AIM: To examine the pharmacodynamics of a self-developed oral colon-specific delivery coated tablets of 4-aminosalicylic acid (4-ASA) on rats. METHODS: Ulcerative colitis rat model was developed by intrarectal administration of 2, 4, 6-trinitrobenzenesulfonic acid (TNBS) in alcohol. Rats were divided randomly into healthy control group, TNBS control group, TNBS + lower dose (coated tablets) group, TNBS +medium dose (coated tablets) group, TNBS + higher dose (coated tablets) group, TNBS + sulfasalazine (SASP) group, TNBS + medium dose non-coated tablet group. Several indices including macroscopic change,histological damage, and tissue myeloperoxidase (MPO) activity were examined after 5 consecutive oral drug administration to assess pharmacodynamics of the coated tablets. RESULTS: An experimental ulcerative colitis in rats was induced by TNBS. Compared with 4-ASA non-coated tablet group, decreased macroscopic and histological damage score and lower MPO activity were observed after the oral administration of 4-ASA coated tablets or SASP. There was no significant difference between the effects on the indices of higher dose of coated tablets and SASP (P ＞ 0.05) CONCLUSION: The self-made 4-ASA oral colon-specific delivery coated tablet showes higher effect than non-coated tablets to treat ulcerative colitis in rats.

AIM:To establish the method of determining sodium new houttuyfonate in plasma and study its pharmacokinetics in beagle dogs.METHODS:The HPLC was employed with chromatographic conditions,such as octa-silicane bond silica gel column(250 mm?4.6 mm,5 ?m)as analytical column,methanol-water-ammonium hydroxide with 4 butyls(70 ∶30 ∶0.3)as mobile phase and at the flow-rate of 1.0 mL/min.The UV detection was set at 286 nm.The pharmacokinetic parameters were calculated by DAS(ver 1.0)program and compared by statistic analysis.RESULTS:The calibration curve was linear in blood plasma over the concentration range of 0.128～25.575 mg/L(r= 0.999 2),good precision and high recoveries.The parameters were T_ max= 5.0 min,C_ max= 4.982 mg/L,T_ 1/2=8.67 min.CONCLUSION:The analytical method established in this study is sensitive and exact,and can be used to measure the pharmacokinetics of sodium new houttuyfonate in beagle dog.The sodium new houttuyfonate can metabolize quickly following intravenous injection.

Objective:To analyze the results of syphilis specific serological tests among entry personnel in Beijing port during year 201 2 -201 4 in order to provide evidence for the prevention and control of syphilis.Methods:Demographics data and syphilis specific test results of entry personnel were obtained from the information system of Beijing International Travel Healthcare Center and input into Excel 201 6. Database for entry personnel was built up accordingly and was analyzed by IBMSPSS22.0.Results:The number of entry personnel in Beijing port during year 201 2 -201 4 was 1 06 302 person-time.According to the evaluation criteria,71 308 persons were recruited and analyzed,of whom 277 were tested serologi-cally positive and the total prevalence was 0.39% (95% CI:0.34% -0.43%).The prevalence was highest in the persons aged 40 -49 years (0.81 %)and was higher in males (0.50%)than in females (0.23%).The persons from Africa held higher prevalence (1 .27%)than from other five regions.As multivariate logical regression analysis indicated that the risk of syphilis infection was 1 0.38 times more in the persons aged 40 -49 years than in the persons <20 years (95%CI:5.59 -1 9.28),and 1 .85 times more in males than in females (95%CI:1 .40 -2.44).For the people from Africa,South America and Asia,the infection risks were respectively 4.89 times (95%CI:2.97 -8.06),4.82 times (95%CI:2.39 -9.74)and 1 .72 times (95%CI:1 .1 5 -2.59)more than that for the people from North Ameri-ca.Rising trend of the prevalence was observed in both genders by age groups (P value for trend χ2 <0.05).Except for Asia,the prevalences of the people from other five regions were rising slightly by years,however there were no obvious trends (P value for trend χ2 >0.05).Twenty-seven seropositive cases were found within 6 246 entry persons who were tested repeatedly during the research period,9 of which were seroconversion cases so that the cumulative conversion rate was 0.1 4% (9 /6 228).The average conversion time was (6.3 ±3.0)months.There was no statistical significance between the cu-mulative seroconversion rates of the persons with different genders and nationalities (P of Fisher’s exact test >0.05).Conclusion:Serological detection of syphilis for entry personnel in Beijing port and syphi-lis-related health education should be reinforced to reduce the risk of disease importing and spreading, protect susceptible subjects and promote health.

Obiective:To investigate the effect of interleukin-6(IL-6)on apolipoprotein(apo)M expression in a human hepatoblastoma cell line(HepG2).Methods:HepG2 cells were cultured and incubated with different concentrations of IL-6 (0,1.25,2.5,5,10,20,40 and 80 μg/L)for 24 hours.After the incubations,total RNAs were extracted and applied to reverse transcript PCR and real-time quantitative PCR to detect the expression levels of apoM and apoA-I.The effect of IL-1α on apoM expression was also determined.Results:IL-6 significantly inhibited the expression of apoM(F=10.778,P ＜ 0.01).Whereas IL-6 did not influence the expression of apoA-I(F=2.004,P ＞ 0.05).IL-1α(0,1.25,2.5,5,10,20,40 and 80 μg/L)did not decrease the expression of apoM(F=2.038,P ＞ 0.05).Cooclusion:IL-6 inhibits apoM mRNA transcription,which may contribute to the pathogenesis of abnormal lipid metabolism and macrovascular complications in type 2 diabetes.

