Octreotide(acetate)isalong-actingoctapeptideandsomatostatinanalogwithpharmacologicactionsmimickingthoseofthenaturalhormonesomatostatin.

Octreotide-treatedgroupsshowasignificantreductioninthetumorvolumewhencomparedwithsalinegroup.Octreotide-PPSG(1.4mg/kg,i.p.)showsgreaterantitumoreffectthanOctreotide-soln(100μg/kg,i.p.).Octreotide-treatmentsresultsinsignificantinhibitoryeffectontheexpressionlevelsofSSTR2andSSTR5inprimaryHCC-bearingratscomparedwiththesalinegroup.Octreotide-PPSGappearstoinhibittheexpressionofSSTR2andSSTR5toagreaterextentthanthatofOctreotide-solntreatedgroup^[1].Atestdoseofoctreotideacetatesignificantlydecreasestheserumgastrinleveltoapproximatelyonethirdofthebaselinein2hrandtheeffectlastedapproximatelyfor6hr.Onday21,treatmentwithsustained-releaseformulationofoctreotideacetatea(5mgintramuscular,q4wk)isinitiated^[2].

• [1].WangM,etal.Pharmacokineticandpharmacodynamicstudyofaphospholipid-basedphaseseparationgelforonceamonthadmiNISTrationofoctreotide.JControlRelease.2016May28;230:45-56.

  [2].KimS,etal.TreatmentofGastrin-SecretingTumorWithSustained-ReleaseOctreotideAcetateinaDog.JAmAnimHospAssoc.2015Nov-Dec;51(6):407-12.

Octreotide(acetate)isformulatedinsaline.

Mice^[1]
ThirtymicewithHCCxenograftsarerandomLydividedintothreegroups:(A)Octreotide-solngroup,(B)Octreotide-PPSGgroup,and(C)controlgroup.Octreotide-solngroupreceivesi.p.injectionof100μg/kgoctreotide-solnonceadayandtotallyforconsecutive14days.Octreotide-PPSGgroupreceivesasinglesubcutaneousinjectionof1.4mg/kgOctreotide-PPSG,andtheinjectionvolumeisabout0.2mL.Controlgroupreceivesi.p.injectionofsalineonceadayforconsecutive14days.TreatmentstartsonthenextdayafterinjectionofH22hepatomacellsUSPensionandmaintainsfor14days.Tumorgrowthismonitoredbyperiodiccalipermeasurementsonday7andday14postseeding.Tumorvolumes(V)arecalculatedbasedonthelengthandwidthoftumorbyEq.
Rat^[1]
TwelvemaleSDratsaredividedintotwogroups,andhousedinstandardcagesat25°C,withfreeaccesstofoodandwaterforaweekpriortotheexperiment.RatsaresubcutaneouslyinjectedwithOctreotidereotidesolution(Octreotide-soln)orOctreotide-PPSGatanequivalentsingledoseof20 mg/kg.ThedoseisdeterminedbasedontheclinicaldoseofOctreotide-solninhuman.Ratsarefastedfor12 hbeforedosingandfoodisreturnedapproximately2 hpostdosing.BloodsamplesarecollectedatpredeterminedtimepointsusingheparinizedEppendorftubes.Immediatelyaftercollection,thebloodsamplesareplacedoniceuntilcentrifugedat3000 g for10 minwithin1 h.Theplasmaiscollectedandstoredat−20°Cuntilanalysis.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].WangM,etal.Pharmacokineticandpharmacodynamicstudyofaphospholipid-basedphaseseparationgelforonceamonthadministrationofoctreotide.JControlRelease.2016May28;230:45-56.

  [2].KimS,etal.TreatmentofGastrin-SecretingTumorWithSustained-ReleaseOctreotideAcetateinaDog.JAmAnimHospAssoc.2015Nov-Dec;51(6):407-12.

1079.29

C₅₁H₇₀N₁₀O₁₂S₂

79517-01-4

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥29mg/mL

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

Purity:99.78%

SelectBatch:HY-17365-19289HY-17365-21293HY-17365-23972

DataSheet(124KB)SDS(120KB)

COA(99KB)HNMR(204KB)LCMS(219KB)

HandlingInstructions(1252KB)

• [1].WangM,etal.Pharmacokineticandpharmacodynamicstudyofaphospholipid-basedphaseseparationgelforonceamonthadministrationofoctreotide.JControlRelease.2016May28;230:45-56.

  [2].KimS,etal.TreatmentofGastrin-SecretingTumorWithSustained-ReleaseOctreotideAcetateinaDog.JAmAnimHospAssoc.2015Nov-Dec;51(6):407-12.

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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