无统计学差异。大黄蒽醌类化合物主要分布于肾、肝、心和血中,并依次减少,蒽醌类化合物在体内主要以大黄酸的形式存在并由肾排出体外。可以以大黄酸作为指标成分来进行含大黄类成分的复方制剂在体内的药代动力学研究。
The main active ingredient of rhubarb is anthraquinones mostly in the form of glycosides. We used high-performance liquid chromatography to determine the concentrations of anthraquinones (aloe-emodin, emodin, rhein, chrysophanol and physcion) in tissues and plasma. The pharmacokinetic parameters and distribution characteristics of anthraquinones of Rhubarb after intragastric administration of different formulations in rabbits and rats were studied. The results showed that the elimination process of rhubarb anthraquinones in rabbits and rats satisfied the two-compartment model, There was no statistical difference in the main pharmacokinetic parameters calculated from rhein and total anthraquinone in the rat body. Rhubarb anthraquinones are mainly distributed in the kidney, liver, heart and blood, and in turn reduce the anthraquinones in the body mainly in the form of rhein and excreted by the kidneys. Rhein can be used as an index component to perform pharmacokinetic studies in vivo of compositions containing rhubarb.