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，einwat

2、er．thectinicaluse、、。aslimited．Themethodstoillcreasethesolubility’ofFlorfenicolatpresentmainlyincludessyntheticwater·solubleprodrug。preparationofFlorfenicolsolublepowder．prepareitssoliddispersionsbyPEG-6000andus’ingDMForotherorganicsolventsassolvent．Butthereare

3、manyproblemswiththesesolubilizationmethods．suchasharmfulby—productresidues，pooreffectofsolubilizationandstimulatebodybyorganicsolvents．SofindasuitablesolubilizationmethodofFlorfenicolisverymeaningfulandnecessaryParticlesizeofthedrugiscloselyrelatedtothestrippi

4、ngproperties，accordingtoNoyes-Whitneyequation，dissolutionrateofmaterialsisproportionaltothesurfacearea,andthedecreaseinparticlesizeCanincreasethesurfaceareaofthematerial，SOitCanimprovethesolubilityofthedrug．Atpresent，themicronizationtechnologiestoincreasedrugs

5、olubilitybyreducedrugparticlesizeareverypopular．mainlyincludesTop·downandBottom—up．Top-downmainlyreferstocrushingmaterialsfrombigtosmallbymechanical，andBottom—upreferstousechemicalmethods，firstdissolvingthedrug．thencrystallizethesmallerdrugcrystal．Thisexperime

6、ntadoptsthelattermethod，whichCanreducethepossibilityofdestroydrugstructurebymechanicalenergyandreducesthepreparationcost．Improvedsolvent—antisolventrecrystallizationmethodwasusedinthisexperiment，andFlorfenicolmicrocrystalwithsmallerparticlesizewasgetbyaddingst

7、abilizertoinhibitcrystalgrowthintheantisolvent．Atthesanletime，throughthesinglefactorandorthogonalexperiments，screeningtheoptimtmlconditionsofpreparationandthestabilizer．Experimentsshowthat，wheretheacetoneassolventjwaterasanti．solvent．solventanti．solventratioiS

8、1：9，HPMCconcentrationof4mg／mlasstabilizer．concentrationofFlorfenicolas160mg／ml，FlorfenicolIII万方数据It4ICt’。10i．j){：ll、、i【11attl；．INillll．11115atUFdtiOtlSl+Itibi“t＼{j．1j{110i11l}in37(