In this paper, absorption and pharmacokinetic study of Radix Rehmanniae was studied by liquid chromatography coupled with mass spectrometry method after oral administration to rats. By comparing the chromatograms of ultraviolet, full scan, extracted ion and selective reaction monitoring (SRM) of standard solution, Radix Rehmanniae, blank plasma and rat plasma post drug administration, catalpol and ajugol were found to be the main compounds absorbed from Radix Rehmanniae. Plasma concentrations of aucubin, dihydrocatalpol, rehmannioside A (or rehmannioside B/ melittoside) and rehmannioside D were very low. Quantitative method for catalpol and aucubin and semi-quantitative method for other compounds in rat plasma were established. The pharmacokinetic study of those absorbed components was conducted after oral administration of 6 g x kg(-1) Radix Rehmanniae water extract to rats. Cmax, t(1/2) and AUC(0-infinity) of catalpol and ajugol were (2349.05 +/- 1438.34) and (104.25 +/- 82.05) ng x mL(-1), (0.86 +/- 0.32) and (0.96 +/- 0.37) h, (4407.58 +/- 2734.89) and (226.66 +/- 188.38) ng x h x mL(-1), respectively. tmax was at 1.00 h for catalpol and ajugol. Both catalpol and ajugol were absorbed and excreted rapidly.

Objective To investigate the feasibility of achieving consistent image quality with dose reduction technology in lumber spine MSCT examination with Z-axis automatic tube current modulation (ATCM). Methods Forty-eight patients diagnosed as lumber intervertebral disc protrution scanned twice by MSCT before and after interventional operations with the same coverage from third lumbar vertebra to first sacral vertebra. The first scan (FM) was with fixed tube current of 320 mAs. The follow-up scan was with ATCM with noise index (NI) of 12.0 HU. At the levels of L3-4, L4-5 and 15-S1, image quality, image noise and radiation dose were measured and analyzed. Image quality and radiation dose were compared by paired t-test and the image noise was compared by ANOVA test. Results The dosage of the ATCM had a 31.3% reduction compared with FM, the average DLP was(187.9±66.4)mGy·cm and(273.4±45.4) mGy·cm respectively, where t = 8.205, P < 0.05. The average noise and their deviations for the FM group were (9.8±2.4) HU,(9.9±2.4) HU, and (11.5±3.2) HU at level of L3-4, L4-5, 15-S1, respectively. With ATCM, the average noise was(12.0±0.8) HU, (11.7±0.6) HU, and (11.7±1.4) HU, respectively. There was statistical difference between the two groups (F = 23.31, P < 0.05). The image quality scores for the FM group were (4.7±0.3), (4.5±0.2), (4.5±0.2) and showed no statistical difference to ATCM group (4.6±0.3), (4.5±0.2), (4.5±0.2) at level of L3-4, L4-5, L5-S1, respectively, where t = 1.000, P > 0.050 Conclusion ATCM technique with the noise index setting at 12.0 HU can achieved a 31.3% dose reduction while keep the consistent image quality for lumbar spine MSCT study.

objective To study the pharmacokinetics of lignans components in Shengmai granule in volunteers and in mice. Methods After oral administration of Shengmai granule (3.6 g/person) for the volunteers and ig administration of the drug (4.7 g/kg) for the mice, the plasma was collected at different time points. The lignans components in Shengmai granule and in the plasma were analyzed by HPLC to monitor the changes of plasma concentration of schisandrind. Pharmacokinetic parameters were calculated from the plasma concentration- time data with the 3P97 software package. Results After oral administration of Shengmai granule by volunteers and mice, schisandrin and some new components in plasma were detected. The new components may be the metabolites of schisandrin. The main pharmacokinetic parameters of schisandrin in mice and in volunteers were as follows: T1/2ka was 0.03 and 0.04 hour, T1/2ke 0.88 and 0.86 hour, Vd 19.12 and 1.73 L? kg- 1, CL 15.06 and 1.46 L? h- 1? kg- 1, Cmax 1.196 and 0.098 mg? L- 1, Tpeak0.21 and 0.50 h, AUC0- ∞ 1.096 and 0.137 mg? h? L- 1, respectively. Conclusion Schisandrin in Shengmai granule can be absorbed in the volunteers and mice after oral administration. It can be absorbed and eliminated rapidly, and can be transformed into the metabolite. The pharmacokinetics of plasma Schizandrin complies with linear kinetic course.

