資源描述：
《藥物晶型研究.ppt》由會員上傳分享，免費(fèi)在線閱讀，更多相關(guān)內(nèi)容在應(yīng)用文檔-天天文庫。
1、2021/7/27藥物的多晶型研究2021/7/27提綱什么是晶體，多晶型？多晶型研究對藥物開發(fā)的重要性如何篩選和選擇藥物的新晶型多晶型的主要分析手段晶型篩選實驗的經(jīng)驗分享----溶劑選擇2021/7/27CrystalAsolidmaterialwhoseconstituentatoms,molecules,orionsarearrangedinanorderlyrepeatingpatternextendinginallthreespatialdimensions.Pharmaceuticalcrysta
2、lsMostdrugsaredevelopedascrystallineStabilityProcessabilityIPprotection什么是晶體？什么是多晶型？Polymorphismistheabilityofasolidmaterialtoexistinmorethanoneformorcrystalstructure.PolymorphsSoldphaseSamechemicalcompositionDifferentmoleculararrangementsInpractice,wearein
3、terestedinallthecrystallineandamorphousphasesforachemical/pharmaceutical2021/7/272021/7/272021/7/27多晶型研究對藥物開發(fā)的重要性2021/7/27藥物多晶型研究的重要性2021/7/272021/7/27如何篩選和選擇藥物的新晶型2021/7/272021/7/272021/7/27晶型的化學(xué)和物理分析手段2021/7/272021/7/272021/7/27Experiencesharingonpolymorp
4、hscreening——solventselection2021/7/27ThepurposeofpolymorphscreeningForInnovatorcompanies-selecttheoptimalsolid-stateofAPIfordevelopment-studyrelevantpolymorphsforIPprotectionForCROcompaniesbasedonthecustomersneeds-toidentifyasmanynewpolymorphs(includesolvat
5、e/hydrate)andamorphousformaspossible-ortofindthemoststableformThemethodofpolymorphscreening2021/7/27crystallizationcrystallizationfromsolution(slurry,anti-solventprecipitation,Solvent-thermalheating/coolingSlow/fastprecipitationfromsaturatedsolutions)recrys
6、tallizationfromaneatcompound(thermalheating/cooling,grinding,andhighpressure)polymorphscreening—— crystallizationfromsolution2021/7/27degreeofsupersaturationandTemperatureareconsideredasthedrivingforceofcrystallisationdiversesolventsresultinthediscoveryofmo
7、repolymorphscrystallizationfromsolution——Solventselection2021/7/27SlurryAnti-solventprecipitationSolvent-thermalheating/coolingexperimentsSlow/fastprecipitationfromsaturatedsolutionsmethodSolventVisualsolubility(mg/mL)MeOHEtOHIPA1-ButanolACNMEKMIBKEtOAciPrO
8、AcMTBE2-MeTHFDMFNMPDMSOCH2Cl2Toluene1,4-DioxaneHeptaneTHFAcetoneWatercrystallizationfromsolution—— rationalexperimentaldesign2021/7/27LimitedresourceHowtofindasmanynewpolymorphsandamorphousformaspossib
