简介：Thepresentworkisaimedtostudythepharmacokineticparametersofoptimizedrepaglinidefloatingdrugdeliverysystem(FDDS)by24factorialdesigns,followedbycomparisonwithacommerciallyavailableformulation.Themaineffectsandinteractionsofformulationvariableswerestudiedbyusingnormalandparetocharts.Theoptimizedformulationshowsafickiandiffusiondrugreleasemechanism.Pharmacokineticparametersofthedesigneddrugdeliverysystemwereevaluatedinrabbitmodels.Meanwhileasimple,specifichighperformanceliquidchromatographicmethodwasdevelopedandvalidatedasperbiopharmaceuticalspecifications,thelinearitywasobservedattherangeof110-550ng/mL(r2=0.999).Byusingmethanol-phosphatebuffer(pH2.5)(70:30,v/v)asmobilephaseattheflowrateof1.0mL/minthevalidationshowsabetterretentiontimeof5.2minforrepaglinide.AndthesamevalidationmethodwasusedforpharmacokineticprofileanalysisofrepaglinidemarketedproductsandFDDS.Thecomparativepharmacokineticresultssuchastmax,half-life,areaunderthecurve,meanresidencetimeswereincreasedsignificantlyfortherepaglinideinFDDSthanthemarketedproductofrepaglinideexceptCmaxandeliminationrateconstant.

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简介：Differentsystemshavebeenusedovertheyearstodeliverdrugparticlestothehumanskinforpharmaceuticaleffect.Researchhasbeendonetoimprovetheperformanceandflexibilityofthesesystems.Inrecentyearsauniquesystemcalledthetransdermaldrugdeliveryhasbeendeveloped.Transdermaldrugdeliveryopenedanewdoorinthefieldofdrugdeliveryasitismoreflexibleandoffersbetterperformancethantheconventionalsystems.Theprincipleofthissystemistoacceleratedrugparticleswithahighspeedgasflow.Amongdifferenttransdermaldrugdeliverysystemswewillconcentrateonthecontourshocktubesysteminthispaper.Acontouredshocktubeisconsistsofarupturechamber,ashocktubeandasupersonicnozzlesection.Thedrugparticlesareretainedbetweenasetofburstingdiaphragm.Whenthediaphragmisrupturedatacertainpressure,ahighspeedunsteadyflowisinitiatedthroughtheshocktubewhichacceleratestheparticles.Computationalfluiddynamicsisusedtosimulateandanalyzetheflowfield.TheDPM(discretephasemethod)isusedtomodeltheparticleflow.AsanunsteadyflowisinitiatedthoughtheshocktubethedragcorrelationproposedbyIgraetalisusedotherthanthestandarddragcorrelation.Theparticlevelocitiesatdifferentsectionsincludingthenozzleexitareinvestigatedunderdifferentoperatingconditions.Staticpressurehistoriesindifferentsectionsintheshocktubeareinvestigatedtoanalyzetheflowfield.Theimportantaspectsofthegasandparticledynamicsintheshocktubearediscussedandanalyzedindetails.

简介：Severaldrug-resistantvariantshavebeendevelopedbygrowingtheparentalMELcellsinpresenceofcolchicine,adriamycinandvincristinerespectivelywithstepwiseincreasingconcentration.Boththecolchicine-resistantSc9(ColO)andvincristine-resis-tantSc9(VCR5)cellsdisplayedanacceleratedHMBA-inducedcommitmenttoterminalcelldifferentiation,whereastheadriamycin-resistantSC9(A120)showednoaccelerationbutratherasubstantialdelayinHMBA-induceddifferentiation.ThestudiesprovidemorecluesaswellasexperimentalmodelsforfurtherstudyonthemechanismofinduceddifferentiationofMELcells.

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简介：Naturalproducts(NPs)arecompoundsthatarederivedfromnaturalsourcessuchasplants,animals,andmicroisms.Therapeuticshasbenefitedfromnumerousdrugclassesderivedfromnaturalproductsources.TheBiopharmaceuticsDrugpositionClassificationSystem(BDDCS)wasproposedtoserveasabasisforpredictingtheimportanceoftransportersandenzymesindeterminingdrugbioavailabilityanddisposition.Itcategorizesdrugsintooneoffourbiopharmaceuticalclassesaccordingtotheirwatersolubilityandextentofmetabolism.Thepresentpaperreviews109drugsfromnaturalproductsources:29%belongtoclass1(highsolubility,extensivemetabolism),22%toclass2(lowsolubility,extensivemetabolism),40%toclass3(highsolubility,poormetabolism),and9%toclass4(lowsolubility,poormetabolism).HereinweevaluatedthecharacteristicsofNPsintermsofBDDCSclassforall109drugsaswellsasforsubsetsofNPsdrugsderivedfromplantsourcesasantibiotics.Inthe109NPsdrugs,wepiled32drugsfromplants,50%(16)oftotalinclass1,22%(7)inclass2and28%(9)inclass3,nonefoundinclass4;Meantime,theantibioticswerefound5(16%)inclass2,22(71%)inclass3,and4(13%)inclass4;nodrugwasfoundinclass1.Basedonthisclassification,weanticipateBDDCStoserveasausefuladjunctinevaluatingthepotentialcharacteristicsofnewnaturalproducts.

