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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 investigate the mechanism of promoting intestinal absorption of cyclosporine A (CsA) and its dosage form factors. METHODS: CsA-Lip, cyclosporine A-liposome and cyclosporine A-liposome were compared with CsA capsule (trade name: Neoral) Eudragit L100-nanoparticles, CsA-L100-NP and cyclosporine A-Eudragit S100-nanoparticles, and absorption enhancers such as sodium deoxycholate (SDCh) , Sodium dodecyl sulfate (SDS), poloxamer and hydroxypropyl-β-cyclodextrin (HP-β-CD) Its influencing factors. RESULTS: The permeation coefficients of CyA-Lip and Neoral in duodenum and jejunum were significantly higher than those in CsA-L100-NP and CsA-S100-NP (P <0.05). The permeability coefficient of CsA-Lip in ileum was significantly higher than that in Neoral , CsA-L100-NP and CsA-S100-NP (P <0.05). There was no significant difference in absorption rate between the three preparations (P> 0.05). Conclusion: CsA-Lip has a more obvious role in promoting absorption.