Physical properties and compact analysis of commonly used direct compression binders

This study investigated the basic physico-chemical property and binding functionality of commonly used commercial direct compression binders/fillers. The compressibility of these materials was also analyzed using compression parameters derived from the Heckel, Kawakita, and Cooper-Eaton equations. Five classes of excipients were evaluated, including microcrystalline cellulose (MCC), starch, lactose, dicalcium phosphate (DCP), and sugar. In general, the starch category exhibited the highest moisture content followed by MCC, DCP, lactose, and finally sugars; DCP displayed the highest density, followed by sugar, lactose, starch, and MCC; the material particle size is highly processing dependent. The data also demonstrated that MCC had moderate flowability, excellent compressibility, and extremely good compact hardness; with some exceptions, starch, lactose, and sugar generally exhibited moderate flowability, compressibility, and hardness; DCP had excellent flowability, but poor compressibility and hardness. This research additionally confirmed the binding mechanism that had been well documented: MCC performs as binder because of its plastic deformation under pressure; fragmentation is the predominant mechanism in the case of lactose and DCP; starch and sugar perform by both mechanism.     

Compressional Behavior of a Mixture of Granules Containing High Load of Phyllanthus niruri Spray-Dried Extract and Granules of Adjuvants: Comparison between Eccentric and Rotary Tablet Machines

The purpose of this paper was to evaluate the compressional behavior of granules containing high load of a Phyllanthus niruri spray-dried extract in eccentric (ETM) and rotary (RTM) tablet presses. Tablets were constituted by spray-dried extract granules (SDEG, 92%), excipient granules (EXCG, 7.92%), and magnesium stearate (0.08%). SDEG was obtained by dry granulation and EXCG, composed of microcrystalline cellulose (62.9%) and sodium starch glycolate (37.1%), by wet granulation. Particle size distribution was fixed between 0.250 and 0.850 mm. Tablets did not evidence any mechanical failures, such as lamination or capping, or anomalous weight variation in either tablet machine types. Upper and lower tablet surface photomicrographs from ETM and RTM tablets showed differences in porosity and texture. Different RTM speeds suggested the visco-plastic behavior of the formulation, since, by slowing down rotation speeds, the tensile strength of the tablets increased significantly, but the porosity and disintegration time were not affected. Tablets produced in RTM showed lower friability and porosity than ETM tablets, which did not reflect on higher tensile strength. The EXCG distribution at upper and lower surfaces from ETM and RTM tablets was quantified by image analysis and evaluated through statistical methods. Spray-dried extract release was not influenced by the type of equipment or operational conditions to which the compacts were submitted. Construction and operation differences between both tablet presses influenced the final product, since tablets with similar tensile strength, made by distinct tablet machines, exhibited different quality parameters.     

Effect of Different Excipients on the Physical Characteristics of Granules and Tablets with Carbamazepine Prepared with Polyethylene Glycol 6000 by Fluidized Hot-Melt Granulation (FHMG)

The objective of this study was to investigate the properties of granules and tablets with carbamazepine which were prepared employing a fluidized hot-melt granulation (FHMG) technique. The FHMG process was carried out at 65°C. Macrogol 6000 (PEG 6000) was used as a binder at the content 10% (w/w) of the granulated mass. Granules containing up to 70% (w/w) of the drug and 20–90% (w/w) of a filler (lactose, mannitol, calcium hydrogen phosphate (Di-Cafos), pregelatinized starch, and microcrystalline cellulose (MCC)) were produced. When the drug content was 30% (w/w), the yield of the process was satisfying (>95%) and flowability of the granules was better than placebo granules or drug-loaded granules prepared by wet granulation. Type of a filler had strong impact on physical properties of granules, and size distribution of the particles was the most homogenous when lactose or Di-Cafos were used. The FHMG technique enabled preparation of granules with better compressability compared with the wet-granulated product or with non-granulated powders. Tablets with shorter disintegration time than 10 min were obtained with 2.0% crospovidone added as a disintegrant. In comparison to tablets prepared from the wet-granulated mass, employment of the FHMG method resulted in tablets with faster dissolution of carbamazepine (more than 80% of the drug released within 15 min). This was achieved with mannitol or lactose/MCC, as fillers.     

