OBJECTIVE:To ensure the safety of the elderly medication. METHODS:The package inserts of 38 kinds of com-mon oral antihypertensive drugs were collected from our hospital,and analyzed statistically in respects of drug information for the elderly in package inserts of domestic and foreign drugs and those of antihypertensive drugs. RESULTS:In 21 package inserts (55.26%),there were specific dosage for elderly;in 16(42.10%),there were certain matters needing attention in“drug use for the elderly”;in 15,the marked rate of“pharmacokinetics study for the elderly”was 39.47%.Except for ARB antihypertensive drugs, related drug information was hardly labeled in package inserts of other types. The label of“starting at low dose”accounted for 21.05%;the label of“no need to adjust dose,“use drug carefully”,“no age differences”accounted for 15.79%,15.79% and 13.16%,respectively. The label rates of other items were in low level. The drug package inserts at home were lack of information of drug use for the elderly,compare to abroad. CONCLUSIONS:There are some problems in package inserts of common oral anti-hypertensive drugs,such as usage and dosage,matters need attention,pharmacokinetics,poor description in details. Drug informa-tion for the elderly in the package inserts of antihypertensive drug needs to be more detailed;the drug regulatory agency and the drug manufactures should make joint efforts to let drug package inserts more detailed about drug use for the elderly to ensure medi-cation safety.

Aim: To determine the uptake characteristics of salvianolic acid B(Sal B) in myocardial cells and blood vessel endothelial cells. Method: The effects of various factors, such as time, temperature, drug concentration, pH of the medium, on the uptake of Sal B in myocardial cells and aorta endothelial cells were investigated. LC/MS was employed to determine the intracellular concentration of Sal B. Results: Uptake kinetics of Sal B in the myocardial cells and aorta endothelial cells fitted well to the logarithmic model at 37 ℃ and 4 ℃. The a-mount of uptake was in direct proportion to the extracellular concentration of Sal B in the experimental concentration range. Uptake of Sal B both in the myocardial cells and blood vessel endothelial cells would significantly increase while the medium pH decreased, and some water-soluble components extracted from danshen would also facilitate the uptake of Sal B both in the myocardial cells and blood vessel endothelial cells obviously. The energy metabolism inhibitors would significantly inhibit the uptake of Sal B in the myocardial cells and blood vessel endothelial cells. When lactic acid and fatty acid were added to the incubation solution, the uptake of Sal B both in the myocardial cells and aorta endothelial cells increased more than 20%. Conclusion: pH is the most important factor influencing the cellular uptake of Sal B, and the amount of uptake tends to increase in acidic medium. Results suggest that the uptake of Sal B would increase in the acidified internal environment induced by myocardial ischemia, thus exerting better cardiovascular activities.

Two cases of Paneth's cell adenoma of the stomach are reported and their morphological, histochemical, immunohistochemical, ultrastructural and immunocytochemical features are described. Both surgical specimens showed varied dysplasia with severe atrophic gastritis and intestinal metaplasia. 60%-70% of the tumor cells contained coarse eosinophilic cytoplasmic granules that are PAS positive but unstained by alcian blue at pH 2.5, and exhibited positive antiserum immunoreaction for ly-sozyme. The Paneth's nature of these granules was confirmed by electron microscopy and immunoelec-tron microscopy. In addition, some endocrine cells were detected in the neoplastic glands. The characteristics of Paneth's cell adenoma of the stomach are discussed and a close relationship between the histogenesis and intestinal metaplasia is suggested.