简介：目的：观察针药并用治疗非特异性急性腰扭伤的临床疗效。方法：将69例患者按就诊川页序随机分为针药并用组、针刺组和药物组。针刺组24例，采用针刺治疗，每日1次，共治疗5次；药物组20例，采用口服双氯芬酸钠治疗，50mg每次，每日2次，连服5日；针药并用纽25例采用与针刺组、药物组相同的针刺和药物治疗。以疼痛量表和下腰痛量表评价临床疗效。结果：三组患者治疗后在疼痛，活动度方面均有一定改善，但针药并用组疗效最佳，与针刺组、药物组比较，差异有统计学意义（P〈0．01）；针刺组与药物组比较，差异无统计学意义。结论：针药并用治疗急性腰扭伤疗效优于单纯针刺治疗或常规剂量双氯芬酸钠治疗。

简介：Glioblastoma(GBM)isoneofthemostlethalhumancancers.GenomicanalysesdefinethemoleculararchitectureofGBMandhighlightacentralfunctionformechanistictargetofrapamycin(mTOR)signaling.mTORkinaseexistsintwomultiproteincomplexes,namely,mTORC1andmTORC2.Thesecomplexesdifferintermsoffunction,regulationandrapamycinsensitivity.mTORC1iswellestablishedasacancerdrugtarget,whereasthefunctionsofmTORC2incancer,includingGBM,remainspoorlyunderstood.ThisstudyreviewstherecentfindingsthatdemonstrateacentralfunctionofmTORC2inregulatingtumorgrowth,metabolicreprogramming,andtargetedtherapyresistanceinGBM,whichmakesmTORC2asacriticalGBMdrugtarget.

简介：Thepaperdescribesdrugreleaseevaluationofabiodegradablelong-actingcon-traceptiveCapsule(CaproF)containinglevonorgestrel(LNG)invivo.Poly(E-Capro-lactone)(PCL)biodegradablematerial,suitableformanymedicalapplication,wasusedinthisstudy.Itwasextrudedintotubes.ThetubeswerethencutandloadedwithLNGpowderbeforemelting-sealedonbothendstogetdrugcapsules.Thissub-dernalimplanthasbeenfoundtobehighlyeffectiveinanimalexperiments.Twoad-

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简介：Wepresentherethedevelopmentofcholesterol(Chol)-modifieddendrimersystemfortargetedchemotherapyoffolate(FA)receptor-expressingcancercells.Inourstudy,poly(amidoamine)(PAMAM)dendrimersofgeneration5(G5)werefunctionalizedstepby-stepwithChol,fluoresceinisothiocyanate(FI),andFAviaapoly(ethyleneglycol)(PEG)spacer(PEG-FA),andthenacetamidetoshieldtheirremainingsurfaceamines.ThesynthesizedG5.NHAc-Chol-FI-PEG-FA(forshort,G5-CFPF)dendrimerswereutilizedtoencapsulate10-hydroxycamptothecin(HCP),ahydrophobicanticancerdrug.WefindthateachG5-CFPFdendrimercanencapsulate13.8HCPmolecules.ThecomplexesshowaslowerreleaseprofilesofHCPinapH-dependentmannerthanthecontrolcomplexesformedusingthesamedendrimerswithoutCholunderthesameconditions.ThankstothetargetingroleplayedbyFA,thecomplexesdisplayaspecificinhibitionefficacytoFAreceptor-expressingcervicalcancercells.ThedesignedChol-modifieddendrimersmaybeadoptedasapromisingcarrierforapplicationintargetedcancertherapy.

简介：Thepresentworkshowsdrug-carrierinteractions,releasebehaviorsandcellresponsesofhydroxyapatite(HA)containingsalvianolicacidB(SalB),astragaluspolysaccharide(APS),andnaringin.X-raydiffraction(XRD)showedthatthecrystallinityandcrystalsizeofHAdecreasedsignificantlywhenSalBwasadded(p<0.05).Transmissionelectronmicroscope(TEM)confirmedthatthenano-acicularcrystalsofHAcontainingSalBwerethemostfineamongallspecimens.ItwasconjecturedthatSalBpreferentiallyadsorbedonthepositivelychargedsurfaceofHAcrystalstoinhibittheirgrowth.InvitroreleaseofHAcontainingChinesemedicinesfollowedthefirst-orderequation.Thedrug-carrieraffinitybetweenHAandSalBmighthaveprolongedthereleaseofSalB.TheproliferationanddifferentiationofosteoblastswerepromotedbyChinesemedicinescontainingHAinthetimeanddosagedependentmanner.Theosteoblastsdisplayedapolygonalmorphologywithcell-celljunctionsinallcases.ItissuggestedthatthecontainedChinesemedicineswouldpromotetheactivitiesoftheosteoblasts.

