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1、學(xué)報(bào)60JournalofChinaPharmaceuticalUniversity2007,38(1):60-64藥物轉(zhuǎn)運(yùn)蛋白對(duì)燈盞花素小腸吸收的影響12X張海燕,平其能(12蘇州東瑞制藥有限公司研發(fā)部,蘇州215128;中國(guó)藥科大學(xué)藥劑學(xué)教研室,南京210009)摘要目的:研究藥物轉(zhuǎn)運(yùn)蛋白P2糖蛋白(P2gp)和多藥耐藥相關(guān)蛋白(MRP2)對(duì)燈盞花素小腸吸收的影響。方法:HPLC法測(cè)定大鼠腸液中燈盞花素的濃度,以大鼠在體單向灌流實(shí)驗(yàn)(SPIP)研究藥物的小腸吸收,計(jì)算不含抑制劑藥物組和含抑制劑藥物組
2、的小腸表觀滲透系數(shù)(Papp)。結(jié)果:含P2gp抑制劑藥物組與原藥組相比,Papp沒(méi)有顯著變化;含MRP2抑制劑藥物組與原藥組相比,Papp顯著增加。結(jié)論:P2gp對(duì)燈盞花素的小腸吸收基本沒(méi)有影響,而MRP2可將吸收的燈盞花素從腸上皮細(xì)胞內(nèi)又轉(zhuǎn)運(yùn)回腸腔,從而降低燈盞花素的吸收。關(guān)鍵詞燈盞花素;P2糖蛋白;多藥耐藥相關(guān)蛋白;小腸吸收;單向灌流中圖分類號(hào)R969.2文獻(xiàn)標(biāo)識(shí)碼A文章編號(hào)1000-5048(2007)01-0060-05Effectsofdrugtransportersonintestinal
3、absorptionofbreviscapine12ZHANGHai2yan,PINGQi2neng1DepartmentofResearchandDevelopment,DawnraysPharmaceuticalCo.,Ltd.,Suzhou215128;2DepartmentofPharmaceutics,ChinaPharmaceuticalUniversity,Nanjing210009,ChinaAbstractAim:Toinvestigatetheeffectsofdrugtranspo
4、rters,includingP2glycoprotein(P2gp)andmultidrugresis2tance2associatedprotein(MRP2),onintestinalabsorptionofbreviscapine.Methods:BreviscapineconcentrationinratintestinalperfusionsolutionwasdeterminedbyHPLC.Ratsinglepassintestinalperfusion(SPIP)wasemployed
5、tostudybreviscapineintestinalabsorptioninordertoevaluatetheintestinalapparentpermeationcoefficients(Papp)ofbreviscap2inegroupandinhibitorgroup.Results:BasedonthestatisticalanalysisofPapp,P2gpinhibitorhasnomarkedeffectsontheintestinalabsorptionofbreviscap
6、ine.WhileforMRP2inhibitor,Pappweresignificantlyhigherthanthatofthebreviscapinegroup.Conclusion:P2gptransporterhasnoeffectonintestinalabsorptionofbreviscapine,andMRP2transporterisinvolvedintheintestinalabsorptionofbreviscapinepossiblyviatransportingbrevis
7、capinefromintestinalepitheliumtointestinalcavity.Keywordsbreviscapine;P2glycoprotein;multidrugresistance2associatedprotein;intestinalabsorption;singlepassin2testinalperfusionThisprojectwassupportedbytheNationalNaturalScienceFoundationofChina(No.30430790)
8、燈盞花素是從菊科植物短葶飛蓬中提取的黃泌回腸腔,導(dǎo)致藥物吸收減少,生物利用度降低。酮類成分,以燈盞乙素為主,化學(xué)名為4′,5,62三羥已報(bào)道的藥物轉(zhuǎn)運(yùn)蛋白有:P2糖蛋白(P2gp)、多藥基黃酮272葡萄糖醛酸苷。燈盞花素普通片劑生物耐藥相關(guān)蛋白(MRP)、有機(jī)陰離子轉(zhuǎn)運(yùn)載體[1]利用度只有(014±0119)%。為提高其口服生物(OAT)、有機(jī)陽(yáng)離子轉(zhuǎn)運(yùn)載體(OCT)和陽(yáng)離子交換[2]利用度,近年來(lái)人們開(kāi)始在細(xì)胞分子水平上研究影載體(OET
