OBJECTIVE:To prepare Venlafaxine hydrochloride sustained-release tablets,and to investigate the characteristics of drug release. METHODS:Using glyceryl behenate as lipidic matrix material and HPMC as hydrophilic matrix material,the kind and dosage of excipients were screened by single factor experiment. Using 4,8,24 h accumulative release rate and the deviation summation of ideal values as index,the viscosity of HPMC,the amounts of HPMC K15M and glyceryl behenate were optimized by orthogonal test. The dissolution curves were fitted by different equations. RESULTS:The optimal formulation was as follows as venlafaxine hydrochloride 8.5 kg,HPMC K15M 15 kg,glyceryl behenate 26 kg,magnesium stearate 0.5 kg. 4,8,24 h accumula-tive release rates of prepared matrix sustained-release tablets were 34.3%,63.9% and 99.2%,respectively. The releases profiles of hydrophilic and lipidic matrix sustained release tablets followed first-order equation in vitro mainly through matrix erosion. CON-CLUSIONS:Venlafaxine hydrochloride hydrophilic and lipidic matrix sustained-release tablets with good sustained-release effect have been prepared successfully.

Objective To investigate the risk factors for bacterial pneumonia and the predictive value of early serum procalcitonin (PCT) level for bacterial pneumonia and sepsis classification in patients with acute stroke. Methods The patients with acute stroke in neurological intensive care unit were enroled retrospectively and divided into either a bacterial pneumonia group or a non-infection group according to whether they had bacterial pneumonia or not. The former was redivided into a non-severe sepsis subgroup and a severe sepsis subgroup according to the sepsis classification. The demographics, baseline clinical data, and PCT level (the bacterial pneumonia group was the PCT level when infection occurred, the non-infection group was the PCT level within 24 h of admission) were compared. Multivariate logistic regression analysis was used to identify the independent risk factors for bacterial pneumonia. Receiver operator characteristic (ROC) curve was used to analyze the predictive value of serum PCT level for bacterial pneumonia and sepsis
classification. Results A total of 164 patients with acute stroke were enroled in the study, including 114 in the bacterial pneumonia group (66 in the non-severe sepsis subgroup and 48 in the severe sepsis subgroup) and 50 in the non-infection group. There were significant differences in age, fasting blood glucose level, Glasgow coma scale (GCS) score, and PCT level between the bacterial pneumonia group and the non-infection group (P < 0. 05 ). Multivariate logistic regression analysis showed that fasting blood glucose level ≥7 mmol/L (odds ratio [ OR] 8. 488, 95% confidence interval [ CI] 2. 739 - 26. 300; P < 0. 01), GCS score ≤8 (OR 11. 361, 95% CI 2. 175 - 59. 352; P < 0. 01), and PCT level ≥0. 050 ng/ml (OR 16. 715, CI 5. 075 - 55. 049; P < 0. 01) were the independent risk factors for bacterial pneumonia. In the bacterial pneumonia group, the PCT level (median; interquartile range) in the severe sepsis subgroup was significantly higher than that in the non-severe sepsis subgroup (0. 835 [ 0. 164 - 1. 715 ] ng/ml vs. 0. 114 [0. 073 - 0. 275 ] ng/ml; Z = 4. 818, P < 0. 01 ). ROC curve analysis showed that PCT ≥0. 070 ng/ml could better predict the occurrence of bacterial pneumonia in patients with acute stroke, with sensitivity of 84. 2% , specificity of 74. 0% and the area under the ROC curve of 0. 865 (CI 0. 806 - 0. 924, P < 0. 01); PCT 0. 669 ng/mlcould better predict the occurrence of severe sepsis in acute stroke patients with bacterial pneumonia, with sensitivity of 56. 3% , specificity of 92. 4% and the area under the ROC curve of 0. 765 (CI 0. 672 - 0. 858; P < 0. 01). Conclusions The early PCT level ≥0. 050 ng/ml was an independent risk factor for occurring bacterial pneumonia in patients with acute stroke, its level had certaln predictive value for bacterial pneumonia and the severity of infection.

