中文摘要：

为寻找染料木素（GE）新的前药,采用建立的生物样品中药物浓度测定的液相色谱法对新型大豆异黄酮染料木素磺酸酯（GB）进行前药判定以及大鼠体内药物动力学研究,以考察前药中染料木素的口服生物利用度是否改善。在大鼠体内药物代谢实验中,灌胃给予GB的大鼠血浆中能检测到明显的GE。在临床前药物动力学实验中,该前体静注给药和以40 mg/kg灌胃药后,GE在大鼠体内的动力学过程均符合一室模型。GB中GE的相对口服生物利用度为原药的110.9%。研究表明,相对于原药GE,前药中GE的相对口服生物利用度达到预期的改善,该前药有进一步研究意义。

英文摘要：

The oral bioavailability of genistein（GE） in its benzensulfonate prodrug was studied in search for new drug.The plasma were collected at different points of time after the intragastric or intravenous administration of genistein benzensulfonate（GB） 40 mg/kg to rats.The GB and GE contents in plasma were determined by high performance liquid chromatography（HPLC）.The compartment model was fitted and pharma cokinetic parameters were calculated by DAS 2.1.1.The results indicated that the dynamic processes of GE was consistent with one compartment model after intragastric or intravenous administration of GB prodrug to rats.The relative oral bioavailability of GE in prodrug GB was 110.9%.In conclusion,the above results demonstrated that the oral bioavailability of GE in prodrug had been improved remarkably.