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移植技术长足进展在很大程度上归功于发现免疫抑制剂。首选的环孢菌素(CyA)多能成功地抑制移植排斥,无骨髓毒性,术后感染率低,但有肝肾毒性.作者在日本津轻地区土壤中分离培养微生物,于1984年发现了具有抑制混合淋巴细胞反应(MLR)的新免疫抑制剂FK506。该药溶于甲醇、乙醚、丙酮,不溶于水和乙烷。因疏水故消化道吸收常很差。但经剂型研究,发现在丙酮甲基纤维素中的固态散剂,适合口服吸收和稳定性要求.经研究推测,它属大环内脂类,在23环结
Much of the advances in transplantation have been attributed to the discovery of immunosuppressive agents. The preferred cyclosporin (CyA) can successfully inhibit graft rejection, no bone marrow toxicity, postoperative infection rate is low, but with liver and kidney toxicity. The author isolated and cultured microorganisms in soil in Japan Jin light region, found in 1984 A novel immunosuppressive agent FK506 with mixed lymphocyte reaction (MLR) inhibition. The drug is soluble in methanol, ether, acetone, insoluble in water and ethane. Absorption due to hydrophobic so often very poor. However, the dosage form study found that the solid powder in acetone methyl cellulose, suitable for oral absorption and stability requirements.Studied that it is a macrocyclic lipids, in the 23 ring junction