【摘要】 目的对比研究2种不同苦参碱自纳米乳化制剂肠淋巴转运差异。方法采用大鼠三重在体单向肠灌流(T-SPIP)实验,以苦参碱原药为参比,利用乳糜流动阻断剂(秋水仙碱),对比研究2种不同苦参碱自纳米乳化制剂在大鼠不同肠段淋巴吸收特性的差异。结果自乳化制剂粒径小且分布均匀,在大鼠的不同肠段均有较高吸收,苦参碱磷脂复合物自纳米乳化制剂(MPC-SN)在回肠段渗透系数最高,且受乳糜流动阻断剂的影响最大。结论自乳化制剂可通过肠淋巴通道增加药物吸收。脂溶性高且粒径较小的苦参碱-磷酸复合物自乳化纳米粒(MPC-SN)更易经肠淋巴系统转运。更多还原

【Abstract】 OBJECTIVE To investigate the differences of two matrine( MA) self-nanoemulsifying drug delivery systems( SNEDDS) in intestinal lymphatic transport. METHODS Triple single pass intestinal perfusion model( T-SPIP) was established to study the intestinal absorption kinetics of MA in different absorption segments of rats with chylomicron flow blocking approach using colchicine as the blocker. The concentration of MA in the perfustae was measured by HPLC. RESULTS The two SNEDDSs had regular spherical surface and narrow particle size distribution. MA showed high P eff. The phospholipid complex formulation( MPC-SN) exhibited higher intestinal lymphatic transport especially in distal ileum,and it was influenced more significantly by the chylomicron flow blocker in distal ileum compared to in proximal jejunum and mid-small intestine. CONCLUSION SNEDDS can improve the absorption of MA by intestinal lymphatic transport. MPC-SN might be easier to be absorbed via lymphatic transport because of its high lipophilicity and small particle size.更多还原