Sai Laxmi Kesana1*, Dodle Jaya Prakash1, Vamaraju Harinadha Babu2, P.C .Sastry3
1College of Technology, Osmania University- 500007, Telangana, India
2G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad – 500028, Telangana, India
3Institute of Engineers, Kolkata-700020, West Bengal, India
*Address for Corresponding Author
Sai Laxmi K.
G. Pulla Reddy College of Pharmacy,
Mehdipatnam, Hyderabad – 500028, Telangana State, India
Background: Metabolite profiling has become one of the main drives 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. Objective: The main objective of this work is to build an in vitro methodology for identification of the probable metabolites and the extent of metabolism in various species. Material and methods: 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 metabolites identified were confirmed by MS/MS and Accurate mass analysis using the analytical tool LC-Q-TOF Mass spectrometry. Results and conclusion: The major metabolic pathway was through oxidation and metabolites identified are 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. Tamsulosin is more stable in human and less in rat showing there is species difference in its in vitro metabolism.
Keywords: Tamsulosin, Microsomes, UPLC, Xevo QTOF