ABSTRACT
OBJECTIVE To establish a method for simultaneous determination of two third-generation anti-epileptic medicines such as lacosamide and perampanel in human plasma and apply this method in clinical practice. METHODS Using clozapine as internal standard， the concentrations of lacosamide and perampanel of plasma samples in 10 epileptic patients were determined by LC-MS/MS after protein precipitation with acetonitrile and dilution with acetonitrile-water （20∶80，V/V）， and the plasma minimum concentrations were obtained by dilution of multiple. The determination was performed on Welch Ultimate XB-C18 column， with mobile phase A consisted of 10 mmol/L ammonium formate and mobile phase B consisted of methanol-acetonitrile-isopropanol （0.2% formic acid） mixed solution （7∶1.5∶1.5， V/V/V） for gradient elution at the flow rate of 0.4 mL/min. The column temperature was set at 40 ℃ ， and the sample size was 5 μL. The electrospray ion source and multi-reaction monitoring mode were used for positive iron scanning. The ion pair used for quantitative analysis of lacosamide， perampanel and internal standard were m/z 251.2→ 144.1， m/z 350.2→219.2 and m/z 327.2→270.0， respectively. RESULTS The linear ranges of lacosamide and perampanel were 0.001 25-0.125 μg/mL（r＞0.99）， 0.037 5-3.75 ng/mL （r＞0.99）； the limits of quantification were 0.001 25 μg/mL and 0.037 5 ng/mL， respectively. The precision and accuracy within and between batches， extraction recovery rate， matrix effect， and stability all met relevant requirements. The minimum concentrations of lacosamide in No. 1-5 patients were 5.3-12.2 μg/mL， and the minimum concentrations of perampanel in No.6-10 patients were 208-510 ng/mL， respectively. CONCLUSIONS The established method is simple， rapid and suitable for the therapeutic drug monitoring of lacosamide and perampanel.
ABSTRACT
Objective: To investigate the application and tendency of carbapenems in the hospitals of Wuhan area.Methods: The application of carbapenems in 34 hospitals of Wuhan area during 2007-2014 was analyzed statistically in terms of consumption sum, DDDs, DDC and so on.Results: The total consumption sum of carbapenems increased year by year.Compared with that in 2007, the total consumption sum increased by 4-fold in 2014.The growing rate of total consumption sum of biapenem was the fastest among various varieties.Since 2009, three injections including meropenem, biapenem and imipenem / cilastatin predominated the market of Wuhan area, followed by faropenem with oral administration.The changing trend of DDDs was basically consistent with the total consumption sum.DDC of all the drugs was relatively high and demonstrated decreasing tendency, and that of biapenem decreased most notably, while still ranked the first place.DDC of meropenem and imipenem/cilastatin both exceeded 400 yuan.The price of faropenem fluctuated notably during 2007-2009, while increased by 2-fold in 2009 (453 yuan) and then remained stable.Conclusion: The special rectification measures show positive impact on the selection of antimicrobial agents in Wuhan area.The drug varieties are proper, while the average daily cost is still high.The government should continue to strengthen the management of antibiotics to ensure the rational use of carbapenems.
ABSTRACT
Objective To investigate the association between SERPINH1 gene expression in gastric cancer tissue with the pathology and prognosis and its action mechanism in gastric cancer.Methods The gastric cancer data in the TCGA and GEO public databases were collected,and the retrospective analysis and survival analysis were conducted on the SERPINH1 expression data of the tumor tissue samples and related clinical information;the gene set enrichment analysis(GSEA) was used to analyze the SERPINH1 expression related functional gene sets and to investigate the SERPINH1 action mechanism.Results In 421 cases of gastric cancer sample,the SERPINH1 expression level had no significant differences with the tumor grade,N stage and metastasis.However,its high expression was significantly correlated with the tumor invasion depth(T stage)(P=0.049).The higher the expression level,the preater the invasion depth.In the survival analysis,the patients with high SERPINH1 expression showed a poorer prognosis than those with low SERPINH1 expression[P<0.001,HR(95%CI):1.97 (1.61-2.41)].The gene set enrichment analaysis found that the related gene sets such as tumor signal pathway and tumor microenvironment were enriched in the SERPINH1 high expression samples.The gene expression chip data in 69 cases of gastric cancer and paracancerous tissue also suggested that SERPINH1 was highly expressed in gastric cancer (P<0.000 1) with a greater diagnostic value (AUC=0.988 1).Conclusion High expression of SERPINH1 is correlated with the occurrence and development of gastric cancer,and has a greater clinical significance.
