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1、骨形成蛋白微球溫敏性凝膠復(fù)合系統(tǒng)的制備及釋藥特性研究符旭東基金項(xiàng)目：湖北省科技攻關(guān)計(jì)劃（2005AA301C38）通訊作者：符旭東，女，副主任藥師Tel/Fax:(027)87649309E-mail:fuxudong2005@yahoo.com.cn，劉宏，湯韌，張孟佑（廣州軍區(qū)武漢總醫(yī)院藥劑科，武漢，430070）摘要目的考察了處方和制備工藝對(duì)人重組骨形成蛋白－2（rhBMP-2）微球釋放度的影響，并比較BMP微球和BMP微球溫敏性凝膠復(fù)合系統(tǒng)的體外釋藥特性。方法采用W/O/W型乳化溶劑揮發(fā)法以聚乳酸-乙醇酸共聚物（PLGA）為材料制備空白微球，通過吸附法制備rhBMP-2載藥微球
2、。以單甲基聚乙二醇－羥基乙酸共聚物（MPEG-PLGA）為材料制備凝膠，采用夾心法酶聯(lián)免疫吸附法測定釋藥速度。結(jié)果微球呈現(xiàn)三相釋藥模式，而微球凝膠劑體外釋藥曲線符合Higuchi方程。采用PLGA-COOH制備的rhBMP-2微球，其突釋明顯小于以PLGA為材料制備的微球，增加內(nèi)水相與油相的體積比、在內(nèi)水相中加入氯化鈉均可以在一定程度上減小突釋。結(jié)論BMP微球溫敏性凝膠復(fù)合系統(tǒng)制備工藝，具有比rhBMP-2微球劑更理想的體外釋藥特性。關(guān)鍵詞：人重組骨形成蛋白－2;聚乳酸-乙醇酸共聚物；單甲基聚乙二醇－羥基乙酸共聚物;微球；溫敏性凝膠；突釋Preparationofrecombinant
3、humanbonemorphogeneticprotein-2Loadedmicrospheres/thermosensitivehydrogelscomplexanditsinvitroreleasecharacteristicFuXu-dong,LiuHong，TangRen,ZhangMeng-you（WuhanGeneralHospitalofGuanzhouCommand,Wuhan430030,China）ABSTRACT：OBJECTIVEToexaminetheeffectsofformulationfactorsoninvitroreleaserateofrecomb
4、inanthumanbonemorphogeneticprotein-2(rhBMP-2)loadedmicrospheresandcomparedrugreleaseprofilesofmicrospheresandmicrospheres/thermosensitivehydrogelscomplex.METHODSBlankmicrosphereswerepreparedwithW/O/Wemulsionsolventevaporationmethod.RhBMP-2loadedmicrosphereswaspreparedwithabsorptionmethod.Thermos
5、ensitivehydrogelswerepreparedwithMPEG-PLGA.Enzyme-linkedimmunosorbentassaywasusedto8determinedrugcontentandinvitroreleaserate.RESULTSTheprofilesofRhBMP-2microsphereswerecharacterizedbythreephase,whiletheinvitroreleaseprofileofrhBMP-2microspheres/thermosensitivehydrogelscomplexconformedtoHiguchie
6、quation.TheamountofrhBMP-2releasedfrommicrospheresintheinitialburstphasewasdecresedmarkedlywhenPLGA-COOHwasusedtopreparemicrospheresinsteadofPLGA.IncreasingthevolumeratioofinternalaqueousandaddingNaCLtointernalaqueousphasecouldreduceinitialrelease.CONCLUSIONRhbmp2–loadedmicrospheres/thermosensit
7、ivehydrogelscomplexexertedadesirablereleasecharacteristic.KEYWORDSrecombinanthumanbonemorphogeneticprotein-2;PLGA;MPEG-PLGA;thermosensitivehydrogels;microsphere；initialburstrelease牙周病是世界衛(wèi)生組織列為重點(diǎn)防治的、人類普遍罹患的口腔疾病之一，是成年人失牙的主要原因，
