Objective:To evaluate the bioequivalence of two kinds of domestic nimesulide granules in healthy volunteers. Meth-ods:In self-control and two-way crossover design, 18 healthy male volunteers were divided into two groups randomly. Each subject was given 100 mg test or reference nimesulide granules with single dose. The concentration of nimesulide in plasma was determined by HPLC. The concentration of nimesulide in plasma was calculated and compared statistically to evaluate the bioequivalence between the two kinds of granules by DAS 2. 1 software. Results:The main pharmacokinetic parameters of test and reference preparations were as follows:Cmax was(9. 28 ± 2. 05) and(9. 41 ± 2. 31)μg·ml-1;Tmax was(3. 50 ± 1. 86)and(3. 56 ± 1. 65)h;T1/2 was (3. 43 ± 0. 85) and(3.38 ±0.68)h;AUC0-24 was(77.78 ±18.42)and(81.69 ±23.50)μg·ml·h-1;AUC(0-∞) was (79.07 ±19.21)and(82.92 ± 24. 11)μg·ml·h-1, respectively. The 90% confidential interval of ln(AUC0-24), ln(AUC0-∞) and ln(Cmax) of the test preparation was 90. 7%-107. 9%,90. 6%-111. 2% and 90. 7%-103. 0%, respectively. The relative bioavailability was (96. 7 ± 37. 6)%. Con-clusion:The two nimesulide granules are bioequivalent.

Objective To observe the antibacterial activity of artificial antimicrobial peptides (AMPs) to Blastomyces albicans, E. coli and Staphylococcus aureus in oral infection in vitro. Methods The AMPs were dissolved into PBS or sterilized saliva, then the inhibi-tion of different concentration AMPs to E. coil was evaluated by tube testing. The inhibition effect of different concentration of AMPs to Staph-ylococcus aureus and Blastomyces albicans were evaluated by antibiotic-susceptive test paper. Results When the concentration of AMPs added to broth of E. coli is from 150μmol/L to 300μmol/L , the bacterium count is 0 while the number in control is 6700 ～ 9200cfu/ml. At 100μg/tablet AMPs, the diameter of inhibitor zones of Staphylococcus aureus and Blastomyces albicans are 13mm and 11 mm. At 300μg/ tablet, the diameter are 16 mm and 17mm. AMPs dissolved in PBS and saliva have similar antimicrobial activity. Gonclusions The AMPs is effective to prevent Blastomyces albicans, E. coli and Staphylococcus aurcus in oral infection in vitro.

OBJECTIVEThis research aimed to investigate the expression of osteoprotegerin (OPG) and receptor activator of nuclear factor-κB ligand (RANKL) in mandibular distraction osteogenesis (DO) regulated by parathyroid hormone (PTH) and to explore the mechanism by which PTH promotes DO.

METHODSA rabbit mandibular DO model was established. The rabbits were randomly divided into experimental group and control group. The former were subcutaneously injected with different doses of PTH on alternate days, the latter was injected with normal saline every other day. Serum OPG levels were detected through enzyme-linked immunosorbent assay. The OPG and RANKL expression levels in the DO-induced formation of a new bone tissue were examined through immunohistochemistry staining.

RESULTSThe serum OPG levels gradually increased during distraction. At the end of the stretch, the OPG expression in the experimental group was significantly stronger than that in the control group. As the fixed period was extended, the OPG expression in the new bone gradually decreased, but the RANKL expression increased.

CONCLUSIONIntermittent subcutaneous PTH injection can upregulate the OPG expression and accelerate bone metabolism. Thus, this procedure promotes the early generation of a new bone in the mandible through DO.

Animals ; Enzyme-Linked Immunosorbent Assay ; Mandible ; NF-kappa B ; metabolism ; Osteogenesis, Distraction ; methods ; Osteoprotegerin ; metabolism ; Parathyroid Hormone ; metabolism ; RANK Ligand ; metabolism ; RNA, Messenger ; Rabbits ; Random Allocation

An acute myocardial infarction rat model was established by ligation of the left ventricular coronary artery.Plasma samples of rats were collected and analyzed by ultra performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS) to study the myocardial protection mechanism of compound Danshen dropping pill (CDDP).After principal component analysis (PCA) and partial least squares discriminant analysis (PLS-DA), 22 metabolites were identified as potential biomarker of AMI.Furthermore, CDDP had remarkable effect on AMI rats.p-Tolyl sulfate, hippuric acid, equol 7-O-glucuronide, lysoPC(16∶0), cholic acid, oleamide, palmitic amide and SM(d18∶1/16∶0) were significantly changed in treatment group.The results showed that CDDP had a very good myocardial protection effect on AMI rats, and might influence the pathways of phenylalanine metabolism, glycerophospholipid metabolism, fatty acid metabolism, primary bile acid biosynthesis and Sphingolipid metabolism.

