Preparation of Tolterodine Metabolite Loaded Biodegradable PLGA Microspheres

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摘要 Biodegradablepolymerpoly(lactic-co-glycolicacid)(PLGA)wasusedtoencapsulatethepharmacologicalactivitymetaboliteoftolterodinebymeansofO/Wemulsionsolventevaporationmethodviahomogenizationintheemulsificationprocess.Theinfluencesofpreparationparameterswereinvestigated.TheresultsindicatethatincreasingPLGAconcentrationfrom15%to40%madetheencapsulationefficiencyof5-hydroxymethylderivativeoftolterodine(5-HMT)increasedfrom55.39%to76.32%,andtheparticlesizeincreasedfrom34.33μmto70.78μm.Inaddition,whenhomogenizationspeedincreasedfrom850r/minto2300r/min,bothparticlesizeandencapsulationefficiencyofmicrospheresdecreased.Anincreaseinthevolumeofaqueousphaseledtohigherencapsulationefficiencyandbiggerparticlesize.Increasingtemperaturemadeencapsulationefficiencyandparticlesizechangesignificantly.Whilereactiontemperatureincreasedfrom20°Cto50°C,theencapsulationefficiencydecreasedfrom70.44%to24.07%,andparticlesizeincreasedfrom38.66μmto69.38μm.Highreactiontemperature(over40°C)mayleadtoporoussurfaceofmicrospheres.Poroussurface,encapsulationefficiencyandparticlesizeinfluencedontheinvitroreleaseof5-HMTtogether.
机构地区 不详
出版日期 2010年01月11日(中国期刊网平台首次上网日期,不代表论文的发表时间)
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