新型染料木素磺酸酯的前药判定与大鼠体内生物利用度

doi:A

天然产物研究与开发 ›› 2012, Vol. 23 ›› Issue (1): 35-41.doi: A

新型染料木素磺酸酯的前药判定与大鼠体内生物利用度

彭游^1,2*，刘新强¹，邓泽元²

¹九江学院化工学院，九江332005；²南昌大学食品科学与技术国家重点实验室，南昌 330047

收稿日期:2011-05-05 出版日期:2012-01-30 发布日期:2012-02-15

Prodrug Decision of Novel Genistein Sulfonate and Its Bioavailability in Rats

PENG You^1,2*, LIU Xin-qiang ¹, DENG Ze-yuan ²

¹Department of Chemistry and Engineering, Jiujiang University, Jiujiang 332005, China; ²State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang 330047, China

Received:2011-05-05 Online:2012-01-30 Published:2012-02-15
Supported by:
The authors acknowledge support from the National Natural Science Foundation of China (No. 81160412), the Natural Science Foundation of Jiangxi, China (No. 2010GZN0106) and the Science and Technology Item of the Education Department of Jiangxi Province (No. GJJ11626).

摘要/Abstract

摘要： 为寻找新的前药或食品功能成分，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（GE）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，该前体药以40 mg/kg灌胃和静注给药后，GE在大鼠体内的动力学过程符合二室模型。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。

关键词: 染料木素, 磺酸酯, 前药, 药物动力学, 生物利用度

Abstract: The oral bioavailability of genistein (GE) in its benzensulfonate prodrug was studied in search for new drug or food functional ingredient. 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 two 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.

Key words: genistein, sulfonate, progrug, pharmacokinetics, bioavailability

中图分类号:

R284.2

彭游，刘新强，邓泽元. 新型染料木素磺酸酯的前药判定与大鼠体内生物利用度[J]. 天然产物研究与开发, 2012, 23(1): 35-41.

PENG You, LIU Xin-qiang, DENG Ze-yuan. Prodrug Decision of Novel Genistein Sulfonate and Its Bioavailability in Rats[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2012, 23(1): 35-41.

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新型染料木素磺酸酯的前药判定与大鼠体内生物利用度

Prodrug Decision of Novel Genistein Sulfonate and Its Bioavailability in Rats

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