灯盏花素前体脂质体胶囊突释的评价方法.docx

灯盏花素前体脂质体胶囊突释的评价方法[摘要]目的：建立灯盏花素前体脂质体胶囊的突释考察方法。方法：采用透析-高效液相色谱法（HPLC）水化前体脂质体后用透析袋分析游离药物和脂质体并用HPLC法测定含量。采用DiamonsilODSC18色谱柱（4.6mm×250mm5μm）流动相为甲醇-乙腈-40mmol/LKH2PO4(磷酸调pH至2.5)（18∶12∶70）；检测波长335nm；流速1.0ml/min；柱温35℃。结果：游离药物在透析膜两侧均匀分布而脂质体被截留于透析袋中。含量测定方法平均加样回收率为103.32%RSD为1.12%（n＝9）。结论：本法操作简便、准确可用于灯盏花素前体脂质体胶囊突释的评价。[关键词]灯盏花素；前体脂质体；突释；透析[中图分类号]R944.9[文献标识码]A[文章编号]1673-7210（2008）03（b）-034-02ThestudyoninitialburstreleaseofScutellarinProliposomeCapsulesLIWen-xiuDENGYing-jie*WEIWeiGAOXiao-feiCAOJin-na(TheSchoolofPharmcyShenyangPharmaceuticalUniversityShenyang110016China)[Abstract]Objective:ToestablishamethodfordeterminingtheinitialburstreleaseofScutellarinProliposomeCapsules.Methods:Adialysis-HPLCmethodwasapplied.AfterthehydrationofproliposomebagfilterwasusedtoseparatefreedrugandliposomethendeterminedthecontentbyHPLCwithDiamonsilODSC18(4.6mm×250mm5μm)usingthemobilephaseofmethanol-acetonitrile-40mmol/LKH2PO4(adjustedpHto2.5byphosphoricacid)(18∶12∶70)withaflowrateat1.0ml/minandthedetectivewavelengthwas335nmandthecolumntemperaturewas35℃.Results:Thedistributionoffreedrugswasequivalentontwosidesofbagfilterbutliposomeswerekeptinthebag.TheaveragerecoveryandRSDofthecontentdeterminationmethodwere103.32%and1.12%(n=9)respectively.Conclusion:Themethodisconvenientandaccurate.ItcanbeusedtoevaluatetheinitialburstreleaseofScutellarinProliposomeCapsules.[Keywords]Scutellarin;Proliposome;Initialburstrelease;Dialysis灯盏花素（breviscapine）是从菊科飞蓬属植物灯盏花Erigeronbreviscapus(vant.)Hand.-Mazz.中提取的黄酮类有效成分以灯盏乙素（scutllarin）为主（占95%以上）含少量灯盏甲素。临床多用于治疗脑梗死、脑血栓、脑出血[1]。由于现有片剂生物利用度低[2]现将其制成前体脂质体粉末并灌装于胶囊中以提高灯盏花素的生物利用度。药物在脂质体中的情况中一般有3种：吸附、包入、嵌入。在体外释放实验时表面吸附的药物会快速释放称为突释效应。制成脂质体制剂后应检查其是否有突释效应。为评价灯盏花素前体脂质体是否存在突释本文建立了释放的检查方法并测定其在0.5h的释放量为突释的评价提供依据。1仪器与试剂高效液相色谱仪（L-2400UVDet