Aim To evaluate the bioequivalence of demestic brodimoprim capsules and imported hyprim tablets and provide experimental basis for clinical application. MethodsA single dosage of Brodimoprim or hyprim was given to 18 healthy volunteers in a randomized 2-way cross-over test and the brodimoprim concentrations in plasma were determined by HPLC with β-naphtol as internal standard. The pharmacokinetic parameters and the relative bioavailability of the two preparations were calculated and their bioequivalence was evaluated. ResultsThe major pharmacokinetic parameters of test and reference preparations were as follows respectively:t1/2(α) (2.1 + 1.0) and (1.9+± 0.9) h, t1/3(β)(43.2±4.8) and (42.4±4.3)h, Tpeak(3.4±1.6) and (3.1±1.5) h,Cmax(5.9+ 0.9) and (5.9±1.0)μg · ml-1, AUC0～132(360.2± 55.3) and (358.7±52.6) μg · h · ml-1, AUC0～∞ (423.8±56.0) and (422.5±51.1) μg · h · ml-1. The relative bioavailability(F) of brodimprim capsules was (99.7± 4.8)%。 Conclusion . The multi-factorial analysis of variance showed that there was no significant difference in AUC0- 132between the test and reference preparations (P＞ 0.05) . The bioequivalent assumption was proved by further two one-side t-test and (1～2 α) confidence interval analysis in individuals, periods and forms of these two preparations.

[Objective] To discuss the mechanism and relative problems of lumbar traction. [Method] Relevant articles and retrospect clinical data in the author's hospital were reviewed. Review relevant articles and retrospect clinical data of our hospital. [ Result ] Traction force : 40 kg + 15% ～ 20% of body weight, fineness rate reached 83.5% in 1606 patients being treated. According to course of disease, fineness rate was 90. 1% in the group of less than 3 years, 68.2% in the group of more than 3 years. [ Conclusion] Lumbosacral nerve root leave the peak of the protruding nucleus and establish a new harmonious "root-disc" relationship after traction. The pressure and tension to the nerve root reduces or disappears, meanwhile, the pain of low back and leg is alleviated or eradicated. Appropriate traction weight and correct traction body posture are key factors of good therapeutic effect.

Objective: To analyze the chemical constituents of Polygonum multiflorum extract which may cause human liver cell damage and to explore the mechanism. Methods: Raw and processed Polygonum multiflorum were extracted by 70% ethanol, then raw and processed Polygonum multiflorum water-eluted material (RW and PW), 50% ethanol-eluted material (R50 and P50) and 95% ethanol-eluted material (R95 and P95) were obtained by absorbing through AB-8 macroporous resin, followed by water, 50% ethanol and 95% ethanol elution in order. The water extracts of raw and processed Polygonum multiflorum (RWE or PWE) were obtained by boiling them in water as usual. Normal human liver L02 cells were treated by different concentrations of eluted Polygonum multiflorum materials for different time, and the cell growth inhibition of each group was determined by methylthiazolyldiphenyl-tetrazolium bromide method. The chemical constituents which had a significant cytotoxicity to L02 cells were analyzed by high-performance liquid chromatography (HPLC). Morphological changes of L02 cells were observed by Giemsa staining and cell cycle distribution was observed by flow cytometry. Results: It was found that 95% ethanol-eluted extracts of raw and processed Polygonum multiflorum showed significant growth inhibition on normal human liver L02 cells, while the other components showed no significant inhibition on cell growth. HPLC analysis showed that the main component in 95% ethanol-eluted extract of raw and processed Polygonum multiflorum was emodin at content of (18.53+/-2.96)% and (10.28+/-1.34)% respectively. Cell cycle analysis showed that 95% ethanol-eluted material of Polygonum multiflorum and emodin had a similar significant effect of S phase arrest and all could induce L02 cell apoptosis. Conclusion: The main part of Polygonum multiflorum causing liver cell damage is the 95% ethanol-eluted extract, and emodin is one of the important chemical constituents leading to liver cell damage.

