Mon, 18 Dec 2017

In Vitro Metabolite Identification of Tamsulosin Using LC-Q-TOF Mass Spectrometry

Laxmi1, , Dodla Jaya Prakash1,Harinadha babu2, Venkataiah3

1.G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad,– 500028, Telangana State, India

2.Department of Chemical Technology, Osmania University- 500007 , Telangana State, India

3.Indian Institute of Chemical Technology, Tarnaka, Hyderabad – 500007, Telangana State, India.

 


ABSTRACT

Metabolite profiling has become one of the main drive in the drug discovery process to optimize pharmacokinetic properties and to increase the success rate of drugs. In vitro metabolism of Tamsulosin, the only alpha-1 adrenoceptor antagonist used in treatment of benign prostatic hyperplasia was investigated in several species. Tamsulosin was incubated with liver microsomes of Human, Rat and Dog. Simultaneous extraction and separation technique in combination with high resolution accurate mass spectrometric detector was used for the parent and the metabolite identification. The major metabolic pathway was through oxidation and metabolites identified were found to be M1, M2, M3, M4, M5 and M6. These are confirmed by MS/MS and Accurate mass analysis using the analytical tool, LC-Q-TOF Mass spectrometry. Overall, Tamsulosin is more stable in human and less in rat showing there is species difference in its invitro metabolism.

Keywords: Tamsulosin, Microsomes, UPLC, Xevo QTOF.


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