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URINE EXCRETION STUDY OF TAMOXIFEN METABOLITE, 3-HYDROXY-4-METHOHY TAMOXIFEN BY GC-MS

15 Jan 2016

Background; Tamoxifen, is a first-generation selective estrogen receptor modulator which  is widely used for adjuvant breast cancer therapy. Tamoxifen metabolite completely bind to estrogen receptor on tumors as well as other tissues and target a nuclear complex that decreases DNA synthesis and inhibits estrogen effects. But these Selective Estrogen Receptor Modulators (SERMs)  are classified as Prohibited substances according to the list of forbidden substances in sports by the World Anti-Doping Agency(WADA) In sports male athletes use tamoxifen in fighting against increase of estrogen level in the body, breast swelling , gynecomastia and fat forming a pear-silhouette very successfully. Aim; In the present study  Tamoxifen was investigated carefully by administering to a Healthy volunteer . Material And Method; Urine samples are collected at different hours  from 1st day to 5th day and analyzed by GC-MS. Result; It was  found that Tamoxifen is rapidly metabolized in to their metabolite 3-hydrohy-4-methoxy Tamoxifen. Urinary extracts were analyzed by Gas Chromatography-Mass spectrometric Detector by using Selective ion modulator(SIM) and targeted GC-MS techniques with accurate mass. By the GC-MS study it is observed that 3-hydroxy-4-methoxy Tamoxifen metabolite gives two neutral loss m/z value at 58 & 72,  but m/z value 58 shows more abundance than 72m/z value, hence it was selected as the marker m/z  value to check the presence of metabolite in urine. Conclusion; After oral administration, Tamoxifen metabolite can be detected in to their maximum period up to 5 days.

 

Click here to view the full article which appeared in Journal of Drug Delivery and Therapeutics