Aim To study on the protective effects on vein endothelial cell of scallop skite-glycosaminoglycan(SS-GAG)and the mechanism of anti-atherosclerosis action of SS-GAG.Methods The endothelial cell of human umbilical vein had been cultured in vitro, and we established an model of endothelial cell oxidative damage induced by oxidized low density lipoprotein (OX-LDL), MTT assay and chemical methods were used to test the influence of SS-GAG on proliferation activity of endothelial cell oxidative damage and analyze nitric oxide (NO) and endothelial nitric oxide synthase (eNOS).Results Oxidized lowdensity lipoprotein (OX-LDL) remarkably inhibited the ability of cell proliferation, decreased nitric oxide (NO) and endothelial nitric oxide synthase (eNOS) (P

Purpose To explore the feasibility of double low dose technology in multi-slice head and neck CT angiography, so to reduce contrast agent as well as reduce radiation dose. In that way, the hazards of radiation and the risk of contrast induced nephropathy would be reduced. Materials and Methods Fifty-one patients took double low proposal were recruited as double low group. Another 51 patients who took conventional proposal were recruited as conventional group. The scanning parameters of double low group were 100 kV, 300 mA, 0.7 ml/kg iodinated contrast agent and which of conventional group were 120 kV, 350 mA, 1.0 ml/kg iodinated contrast agent. The CT value of the vessels and image noise were measured. Signal-to-noise ratio (SNR), contrast-to-noise ratio (CNR), subjective image quality score, radiation dose and iodine load between the two groups were compared. Results The volume CT dose index (CTDIvol) of the double low group and the conventional group were 18.00 mGy and 33.86 mGy, respectively. And the effective dose were 3.85 mSv/(mGy · cm) and 7.25 mSv/(mGy · cm), respectively. The iodine loads were 224 mgI/kg and 320 mgI/kg, respectively. SNR and CNR at the aortic arch were higher in double low group than in conventional group, but which was not statistic significant (t=-1.572 and -1.783, P>0.05). The SNR and CNR of bilateral carotid arteries, internal carotid arteries, and middle cerebral arteries had no statistic significance between the two groups (t=0.341-1.739, P>0.05). The subjective image quality scores of double low group and conventional group were (3.69±0.47) scores and (3.70±0.46) scores, which showed no statistic difference (Z= - 0.213, P>0.05). Conclusion Approving images of multi-slice head and neck CT angiography can be obtained by using double low dose technology without adaptive statistical iterative reconstruction.

Objective To evaluate the changes in the expression of CC-chemokine ligand 3 (CCL3) and CC-chemokine receptor 5 (CCR5) in the spinal cord during hyperalgesia induced by remifentanil in rats with incisional pain.Methods Thirty-two male Sprague-Dawley rats,aged 2-3 months,weighing 240-260 g,were randomly divided into 4 groups (n=8 each) using a random number table:control group (group C),incisional pain group (group Ⅰ),remifentanil group (group R) and remifentanil+incisional pain group (group R+I).A 1-cm longitudinal incision was made in the plantar surface of the left hindpaw in anesthetized rats.While the model of incisional pain was established,remifentanil was infused for 60 min at 1 μg · kg-1 · min-1.At 24 h before infusion of remifentanil (baseline) and 2,6,24 and 48 h after the end of infusion,the mechanical paw withdrawal threshold (MWT) and thermal paw withdrawal latency (TWL) were measured.The rats were sacrificed after the last measurement of pain threshold,the lumbar segment (L4-6) of the spinal cord was removed for determination of CL3 and CCR5 mRNA expression (by real-time PCR) and CL3 and CCR5 expression (by Western blot).Results Compared with group C,the MWT was significantly decreased,the TWL was shortened,and the expression of CCL3 and CCR5 mRNA and protein was up-regulated in I,R and R+ I groups.Compared with I and R groups,the MWT was significantly dccreascd,the TWL was shortened,and the expression of CCL3 and CCR5 mRNA and protein was up-regulated in group R+I.Conclusion The mechanism by which remifentanil induces hyperalgesia is related to up-regulated expression of CCL3 and CCR5 in the spinal cord of rats with incisional pain.

