口服固体缓释制剂工艺

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1、口服固体缓释制剂工艺李冬2016/10/26缓释制剂概述Whyoralmodifiedrelease?为什么开发控释制剂Driversformodifiedrelease研发缓释制剂的驱动力•Therapeuticefficacy疗效•Optimizingperformance优化产品性能•ChallengingAPI有挑战性的API•Reducingside-effects减少副作用•Prolongingaction延长作用时间•Improvingpatientcompliance提升患者的顺应

2、性•Minimizingvariability最小化差异•Life-cyclemanagement产品的生命周期管理•BypassingIPhurdle绕过专利壁垒2缓释制剂概述Typesofmodifiedreleasedosageforms控释剂型的种类Modifiedreleasedosageforms缓释剂型的定义与速释制剂的给药途径相同，但以一定的速率或在特定部位释放药物活性成分的制剂。Delayedreleasedosageforms迟释剂型Thereleaseoftheactiv

3、esubstanceisdelayedforapredefinedperiodafteradministrationorapplicationofthedosageformandthenreleasesasaconventionaldosageformresultinginalagtimewithoutanychangeinotherpharmacokineticparameters.Sustainedrelease=Extendedrelease=Prolongedreleasedosagef

4、orms持续释放=扩展释放=延长释放剂型Dosageformsshowingaslowerreleasethanthatoftheconventionalreleasedosageformadministeredbythesameroute.Multiphasicorprogrammedreleasedosageforms多相或编程释放剂型e.g.pulsatilerelease:intendedtodeliveraburstofdrugreleaseatspecifictimeinterval

5、s.biphasicrelease:firstphaseofdrugrelease=fastreleasedosefraction,secondphase=extendedreleaseSite-specificrelease=targetedreleasedosageforms靶点释放=目标释放剂型definitionsbasedonEMAguidelinesEMA/CPMP/EWP/280/96Corr1andEMA/CHMP/QWP/428693/20133缓释制剂概述哪些种类的API会

6、从缓释制剂开发中收益?e.g.APIswithfasteliminationAPIswithsmalltherapeuticwindowAPIsthatsofarhavetobedosedfrequently,e.g.severaltimesperdayveryhydrophilicandwellsolubleAPIswherethekineticsaretobecontrolled…almosteveryAPIcanpotentiallybenefit,dependingonthei

7、ndicationandformulationtarget4缓释制剂概述ConcerningPointsfordevelopmentofsustainedreleasedosageform缓释剂型研发的关注点1.Simplyandreproducedmanufactureprocess简便的可重现的生产工艺2.ConsistentbehaviorofAPIreleasewithvariouscompressionforces在不同压片压力下的稳定的API释放行为3.Consistentbehavi

8、orofAPIreleaseoverbroadpHrange在宽泛的1.›pH范围下稳定的API释放行为4.Patientcompliance专利合规性5.Nodosedumpingrisk无剂量突释的风险6.Stability产品稳定性5缓释制剂概述Whatisdosedumping?什么是剂量突释缓释制剂是在一段较长时间内以需要的浓度来释放药物的。因此，其含有超过单剂量配方的大量药物。剂量突释:在短时间内从控释制剂里释放出大量药物的现象.*grinding/crtamperi