Objective To determine the in vitro antibacterial activity of levornidazole against 375 anaerobic isolates.Methods Agar dilution method was used to determine the minimum inhibitory concentrations (MICs)of levornidazole,3 comparators (metronidazole,ornidazole and dextrornidazole)against 375 anaerobic isolates.Results For anaerobic gram-negative and gram-positive bacilli,and anaerobic gram-positive cocci,levornidazole displayed activity similar to or slightly higher than that of met-ronidazole,ornidazole and dextrornidazole.Levornidazole showed good activity against B.fragilis,Bacteroides thetaiotaomi-cron ,Clostridium difficile ,Clostridium perfringens ,and Peptostreptococcus magnus .The MIC90 value of levornidazole a-gainst the above-mentioned anaerobes was 0.5,1,0.25,2 and 1 mg/L,respectively.However,levornidazole and the compa-rators had poor antibacterial activity against Veillonella spp.among anaerobic gram-negative cocci.Conclusions The in vitro anti-anaerobic activity of levornidazole is similar to or slightly higher than that of metronidazole, ornidazole and dex-trornidazole.Levornidazole has good activity against both gram-negative and gram-positive anaerobic bacilli,and gram-positive anaerobic cocci,suggesting its promising clinical use.

Purpose Lipotoxicity plays an important role in the progression of diabetes and its complications,and the gold standards for organs' lipid quantification are biopsy or histochemical staining,which are invasive and have their own limitations.Thus,our research was to identify the difference in organ lipid deposition between type 2 diabetic patients and healthy volunteers by using noninvasive three-point T2* corrected Dixon imaging.Materials and Methods Sixty-five type 2 diabetic patients and 34 healthy volunteers were included in this study.All participants underwent three-echo Dixon with 3.0T MR imager.Dixon imaging parameters [hepatic fat fraction (HFF),splenic fat fraction (SFF),pancreatic fat fraction (PFF)] were collected.All of the MRI parameters were compared.The relationship between HFF,SFF,PFF and BMI,age were analyzed.Results The hepatic and splenic lipid percentage in diabetic group [HFF=(5.4±4.3)％;SFF=(3.7± 1.4)％] was significantly higher than healthy volunteers group [HFF=(2.9± 1.3)％;SFF=(3.0± 0.9)％;P＜0.05,respectively].However,there was no significant difference in pancreatic fat fraction between diabetic and healthy groups (P＞0.05).There were positive correlations between HFF,SFF,PFF and BMI (r=0.379,0.305 and 0.306,P＜0.05).Moreover,only the positive correlation between pancreatic fat fraction and age were observed (r=0.261,P＜0.05).Conclusion The three-point T2* corrected Dixon revealed the abnormalities of hepar and spleen lipid accumulation in diabetic patients.Thus,the three-point Dixon imaging may potentially aid in evaluating the lipid deposition of abdominal organs.

ObjectiveTo investigate the clinical pharmacokinetics (PK) and pharmacodynamics (PD) of gemifloxacin tablet in healthy Chinese volunteers and to provide evidences for optimal clinical dosing.MethodsTwenty volunteers were enrolled in the randomized (1∶1) double-blind study,and divided into administration group and control group.Each group received multiple oral doses of 320 mg of gemifloxacin tablet or placebo.The plasma and urine samples for gemifloxacin were analyzed by igh-performance liquid chromatogram(HPLC)-fluorometricmethod. Theminimuminhibition concentrations (MIC)of gemifloxacin against190clinical isolateswere determinedby broth microdilution method.The fAUC0～24 h/MIC and fCmax/MIC,with target value of 25 and 5,were used as the indices to evaluate PK and PD characteristics of gemifloxacin. The cumulative fraction of response (CFR) of gemifloxacin against each bacterium and the probability of target attainment (PTA) under various MIC level were evaluated using Monte Carlo simulation following multiple administration at steady state.ResultsThe Cmax of gemifloxacin after once-daily oral doses for 7 days were (1.55 ±0.32) μg/mL and (1.57±0.31) μg/mL for the first and last dose,while the AUC0～24 h were (7.91±1.52) and (8.91±1.15) h · μg · mL-1,respectively.The accumulation factor was 1.13±0.05.The time-profile of gemifloxacin could be described using two-compartment model and the half-life of distribution and elimination phase were (0.64 ± 0.17) and (7.10 ± 2.10) h,respectively. The cumulative urinary excretion rates within 24 h of gemifloxacin were 34.83 ％ and 38.95 ％ for the first and the last dose,respectively.PD study showed that the MIC90 of gemifloxacin were 0.25 mg/L and 0.125 mg/L against Streptococcus pneumoniae and Moraxelle catarrhalis,respectively,while the MIC90 was 2 mg/L against Hemophilus influenza. However,most of Klebsiella pneumoniae and methicillin-resistant Staphylococcus aureus (MRSA) were resistant to gemifloxacin ( MIC90 ＞ 32mg/L).The PTA values of fAUC0～24 h/MIC and fCmax/MIC of gemifloxacin 320 mg daily for 7 days were close to 100％ when MIC was ≤0.06 mg/L.ConclusionsGemifloxacin is rapidly absorbed after oral administration of single doses in healthy Chinese volunteers,and the plasma concentration could reach steady state at the third day,while a minimal accumulation is shown after consecutive 7 days dosing.The PK/PD analysis suggests that the favorable clinical and bacteriological efficacy could be obtained when using thisregimen in treatment of sensitive patients with community-acquired pneumonia and acute exacerbation of chronic obstructive pulmonary disease.

