hpmc修饰的氟苯尼考微晶体的制备、表征及其药动学-研究

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1、万方数据Preparation，CharacterizationandPharmacokineticsofFlorfenicolmicrocrystalmodifiedbyHPMCAbstractFloi’tk-nicolalso女jMHlnasfluorothialnphenic01．‘}hichisabroadspectrumantibacterialagentsusedinthelateeighty’StOtheanimals．Becauseit‘Sver，vdifficulttodissolx，einwater．thectinicaluse、、。aslimited．Themet

2、hodstoillcreasethesolubility’ofFlorfenicolatpresentmainlyincludessyntheticwater·solubleprodrug。preparationofFlorfenicolsolublepowder．prepareitssoliddispersionsbyPEG-6000andus’ingDMForotherorganicsolventsassolvent．Buttherearemanyproblemswiththesesolubilizationmethods．suchasharmfulby—productresidu

3、es，pooreffectofsolubilizationandstimulatebodybyorganicsolvents．SofindasuitablesolubilizationmethodofFlorfenicolisverymeaningfulandnecessaryParticlesizeofthedrugiscloselyrelatedtothestrippingproperties，accordingtoNoyes-Whitneyequation，dissolutionrateofmaterialsisproportionaltothesurfacearea,andth

4、edecreaseinparticlesizeCanincreasethesurfaceareaofthematerial，SOitCanimprovethesolubilityofthedrug．Atpresent，themicronizationtechnologiestoincreasedrugsolubilitybyreducedrugparticlesizeareverypopular．mainlyincludesTop·downandBottom—up．Top-downmainlyreferstocrushingmaterialsfrombigtosmallbymechan

5、ical，andBottom—upreferstousechemicalmethods，firstdissolvingthedrug．thencrystallizethesmallerdrugcrystal．Thisexperimentadoptsthelattermethod，whichCanreducethepossibilityofdestroydrugstructurebymechanicalenergyandreducesthepreparationcost．Improvedsolvent—antisolventrecrystallizationmethodwasusedin

6、thisexperiment，andFlorfenicolmicrocrystalwithsmallerparticlesizewasgetbyaddingstabilizertoinhibitcrystalgrowthintheantisolvent．Atthesanletime，throughthesinglefactorandorthogonalexperiments，screeningtheoptimtmlconditionsofpreparationandthestabilizer．Experimentsshowthat，wheretheacetoneassolventjwa

7、terasanti．solvent．solventanti．solventratioiS1：9，HPMCconcentrationof4mg／mlasstabilizer．concentrationofFlorfenicolas160mg／ml，FlorfenicolIII万方数据It4ICt’。10i．j){：ll、、i【11attl；．INillll．11115atUFdtiOtlSl+Itibi“t＼{j．1j{110i11l}in37(