NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2012, Vol. 23 ›› Issue (1): 35-41. doi: A

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Prodrug Decision of Novel Genistein Sulfonate and Its Bioavailability in Rats

PENG You1,2*, LIU Xin-qiang 1, DENG Ze-yuan 2   

  1. 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).

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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

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