A sensitive and selective liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the determination of betamethasone in human plasma. The analyte was isocratically eluted on a Venusil XBP C8 column (200 mm ×3.9 mm ID, 5 μm) with methanol-water with a triple quad LC-MS/MS using ESI with positive ionization. Ions monitored in the multiple reaction monitoring (MRM) mode were m/z 393.3→355.2 for betamethasone and m/z 361.3→343.2 for prednisolone (IS). Betamethasone was extracted from 0.5 mL human plasma with ethyl acetate. The validation study demonstrated excellent precision and accuracy across the calibration range of 0.5 - 80.0 injection in healthy Chinese volunteers.

Objective To evaluate the effects of different ratios of medicine dosage for sevoflurane and propofol on postoperative cognitive function in aged rats.Methods Sixty healthy male Wistar rats,aged 18-20 months,weighing 600-650 g,were divided into 6 groups (n =10 each) using a random number table:control group (group C),sevoflurane anesthesia group (group S),propofol anesthesia group (group P) and different ratios of mmedicine dosage for sevoflurane and propofol groups (group SP1,group SP2 and group SP3).Normal saline 10 ml was infused intravenously in group C.Group S inhaled 3.1％ sevoflurane.Propofol was infused intravenously at a rate of 40 mg · kg-1 · h-1 in group P.In group SP1,2.4％ sevoflurane was inhaled,and propofol was intravenously infused at a rate of 10 mg · kg-1 · h-1.In group SP2,1.8％ sevoflurane was inhaled,and propofol was intravenously infused at a rate of 20 mng · kg-1 · h-1.In group SP3,1.2％ sevoflurane was inhaled,and propofol was intravenously infused at a rate of 30 mg · kg-1 · h-1.Duration of anesthesia was 2 h in all the groups.After loss of righting reflex,open reduction and internal fixation was performed after tibial fracture was induced in the other five groups except group C.At 1 day after anesthesia,Y-maze test was performed,and the time spent on the novel arm and total number of entries into each arm were recorded,and fear conditioning test was carried out for determination of the rate of freezing time to reflect the cognitive function.The rats were sacrificed after behavioral testing,and the hippocampus was removed for determination of occludin,matrix metalloproteinase-2 (MMP-2) and MMP-9 expression by Western blot.Results Compared with group C,the time spent on the novel arm was significantly shortened,the total number of entries into each arm and rate of freezing time were decreased,the expression of occludin was down-regulated,the expression of MMP-2 and MMP-9 was up-regulated in the other five groups,and the most unmarked change in the indices mentioned above was found in group SP2 (P＜ 0.05 or 0.01).Conclusion Different ratios of medicine dosage for sevoflurane and propofol can induce postoperative cognitive decline,and inhaling 1.8％ sevoflurane and infusing propofol 20 mg · kg-1 · h-1 produce little influence on postoperative cognitive function in aged rats.

