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业已证明,茜草(Rubia Cordifolia L)的提取物具有升高外周血白细胞的作用(简称升白)。近年来又从茜草提取物中进一步分离出2个具有升白作用的茜草酸甙Ⅰ和Ⅱ,两种甙的甙元相同,化学结构为1,4-萘二酚-2-羧酸,由此合成的1,4-萘二酚2,3-二羧酸乙酯(简称茜草双酯),在动物实验中也具有明显的升白作用,它在小鼠中能促进骨髓造血干细胞增殖,在狗中对环磷酰胺所致的白细胞减少也有一定的防治作用。本药毒性小,合成工艺简单,值得作进一步研究及临床试用。为此,本文在狗中研究了口服茜草双酯后的药代动力学特性,及其与升白作用的相应关系,以便为临床试用时如何制定最佳给药方案提供依据。
Rubia Cordifolia L. extract has been shown to have an effect of raising peripheral white blood cells (simply referred to as “whitening”). In recent years, from Rubia cordifolia extract two further with the role of white Qian Qian glycosides Ⅰ and Ⅱ, glycosides two glycosides the same chemical structure of 1,4-naphthalene-2-carboxylic acid, from The synthesized 1,4-naphthalenediol 2,3-dicarboxylic acid ethyl ester (Rubiacetin) has obvious whitening effect in animal experiments, which can promote the proliferation of bone marrow hematopoietic stem cells in mice, In dogs caused by cyclophosphamide leukopenia also have some control effect. The drug toxicity is small, the synthesis process is simple, it is worth further study and clinical trial. Therefore, we studied the pharmacokinetics of Rubiacet after oral administration in dogs, and the corresponding relationship between the pharmacokinetics and the whitening effect in order to provide the basis for the best dosing regimen in clinical trial.