In order to improve the supersaturation and maintenance time of drug dispersion in curcumin self-nanoemulsion(CUR-SNEDDS), precipitation inhibitors(PPIs) were introduced to prepare curcumin supersaturated self-emulsion(CUR-SSNEDDS). The composition of CUR-SNEDDS prescriptions was selected through the solubility test, the compatibility of oil phase and surfactant, the investigation of the emulsifying ability of the surfactant and the drawing of the pseudo-ternary phase diagram. Analytic hierarchy process was used in combination with central composite design-response surface method to optimize the prescription. The type and dosage of precipitation inhibitors(PPIs) were selected to maintain the supersaturated concentration and duration of CUR in artificial gastrointestinal fluids. At the same time, polarizing microscope was used to evaluate the crystallization inhibition effect and the quality and in vitro release behavior of CUR-SSNEDDS. The prepared CUR-SSNEDDS prescription was capryol 90-kolliphor RH40-transcutol HP-Soluplus(7.93∶66.71∶25.36∶5), with the drug loading of(65.12±1.25) mg·g~(-1). CUR-SSNEDDS was transparent yellow, and the nanoemulsion droplets were spherical with uniform distribution. The emulsification time was(21.02±0.13) s, the average particle size was(57.03±0.35) nm, the polydispersity index(PDI) was(0.23 ± 0.01), and the Zeta potential was(-18.10±1.30) mV. CUR-SSNEDDS significantly inhibited the generation and growth of crystals after in vitro dilution. The supersaturation could be maintained above 10 within 2 h, and the dissolution rate and degree of CUR in artificial gastrointestinal fluid were significantly increased. Soluplus could effectively maintain the supersaturated state of CUR and enhance CUR dissolution in vitro.
Biological Availability ; Curcumin ; Emulsions ; Nanoparticles ; Particle Size ; Solubility ; Surface-Active Agents

This study aimed to investigate the influence of combinating Huangqi with Fuzi on the pharmacokinetics of six Aconitum alkaloids, i.e. aconitine (AC), hypaconitine (HA), mesaconitine (MA), benzoylaconine (BAC), benzoylhypaconine (BHA) and benzoylmesaconine (BMA). The plasma concentrations of the drugs were determined by LC-MS for dose response and time dependent curves. The pharmacokinetic parameters were calculated by DAS 3.3, and SPSS 12.0 was used to analyze the differences of main pharmacokinetic parameters between the two groups. Comparing with Fuzi group, the AUC_0-t and AUC_0-∞ of six alkaloids in Fuzi-Huangqi group was significantly decreased, the CL_z/Fof six alkaloids except HA was significantly increased; the C_max was decreased and the t_max was prolonged in 3 monoester alkaloids, and the apparent volume of distribution of BMA and MA (V_z/F) increases. These data indicated that Huangqi can inhibit the absorption of aconite alkaloids, induce the distribution of aconite alkaloids to the whole body, and accelerate the elimination of aconite alkaloids. The animal experiment scheme in this study has been approved by the Experimental Animal Ethics Committee of Jiangxi University of Traditional Chinese Medicine.

Objective To estimate the prevalence of overweight and obesity , and their relationship between overweight , obesity and chronic diseases among adults in Pinghu City . Methods A total of 3 106 local registered permanent residents aged above 18 years were selected by multi-stage random sam-pling and questionnaire surveys were conducted .The blood glucose , blood lipid , blood pressure , height and weight of the participants were tested . Results The prevalence rate of overweight was 31 .6%( the standardized rate was 29 .5%) and the prevalence rate of obesity was 8 .1% ( the standardized rate is 7 .8%) in residents aged above 18 years in Pinghu City .The prevalence rate of overweight and obesity was highest among population aged from 50 to 59 years.The prevalence rates of overweight of the population in different ages and with different education backgrounds had significant differences ( P <0.05 ).The prevalence rates of diabetes , hypertension and dyslipidemia among overweight and obese population were higher than those with normal weight ( P <0 .01 ) .BMI was the risk factor of hypertension , diabetes mellitus and dyslipidemia , and the OR value was 1 .508 , 2 .127 and 1 .571 , respectively . Conclusion The prevalence of overweight and obesity in Pinghu City is serious and has close relation with chronic diseases .Prevention and intervention measures are necessary for the overweight and obesity population .

OBJECTIVETo investigate factors related to hemorrhagic transformation and favorable outcomes in wake-up ischemic stroke (WUIS) patients undergoing intravenous thrombolytic therapy.

METHODSClinical data of 600 patients undergoing multimodal image-guided intravenous recombinant tissue plasminogen activator (rt-PA) therapy in Department of Neurology, the Second Affiliated Hospital, Zhejiang University School of Medicine center from May 2009 to May 2015 were retrospectively analyzed. Among 600 patients, 68 were diagnosed as WUIS including 17 cases aged 80 or older. Hemorrhagic transformation within the first 24 h after thrombolysis was assessed according to ECASS II criteria. Favorable outcome was defined as three-month modified Rankin Scale (mRS) 0-3. Univariate and binary logistic regression were used to analyze the risk factors of hemorrhagic transformation and poor clinical outcomes in WUIS patients.

