1.Anticaries potential of salivary gland extract
Guangyu CHENG ; Zijin TANG ; Mingxuan TAO
Journal of Practical Stomatology 1996;0(02):-
Objective: To study the anticaries effects of salivary gland extract (SGE). Methods: Dental caries model was established in 80 SD rats by feeding with cariogenic diet 2000 and by infecting with cariogenic bacteria. 20 model rats in each of the 4 experimental group were fed with SGE at 400 mg/kg, 1 500 mg/kg or 5 mg/L of NaF or deionic water respectively,another 20 were fed with ordinary diet as blank control. The anticaries effects were evaluated by Keyes caries scores, SOD activity in blood cells was determined by NBT test. The effect of SGE on dissoluble Ca 2+ from teeth was determined in electrochemical artificial caries model in vitro. Results: caries was not observed in the blank control. According to Keyes caries score, at E, Ds, Dm and Dx levels, the score in SGE groups was significantly lower than that in the model group (P0.05). SGE obviously enhanced SOD activity (P
2.Optimized synthesis process of tofacitinib citrate
Li LIU ; Zijin LIU ; Jun TANG ; Guangwei HE ; Weizhong LIU
Journal of China Pharmaceutical University 2022;53(6):685-689
In order to improve the yield and simplify the operation, the synthesizing process of JAK3 inhibitor tofacitinib citrate was improved based on the analysis of the methods previously published.Using 2, 4-dichloro-7H-pyrrolo [2, 3-d] pyrimidine and (3R, 4R)-1-benzyl-N, 4-dimethylpiperidin-3-amine dihydrochloride as starting materials, tofacitinib citrate was obtained through four steps of nucleophilic substitution, catalytic transfer hydrogenation, cyanide acetylation and citrate salt, and its crystal form was consistent with the original research.After optimization, the yield was better than those reported in literature, and the mild reaction conditions were suitable for industrial production.