Isolation and Identification of the Major Degradation Impurity of Sirolimus Tablets
OBJECTIVE:To improve the quality of sirolimus tablets,unknown impurity was isolated from sirolimus tablets,and its structural identification and preliminary biological activity were carried out.METHODS:Unknown impurity in siro-limus tablets was isolated by silica gel column chromatography,and then purified by preparativeliquid chromatography tech-nique.The structure was characterized by UV,IR,MS and NMR.Antifugi activity was tested by doubling dilution and anti-tumor activity was detected by sulforhodamine B assay.RESULTS:The purity of the unknown impurity of sirolimus tablets was 96.8%.It was identified as secorapamycin.CONCLUSION:Secorapamycin is the main impurity in the processing of sirolimus tablets,and its biological activity is lower than that of sirolimus.
Sirolimus tabletsSecorapamycinSeparation and purificationStructural characterization
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