ABSTRACT:The current work offers a rigorous way for the microwave‐assisted synthesis of N and S doped carbon quantum dots (QDs). The latter are deemed highly sensitive and selective fluorescence sensors that were widely investigated in pharmaceutical analysis. Quenching of luminescence of the prepared QDs in lab fabricated sensor at λ emission = 418 nm after excitation at 370 nm was implemented to quantify the anti‐HCV drug Ledipasvir (LDP). LDP showed a linear response within the dynamic range of 1–40 μM. The calculated LDP detection and quantification limits were 313.06 and 948.67 nM, respectively. Besides the analysis of LDP in bulk and commercial dosage form, the scope of application extended to evaluate the effect of the nutraceutical silymarin (liver support) on the excretion of LDP in rat feces. The compliance with the green and white analytical chemistry fundamentals is comprehensively investigated and compared with selected versatile reported procedures. Numerous prevalent metrics, namely, analytical eco‐scale, AGREE, RGB12, RGB fast, BAGI, and complex GAPI, were employed. Our developed fluorometric procedure demonstrated great sensitivity, selectivity, and functionality that outperformed other sophisticated platforms. Thus, the utility of the depicted procedure in pharmaceutical analysis and studying pharmacokinetics aspects is profoundly proven.