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他莫昔芬柠檬酸盐具有抗雌激素性质,用于治疗人乳腺癌。他莫昔芬中乙烯双键可形成几何异构体(E和Z)。活性药物Z-他莫昔芬含有少量E异构体副产物。最新的美国药典和英国药典采用不同的HPLC分离这两种异构体(E异构体不得超过1%),但USP方法缺少稳定性指征,BP采用的碱性流动相对固定相有损害作用。本文报道的HPLC没有上述缺点。两种异构体分离完善,具有稳定性指征,可用于分析原料药及片剂中他莫昔芬柠檬酸盐和E异构体杂质,精密、准确、快速和实用,柱的寿命也较长。
Tamoxifen citrate has anti-estrogenic properties and is used to treat human breast cancer. Tamoxifen double bonds can form geometric isomers (E and Z). The active drug Z-tamoxifen contains a small amount of the E isomer byproduct. The latest United States Pharmacopoeia and British Pharmacopoeia use separate HPLC separations of these two isomers (E isomers should not exceed 1%), but the USP method lacks stability indications and the basic mobile phase used by BP is detrimental to the stationary phase . The HPLC reported here does not have the above drawbacks. The two isoforms are well separated and have indications of stability and can be used to analyze tamoxifen citrate and E isomer impurities in APIs and tablets, with precision, accuracy, speed, and utility, and longer column life long.