广西植物
廣西植物
엄서식물
GUIHAIA
2012年
3期
392-399
,共8页
染料木素磺酸酯%前药%药物动力学%生物利用度
染料木素磺痠酯%前藥%藥物動力學%生物利用度
염료목소광산지%전약%약물동역학%생물이용도
genistein sulfonate%prodrug%pharmacokinetics%bioavailability
为寻找新的大豆异黄酮前药,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(GBS)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)的口服相对生物利用度是否改善.在大鼠体内药物代谢实验中,灌胃给予的大鼠血浆中能检测到GE的存在.在临床前药物动力学实验中,该前体药以40 mg/kg GE在大鼠体内的动力学过程符合一室模型.GBS中GE的相对口服生物利用度为原药的198.6％.结果表明:相对于原药GE,前药中GE的相对口服生物利用度得到极大地改善.该前药有进一步研究的意义.
為尋找新的大豆異黃酮前藥,採用建立的生物樣品中藥物濃度測定的液相色譜法對新型大豆異黃酮染料木素磺痠酯(GBS)進行前藥判定以及大鼠體內藥物動力學研究,以攷察前藥中染料木素(GE)的口服相對生物利用度是否改善.在大鼠體內藥物代謝實驗中,灌胃給予的大鼠血漿中能檢測到GE的存在.在臨床前藥物動力學實驗中,該前體藥以40 mg/kg GE在大鼠體內的動力學過程符閤一室模型.GBS中GE的相對口服生物利用度為原藥的198.6％.結果錶明:相對于原藥GE,前藥中GE的相對口服生物利用度得到極大地改善.該前藥有進一步研究的意義.
위심조신적대두이황동전약,채용건립적생물양품중약물농도측정적액상색보법대신형대두이황동염료목소광산지(GBS)진행전약판정이급대서체내약물동역학연구,이고찰전약중염료목소(GE)적구복상대생물이용도시부개선.재대서체내약물대사실험중,관위급여적대서혈장중능검측도GE적존재.재림상전약물동역학실험중,해전체약이40 mg/kg GE재대서체내적동역학과정부합일실모형.GBS중GE적상대구복생물이용도위원약적198.6％.결과표명:상대우원약GE,전약중GE적상대구복생물이용도득도겁대지개선.해전약유진일보연구적의의.
The oral bioavailability of genistein (GE) in its benzensulfonate prodrug was studied in search for its novel prodrug.The plasmas were collected at different points of time after the intragastric or intravenous administration of genistein benzensulfonate (GBS) 40 mg/kg to rats.The GBS and GE contents in plasma were determined by 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 were consistent with two compartment model after intragastric administration of GBS prodrug to rats.The relative oral bioavailability of GE in prodrug GBS was 198.6％.In conclusion,the above results demonstrated that the oral bioavailability of GE in prodrug had been improved remarkably.
