Gouteng Xuanshen Granules, as an institutional preparation of Shandong University of Traditional Chinese Medicine Affiliated Hospital, have shown significant efficacy in reducing blood pressure, but their mechanisms of action are not yet fully understood. This study used HPLC-MS to perform non-targeted metabolomics analysis on serum samples from subjects, including those with prehypertension (PHT) and healthy individuals. TCMSP was used to identify the active components of Gouteng Xuanshen Granules. Databases like Gene Cards and OMIM were used to predict potential targets related to normal high blood pressure and to explore the antihypertensive effects of the granules on PHT. The study recruited 20 patients with prehypertension meeting the diagnostic criteria into the PHT group (Group P) and 20 healthy volunteers into the control group (Group C). The prehypertension group was administered Gouteng Xuanshen Granules (Group GT). The study was approved by the Ethics Committee of Shandong University of Traditional Chinese Medicine Affiliated Hospital, and informed consent was obtained from all participants [ethical review approval number: (2022) Lun Review No. (036)-KY]. All subjects underwent four lipid tests and blood pressure measurements. Blood samples were collected once before and after administration of the granules in the prehypertension group, and once at enrollment in the control group. HPLC/MS was used to analyze serum samples from all subjects. The results showed that after administration of the granules, patients with prehypertension had a significant decrease in blood pressure and changes in the four lipid parameters. Metabolomics analysis revealed significant changes in purine metabolism, arginine biosynthesis, and sphingolipid metabolism after granule administration. Network pharmacology analysis suggested that the granules primarily exert their antihypertensive effects by acting on targets such as SIRT1, STAT3, and AKT1. This study provides preliminary insights into the metabolic differences among healthy individuals, those with prehypertension, and the treatment group, offering valuable references for the prevention and treatment of prehypertension. The study preliminarily analyzed the metabolic differences among healthy individuals, patients with elevated blood pressure within the normal range, and those treated with Gouteng Xuanshen Granules, providing valuable reference for the prevention and treatment of elevated blood pressure within the normal range.