《药物晶型研究》PPT课件.ppt

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1、2021/9/3药物的多晶型研究2021/9/3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2021/9/3CrystalAsolidmaterialwhoseconstituentatoms,molecules,orionsarearrangedinanorderlyrepeatingpatternextendinginallthreespatialdimensions.PharmaceuticalcrystalsMostdrugsaredevelopedas

2、crystallineStabilityProcessabilityIPprotection什么是晶体？什么是多晶型？Polymorphismistheabilityofasolidmaterialtoexistinmorethanoneformorcrystalstructure.PolymorphsSoldphaseSamechemicalcompositionDifferentmoleculararrangementsInpractice,weareinterestedinallthecrystallineandamorphousphasesfo

3、rachemical/pharmaceutical2021/9/32021/9/32021/9/3多晶型研究对药物开发的重要性2021/9/3药物多晶型研究的重要性2021/9/32021/9/3如何筛选和选择药物的新晶型2021/9/32021/9/32021/9/3晶型的化学和物理分析手段2021/9/32021/9/32021/9/3Experiencesharingonpolymorphscreening——solventselection2021/9/3ThepurposeofpolymorphscreeningForInnovatorcom

4、panies-selecttheoptimalsolid-stateofAPIfordevelopment-studyrelevantpolymorphsforIPprotectionForCROcompaniesbasedonthecustomersneeds-toidentifyasmanynewpolymorphs(includesolvate/hydrate)andamorphousformaspossible-ortofindthemoststableformThemethodofpolymorphscreening2021/9/3cryst

5、allizationcrystallizationfromsolution(slurry,anti-solventprecipitation,Solvent-thermalheating/coolingSlow/fastprecipitationfromsaturatedsolutions)recrystallizationfromaneatcompound(thermalheating/cooling,grinding,andhighpressure)polymorphscreening——crystallizationfromsolution20

6、21/9/3degreeofsupersaturationandTemperatureareconsideredasthedrivingforceofcrystallisationdiversesolventsresultinthediscoveryofmorepolymorphscrystallizationfromsolution——Solventselection2021/9/3SlurryAnti-solventprecipitationSolvent-thermalheating/coolingexperimentsSlow/fastprec

7、ipitationfromsaturatedsolutionsmethodSolventVisualsolubility(mg/mL)MeOHEtOHIPA1-ButanolACNMEKMIBKEtOAciPrOAcMTBE2-MeTHFDMFNMPDMSOCH2Cl2Toluene1,4-DioxaneHeptaneTHFAcetoneWatercrystallizationfromsolution——rationalexperimentaldesign2021/9/3LimitedresourceHowtofindasmanynewpolymor

8、phsandamorphousformaspossibleAPIpropertiesdiffe