SBE-β-CDisasulfobutyletherβ-cyclodextrinderivative,itisanexcipientoraformulatingagentusedtoincreasethesolubilityofpoorlysolubledrugs.

SBE-β-CDisachemicallymodifiedβ-CDthatisacyclichydrophilicoligosaccharidewhichisnegativelychargedinaqueousmedia.β-CDfunctionedisasolubilizeronlyatlowconcentrations,whereasSBE7-β-CDexhibitsstrongsolubilizingeffectsoverawideconcentrationrange^[1].

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].

• [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.

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.

• [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.

1451.29

C₅₀H₈₄Na₂O₄₁S₂

182410-00-0

4°C,protectfromlight

RoomtemperatureincontinentalUS;mayvaryelsewhere

H₂O:≥33mg/mL;DMSO:5.625mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:>98.0%

SelectBatch:HY-17031-22981HY-17031-22970HY-17031-26609HY-17031-24580HY-17031-20021

DataSheet(130KB)SDS(389KB)

COA(102KB)

HandlingInstructions(1252KB)

• [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.

品牌介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-Tropanylindole-3-carboxylate;lαH，5Αh-Tropan-3α-ylindole-3-carboxylate中文名称:托烷司琼中文同义词:托普西隆;托普西龙;曲匹西龙;托烷司琼;Β-托烷司琼;CS-348;Β-内托烷司琼;吲哚-3-甲酰氯;Β-托烷司琼(光学异构体);Β-托烷司琼,托烷司琼异构体CBNumber:CB3236404分子式:C17H20N2O2分子量:284.35MOLFile:89565-68-4.mol化学性质安全信息用途供应商112化学性质安全信息用途供应商112托烷司琼化学性质熔点:201-202°C沸点:448.5±35.0°C(Predicted)密度:1.26储存条件:2-8°C溶解度:H2O:soluble形态:solid酸度系数(pKa):15.38±0.30(Predicted)颜色:whiteCAS数据库:Chemicalbook89565-68-4(CASDataBaseReference)安全信息WGKGermany:3托烷司琼化学药品说明书托烷司琼|药物应用信息托烷司琼性质、用途与生产工艺临床评价Sorbe等报道本品对含顺铂(剂量50～89mg/m2)化疗方案引起的急性呕吐完全控制率为63%。58例恶性肿瘤化疗所致恶心、呕吐者，应用托烷司琼或昂丹司琼8mg分别在同一病人前后2个化疗周期的第1d给药前30min静脉注射，并用地塞米松10mg静脉滴注。结果两药控制急性及迟发性恶心、呕吐的疗效基本相似，均可达81%～100%。本品对强致吐化疗药物顺铂的止吐疗效突出。药物相关作用饮食可略为延长本品的吸收。本品与利福平、苯巴比妥等肝酶诱导药同时使用，可加快代谢，故快代谢型者需增加剂量，慢者则不必。西咪替丁等肝酶抑制药对本品血药浓度无明显影响。适应症托烷司琼临床用于预防和治疗癌症化疗引起的恶心和呕吐。化学性质结晶，熔点201-202℃(二氯甲烷-乙酸乙酯)。单盐酸托烷司琼(TropisetronMonohydroehloride)：C17H20N2O2?HCI。[105826-92-4]。熔点283-285℃(分解)。用途有高效性和选择性的5-HT3受体拮抗剂。用于化疗所致的呕吐。用途为5-羟色胺拮抗药生产方法托品醇(I)和酰氯(Ⅱ)反应，可得托烷司琼。托烷司琼上下游产品信息上游原料托品醇下游产品

公司介绍

托烷司琼临床评价药物相关作用适应症托烷司琼CAS号:89565-68-4英文名称:Tropisetron英文同义词:icf205-930;TROPICACID;TROPISETRON;SS-TROPISETRON;BETA-TROPISETRON;Tropisetron(ICS205930);TROPISHTRONHYDROCHLORIDE;Indole-3-carbonylchloride;3-

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类固醇 生物碱 糖类和糖苷类 染料试剂 生化分析试剂

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