1.Preparation of Clopidogrel Bisulfate Tablets and Optimization of the Formulation and Technology
Xia SUN ; Xue WANG ; Qingming GUO ; Wei XIAO
China Pharmacy 2015;26(31):4429-4432
OBJECTIVE:To prepare Clopidogrel bisulfate tablets,and to optimize its formulation and technology. METHODS:The single factor test and compatibility test were used to optimize the fillers,disintegrating agents,adhesive,lubricants and prepa-ration technology;using sticking situation and disintegration time as indexes,the orthogonal test was used to optimize the amount of disintegrating agents [low substituted hydroxypropyl cellulose(L-HPC)],lubricants(hydrogenated vegetable oil and PEG6000), and the optimal technology was validated. The dissolution of prepared tablet and imported tablet(Plavix)in water,pH 2.0 hydro-chlorate buffer,pH 4.5 phosphate buffer(PBS)and pH 6.8 PBS were investigated,and influential factor test was conducted. RE-SULTS:Clopidogrel bisulfate tablets were prepared with dry granulating. The optimal formulation (1 000 tablets) was as follows as clopidogrel bisulfate 97.8 g,mannitol 84 g,amylum pregelatinisatum 36 g,L-HPC 8 g,hydrogenated vegetable oil 8 g, PEG6000 6 g;no tablet compressing sticking situation was found in prepared tablets and it owned medium disintegration time;ac-cumulative dissolution curves of prepared tablets in 4 kinds of medium were similar to those of Plavix;there were no significant dif-ference in results of influential factor test between prepared tablet and Plavix. CONCLUSIONS:Clopidogrel bisulfate tablets are prepared successfully,and the formulation is reasonable,practical,stable and controllable in quality.
2.Immunostimulatory role of CpG-containing oligodeoxynucleotide on the monocyte-derived dendritic cell in patients with chronic hepatitis B
Xiao-Xing XIANG ; Xia-Qiu ZHOU ; Jun-Xue WANG ;
Chinese Journal of Infectious Diseases 2001;0(06):-
0.05).However,neither CpG-ODN nor hTNF-? failed in improving the expression rates of CD1a.Conclusions CpG-ODN,like hTNF-?,has remarkable im- munostimulatory effect on the differentiation and maturation of monocyte-derived DC from patients with chronic hepatitis B.
3.Effect of Comprehensive Intervention Therapy of Losing Weight on Blood Leptin,Blood Lipid,Blood Glucose,Insulin in Adolescent Girl Students with Simple Obesity
xiao-yin, WANG ; yan-xia, CHEN ; xue-peng, GUO
Journal of Applied Clinical Pediatrics 2004;0(07):-
Objective To investigate the effect of comprehensive intervention therapy of losing weight on leptin and blood lipid,blood glucose,insulin in adolescent girl students with simple obesity.Methods Simple obesity adolescent girl students were accepted the losing weight therapy composed of the aerobic exercise,reasonable diet,behavior modification and medical supervision for 10 months.Then the changes of blood leptin and correlated hormone were examined before test,during test and after test,respectively.Results The leptin and correlated hormone levels were significantly higher in obesity subjects than that in normal subjects,and the levels of serum leptin was positively correlated with BMI and insulin.The blood leptin and blood lipid,blood glucose,insulin were decreased obviously after experimental losing weight.Conclusion Comprehensive intervention therapy of losing weight can significantly lose weight,leptin and insulin,so it plays an important role in modifying the metabolism disorder
4.Anti-depressant effect and mechanism of supercritical CO2 extract from Compound Chaigui Fang.
Lei CHEN ; Xiao-Fen ZHENG ; Xiao-Xia GAO ; Yu-Zhi ZHOU ; Xiao-Qing GUO ; Jun-Sheng TIAN ; Xue-Mei QIN
China Journal of Chinese Materia Medica 2014;39(14):2744-2750
The tail suspension test (TST), forced swimming test (FST) and chronic unpredictable mild stress (CUMS) model were used to evaluate the anti-depressant effect of supercritical CO2 extract from Compound Chaigui Fang (FFCGF). A nuclear magnetic resonance (NMR)-based metabonomics combined with multivariate statistical analysis was performed to explore the mechanism of FFCGF. Rats were conducted by CUMS procedure for 28 days and drugs were administrated at the same time. The body weight, sucrose preference, crossings and rearings in open-field tests were evaluated and the urine was collected simultaneously. The metabonomic profiles of rats' urine were analyzed by NMR and potential biomarkers were searched by multivariate statistical analysis. The results showed that administration of FFCGF significantly decreasing the immobility time in FST and TST and improving rats' body weight, sucrose preference, crossings and rearings in CUMS, which were indication that the anti-depressant effect of FFCGF was abvious. Significant differences in the metabolic profile of the CUMS treated group and the control group were observed, which were consistent with the results of behavioral tests. Decreased levels of acetic acid, succinic acid, 2-oxidation glutaric acid and citric acid and increased glycine and pyruvic acid in urine were significantly affected by the CUMS procedure and the 6 biomarkers were reversed evidently after administration of FFCGF. These changes were suggestion that the anti-depressant mechanism of FFCGF was associated with energy metabolism, lipid metabolism and amino acid metabolism.