ABSTRACT
Objective:To investigate the effect of extract of mung bean seed coat ( MBSC) on the activity of CYP3A4 in vitro. Methods:Midazolam was used as the probe drug, and an HPLC method for determining the metabolite of midazolam ( l-hydroxyl mid-azolam) in rat liver microsome incubation system was established. Three important parameters including the incubation time, concen-tration of rat microsome and probe concentration were optimized for rat liver microsome incubation system, and then the optimal incuba-tion system was applied to study the effect of MBSC extract on CYP3A4 activity and the potential mechanism. Results: The results showed MBSC crude extract could inhibit CYP3A4 activity to 38. 14% as that in the control group(P<0. 05) with IC50 value of 489. 7μg·ml-1 . The mechanism might be related to competition-noncompetition inhibition. Conclusion: MBSC extract exhibits inhibitive potency to CYP3A4 in in-vitro model. Further studies should be conducted to check the influence of MBSC on CYP3A4 in vivo.
ABSTRACT
Objective:To investigate the effect of extract of mung bean seed coat ( MBSC) on the activity of CYP3A4 in vitro. Methods:Midazolam was used as the probe drug, and an HPLC method for determining the metabolite of midazolam ( l-hydroxyl mid-azolam) in rat liver microsome incubation system was established. Three important parameters including the incubation time, concen-tration of rat microsome and probe concentration were optimized for rat liver microsome incubation system, and then the optimal incuba-tion system was applied to study the effect of MBSC extract on CYP3A4 activity and the potential mechanism. Results: The results showed MBSC crude extract could inhibit CYP3A4 activity to 38. 14% as that in the control group(P<0. 05) with IC50 value of 489. 7μg·ml-1 . The mechanism might be related to competition-noncompetition inhibition. Conclusion: MBSC extract exhibits inhibitive potency to CYP3A4 in in-vitro model. Further studies should be conducted to check the influence of MBSC on CYP3A4 in vivo.
ABSTRACT
Calculus Bovis (CB) is one of the precious traditional Chinese medicines (TCM) and has been widely used in oriental countries over 2000 years.It possesses a broad spectrum of pharmacological properties such as relieving fever,analgesic,diminishing inflammation,sedation,reducing blood pressure,recovering gallbladder functions,antioxygenation,and anti-tumor and improving immunity,et al.Due to the scarce resource and high price of natural CB,its substitutes,artificially synthesized CB and C.Bovis Sativus (CBS),also called in vitro cultured C.Bovis,have already been developed and widely used in medicine preparation.By using the literature material method,the current article explored literatures regard to pharmacological activities and clinical application of CB and its substitute,and the compound preparations were also included,from 1949 to 2016 in journals of domestic and foreign.All documents are summarized to provide a valuable reference for further basic or clinical research about CB and its substitute.
ABSTRACT
OBJECTIVE@#Evaluation and analyze the characteristics of balance function in patients with type 2 diabetes, and to find out the importance of proprioception, vision and vestibular in postural control.@*METHOD@#All subjects were divided into two groups, 37 normal individuals, 33 patients with type 2 diabetes mellitus. All were assessed by computerized posturography under six upright stance.conditions: including standing on the firm surface and foam with eyes open and closed.@*RESULT@#(1) On anteroposterior,the scores of proprioception, vision and vestibular were 93.96 ± 7.95, 80.22 ± 16.24, 70.87 ± 20.99, the normal were 98.00 ± 2.18, 91.44 ± 6.01, 80.44 ± 7.81. There were significances between diabetes mellitus group and normal control group (P 0.05.@*CONCLUSION@#The balance function of patients with type 2 diabetes decreased. It is the main characteristic that the vision and vestibular decreased more significantly in the postural control.
Subject(s)
Humans , Case-Control Studies , Diabetes Mellitus, Type 2 , Dizziness , Postural Balance , Proprioception , Vertigo , Vestibule, Labyrinth , Vision, OcularABSTRACT
[ABSTRACT]OBJECTIVETo investigate the change of fibrinogen, soluable intercellular adhesion molecules-1 (sICAM-1), soluable vascular cell adhesion molecule-1 (sVCAM-1) in the blood of elderly patients with sudden sensorineural hearing loss (SSHL) and the difference between different type of SSHL.METHODS40 elderly patients with SSHL were subdivided into different types according to the newest guideline of diagnosis and treatment of Chinese medical association.They were subdivided into two groups with or without comorbidities.The control group were made of 40 healthy elderly people.The expression of fibrinogen, sICAM-1 and sVCAM-1 in the blood serum were detected and statistically analysed.RESULTSThe expression of fibrinogen, sICAM-1 and sVCAM-1 in SSHL patients were higher than that of the control group with statistical significance.There is no significant difference between different types of SSHL,though significant difference were found between groups with and without comorbidities. CONCLUSIONThere is increased expression of fibrinogen, sICAM-1 and sVCAM-1 in elderly SSHL patients;microcirculation dysfunction may play an dominant role in the pathogenesis of elderly patients with SSHL.
