OBJECTIVE: To investigate the pharmacokinetics of 10 mg adefovir dipivoxil tablet formulations in 12 Chinese healthy subjects after a single dose and multiple doses. METHODS: A single dose and multiple doses of the formulations of adefovir dipivoxil tablets were given to each of 12 healthy male subjects. The concentrations of adefovir in plasma were determined by LC-MS/MS. The pharmacokinetic parameters were calculated by DAS2.0 programme. RESULTS: The obtained pharmacokinetic parameters of adefovir following adefovir dipivoxil tablets in a single dose and multiple doses group were as follows: ρmax were (24 ± 9), (24 ± 8) μg · L-1; AUC0-24 h were (210 ± 54), (213 ± 73) μg · h · L-1; AUC0-∞ were(236 ± 64), (250 ± 90) μg · h · L-1; t1/2 were (7.4 ± 1.2), (8.5 ± 2.1)h; tmax were (1.3 ± 0.7), (1.5 ± 0.6) h, respectively. Other main parameters in multiple doses group were ρavss (8.90 ± 3.06) μg · L-1 and DF (2.52 ± 0.66). CONCLUSION: There was no significant difference in pharmacokinetic parameters between single dose and multi-dose group. There is no accumulation following multiple doses of adefovir dipivoxil. Adefovir dipivoxil tablets were safe and well tolerated in Chinese subjects. Copyright 2012 by the Chinese Pharmaceutical Association.

Objective:To investigate the effect of Vitapex paste in the root canal for deciduous teeth with chronic apical periodontitis.Methods:200 children with chronic apical periodontitis were selected and divided into two groups.The observation group (108 cases)was given Vitapex paste.The control group (92 cases) was given Zinc oxide iodoform paste.The effect of Vitapex paste in root canal for deciduous teeth with chronic apical periodontitis was evaluated by filling quality after 1 month'treatment,the VAS scores before and after treatment,long-term curative effect were compared between two groups.Results:After 1 month'treatment,the suitable filling rate of observation group was higher than that of the control group(P＜0.05).There was no statistical significance in the VAS scores between two groups (P＞0.05).After 1 week'and 1 month'treatment,the pain feeling were alleviated in two groups and significantly lighter in the observation group(P＜0.05).After 6 months' follow-up,the success rate was 96.3％ in the observation group and 87.0％ in the control group,the success rate of observation group was higher than that of the control group (P＜0.05).Conclusion:The filling process of Vitapex paste was simple and easy,which had a good therapeutic effect on chronic apical periodontitis of deciduous teeth and could relieve the toothache of patients.

Objective To investigate the effects of rigid gas permeable contact lens (RGPCL) wearing 3 years on ocular surface in keratoconus.Design Retrospective case series.Participants 73 patients with keratoconus.Methods From July 2001 to July 2004,73 patients (142 eyes) wearing RGPCL for more than 3 years were collected in Peking University Optometry & Ophthalmology Center.Be- fore and at 1 year,2 years and 3 years of RGPCL wearing,density and morphologic changes of corneal endothelium were examined with non-contact specular microscope.Eye axial length,central and peripheral thickness of cornea were measured with A-scan pachymeter. All eyes were examined with slit-lamp microscope periodically.Main Outcome Measures Corneal endothelial density and morphology, corneal thickness,eye axial length,ocular surface changes.Results Before and at 1 year,2 years and 3 years of RGPCL wearing,aver- age corneal endothelial density was 2901.92?445.20,2862.78?497.13,2854.71?526.80,3015.61?421.22 (cells/mm~2)without significant difference statistically (F=1.571,P=0.20).Morphologic changes were not significant during 3 years.Eye axial length was 25.15?1.50, 24.93?1.36,24.78?1.25,25.39?1.31 (mm) without significant difference statistically (F=2.218,P=0.10).Corneal central thickness was 489.09?59.64,484.02?60.80,496.61?59.74,487.44?54.25(?m)without significant difference statistically (F=0.991,P=0.40).Peripheral thickness changes were also not significant statistically during 3 years.69 eyes with mild conjunctival congestion,12 eyes with corneal fluorescence stain and 6 eyes with corneal epithelial rough were found with slit-lamp microscope during follow-up.Conclusions For the patients with keratoconus,long term of RGPCL wear will not lead to significant ocular changes or severe ocular complications.

Objective To evaluate the quality status of recombinant human interferon α1b injection and find out some quality problems.Methods Totally 31 batches of recombinant human interferon α1b for injection and 11 batches of recombinant human interferon α1b injection from two enterprises were examined according to Chinese Pharmacopoeia Volume Ⅲ (2010),and the quality status of recombinant human interferon α1b injection was evaluated by statistical analysis of the results.Results All 42 batches of samples were qualified.The production process of each enterprise was steady.Conclusion At present the quality of recombinant human interferon αlb injection is generally good.The current standards are feasible,but the specified standard of osmolality needs to be improved.