Comparison of porcine brain mechanical properties to potential tissue simulant materials in quasi-static and sinusoidal compression

In both finite element and physical surrogate models of head blast injury, accurate material properties of the brain and/or tissue simulants are necessary to ensure biofidelity in predicted response. Thus, there is a need for experimental comparisons between tissue and simulant materials under the same experimental conditions. This study compares the response of porcine brain tissue and a variety of brain tissue simulants in quasi-static and sinusoidal compression tests. Fresh porcine brain tissue was obtained from a local abattoir and tested within 4 h post mortem. Additionally, the effect of post mortem time was investigated by comparing samples stored at room temperature and stored frozen (−18 °C), at various time intervals. The brain tissue simulants tested were bovine gelatin (3%, 5%, and 10% concentration), agarose gelatin (e0.4%, 0.6%, 0.8% concentration), and Sylgard 527. The experiments were performed using a DMA apparatus (TA Instruments Q800). The quasi-static compression data were fit to Ogden hyperelastic functions so that parameters could be compared. It was found that bovine gelatin at 3% and 5% concentration demonstrated the closest response to brain tissue in quasi-static compression. Conversely, in sinusoidal compression, the agarose gel and Sylgard 527 were found to be in closer agreement with the tissue, than bovine gel. In terms of post mortem time and storage, there was no statistically significant difference detected in the response of tissue samples after 48 h, regardless of storage method. However, samples stored at room temperature after 48 h appeared to demonstrate a reduction in stiffness.     

曼月乐与妇康片治疗单纯性子宫内膜增生的临床疗效比较

目的:比较曼月乐与妇康片治疗单纯性子宫内膜增生(simple endometrial hyperplasia,SHE)的临床疗效.方法:选择SHE患者102例,在患者知情同意自愿的前提下,分为妇康片组(n=46例)和曼月乐组(n=56例),妇康片组给予妇康片治疗,曼月乐组给予曼月乐治疗,比较两组患者治疗3个月后的临床疗效、PBAC评分、子宫内膜厚度、血红蛋白水平,同时记录并比较两组患者在治疗过程中不良反应的发生情况.结果:治疗3个月后,两组患者显效例数与无效例数比较,差异具有统计学意义(P＜0.05);曼月乐组患者PBAC评分、子宫内膜厚度均显著低于妇康片组,而血红蛋白水平显著高于妇康片组,差异均具有统计学意义(P＜0.05);治疗期间出现肝肾功能异常例数比较,差异具有统计学意义(P＜0.05),曼月乐组均优于妇康片组.结论:曼月乐治疗SHE的疗效较妇康片更好,并能减少不良反应.     

椎体成形术和椎体后凸成形术治疗老年人骨质疏松性压缩性骨折的疗效比较

目的:比较经皮椎体成形术(percutaneous vertebroplasty,PVP)和经皮椎体后凸成形术(percutanous kyphoplasty,PKP)治疗骨质疏松性压缩性骨折(Osteoporotic vertebral compression fracture,OVCF)的疗效。方法:回顾性分析2011年5月到2014年4月我院收治的老年骨质疏松性脊椎压缩性骨折患者共120例124椎,其中PVP术66例70椎,PKP术54例54椎。病椎范围从T6至L5。比较两组病人术前1天、术后第2天椎体恢复高度,后凸角变化;术前1天、术后第2天、末次随访时间疼痛视觉模拟评分(Visual analogue scale,VAS);术前1天、末次随访时间Oswestry功能障碍指数(Oswestry Dability Index,ODI),平均住院日(average length of stay,ALOS)和住院费用。结果:随访3~35个月,平均17.4月,术后椎体高度恢复情况:PVP组vs PKP组组间差异无显著(8.05±0.59 mm vs 7.44±0.53 mm,P=0.440)。两组术后后凸角均变小(PVP组10.33,PKP组9.96,P=0.731),两组间差异无显著性;患者的VAS评分(术前PVP组8.65±0.14,PKP组8.44±0.15,P=0.750;术后PVP组2.91±0.12,PKP组2.85±0.13,P=0.443)两组间差异无显著性;ODI术前、术后两组间比较差异无显著性;平均住院日两组间差异无显著性(P=0.854),平均住院费用差异有显著性(P=0.000),PVP术住院费用显著低于PKP术。结论:两种手术方式临床疗效没有差异,但PVP术住院费用显著低于PKP术,PVP术是基层医院老年人OVCF治疗的合适的治疗方式。     

