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目的:探讨姜黄素-羧甲基壳聚糖偶联物对环孢素肠吸收的影响,为其临床应用提供理论基础。方法:采用大鼠在体单向肠灌流实验,用HPLC测定灌流液中环孢素的含量,计算不同浓度的姜黄素(Cur)、羧甲基壳聚糖(CMCS)、CMCS-Cur(CC)、CMCS-EDA-Cur(CEC)对环孢素在十二指肠和空肠的表观吸收速率常数(Ka)和肠壁有效通透性系数(Peff)的影响。结果:在十二指肠和空肠部位,加入Cur、CMCS、CC、CEC的实验组环孢素的Ka和Peff值高于单纯环孢素组(P<0.05);0.1%CsA&CMCS组高于0.1%CsA&Cur组(P<0.05);0.1%CEC&CsA组Ka、Peff值高于0.01%和1%CEC&CsA(P<0.05)。结论:Cur、CMCS、CC、CEC均能促进CsA在十二指肠和空肠部位的吸收,相同浓度下CMCS的促环孢素吸收作用优于Cur。
Objective: To investigate the effect of curcumin-carboxymethyl chitosan conjugate on the absorption of cyclosporin, providing a theoretical basis for its clinical application. Methods: The rats were subjected to unilateral intestinal perfusion in vivo. The content of cyclosporine in the perfusate was determined by HPLC. Curcumin, carboxymethyl chitosan (CMCS) and CMCS-Cur (CC) , CMCS-EDA-Cur (CEC) on the apparent absorption rate constant (Ka) and effective permeability coefficient (Peff) of ciclosporin in the duodenum and jejunum. Results: In the duodenum and jejunum, the Ka and Peff values of cyclosporin in the experimental group were significantly higher than those in the cyclosporin alone group (P <0.05), while those in the 0.1% CsA & CMCS group were higher than 0.1 (P <0.05). The Ka and Peff values in 0.1% CEC & CsA group were higher than those in 0.01% and 1% CEC & CsA groups (P <0.05). CONCLUSION: Curcumin, CMCS, CC, and CEC can promote the absorption of CsA in the duodenum and jejunum, respectively. The cytotoxicity of CMCS is better than Cur in the same concentration.