Long-tem culture initiating cells(LTC-IC), and in vitro assay of hematopoietic stem/progenitor cells, still represent a heterogeneous population in terms of proliferative capacity and sensitivity to different growth factors. Human umbilical cord (CB) is rich of hematopoietic progenitor cells measured by clonogenic assays and stem cells capable of reconstituting the marrow after transplantation. The influence of culture conditions on the in vitro behavior of LTC-IC from CB was evaluated. First, by using IRES sequence, FL and TPO cDNA were recombined with retroviral vector pLXSN by gene recombination technology. The recombinant plasmid pLFSN, pLTSN, pLFTSN were transfected into human stromal cell line HFCL. Then, LTC-IC were evaluated in long term cultures, comparing five types of stromal feeder layers: human bone marrow stromal cell, human stromal cell line HFCL, and stromal cell lines HDF tranfected with FL gene, HLT transfected with TPO gene or HFT co-transfected with FL and TPO genes. The results were demonstrated that after 8 weeks of coculture, three types of stromal cell lines that supported the maintenance of CFU-C for up to 3 weeks in vitro were identified. However, cocultivation of human bone marrow stromal cell and CB CD34(+) cells on HFT, CFU-C production continued up to 6 weeks or longer on these stroma. The absolute LTC-IC frequency in CD34(+) cells on human bone marrow stromal cell (2.65 +/- 0.76/1 000 cells) was no significant difference with on HFT (3.65 +/- 0.58/1 000 cells). Thus, HFT acts by direct contact to maintain the phenotype and function of the most primitive and quiescent human progenitors. Furthermore, HFT cell line was selected as the optimal one for supporting long-term culture feeder. It was concluded that LTC-IC progenitors from cord blood maintain growing upon the FL/TPO gene-modified stromal feeder layers in vitro.

BACKGROUNDTo investigate whether Borna disease virus (BDV) infection is related to the schizophrenic patients from China.

METHODSA reliable Western-blot method for detection of BDV-p24 antibody was established by adjusting the reaction conditions of BDV-p24 recombinant protein and specific antibodies. The sera of schizophrenic patients and normal controls from Heilongjiang Province were screened for specific BDV-p24 antibody by this method, and the BDV-p24 antibody positive sera were confirmed by the Western-blot method with sera-GST protein absorption.

RESULTSTen of 116 (8.6%) schizophrenic patients were found to be positive for BDV-p24 specific antibody, while no BDV-p24 specific antibody was found in sera of normal controls.

CONCLUSIONSThe results demonstrate that the Borna disease virus infection also exists in China, and the infection is possibly associated with schizophrenia in some way.

Antibodies, Viral ; blood ; Blotting, Western ; Borna disease virus ; isolation & purification ; Humans ; Schizophrenia ; virology ; Viral Proteins ; immunology

OBJECTIVETo evaluate the early diagnostic value of contrast-enhanced ultrasound (CEUS) in acute renal failure (ARF) of rabbit.

METHODSThe rabbit model of ARF was established by intramuscular injection of 50% glycerin (12 ml/kg) into the hind legs of 18 New Zealand rabbits. CEUS was performed for both kidneys before injection and 6 hours after the injection. The slope rate of ascending curve (A), the slope rate of descending curve (alpha), area under curve (AUC), derived peak intensity (DPI), and time to peak (TTP) were measured in renal cortex of rabbits using Q-lab software package. Blood serum urea nitrogen (BUN) and serum creatinine (SCr) were measured.

RESULTSThe values of A and alpha before the injection of glycerin were (3.07 +/- 1.83) dB/s and (0.19 +/- 0.15)/s, respectively, which were significantly higher than the values after injection [ (2.76 +/- 1.31) dB/s and (0.09 +/- 0.02)/s, respectively] (P < 0.05). The values of AUC and TTP before the injection of glycerin were (137.4 +/- 68.4) dB s and (6.33 +/- 3.71) s, which were significantly lower than the values after injection [(309.5 +/- 88.9) dB s and (8.61 +/- 3.97) s, respectively] (P < 0.01). No significant change of DPI, BUN or SCr was found.

CONCLUSIONSCEUS can precisely display the hemodynamic change of ARF model of rabbit in the early stage, with superior sensitivity than BUN and SCr. It may be a promising imaging method for the early diagnosis of ARF.