RESULTSUnivariate analysis showed that WUIS patients aged ≥ 80 years had a lower rate in males (41.2% vs 76.5%, P=0.007), smokers (11.8% vs 43.1%, P=0.019) and favorable outcome (52.9% vs 78.4%, P=0.043); and a higher rate of cardiac embolism (64.7% vs 35.3%, P=0.034) compared with those aged <80 years. Binary logistic regression showed that age was not an independent risk factor for favorable outcome (OR=0.524, 95% CI:0.141-1.953, P=0.336) or hemorrhagic transformation (OR=1.039, 95% CI: 0.972-1.111, P=0.262).

CONCLUSIONOlder age is not related to the favorable outcome or hemorrhagic transformation in WUIS patients undergoing multimodal image-guided intravenous thrombolytic therapy.

Administration, Intravenous ; Age Factors ; Aged ; Aged, 80 and over ; Brain Ischemia ; diagnosis ; drug therapy ; Female ; Fibrinolytic Agents ; administration & dosage ; therapeutic use ; Humans ; Male ; Recombinant Proteins ; administration & dosage ; therapeutic use ; Retrospective Studies ; Risk Factors ; Stroke ; diagnosis ; drug therapy ; Thrombolytic Therapy ; Tissue Plasminogen Activator ; administration & dosage ; therapeutic use ; Treatment Outcome

To explore the mechanism of the absorption enhancement of Angelica dahurica extract (Ade), the absorption mechanism of baicalin in the Scutcllaria water extraction as well as the effect of Angelica dahurica extract on absorption of baicalin were investigated. In order to determine the main absorption site, everted intestinal sac model was used to study the effect of Angelica dahurica extract on the absorption of baicalin at duodenum, jejunum, ileum and colon. In situ single pass intestinal perfusion model was performed to study the absorption of various concentrations of baicalin and the effect of Angelica dahurica extract on the absorption of baicalin at the main absorption site. To authenticate the consequence of perfusion by getting the blood from the hepatic portal vein and determine the concentration of the baicalin in the blood. The result showed that baicalin could be absorbed at all of the four intestinal segments with increasing absorption amount per unit as follows: ileum > colon > jejunum > duodenum. The absorption ofbaicalin in the duodenum significantly increased with Angelica dahurica extract, thus, duodenum was chosen to be the studying site. Apparent permeability values (Papp) and absorption rate constant (Ka) of baicalin in the duodenum increased gradually with higher concentrations. When the concentration of baicalin rises to a certain degree, the absorption increase had a saturable process, the absorption of baicalin may be an active transportation. Baicalin may be not a substrate of P-gp as verapamil which had not significantly affected the Papp and Ka of baicalin. The absorption of baicalin in the duodenum significantly increased (P < 0.01) in the two models with Angelica dahurica extract and the concentration of baicalin in the blood from the hepatic portal vein showed that the Angelica dahurica extract can increase the absorption of baicalin.
Angelica ; chemistry ; Animals ; Drug Synergism ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Duodenum ; metabolism ; Flavonoids ; isolation & purification ; pharmacokinetics ; Herb-Drug Interactions ; Intestinal Absorption ; drug effects ; Intestines ; metabolism ; Male ; Perfusion ; Permeability ; Plants, Medicinal ; chemistry ; Portal Vein ; metabolism ; Rats ; Rats, Sprague-Dawley ; Scutellaria ; chemistry ; Verapamil ; pharmacology

OBJECTIVETo investigate the relevant factors of liver histological changes in chronic hepatitis B (CHB) patients with mildly elevated ALT and to explore the clinical values of these factors on anti-viral treatment.

METHODSA total of 152 CHB patients with mildly elevated ALT (less than 2 x ULN) who underwent liver biopsy were included in the study. Correlations between routine laboratory markers, liver histological inflammation grade and fibrosis stage were statistically assessed by Spearman correlation analysis, one-way ANOVA, area under the curve (AUC) of the receiver operating characteristic curves (ROC) and Logistic regression statistical analysis.

RESULTSAll patients in the study showed various hepatic histological damages. Among the 152 patients 50 (32.9%) were found with inflammation grade 1 (G1), 42 (27.6%) with G2, 46 (30.3%) with G3 and 14 (9.2%) with G4. 16 patients (10.5%) were found with fibrosis stage 2 (S2), 25 (16.5%) with S3 and 41 (27.0%) with S4. Routine laboratory markers Alb, BPC and WBC were significantly correlated with hepatic histological inflammation grade and fibrosis stage. Marked liver fibrosis and moderate to severe liver damage were significantly higher in patients aged more than 40 years as compared to those less than 40 years of age (P = 0.002, P = 0.010). The regression equation P = 1/[1+e-(9.36250-1625Alb-0.0234BPC)] was established with sensitivity and specificity of 83.3% and 65.0%, respectively.

CONCLUSION67.8% of CHB patients with mildly elevated ALT have significant injury to the liver tissue. CHB patients aged more than 40 years have a significant increase of marked liver fibrosis and moderate to severe liver damage. The regression equation is valuable to predict whether CHB patients need antiviral therapy or not.

Adolescent ; Adult ; Alanine Transaminase ; metabolism ; Female ; Hepatitis B, Chronic ; enzymology ; metabolism ; pathology ; Humans ; Liver ; pathology ; Liver Cirrhosis ; pathology ; Male ; Middle Aged ; Young Adult