Objective To study the effects of different transport protein on the transport of 7,4'-dihydroxyflavone (7,4'-DHF) and its metabolite (7,4'-DHF-S) in Caco-2 cell model.Methods Ultra performance liquid chromatography was employed to determinethe content of 7,4'-DHF and 7,4'-DHF-S incubation buffer,their structures were identified by LC-MS/MS.Bidirectional transport of Caco-2 cells model was used to investigate the influence of ko143 (the inhibitor of BCRP) and MK571 (the inhibitor of MRP2) on the transport of 7,4'-DHF and 7,4'-DHF-S,respectively.Results Metabolic product of 7,4'-DHF in Caco-2 monolayer cell was identified as one monosulfate;PDR of 7,4'-DHF was (1.43 ± 0.11),PDR of ko143 and MK571 on the apparent permeability of 7,4'-DHF was (1.59 ± 0.04) and (1.48 ± 0.07) (P ＞ 0.05);PDR of 7,4'-DHF-S was (1.60 ± 0.06);ko143 could significantly reduce the apparent permeability of 7,4'-DHF-S,and the PDR was (0.23 ±0.03) (P ＜ 0.01);MK571 had no significant effect on the apparent permeability of the 7,4'-DHF-S,and the PDR was (1.51±0.04) (P ＞ 0.05).Conclusion Caco-2 cells can mediate the suffonated reaction of 7,4'-DHF;7,4'-dihydroxyflavone sulfonated combination product may be a substrate for BCRP.

Health promoting lifestyle can help patients with chronic diseases to prevent diseases, maintain their health, and reduce or eliminate dangerous behaviors by changing the incorrect lifestyle of chronic diseases. This article reviews the overview, measuring tool, status quo, influencing factors, and interventions of health promotion lifestyle for patients with chronic diseases, and puts forward the corresponding prospects.

Objective To establish a high-throughput evaluation model for anaphylactic reactions; To screen and identify potential anaphylactogens from TCM monomeric compounds.MethodsCell model of stably expressed MrgX2 was established. Recombinate plasmid pmCherry-C1-MrgX2 was transfected to HEK293 to establish cell line for screening model. MrgX2 agonist and antagonist were used to identify the validation and stability of the cell line. A small library consisting of 180 compounds was profiled by using a cell-based calcium mobilization assay to find novel compounds targeting the MrgX2 receptor. EC50 test, IC50 test, specificity validation and cytotoxicity evaluation were carried out to detect the function of the positive agonist.ResultsThe EC50 of C48/80 to MrgX2 model was 2.7 μg/mL and the IC50 of 2-APB (evoked by 10 μg/mL C48/80) was 46.29 μmol/L. The first generation cell model of MrgX2 was similar to the 20th generation, and the Z factor of MrgX2 cell model was 0.78. In the primary screening for agonist, isoliensinine was identified as a novel agonist targeting receptor MrgX2 with an EC50 of 4.5 μmol/L and IC50 of39.47 μmol/L. Moreover, isoliensinine was validated to activate MrgX2 receptor specifically without cytotoxicity. Conclusion A high-throughput evaluation method for anaphylactic reactions can be established in vitro through calcium mobilization assay. A potential anaphylactogen isoliensinine is identified and validated.

Objective To investigate the metabolic profile of chrysin in SULT1A3 and human small intestine S9.Methods After incubation of chrysin using in vitro SULT1A3 and human small intestine S9 system, high-performance liquid chromatography was utilized to determine the sulfates of chrysin.Mass spectrum(MS) were employed to elucidate the structures of metabolite.Results In the SULT1A3 with PAPS, Km were (3.06 ±1.04) and (0.41±0.06) μM, Vmax were (12.13 ±1.30) and (6.72 ±1.61) nmol/(min· mg), Vmax/Km were 3.96 and 16.39 mL/(min· mg), respectively.In the human small intestine S9 with PAPS, Km were (1.92 ±0.35) and (0.01 ±0.00) μM, Vmax were (0.52 ±0.02) and (0.08 ± 0.02) nmol/(min· mg), Vmax/Km were 0.27 and 8.00 mL/(min· mg).The metabolic behavior of chrysin in SULT1A3 and human small intestine S9 both were followed biphasic kinetics.The sulfation of chrysin in SULT1A3 showed a significant correlation with that in human small intestine S9(R2 =0.985).Conclusion The result indicates that SULT1A3 is the major enzyme to the metabolism of chrysin, human small intestine may be the main metabolic organs of chrysin.

Objective To study the effects of repeated hypoxic exposures (HEs) on glycolysis, mitochondrial oxi-dative phosphorylation and energy charge in mouse brain. Methods Adult BALB/c mice were repeatedly exposed to hypoxia for 5 times and the standard tolerant time and body temperature were recorded. The activities of PFK, PK and mitochondrial complex Ⅰ in the brain were assayed. Phosphoadenosines and energy charge were measured. Results Repeated HEs prolonged the hypoxic tolerance and reduced the body temperature. The activities of PFK and PK experienced regular changes, with an increase in 1st and 3rd HEs and a decline to control levels in 5th HE. The complex Ⅰ activity continued to decrease during HEs. The energy charge was stable. Conclusion HEs lead to a regular change of glycolysis, a continued inhibition of mitochondrial oxidative phosphorylation, and a main-tained energy charge in the brains of mouse.

