2012•Tianran chanwu yanjiu yu kaifaRequires access

Prodrug Decision of Novel Genistein Sulfonate and Its Bioavailability in Rats

Zeyuan Deng

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Abstract

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.

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What this paper is about

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.

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Available abstract

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.

Key concepts: Bioavailability, Prodrug, Genistein, Oral administration, Chemistry, Pharmacology, Plasma concentration, Pharmacokinetics

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