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 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 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 analyze mutations in the ATP2A2 gene in a Kazakh family with Darier's disease.Methods Clinical data were collected from 49 members from a family with Darier's disease,and peripheral blood samples were obtained from 44 family members and 100 unrelated healthy people.Genomic DNA was extracted from these blood samples.PCR and DNA sequencing were performed to detect mutations in the ATP2A2 gene.Results Darier's disease was inherited in an autosomal dominant manner in this family.A G→A heterozygous mutation (1288-1G→A) was identified at position 1288-1 at the splice site in exon 12 of the ATP2A2 gene in 11 patients in this family,but not in 33 healthy members or 100 healthy controls.Conclusion Darier's disease in this family may be caused by the heterozygous mutation (1288-1G→A)at the splice site in exon 12 of the ATP2A2 gene.

Objective To investigate the kinectics characteristics of sulfation of apigenin mediated by SULTIA3.Methods After incubation of apigenin using in vitro SULT1A3 system, high-performance liquid chromatography was utilized to determine the sulfates of apigenin.Mass spectrum(MS) were employed to elucidate the structure of metabolite.The program GraphPad Prism 5 was used to perform the kinetic characterization of SULT1A3 catalyzed metabolism of apigenin.Results A liner calibration curve for the assay of apigenin was validated in the range of 0.15625 ~30 μM with the recoveries of at least 80% and intra-day and inter-day RSD of less than 15%.Metabolic product of apigenin and SULT1A3 in the incubated system was identified one monosulfate.The metabolic behavior of apigenin in SULT1A3 was followed substrate inhibition kinetics.Apparent kinetic parameters of metabolism of apigenin by SULT1A3, Kmwas(0.355 ±1.04) μM and Ksi was(23.62 ±0.06) μM,Vmax was(65.71 ±1.30) nmol/(min? mg),Vmax/Km was 185.10 mL/(min? mg).Conclusion SULT1A3 can mediate the binding of apigenin sulfonated reaction, and the character of enzymatic kinetics shows substrate inhibition.Sulfation of apigenin mediated by SULTIA3 may play an important role in phaseⅡmetabolic in vivo.

Aim To investigate the effect of astragalo-side IV ( ASIV) on myocardial energy metabolism and mitochondrial biosynthesis in myocardial cells of dia-betic rats induced by streptozotocin ( STZ ) . Methods
50 SD rats at 6 weeks of age were assigned to 5 groups,10 for each group:control group, model group, ASIV 10 mg·kg-1 ·d-1 group, ASIV 20 mg·kg-1 ·d-1 group, ASIV 40 mg·kg-1 ·d-1 group. Except the control group,the remaining 40 were used to estab-lish type 1 diabetes model by the tail vein injection of STZ (35 mg·kg-1 ) . At the end of 16 weeks of treat-ment, left ventricular systolic pressure ( LVSP ) , left ventricular diastolic final pressure ( LVEDP ) and left ventricular maximum rising/falling rate ( ± dp/dtmax ) were tested. Pathological section was observed by HE staining. ATP, ADP, AMP levels were detected by ELISA. The expressions of PGC-1α and NRF-1 protein were assessed by Western blot. The expressions of PGC-1α and NRF-1 mRNA were determined by RT-PCR. Results Compared with control group, model group markedly elevated LVEDP and decreased LVSP, ± dp/dtmax , ATP/AMP and ATP/ADP ratio. Com-pared with model group, low-dose ASIV group did not change significantly,middle-dose ASIV group and high-dose ASIV group obviously decreased LVEDP, and im-proved LVSP, ± dp/dtmax , ATP/ADP and ATP/AMP ratio. Meanwhile, the expressions of PGC-1α and NRF-1 protein and mRNA were increased in a dose-de-pendent manner. Conclusion ASIV could promote mitochondrial biosynthesis, improve energy metabolism in myocardial cells of type 1 diabetic rats by PGC-1αand NRF-1 .

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.