Objective:To study influence of intravenous injection urapidil and nitroglycerin micro pump on blood pressure and heart rate (HR) of hypertension patients undergoing tooth extraction.Methods:116 hypertension patients underwent electrocardiographic monitoring tooth extraction in our hospital from January 2015 to October 2016 were enrolled in this study.According to the random number table method,the patients were divided into observation group and control group with 58 cases,the control group was given nitroglycerin plus pump static point to maintain,the observation group was given intravenous urapidil and pump maintenance,compared the changes of systolic blood pressure (SBP),diastolic blood pressure (DBP) and HR in two groups before operation,at anesthesia,10min after anesthesia,in operation,10 min after operation,and compared the adverse reactions condition of the two groups.Results:The levels of SBP and DBP in two groups in operation and 10 min after operation were significantly lower than that before operation,and the SBP and DBP levels in the observation group in operation were significantly lower than control group,the differences were statistically significant (all P＜0.05).The HR in control group in operation,10 min after operation were significantly higher than before operation,while the observation group were significantly lower control group,the differences were statistically significant (P＜0.05).The total incidence of adverse reactions in the observation group was 6.90％(4/58),which has no significant difference than 10.34％ (6/58) in control group (P＞0.05).Conclusion:Intravenous injection urapidil has little effect on blood pressure and HR in hypertension patients undergoing tooth extraction,and with good safety,which is worthy of promotion.

Objective To investigate the CT performances and causes of misdiagnosis of parovarian cyst,to improve its diagnostic accuracy.Methods CT data of 75 patients with surgically and pathologically confirmed parovarian cyst were analyzed retrospectively. Results Among the 75 patients,there were 79 cysts,in which 48 patients (51 cysts)originated from the epoophoron and 27 patients (28 cysts) from the mesosalpinx.77 were simple serous cysts and 2 serous cystadenomas.38 were located in the right ovarian adnexa,36 in the left ovarian adnexa,3 in the anterosuperior uterus,1 in the rectouterine pouch and 1 in the right iliac fossa.The size of the cysts ranged from 10 mm × 13 mm to 174 mm × 227 mm.75 were single cysts and 4 double cysts,34 presented as ovoid cysts,25 as irregular cysts, 17 as round cysts and 3 as gourd-shaped cysts.All the 79 cysts showed clear boundaries,thin walls,non-mural nodules,cystic fluid with a homogeneous densitywith CT value of 0-31 HU.Enhanced scanning revealed curved “obvious enhancement of the fallopian tube”at the edge of 68 cysts.In addition,the ipsilateral ovary could be detected in 76 cysts.“Holding ball”was found in 1 9 cysts.Conclusion Indication in ipsilateral ovary,curved “obvious enhancement of the fallopian tube”at the edge of cysts and “holding ball”are distinctive CT performances of parovarian cysts.CT has an important diagnostic value in parovarian cyst.

Ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF/MS) was developed to identify the absorbed parent components and metabolites in rat bile, plasma and urine after oral administration of Radix Paeoniae Alba extract (RPAE). A total of 65 compounds were detected in rat bile, plasma and urine samples, including 11 parent compounds and 54 metabolites. The results indicated that glucuronidation, hydroxylation and methylation were the major metabolic pathways of the components of RPAE. Furthermore, the results of this work demonstrated that UPLC-Q-TOF/MS combined with MetaboLynx? software and mass defect filtering (MDF) could provide unique high throughput capabilities for drug metabolism study, with excellent MS mass accuracy and enhanced MSE data acquisition. With the MSE technique, both precursor and fragment mass spectra can be simultaneously acquired by alternating between high and low collision energy during a single chromatographic run.