Animals
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Antidepressive Agents
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chemistry
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isolation & purification
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pharmacology
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therapeutic use
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Behavior, Animal
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drug effects
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Body Weight
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Carbon Dioxide
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chemistry
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Depression
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drug therapy
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Drugs, Chinese Herbal
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chemistry
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isolation & purification
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pharmacology
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therapeutic use
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Male
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Mice
5.Comparison of adherence ability of bacteria on the surface of rigid gas-permeable contact lens made with different materials
Ying-ming, WANG ; Xue-feng, QIAN ; Xiao-feng, ZHANG ; Wei, XIA ; Lei, ZHONG ; Zheng-tai, SUN ; Jing, XIA
Chinese Journal of Experimental Ophthalmology 2013;31(8):717-721
Background Wearing contaclenincreasethe risk of infection of the cornea.Some studieshowed the gas-permeability of materialused foconstructing corneal contaclenione of the contributing factorrelated to corneal health.Objective Thistudy wato observe the in vitro adherence ability of differenbacterito rigid gas-permeable contaclense(RGP-CL) made with varioumaterials.MethodContaclensemade with hexafocon,enflufocon opolymethyl methacrylate (PMMA) were placed into Staphylococcuaureus,Staphylococcuepidermidis,oPseudomonaaeruginosbacterial suspension(0.5 MCF) fo24 hours.The strength of bacterial adherence watested and studied by the methyl thiazolyl tetrazolium (MTT) colorimetrimethod based on absorbance (value),and the vortex method waused to calculate the colony forming units.The bactericlump formation waexamined with scanning electron microscope (SEM).ResultMTcolorimetrimethod showed thathe adherence ability of Staphylococcuaureuto hexafocon (value) wasignificantly lowethan thato enflufocon and PMMA,respectively (q=7.379,8.207,P<0.01),buno significandifference wafound in the adherence ability of Staphylococcuaureubetween enflufocon and PMM(q =0.828,P>0.05).The adherence ability of Staphylococcuepidermidito XO and enflufocon walowethan thato PMM(q =14.000,12.800,P<0.01),buno significandifference wafound between the adherence of Staphylococcuepidermidito hexafocon and enflufocon material (q =1.200,P>0.05).There wano significandifference in the adherence ability of Pseudomonaaeruginosto all three material(F=2.155,P=0.138).The vortex method presented the colony forming unitof Staphylococcuaureuto hexafocon,enflufocon and PMMwith (37.9± 1.5)×106,(49.9±2.2)×106 and (67.4± 1.6)×106,respectively,with significandifference among them (F =206.240,P<0.01),showing the lowesvalue in hexafocon,the highesvalue in PMMand middle value in enflufocon (q=11.650,28.640,16.990,P<0.01),Moreover,colony forming uniof Staphylococcuepidermidito hexafocon,enflufocon and PMMwa(7.9 ± 1.3) × 106,(10.5 ± 1.5) × 106,(11.2 ±1.2) × 106,respectively.And thaof hexafocon walowethan one of the PMMmaterial (q =5.060,P<0.05).No significandifference wafound between hexafocon and enflufocon nobetween hexafocon and PMM(q =3.290,1.770,P>0.05).In addition,the resultthacorresponded to the vortex method were seen in the MTcolorimetriassay (F =0.232,P =0.799).SEM examination showed dispersed population of Staphylococcuaureuand Staphylococcuepidermidion the surfaceof hexafocon and enflufocon;while much more Staphylococcuaureuand Staphylococcuepidermidiadhered on the surface of PMMA,forming net-like appearance.Conversely,high numbeof Pseudomonaaeruginoswaseen on the surface of all three materials,withounoticeable differencein the bacterial shape and quantity on each of the material.ConclusionThe adherence ability of bacterito PMMistrongethan thaof hexafocon and enflufocon,and gas-permeable material of RGP-CL doenoimpacthe adherence ability of bacteria.
