Proactive surveillance of foodborne bioactives by integrated dietary exposure and urinary excretion assessment.

Unintentional ingestion of pharmacologically-active substances through foods and dietary supplements presents growing challenges for food safety and anti-doping regulation. We developed a high-throughput LC-MS/MS platform to simultaneously screen 331 compounds and quantify 214 analytes, with matrix-matched validation in pork, oat, and beverage. The method showed applicability across ten food types and was applied to seventy-eight commercial products, revealing frequent detection of bioactives such as octopamine, coclaurine, and olodaterol. Simulations of dietary exposure and urinary excretion demonstrated that some of these substances exceed World Anti-Doping Agency reporting thresholds under realistic consumption scenarios, risking adverse analytical findings even without intentional use. This study presents an integrated framework linking analytical detection with exposure assessment, enabling proactive identification of regulatory-relevant substances across complex food matrices. The approach provides a practical tool for monitoring foodborne chemical exposure and supports risk management for both the general population and athletes subject to strict doping control standards.