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Objective: To study the physiopathologic basis of Weikangfu Granule ( 胃康复冲剂, WKFG)in treating precancerosis of gastric mucosa in patients of chronic gastritis with Pi-deficiency syndrome (CG-PDS). Methods: One hundred and fifteen patients of CG-PDS who suffered from intestinal metaplasia (IM)and atypical hyperplasia (ATHP) of gastric mucosa, were divided into two groups. The treated group (n =61 ) was treated by WKFG with its ingredients modified according to the syndrome type of patients. The constructural changes were detected by optical microscope, screening electronic microscope, transmission electronic microscope and histochemical staining; the nuclear and mitochondrial ultrastructure of gastric mucosa were analyzed with energy dispersion X-ray analyser and image analysis system. And the changes of cAMP,lipid peroxide (LPO), superoxide dismutase (SOD) before and after treatment in the treated group were measured and compared with those of the health control group consisting of 15 volunteers. Results: The symptomatic and pathological therapeutic effect in the treated group were significantly superior to those in the control group (P＜0.05). The contents of Zn, Cu, cAMP, SOD and 3H-TdR LCT in gastric mucosa of the treated group before treatment were all lower than those of the healthy control group, yet all these indexes markedly increased after treatment, while serum LPO level, which increased before treatment was lowered after treatment. All the changes showed statistical significance (P＜0.05 or P＜0.01). Conclusion: WKFG can reverse IM and ATHP in patients of CG-PDS, and the effect may be realized by way of increasing the level of Zn, Cu, cAMP and SOD in gastric mucosa, promoting cell differentiation, enhancing cellular immunity and reducing oxygen free radicals and lipid peroxidation.