简介：Weinvestigatedthepharmacokineticsofcaroverineintheperilymph,cerebrospinalfluidandplasmaaftersystemicandlocaladministrationsinguineapigsbyusinghigh-performanceliquidchromatography.Auditorybrainstemresponsesweremeasuredtoevaluateauditoryfunctionaleffect.Theresultsshowedthatlocalapplicationwasabothsafeandefficientmethod.Wefurtherreviewedliteratureandpinpointedthattheroundwindowiseffectivelylocaldrugdeliverymeansforfutureinnereartreatment.

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简介：Bothenantiomersofdenopamineweresynthesizedusingmicrobial-chemicalapproachviabioreductionof1-(acetoxyphenyl)ketone4(R=CH2C1)and5(R=CO2Et)withfungusGeotrichumsp.G38.

简介：Inthefightagainstcancer,controlleddrugdeliverysystemshaveemergedtoenhancethetherapeuticefficacyandsafetyofanti-cancerdrugs.Amongthesesystems,mesoporoussilicananoparticles(MSNs)withafunctionalsurfacepossessobviousadvantagesandwerethusrapidlydevelopedforcancertreatment.Manystimuli-responsivematerials,suchasnanoparticles,polymers,andinorganicmaterials,havebeenappliedascapsandgatekeeperstocontroldrugreleasefromMSNs.ThisreviewpresentsanoverviewoftherecentprogressintheproductionofpH-responsiveMSNsbasedonthepHgradientbetweennormaltissuesandthetumormicroenvironment.Fourmaincategoriesofgatekeeperscanrespondtoacidicconditions.Thesecategorieswillbedescribedindetail.

简介：背景：训练的整个身体颤动(WBV)出现到豆子为在更老的个人训练的常规抵抗的有效选择。到目前为止，没有数据在心和肺的健康上关于振动效果存在。目的：这随机的ised控制了估计的试用在超过60岁的社区住所成年人在心和肺的健康和肌肉力量上训练的1年的WBV的效果。方法：220个成年人的一个总数(意味着年龄67.1年)随机被分到一个WBV组，健康组或控制组。在一个颤动平台上行使的TheWBV组，和健康组表演了心血管，抵抗，平衡和拉长的锻练。控制组没参予任何训练。心率在一个单个WBV会议期间被测量。山峰氧举起(VO2peak)和time-to-peak锻练(TPE)在进步自行车ergometry期间被测量。肌肉力量被一个测力计估计。结果：心率在WBV训练期间显著地增加了。在1年以后，VO2peak,TPE和肌肉力量在WBV和健康组显著地增加了。两个都训练的组在VO2peak和肌肉力量同样改善了。健康组比WBV组在TPE更显著地改善了。结论：WBV在社区住所训练老看起来有效改进心和肺的健康和肌肉力量。

简介：OpticalmethodsandMTTmethodareusedtocharacterizetheantiproliferationeffectofantitumordrug9-aminoacridine(9AA)withandwithoutsilvernanoparticles.IntracellularsurfaceenhancedRamanscattering(SERS)spectraandfluorescentspectraof9AAindicatetheformof9AAadsorbedonthesurfaceofsilvernanoparticles.AlthoughbothsilvernanoparticlesandantitumordrugcaninhibitthegrowthofHelacells,silvernanoparticlescanslowdowntheantiproliferationeffectonHelacellsatlowconcentrationofantitumordrugs.Ourexperimentalresultssuggestthatsilvernanoparticlesmayserveasslow-releasedrugcarriers,whichisimportantinantitumordrugdelivery.

简介：Objective:Toinvestigatetheeffectoftwoantisenseoligonucleotidesoncellsurviving,bcl-2expressionandapoptosisofleukemiacells.Methods:Theexperimentalassayswereperformedwithcellculture,immunochemistryandflowcytometry.Results:Thetwoantisenseoligodeoxynucleotides,combinedwithVp16orAra-corDNR,wereabletodeclinethesurvivalrateofmyeleukemiccells,downregulatebcl-2geneexpressionandinduceapoptosisofleukemiccellssignificantly,ascomparedwithVp16orAra-corDNRalone.Conclusion:Itispossibleforthetwonewbcl-2antisensestobedevelopedintoclinicaltrialsforleukemiaandtumorwithbcl-2geneoverexpression.