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鼻腔给药地西泮微乳的制备及性质考察.pdf

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鼻腔给药地西泮微乳的制备及性质考察.pdf

»6»4ùÏS04нVol.6No.42008M7ChineseJournalofPharmaceuticsJul.2008p.156là°ù20080317T€eºŠîÅ1980–,oqB,Ħ,«Vùî3,Emailchengmei_jiaoyahoo.com.cnÙØþ1957–,3qB,a7ð¦,q,pVö1VY0þ4˜Ð/Œùî,Tel.024–23984063,Emailli_sanmingsina.combÓcI|200804–0156–0608ó0¹º±Ä¥ÅŸÉI³ŠîÅÁÓfÓÙØþ0SvÐ0Ðýa110016K1¥Å¹º±ÄiÉ›ÉßNbZE¨ÀØíMm’ç±ÄZI³aȝqaVëfïaìå08°ýŸb²T±ÄZ¥És”Fî¹8.0ÏýØŲa21.3Tween80a10.7PEG400a60.0£bÄóbaiüb¹1€102Pasȝq¹12.3mSm1Vëfï¹48.5mNm1ìå¹31.2nmiO8°ýŸ®b²‚Źº±Ä¹7¹º˜08ó0Å44Gb1oM04бÄÀØíMm¹º08°ýŸÏmsË|R94ÓDS½’AÙ€ûÃÿstatusepilepticusBQÙ€ûÃ30minõÃQTTWuùiMÿÜÿÃë¯Àϳù£Ü€8SÈn¥²¡­Bb¹º¹‹ËFŠn0áÿ¹Í–uûÃÿ¥nÊ0b5Ȩáÿ¥™Tó0³1P£•¤Í„ÿѹiÑbNªÄïa’HW|SA±ä/4³Ï8°Ãåî5bíªÒÏ°À8°åîT¸cVó07SÀ8°åîT¸îûÃ¥HW9bLʨ3Ø÷£¹|ŸvÖµø8°ýŸ¥És”¹1¥€‰Ö¹ŸvÖßN¹º±Ä¥08°ýŸÏò0AXØÀ©1b2.5.1óÍsk0Aª8°åîHW¥©çsYó͍sk0Aó0ª8°îûÃHWT¹I³SßNòÅ4¥ýŸb²TnV3bTable3Ciliarybeatdurationevaluatedwithtoadpalatemucosaciliamodelinvitron5Solutiontciliarybeatduration/minSaline480±43Microemulsionofdiazepam450±501Sodiumdeoxycholate18±3160ÏS04н»61602.5.2óÍsk0Aª8°™ÿ¥4³¨šÂT3þA±ä4³óÍòsk0Aª¥8°™ÿiÉ›v²Tnm3bABCFig.3MorphologyoftheciliaunderopticalmicroscopeafteradministrationofnegativecontrolAsaline,ciliaonthemucosakeptintact,denseandbeatactively8haftertreatment,microemulsionofdiazepamBsimilarphenomenonwiththatofsalinevisualized8haftertreatment,positivecontrolC1sodiumdeoxycholate,nociliaonthemucosaobservedbutafewexfoliatedcilia30minaftertreatment²TVüóÍ3Ø÷£ª8°VëbVn†œOµp¹_BñZ_åîÔq“ÚûÃåîHW¹480±43minbó͹º±ÄME2ªj7b8°AyŒîG–ÛHW¥üÉφ8°îïvM¤7Hø8°G–EsbîEs°À450±50min8°îT¸bªü±Ä0εBç¥åÊT¨Œ•Y‚v8°ýŸ“lbó̀‰ÖªA±ä/™ÿEsy´‚bœñj7S¶íEsžžåî¥8°8°X›†‚‹Vü€‰ÖF®µø¥åÊT¨8°îµø¥‚VI¥ÅT¨b3‚a.LMiglyol812¹²MTween80¹VëŸ4PEG400¹ùVëŸ4bMiglyol812¹ÏýØŲ¸™î¸ëiOµz¥îŸa³Ÿ„ÄÄŸ±þ²ËzbTween80¹cY¥dÖ0˜VëŸ4HLB´¹15.0˜†ÅO/W˜±Ä¥1pOýŸlÄÄïbùVëŸ4V£ù³0þ†®Vëfï9vį¸ë¥¼¨ŸT€Ê¨ýŸlO3ØM¸Ÿz¥PEG400¹ùVëŸ4bb.