ABSTRACT
Objective:To evaluate the inhibitory effect of 5 Chinese herbal medicinal ingredients baicalin, andrographolide, hes-peridin, polyphenols and daidzein on the activity of carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2). Methods: The spe-cial probes respectively for CES1 and CES2, namely imidapril and CPT-11, imidaprilat and SN-38, were used to investigate the poten-tial effect of the above drugs on CES1 and CES2 in rat liver microsomes incubation system. Results:Compared with that in the control group, the activity of CES1 and CES2 was not significantly influenced by the above 5 Chinese herbal medicinal ingredients ( P <0. 05). Conclusion:Baicalin, andrographolide, hesperidin, polyphenols and daidzein exhibit no inhibitory effect against CES1 and CES2, and further studies should be conducted to confirm the effect in vivo.
ABSTRACT
With the advent of bezoar substitutes, bezoar compound has been widely used in clinics. Bezoar is commonly applied in the traditional prescriptions for emergency. Due to the complex compositions and difficult soluble constituents, the prescriptions show the disadvantages of low bioavailability and slow onset in clinical application, and the effectiveness is usually related with the adminis-tration route and characteristics of dosage form of the preparations. The exiting bezoar compound and its new dosage forms were summa-rized in the paper, and the existing bezoar compound preparations were stated according to the characteristics of dosage forms and com-pound clinical application in order to promote the development and application of bezoar new dosage forms.
ABSTRACT
OBJECTIVE:To provide reference for rational clinical use of drugs and sound management thereof. METH-ODS:The relative data of antihypertensive drugs applied in 34 hospitals in Wuhan city during 2011 and 2013 were analyzed sta-tistically by using the analytical method of the Defined Daily Dose(DDD)recommended by WHO. RESULTS:Both consump-tion amount and DDDs of antihypertensive drugs in Wuhan city were increasing during 2011 and 2013,where calcium-channel blockers(CCB)enjoyed the largest consumption amount and the highest DDDs,with the constituent ratio of over 40% respec-tively,followed by angiotensinⅡreceptor antagonist (ARB) and angiotensin converting enzyme inhibitors (ACEIs). The con-sumption amount and DDDs of new compound preparation also increased. Top three single drugs in terms of consumption amount were amlodipine,levamlodipine and valsartan,while amlodipine,nifedipine and felodipine ranked the top three in DDDs list. CONCLUSIONS:Wide usage of antihypertensive drugs in Wuhan City are respectively CCB,ARB,ACEI,adrener-gic receptor blockers and diuretics,which are applied in current principle of antihypertensive drugs use and basically rational in clinical application.
ABSTRACT
To establish the HPLC fingerprints of Eucommia ulmoides at different ages of different varieties with pi-noresinol diglucoside as the reference material to provide the basis for the HPLC fingerprints in the enterprise quality standards of Eu-commia ulmoides from the GAP base of Chenzhou Dacheng Chinese Herbal Medicine Co. Ltd. . Methods: A column of ZORBAX E-clipse XDB-C18 (250 mm × 4. 6 mm, 5μm) was used. The mobile phase consisted of methanol-0. 1% phosphoric acid with gradient e-lusion. The detection wavelength was 277 nm, the column temperature was 25℃,the flow rate was 1. 0 ml·min-1 , and the injection volume was 5 μl. Results:The Eucommia ulmoides HPLC fingerprints including 14 common peaks were established with pinoresinol diglucoside as the reference material. The similarity of the HPLC fingerprints of 10 samples was over 0. 939. Conclusion:The method is accurate and reliable. The HPLC fingerprints can be used as the enterprise quality standards of Eucommia ulmoides for Chenzhou Dacheng Chinese Herbal Medicine Co. Ltd. .
