Takemoto M, Tsuchida M, Konishi M, Suga A, Iojima K, Naito K
Department of Urology, Yamaguchi University School of Medicine, Japan.
J Pharm Pharmacol. 1997 Jul;49(7):657-60. doi: 10.1111/j.2042-7158.1997.tb06088.x.
The oral adsorbent AST-120 is used to inhibit the progression of renal failure by adsorbing uraemic toxins in the gastrointestinal tract. When AST-120 is administered to patients receiving immunosuppressive medicines, it is important to study the effect of AST-120 on the amount of these and other drugs absorbed. We have, therefore, studied the in-vitro adsorption of cyclosporin by AST-120 and investigated the effect of oral administration of AST-120 on the absorption of cyclosporin in rats. The in-vitro adsorption ratios of AST-120 for cyclosporin were more than 80%. When pure cyclosporin powder was administered with AST-120, blood cyclosporin concentrations were significantly higher than when cyclosporin was administered alone. When cyclosporin dissolved in medium-chain triglyceride was administered to rats by intramuscular injection there was no significant difference in the blood cyclosporin concentration of rats given combined AST-120 and cyclosporin and those given cyclosporin alone. There was no significant difference between the serum concentration of total bile acids, in rats receiving combined oral AST-120 and cyclosporin dissolved in olive oil, and those receiving orally solely a solution of cyclosporin dissolved in olive oil. These results suggest that oral administration of AST-120 accelerates the absorption of orally administered cyclosporin from the gastrointestinal tract and does not affect the metabolism of cyclosporin. When a solution of cyclosporin in olive oil is administered orally, however, oral administration of AST-120 has no influence on cyclosporin absorption and does not affect the enterohepatic circulation of bile acids.
口服吸附剂AST - 120通过在胃肠道吸附尿毒症毒素来抑制肾衰竭的进展。当给正在接受免疫抑制药物治疗的患者使用AST - 120时，研究AST - 120对这些药物以及其他吸收药物量的影响很重要。因此，我们研究了AST - 120对环孢素的体外吸附作用，并研究了口服AST - 120对大鼠体内环孢素吸收的影响。AST - 120对环孢素的体外吸附率超过80%。当纯环孢素粉末与AST - 120一起给药时，血中环孢素浓度显著高于单独给予环孢素时。当将溶解于中链甘油三酯的环孢素通过肌肉注射给大鼠时，联合给予AST - 120和环孢素的大鼠与单独给予环孢素的大鼠血中环孢素浓度没有显著差异。口服AST - 120与溶解于橄榄油的环孢素联合给药的大鼠与仅口服溶解于橄榄油的环孢素溶液的大鼠相比，血清总胆汁酸浓度没有显著差异。这些结果表明，口服AST - 120可加速胃肠道中环孢素的口服吸收，且不影响环孢素的代谢。然而，当口服溶解于橄榄油的环孢素溶液时，口服AST - 120对环孢素吸收没有影响，也不影响胆汁酸的肠肝循环。