AIM: To study the pharmacokinetics of flavonoids in mice after ig administration of Xiexin Decoction (Radix et Rhizoma rhei, Rhizoma coptidis, Radix Scutellariae). METHODS: Mice were given a single ig dose of Xiexin Decoction 4.5, 9.0 or 18.0 g/kg. Flavonoids in plasma were analysed by HPLC and plasma concentration of baibalin was determined. Pharmacokinetic parameters were calculated from the plasma concentration-time data with the DAS software package. RESULTS: After ig administration of Xiexin Decoction in mice, baicalin, baicalein and another flavonoid were detected in plasma and baicalin concentration was the highest of the three kinds of flavonoids in plasma. After a single ig dose of Xiexin Decoction 4.5, 9.0 or 18.0 g/kg, the pharmacokinetic parameters of baicalin were as follows:T_ 1/2 =2.77、5.69、6.20 h,AUC_ 0-∞ =9.09、23.49、39.57 ?g?h/mL,CL= 12.52 、 6.962 、 11.50 L?h/kg,V_d= 50.11 、 79.56 、 102.95 L/kg,C_ max1 =1.89、3.32、4.79 ?g/mL(T_ p1 = 0.08 h ), C_ max2 =1.46、2.57、4.16 ?g/mL(T_ p2 =3 h), respectively. CONCLUSION: Three kinds of flavonoids can be absorbed after ig administration of Xiexin Decoction in mice, of which baicalin is the major component.

AIM: To observe the effects of Egr-1 gene knockout on the expression of inflammatory-related factors in pancreatic tissue in a mouse acute pancreatitis model.METHODS: The experimental pancreatitis was induced by high-dose of cearulein in wildtype mice and Egr-1 knockout mice.The pancreatitis indexes,such as serum amylase,pancreata edema,and myeloperoxidase(MPO) levels in pancreata and lungs were recorded.The mRNA levels of tissue factor(TF),plasminogen activator inhibitor(PAI-1),monocyte chemoattractant protein(MCP-1),Gro-1,IL-6 and ICAM-1 were measured by quantitative PCR.RESULTS: Contrary to wildtype mice,typical pancreatitis was not induced by high-dose cearulein in the Egr-1 knockout mice,not only markedly reduced edema in pancreata and lungs,but decreased MPO levels in lungs as well were found.Furthermore,the mRNA of TF,PAI,MCAP,ICAM-1 and IL-6 in pancreata were significantly decreased in Egr-1 knockout mice.CONCLUSION: The severity of pancreatitis and lung damage is ameliorated in Egr-1 knockout mice stimulated by high-dosage of cearulein,which was probably mediated by decreasing expression of inflammatory-related factors in pancreata,such as TF,PAI,MCP-1,ICAM-1 and IL-6.

OBJECTIVETo evaluate the efficacy and safety of vardenafil on men with erectile dysfunction (ED) of various etiologies.

METHODSA total of 88 men with mild to severe erectile dysfunction were enrolled in the randomized, double-blind, placebo-controlled, fixed-dose trial of 12 weeks of treatment with either placebo or 5, 10 and 20 mg of vardenafil.

RESULTSThis study indicated that vardenafil dosages of 5, 10 and 20 mg were significantly superior to placebo for the treatment of ED, on the basis of the primary study endpoints of the EF domain score of the IIEF, diary-recorded success rates for penetration and maintenance of erection during the intercourse and the GAQ. Vardenafil was well tolerated. The incidence of adverse events was higher for vardenafil than for placebo.