ABSTRACT
Objective To explore the influence of different administration time on antidepressant effect of seven clinical common antidepressants. Methods Male mice were randomly divided into eight groups:venlafaxine (75 mg/kg), sertraline (20 mg/kg), fluoxetine (20 mg/kg), doxepin (15 mg/kg), mirtazapine (15 mg/kg), citalopram (40 mg/kg), trazodo?ne (50 mg/kg) and control (saline) groups. Each group contained 36 mice. Drugs were administered to 6 mice per group 30 min before forced swimming test at the 6 time points (9:00, 13:00 and 17:00 as light phase and 21:00, 1:00 and 5:00 as dark phase). Forced swimming test was applied to determine the influence of dosing time on anti-immobility effect of seven antidepressants at each time point. Results Immobility time in venlafaxine group and sertraline group significant?ly decreased compared with that of control group at all time points(all P<0.05). Moreover, anti-immobility effects of ven?lafaxine, fluoxetine, mirtazapine and doxepin were better during the dark phase than during the light phase (all P<0.05). In addition, immobility time in sertraline group decreased at the late part of dark phase (5:00) and the early part of light phase (9:00) compared with other phases (P<0.05). Conclusions Most antidepressants show 24-h rhythm dependent an?ti-immobility effects, but rhythmic patterns are not completely consistent among different antidepressants. Further study is needed to explore the chronopharmacological mechanism and clinical applications of these antidepressants.
ABSTRACT
Objective:To analyze the utilization and tendency of oral hypoglycemic agents in some hospitals of Wuhan from 2010 to 2012. Methods:The relative data of oral hypoglycemic agents used in 32 hospitals of Wuhan area during 2010-2012 were analyzed using consumption sum, DDDs and defined daily dose as the indices. Results:The consumption sum of oral hypoglycemic agents was increased year after year;acarbose and gliclazide were widely used and occupied front places among the drugs. However, the percent-age of traditional Chinese medicine used for decreasing blood sugar was declined. Conclusion:During 2010-2012, the DDDs value and the consumption sum of oral hypoglycemic agents in Wuhan area are stable and normal, and the application will be further developed.
ABSTRACT
Objective:To explore the effects of total saponins of panax ginseng ( TSPG) combined with icariin ( ICA) on learning and memory capability, oxygen free radical and apoptosis of hippocampal CA1 pyramidal cells in vascular dementia ( VD) rats. Meth-ods:The VD rats were obtained by occlusion of bilateral common carotid artery and reperfusion repeatedly combined with intraperitoneal injection of sodium nitroprusside. Spacial learning and memory ability was evaluated by 8-arm radial electric maze test on the 21st day af-ter the drug treatment, the activity of SOD and the level of MDA in the brain were determined, and the adjacent sections were used to de-tect fragmented DNA in apoptotic cells( TUNEL) . Results:The learning and memory ability of the model rats judged by the 8-arm radial electric maze test was significantly decreased compared with that in the sham-operated group (P <0.05). The combination treatment could significantly protect and improve all the evaluated indices of the model rats after the 3-week treatment (P<0. 05) with increased SOD (P<0. 05), and decreased MDA (P<0. 01) and TUNEL positive cells (P<0. 05). Conclusion:The combination drug treatment can significantly protect and improve the spacial learning and memory ability of VD rats, which is related with such effects as improving oxygen free radical metabolism and nerve cell injure in hippocampal CA1 region.
ABSTRACT
Objective: To study the input and output efficiency of the general hospitals based on the sampling data, in order to infer the operational efficiency of the general hospital in Hubei Province. Methods: Cobb-Douglas production function is extended and the input-output efficiency of 50 hospitals is analyzed by Data Exchange Agreement ( DEA). Results: Based on C-D production function expansion, through the sampling survey of input and output data, screening the input and output indicators of general hospitals, use DEA to conclude the put-output efficiency of 50 general hospitals in Hubei. Conclusion: The bed utilization rate of 50 general hospitals is low, the general hospital beds should be appropriately reduced, and corresponding policy recommendations are proposed.
ABSTRACT
OBJECTIVE To establish secretory otitis media(SOM) model induced by endotoxin and evaluate its reliability. METHODS Healthy 50 Sprague-Dawley rats of either sex( 250-300g)were randomly divided into experimental group(ET group) and control group(NS group),with 30 and 20 rats respectively. 35ul volume of 1mg/ml endotoxin from Pseudomonas aeruginosa and same amount of saline(NS) were transbullaly injected into the right tympanic bullas of the two groups. Six rats of ET group and four rats of NS group were killed postoperative on 6h,1d,3d,7d,14d respectively. The temporal bones were harvested for histological study. The left tympanic bullas served as control. Another four rats(each group 2 rats) were used for SEM study with the same method. One rat was killed and harvested for SEM observation of mucocilliary transporting system on the tympanic ostium of Eustachian tube. RESULTS ①LM(light microscope):The epithelial layer and subepithelial space(SES) were thicked mildly in ET group at 6 hours,and more heavily at 1 day with inflammatory cells infiltration (mostly polymorphonuclear leukocytes,PMNs). At 3 days,the same changes were observed most severely. By 14 days,the mucosal lining returned to normal. No obvious changes were observed in the NS group. ②SEM(scan electrical microscope):In ET group,the impairment of mucociliary transport system such as lodging,shedding of cilias were observed at 3 days and returned to normal at 14 days. No abnormal changes were observed in NS group. CONCLUSION Endotoxin can induce SOM with inflammatory changes peak at day 3 and return to normal by day 14.
