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1、地塞米松磷酸钠脂质体壳聚糖胶囊的结肠定位释药与吸收研究李国锋,陈建海,任非,杨西晓,郭丹,杨莉,王新亚,李治军,侯连兵,陈志良(南方医科大学南方医院药学部,广东广州510515)摘要:目的利用壳聚糖作为载体将地塞米松磷酸钠(DSP)脂质体冻干粉剂导向结肠并探索载药脂质体经结肠黏膜吸收分布的规律性。方法用二次乳化法,经正交试验来筛选DSP脂质体的配方。测定脂质体的包裹率和载药量,观察脂质体的形态和粒径大小分布。建立HPLC测定DSP浓度的方法。制备DSP脂质体冻干剂,将其装入壳聚糖胶囊中,再以HPMCP包裹胶囊。分别给大鼠口服各种DSP制剂,测定经时血药浓度和结
2、肠组织中分布量,计算药物的相对靶向释药指数(DDI)。结果用二次乳化法制备DSP脂质体时,平均包裹率为54182%,载药量为8167%,粒径分布在120~265nm之间,平均粒径为178nm;口服给药时,和DSP粉剂壳聚糖胶囊或DSP溶液剂比较,DSP脂质体冻干剂壳聚糖胶囊被吸收入血的程度最低,而经时在结肠局部的分布程度最高。DSP壳聚糖胶囊结肠DDI分别是DSP溶液的29118和DSP壳聚糖胶囊的2128。结论DSP脂质体冻干剂壳聚糖胶囊较DSP粉剂壳聚糖胶囊对结肠局部组织具有更好的定位释药作用和局部治疗效果,值得进一步开发研究。关键词:地塞米松磷酸钠;壳聚
3、糖胶囊;脂质体;结肠定位释药中图分类号:R943133文献标识码:A文章编号:1001-2494(2005)03-0207-05Studyonthecolonsite-specificdeliveryofchitosancapsulefilledwithdexamethasonesodiumphosphateliposomelyophilizedpowderLIGuo-feng,CHENJian-hai,RENFei,YANGX-ixiao,GUODan,YANGLi,WANGXin-ya,LIZh-ijun,HOULian-bin,CHENZh-iliang
4、(ClinicalPharmaceuticalInstitute,NanfangHospitalofNanfangMedicalUniversity,Guangzhou510515,Chi-na)ABSTRACT:OBJECTIVEToinvestigatetheabsorptionanddistributionofchitosancapsulefilledwithdexamethasonesodiumphosphate(DSP)liposomelyophilizedpowderinrats1METHODSDSPliposomewaspreparedbydup
5、licatedemulsificationmethod1Itsformulawasde-terminedwiththeorthogonalexperiment1ThequalityofDSPliposome,suchastheencapsulationrate,drug-loading,morphologyandsizedis-tribution,wasestimated1Thechosenliposome,madeintoitslyophilizedpowder,wasthenfilledintothecapsulecoatedwithHPMCP1Theca
6、psulesaswellastheotherDSPdosageformswereadministeredorally1Bloodandcolontissuewerecollectedperiodically1TheconcentrationofDSPwasmeasuredbyHPLC,andusedtocalculatetherelativetargetingdrugdeliveryindex(DDI)ofDSP1RESULTSThepreparedDSPliposomewascharacterizedbyitsaverageencapsulationrate
7、of54182%,drug-loadingof8167%,andthesizedistributionfrom120nmto265nm(averaged178nm)1Afteroraladministration,thebloodlevelofDSPlyophilizedliposomecapsulewasthelowestinalltheDSPdosageforms,butthedistributionofDSPincolonwasthehighest1TherelativetargetingDDIofDSPlyophilizedliposomecapsul
8、ewas29118or2128,aga
