版权说明：本文档由用户提供并上传，收益归属内容提供方，若内容存在侵权，请进行举报或认领
文档简介
提纲什么是晶体，多晶型？多晶型研究对药物开发的重要性如何筛选和选择药物的新晶型多晶型的主要分析手段晶型筛选实验的经验分享----溶剂选择2022/12/30提纲什么是晶体，多晶型？2022/12/291Crystal
Asolidmaterialwhoseconstituentatoms,molecules,orionsarearrangedinanorderlyrepeatingpatternextendinginallthreespatialdimensions.PharmaceuticalcrystalsMostdrugsaredevelopedascrystallineStabilityProcessabilityIPprotection什么是晶体？2022/12/30Crystal什么是晶体？2022/12/292什么是多晶型？Polymorphismistheabilityofasolidmaterialtoexistinmorethanoneformorcrystalstructure.PolymorphsSoldphaseSamechemicalcompositionDifferentmoleculararrangementsInpractice,weareinterestedinallthecrystallineandamorphousphasesforachemical/pharmaceutical2022/12/30什么是多晶型？Polymorphismistheab32022/12/302022/12/294多晶型研究对药物开发的重要性2022/12/302022/12/295药物多晶型研究的重要性2022/12/30药物多晶型研究的重要性2022/12/2962022/12/302022/12/2972022/12/302022/12/298如何筛选和选择药物的新晶型如何筛选和选择药物的新晶型92022/12/302022/12/29102022/12/302022/12/2911晶型的化学和物理分析手段2022/12/30晶型的化学和物理分析手段2022/12/29122022/12/302022/12/29132022/12/302022/12/2914Experiencesharingonpolymorphscreening——solventselection2022/12/30Experiencesharingonpolymorp15ThepurposeofpolymorphscreeningForInnovatorcompanies-selecttheoptimalsolid-stateofAPIfordevelopment-studyrelevantpolymorphsforIPprotectionForCROcompaniesbasedonthecustomersneeds-toidentifyasmanynewpolymorphs(includesolvate/hydrate)andamorphousformaspossible-ortofindthemoststableform
2022/12/30Thepurposeofpolymorphscree16Themethodofpolymorphscreeningcrystallizationcrystallizationfromsolution(slurry,anti-solventprecipitation,Solvent-thermalheating/coolingSlow/fastprecipitationfromsaturatedsolutions)recrystallizationfromaneatcompound(thermalheating/cooling,grinding,andhighpressure)2022/12/30Themethodofpolymorphscreen17polymorphscreening——
crystallizationfromsolutiondegreeofsupersaturationandTemperatureareconsideredasthedrivingforceofcrystallisationdiversesolventsresultinthediscoveryofmorepolymorphs2022/12/30polymorphscreening——
18crystallizationfromsolution——SolventselectionSlurryAnti-solventprecipitationSolvent-thermalheating/coolingexperimentsSlow/fastprecipitationfromsaturatedsolutionsmethodSolventVisualsolubility(mg/mL)MeOH
EtOH
IPA
1-Butanol
ACN
MEK
MIBK
EtOAc
iPrOAc
MTBE
2-MeTHF
DMF
NMP
DMSO
CH2Cl2
Toluene
1,4-Dioxane
Heptane
THF
Acetone
Water
2022/12/30crystallizationfromsolution19crystallizationfromsolution——
rationalexperimentaldesignLimitedresource
Howtofindasmanynewpolymorphsand
amorphousformaspossibleAPIpropertiesdifferentsolubilityinthesolvent
poorsolubilityorgoodsolubilitySolventproperties
Polarity-differentsortofsolvents(alcohols,ethers,esteretc.)BoilingpointFreezingpointToxicitymiscibility？2022/12/30crystallizationfromsolution20Slurry——solventselectionMakesurethesampleissuspension
solvent/mixedsolventssolubilityispoor2022/12/30Slurry——solv21Anti-solventprecipitation
—solventselectionPreparesolventgoodsolubilityAnti-solventselectionPoorsolubilitypolaritymiscibility
miscibilityWaterDMFHeptaneACN1,4-DioxaneMTBEDMSO2022/12/30Anti-solventprecipitation
22Solvent-thermal
heating/coolingexperimentschangetemperaturesupersaturation
goodsolubilitySolventselectionsolubilityvarieswiththetemperature
freezingpointofthesolvent2022/12/30Solvent-thermal
heating/cool23Slow/fastprecipitationfromsaturatedsolutionsmethodEvaporatethesolventsupersaturationSlow/fastrateofcrystallization
SolventselectionlowboilingpointsolventboilingpointDMF152.8ºCDMSO189ºCNMP202ºC2022/12/30Slow/fastprecipitationfroms24Summary—Solventselectionkeypointofthemethodselectappropriatesolventdifferentsolubilityinthesolventsolventpropertiesmiscibilitybetweensolvents
PolarityboilingpointfreezingpointToxicity2022/12/30Summary—Solventselectionkeyp25提纲什么是晶体，多晶型？多晶型研究对药物开发的重要性如何筛选和选择药物的新晶型多晶型的主要分析手段晶型筛选实验的经验分享----溶剂选择2022/12/30提纲什么是晶体，多晶型？2022/12/2926Crystal
