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.

Objective To investigate the relationship between pharmacokinetics(PK) and pharmacodynamics PD of epigoitrin,a main component in total alkaloids of Radix Isatidis,in yeast-induced febrile rats with the combined PK-PD model.Methods The plasma concentration of epigoitrin after ig administration with total alkaloids of Radix Isatidis was determined by HPLC method and the body temperature was recorded by electronic thermometer.The individual PK parameters were fitted using one compartmental model.The PD parameters were fitted by three kinds of PK-PD binding models,such as indirect inhibition-Kin model,indirect stimulation KoutPD model,and Sigmoid-Emax model.Results The main PK parameters t1/2,Cmax,AUC were(4.94?0.84) h,(4.01?0.21) ?g/mL,(28.37?2.42) ?g?h/mL and(5.71?0.91) h,(4.15?0.25) ?g/mL,(30.35?2.58) ?g?h/mL in both normal and febrile rats,respectively.The relationship between pharmacological effects and effect compartment concentration was better fitted with the indirect inhibition-Kin PD model.The corresponding PD parameters were Kin=(0.70?0.10) h-1,Kout=(0.54?0.12) h-1,R0=1.33?0.16,IC50=(0.94?0.66) mg/L.ConclusionThe PK parameters of epigoitrin in total alkaloids of Radix Isatidis show that there is no significant difference in PD behavior in vivo in both normal and febrile rats.Relationship between in vivo PK and PD of epigoitrin in febrile rats is established using indirect inhibition Kin model.

Aim: To study the pharmacokinetic effects of salvianolic acid B( Sal B) on danshensu( DSS) in Danshen injection in rats. MGthod: Following the intravenous administration of Danshen injection and Danshen injection added with Sal B to rats, the plasma kinetic study, tissue distribution and urine excretion were studied. The plasma kinetic study was also investigated by giving DSS and DSS in combination with Sal B to rats. Plasma, tissue and urine drug levels of danshensu were analyzed by LC-MS. Results: Compared with danshensu given alone, no significant difference of the pharmacokinetic behavior of danshensu was found when danshensu was given in combination with salvianolic acid B. However, compared with Danshen injection given alone, the pharmacokinetic behavior of danshensu changed remarkably when Danshen injection was given in combination with salvianolic acid B which might be caused by the decrease of DSS in kidney distribution and urine excretion. Conclusion: The pharmacokinetic effects of salvianolic acid B on danshensu depend on the existence of multiple components in Danshen injection. Results suggest that the pharmacokinetic interactions of the multiple components are closely related to the integrity of herbal medicines.

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.

Type 2 diabetes is a metabolic disease with increasing prevalence,which causes great socioeconomic burden.Intestinal flora is the microbiota located in the human intestines,which are participating in human growth and development,physiological procedures,or even pathogenesis as a closely connected environmental factor.There have recently been rapid progresses in the research on the relationship between intestinal flora and type 2 diabetes in the field of endocrinology and metabolism.In this article,we reviewed the overall framework and research progress in the relationship between intestinal flora and type 2 diabetes,aiming to shed some light on the future research about this topic.

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 understand the characteristics of sexual partners and the influence of having multiple sexual partners on substance use among young male students man who have sex with men (MSM) in China, and to provide scientific basis for the prevention and control of HIV/AIDS among young MSM students. Methods: A mixed recruitment method of snowball sampling and respondent driven sampling was used to recruit young MSM students in Beijing and Tianjin, and a questionnaire survey was conducted among 220 participants from November to December 2019. Chi-square test and generalized linear model multi-factor Logistic regression were used to analyze the influencing factors of substance use before sexual behavior. Results: The average age of them was (22.39±2.57) years old, 84.5% of them were students, the average age of first sexual behavior was (18.83±2.45) years old, 44.1% of them had two or more sexual partners (including fixed sexual partners, temporary sexual partners and commercial sexual partners), 22.7% had more than one male fixed partner. After adjusting for age and education, having multiple sexual partners was risk factor for drinking alcohol before sex (aOR=2.97) or substance abuse (aOR=2.39). Having male temporary sexual partner was an risk factor in substance use before sexual behavior(OR=4.10). Conclusion The characteristics of sexual partners among young MSM students are complex, and the proportion of multiple sexual partners is high. Having fixed single sexual partner can reduce the risk of substance use before sexual behavior. AIDS prevention education for young MSM students should be further strengthened.

e negatively corre-lated with serum viral copies and play an important role in detecting viral replication of HBV and HCV.