To ensure the safety of the commercially available chenpi, a convenient and fast analytical method was developed for the determination of 133 pesticide residues in chenpi using gas chromatography-tandem mass spectrometry (GC-MS/MS). In this study, different extraction solvents, redissolution solvents and adsorbents were tested according to the recovery and purification effect to obtain a modified QuEChERS method. The samples were extracted with acetonitrile. During the clean-up step, octadecyl-modified silica (C18) and graphitized carbon black (GCB) were selected, and aminopropyl (NH2) was used instead of primary secondary amine (PSA) because of its weaker ion exchange capacity which had little effect on the recovery of ditalimfos. Samples were quantified by matrix-matched calibration with internal stan-dards. All pesticides showed good linearity in the respective range, both with values of r2 >0.99. The average recoveries of the pesticides spiked samples ranged from 70.0％ to 112.2％ with the RSDs of 0.2％–14.4％. The modified QuEChERS method was validated and applied to twenty real samples. Five pesticides were found in eight batches, but no pesticide exceeded the maximum residue limits (MRL, MRL reference to European commission).

AIM:To investigate the effect of signal transducer and activator of transcription 1 ( STAT 1 ) on proliferation and interferon-β(IFN-β) sensitivity of human non-small-cell lung cancer H1299 cells.METHODS:STAT1 or EGFP gene was transfected into H1299 cells by the lentiviral vectors system.The cell number was counted under a mi-croscope and cell proliferation was tested by MTT assay.In addition, the cells transfected with STAT1 and EGFP were trea-ted with IFN-βand cell viability was measured by MTT assay.The protein levels of p-STAT1, ICAM-1 and PCNA were de-tected by Western blot.RESULTS: Over-expression of STAT1 inhibited H1299 cell proliferation (P<0.05).H1299 cells transfected with STAT1 gene had a higher sensitivity to IFN-βthan the control cells transfected with EGFP ( P <0.05).Overexpression of STAT1 increased the protein level of p-STAT1, and reduced IACM-1 expression in H1299 cells. Moreover, STAT1 enhanced STAT1 phosphorylation and downregulated the expression of PCNA in H1299 cells treated with IFN-β.CONCLUSION:STAT1 inhibits the proliferation and enhances the IFN-βsensitivity of non-small-cell lung cancer H1299 cells.

Aim To investigate and compare the phar-macokinetics of doxapram injection in healthy subjects of different Chinese nationalities including Han, Mon-golian, Korean, Hui and Uigur, and the influence of gender,in order to provide instruction and help for the usage of doxapram for both clinic and remedy of battle wound. Methods An HPLC-UV method was used to determine the plasma concentration of doxapram. Fifty healthy subjects ( five males and five females of each nationality) were recruited for the study. A single dose of 50 mg doxapram was administered intravenously to the healthy subjects, and blood samples were collected at various predetermined time points. The pharmacoki-netic parameters were calculated by DAS software and were compared by SPSS 13. 0 software, in order to as-sess the influence of nationality or gender on pharmaco-kinetics of doxapram. Results The results indicated that the pharmacokinetic profile of doxapram in vivo could be described as two-compartment model. The main pharmacokinetic parameters for Han, Mongolian, Korean, Hui and Uygur were as follows: Cl ( 0. 25 ± 0. 11 ) , ( 0. 33 ± 0. 11 ) , ( 0. 27 ± 0. 07 ) , ( 0. 26 ± 0. 06) and (0. 39 ± 0. 25) L·h-1 ·kg-1 , while Cmax (1. 55 ± 0. 52 ) , ( 1. 02 ± 0. 30 ) , ( 1. 31 ± 0. 47 ) , (1. 48 ± 0. 46 ) and ( 0. 99 ± 0. 35 ) mg · L-1 . The AUC0-12. 5 , AUC0-∞ and Cmax of Chinese Han were sig-nificantly higher than those of Uigur and Mongolian ( P<0. 05 ) , while there was no significant difference in other parameters ( P>0. 05 ) . There were statistically significant differences in Vc , Vd and CL between young males and females ( P < 0. 05 ) . Conclusion The large inter-individual variation in the main pharmacoki-netics suggests the dosage of doxapram should be ad-justed for different nationalities for both clinic and rem-edy of battle wound.