简介:由乙酰苯胺经Vilsmeier反应步骤制备对甲酰基乙酰苯胺时,以86%收率意外得到N,N-二甲氨基甲基苯亚胺.产物结构经MS,IR1HNMR,13CNMR光谱及其盐酸盐和硫酸盐的C、H、N、元素分析给以确正.此法为N,N-二甲基脒类化合物提供了新的合成途径.
简介:Although5-fluorouracilisoneofthemostwidelyusedcytotoxicdrugsinthetreatmentofsolidtumorsinmanyorgans,ithasaseveredrawbackinitsseriousside-effects(e.g.gastrointestinalandbonemarrowtoxicity)andtheproperties(e.g.lowlipophilicity)leadingtovariousdeliveryproblems.Thelowlipophilicityof5-fluorouracilmaybeapredominantfactorforitspoorbiomembranepermeability.
简介:Aim:Tostudypercutaneousabsorptionandmetabolismofketoprofenisopropylester(KPE)viaexcisednudemouse'sandmonkey'sskin.Methods:Excisedskinwaspreparedbysurgicalexcisionandenzymedigestion.Sideby-sidediffusioncellswereusedforinvitropermeationstudies.TheconcentrationsofKPEanditsmetaboliteinsampleswereassayedbyHPLC.Results:AllKPEpenetrationthroughwholethicknessskinandstrippedskinwasmetabolizedtoketoprofen(KP).theconcentrationofwhichinthereciiversolutionincreasedlinearlywithtime.Astothenudemouseskin.thesteady-statefluxofKPthroughwholethicknessskinwas2.5timesthatofKPEthroughthewhloethicknessskin,buttheKPandKPEremaininginthewholethicknessskinafterthefinishingofKPEpenetrationwas22.2timesincomperedwiththeKPremaininginthewholethicknessskinafterthefinshingofKPpenetration.TherateofformationofthesteadystateKPfromKPEthroughtdermiswassignificantlylowerthanthatofKPEthroughthewholethicknessskin.Inhemonkeyskin,therateofformationofthesteady-stateKPfromKPEthroughthewholethicknessskinwas0.7timesthatfromKPEthroughstrippedskin.TheKPandKPEremaininginthewholethicknessskinafterthefinishingofKPEpenetrationwas2.0timethatinthestrippedskinafterthefinishingofKPEpenetration.Therateoffornationofthesteady-stateKPfromKPEthroughdermiswaslowerthanthatfromKPEthroughthewholethicknessskinandthestrippedskin.theKPremainingindermisafterthefinsihingofKPEpenetrationwasalsosignificantlylowerthantheKPremaininginthewholethicknessskinandthestrippedskinafterthefinishingofKPEpenetration.Conclusion:KPestersareofbenefittoimporovethelocalactionofKP.andskinesterasemetabolismmainlydevelopsintheepidermis.
简介:在褪黑激素的结构修饰中引入L-氨基酸形成N-(N-乙酰基-L-氨基酰基)-5-甲氧基色胺,这些化合物分别用小鼠甩尾法和人皮肤黑色素瘤细胞评价了镇痛活性和抗肿瘤活性,结果显示部分化合物的活性优于褪黑激素。
简介:1990年,彼得·圣吉的《第五项修炼——学习型组织的艺术与实务》以其对学习型组织诱人而美好状态的描述及到达途径的详尽阐释,使得“学习型组织”这一概念迅速在全世界受到追捧。时至今日,“学习型组织”依然是所有类型企业共同的梦想。药品零售连锁企业因其专业而特殊的特质,从诞生之日起就打下了“终生学习”的烙印,无论市场环境怎样变幻,无论企业发展到哪一个阶段,无论是着重于人的发展还是企业业绩的提升,培训是贯穿连锁药店企业成长始终的旋律。正如老百姓大药房执行总裁石展所说,培训不只是专业知识.服务技能的训练,而是关涉到企业文化的宣传和认知。企业采用什么样的培训理念.培训体系,与企业文化以及企业的价值观密不可分。
简介:目的建立实时监测尼莫地平片溶出过程的方法,初步评价制剂质量。方法用光纤溶出度实时测定仪监测尼莫地平片的溶出过程。结果考察1个厂家10批产品的溶出曲线,结果显示样品批间差异和批内差异均很大,说明该厂家生产工艺不稳定。结论光纤溶出度实时测定仪能够有效测定固体药物的体外溶出过程,可为监控制剂稳定性、改进制剂工艺提供有益的参考。
简介:目的探讨乙型肝炎病毒pre—S1Ag、pre—S2Ag、HBV—DNA、HBV—M的相关性及其临床意义。方法HBV—DNA采用荧光定量PCR法;HBV—M及pre—S1Ag、pre—S2Ag采用ELISA法,检测96例HBV—DNA阳性感染者血清中pre-S1Ag、pre—S2Ag、HBV—M,同时以30例HBV—M全阴性的健康体检者血清作为对照,并对结果进行统计学分析。结果96例HBV—DNA阳性患者中HBsAg、HBeAg、HBcAb阳性检出率为64.6%;HBsAg、HBeAb、HBcAb阳性检出率为20.8%;HBsAg、HBcAb阳性栓出率为14.6%;pre—S1Ag在96例HBV—DNA阳性标本中检出率为70.8%;pre—S2Ag检出率为79.2%;均明显高于HBeAg的阳性率64.6%,30例对照中未检测出pre—S1Ag、pre—S2Ag及HBV—DNA。结论HBeAg、HBV—DNA、pre—S1Ag、pre—S2Ag之间具有一定的关联性。pre—S1Ag和pre—S2Ag均较HBeAg敏感。pre—S1Ag与pre—S2Ag的栓出率差异无显著性,ELISA检测HBV—M、pre—S2Ag及pre—S1Ag只是表型指标,只能提供HBV感染的间接证据。而HBV—DNA的检测是HBV感染与否的直接证据。HBV—M、pre—S1Ag、pre—S2Ag、HBV—DNA的检测各自有其独特的临床意义。应用pre—S1Ag、pre—S2Ag、HBV—DNA及HBV—M进行联合检测,对HBV感染的早期诊断,了解HBV复制、转归及监测疗效和预后有重要的意义。
简介:Pyrimidinederivativeshavebeenreportedasneuroprotectiveagentsusefulforthetreatmentofvariousneurodegenerativedisorders.Inthepresentstudy,severalpyrimidineanalogueshavebeenevaluatedasneuroprotectiveagentsinMorriswatermazemodel.Itwasobservedthatpyrimidinederivatives8–17considerablyimprovelearning,memory,andmovementdeficitsinanimalmodels.Biochemicalestimationsofbrainserumoftreatedanimalsrevealedsuppressionofoxidativeandnitrosativestress,acetylcholinesteraseactivity,andotherparameterswhichleadstoneurodegenerationofbrain.Ofallthepyrimidinederivatives,thiomorpholinederivative8andpiperazineethanolderivative17werefoundtobethemostactiveneuroprotectiveagentsandproducedeffectscomparabletostandarddrugrivastigmineintermsofbehavioral,biochemical,andmolecularaspects.