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The effective components of flavonoids in the "Pueraria lobata-Hovenia dulcis" drug pair have low bioavailability in vivo due to their unstable characteristics. This study used microemulsions with amphoteric carrier properties to solve this problem. The study drew pseudo-ternary phase diagrams through titration compatibility experiments of the oil phase with emulsifiers and co-emulsifiers and screened the prescription composition of blank microemulsions. The study used average particle size and PDI as evaluation indicators, and the central composite design-response surface method(CCD-RSM) was used to optimize the prescription; high-dosage drug-loaded microemulsions were obtained, and their physicochemical properties, appearance, and stability were evaluated. The results showed that when ethyl butyrate was used as the oil phase, polysorbate 80(tween 80) as the surfactant, and anhydrous ethanol as the cosurfactant, the maximum microemulsion area was obtained. When the difference in results was small, K_(m )of 1∶4 was chosen to ensure the safety of the prescription. The prescription composition optimized by the CCD-RSM was ethyl butyrate(16.28%), tween 80(9.59%), and anhydrous ethanol(38.34%). When the dosage reached 3% of the system mass, the total flavonoid microemulsion prepared had a clear and transparent appearance, with average particle size, PDI, and potential of(74.25±1.58)nm, 0.277±0.043, and(-0.08±0.07) mV, respectively. The microemulsion was spherical and evenly distributed under transmission electron microscopy. The centrifugal stability and temperature stability were good, and there was no layering or demulsification phenomenon, which significantly improved the in vitro dissolution of total flavonoids.
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Polissorbatos/química , Flavonoides , Pueraria , Tensoativos/química , Etanol , Emulsões , Tamanho da Partícula , SolubilidadeRESUMO
ObjectiveTo explore the optimal formula of Maxing Shigantang in regulating epidermal growth factor receptor（EGFR）expression and alleviating airway injury in asthmatic rats and to reveal the underlying mechanism. MethodSD male rats were randomly divided into normal group, model group, dexamethasone group (5×10-4 g·kg-1) and Maxing Shigantang 1∶0.5, 1∶1, 1∶2 groups (group A, B, C, 10 g·kg-1), with 8 rats in each group. The other groups except the normal group received nebulization of 2% acetylcholine chloride and 0.4% histamine phosphate for the modeling of asthma. One hour before modeling， the normal group and the model group were given the same amount of normal saline， and the other groups were given the same amount of corresponding drugs， once a day for 7 days. On the 7th day， the model was established and the incubation period of asthma was recorded. The rats were then immediately anesthetized， and arterial blood and tracheal tissue were collected. Enzyme-linked immunosorbent assay （ELISA） was employed to detect the levels of interleukin-2 （IL-2）， interleukin-4 （IL-4）， and tumor necrosis factor-α （TNF-α） in serum. Pathological sections were prepared for the observation of the pathological changes of tracheal tissues and the ultrastructure of epithelial cells in each group. Terminal-deoxynucleotidyl transferase-mediated nick-end labeling （TUNEL） was adopted to detect epithelial cell apoptosis， and in situ hybridization and Western blot were employed to determine the mRNA and protein levels of epidermal growth factor receptor （EGFR）， respectively. ResultCompared with the model group， groups A， B and C prolonged the incubation period of asthma （P<0.05，P<0.01）. Compared with the control group， the model group showed declined IL-2 level （P<0.01）， risen IL-4 and TNF-α levels （P<0.05，P<0.01）， increased airway pathology score， collagen volume fraction， and airway epithelial cell apoptosis index （P<0.01）， and up-regulated mRNA and protein levels of EGFR in trachea tissue （P<0.01）. Compared with the model group， group A showed increased IL-2 level （P<0.05） and declined IL-4 （P<0.05，P<0.01） level， and group B showed declined IL-4 level （P<0.05）. The level of TNF-α in groups A， B， and C declined compared with that in the model group （P<0.01）. Maxing Shigantang repaired the tracheal tissue to different degrees （P<0.05）. Among the three groups， group A inhibited tracheal fibrosis （P<0.05） and had the most significant effect of repairing the ultrastructural changes of airway epithelial cells. Groups A， B and C all inhibited the apoptosis of airway epithelial cells （P<0.05）. All the three groups inhibited the up-regulation of EGFR mRNA level （P<0.05，P<0.01）， and groups B and C inhibited the up-regulation of EGFR protein level （P<0.05，P<0.01）. ConclusionMaxing Shigantang can inhibit the abnormal changes of airway epithelial structure， alleviate airway injury， and can down-regulate the expression of EGFR in the tracheal tissue of asthma model rats. In this study， the optimal compatibility of Maxing Shigantang to repair airway epithelial injury in asthmatic rats was group A， with the Ephedrae Herba-Armeniacae Semen Amarum-Glycyrrhizae Radix et Rhizoma-Gypsum Fibrosum ratio of 1∶0.5∶4∶1.
