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使用液相色谱-串联质谱法同时测定大鼠血浆中的炔诺孕素、他莫昔芬及其代谢物。

Simultaneous determination of centchroman and tamoxifen along with their metabolites in rat plasma using LC-MS/MS.

作者信息

Rama Raju Kanumuri Siva, Taneja Isha, Singh Sheelendra Pratap, Tripathi Amit, Mishra Durga Prasad, Hussain K Mahaboob, Gayen Jiaur Rahman, Singh Shio Kumar, Wahajuddin Muhammad

机构信息

Academy of Scientific & Innovative Research, New Delhi, India.

出版信息

Bioanalysis. 2015;7(8):967-79. doi: 10.4155/bio.14.253.

DOI:10.4155/bio.14.253
PMID:25966009
Abstract

AIM

Tamoxifen and centchroman are two non-steroidal, selective estrogen receptors modulators, intended for long term therapy in the woman. Because of their wide spread use, there is a possibility of co-prescription of these agents.

MATERIALS & METHODS: We studied the probable pharmacokinetic interaction between these agents in breast cancer model rats. A simple, sensitive and rapid LC-ESI-MS/MS method was developed and validated for the simultaneous determination of tamoxifen, centchroman and their active metabolites.

RESULTS

The method was linear over a range of 0.2-200 ng/ml. All validation parameters met the acceptance criteria according to regulatory guidelines.

CONCLUSION

LC-MS/MS method for determination of tamoxifen, centchroman and their metabolites was developed and validated. Results show the potential of drug-drug interaction upon co-administration these two marketed drugs.

摘要

目的

他莫昔芬和醋甲孕酮是两种非甾体类选择性雌激素受体调节剂,用于女性的长期治疗。由于它们的广泛使用,存在这两种药物联合处方的可能性。

材料与方法

我们在乳腺癌模型大鼠中研究了这两种药物之间可能的药代动力学相互作用。开发并验证了一种简单、灵敏且快速的液相色谱 - 电喷雾串联质谱(LC - ESI - MS/MS)方法,用于同时测定他莫昔芬、醋甲孕酮及其活性代谢物。

结果

该方法在0.2 - 200 ng/ml范围内呈线性。所有验证参数均符合监管指南的验收标准。

结论

开发并验证了用于测定他莫昔芬、醋甲孕酮及其代谢物的LC - MS/MS方法。结果表明,同时服用这两种上市药物时存在药物相互作用的可能性。

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