气滞胃痛颗粒为理气类中成药,由柴胡、延胡索、枳壳、香附、白芍、甘草6味中药组成,功效为舒肝理气、和胃止痛.由于本复方制剂含有多味药材,且每味中药又含有多种化学成分,故对其进行质量控制尤为重要.此药对胃炎、功能性消化不良、肠易激综合征、反流性食管炎等消化系统疾病具有明确疗效.本文对气滞胃痛颗粒质量控制与临床应用的研究进展进行综述,以期为本药品的质量控制与临床合理用药提供参考.

Context: Pharmacokinetics of drug may be altered by abnormal physiological functions in illness, which will affect its pharmacodynamic efficacy in turn.Objective: To assess the preventive effects of tetramethylpyrazine (TMPZ) phosphate on hepatocarcinogenesis and its pharmacokinetic differentiations in model mice.Methods: Diethylnitrosamine (DEN) was adopted to induce hepatic precancerous model in mice through intraperitoneal injection, and prevention efficacy of TMPZ at a dose of 162 mg/kg was examined by liver histological analysis and activities of serum marker enzymes. Pharmacokinetic variations of TMPZ between control and model mice were measured for single oral administration.Results: DEN initiation led to a remarkable increase of serum marker enzymes, and abnormality such as bile canaliculi hyperplasia and presence of tumor cells were observed in liver histopathological examination in model mice, while the control ones revealed normal architecture. Oral treatment of TMPZ resulted in a marked reduction in serum marker enzymes and improvement in liver histopathology compared with model ones. In pharmacokinetic study, values of AUC and T-max of TMPZ became significantly greater with increase of doses in both control and model mice, which elucidated the absorption was enhanced and delayed; meanwhile, its elimination was not affected markedly. When the mice were treated at same dose, the adsorption of TMPZ in model mice was greatly improved than that in control ones, while T-max and MRT had no significant difference.Conclusion: TMPZ was partly effective to protect liver from carcinogenesis initiated by DEN, and hepatic insufficiency could change its pharmacokinetics.

Objective: To confirm the protective effect of curcumin on diethylnitrosamine(DEN)-induced hepatic precancerous lesions in mice.Method: The male mice were randomly divided into four groups.The hepatic precancerous lesions in mice were replicated with DEN(95 mg·kg-1) intraperitoneal administration once a week for 10 weeks,meanwhile curcumin(120.0 mg·kg-1) with or without Rhizoma Dioscoreae(3.03 g·kg-1) was administrated intragastrically once a day to protect the hepatic precancerous lesions.On the 71st day,the blood was collected to detect the hepatic injury biomarkers,and partial liver was fixed to observe the pathological changes.Result: Compared with those in the control mice,the hepatic precancerous lesions in the model mice were confirmed as the alterative and proliferative changes of liver,the proliferative hepatocytes were demonstrated as the atypia similar to hepatic carcinoma,the alterative changes were supported by the elevated activities of serum ALT(195.57±91.56) U·L-1,AST(39.68±24.20) U·L-1 and GST(42.31±8.19)U·L-1.The administration of curcumin relieved the hepatic precancerous lesions significantly(P<0.01),and the combination use of curcumin and Rhizoma Dioscoreae could enhance the effect(P<0.05) in the treatment groups with ALT(82.75±38.54) U·L-1,AST(30.32±7.80) U·L-1and GST(24.61±7.58) U·L-1,respectively.Conclusion: Curcumin can protect the hepatic precancerous lesions in the mice attacked by diethylnitrosamine,and combination use of curcumin and Rhizoma Dioscoreae can be more effective.

Objective:To observe the effect of ursolic acid on hepatic precancerous lesion in mice.Methods:Except for rats in control,model rats were intraperitoneally injected with diethylnitrosamine(DEN) for inducing hepatic precancerous lesions.Ursolic acid(225.0mg/kg) or it(112.5 mg/kg) with medlar Abstraction(1 200.0mg/kg) was administrated intragastricall for treating the lesions in 10 weeks.Hepatic function was detected as ALT,AST,ALP,GST.Pathological changes were observed under microscopy and their degrees were evaluated by morphormetry.Results:Compared with those of control rats,the hepatic precancerous lesions of model rats were indicated as the hepatic dysfunction as elevated ALT,AST,ALP activities in sera,the hepatic cirrhosis as decreased hepatic indexes,collagen deposition and pseudolobule formation,and the atypia of hepatocytes as the increased nuclear volloms.The lesions in model rats were confirmed with their morphormetries.The pathological changes were relived with ursolic acid,more with the ursolic acid jointed with medlar Abstraction.Conclusion:Ursolic acid has the potency to relieve hepatic precancerous lesions.This effect was enhanced with medlar.