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Objective:To characterize the trends in the incidence and mortality of colorectal cancer in Jing'an District of Shanghai， thus optimizing the prophylactic options for this malignancy. Methods:Data from Shanghai Cancer Registration and Reporting System were used to analyze the colorectal cancer prevalence in Jing'an District from 1993 to 2017. Joinpoint software was used to analyze the trends in the standardized incidence rate and mortality rate by calculating the annual percentage of change （APC） and the average annual percentage of change （AAPC）. Results:A total of 13 580 new cases of colorectal cancer were reported in Jing'an District during 1993 and 2017， with an average crude incidence rate of 52.94/105 and a standardized incidence rate of 24.77/105. The total number of deaths was 7 572， with an average crude mortality rate of 29.52/105 and a standardized mortality rate of 12.20/105. The standardized incidence rate of colorectal cancer in Jing'an District from 1993 to 2017 showed an increasing trend （AAPC=1.64%，P<0.001）， and the standardized incidence rate of colorectal cancer in both sexes increased （AAPC： 2.10% in men， 1.04% in women）. The age-standardized mortality rate （ASMR） did not change significantly. The incidence rate of colorectal cancer increased in men in both age groups of 50 to 74 years and 75 years and older， with an AAPC of 2.07% and 3.32%， respectively. However， this was not evident in women of all age groups. The mortality rate of colorectal cancer in men aged 0-49 years， as well as in men and women at 50-74 age groups， decreased significantly， with an AAPC of -7.46%，-1.13%， and -2.72%， respectively. The mortality rate of colorectal cancer in men of 75 years or older showed no significant trend， while that in women of 75 years or older increased （AAPC=2.30%）. Conclusion:The overall standardized incidence rate of colorectal cancer in Jing'an District from 1993 to 2017 was increased， and ASMR did not change significantly. Public health prophylactic options are suggested， including improvement of lifestyle/physical activity and eradication of precancerous lesion polypus in males aged ≥50 years to reduce the incidence of colorectal cancer， and enforcement of second-grade prophylaxis in females aged ≥75 years to decrease the mortality of colorectal cancer.
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Objective To explore and analyse the prevalence of thyroid cancer among population of Jing′an District, Shanghai, providing a scientific basis for prevention and intervention. Methods Analysis was made on the prevalence of thyroid cancer in Jing′an District in 2014 and its incidence and death trend from 2009 to 2014 based on the data of Shanghai Cancer Registration and Reporting System. Results From 2005 to 2014, the total number of thyroid cancer cases in Jing′an District were 2 430, ranking fourth of all malignant tumors.The crude incidence rate of thyroid cancer was 24.33/100 000, the standardized incidence rate was 16.67/100 000.The ratio of male to female was 0.34 : 1;the difference in incidence between male and female was significant(χ2=579.77, P < 0.01).In different age groups the difference in incidence was also statistically significant(χ2=419.90, P < 0.01).The highest incidence was in 45-64 years old group, followed by 15-44 years old group. Only 155 deaths occurred; the ratio of death to morbidity was 1 : 15.68.Standardized incidence of thyroid cancer was increasing in Jing′an District from 2005 to 2014(trend Chi-square tests, χ2=7.33, P < 0.01).APC was 20.69%(male 23.81%, female 19.44%).The standardized mortality rate from 2005 to 2014 was at a relatively low level, and the trend of change was not statistically significant. Conclusion The government and society should pay high attention to the status of high detection rate and low mortality rate of thyroid cancer.The focus of prevention and control is rational diagnosis and treatment for a large number of thyroid cancer patients.
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Objective: To investigate transport mechanism of cyperotundone in Caco-2 cell model and provide experimental basis for clinical application of Cyperi Rhizoma. Method: The toxicity of cyperotundone with different concentrations to Caco-2 cells was investigated by methyl thiazolyl tetrazolium (MTT) colorimetry, in order to determine the concentration of administration in transport test. The content of cyperotundone was determined by liquid chromatography-mass spectrometry (LC-MS) with apparent permeability coefficient (Papp) and cumulative transport capacity as indexes. The chromatographic conditions were as following:mobile phase of acetonitrile (A)-water (B) for gradient elution (0-1.5 min, 35%A; 1.5-2 min, 35%-90%A; 2-4 min, 90%A; 4-4.1, 90%-35%A; 4.1-8 min, 35%A), the flow rate at 0.3 mL · min-1, injection volume of 1 μL, and temperature of column at 30℃. The mass spectrometric conditions was electrospray ionization (ESI) and positive ion mode, the detection ions of cyperotundone and osthole (internal standard substance) were m/z 219.2-110.9 and m/z 245.0-189.0, respectively. Effect of concentration of cyperotundone, administration time, ethylenediamine tetraacetic acid (EDTA) and P-glycoprotein (P-gp) inhibitor on the transmembrane transport of cyperotundone on in vitro cell model were investigated. Result: Cyperotundone didn't have significant toxicity to Caco-2 cells at 3-90 mg · L-1 after incubation for 4 h. The transportion of cyperotundone in Caco-2 cell model was related to the concentration and time to a certain extent, its Papp was higher than 1×10-6 cm · s-1, which indicated that absorption of cyperotundone was good, the efflux rate (ER) of cyperotundone was 0.5-1.5.There was no significant difference in bidirectional Papp of cyperotundone after the addition of cell bypass transport inhibitor (EDTA) and P-gp transport inhibitor (verapamil). Conclusion: The transport mechanism of cyperotundone in Caco-2 cell model is mainly passive diffusion, and cell bypass transport and P-gp are not involved in its transport.
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This article introduces the development of Common Terminology Criteria Adverse Events (CTCAE), and compares the characteristics of Common Terminology Criteria Adverse Events Version 3.0 (CTCAE v3.0) with CTCAE v4.0. The essential features of CTCAE v4.0 are reviewed, and the trends and prospects of CTCAE v4.0 in evaluation of adverse events in cancer treatment are analyzed. Copyright © 2012 by TUMOR.
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<p><b>OBJECTIVE</b>To improve the clinician's ability for emergency treatment of priapism.</p><p><b>METHODS</b>Both cases received 2 mg to 8 mg of metaraminol injection at the root of cavernous body, and perfusion of heparinized saline at glans and root of cavernous body of the penis by contrecoup, but they had not good response to the above therapy. At last surgery was performed.</p><p><b>RESULTS</b>Total penectomy was performed for both cases. One case was diagnosed of penile sarcoma, and another was metastatic transitional cell carcinoma.</p><p><b>CONCLUSION</b>Priapism due to neoplasma is infrequent, it should not be misdiagnosed in case of emergency.</p>