Acute Kidney Injury ; diagnostic imaging ; physiopathology ; Animals ; Blood Urea Nitrogen ; Contrast Media ; Creatinine ; blood ; Early Diagnosis ; Rabbits ; Ultrasonography

BACKGROUNDAssessment of perfusion in the early period of acute renal failure (ARF) is important, and can not be made by conventional ultrasound. The aim of this study was to prospectively test in a rabbit ARF model whether real-time contrast-enhanced ultrasound (CEUS) can quantitatively evaluate the hemodynamic changes of renal cortex in the early period.

METHODSThe model of ARF was induced in 30 healthy New Zealand white rabbits (2.5 - 3.0 kg), by intramuscular injection of 50% glycerin solution (12 ml/kg). CEUS were performed on right kidneys before, 6 and 24 hours after glycerin injection. CEUS quantitative indexes were measured in renal cortex using QLAB software. Comparisons between different stages were performed using paired t test. The sensitivity of CEUS in diagnosing ARF was compared with blood serum urea nitrogen (BUN), serum creatinine (SCr) level and color Doppler flow imaging (CDFI).

RESULTSAmong quantitative indexes, time to peak (TTP) and area under curve (AUC) increased significantly from (5.86 ± 2.57) seconds and (124.4 ± 46.7) dB·s before glycerin injection to (7.66 ± 2.05) seconds and (288.1 ± 64.9) dB·s 6 hours after injection (P < 0.05). Slope rate of ascending curve (A) and descending curve (a) decreased slightly from (3.00 ± 1.22) dB/s and (0.19 ± 0.15) 1/s to (2.80 ± 1.45) dB·s and (0.09 ± 0.02) 1/s (P < 0.05). Twenty-four hours later, only AUC increased significantly from (124.4 ± 46.7) dB·s to (466.2 ± 52.2) dB·s (P < 0.05).

CONCLUSIONQuantitative indexes of CEUS might be useful in predicting the hemodynamic changes of renal cortex in the early six hours of ARF model.

Acute Kidney Injury ; diagnostic imaging ; Animals ; Contrast Media ; Rabbits ; Ultrasonography

Rh is a very important blood group like ABO blood system in transfusion medicine. It causes severe transfusion reaction and hemolytic disease of the newborn (HDN) if RhD blood group does not match between the donor and the recipient. The population of RhD negative is only about 0.2% - 0.5% in Chinese. Conversion of RhD positive RBCs to RhD negative is very important in clinical transfusion. This study was to try to modify RhD antigen located on the surface of A, B, O and AB red blood cells in order to convert RhD positive to RhD negative by the modification of four kinds of methoxypolyethylene glycol (mPEG) derivatives and to observe the effect of mPEG modification on cell morphology, structure and function. The result demonstrated that modification efficiency of mPEG-BTC (mPEG-benzotriazole carbonate) was better than other three kinds of mPEG derivatives. It could camouflage RhD antigen efficiently when the concentration reached to 1 mmol/L. The result also showed that there were no harmful effects of mPEG modification on cell morphology, osmotic fragility, hemolysis, AchE, cholesterol, ATP, 2,3-DPG and deformability. It is suggested that success in converting RhD positive RBCs to RhD negative was preliminarily achieved.
Erythrocytes ; drug effects ; immunology ; physiology ; Humans ; Polyethylene Glycols ; pharmacology ; Rh-Hr Blood-Group System ; immunology

The roots of Glycyrrhiza uralensis are widely used in Chinese medicine for their action of clearing heat, detoxicating, relieving cough, dispelling sputum and tonifying spleen and stomach. The reason why Glycyrrhiza uralensis has potent and significant actions is that it contains various active secondary metabolites, especially glycyrrhizic acid. In the present study, we cloned the cDNA coding 3-hydroxy-3-methylglutary CoA reductase (HMGR) involved in glycyrrhizic acid biosynthesis in Glycyrrhiza uralensis. The corresponding cDNA was expressed in Escherichia coli as fusion proteins. Recombinant HMGR exhibited catalysis activity in reduction of HMG-CoA to mevalonic acid (MVA) just as HMGR isolated from other species. Because HMGR gene is very important in the biosynthesis of glycyrrhizic acid in Glycyrrhiza uralensis, this work is significant for further studies concerned with strengthening the efficacy of Glycyrrhiza uralensis by means of increasing glycyrrhizic acid content and exploring the biosynthesis of glycyrrhizic acid in vitro.
Amino Acid Sequence ; Cloning, Molecular ; DNA, Complementary ; genetics ; Escherichia coli ; genetics ; metabolism ; Glycyrrhiza uralensis ; enzymology ; genetics ; Glycyrrhizic Acid ; metabolism ; Hydroxymethylglutaryl CoA Reductases ; genetics ; metabolism ; Mevalonic Acid ; metabolism ; Phylogeny ; Plant Roots ; enzymology ; Plants, Medicinal ; enzymology ; genetics ; Recombinant Proteins ; genetics ; metabolism