DEVELOPMENT AND VALIDATION OF UV SPECTROSCOPIC METHOD FOR ESTIMATION OF ABACAVIR IN TABLET DOSAGE FORM

Objective: To develop and validate simple, rapid, linear, accurate, precise and economical UV Spectroscopic method for estimation of Abacavir in tablet dosage form. Methods: The drug is freely soluble in analytical grade methanol. The drug was identified in terms of solubility studies and on the basis of melting point done on the melting point apparatus of Equiptronics. It showed absorption maxima were determined in analytical grade methanol. The drug obeyed the Beer’s law and showed good correlation of concentration with absorption, which reflect in linearity. The UV spectroscopic method was developed for estimation of Abacavir in tablet dosage form and also validated as per ICH guidelines. Results: The drug is freely soluble in analytical grade methanol, slightly soluble in water and practically insoluble in ethanol. So, the analytical grade methanol is used as a diluent in method. The melting point of Abacavir was found to be 164-165 ˚C (uncorrected). It showed absorption maxima 256 nm in analytical grade methanol. On the basis of absorption spectrum the working concentration was set on 15µg/ml (PPM). The linearity was observed between 5-25 μg/ml (PPM). The results of analysis were validated by recovery studies. The recovery was found to be 98.75, 101 and 99.17% for three levels respectively. The % RSD for precision was found to be 0.32% and for Ruggedness is 0.46% Conclusion: A simple, rapid, linear, accurate, precise and economical UV Spectroscopic method has been developed for estimation of Abacavir in tablet dosage form. The method could be considered for the determination of Abacavir in quality control laboratories

SYNTHESIS AND ANTICANCER SCREENING OF TRIAZINE ANALOGUES

Objective: The study was aimed to investigate the cytotoxic effect of S-5H-[1,2,4]-triazino (5,6-b) indol-3-yl-3,4-phenylethane-thioate derivatives as epidermal growth factor Receptor (EGFR) inhibitors. Methods: In the present study 14 novel triazine analogues were synthesized and characterized using different spectroscopic techniques such as FT-IR, NMR and Mass Spectroscopy. The anticancer activity was performed using MCF-7 (breast cancer) and K-562 (leukaemia) cell lines. Further, molecular docking was carried out using Vlife Molecular Docking Software (MDS) on crystal structure of epidermal growth factor receptor (EGFR) to identify the binding mode of interaction with an active site. Results: Compounds MA-7, MA-8, MA-12, MA-13 and MA-14 show potent activity against cancer cell lines in the range of<10 to 84.4 µg/ml. Further molecular docking on EGFR also supports that there is a strong correlation between in silico and in vitro biological activity. The results of this study may be further useful for lead optimization process. Conclusion: The results of this study indicates that the synthesized triazine analogues can give a potential lead as an anticancer agent