The present invention discloses a use of lotus procyanidin as an advanced glycosylation end product formation inhibitor. The drug composition adopting the lotus procyanidin as a main active component comprises the following nature active component extracts, by weight, 70-80% of lotus procyanidin, 10-20% of a synergist such as VE, VC, epigallocatechin gallate (EGCG), cysteine and other ??complexes, and 5-10% of other nature extracts such as a lotus leaf extract, a ginkgo leaf extract and the like. According to the present invention, a high performance liquid chromatography method is adopted to detect a methylglyoxal removing effect of the lotus procyanidin and the main structure unit thereof (catechin), wherein methylglyoxal is an important intermediate substance during an advanced glycosylation end product formation process; a high performance liquid chromatography / multi-stage mass spectrometry method is adopted to identify adducts of four catechin and methylglyoxal and adducts of nine lotus procyanidin and methylglyoxal; and results show that lotus procyanidin provides good inhibition effects for advanced glycosylation end product formation in simulated physiological environments and simulated food systems.