摘要
目的:考察促进环孢素A(cyclosporine A,CsA)肠道吸收的机制及其剂型因素。方法:与CsA胶囊(商品名:新山地明,Neoral)为对照,比较CsA脂质体(cyclosporine A-liposome,CsA-Lip)、环孢素-A-EudragitL100纳米粒(cyclosporine A-Eudragit L100-nanoparticles,CsA-L100-NP)和环孢素A-Eudragit S100纳米粒(cyclosporine A-Eudragit S100-nanoparticles,CsA-S100-NP)以及吸收促进剂,如去氧胆酸钠(SDCh)、十二烷基磺酸钠(SDS)、泊洛沙姆(poloxamer)和羟丙基-环糊精(HP-β-CD)等在大鼠肠道各段透膜的促吸收机制及其影响因素。结果:CyA-Lip和Neoral在十二指肠、空肠的通透系数显著大于CsA-L100-NP和CsA-S100-NP(P<0.05);回肠中CsA-Lip的通透系数明显大于Neoral、CsA-L100-NP和CsA-S100-NP(P<0.05),而3种制剂之间的吸收速率差异无统计学意义(P>0.05)。结论:CsA-Lip具有更明显的促进吸收作用。
Objective：To study the mechanism to promote intestinal absorption of cyclosporine A（cyclosporine A,CsA） and the formulation factor that affects absorption.Methods：Comparing the mechanism to promote absorption across the membranes at different intestine segments of the rat and influencing factors of neural,cyclosporine A liposome（CsA-Lip）,cyclosporine A-EudragitL100（CsA-L100-NP）,cyclosporine A-EudragitS100（CsA-S100-NP） nanoparticles and the absorption enhancers：including sodium deoxycholate,sodium dodecyl sulfate poloxamer and H-CD.Results：Permeability coefficients of CsA-Lip and Neoralare much higher than those of CsA-L100-NP and CsA-S100-NP in the duodenum,jejunum（P 0.05）;the absorption of NeoralCsA-L100-NP and CsA-S100-NP have no significant differences in the ileum（P0.05）,and CsA-Lip＇s permeability coefficient is significantly larger than that of the other three agents（P0.05）.Conclusion：The liposome has more obvious impact on promoting absorption.
出处
《抗感染药学》
2010年第4期246-250,共5页
Anti-infection Pharmacy
基金
国家科技支撑计划课题基金(编号:2006BAI09B00)
国家科技部科技型中小企业技术创新基金(立项代码:07C26223201333)
江苏省卫生厅招标课题(编号:H200630)
关键词
环孢素A
吸收
剂型
影响因素
CsA
absorption
formulation
influencing factors