CONCLUSIONOral vardenafil therapy has a high efficacy and a low incidence of adverse events for ED patients with mixed etiologies.

Administration, Oral ; Adult ; Aged ; Double-Blind Method ; Erectile Dysfunction ; drug therapy ; Humans ; Imidazoles ; adverse effects ; therapeutic use ; Male ; Middle Aged ; Phosphodiesterase Inhibitors ; adverse effects ; therapeutic use ; Piperazines ; adverse effects ; therapeutic use ; Sulfones ; adverse effects ; therapeutic use ; Triazines ; adverse effects ; therapeutic use ; Vardenafil Dihydrochloride

Objective To quantitatively compare the diagnostic capability of 68Ga-NGR and 18F-FDG in well-differentiated hepatocellular carcinoma (HCC) bearing mice by microPET/CT imaging.Methods The in vitro cellular uptake, in vivo microPET/CT imaging and biodistribution studies of 68Ga-NGR and 18F-FDG were quantitatively compared in SMMC-7721-based well-differentiated HCC.The human fibrosarcoma (HT-1080) and human colorectal adenocarcinoma (HT-29) cells/xenografts were respectively used as positive and negative reference groups for CD13.The expression of CD13 was qualitatively verified by immunohistostaining.The levels of CD13 and glucose-6-phosphatase (G6Pase) were semi-quantitatively analyzed by Western blot test for all 3 types of tumors.Two-sample t test was used for data analysis.Results The in vitro cellular uptake showed that the 68Ga-NGR uptake in SMMC-7721 and HT-1080 cells was higher than that in HT-29 cells, and the 68Ga-NGR uptake was higher than 18F-FDG uptake in SMMC-7721 cells.The in vivo microPET/CT imaging results revealed that the uptake of 68Ga-NGR in SMMC-7721 tumor was (2.17±0.21) %ID/g, remarkably higher compared to (0.73±0.26) %ID/g of 18F-FDG uptake (t=8.826, P<0.01).The tumor/liver ratio of 68Ga-NGR was 2.05±0.16, which was 2.03-fold higher than that of 18F-FDG.In the HT-1080 tumors, the uptakes of 68Ga-NGR and 18F-FDG were both high, and the values were (2.46±0.23) %ID/g, (3.47±0.31) %ID/g.The uptake of 68Ga-NGR was significantly lower than that of 18F-FDG in HT-29 tumors: (0.67±0.20) %ID/g vs (3.17±0.29) %ID/g;t=4.221, P<0.01.Western blot and immunohistostaining results were as follows: HT-1080(CD13+, G6Pase-), SMMC-7721(CD13+, G6Pase+), HT-29(CD13-, G6Pase-).Conclusions The uptake of 68Ga-NGR is higher than 18F-FDG uptake in SMMC-7721 tumor bearing mice, therefore it is worthwhile to consider the feasibility of clinical translation for PET/CT in diagnosis of HCC.Furthermore, because of the difference in 68Ga-NGR and 18F-FDG avidities in tumors with different molecular phenotypes of CD13 and G6Pase, there is an underlying potential for molecular imaging in the determination of molecular phenotypes.