6.Therapeutic Observation of Acupuncture plus Auricular Point Sticking forPrimary Dysmenorrhea
Xia DENG ; Xiao XUE ; Guoran PENG ; Chun CHEN ; Panan WANG ; Xin GUO ; Kaipeng LIANG
Shanghai Journal of Acupuncture and Moxibustion 2015;(10):955-957
ObjectiveTo compare the clinical efficacies of acupuncture, auricular point sticking, and the combination of the two methods in treating primary dysmenorrhea by using randomized controlled method, for selecting the optimal treatment in treating primary dysmenorrhea, and to explore the nursing care method for primarydysmenorrhea from the perspective of Chinese medicine. MethodNinety patients with primary dysmenorrhea were randomized into an acupuncture group of 30 cases (group A), an auricular point sticking group of 30 cases (group B), and a combined group of acupuncture plus auricular point sticking of 30 cases (group C). The patients were given treatment 7 d ahead of the menstrual period, a menstrual cycle as a treatment course, totally for 3 courses. The pain score and clinical efficacies were observed and compared among the three groups for statistical analyses.Result The pain scores were significantly changed in the three groups after intervention (P<0.05), there were significant differences in comparing the pain scores among the three groups after intervention (P<0.05), group A and C were superior to group B (P<0.05), and group C was superior to group A (P<0.05). The total effective rate was 96.7% in group A, versus 93.3% in group B and 100.0%in group C, and the rank-sum test showed thatZ=7.675,P=0.022 (P<0.05).ConclusionThe three treatment methods are all effective in treating primary dysmenorrhea, while combining acupuncture and auricular point sticking can approach the optimal effect.
7.An exploration in the action targets for antidepressant bioactive components of Xiaoyaosan based on network pharmacology.
Yao GAO ; Li GAO ; Xiao-xia GAO ; Yu-zhi ZHOU ; Xue-mei QIN ; Jun-sheng TIAN
Acta Pharmaceutica Sinica 2015;50(12):1589-1595
The present study aims to predict the action targets of antidepressant active ingredients of Xiaoyaosan to understand the "multi-components, multi-targets and multi-pathways" mechanism. Using network pharmacology, the reported antidepressant active ingredients in Xiaoyaosan (saikosaponin A, saikosaponin C, saikosaponin D, ferulic acid, Z-ligustilide, atractylenolide I, atractylenolide II, atractylenolide III, paeoniflorin, albiflorin, liquiritin, glycyrrhizic acid and pachymic acid), were used to predict the targets of main active ingredients of Xiaoyaosan according to reversed pharmacophore matching method. The prediction was made via screening of the antidepressive drug targets approved by FDA in the DrugBank database and annotating the information of targets with the aid of MAS 3.0 biological molecular function software. The Cytoscape software was used to construct the Xiaoyaosan ingredients-targets-pathways network. The network analysis indicates that the active ingredients in Xiaoyaosan involve 25 targets in the energy metabolism-immune-signal transmutation relevant biological processes. The antidepressant effect of Xiaoyaosan reflects the features of traditional Chinese medicine in multi-components, multi-targets and multi-pathways. This research provides a scientific basis for elucidation of the antidepressant pharmacological mechanism of Xiaoyaosan.