葡萄糖测定方法的比较研究

比较了传统斐林定糖,葡萄糖氧化酶－过氧化物酶比色法,葡萄糖氧化酶电极自动分析仪法测定葡萄糖。比较测定了的结果显示,三法的平均标准误差（ＳＤ）,变异系数（ＣＶ）均十分接近。通过对此三种方法的回归相关性分析显示：斐林法－酶终点比色法的回归方程为ｙ＝０．９８４３ｘ＋６．３２３９,相关系数Ｒ＾２＝０．９９８９,斐林法－自动分析仪法的回归方程为ｙ＝１．００８８ｘ＋２．０４８３,相关系数Ｒ＾２＝０．９９９１,     

Characterization and Distribution of the Selected Metals in the Scalp Hair of Cancer Patients in Comparison with Normal Donors

Eighteen metals were estimated in the scalp hair samples from cancer patients (n = 111) and normal donors (n = 113). Nitric acid–perchloric acid wet digestion procedure was used for the quantification of the selected metals by flame atomic absorption spectrophotometry. In the scalp hair of cancer patients, highest average levels were found for Ca (861 μg/g), followed by Na (672 μg/g), Zn (411 μg/g), Mg (348 μg/g), Fe (154 μg/g), Sr (129 μg/g), and K (116 μg/g), whereas in comparison, the dominant metals in the scalp hair of normal donors were Ca (568 μg/g), Zn (177 μg/g), Mg (154 μg/g), Fe (110 μg/g), and Na (103 μg/g). The concentrations of Ca, Cd, Co, Cr, Fe, K, Mg, Mn, Na, Ni, Pb, Sb, Sr, and Zn were notably higher in the hair of cancer patients as compared with normal donors, which may lead to a number of physiological disorders. Strong positive correlations were found in Mn–Pb (0.83), Cd–Cr (0.82), Cd–Li (0.57), Fe–Pb (0.56), and Fe–Mn (0.55) in the hair of cancer patients whereas Na–Cd, Li–Cr, Li–Co, Co–Cd, Li–Cd, Na–Co, Na–Li, Ca–Mg and Na–Cr exhibited strong relationships (r > 0.50) in the hair of normal donors. Principal Component Analysis (PCA) of the data revealed seven PCs, both for cancer patients and normal donors, but with significantly different loadings. Cluster Analysis (CA) was also used to support the PCA results. The study evidenced significantly different pattern of metal distribution in the hair of cancer patients in comparison with normal donors. The role of trace metals in carcinogenesis was also discussed.     

An extraordinary new genus of spiders from Western Australia with an expanded hypothesis on the phylogeny of Tetragnathidae (Araneae)

We describe Pinkfloydia Hormiga & Dimitrov gen. nov. , a new genus of tetragnathid spiders from Western Australia and study its phylogenetic placement. The taxon sampling from our previous cladistic studies was expanded, with the inclusion of representatives of additional tetragnathid genera and outgroup taxa. Sequences from six genetic markers, 12S, 16S, 18S, 28S, cytochrome c oxidase subunit 1, and histone 3, along with morphological and behavioural data were used to infer tetragnathid relationships. These data were analysed using parsimony (under both static homology and dynamic optimization) and Bayesian methods. Our results indicate that Pinkfloydia belongs to the ‘Nanometa’ clade. We also propose a revised set of synapomorphies to define this lineage. Based on the new evidence presented here we propose a revised hypothesis for the intrafamilial relationships of Tetragnathidae and show that Mimetidae is most likely the sister group of Tetragnathidae. The single species in this genus so far, Pinkfloydia harveii Dimitrov& Hormiga sp. nov. , is described in detail and its web architecture documented and illustrated. © 2011 The Linnean Society of London, Zoological Journal of the Linnean Society, 2011, 161 , 735–768.     