Objective:To investigate the effect of Zhitong-Rusheng Decoction on wound healing and serum fibronectin (FN) and epidermal growth factor (EGF) levels after anal fistula operation. Methods:A total of 102 patients after anal fistula operation in our hospital from March 2018 to March 2020 were randomly divided into control group (51 cases) and observation group (51 cases) according to the random number table method. The control group was treated with conventional western treatment, while the observation group was treated with Zhitong-Rusheng Decoction on the basis of control group. The two groups were treated for 3 weeks. The clinical symptoms were scored before and after treatment, and the levels of serum FN and EGF were detected by ELISA. The wound healing time, hematochezia disappearance time, wound longitudinal diameter and wound area before and after treatment were observed. The clinical efficacy was evaluated after treatment. Results:The total effective rate was 98.0% (50/51) in the observation group and 72.6% (37/51) in the control group, with significant difference between the two groups ( χ2=13.209, P<0.01). After treatment, the pain degree score, wound exudation score and granulation morphology score of the observation group were significantly lower than those in the control group ( t=15.448, 21.424, 28.641, P<0.001). After treatment, the wound healing time [(6. 04 ± 1.20) d vs. (9.42 ± 1.58) d, t=12.166] and the disappearance time of hematochezia [(15.72 ± 2.86) d vs. (19.95 ± 4.33) d, t=6.862] of the observation group were significantly shorter than thosse of the control group( P<0.01). After treatment, the wound longitudinal diameter [(1.89 ± 0.31) cm vs. (2.82 ± 0.54) cm, t=10.666] and wound area [(3.26 ± 0.54) cm 2vs. (4.98 ± 1.10) cm 2, t=10. 024] of the observation group were significantly less than those in the control group ( P<0.01). The serum FN [(2.92 ± 0.50) mg/L vs. (2.45 ± 0.39) mg/L, t=5.293], EGF [(7.03 ± 1.44) μg/L vs. (5.47 ± 1.03) μg/L, t=6.293] of the observation group were significantly higher than those in the control group ( P<0.01). Conclusion:Zhitong-Rusheng Decoction on the basis of conventional treatment on patients after anal fistula operation has a good efficacy, which is conducive to wound healing, reducing clinical symptoms, and improving serum levels of FN and EGF.

OBJECTIVETo study the signaling pathways associated with lipopolysaccharide (LPS)-induced inflammation in islet micro-endothelial cells (IMECs) and the mechanism of pravastatin intervention.

METHODSIMECs exposed to LPS, SB203580, pravastatin, or SB203580+pravastatin were examined for cell apoptosis with Hoechst staining and flow cytometry and for expression levels of total-p38, photophosphorylation-p38 (p-p38) and iNOS with Western blotting.

RESULTSThe apoptosis rate and expression levels of total-p38, p-p38, iNOS in IMECs all increased after LPS exposure. Pravastatin, SB203580, and their combination significantly attenuated LPS-induced enhancement of cell apoptosis and total-p38, p-p38, and iNOS expressions in IMECs.