Antidepressive Agents
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pharmacology
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Benzoates
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Bridged-Ring Compounds
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Coumaric Acids
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Drug Evaluation, Preclinical
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Drugs, Chinese Herbal
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pharmacology
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Flavanones
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Glucosides
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Glycyrrhizic Acid
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Lactones
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Medicine, Chinese Traditional
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Monoterpenes
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Sesquiterpenes
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Software
8.Surveillance of antimicrobial resistance of clinical bacterial isolates in a hospital during 2013
Rongfeng YAO ; Guoxiang XU ; Long XUE ; Juying SHEN ; Zhi LI ; Rong XIA ; Qiwen XIAO
Chinese Journal of Infection and Chemotherapy 2015;(3):244-248
Objective To investigate the antibiotic resistance of clinical isolates from hospital for the guidance of rational use of antibiotics .Methods Automatic VITEK‐2 system was used to identify bacterial strains and analyze the antimicrobial resistance . WHONET 5 .6 was applied for data analysis according to the breakpoints of Clinical and Laboratory Standards Institute 2013 . Results A total of 3 880 nonduplicate strains were collected in 2013 ,35 .2% (1 366/3 880) of which were gram positive organisms ,64 .8% (2 514/3 880) were gram negative bacteria .The top 6 most frequently isolated microorganisms were E . coli (20 .2% ) , K . pneumoniae (12 .0% ) , P . aeruginosa (11 .1% ) , coagulase negative Staphylococcus (9 .8% ) , A . baumannii (9 .8% ) ,E .f aecalis (8 .1% ) .The bacteria were mainly isolated from respiratory tract (51 .0% ) ,urine (26 .2% ) , and blood (9 .4% ) .The prevalence of both meticillin‐resistant Staphylococcus was higher than 72 .0% .No staphylococcal strainwasfoundresistanttolinezolid,vancomycinortigecycline.Amongthe509Enterococcusisolates,E.faecalisandE. f aecium accounted for 61 .5% and 32 .8% ,respectively .No enterococcal strain was resistant to vancomycin or tigecycline . Enterococcal isolates also showed low resistance (<2 .0% ) to teicoplanin and linezolid .About 67 .4% of the E .coli strains and 32 .0% of the K lebsiella isolates produced extended spectrumbeta‐lactamases.Thestrainsof E.coli,Klebsiella spp.,Enterobacterspp.,and Proteusspp.wererelatively susceptible to beta‐lactam/beta‐lactamase inhibitor combinations such as cefoperazone‐sulbactam and piperacillin‐tazobactam , carbapenems such as meropenem ,imipenem and ertapenem ,and amikacin (< 15 .0% of the strains were resistant) . K . pneumoniae isolates were more resistant than other gram‐negative bacilli .P .aeruginosa was relatively susceptible to amikacin , tobramycin ,cefepime ,gentamicin ,piperacillin‐tazobactam ,but more than 20% of these strains were resistant to meropenem and imipenem .More than 35 .0% of the A . baumannii isolates were resistant to any of the antimicrobial agents tested . Conclusions Antimicrobial resistance is still a serious threat in clinical antimicrobial therapy .It is important to promote the rational use of antimicrobial agents so that resistance is minimized . It is necessary to conduct epidemiological survey and proactively implement effective interventions in the clinical setting with relatively heavy burden of antimicrobial resistance .
9.Effects of agmatine on excessive inflammatory reaction and proliferation of splenic cells in mice with trauma
Zheng LIU ; Fengyan HOU ; He JIN ; Ya XIAO ; Xia FAN ; Xue YANG ; Jun YAN ; Huaping LIANG
Chinese Critical Care Medicine 2015;(2):110-114
