简介：研究观察年龄对潘库溴铵药代动力学的影响。选择２４例施择期整形外科手术的患者，根据年龄分成三组：１组为５例婴幼儿，年龄０．７５～２．９５岁；２组为１３例儿童，年龄４～１４岁；３组为６例成人，年龄１６～２７岁。静注潘库溴铵１００μｇ／ｋｇ后用改良荧光法测定其血浓度。潘库溴铵的体内过程能用二室开放模型完整描述，年龄愈小，分布容积愈大，血浆清除率愈高，潘库溴铵的血药浓度愈低。Ｖ１（中央室分布容积）、Ｖ２（周边室分布容积）、Ｖｄｓｓ（稳态分布容积）、Ｃｌ（血浆清除率）和ＡＵＣ（曲线下面积）在三组间有明显差别。１组的Ｔ１／２β和ＭＲＴ明显比２、３组长，但Ｔ１／２α和Ｋ２１在三组间无明显差别。

简介：High-performanceliquidchromatographic(HPLC)analysisoffluorouracil(5-FU)contentofthebloodandcolonofrabbitsisdescribed.Therewasnomarkeddifferenceintheplasma5-FUlevelandbloodconcentrationtimecurvefollowingintravenous(I.V.)(earvein)orintraarterial(I.A.)(inferiormesentericartery)injectionof5-FU15mg/kg.However,thedistributionof5-FUinthecolonafterIA.administrationwasquitedifferentthatafterI.V.administration.At10,20and30minutes,the5-FUcontentinthecolonwasshowntobe31-,17-and14-foldhigherwithI.A.thanwithI.V..ColonictissueAUCo-480min.was2453and690min/mg/mlrespectively(p<0.05).Itissuggestedthattoinject5-FUintoselectedarteriestotreatadvancedcolorectalcancermaybemoreusefulthanI.V.administration.

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简介：健康志愿者１０名，随机交叉口服硫酸吗啡控释片（ＣＲＭＳ）３０ｍｇ（３０ｍｇ×１）和硫酸吗啡普通片（ＩＲＭＳ）２０ｍｇ（１０ｍｇ×２），分别于服药前后各时点取静脉血，用ＧＣＭＳ测定血浆中吗啡含量。以药代软件程序处理，分别求得ＣＲＭＳ和ＩＲＭＳ的Ｃｍａｘ为１９．３８±３．８０和２１．２７±６．２１ｎｇ／ｍｌ；ｔｍａｘ为２．３６±０．３７ｈ和０．５５±０．１６ｈ；ｔ１／２β为３．５３±０．８７ｈ和３．０３±０．７４ｈ，曲线下面积ＡＵＣ为１４５．１５±１７．６５和９３．０８±１６．６５ｎｇ·ｈ／ｍｌ。癌症病人多次口服硫酸吗啡至稳态，ＣＲＭＳ和ＩＲＭＳ的峰浓度分别为２７．４３±０．３３ｎｇ／ｍｌ，２２．６８±０．１６ｎｇ／ｍｌ；谷浓度分别为１９．４５±１．４４ｎｇ／ｍｌ；１８．１４±０．４９ｎｇ／ｍｌ。

简介：ThisstudydevelopedapopulationpharmacokineticmodelforsodiumtanshinoneIIAsulfonate(STS)inhealthyvolunteersandcoronaryheartdisease(CHD)patientsinordertoidentifysignificantcovariatesforthepharmacokineticsofSTS.Bloodsampleswereobtainedbyintensesamplingapproachfrom10healthyvolunteersandsparsesamplingfrom25CHDpatients,andapopulationpharmacokineticanalysiswasperformedbynonlinearmixed-effectmodeling.Thefinalmodelwasevaluatedbybootstrapandvisualpredictivecheck.Atotalof230plasmaconcentrationswereincluded,137fromhealthyvolunteersand93fromCHDpatients.Itwasatwo-compartmentmodelwithfirst-orderelimination.Thetypicalvalueoftheapparentclearance(CL)ofSTSinCHDpatientswithtotalbilirubin(TBIL)levelof10μmol(L?1was48.7L(h?1withinterindividualvariabilityof27.4%,whereasthatinhealthyvolunteerswiththesameTBILlevelwas63.1L(h?1.Residualvariabilitywasdescribedbyaproportionalerrormodelandestimatedat5.2%.TheCLofSTSinCHDpatientswaslowerthanthatinhealthyvolunteersanddecreasedwhenTBILlevelsincreased.Thebootstrapandvisualpredictivecheckconfirmedthestabilityandvalidityofthefinalmodel.TheseresultssuggestedthatSTSdosageadjustmentmightbeconsideredbasedonTBILlevelsinCHDpatients.

简介：Ginkgoditerpenelactonesmeglumineinjection(GDLI)isacommerciallyavailableproductusedforneuroprotection.However,thepharmacokineticpropertiesoftheprototypesandhydrolyzedcarboxylicformsoftheprimarycomponentsinGDLI,i.e.,ginkgolideA(GA),ginkgolideB(GB),andginkgolideK(GK),haveneverbeenfullyevaluatedinbeagledogs.Inthiswork,asimple,sensitive,andreliablemethodbasedonultra-fastliquidchromatography-tandemmassspectrometry(UFLC-MS/MS)wasdeveloped,andtheprototypesandtotalamountsofGA,GB,andGKweredeterminedinbeagledogplasma.Theplasmaconcentrationsofthehydrolyzedcarboxylicformswerecalculatedbysubtractingtheprototypeconcentrationsfromthetotallactoneconcentrations.Forthefirsttime,thepharmacokineticsofGA,GB,andGKwerefullyassessedinthreeforms,i.e.,theprototypes,thehydrolyzedcarboxylicforms,andthetotalamounts,afterintravenousadministrationofGDLIinbeagledogs.Itwasshownthatginkgolidesprimarilyexistedinthehydrolyzedforminplasma,andtheratioofhydrolysatestoprototypeformsofGAandGBdecreasedgraduallytoahomeostaticratio.AllofthethreeformsofthethreeginkgolidesshowedlinearexposureofAUCtothedosages.GA,GB,andGKshowedaconstanthalf-lifeapproximately2.7,3.4,and1.2h,respectively,whichwereconsistentfortheformsatthreedoselevels(0.3,1.0,and3.0mg·kg~(-1))andafteraconsecutiveinjectionofGDLIfor7days(1.0mg·kg~(-1)).

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