CONCLUSIONLPS-induced inflammatory toxicity in IMECs is associated with the activation of P38MAPK and iNOS/NO signaling pathways. Pravastatin can inhibit these pathways and suppress the apoptosis and necrosis of IMECs to relieve the cell inflammatory injuries.

Animals ; Apoptosis ; Endothelial Cells ; drug effects ; metabolism ; Endothelium, Vascular ; cytology ; Inflammation ; Islets of Langerhans ; blood supply ; MAP Kinase Signaling System ; drug effects ; Mice ; Nitric Oxide Synthase Type II ; metabolism ; Phosphorylation ; Pravastatin ; pharmacology ; p38 Mitogen-Activated Protein Kinases ; metabolism

Objective To evaluate the changing pattern of pelvic incidence (PI) during peak skeleton growth in adolescence and to study whether PI is associated with the anatomical morphology changes of pelvis and sacrum.Methods This retrospective longitudinal study recruited adolescent idiopathic scoliosis (AIS) patients,age between 9 and 18 years with full spine images and have at least 3 times' follow-up.The radiological anatomical parameters were measured in each follow-up including PI,pelvic height (PH),pelvic width (PW),sacral width (SW),femoral head-sacrum (FH-S),sacrum-coccyx (S-C) length,sacrum-coccyx (S-C) distance and sacral curvature ratio.△Parameter and growth velocity of each parameters were calculated.According to the skeletal maturity,all subjects were divided into 3 groups:Low Risser Group (first visit at Risser 0 and follow up through Risser 0 to 1),Moderate Risser Group (first visit at Risser 1 and follow up through Risser 1 to 3) and High Risser group (first visit at Risser 3 and follow up through Risser 3 to 5).Each group has 106 patients.We increased the male ratio to detect the gender difference.A total of 318 AIS patients were included in our study and there are 117 male patients.Descriptive analysis was conducted on the sample age,gender and measured parameter values with mean and standard deviation (SD).The intra-and inter-observer reliability analysis,and the intraclass correlation coefficient (ICC) were calculated.The correlation between △PI and △parameter was evaluated by calculating Pearson correlation coefficient R value.Results The mean age of all subjects was 12.86 years and the mean Cobb angle was 26.67° at first visit.The peak growth velocity of PI was in Risser I (female 1.5°/year and male 1.6°/year).The PI was also increasing rapidly in Risser 0.5 (female 1.2°/year and male 1.5°/year) and Risser 2 (female 1.1°/year and male 1.4°/year).When the Risser grade reached 3 which was a sign of the end of skeleton growth,the PI still had increasing potential and it increased slower in Risser 4 and Risser 5.There showed significant correlation between △PI and △age in the three group(P＜0.05)and the correlation was stronger in Low Risser group and Moderate Risser group than that in High Risser group.There showed significant correlation between △PW and △PI in all groups while △PH and △PI showed correlation only in Low Risser group.There showed significant correlation between △SW and △PI,△FH-S and △PI,△S-C length and △PI (P＜0.05) except △S-C length in male Low Risser group and △FH-S in female High Risser group and the Moderate Risser group had the strongest correlation.The △S-C distance and △S-C ratio didn't show any correlation with △PI (P＜0.05) expect the male of High Risser group.Conclusion Pelvic incidence is increasing during skeleton growth at the age of 9 to 17.It has the peak growth velocity in Risser 1 and remains growth potential in Risser 5.PI growth is correlated with pelvic height,femoral head-sacrum distance,pelvic width and sacral width.

Hereditary leiomyomatosis and renal cell cancer (HLRCC) syndrome is a rare hereditary disease and characterized by cutaneous leiomyoma, uterine leiomyoma and/or renal cell carcinoma, but rarely associated with vena cava embolism. We treated 1 case of HLRCC syndrome patients with inferior vena cava tumor emboli (Mayo grade Ⅳ), confirmed after genetic testing, the patient and her family refused further treatment. The patient died after two months of follow-up after discharge.