1.Plasma ibuprofen enantiomers and their pharmacokinetics in Beagle dogs determined by HPLC.
Hong-yan WANG ; Ai-ying KONG ; Bo YANG ; Liang-ping YAN ; Xin DI
Acta Pharmaceutica Sinica 2015;50(12):1607-1612
A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76.4% ± 36.2%, respectively, after intravenous administration of racemic- and R-ibuprofen. This study provides a theoretical basis for the safety of ibuprofen formula of injection drug.
Animals
;
Chromatography, High Pressure Liquid
;
Dogs
;
Ibuprofen
;
blood
;
pharmacokinetics
;
Stereoisomerism
2.Study of left ventricular systolic volume and synchrony in patients with premature ventricular complexes from the right ventricular outflow tract by instantaneous full-volume imaging
Jing YAO ; Di XU ; Fengxiang LU ; Yonghong YONG ; Hongping WU ; Meijuan LU ; Jian HONG ; Liang XU
Chinese Journal of Ultrasonography 2011;20(5):369-373
Objective To assess alternations in left ventricular volume and systolic synchrony in patients with frequent premature ventricular complexes(PVCs) from the right ventricular outflow tract(RVOT).Methods Twenty-nine patients with frequent isolated PVCs from RVOT were included and 30 healthy subjects as control.Instantaneous full-volume imaging(IFI) was performed to evaluate left ventricle volumetric parameters,including end-systolic volume (ESV),end-diastolic volume (EDV),stroke volume (SV),ejection fraction (EF),and systolic synchrony parameters,including systolic dyssynchrony index (SDI),dispersion end-systole (DISPES),mean end-systolic time (MES),pre-contraction time volume (PreContr) and post-contraction time volume (PostContr).Contraction front mapping was performed to visualize volumetric contraction sequence.All values of patients with PVCs were recorded during sinus beats (PVC-S) and premature ventricular beats (PVC-V) respectively.Results Significant differences were observed in left ventricular systolic volumetric and synchrony parameters between PVC-V and control subjects (P<0.01),as well as in MES and PreContr between PVC-S and control subjects (P<0.01).Conclusions Left ventricular systolic dysynchrony was demonstrated in patients with PVCs from RVOT.IFI was a novel tool to analyze left ventricular global and regional volumetric alternations.
3.Diagnostic Value of Lymphoscintigraphy in Chylous Ascites in Children
chu-gang, LI ; hong-liang, FU ; de-di, XU ; cheng-ren, SHI
Journal of Applied Clinical Pediatrics 2004;0(12):-
Objective To evaluate the value of lymphoscintigraphy in diagnosis of chylous ascites in children.Methods Lymphoscintigraphy was done in 6 cases,computed tomography(CT) was done in 4 cases,X-ray exam was done 42 times.And their video repore were compared.Results Lymphoscintigraphy was done in 6 cases,5 cases′ results were positive which diagnosed chylous ascites,and their leaking positions were also found.Conclusion Lymphoscintigraphy has the qualitative and orientational effect on diagnosis of children with chylous ascites.
6.The characteristics of hantanvirus Hunan03 strain S gene and the nucleoprotein structure prediction
Liang CAI ; Lidong GAO ; Yunzhi LIU ; Di QIN ; Jiangao LIU ; Shixiong HU ; Fuqiang LIU ; Zhifei ZHAN ; Ge ZENG ; Jiahui LIU ; Hong ZHANG
Chinese Journal of Microbiology and Immunology 2012;32(8):725-729
Objective To analyze the conding region of hantanvirus S gene and predict the structure of nucleoprotein for diagnostic antigen study.Methods RT-PCR was used to amplify the S gene of hantanvirus Hunan03 strain after designing specific primers.The amplification product was cloned into pGM-T vector and then the recombinant vector was transformed into E.coli TOP10,gene sequencing was carried out after blue-white selection and PCR screening for positive clones.The database of NCBI and Swiss-Prot/TrEMBL were used to predict and analyze the structure,biological characteristics and protein structures of S gene.Results The amplification product was about 1290 bp,the pGM-T/S vector was constructed and successfully sequenced,the whole length of the open reading frame (ORF) was composed of 1290 nucleotide residues,among them the GC content was 44.11% and the AT content was 55.89%,it was composed of 429 amino acids (20 kinds),the accession number of the sequence submitted to GenBank was JN712306,its homology of nucleotides to the 76-118 strain was 83% and the homology of amino acids was 98%,ten nonspecific variation sites were found.The grand average of hydropathicity was-0.405.There were three transmembrane domains and four non transmembrane domains in the secondary structure of nucleoprotein including 55% of helix structure,6.1% of sheet structure and 38.9% of loop structure.Conclusion The bioinformatics analysis of Hunan03 strain S gene might be important for provide the substructure data to reveal the significance of S gene characteristics on hemorrhagic fever renal syndrome (HFRS) prevention and control.