Objective To probe the feasibility of susceptibility weighted imaging (SWI) for evaluation of renal blood oxygenation level of healthy volunteers after water loading.Methods SWI of 11 healthy volunteers,acquired before (group 1) and after water loading (group 2),were assessed retrospectively by two radiologists with more than 10 years abdominal work experience independently.In those images of the same section plane derived from two groups,the phase values in cortex ((φ)cor) and medulla ((φ)med),difference between the same vein and surrounding tissue on phase map (△(φ)) were measured using SPIN software package,and the oxygen extraction fraction changes (△OEF) was calculated.The (φ)cor,(φ)med and △(φ) between two groups were compared by paired t test.And the intraclass correlation coefficient (ICC)was used to evaluate the consistency between two radiologists.Results For the radiologist 1,the (φ)cor,(φ)med and △(φ) were (0.046 ±0.019),(-0.014 ±0.003) and (1.3 ±0.4) rad in group 1,and were (0.047 ±0.014),(-0.012 ±0.005) and (1.1 ±0.4) rad in group 2 respectively,and no significant change was found in (φ)cor and (φ)med after water loading (t =-0.589 and-0.206,P ＞ 0.05 in all),except of in △(φ) (t =2.400,P ＜ 0.01).For the radiologist 2,the (φ)cor,(φ)med and △△(φ) were (0.049 ± 0.011),(-0.012 ± 0.004)and (1.5 ±0.4) rad in Group 1,and were (0.046 ±0.017),(-0.011 ±0.003) and (1.3 ±0.2) rad in group 2 respectively,there was no significant change in (φ)cor and (φ)med after water loading (t =0.590 and -0.974,P ＞ 0.05 in all),except of in △(φ) (t =2.760,P ＜ 0.05).Between two radiologists,the ICC of (φ)cor,(φ)med and △(φ) were 0.623,0.472 and 0.328 in group 1 and 0.599,0.442 and 0.445 in group 2 respectively.△OEF decreased about (-4.2 ± 2.3) c％ and (-4.3 ± 2.8) c％ measured by two radiologists respectively,and the consistency is good between two radiologists (ICC =0.784).Conclusion SWI provides a novel method to assess indirectly the oxygenation level of kidney,△OEF is an indicator with suitable reliability.

Objective To explore the influence of social support and coping style on body and mind symptoms of patients with laryngeal carcinoma. Methods SCL-90, SSRS and MCMQ were used for the questionnaire survey of 168 patients with laryngeal carcinoma. Results The result of SCL-90 showed that all items were higher than those of norm in China, except the interpersonal relationship sensitivity and psychotic symptoms. The result of SSRS showed that the total score of social support was higher than that of norm, while the availability of support was obviously lower than that of norm. The result of MCMQ showed that avoidance and submissiveness were used frequently in patients, and avoidance was negatively correlat-ed with the factors of psychology. Conclusions Before the nursing plan and health consultation are set for patients with laryngeal carcinoma, the patients' social support should be used sufficiently, and the effect of coping style on patients' mental health should be evaluated.

Objective:To investigate the proliferation of rat glomerular mesangial cells (GMC) influenced by different ethanol extracts of Tripterygium wilfordii HooK F.(TWHF).Methods:An HPLC method was used to establish the fingerprints of 5 different ethanol extracts of TWHF,and GMC was chosen to study the effects of different ethanol extracts of TWHF on cell proliferation.After statistical analysis,the spectrum-activity relationship was analyzed by using partial least squares regression(PLSR).Results:The HPLC fingerprints of the 5 different ethanol extracts of TWHF were established,and 32 characteristic peaks were characterized by the HPLC fingerprints.60%,70% and 95% ethanol extracts and glycosides tablets showed dose-effect relationship,and with the increase of dose,the more significant inhibition of cell proliferation was exhibited.The absorbance values of the 60% ethanol extracts at medium and high doses were lower than those of the other extracts at the same dose.The proliferation inhibition rate of GMC was used as the potency index and analyzed by PLSR,and 20 peaks were potency peaks at high dose(40 μg·L-1),17 ones were potency peaks at medium dose(20 μg·L-1) and 15 ones were potency peaks at low dose(10 μg·L-1).Conclusion:Part of the potency peaks has regular dose-effect relationship with the changes of dose.