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1、冰片-薄荷腦低共熔物對納米粒鼻腔給藥載藥入腦的影響[基金項(xiàng)目]國家自然科學(xué)基金項(xiàng)目（30772793），浙江省衛(wèi)生高層次創(chuàng)新人才培養(yǎng)工程柴國寶[作者簡介]柴國寶，男，碩士研究生，研究方向：藥物新劑型與新技術(shù)，Tel：（0571）86613726，夏愛曉，蔡鑫君，魏穎慧，馮健，李范珠*[通訊作者]李范珠，教授，博士生導(dǎo)師，Tel：（0571）86633030Fax：（0571）86613606Email：lifanzhu@zjtcm.net（浙江中醫(yī)藥大學(xué)藥學(xué)院，杭州，310053）摘要目的：考察中藥冰
2、片-薄荷腦低共熔物對神經(jīng)毒素納米粒鼻腔給藥吸收入腦的影響。方法：采用125I同位素標(biāo)記法，以清醒自由活動(dòng)大鼠為實(shí)驗(yàn)?zāi)Ｐ?，運(yùn)用腦微透析取樣技術(shù)，測定腦內(nèi)神經(jīng)毒素濃度的變化，并應(yīng)用藥動(dòng)學(xué)軟件計(jì)算藥動(dòng)學(xué)參數(shù)。結(jié)果：中藥冰片-薄荷腦低共熔物納米粒腦藥動(dòng)學(xué)符合二室模型，Tmax、Cmax、AUC、t1/2(β)分別為0.68h、27.32ng/mL、132.68ng·h/mL、3.1076h，其入腦的速度與程度均優(yōu)于單用薄荷腦或者冰片。結(jié)論：神經(jīng)毒素納米粒在冰片-薄荷腦低共熔物作用下，可顯著增加其鼻腔吸收入腦的
3、藥量，且能較快達(dá)到峰濃度，消除緩慢。關(guān)鍵詞：冰片-薄荷腦低共熔物;納米粒;鼻腔給藥;腦藥動(dòng)學(xué)Effectofborneol/mentholumeutecticmixtureonnasal-braindeliveryofneurotoxinloadednanoparticlesCHAIGuo-bao,XIAAi-xiao,CAIXin-jun,WEIYing-hui,FenJian,LIFan-zhu*(CollegeofPharmacy,ZhejiangUniversityofTraditionalC
4、hineseMedicine,Hangzhou,310053)ABSTRACTObjectiveToinvestigatetheabsorptionenhanceneffectofborneol/mentholumeutecticmixture(BO/ME)onnasal-braindeliveryofneurotoxinloadednanoparticles.MethodsUsingmicrodialysissamplingtechniqueinawakefreely-movingrats,thec
5、ounterperminute(cpm)ofdialysatesinrightPAGofNT-loadednanoparticleswiththeBO/ME(BO/ME-NT-NP),radiolabeledwithsodium125I-Iodide,weremeasuredinagamma-counterforradioactivity.AfterconvertingcpmintocorrespondingconcentrationsofNTbyinvivorecoveryofmicrodialys
6、isprobes,thepharmacokineticparameterswerecalculated.ResultsThelocatedintheTomb,DongShenJiabang,deferthenextdayfocusedontheassassination.Linping,Zhejiang,1ofwhichliquorwinemasters(WuzhensaidinformationisCarpenter),whogotAfewbayonets,duetomissedfatal,when
7、nightcame7BO/ME-NT-NPcouldbeabsorbedintothebrain,muchbettertoNT-NPandthenanoparticleswithborneolormentholumonly,andthepharmacokineticsaccordedwiththetwo-compartmentmodel.Theparameterstmax,cmax,AUC,t1/2(β)were0.68h,27.32ng/mL,132.68ng·h/mL,3.1076h.Conclu
8、sionWithaddingBO/MEasabsorptionenhancer,NTcouldbesignificantlyincreasedinthebrainwiththehelpofnanopartilcesascarriers,andthetimetomaximalconcentrationwasshort,theeliminationprocesswasprolonged.KeyWords:bornel/mentholumeutecticmix
