Objective:To investigate the adverse drug reactions ( ADR) caused by carbapenem antibiotics and discuss the influen-cing factors to provide reference for the rational use of carbapenems in clinics. Methods:The ADR caused by carbapenems from March 1, 2008 to August 1, 2014 in our hospital were statistically analyzed. Results:Totally 73 cases of ADR were caused by carbapenems. The number of ADR for men and women was similar. The ADR occurred in 80-year-old people with more frequency. The incidence of ADR on the first day of administration was relative high. The ADR were mainly manifested as skin and appendages disorders and nerve system damage. Conclusion: Great attention should be paid to the ADR of carbapenems and the state of patients. The medication should be adjusted in the patients with declined renal function and nerve system basic diseases in order to reduce the damage of ADR.

Objective To explore the correlation between the strength of trunk flexors and extensors obtained by isometric and isokinetic concentric tests. Methods The strength of trunk extensors and flexors were measured by isometric and isokinetic concentric tests during trunk flexion and extension in 50 healthy subjects, and the peak torque of flexion and extension (FPT and EPT) and the ratios of FPT/EPT were analyzed with correlation and regression analysis. Results The FPT and EPT of trunk flexors and extensors were positively correlated (r_F=0.827,P0.05, respectively), the regression equations of FPT and EPT were y^=8.158+1.097X and y^=-12.375+0.781X, respectively. Conclusion The isometric test of the trunk extensors and flexors could assess accurately the changes of the trunk muscle strength without aggravating pain and diseases. It is more reasonable to evaluate the stability of trunk with the FPT/EPT ratio at neutral position.

The safety of Chuangyuling (CYL) dressing-a multifunctional medicine carrying biomaterial was evaluated in order to provide foundation for the application of CYL as material used in the wound healing. The traditional Chinese medicine (TCM) extract solution was compounded with scaffolds (gelatin and Bletilla hyacinthine gum), and then frozen and dried to form spongy and porous material CYL. According to the standard of biological evaluation of medical devices that was instituted by the ministry of health of China, the biological evaluation of CYL dressing was conducted. The results showed that all the contents of biological evaluation test consisting of acute toxicity, skin irritation, sensitization and cytotoxicity met the requirement of standards. It was concluded that the biomaterial carrying TCM (CYL dressing) is safe for application of wound healing.
Drugs, Chinese Herbal/*administration & dosage ; Drugs, Chinese Herbal/toxicity ; Gelatin ; Occlusive Dressings ; Phytotherapy ; Salvia miltiorrhiza ; Wound Healing/*drug effects

AIM: To study the influences of P1 promoter activity of furin gene on the functions of hepatocytes in patients with liver cirrhosis.METHODS: The patients with liver cirrhosis of 180 cases were recruited.The single nucleotide polymorphism(SNP-229 C/T) in P1 promoter of furin gene was genotyped using competitively differentiated polymerase chain reaction.The relationships between the promoter activity based on genotyping and the serum levels of liver enzymes,total bilirubin,albumin and prothrombin were observed.RESULTS: The distribution frequencies of allele C and T were 75.3%(271/360) and 24.7%(89/360).Those of genotypes CC,CT and TT were 62.2%(112/180),26.1%(47/180) and 11.7%(21/180),respectively.The distribution frequencies of the genotypes were not related to the serum levels of major liver enzymes,albumin,total bilirubin and prothrombin,except for alkaline phosphatase and ?-glutamyl transferase.CONCLUSION: The activity of furin promoter exerts no effects on the main functions of hepatocytes,suggesting that furin may be a new therapeutic target for HBV infection.

Objective To investigate the effect of nitric oxide(NO)on the prostatic proliferation/apoptosis in rat models. Methods Twenty adult male rats were randomly divided into 3 groups.Group 1 were normal controls (n=6);group 2 (n=7) and group 3 (n=7) were treated with subcutaneous injection of nitric oxide synthase (NOS) inhibitor-L-NG-Nitroarginine methyl ester (L-NAME) 50mg/kg and 100mg/kg, bid, respectively.The weight of the prostate was measured after 2 weeks and morphological changes were examined with light microscope.Detection of ki-67 and TUNEL in prostatic epithelial cells were undertaken so as to assess the proliferation and apoptosis index.The protein and mRNA expression of NOS were analyzed by means of immunohistochemistry and RT-PCR. Results The prostate weight of 3 groups was not significantly different.Compared with group 1, remarkable atrophy of prostatic epithelial cells,marked decrease in proliferation rate of epithelial and interstitial cells, and significant increase in apoptosis rate of epithelial cells were noted in group 2 and group 3 (P

Objective:To investigate the efficacy and safety of ticagrelor and clopidogrel in patients with coronary atherosclerotic heart disease (CHD) and hyperhomocysteinemia (Hhcy).Methods:A total of 101 patients with CHD complicated with HHcy who had successfully undergone percutaneous coronary intervention (PCI) were enrolled. They were divided into ticagrelor group ( n=49) and clopidogrel group ( n=52) according to the different antiplatelet drugs used. The clinical data of the two groups were collected, and the incidence of major cardiovascular and cerebrovascular adverse events (MACCE) and bleeding events in one year were compared between the two groups. Results:There was no statistical difference in baseline datas and PCI datas between the clopidogrel and ticagrelor groups ( P>0.05). Compared with clopidogrel group, ticagrelor can reduce the total MACCE (8.16% vs 32.69%, P<0.05) and the incidence of unstable angina pectoris events (0 vs 13.46%, P<0.05) in patients with hyperhomocysteinemia PCI 1 year after operation. The incidences of ischemic stroke, unstable angina pectoris, recurrent myocardial infarction, and cardiogenic death were compared separately between the two groups, and the difference was not statistically significant ( P>0.05). The incidence of major bleeding events, minor bleeding events, and minimal bleeding events were similar between the two groups, and the difference was not statistically significant (4.08% vs 0; 4.08% vs 1.92%; 20.41% vs 9.62%; P>0.05). Conclusions:In patients with CHD and Hhcy, ticagrelor can play a better antithrombotic effect, reduce the incidence of ischemic events, and has good security, which is more worthy of clinical recommendation.

This paper is aim to investigate the pharmacokinetics and absolute bioavailability of neoline in Beagle dogs, and provide a theoretical basis for further study. Ethyl acetate was used for liquid-liquid extracting after 10% ammonia alkalizing. The method of UPLC-Q-TOF-MS was established for the determination of neoline plasma concentrations. Beagle dogs were orally or intravenously administered with neoline for pharmacokinetic and absolute bioavailability study. Good linear relationship of neoline was found over the range of 0.1-4 mg x L(-1) (R2 = 0.9982) and 2-100 microg x L(-1) (R2 = 0.9945). Intra-and inter-day precision, expressed as the relativestandard (RSD) were less than 5.0%. Accuracy, expressed as the relative error (RE) was within 90.0%-115%. The recovery of neoline in dog plasma was more than 80%. After 6 mg x kg(-1) for ig and 1 mg x kg(-1) for iv administration of neoline, the main pharmacokinetic parameters were analyzed with Winnonlin software. t(1/2) were (313.88 +/- 63.18), (236.33 +/- 229.84) min, and AUC(0-infinity) were (58,027.40 +/- 14,132.69), (473,578.02 +/- 82,333.08) min x microg x L(-1) for ig and iv administration respectively. The absolute bioavail ability was (73.15 +/- 10.29) %. The method of UPLC-Q-TOF-MS described in the report was sensitive, reliable and specific, and suitable for pharmacokinetic study of neoline in Beagle dog. The high absolute bioavailability of neoline in dog suggested good absorption of neline which was worth of further investigation.
Aconitine ; analogs & derivatives ; chemistry ; pharmacokinetics ; Animals ; Biological Availability ; Dogs ; Drug Stability ; Female ; Male

Objective To prepare a novel radiolabeled FR?positive tumor targeting agent 99 Tcm?( HYNIC?NHHN?FA) ( EDDA) and evaluate its biological properties. Methods FA derivative FA?NHHN?HYNIC was synthesized and radiolabeled with 99 Tcm using EDDA as a coligand. The radiochemical purity, octanal/water partition coefficient and in vitro stabilities of the complex were studied after purified by HPLC. In vitro cellular uptakes were performed on FR?positive KB cells ( human oral epidermoid carcinoma cells) . Biodistribution and microSPECT/CT imaging were investigated on normal Kunming mice and nude mice bearing KB tumors, respectively. Results The radiochemical purity of the complex was over 95% after pu?rified by HPLC. It displayed high stability both in saline and in serum. It also exhibited high specific FR binding in FR?positive KB cells in vitro. The binding ratio was (6.76±0.60)%1 h after incubation, and de?creased to (0.24±0.02)% after adding excessive FA. The results of biodistribution showed high kidney up?take in normal mice, and the uptake reached (21.79±9.79) %ID/g 0.5 h after injection. Flank KB tumors were clearly visualized with 99 Tcm?( HYNIC?NHHN?FA ) ( EDDA ) by microSPECT/CT imaging at 2 h postinjection, and the uptake could be inhibited by excessive FA. Conclusions 99 Tcm?( HYNIC?NHHN?FA) ( EDDA) exhibits good pharmacokinetic properties, suggesting its potential as a promising FA targeting agent for tumor imaging.

AIM:To investigate the role of p38 MAPK signaling pathway in the receptor-mediated endocytosis.METHODS:The effects of p38 MAPK on the receptor-mediated endocytosis were observed by using Alexa 594-conjugated Transferrin,in the presence of p38 specific inhibitor SB203580 or ERK pathway specific inhibitor PD98059,or using p38 knockout techniques.RESULTS:In the process of receptor-mediated endocytosis,p38 was activated by phosphorylation.Furthermore,the receptor-mediated endocytosis was inhibited by pretreatment with SB203580 or p38 knockout,while pretreatment with PD98059 had no effect on this process.CONCLUSION:p38 MAPK signaling pathway plays a role in the regulation of receptor-mediated endocytosis.

Objective To establish an HPLC method for simultaneous separation and determination of chlorogenic acid, quercetin and kaempferol inPyrrosia lingua (Thumb.) Farwell. Methods The separation was performed on Phenomenex C18 column (250 mm×4.6 mm, 5μm) with the mobile phase of methanol-acetic acid (pH=3.0) solution and gradient elution. Flow rate was 1.0 mL/min;the UV detection wavelength was 254 nm;column temperature was 35℃.Results The calibration curves for chlorogenic acid, quercetin, and kaempferol were in good linearity in the range of 0.000 24-3.00μg (r=0.999 9), 0.000 16-2.00μg (r=0.999 9), and 0.000 16-2.00μg (r=0.999 9), respectively. The limits of detection (S/N=3) were 3.29, 0.43 and 0.33 ng/mL, respectively. The average recovery rates were 97.73%, 98.07% and 96.92%, respectively. ConclusionThe method is simple, precise and sensitive. It provides scientific proof for separation and determination of chlorogenic acid, quercetin and kaempferol inPyrrosia lingua (Thumb.) Farwell.