±ÄÅVñϐ¨ÀØíMmªÄZMiglyol812Tween80PEG400£8Ï’VëŸ4ÐùVëŸ4¥É1Km2H²MµKDÄÄrTbNñ5ñ±ÄZØÄŸÉ0É›I³KԒ繺±Ä¥KªZbc.08VëBªL¯ªøÃVsßv¥Ai­Â8°bžÈfƒ/8°xØBÁ¥åîb08¥sþb’8shý˙H8°î„Asßsž•Y¸˙òÕ¤Ÿ«¡hb08ó0n5så¥8°0þ£08°µýŸT¨ø€Îö•Yž08¥žÈ3Øÿ10byNùî08ó0Å4HI³Å40F®„08°¥ýŸ­¹1bT€¨©ç8°ûÃîHW¥ZEŸßN0þÅ408°¥ýŸ²TVü¹º±ÄME2¥8°ýŸlb»4ùŠîÅ©08ó0¹º±Ä¥ÅŸÉI³161•IÓD1VYASTK,BABBARAK,SHARMARK,etal.IntranasalmucoadhesivemicroemulsionsofclonazepampreliminarystudiesonbraintargetingJ.JournalofPharmaceuticalSciences,2006,95570–580.2LIANLL,SUDHIRG,YONGMC,etal.RapidonsetintranasaldeliveryofanticonvulsantspharmacokineticandpharmacodynamicevaluationinrabbitsJ.IntJournalofPharmaceutics,2000,19965–76.3AMMONCS,SHAFIRB.TransdermaldrugdeliveryusingmicroemulsionandaqueoussystemsInfluenceofskinstorageconditionsontheinvitropermeabilityofdiclofenacfromaqueousvehiclesystemsJ.IntJournalofPharmaceutics,2006,31155–62.4LINDHARDTK,OLAFSSONDR,GIZURARSON,etal.IntranasalbioavailabilityofdiazepaminsheepcorrelatedtorabbitandmanJ.IntJournalofPharmaceutics,2002,23167–72.5Z‡,fÑl.Èn0±ÄÅ4ŸJ.»BDvÐÐ,2001,211280–83.6ñ¨X,ÙØþ,´ç¢,©.£²˜±Ä™îyÍ¥I³J.0SvÐÐ,2005,22296–99.7f²,€S.08ó0d¥0TýŸ³oåJ.ÏSD0ý½,2001,327323–327.8¦±.ÛEssdp,ÜÄ4¥ìåvlÐsƒJ.0SvÐÐ,2003,205336–338.9GAOXL,TAOWX,LUW,etal.LectinconjugatedPEGPLAnanoparticlesPreparationandbraindeliveryafterintranasaladministrationJ.Biomatericals,2006,273482–3490.10ŒA.0ýŸùîÉZJ.0н,2005,20288–89.PreparationandevaluationofdiazepammicroemulsionforintranasaldeliveryJIAOChengmei,LIUHongzhuo,JINGLingyu,ZHANGYu,LISanmingSchoolofpharmacy,ShenyangPharmaceuticalUniversity,Shenyang110016,ChinaAbstractObjectiveTopreparediazepammicroemulsionandevaluateitsquality.MethodsTheformulationofdiazepammicroemulsionwasselectedusingpseudoternaryphasediagram.Theviscosity,conductivity,surfacetension,dropletsizeandnasalciliotoxicityofthemicroemulsionwerecharacterized.ResultsThemicroemulsionwascomposedofMiglyol8128.0,Tween8021.3,PEG40010.7andwater60.0,anditsviscosity,conductivity,surfacetensionanddropletsizewere0.010Pas,12.3mSm1,48.5mNm1and31.2nm,respectively.Thediazepammicroemulsionhadonlyslightnasalciliotoxicity.ConclusionDiazepammicroemulsioncouldbepreparedusingMiglyol812Tween80PEG400watersystem,whichcanbeusedforintranasaladministration.Keywordspharmaceuticsmicroemulsionpseudoternaryphasediagramdiazepamnasalciliotoxicity3©IuI¤

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