Introduction: The drug analyses processes include a number of steps starting from samples collection to the final reporting of the results. The process of the drug extraction is usually, time consuming, labour-intensive, complex and prone to contamination. Therefore, the drug extraction can be considered to be one of the most important stages because it is a possible source of inaccuracy in the overall analysis. Objective: The aim of this work is fabricating a new material with the ability to pre-concentrate drugs of abuse in biological fluids with high extraction efficiency. This was achieved by the fabrication of silica-based monolithic materials, followed by chemical on column modifications of the silica surface with active lysine groups. Method: The columns modifications were characterised by using different analytical techniques, such as Brunauer EmmettTeller (BET) analysis and scanning electron microscopy (SEM) coupled with energy dispersive X-ray (EDAX) analysis. Result: In this study, the isolation of non-steroidal anti-inflammatory drugs (NSAIDs), namely acetylsalicylic acid and ibuprofen (IBP), was achieved successfully by using an active lysine silica monolith in which the drugs were adsorbed on solid support while any contaminants were removed by washing the monolithic materials; finally the purified drugs were eluted from the monolithic material. Conclusion: The promising results indicated that the extraction efficiencies of the two NSAIDs were both more than 85%. Linearity was obtained in the range of 10-100 ng ml-1. The intra- and inter-monolithic columns indicated good monolith reproducibility, with relative standard deviations (RSDs) of less than 4.4% and 6.1%, respectively.