Micronization and Nanoization of Active Pharmaceutical Ingredients

(整期优先)网络出版时间:2018-03-13
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Morethan40%ofnewlydiscovereddrugshavelittleornowatersolubilitywhichpresentsaseriouschallengetothesuccessfuldevelopmentandcommercializationofnewdrugsinthepharmaceuticalindustry.Additionally,morethan90%ofdrugsapprovedsince1995havepoorsolubility,poorpermeability,orboth.Therefore,itmaybenecessarytoincreasethedoseofapoorlysolubledrugtoobtaintherequiredefficacywhichcanleadtomoresideeffectsandhighercosttothepatient.Performanceofdrugscanbeimprovedbydecreasingtheparticlesizeand,atthesametime,increasingspecificsurfacearea,dissolutionrateandthebioavailabilityofthedruginthehumanbody.Theroutesofadministrationaredifferentandlistedas60%fororal,5%forpulmonary,5%forocular,5%fortopicaland25%forinjectable,approximately.Theinjectabledrugsarethemostinterestingonesfornanoization,becausesmallerparticleswillincreaseperformance,andwillbeusefulwhenusingmicroneedles.InatypicalmanufacturingprocessofAPIs(activepharmaceuticalingredients)topdownprocesseslikehighpressurehomogenizationandwetbeadmillingareusedasstandardmethodstodecreasetheparticlesizesdowntoafinenessrangeof10to500nanometers.