罗哌卡因乳酸羟基乙酸共聚物微球的制备及体外释药研究

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1、硕士学位论文Preparationofpoly(1actide--CO——glycolide)microspherescontainingropivacaineandtheevaluationofreleaseprofilesinvitroName：BiXiaobaoSupervisor：ChenZhongqingABSTRACTBackground&objectiveLocalanestheticsasalleffectivepaintreatmenthasbeenwidelyusedinclinicalmedic

2、ine，butitsactiontimecallonlymaintainfor6,--12hours，itcannotmeettheneedofintractablepaincontrolandtreatment，suchasadvancedcancerpainandtrigeminalneuralgia．Overtheyears，peopleusedifferentwaystoextendlocalanestheticsanalgesia,buttheresultsarenotsatisfactory。Micro-

3、balltechnologyisanewtechnologyusedinthefieldofpharmaceuticalpreparationsinthepast30years，whichischaracterizedbynaturalorsyntheticpolymersascontrolledreleasedrugcarrierforthepurposeofextendingtheefficacytimeofdrug。Withthedevelopmentofcontrolled-releasemicrospher

4、es，thedevelopmentdirectionoflong-actinganestheticsagentshasshiftedtothevariousformsoflocalanestheticsmicrospherespreparation，whichcanflowdownitsplasmaconcentrationfluctuationsinordertoreducethetoxicityofdrugsandachievealastingeffectionandreducetimesofadministra

5、tion．PLAandPLGAisakindofcompletelybiodegradableplasticsdevelopedrecently．whichisupfromatypical0【-hydroxyacidpolymerandhasgoodbiocompatibilityandhumanadaptability．Inorganisms，theultimatedegradationproductsofPLGAarelacticacid，whichultimatelycompletelydegradetocar

6、bondioxideandwater,andthenallofthesedegradationproductsaredischargedoutoforganisms．SoPLGAisakindofsafebiodegradablematerial，whichcandeleteABSTRACEobviousinflammatoryresponse，immuneresponseandcelltoxicityresponse．Ithasitsowncharacteristicthatcompletelybiological

7、degradedinvivoanddischargedoutoforganismstoavoidsecondaryvictimizationforpatients．PLAandPLGAmicrosphereshasbeenusedinanticancerdrugs，antibiotics，eyediseases，genetherapy，ckawbetestreatment，andmanyotherstudies．PLAandPLGAmicrosphereshavebeenusedinlocalanestheticsr

8、esearchfor30years．Asearlyas1981，WakiyamaNhaspreparedseveralkindsoflocalanestheticsPLA-MS，1994LeCorrestudiedpreparationsandcharacteristicsofBUP—PLA／PLGA-MS，bothofthemprovedth