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1、ChineseJournalofNewDrugs2009,18(1)·实验研究·蚓激酶口服微乳的制备及性质研究1,21121,3程茂波,金武,王坚成,陈大为,张强(1北京大学药学院药剂系,北京100083;2沈阳药科大学药学院药剂系,沈阳110015;3北京大学天然药物与仿生药物国家重点实验室,北京100083)[摘要]目的:研究可用于亲水性大分子蛋白多肽类药物口服给药的W/O型口服微乳制剂。方法:以蚓激酶(EFE2d,Mw24177)为模型药物,采用滴定法建立伪三元相图,并通过动态激光散射法、电导法、冷冻蚀刻电子显微镜
2、法、差示扫描量热法以及体外释放的研究对蚓激酶W/O型微乳进行了评价。结果:制得的载体为光学上各向同性、均匀分散的、球状的W/O型微乳体系,粒径6.86nm;体外释放研究表明,蚓激酶W/O型微乳中药物的释放速率和累积释放量降低。结论:制备亲水性大分子蛋白多肽类药物蚓激酶W/O型口服微乳具有较好的可行性。[关键词]蚓激酶;W/O型微乳;口服[中图分类号]R943.41[文献标识码]A[文章编号]1003-3734(2009)01-0078-06Preparationandinvitrocharacterizationofor
3、almicroemulsionscontainingearthwormfibrinolyticenzyme1,21121,3CHENGMao2bo,JINWu,WANGJian2cheng,CHENDa2wei,ZHANGQiang(1DepartmentofPharmaceutics,SchoolofPharmaceuticalSciences,PekingUniversity,Beijing100083,China;2DepartmentofPharmaceutics,SchoolofPharmaceuticalSc
4、iences,ShenyangPharmaceuticalUniversity,Shenyang110015,China;3TheStateKeyLaboratoryofNaturalandBiomimeticDrugs,Beijing100083,China)[Abstract]Objective:Todevelopanovelwater2in2oil(W/O)microemulsionfororaldeliveryofhydrophil2icproteindrugusingtheearthwormfibrinolyt
5、icenzyme(EFE2d,Mw24177)asamodelproteindrug.Methods:Thepartialpseudo2ternaryphasediagramwasconstructedbytitrationmethod,andtheviscosityandrefractiveindexofanoptimalW/Omicroemulsionweremeasured.Themeanparticlesizeandthemorphologyofthemicroemulsionwerecharacterizedb
6、ythedynamiclaserscatteringmethodandthetransmissionelectronmicroscopefollowedfreeze2fractureprocess,respectively.Themicrostructureofthemicroemulsionwasdeterminedbyelectricalconductivityanddifferentialscanningcalorimetrymethod.Meanwhile,theinvitroreleaseprofilesoft
7、hemicroemulsionformula2tionsweredeterminedusingadialysismethod.Results:TheoptimalW/Omicroemulsionformulationwasclearandtransparent,andtheaveragesizeoftheparticleswas6.86nm.ThereleaseofEFE2dwasslowerfrommicroemul2sionthanfromtheEFE2dsolution.Conclusion:TheW/Omicro
8、emulsionmayrepresentaneffectiveoraldeliverysystemforhydrophilicbioactivemacromolecules.[Keywords]earthwormfibrinolyticenzyme;W/Omicroemulsion;oral随着分子生物学技术的日益发