Asolidmaterialwhoseconstituentatoms,molecules,orionsarearrangedinanorderlyrepeatingpatternextendinginallthreespatialdimensions.PharmaceuticalcrystalsMostdrugsaredevelopedascrystallineStabilityProcessabilityIPprotection什么是晶体？2022/12/30Crystal什么是晶体？2022/12/2927什么是多晶型？Polymorphismistheabilityofasolidmaterialtoexistinmorethanoneformorcrystalstructure.PolymorphsSoldphaseSamechemicalcompositionDifferentmoleculararrangementsInpractice,weareinterestedinallthecrystallineandamorphousphasesforachemical/pharmaceutical2022/12/30什么是多晶型？Polymorphismistheab282022/12/302022/12/2929多晶型研究对药物开发的重要性2022/12/302022/12/2930药物多晶型研究的重要性2022/12/30药物多晶型研究的重要性2022/12/29312022/12/302022/12/29322022/12/302022/12/2933如何筛选和选择药物的新晶型如何筛选和选择药物的新晶型342022/12/302022/12/29352022/12/302022/12/2936晶型的化学和物理分析手段2022/12/30晶型的化学和物理分析手段2022/12/29372022/12/302022/12/29382022/12/302022/12/2939Experiencesharingonpolymorphscreening——solventselection2022/12/30Experiencesharingonpolymorp40ThepurposeofpolymorphscreeningForInnovatorcompanies-selecttheoptimalsolid-stateofAPIfordevelopment-studyrelevantpolymorphsforIPprotectionForCROcompaniesbasedonthecustomersneeds-toidentifyasmanynewpolymorphs(includesolvate/hydrate)andamorphousformaspossible-ortofindthemoststableform
2022/12/30Thepurposeofpolymorphscree41Themethodofpolymorphscreeningcrystallizationcrystallizationfromsolution(slurry,anti-solventprecipitation,Solvent-thermalheating/coolingSlow/fastprecipitationfromsaturatedsolutions)recrystallizationfromaneatcompound(thermalheating/cooling,grinding,andhighpressure)2022/12/30Themethodofpolymorphscreen42polymorphscreening——
crystallizationfromsolutiondegreeofsupersaturationandTemperatureareconsideredasthedrivingforceofcrystallisationdiversesolventsresultinthediscoveryofmorepolymorphs2022/12/30polymorphscreening——
43crystallizationfromsolution——SolventselectionSlurryAnti-solventprecipitationSolvent-thermalheating/coolingexperimentsSlow/fastprecipitationfromsaturatedsolutionsmethodSolventVisualsolubility(mg/mL)MeOH
EtOH
IPA
1-Butanol
ACN
MEK
MIBK
EtOAc
iPrOAc
MTBE
2-MeTHF
DMF
NMP
DMSO
CH2Cl2
Toluene
1,4-Dioxane
Heptane
THF
Acetone
Water
2022/12/30crystallizationfromsolution44crystallizationfromsolution——
rationalexperimentaldesignLimitedresource
Howtofindasmanynewpolymorphsand
amorphousformaspossibleAPIpropertiesdifferentsolubilityinthesolvent
poorsolubilityorgoodsolubilitySolventproperties
Polarity-differentsortofsolvents(alcohols,ethers,esteretc.)BoilingpointFreezingpointToxicitymiscibility？2022/12/30crystallizationfromsolution45Slurry——solventselectionMakesurethesampleissuspension
solvent/mixedsolventssolubilityispoor2022/12/30Slurry——solv46Anti-solventprecipitation
—solventselectionPreparesolventgoodsolubilityAnti-solventselectionPoorsolubilitypolaritymiscibility
miscibilityWaterDMFHeptaneACN1,4-DioxaneMTBEDMSO2022/12/30Anti-solventprecipitation
47Solvent-thermal
heating/coolingexperimentschangetemperature
温馨提示
- 1. 本站所有资源如无特殊说明，都需要本地电脑安装OFFICE2007和PDF阅读器。图纸软件为CAD,CAXA,PROE,UG,SolidWorks等.压缩文件请下载最新的WinRAR软件解压。
- 2. 本站的文档不包含任何第三方提供的附件图纸等，如果需要附件，请联系上传者。文件的所有权益归上传用户所有。
- 3. 本站RAR压缩包中若带图纸，网页内容里面会有图纸预览，若没有图纸预览就没有图纸。
- 4. 未经权益所有人同意不得将文件中的内容挪作商业或盈利用途。
- 5. 人人文库网仅提供信息存储空间，仅对用户上传内容的表现方式做保护处理，对用户上传分享的文档内容本身不做任何修改或编辑，并不能对任何下载内容负责。
- 6. 下载文件中如有侵权或不适当内容，请与我们联系，我们立即纠正。
- 7. 本站不保证下载资源的准确性、安全性和完整性, 同时也不承担用户因使用这些下载资源对自己和他人造成任何形式的伤害或损失。
最新文档
- 护林员防火安全培训课程
- 观看最美孝心少年颁奖典礼感想心得
- 物业设备安全管理培训
- 引领汽车制造新潮-气压动力驱动产业进步
- 阿尔茨海默病防治培训试题及答案
- 2026年中级注册安全工程师职业资格经典例题附完整答案详解【夺冠】
- 2026年中级经济师金融试题及答案
- 2026年心理咨询师综合提升练习题（模拟题）附答案详解
- 2026道德与法治三年级知识窗 生态知识学习
- 2026年院感防控知识培训试题及答案解析
- sm契约合同协议书
- 节奏律动大钟表教案
- 工业产品生产、销售单位质量安全总监、安全员培训考核题题库及答案
- 2025宁德时代shl考题
- 关工委知识培训探讨课件
- 高考志愿填报指导话术模板
- 新房验收验房清单（毛坯+精装）
- 幼儿园家委会安全工作汇报
- 2025年湖南高考物理试卷（原卷+答案）
- 2025-2030中国高纯三氟化硼行业发展格局及供需趋势预测报告
- 2025 SMETA确保员工合法工作权的核查程序-SEDEX验厂专用文件（可编辑）
评论
0/150
提交评论