Objective To evaluate the effects of hydrogen-rich saline on incisional pain-remifentanil-induced hyperalgesia in rats.Methods Thirty-two male Sprague-Dawley rats,aged 2-3 months,weighing 240-260 g,in which the catheter was successfully inserted into the caudal vein,were randomly divided into 4 groups (n =8 each) using a random number table:control gourp (group C),remifentanil + incisional pain group (group R + I) and different doses of hydrogen-rich saline groups (H1 and H2 groups).A l-cm longitudinal incision was made through skin,fascia and muscle of the plantar aspect of the left hindpaw in chloral hydrate-anesthetized rats.Remifentanil 1 μg· kg-1 · min-1 was infused intravenously for 60 min sarting from beginning of establishment of incisional pain model in R + I,H1 and H2 groups.The equal volume of normal saline was infused intravenóusly for 60 rin instead of remifentanil group C.Hydrogen-rich saline 5 and 10 ml/kg were injected intraperitoneally at 10 min before establishment of incisional pain model in H1 and H2 groups,respectively.Paw withdrawal threshold (PWT) to yon Frey hair stimulation and paw withdrawal latency (PWL) to thermal stimulation were measured at 24 h before remifentanil infusion and 2,6,24 and 48 h after remifentanil infusion (T0-T4).The rats were sacrificed after measuremnt of pain threshold,and L4-6 segments of the spinal cord were removed for determination of the expression of R1 and 2B subunits-containing N-methyl-D-aspartate receptors (NR1 and NR2B) in total and membrane proteins by Western blot.The ratio between the expression of NR1 in membrane protein and in total protein (mNR1/tNR1) and NR2B in membrane protein and in total protein (mNR2B/tNR2B) was calculated.Results Compared with group C,PWT was significantly decreased,PWL was shortened,the expression of mNR1,mNR2B,tNR1 and tNR2B was up-regulated,and the ratios of mNR1/tNR1 and mNR2B/tNR2B were increased in R + I,H1 and H2 groups.Compared with group R + I,PWT was significantly increased,PWL was prolonged,the expression of mNR1 and mNR2B was down-regulated,and the ratios of mNR1/tNR1 and mNR2B/tNR2B were decreased in Ht and H2 groups.Compared with group H1,PWT was significantly increased,PWL was prolonged,the expression of mNR1 and mNR2B was down-regulated,and the ratios of mNR1/tNR1 and mNR2B/tNR2B were decreased in group H2.Conclusion Hydrogen-rich saline can attenuate incisional pain-remifentanil-induced hyperalgesia in rats and inhibition of trafficking of spinal neuronal NR1 and NR2B from cytoplasm to cell membrane may be involved in the mechanism.

Objective To evaluate the changes in the expression of spinal divalent metal transporter 1 (DMT1) during remifentanil-induced hyperalgesia in a rat model of incisional pain.Methods Thirtytwo male Sprague-Dawley rats,weighing 240-260 g,aged 2-3 months,were randomly divided into 4 groups (n =8 each) using a random number table:control group (group C),incisional pain group (group I),remifentanil group (group R),and incisional pain + remifentanil group (group I+R).In group C,normal saline was infused for 60 min at a rate of 0.1 ml · kg-1 · min-1.A 1-cm longitudinal incision was made through skin,fascia and muscle of the plantar aspect of the left hindpaw in sevoflurane-anesthetized rats,and normal saline was infused intravenously for 60 min at a rate of 1.0 μg · kg-1 · min-1 at the same time in group I.In group R,remifentanil was infused for 60 min at a rate of 1.0 μg · kg 1 · min-1 In group I+R,the model of incisional pain was established,and remifentanil was simultaneously infused for 60 min at a rate of 1.0 μg · kg-1 · min-1.At 24 h before normal saline or remifentanil infusion and 6,24 and 48 h after the end of infusion (T0-3),the mechanical paw withdrawal threshold (MWT) and thermal paw withdrawal latency (TWL) were measured.All the rats wcrc sacrificed after the last measurement of pain thresholds,and the spinal cord was removed for determination of DMT1 with/without iron-responsive element [DMT1 (+)IRE and DMT1 (-)IRE] expression (by Western blot analysis and immunohistochemistry).Results Compared with group C,the MWT was significantly decreased,and the TWL was significantly shortened at T1-3,and the expression of spinal DMT1 (-) IRE was significantly up-regulated in I,R and I+R groups (P＜0.05).Compared with I and R groups,the MWT was significantly decreased,and TWL was significantly shortened at T1-3,and the expression of spinal DMT1 (-) IRE was significantly upregulated in group I+R (P＜0.05).There was no significant difference in the expression of spinal DMT1 (+) IRE between the four groups (P＞ 0.05).Conclusion Spinal DMT1 (-)IRE activation may be involved in the mechanism underlying remifentanil-induced hyperalgesia in a rat model of incisional pain.