Bioanalytical method development for momordicinin and its application to long term pharmacokinetics in diabetic rats.

Abstract

OBJECTIVE\nTo develop and validate bioanalytical RP-HPLC method to evaluate pharmacokinetics and tissue distribution pattern of momordicinin (MRN).\n\n\nSIGNIFICANCE\nMRN is one of the major cucurbitane triterpenoid found in Momordica charantia linn (MC). However MRN has not been explored for its pharmacokinetic profile, tissue distribution and stability in order to establish it as an antidiabetic agent.\n\n\nMETHODS\nIn 28\u2009days pharmacokinetic study, 54 diabetic male wistar rats were divided in three different groups and administered with 25, 50, 100\u2009mg/kg MRN orally. The blood samples were collected at 1, 7, 14, 21 and 28th day of the treatment and plasma quantification of MRN was done by validated RP-HPLC method. The rats were sacrificed at end of the study for tissue distribution.\n\n\nRESULTS\nThe developed method was successfully applied to investigate pharmacokinetic profile of MRN. In pharmacokinetic analysis the Cmax for 25, 50 and 100\u2009mg/kg was found to be 8.412, 10.443 and 11.829\u2009µg/ml respectively suggesting the dose dependent activity. The maximum plasma concentration was achieved at 2\u2009h for all doses. MRN showed major distribution in liver followed by kidney, spleen and pancreas.\n\n\nCONCLUSION\nThe newly developed and validated method was used to assay MRN in plasma as well as in tissues to evaluate pharmacokinetics of the drug for the first time. Undoubtedly, these findings can be taken into consideration while concluding its therapeutic effects after oral administration.