ABSTRACT
Objective Through comparing the similarities and differences between respairing effect on rat’s gastric mucosal lesion by electroacupure (EA) at Meridian of Foot Yangming and Meridian of Foot Shaoyang, to explore the specificity of the correlation between Meridian of Foot and Stomach and the mechanism of the healing effect by EA at meridian of Foot Yangming for curing the gastric lesion. Methods Forty rats were randomly divided into 4 groups:blank group, model group, stomach tunnel group, gallbladder tunnel group. All rats (except normal group) were made model by water restraint stress (WRS). After corresponding experimental process, epidermal growth factor (EGF) and transforming growth factor alpha (TGF-?) of plasma, gastric mucous tissue concentration was detected with radioimmunoassay, and the expression of EGFR mRNA of above tissue was detected by the reverse transcriptase-polymease chain reaction (RT-PCR) method. Results The gastric mucosal lesion index of Foot Yangming group decreased significantly in comparison with that of other groups, while EGF, TGF-? of gastric mucous tissue concentration level of Foot Yangming group was obviously higher than that of model group and gallbladder tunnel group. EA oould up-regulate the expression gastric mucosal EGFRmRNA, and there was a more significant difference in the group by EA at Meridian of Foot Yangming than that in the model group and gallbladder tunnel group. Conclusion The curative effect of EA at points of Meridian of Foot Yangming on the gastric mucosa may be realized by the synthesis, secretion and release of the related EGF family factor, such as EGF, TGF-? and so on. Such special regulation of electroacupuncture on gastric mucosal tissue was related to the gene expression of EGFRmRNA, and that may be further mechanism of the curative effect of EA at points of Meridean of Foot-Yangming on gastric mucosal lesion. There existed corresponding correlation between Meridian of Foot Yangming and Stomach.
ABSTRACT
OBJECTIVE:To compare home-made mu'an-eye-gel(acyclovir plus honey) with commercial aciclovir(ACV)-eye-gel in releasing drug characteristics in vitro.METHODS:The in vitro drug release test was conducted by the third method of dissolution determination stated in Chinese Pharmacopeia together with bag filler method.The cumulative drug-releasing percentage and the acyclovir amount in mu'an-eye-gel versus ACV-eye-gel were determined by UV spec-trophotometry,and the accumulative releasing drug percentages of the two preparations were computed and their drug release behaviors w ere compared.RESULTS:The in vitro releasing behaviors of mu'an-eye-gel followed the Weibull kinetic equa-tion,however the vitro releasing behavior of commercial ACV-eye-gel followed the zero order kinetic equation,and the T80%and Q8 h had statistical significances between(mu'an-eye-gel:T80%=3.156?0.013(h),Q8 h=93.28?0.010(%);ACV-eye-gel:T80%=10.16?0.009(h),Q8 h=67.85?0.025(%)) 2 kinds of preparation.CONCLUSION:Mu'an-eye-gel is superior to the commercial ACV ophthalmic gel in both releasing velocity and accumulative drug release percentage.
ABSTRACT
Objective To investigate the expression difference of multidrug resistance and apoptosis related genes and its contribution to mechanisms of multidrug resistance in human lung adenocarcinoma parental cell line A 549 and cisplatin resistant cell line A 549 DDP Methods RT PCR and Immunohistochemical staining were performed to detect the mRNA expressions and protein production of multidrug resistance related protein (MRP),lung resistance protein (LRP),bcl 2,and C erbB 2 in A 549 and A 549 DDP .Results MRP,bcl 2,and C erbB 2 mRNA were expressed in A 549 ,but no LRP mRNA was detected in A 549 MRP,C erbB 2,and LRP mRNA expression levels in A 549 DDP were significant higher than those in A 549 ,otherwise,LRP mRNA was detected in A 549 DDP There was no difference of bcl 2 mRNA expressions between A 549 and A 549 DDP ( P =0 731) Bcl 2 protein expressions were strongly positive both in A 549 and in A 549 DDP MRP protein expressions in A 549 were faint positive,while C erbB 2 and LRP were negative MRP protein expressions in A 549 DDP was median positive C erbB 2 and LRP protein expressions in A 549 DDP were strongly positive Conclusions The heterogenous expression of MRP,C erbB 2,and LRP in A 549 and A 549 DDP may be associated with primary and secondary drug resistance in lung cancer