7.Multicenter research on efficacy and tolerance of memantine in Chinese patients with Alzheimer's disease
Xia CHEN ; Zhen-Xin ZHANG ; Xin-De WANG ; Jing-Li YAO ; Sheng-Di CHEN ; Cai-Yun QIAN ; Shi-Fu XIAO ; Liang SHU ; Hong-chuan TANG
Chinese Journal of Neurology 1999;0(06):-
Objective To evaluate the efficacy and safety of memantine in the treatment of patients with Alzheimer' s disease (AD).Methods This was a 16-week,multi-center,randomized,double blind, placebo-controlled clinical trial (Study 10116).A total of 258 AD patients (MMSE score 5—18) were randomized in a 1:1 ratio into either memantine 10—20 mg/day (MEM,n=128) or placebo (PBO,n= 130) group for 16 weeks.Efficacy was primarily assessed in terms of changes of severe impairment battery (SIB) score in patients from baseline up to SIB assessment in the 16th week (16-week completers set, CS16).While ehanges of MMSE,ADCS-ADL_(19),and NPI (neuropsychiatric inventory) were evaluated as secondary efficacy parameters on both CSI6 and full-analysis set (FAS).Safety was assessed by physical examination,lab assays,ECG,and adverse events.Results 236 subjeets (CS16:MEM n=117,PBO n=119) were eligible for the efficacy assessment.No statistically significant difference between the treatments was observed on the primary and seeondary efficacy analysis,although both treatment groups had a slight increase from baseline in SIB total score.Post hoe evaluation of the data identified two bias factors that had a significant impact on the results of the pre-protoeol specified primary and secondary analyses.In a re-analysis of the data (CS16_(modified),MEM n=94,PBO n=95) excluding patient data affeeted by these factors,memantine-treated patients showed a statistically significant improvement related to placebo in the 16th week on the SIB (MEM 2.2 vs PBO 0.3,P=0.04),MMSE (MEM 1.0 vs PBO 0.1,P=0.03),and ADL (MEM 0.1 vs PBO-1.6,P=0.02) scales,indicating that memantine improved the cognitive function of AD patients and stabilized the activity of daily life.Memantine was well tolerated with an adverse event profile similar to that of placebo.Conclusion This study provides further support for pre-existing data,showing that memantine is efficacious,safe,and well-tolerated in patients with moderate to severe AD.
8.Changes of Cerebrospinal Fluid ?-Endorphin and C-Reactive Protein in Children with Central Nervous System Infection
xiang-hong, DENG ; ru-zhu, LIN ; wen-ying, LAI ; di-hui, LIU ; ming, LI ; jing, RUAN ; jin-sheng, LIANG ; jian, CHEN
Journal of Applied Clinical Pediatrics 2004;0(09):-
Objective To determine the changes of cerebrospinal fluid(CSF) ?-endorphin(?-EP) and C-reactive protein(CRP) in children with central nervous system(CNS) infection.Methods Sixty-five children suffered from CNS infection were determined the plasma and CSF ?-EP and CRP concentration during the acute and recovering stage with radioimmunoassay, which included 48 viral encephalitis, 12 purulent meningitis and 5 tuberculou meningitis,and 24 non-CNS disease children were as control group.Results The concentrations of plasma and CSF ?-EP of every experimental group were obviously higher than those of control group during the early stage of CNS infection and these were obviously lower during the recovering stage. The serum concentration of CRP during acute stage was significantly higher than that during recovering stage. No change of serum and CSF CRP concentration was determined during either the acute or recovering stage in the other two experimental groups.Conclusions Determining the plasma and CSF ?-EP is mea-(ningful) in early diagnosis of CNS infection,and determining the serum CRP at the same time may be helpful in differentiating septic and inseptic infection.
9.Evaluation of global and regional left ventricular systolic function in patients with frequent isolated premature ventricular complexes from the right ventricular outflow tract.
