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 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.

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.

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 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.

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 increase the awareness of autoimmune pancreatitis (AIP) and correct diagnosis rate of AIP by investigating radiologic characteristic of AIP and small pancreatic cancers.Methods The clinical data and radiologic imaging of 24 AIP patients who met the Asia diagnostic criteria of AIP in 2008 and 25 cases of pathologically condirmed small pancreatic cancer were retrospectively reviewed.All imaging findings were reviewed,especially on the shape,enhancement patterns of mass,pancreatic ducts,peripancreatic and extra-pancreatic manifestations. Chi-square test and Fisher test were used for statistical analysis.ResultsThe imaging signs,including location of masses,distal pancreatic atrophy,enhancing mass during portal phase,truncated duct sign of pancreatic duct,capsule-like rim and renal involvement,was significantly different between AIP and small pancreatic cancer ( x2 =9.010,10.506,15.488,8.688,6.292 and 4.966 respectively,P ＜0.05 ).But only two signs,distal pancreatic atrophy and enhancing mass during arterial and portal phase,were statistically different between local AIP and small pancreatic cancer (P ＜0.05).ConclusionsThe typical imaging features of diffuse AIP is distinct and helpful for the differential diagnosis of AIP from small pancreatic carcinoma,but there is limited value in the differential diagnosis between local AIP and small pancreatic cancer.

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.

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 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.