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논문 기본 정보

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학술저널
저자정보
Anjna Sharma (CSIR- Indian Institute of Integrative Medicine) Asmita Magotra (CSIR- Indian Institute of Integrative Medicine) Santosh Kumar Rath (CSIR- Indian Institute of Integrative Medicine) Priya Wazir (CSIR- Indian Institute of Integrative Medicine) Utpal Nandi (CSIR- Indian Institute of Integrative Medicine) Surrinder Koul (CSIR- Indian Institute of Integrative Medicine) Payare Lal Sangwan (CSIR- Indian Institute of Integrative Medicine) Ajai Prakash Gupta (CSIR- Indian Institute of Integrative Medicine) Gurdarshan Singh (CSIR- Indian Institute of Integrative Medicine)
저널정보
한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제48권 제5호
발행연도
2018.9
수록면
565 - 574 (10page)
DOI
10.1007/s40005-017-0350-8

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Plant derived natural products have been the major source for treatment of diseases traditionally but with the advent of modern systems of medicine, there is need to explore the active constituents present in it followed by modification for better therapeutic activity, low toxicity and favorable pharmacokinetics to become a drug molecule. A simple, rapid and sensitive high-performance liquid chromatography?tandem mass spectrometry (LC? MS/MS) method was developed and validated according to Food and Drug Administration guidelines for determination of IS01957, a derivative of naturally occurring para coumaric acid in mice plasma. The extraction of the analyte and the internal standard (Carbamazepine) from the plasma samples involved protein precipitation using acetonitrile. Results of validation parameters were met with the acceptance criteria of the FDA guidelines. Method was highly sensitive (5 ng/mL) that could determine very low concentration of compound in plasma The developed and validated method was successfully applied to determine compound’s metabolic stability in mouse liver microsomes (MLM) and human liver microsomes (HLM). Test compound was found to be stable in MLM and HLM in the experimental conditions. Metabolic stability data was extrapolated which was further correlated to pharmacokinetics study in mice through oral, intraperitoneal and intravenous administration. In-vitro half life was found to be greater than 2 h in both MLM and HLM. Hepatic extraction ratio of the compound was found to be in the intermediate range. Pharmacokinetic evaluations revealed that it is a suitable candidate for intraperitoneal as well as oral administration.

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