Jing YAO ; Jing XU ; Yong-Hong YONG ; Ke-Jiang CAO ; Shao-Liang CHEN ; Di XU
Chinese Medical Journal 2012;125(2):214-220
BACKGROUNDFrequent premature ventricular complexes from the right ventricular outflow tract (RVOT-PVCs) are associated with left ventricular dysfunction. This study adopted two-dimensional speckle tracking imaging to evaluate global and regional left ventricular myocardial function in patients with frequent RVOT-PVCs.
METHODSThis study included 30 patients with frequent RVOT-PVCs and 30 healthy subjects. Aortic systolic velocity-time integral (AoVTI) and myocardium strain in circumferential (CS), radial (RS) and longitudinal (LS) directions were evaluated by conventional echocardiography and speckle tracking imaging. All values of patients with RVOT-PVCs were recorded during sinus (PVC-S) and PVC beats (PVC-V).
RESULTSSignificant differences were demonstrated in global CS, RS and LS between the control subjects and the PVC-V (CS: (17.46 ± 2.48)% vs. (11.52 ± 3.28)%, RS: (48.26 ± 10.20)% vs. (20.92 ± 9.78)%, LS: (19.89 ± 2.62)% vs. (11.79 ± 3.66)%, P < 0.01), and in segmental RS and LS of nearly all the left ventricular segments. Statistical differences in segmental CS between the PVC-V and the control subjects were only observed in anterior, anteroseptal and septal segments (only seen in anteroseptal and septal segments at apex). Furthermore, V/S AoVTI (AoVTI during the PVC beat divided by AoVTI during the sinus beat, then multiplied by 100%) correlated with coupling interval (r = 0.67, P < 0.001) and global strain (CS: r = 0.48, P = 0.007; RS: r = 0.65, P < 0.001; LS: r = 0.65, P < 0.001).
CONCLUSIONSFrequent RVOT-PVCs can induce global and regional left ventricular systolic dysfunction. The reduction of hemodynamic parameters relates to the coupling interval and the global systolic function.
Adult ; Female ; Humans ; Male ; Middle Aged ; Retrospective Studies ; Ventricular Function, Left ; physiology ; Ventricular Premature Complexes ; physiopathology
10.Preliminary report of laryngeal preservation in the surgical salvage of recurrent laryngeal cancer
Xiao-Ming LI ; Bin DI ; Zhen-Feng TAO ; Qi SONG ; Shu-Fen XIAO ; Hong-Xia LI ; Yong-Liang SHAO
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2012;47(7):532-535
Objective To explore the plausibility of laryngeal preservation in salvage surgery of recurrent laryngeal carcinoma.Methods Comprehensive clinical and radiological assessments on a specific group of patients with recurrent laryngeal cancer and their relapsed tumors were carried out to determine the methods and indications of salvage surgery for preservation of laryngeal functions.Salvage surgery with preservation of larynx was performed in a selective of 36 laryngeal cancer patients with relapsed tumors in their larynges after radiotherapy or partial laryngectomies.All patients were regularly followed up after discharge from the hospital. Postoperative survival was calculated by Kaplan-Meier's method.Results Among various laryngeal preservation regimens given,a second transoral laser surgery was carried out in 4 cases,horizontal hemilaryngectomy in 4 cases,vertical hemilaryngectomy in 13 cases and Majer-Piquet's operation in 15 cases,respectively.Simultaneous neck dissection was conducted in 18 cases.Postoperative complications were encountered in 6 cases,most common of which were local infection and laryngeal fistula with no hospital mortality and other major morbidities.Five cases with immediate postoperative complicatios were cured with proper management.The remained one case undergone vertical partial laryngectomy for recurrence after tumor resection via laryngeal fissure received postoperative radiation due to positive surgical margin,and complicated laryngeal atresia and obstruction with loss of his laryngeal functions, Local recurrence was observed in 5 cases and simultaneous locoregional recurrence was seen in 1 case,with the resulting local control rate of 83.3% (30/36).The 3-year postoperative survival rate was 80.6%.The cause of death was tumor recurrence in 3 cases,distant metastasis in 3 cases and non-tumor-associated disease (heart attack) in 1 case,respectively.Conclusions Salvage surgery with laryngeal preservation can be carried out in the selected cases with early or locally-confined recurrent lesions within the larynx,on the condition that the recurrent tumors be assessed thoroughly and indications for associated surgical techniques be evaluated properly.