AIM: To observe the relationship between the reversal effect of 4 alkaloids of TCM on expression of P170 being obtained multi-drug resistance to mouse S180 tumor cell induced by chemotherapy protocol of PFC and the adjustment of the cell apoptosis.And to discuss the difference among alkaloids of TCM on reversion of being obtained multi-drug resistance in clinic.To improve the curative effect thereby. METHODS: By the methods of less dosage of Chemotherapy PFC,to set up the mouse models of multi-drug resistance of S180 tumor cell.At the same time to give the mouse matrine,terandrine,oxymatrine and berberine hydrooh loride for 2 weeks and then to observe the P170,TOPOⅡ,Fas and apoposis by flow cytometry. RESULTS: Matrine and terandrine could obviously reduce the expression of P170,the activation of TOPOⅡ induced by Chemotherapy and increase the ratio of the express of Fas and the apopsis of drug resistance to tumor cell.And berberine hydrochloride could obviously reduce the expression of TOPOⅡ. CONCLUSION: The adjustment to the apoposis of tumor cell by matrine and terandrine is related to the reversion of being obtained multi-drug resistance to tumor cell' expression,besides the different degree

Objective: To observe the effect of 70% ethanol extract from Huanglian Jiedu Decoction on expression of S180 tumor cell apoptosis factor in MDR model mice, and to research the molecule biology base fot directing clinic. Methods: simulate Clinic PFC project was simulated, the mice model of multi-drug resistance of S180 tumour cell was established. 70% Ethanol extract from Huanglian Jiedu Decoction were given for 10 days. The flow cytometry was used to observe Fas, Trail, CD54.,et al. Resluts: 70% Ethanol extract from Huanglian Jiedu Decoction can increase expression rate of Fas, Trail and improve apoptosis of S180 cell, at the same time it can decrease expression of CD54.Conclusions: 70% Ethanol extract from Huanglian Jiedu Decoction improve high level expression of apoptosis factor, and it maybe one of pass reverse multi-drug resistance of tumour.

OBJECTIVE:To determine the pharmacokinetics and relative bioavailability of oxetacillin and sulbactam in oxetacillin-sulbactam tablets.METHODS:20healthy male volunteers were randomly divided into2groups.In a crossover de?sign,a single oral dose of two tablets of domestic oxetacillin-sulbactam tablets or imported Tai Ba Meng LBL 500 tablets(one tablet of the two formulations contains oxetacillin250mg,sulbactam250mg)were given,then the drug concentrations in plas?ma were assayed by RP-HPLC.RESULTS:The pharmacokinetic parameters of oxetacillin in domestic and imported tablets were as follows:T max were(1.04?0.26)h and(1.10?0.28)h;C max were(5.16?1.30)mg/L and(5.25?1.21)mg/L;AUC 0～∞ were(13.30?3.12)mg/(h?L)and(13.33?3.53)mg/(h?L)respectively.The pharmacokinetic parameters of sulbactam in domestic and imported tablets were as follows:T max were(0.80?1.0)h and(0.81?0.17)h,C max were(5.73?1.44)mg/L and(5.70?1.46)mg/L,AUC 0～∞ were(13.25?2.41)mg/(h?L)and(13.28?2.26)mg/(h?L)respectively.CONCL_ USION:Domestic oxetacillin-sulbactam tablets and imported Tai Ba Meng LBL 500 tablets were bioequivalent.

OBJECTIVE:To study the clinical efficacy and adverse drug reactions (ADR) of paclitaxel combined with oxaliplatin and 5-fluorouracil (5-Fu) in the treatment of advanced gastric cancer.METHODS:31 patients with advanced gastric cancer were treated with paclitaxel 175 mg?m-2 (i.v.) for 3 hours followed by oxaliplatin 85 mg?m-2 on the first day and 24 hour infusion of 5-Fu (500 mg?m-2,first to fifth day) every 3 weeks.Total effective rate,survival duration and ADR were observed.RESULTS:The total effective rate was 38.7% (12/31),including complete remission of 9.7% (3/31),partial remission of 29.0%(9/31),steady progress (SD) of 41.9% (13/31) and promotion progress (PD) of 19.4% (6/31).The median time to progression (TTP) was 5.9 months and median survival time (MST) was 10.7 months.The total response rates were 70% for newly diagnosis patients and 23.8% for recurrence patients.The main ADR were neurotoxicity (89.1%),leukopenia (82.6%),nausea/vomiting (72.8%) and alopecia (66.3%).None of chemotherapy-related death occurred.CONCLUSION:Paclitaxel combined with oxaliplatin and 5-Fu POF regimen appears to be effective and tolerated in the treatment of advanced gastric cancer.