Objective To evaluate the clinical application value of multi-slice helical CT volumetric (VH) scanning in lumber spine. Methods One thousand of patients with back and leg pain who underwent CT examinations were selected as subjects. We simulated the traditional protocol of single-slice(SS) discrete scanning for L3/4, L4/5, and LS/S1 intervertebral discs. The VH scanning mode was performed with 120 kV, 210 mAs,pitch of 1.5 and coverage of 97. 5 mm. The simulated SS scanning mode was performed with 120 kV, 240 mAs and coverage of 45.0 mm. The diagnostic outcomes and the radiation doses were compared between the two scanning modes. Two groups doctors observed ten terms, including the osseous spinal stenosis,narrowed intervertebral space and so on in two scanning modes respectively. Then consistency analysis of the data was carried out. Results The VH scanning mode showed far more features than the SS mode. The detection rates of the VH mode in the osseous spinal stenosis, narrowed intervertebral space,herniated nucleus pulposus, narrowed lateral recess, vertebral lesion, hypertrophy of L5 transverse process,abnormal direction of facet, facet degeneration, lumbar spondyloschisis, and paraspinal soft tissue were 11.8% (n =118), 38. 5% (n =385), 9. 3% (n =93), 46. 8% (n =468), 31.4% (n =314), 5.7% (n =57), 25.4% (n = 254), 49. 7% (n = 497), 9.9% (n = 99), and 0. 6% (n = 6) respectively, while the detection rates of the SS mode in ten terms were 5.6% (n = 56), 0, 0. 6% (n = 6), 27. 9% (n = 279),22.4% (n =224), 1.2% (n = 12), 16.7% (n = 167), 37.2% (n =372), 0.5% (n =5), and 0.2%(n = 2) respectively. The difference between the two groups had statistically significance (average P <0.05), except the paraspinal soft tissue abnormal (P > 0.05). The detection rates of the VH mode were higher than the SS mode in the osseous spinal stenosis, narrowed intervertebral space, herniated nucleus pulposus, lumbar spondyloschisis, being 6.2% (n = 62) , 38. 5% (n = 385) , 8.7% (n = 87), and 9.4%(n =94), respectively. In addition, VH mode only partially showed the articular facets, narrowed lateral recess, hypertrophy of L.5 transverse process, and paraspinal soft tissue. We could not acquire the imaging slices paralleling to intervertebral discs in SS mode in 467 patients (46.7%) with lumbosacral angle greater than 35°. The radiation dose of VH mode (164.9 mGy/em) was slightly higher than SS mode (147.0 mGy/cm) Conclusion MSCT VH scanning mode can significantly improve the diagnostic rate of lumbar spine diseases compared with SS mode, and was not restricted by the lumbosacral angle with slightly increasing radiation dosage.

OBJECTIVETo elucidate how chronic prostatitis affects the expression and activity of the plasminogen activator (PA) system and relates to male infertility.

METHODSTwenty-three normal fertile males and 80 chronic prostatitis patients (40 fertile and 40 infertile) were included in this research. SDS polyacrylamide gel electrophoresis and fibrin overlay method were used to estimate the total PA, and tissue PA (tPA), urokinase type PA (uPA) in semen.

RESULTSTotal PA, tPA and uPA highly expressed in normal males, but decreased in the semen of the chronic prostatitis patients of both the fertile and infertile groups. However, there was no significant difference in total PA between the fertile and infertile patients.

CONCLUSIONChronic prostatitis reduces the secretory function and PA synthesis and secretion of the prostate, but the decrease of PA alone does not cause infertility. PA may be one of the tools for estimating the function of the prostate.

Adult ; Case-Control Studies ; Chronic Disease ; Humans ; Infertility, Male ; metabolism ; Male ; Prostatitis ; metabolism ; Semen ; metabolism ; Tissue Plasminogen Activator ; biosynthesis ; Urokinase-Type Plasminogen Activator ; biosynthesis

Objective To compare the serum euron specific enolase(NSE)level before and after treatment in patients with herpes zoster.Methods The serum level of NSE were measured in 100 patients with herpes zoster(observation group)before and after treatment and 100 healthy controls(control group).Results Level of NSE before treatment in observation group was significantly higher than that after treatment and that in control group(P<0.01).There were significant differences in NSE levels between patient with different location,extent and degree of pain(P<0.01).Conclusion Serum NSE level increases significantly in patients with acute herpes zoster,and the NSE level is correlated with the range of skin lesions,the location of the disease and the degree of pain.