ObjectiveTo observe protective effects of agmatine (AGM) on inflammatory response and spleen immune function in mice with trauma.Methods Forty-eight adult male C57BL/6 mice were randomly divided into three groups (n= 16 each), including control group, model group (bilateral femoral fracture and removal of 35% of the total blood volume), and AGM group (trauma/hemorrhage & AGM 200 mg/kg). Eight mice in each group were sacrificed at 3 hours and 24 hours, respectively, after modeling, and blood samples and tissue homogenate of spleen and liver were collected. The contents of tumor necrosis factor-α (TNF-α), interleukins (IL-6, IL-1β) in serum and liver tissue were determined with enzyme linked immunosorbent assay (ELISA). Serum aspartate transaminase (AST), alanine aminotransferase (ALT) and lactic dehydrogenase (LDH) were determined with automatic biochemistry analyzer. Spleen proliferation response stimulated with concanavalin A (ConA) was evaluated with methyl thiazolyl tetrazolium colourimetry (MTT).γ-interferon (IFN-γ) and IL-2 releases were determined with ELISA.Results Compared with control group, 3 hours after trauma/hemorrhage, the levels of serum TNF-α, IL-6, and IL-1β in model group were significantly elevated [TNF-α (ng/L): 145.38±31.50 vs. 23.06±11.14, IL-6 (ng/L): 496.94±50.76 vs. 47.13±17.47, IL-1β (ng/L): 321.31±43.02 vs. 29.25±16.24,allP< 0.01]. It was found that AGM treatment could alleviate the increase in serum pro-inflammatory mediators induced by trauma/hemorrhage, such as TNF-α (ng/L:111.56±25.47 vs. 145.38±31.50), IL-6 (ng/L: 412.56±44.33 vs. 496.94±50.76), IL-1β (ng/L: 273.38±45.25 vs. 321.31±43.02,P< 0.05 orP< 0.01). Twenty-four hours after trauma/hemorrhage, serum pro-inflammatory mediators were recovered to the levels in control group. There was no significant difference in TNF-α and IL-6 levels at 3 hours after trauma/hemorrhage among groups. Compared with control group, the expressions of liver TNF-α and IL-6 in model group were increased at 24 hours following trauma [TNF-α (ng/mg): 32.93±4.90 vs. 26.58±2.33, IL-6 (ng/mg): 11.20±1.66 vs. 8.38±0.89,bothP< 0.01]. However, AGM inhibited the level of TNF-α (ng/mg:28.92±3.16 vs. 32.93±4.90) and IL-6 (ng/mg: 9.03±1.28 vs. 11.20±1.66) in the liver as induced by trauma/hemorrhage (P< 0.05 andP< 0.01). At 24 hours after modeling, model group and AGM group had distinctly higher serum AST, ALT, LDH levels than those of control group [AST (U/L): 405.9±31.2, 245.7±22.1 vs. 128.2±15.9; ALT (U/L): 92.1±6.3, 51.6±5.0 vs. 30.1±3.2; LDH (U/L): 606.7±36.3, 478.7±25.3 vs. 384.0±16.6, allP< 0.01]. Nevertheless,the increase in serum AST, ALT and LDH was alleviated in AGM group (allP< 0.01). Meantime, trauma/hemorrhage produced a noticeable depression of proliferation of splenic cells and IFN-γ and IL-2 release stimulated with ConA compared with control group [proliferation rate: (40.97±4.13)% vs. (89.99±7.76)%, IFN-γ(ng/L): 91.6±12.3 vs. 353.2±21.5,IL-2 (ng/L): 53.4±6.4 vs. 91.0±12.2,allP< 0.01]. In contrast, AGM notably restored the capacity of proliferation response of splenic cells [proliferation rate: (74.86±5.75)% vs. (40.97±4.13)%, P< 0.01],enhanced the release of IFN-γ and IL-2 stimulated with ConA [IFN-γ (ng/L): 327.8±23.6 vs. 91.6±12.3, IL-2 (ng/L): 74.8±10.4 vs. 53.4±6.4, bothP< 0.01].Conclusion AGM can dramatically alleviate spleen immunosuppression, excessive inflammation and organ damage induced by trauma/hemorrhage.
10.Association between rheumatoid arthritis and shared epitope of HLA-DRB1 gene in Han nationality Neimenggu population
Xiao-Min LIU ; Xue-Gang ZHAO ; Chun-Xia GUO ; Shu-Min WEI ;
Chinese Journal of Rheumatology 2003;0(11):-
Objective To investigate the assoiation between rheumatoid arthritis(RA)and the pres- ence of the shared epitope(SE)of HLA-DRBI gene in Han nationality of Neimenggu population.Methods The method of DNA amplification with sequence-specific primers(PCR-SSP)was used to determine 17 alleles of HLA-DRB1*01,*04,*10 genotypes in 80 RA patients and 110 healthy controls from the Han nationality population in Neimenggu.Results The frequencies of SE were significantly increased in RA patiens com- pared with controls(48.8%:20%,P<0.01).Epitope analysis revealed that the most predominant allele subtype of DR4(*0405)was usceptible sequence in Neimenggu patients with RA(28.8%:12%,P<0.01).No statisticall significant difference of other subtypes of DR1,DR4 nd DR10 was noted including DRB1*0101(2.5%:0.9%), *0102(2.5%:0),*0103(1.25%:0.9%),*0104(2.5%:0),*0401(6.25:1.8%),*0402(3.75%:0.9%),*0403 (1.25%:1.8%),*0404(2.5%:1.8%),*0406(2.5%:2.7%),*0407(1.25%:0.9%),*0408(3.75 %:0.9%),*0409 (1.25%:0),*0410(2.5%:0.9%),*0411(0:0)and *1001(8.75%:4.5%)respectively.Logistic regression analy- sis showed that the disease of patients with SE homozgote was more severe than that of patients with heterozy- gote(P<0.01).Conclusion The results suggest that there is an association between SE of HLA-DRBI gene and susceptibility and severity of RA,especially,HLA-DR4 subtypes are strongly associated with RA in Han nationality in Neimenggu population.