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蚂蚁淘在线 / 品牌中心 / MCE / Medchemexpress/SBE-β-CD(Synonyms: Sulfobutylether-β-Cyclodextrin)/HY-17031/10g

Medchemexpress/SBE-β-CD(Synonyms: Sulfobutylether-β-Cyclodextrin)/HY-17031/10g

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￥1920.00

货号：HY-17031-1g

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商品描述

SBE-β-CDisasulfobutyletherβ-cyclodextrinderivative,itisanexcipientoraformulatingagentusedtoincreasethesolubilityofpoorlysolubledrugs.

Description	SBE-β-CDisasulfobutyletherβ-cyclodextrinderivative,itisanexcipientoraformulatingagentusedtoincreasethesolubilityofpoorlysolubledrugs.
InVitro	SBE-β-CDisachemicallymodifiedβ-CDthatisacyclichydrophilicoligosaccharidewhichisnegativelychargedinaqueousmedia.β-CDfunctionedisasolubilizeronlyatlowconcentrations,whereasSBE7-β-CDexhibitsstrongsolubilizingeffectsoverawideconcentrationrange^[1].
InVivo	SBE-β-CDisaderivatizedformofβ-cyclodextrinthathasbeendevelopedasasafeandeffectivesolubilizingagentfordrugsbeingadmiNISTeredbyparenteralandotherroutes(includingoral).SBE-β-CDisacycliccarbohydratecomprisedofsevenglucosemolecules;theresultingtruncatedcone-likestructurebeingfurtherderivatizedwithanaverageofsevensulfobutylethergroups^[2].ThecalorimetricdatafortheCompound1/SBE-β-CDcomplexindicatesanextremelystronginteraction,withanassociationconstantof2.3±(0.2)×10⁶M^-1at25°Cand1.6±(0.2)×10⁶M^-1at37°C^[3].SBE-β-CDaloneevokesamildcardio-depressanteffectindependentofcocainetreatment(p=0.0001comparedtobaseline)butattenuatesfurthercocaine-induceddecreasesinRPP,dP/dtmax,anddP/dtmax_absathighcocaineconcentrations.NosignificanteffectisseenonlinepressureSBE-β-CDalleviatesthemostpronouncedcardiacdepressionforRPP,dP/dtmax,anddP/dtmax_abs.ThisdifferentialeffectofSBE-β-CDatlowandhighconcentrationsproducesaninteractioneffectinthetwo-wayANOVAforRPP(p<0.0001), dp/dtmax="" (p="0.0001)," and="">_abs(p=0.0015),andpreventsanyoveralltreatmenteffect.InfusingSBE-β-CDalsoattenuatesthecardiacdepressionassociatedwithcocaethylenetoxicityforRPPanddP/dtmax.Nodifferencesareobservedbetweenethanol-treatedcontrolsandcocaethyleneplusSBE-β-CDgroups^[4].
References	[1].FukudaM,etal.Influenceofsulfobutyletherbeta-cyclodextrin(Captisol)onthedissolutionpropertiesofapoorlysolubledrugfromextrudatespreparedbyhot-meltextrusion.IntJPharm.2008Feb28;350(1-2):188-196. [2].LockwoodSF,etal.Improvedaqueoussolubilityofcrystallineastaxanthin(3,3"-dihydroxy-beta,beta-carotene-4,4"-dione)byCaptisol(sulfobutyletherbeta-cyclodextrin).JPharmSci.2003Apr;92(4):922-926. [3].CharmanSA,etal.Alterationoftheintravenouspharmacokineticsofasyntheticozonideantimalarialinthepresenceofamodifiedcyclodextrin.JPharmSci.2006Feb;95(2):256-67. [4].FettiplaceMR,etal.Cardiacdepressioninducedbycocaineorcocaethyleneisalleviatedbylipidemulsionmoreeffectivelythanbysulfobutylether-β-cyclodextrin.AcadEmergMed.2015May;22(5):508-17.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	0.6890mL	3.4452mL	6.8904mL
5mM	0.1378mL	0.6890mL	1.3781mL
10mM	0.0689mL	0.3445mL	0.6890mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

AnimalAdministration
^[3]

SBE-β-CDispreparedinsaline^[3].

Rat^[3]
A300gratisadministeredwith1mLofa0.1MSBE-β-CDsolutioncontaining5.64mgofCompound1,andassuminganextracellularvolumeof90mL,lessthan0.1%ofthecomplexwouldrapidlydissociateduetotheinitialeffectsofdilution.Thiscalculation,combinedwiththechangingbloodtoplasmaratiointhepresenceofSBE-β-CD,providesareasonableexplanationfortheobserveddifferencesinthebloodandplasmaprofilesofCompound1afterintravenousadministrationineitherthecyclodextrinorcyclodextrin-freeformulations.AfterIVadministrationofthecyclodextrinformulation,Compound1wouldinitiallybepreventedfromdistributingintoerythrocytestherebyresultinginawholebloodtoplasmaratiooflessthanone.Subsequently,clearanceofSBE-β-CDfromthecirculationwouldleadtochangesinthecomplexationequilibriumsuchthattheunboundfractionofCompound1wouldincrease,therebyreestablishingnormalbloodtoplasmapartitioning(i.e.infavourofwholeblood)andclearance.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].FukudaM,etal.Influenceofsulfobutyletherbeta-cyclodextrin(Captisol)onthedissolutionpropertiesofapoorlysolubledrugfromextrudatespreparedbyhot-meltextrusion.IntJPharm.2008Feb28;350(1-2):188-196.
[2].LockwoodSF,etal.Improvedaqueoussolubilityofcrystallineastaxanthin(3,3"-dihydroxy-beta,beta-carotene-4,4"-dione)byCaptisol(sulfobutyletherbeta-cyclodextrin).JPharmSci.2003Apr;92(4):922-926.
[3].CharmanSA,etal.Alterationoftheintravenouspharmacokineticsofasyntheticozonideantimalarialinthepresenceofamodifiedcyclodextrin.JPharmSci.2006Feb;95(2):256-67.
[4].FettiplaceMR,etal.Cardiacdepressioninducedbycocaineorcocaethyleneisalleviatedbylipidemulsionmoreeffectivelythanbysulfobutylether-β-cyclodextrin.AcadEmergMed.2015May;22(5):508-17.

MolecularWeight	1451.29
Formula	C₅₀H₈₄Na₂O₄₁S₂
CASNo.	182410-00-0
Storage	4°C,protectfromlight
Shipping	RoomtemperatureincontinentalUS;mayvaryelsewhere
Solvent&Solubility	H₂O:≥33mg/mL;DMSO:5.625mg/mL *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> Purity:>98.0% SelectBatch: