Objective To study antidepressant effect and mechanism of different polar fraction of Acorus tatarinowii Schott.on depression mouse model and explore the mechanism. Methods Different polar fractions were prepared by systematic solvent method.The adult dose recommended by Chinese Pharmacopeia (10 g·d-1) was converted to the dose of mouse.Intragastric administration was performed.A total of 80 male mice was randomly divided into normal control group,model control group and different polar fraction groups of Acorus tatarinowii Schott..Depression mouse model was established by chronic unpredictable mild stimulation (CUMS) with solitary feeding,and external performance of mice of different groups was observed.After 21-day feeding,blood was harvested from eyes of the mice.Concentrations of triiodothyronine (T3),tetraiodothyronine (T4),thyroid-stimulating hormone (TSH),adrenocorticotrophic hormone (ACTH) in mouse plasma and 5-hydroxy tryptamine (5-HT),ACTH in brain were measured by ELISA method. Results Concentrations of T3,T4 and ACTH in model control group [(1.203±0.042),(44.80±2.21),(11.27±0.50) ng·mL-1] were significantly increased as compared with the normal control group [(0.794±0.028),(24.87±1.25),(7.04±0.24) ng·mL-1] (P<0.05).Concentration of 5-HT in brain (146.87±10.96) was significantly decreased as compared with that of normal group (237.11±21.87) ng·L-1,and concentration of ACTH (58.94±4.46) ng·L-1 was significantly increased as compared with that of normal group [(38.89±2.26) ng·L-1,P<0.05)].Concentrations of T3 [(0.824±0.067),(0.812±0.051),(0.943±0.049) ng·mL-1],T4 [(25.97±1.96),(27.53±1.88),(31.26±1.97) ng·mL-1] and ACTH [(7.21±0.40),(7.58±0.39),(8.69±0.42) ng·mL-1] in extraction group,cyclohexane group and chloroform group were significantly decreased as compared with model control group.At the recommendation dose of Chinese Pharmacopeia,concentrations of 5-HT in brain [(219.59±10.48),(202.19±11.95),(186.96±10.29) ng·L-1] were significantly increased,and concentrations of ACTH [(41.65±2.65),(44.87±2.95),(47.75±3.06) ng·L-1] were decreased (P<0.05). Conclusion Mouse model of CUMS shows typical depression symptom,and the symptom has relationship with the concentrations of endocrine hormones of T3,T4,ACTH,5-HT,etc.Extraction and low polar fractions (cyclohexane,and chloroform) of Acorus tatarinowii Schott.can partly correct incretion disorder of depression model,which may be parts of the reasons why Acorus tatarinowii Schott.exerts anti-depressant effect.
Objective To examine the effect of berberine hydrochloride (BER) on the pharmacokinetic profiles of midazolam,a substrate of CYP3A,in rats. Methods The rats were intragastrically given different doses of BER (50,100,200 mg·kg-1) or ketoconazole (75 mg·kg-1) for 10 days.Single-pass duodenum perfusion of 20 mg·kg-1 MDZ was performed and the inguinal artery was cannulated for blood sampling.Plasma concentrations of MDZ and 1'-OH-MDZ were analyzed by high performance liquid chromatography (HPLC) with the CYP3A inhibitor ketoconazole serving as positive control. Results BER (50,100,200 mg·kg-1) and ketoconazole (75 mg·kg-1) could significantly increase the AUC(0-t),AUMC(0-t)and Cmax of MDZ in a dose-dependent manner (P<0.05),and reduce the clearance rate (CLz) of MDA and its apparent volume of distribution in the body (Vz) (P<0.05).But they failed to dramatically affect the half-life (t1/2z) and the peak time (tmax) of MDZ.Additionally,BER (100,200 mg·kg-1) and ketoconazole (75 mg·kg-1) could significantly dose-dependently decrease the AUC(0-t),AUMC(0-t)and Cmax of 1'-OH-MDZ,and profoundly increase the CLz,tmax and Vz of 1'-OH-MDZ (P<0.05),but they had no remarkable influences on the t1/2z.The ratio of AUC(1'-OH-MDZ)/AUC(MDZ) was decreased with the increase of BER concentration. Conclusion BER can inhibit the in vivo metabolism of MDZ in a dose-dependant manner,which is associated with the suppression of the activity of CYP3A.
Objective To observe the effects of dexmedetomidine hydrochloride on the cisatracurium-induced neuromuscular blockade in geriatric, young and middle-aged patients. Methods Forty elderly patients and forty young and middle-aged patients undergoing elective abdominal surgery under general anesthesia were randomly divided into 4 groups (n=20 each): elderly dexmedetomidine hydrochloride group (group DE),elderly control group (group CE),young and middle-aged dexmedetomidine group (group DY) and young and middle-aged control group (group CY).In groups DE and DY,a loading dose of 0.5 μg·kg-1 dexmedetomidine was intravenously infused over 10 min before induction of anesthesia,respectively,followed by infusion at a rate of 0.4 μg·kg-1·h-1 until the end of surgery。 Equal volume of 0.9% sodium chloride was given in groups CE and CY.Anesthesia was induced with midazolam,fentanyl,propofol and cisatracurium 0.15 mg·kg-1.Four groups were maintained with infusion of propofol and remifentanil.Neuromuscular blockade was maintained with continuous cisatracurium infusion in the four groups and was monitored with TOF-Watch SX acceleromyography at the adductor pollicis.The onset time,TOF no reaction period,duration of action,the amount of cisatracurium consumption,and the spontaneous recovery index (T1 25% to 75%) were recorded. Results The four groups were comparable in the demographic data.Intubation conditions,the onset time and recovery index were not significantly different among the four groups.The duration of blockade action in groups DE and DY was (61.1±8.9) min and (53.6±9.3) min,which was significantly longer than that in group CE [(49.9±5.8) min] and group CY [(44.8±6.4) min] (P<0.01).The duration of blockade action was significantly longer in groups DE and CE than in groups DY and CY (P<0.05).The amount of cisatracurium consumption in groups CE and CY was significantly higher than that in groups DE and DY (P<0.05). Conclusion The neuromuscular blockade is longer and the requirement of cisatracurium is less in elderly patients than in young and middle-aged patients.Continuous infusion of dexmedetomidine hydrochloride can't accelerate the onset time of cisatracurium.But duration of action is prolonged and the amount of cisatracurium consumption is lower in patients with infusion of dexmedetomidine hydrochloride.
Objective To determine the EC50 of dexmedetomidine hydrochloride (DEX) which causes disappearance of explicit memory by process dissociation procedure (PDP). Methods Forty patients those who had senior middle school or higher educational background undergoing lower extremity surgery with grade ASA Ⅰ or Ⅱ,without hearing impairment,dysphasia,nervous system disorders,and having no drugs in the treatment of the central nervous system were included.PDP was applied to establish study table and record,and calculate performance of explicit memory and implicit memory.Memory performance was statistically compared with 0, 0 memory was considered to be statistically significant and disappearance,respectively.Sequential method was used for determination.According to explicit memory disappearance or not,target concentration of the next patient was adjusted (increase or decrease).DEX target concentration of the first patient was set to 4 ng·mL-1,and the ratio of target concentration between the adjacent patients was 1.2.If the explicit memory of the former patient disappeared,the target concentration of the next patient was decreased by 1 concentration gradient; if the explicit memory of the former patient did not disappear,the target concentration of the next patient was increased by 1 concentration gradient,and so forth.All the 40 patients were determined.The median effective dose (D1) and 95% confidence interval (CI) of DEX were calculated. Results The ED50 of DEX causing explicit memory disappearance was 5.23 ng·mL-1,and the 95% CI was 4.07-6.39 ng·mL-1. Conclusion In clinical,target concentration of dexmedetomidine hydrochloride 5.23 ng·mL-1 levels for sedation,can cause half of patients’ explicit memory disappear,so as to avoid intraoperative awareness.
Objective To compare the effects of propofol and ketamine on long-term memory and the expression of brain N-methylgroup-D-aspartate receptor 2B(NMDAR2B) and Gamma-aminobutyric acid receptor 1(GABAR1) in aged rats,and preliminary investigate the relation between the long-term memory and expression of neurotransmitter receptors in different cerebral areas. Methods The aged male rats were randomly divided into control group,propofol group and ketamine group.Morris water maze training was performed in all the rats of three groups for 5 days.On the 6th day,intraperitoneal injection of 50 mg·mL-1 propofol was administrated in propofol group,80 mg·mL-1 ketamine was intraperitoneally injected in ketamine group,and blank control group was given the same dose of saline.Seven days after the administration,space exploration experiment and navigation experiment test were performed to test the impact on the learning and memory ability of rats.After that,the expression levels of GABAR1 and NMDAR2B in temporal lobe and hippocampal CA1 region of the rat brain were detected by immunofluorescence and FISH technique. Results The results of Morris water maze showed there was no significant difference between propofol group (9.49±1.24) s and blank control group (8.82±2.22) s.There was statistically significant difference between ketamine group (12.04±2.67) s and blank control group (P<0.05),with longer latency time and less number of times of passing through target as compared with blank control group.By using immunohistochemistry and FISH technique,the expression of GABAR1 in temporal lobe and hippocampal CA1 region of the rat brain was not significantly different between propofol group and blank control group,but it was significantly up-regulated in ketamine group as compared with blank control group (P<0.05).The expression of NMDAR2B in temporal lobe and hippocampal CA1 region of the rat brain was not significantly different between propofol group and blank control group,but it was significantly down-regulated in ketamine group as compared with blank control group (P<0.05). Conclusion Propofol anesthesia alone had no effect on long-term learning and memory,but ketamine anesthesia can result in long-term learning and memory impairment.The mechanism may be related with down-regulation of the expression of NMDAR2B receptor and up-regulation of GABAR1 not only in CA1 region hippocampus,but also in temporal lobe.
Objective To observe the effects of sevoflurane and propofol on cerebral oxygen metabolism and postoperative cognitive function during cardiopulmonary bypass (CPB). Methods Fifty ASA Ⅱ or Ⅲ patients aged 40-65 years old scheduled for cardiac valve replacement surgery with CPB were randomly assigned into two groups,sevoflurane group (group S) and propofol group (group P),25 in each group.Two groups of patients used the same method of anesthesia induction: midazolam 0.1 mg·kg-1,sufentanil 0.7 μg·kg-1,vecuronium 0.1 mg·kg-1,and etomidate 0.2 mg·kg-1 were intravenously injected successively,and then tracheal intubation was performed.For maintenance of anesthesia,patients of group S continuously inhaled 3%-4% sevoflurane,and patients of group P were intravenous pumped with propofol 4-6 mg·kg-1·h-1 via vein; midazolam,sufentanil and vecuronium bromide were intermittently injected in both groups.At the time points of pre-bypass (t1),nasopharynx temperature dropping to constant temperature regularly (t2),nasopharynx temperature rising to constant temperature regularly (t3),1 h after the end of CPB (t4),and 6 h after the end of CPB (t5),blood from radial artery and right jugular bulb was harvested for blood gas analysis,and mini-mental state examination(MMSE) score were evaluated before and 24 and 48 h after the surgery. Results The jugular venous bulb oxygen saturation(SjvO2) in the two groups were both increased during T2 period and then decreased during t3 period,but arteriovenous oxygen content difference(AVDO2) and oxygen extraction rate(O2ER) were both decreased during t2 period and then increased during t3 period.There was no significant difference between the two groups during t2 and t3 period (P>0.05).MMSE scores of the two groups after operation were all less than those before operation,but that was significantly higher in the sevoflurane group than in the propofol group 24 h after the surgery (t=4.34,P<0.05). Conclusion The two anesthesia methods can meet the need of valve replacement surgery and maintain the cerebral oxygen balance during CPB period,but sevoflurane anesthesia has fewer influences in post-operation mental nerve functional changes.
Objective To observe the anesthesia effect of dezocine and pentazocine in painless artificial abortion,in order to provide a basis for safe use of anesthesia drug in clinical practice. Methods Totally,300 patients undergoing painless artificial abortion were included in this study.The patients were randomly divided into four groups: group A (simple propofo),group B (propofol combined with fentanyl),group C (propofol combined with dezocine) and group D (propofol combined with pentazocine)(n=75 each).Four groups of patients were intravenously injected with propofol (1-1.5 mg·kg-1) according to the situation in operation when necessary to maintain anesthesia effect.Heart rate (HR),mean arterial pressure (MAP),arterial oxygen saturation (SpO2) and respiratory frequency were observed and recorded before induction,after induction,at the beginning of the operation,during operation and anesthesia recovery.The onset time of anesthesia,the recovery time,the recovery time of orientation,the postoperative pain score and the incidence of adverse reaction of the four groups were recorded. Results All of the patients achieved good effects of anesthesia in operations.There was no significant difference in the onset time of anesthesia (P>0.05).Awakening time and time of orientation recovery in groups B,C and D were significantly shorter than those in group A (P<0.05).The dosages of propofol in group C and D were significantly less than those in group A and B (P<0.05).The changes of HR,MAP,SpO2 and respiratory frequency after induction were not significantly different in group B,C and D (P>0.05),but the changes were relatively stable as compared with group A (P<0.05).The rates of adverse reactions in group B,C and D were significantly lower than that in group A (P<0.05).The incidence rates of respiratory depression,nausea and vomiting in group C and D were significantly lower than those in group A and B (P<0.05).The postoperative pain scores of VAS in group B,C and D were significantly lower than that of group A (P<0.05). Conclusion The analgesia effects of dezocine and pentazocine are similar.Application of them can reduce the dosage of propofol and shorten the anesthesia awakening time in painless artificial abortion,at the same time they have less adverse reactions,and they are safe and effective to be used in clinical anesthesia.
Objective To compare the bispectral index score (BIS) correlationbetween standard frontal sensor position and an alternative zygomatic position under general anesthesia with propofol combined with remifentanil during neurosurgery. Methods Twenty patients undergoing neurosurgery were enrolled.Everyone received total intravenous anesthesia by target-controlled infusion of propofol and remifentanil.Two BISTMQuatro sensors mounted on the frontal and zygomatic regions were connected to BIS VistaTM monitors on each patient during general anesthesia.Data from each position were collected and analyzed at the time of awakening(t1),intubation(t2),incision(t3),the end of surgery(t4),and extubation(t5). Results At t1,zygomatic BIS(88.95±6.42) was significantly lower than frontal BIS (84.85±9.64,P<0.01).But during anesthesia,different of BIS value was no statistical significance between the standard frontal position and an alternative zygomatic position(P>0.05).Scatter plot analysis revealed a significant correlation between BIS of frontal positionand that of zygomatic position(R2=0.892,P=0.000). Conclusion During the anesthesia maintenance period,the zygomatic position can be availably used as an alternative position for monitoring if the operative field renders the standard frontal position unavailable.
Objective To establish an high performance liquid chromatography method for determination of 2-indole ketone derivative and its related substances. Methods Agilent Eclipse XDB-C18 (250 mm×4.6 mm,5 μm) column was adopted.The mobile phase was acetonitrile-water with gradient elution mode at a flow rate of 1.0 mL·min-1; the column temperature was 35 ℃; the injection volume was 20 μL and the detection wavelength was set at 257 nm. Results 2-indole ketone derivative ID and related substances could be well separated.The 2-indole ketone derivative had good linear correlation (r=0.999 4) within the range of 40-300 μg·mL-1.It had a good precision (RSD<1%).The limit of detection was 8 ng. Conclusion The method is accurate,simple,sensitive and selective,which can be used for the quality control of 2-indole ketone derivative and related substances.
Objective To explore a clean and efficient new method for extraction of Diosgenin. Methods Yield of the total saponins was evaluated to determine the optimal enzymolysis temperature,pH,solid to liquid ratio,dosage of enzyme and enzymolysis time.Using diosgenin yield as an index,solid to liquid ratio,concentration of sulfuric acid and hydrolysis time were optimized in the saponins hydrolysis process via orthogonal experiment. Results The best conditions for the enzyme pretreatment were as follows: the temperature for enzymolysis was 70 ℃,pH 5.5,solid to liquid ratio was 1:4,dosage of enzyme was 8 mL·kg-1,and extraction time was 24 h.The best conditions of total saponins hydrolysis were as follows: the solid to liquid ratio was 1:4,concentration of sulfuric acid was 2.0 mol·L-1,and hydrolysis time was 5 h. Conclusion The new method is environmental friendly and highly efficient,and expected to be applied in industrial production.
Objective To optimize extraction technology of flavonesingredients from Herba Epimedii by uniform design. Methods Ultraviolet spectrophotometry was adopted to determine the content of total flavonoids.Content of epimedin A,epimedin B,epimedin C,icariin and baohuosideⅠ were determined by HPLC. U10*(108)uniform design was used to conduct the multiple comprehensive evaluation of six ingredients and comprehensively analyze the influence of the concentration and amount of ethanol,extracting time on extraction of flavonesin gredients from Herba Epimedii. Results The uniform design experiment showed that 15-fold weight of 60% ethanol,extracting 2 times and each time with 165 min were the optimum extraction condition. Conclusion The method is easy and reasonable to handle,has stable and reliable results,and good repeatability and feasibility.It can be applied in industrial production.
Objective To compare the dissolution behavior between domestic trepibutone tablets and original reference product,and provide a basis for evaluating the quality consistency of generic drugs. Methods Four dissolution media recommended by Japanese Orange Book and a domestic standard dissolution media were selected to determined the dissolution profile,and f2 factor was calculated to investigate the consistency of stripping curves. Results In water,pH 4.0 and pH 1.2,the f2 of domestic formulation and reference formulation was under 50,and the dissolution profile was inconsistent.Dissolution behavior of domestic preparations of different manufacturers was dissimilar.In water,the f2 of domestic preparations of different batches of the same manufacturer was over 99.9,and the dissolution behavior was similar. Conclusion The dissolution method of existing domestic standard can not distinguish the dissolution behavior of different products,and it should be revised and completed.There is still great difference in quality between the domestic preparations and reference preparations.
Objective To systematically review the effectiveness and safety of pantoprazole (PAN) vs.ranitidine (RAN) for patients with gastroesophageal reflux disease (GERD). Methods PubMed,Medline,EMbase,The Cochrane Library and three Chinese literature databases (CNKI,VIP and Wan fang) were retrieveed.Randomized controlled trials (RCTs) which compared the clinical outcomes of PAN group vs.RAN group for GERD were included.Two reviewers independently screened literatures in accordance with the inclusion and exclusion criteria,extracted the data and assessed the methodological quality of included studies.Then,meta-analysis was performed using RevMan 5.2 software. Results A total of 8 RCTs involving 1 590 patients were included.The results of meta-analysis showed that the PAN group was significantly superior to RAN group in terms of the healing rates and the relief rates of chief symptom for GERD of grade Ⅰ-Ⅲ.While there was no significant difference in the incidence of adverse events between the two groups [Grade Ⅰ,RR=1.17,95%CI (0.80,1.70),P=0.43; Grade Ⅱ or Ⅲ,RR=0.76,95%CI (0.43,1.36); P=0.36]. Conclusion Current evidence indicates that,pantoprazole is more effective than ranitidine for GERD of grade Ⅰ-Ⅲ,but both treatments are safe and well tolerated.
Objective To investigate status of the intravenous use of antibiotics in outpatients and emergency patients of a tertiary first-class hospital,and provide a reference for developing management measures in next step. Methods By a retrospective method,all the prescriptions using antibiotics by intravenous administration in outpatients and emergency department patients from a tertiary first-class hospital in 2013 were extracted from the hospital information system.The categories of antimicrobial agents,proportion of intravenous use of antimicrobial drugs,ranking of the antibiotic consumption sum and defined daily dose,and the top 10 clinical departments or wards intravenously using antimicrobial drugs were chosen to analyze.The data in 2014 were extracted as a comparison. Results Outpatients and emergency department patients respectively used 8 categories 31 kinds and 8 categories 30 kinds of intravenous antimicrobial drugs,with high consumption of cephalosporins and restricted antimicrobials such as sodium cefoxitin.Intravenous use of antimicrobial drug prescription proportion in emergency department is higher than that in outpatient department. Conclusion After intervention in 2014,antibiotic consumption is effectively controlled as compared that in 2013.But management should be strengthened and appropriate interventions should be taken to ensure the use of intravenous antibiotics in a safe,effective and economical manner.
Objective To investigate the correlation between the use density of antibiotic and antifungal drugs and the positive rate of aspergillus in our hospital from 2009 to 2013,in order to provide a scientific basis for rational use of antibiotic and antifungal drugs. Methods The use density of carbapenems,two third-generation cephalosporins,and antifungal drugs,and the positive rate of aspergillus in our hospital from 2009 to 2013 were studied retrospectively.Their correlation was analyzed using SPSS software. Results There was significantly positive correlation between the use density of imipenem and that of fluconazole (r=0.913,P<0.05).The use density of biapenem was positively correlated with that of voriconazole (r=0.915,P<0.05).The use density of biapenem and that of voriconazole was positively correlated with positive rate of aspergillus,respectively (r=0.918,r=0.955,both P<0.05).The other antibiotic and antifungal drugs were not significantly correlated to the positive rate of aspergillus. Conclusion Rational control over the use density of antibiotic may reduce the use density of antifungal drugs and infection rate of aspergillus.