In vitro Metabolism of Risperidone on Isolated Microsomes of Rat Liver: Metabolite Identification and Profiling by RP-HPLC and LC-MS Techniques

Indian Journal of Pharmaceutical Education and Research

  • Prutha Shirodkar1Department of Pharmaceutical Chemistry, S.M.B.T. College of Pharmacy, Nashik, Maharashtra, INDIA.
  • Harshal Chavan2Department of Pharmaceutical Chemistry, Sandip Foundation’s, Sandip Institute of Pharmaceutical Sciences, Nashik, Maharashtra.
  • Rajendra Mogal3Department of Pharmaceutics, Sandip Foundation’s, Sandip Institute of Pharmaceutical Sciences, Nashik, Maharashtra, INDIA.
  • Avinash Dhake1Department of Pharmaceutical Chemistry, S.M.B.T. College of Pharmacy, Nashik, Maharashtra, INDIA.

Volume 53 Issue 2s Pages s179-s185

DOI: 10.5530/ijper.53.2s.64

Abstract

Objective: The objective of present research work is to study in vitro metabolism of risperidone on isolated microsomes of rat liver. Methods: Its biotransformation was examined using isolated microsomes derived from rat livers. Their separation was accomplished on Jasco RP-HPLC C-18 column (250mm x 4.6mm x 5µm) using methanol: 50mM Potassium dihydrogen phosphate (50:50 %v/v) mobile phase, detected at a wavelength of 280nm. Results: In vitro metabolism of RIS was investigated using the cytochrome P450 (CYP450) enzymes supplemented with an NADPH- generating system. Incubation of RIS with rat liver microsomes resulted in the formation of 2 major hydroxy metabolites. Conclusion: Formation of all the metabolites is correlated with Phase I biotransformation CYP enzyme subfamilies. The method was extended to LC-MS for further characterization of the metabolites using standards and the probable metabolites were proposed.

Keywords

  • RIS
  • Microsomes
  • Cytochrome P450
  • Biotransformation
  • LC-MS
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