仙台病毒BB1株基因组cDNA序列测定及比较分析

该研究对仙台病毒BB1分离株的cDNA全序列进行测序,通过RT-PCR法获得的4个相互重叠的质粒克隆覆盖了全长基因组,并将BB1全长序列与其它已知的仙台病毒序列进行比较。BB1株病毒的基因组为15 384个碱基构成,与其它已知仙台病毒基因组的基因排列与组成规律是一致的,未发现插入或缺失突变。与现已公布5个仙台病毒代表株全基因组序列比较发现,BB1株与其它仙台病毒株同源性均有较大差异。遗传进化分析结果显示,BB1株与Z株和Hamamatsu株的同源性仅为87%和91%,不属于这两株代表的进化分支而归属于第三个基因型。     

Comparison of SR-excited X-ray fluorescence analysis with neutron activation analysis for hair and fiber

Human scalp hair and some kinds of vegetable and animal fibers were analyzed by means of the SR excited X-ray fluorescence method (SRXFA) and the neutron activation method (NAA). Human hair samples collected from five males and five females were washed by the IAEA method prior to analysis. In the SRXFA analysis, samples were excited by monochromated X-rays. Fluorescence X-rays were measured by an Si(Li) detector. The elements detected in all hair samples were S, Ca, Cu, Fe, Zn, Br, and Sr. The elements K, Ti, Cr, Mn, Ni, Se, Hg, and Pb were also detected in several samples. After SRXFA analysis these same samples were analyzed by the NAA method. Elements such as Cu, Zn, and Br were detected by both methods, and their relative concentrations show a good agreement of variation between individuals. However, Pb was only detected by SRXFA, and Na, Au, and Sb were only detected by NAA. Therefore, these two methods are complementary to each other for trace element analysis.     

胫骨远端锁定加压钢板与解剖型钢板内固定治疗Pilon骨折的疗效比较

目的:研究胫骨远端锁定加压钢板(LCP)内固定与解剖型钢板内固定术治疗Pilon骨折的临床疗效,为其治疗提供临床依据。方法:选择2010年1月~2014年12月本院收治的Pilon骨折患者共90例,按照随机数字表法随机分为LCP组(采用胫骨远端LCP内固定治疗)和对照组(采用解剖型钢板内固定治疗),比较两组患者手术时间、术中出血量、骨折愈合时间和术后疗效。结果:LCP组患者手术时间、术中出血量和术后愈合时间均小于对照组,差异有统计学意义(P0.05);LCP组患者术后疗效总优良率为89.6%高于对照组的76.2%,差异有统计学意义(P0.05)。结论:胫骨远端LCP内固定治疗Pilon骨折,具有创伤小、手术时间和术后愈合时间短、术中出血量少、术后疗效总优良率高的优点,是治疗Pilon骨折的有效方法     

Effect of Thiolated Polymers to Textural and Mucoadhesive Properties of Vaginal Gel Formulations Prepared with Polycarbophil and Chitosan

The aim of this study was to design and evaluate of mucoadhesive gel formulations for the vaginal application of clomiphene citrate (CLM) for local treatment of human papilloma virus (HPV) infections. Chitosan (CHI) and polycarbophil (PC) were covalently modified using the thioglycolic acid and L-cysteine, respectively. The formation of thiol conjugates of chitosan (CHI-TG) and polycarbophil (PC-CYS) were confirmed by FT-IR analysis and PC-CYS and CHI-TG were found to have 148.42 ± 4.16 and 41.17 ± 2.34 μmol of thiol groups per gram of polymer, respectively. One percent CLM gels were prepared by combination of various concentrations of PC and CHI with thiolated conjugates of these polymers. Hardness, compressibility, elasticity, adhesiveness and cohesiveness of the gels were measured by Texture profile analysis and the vaginal mucoadhesion was investigated by mucoadhesion test. The increasing in the amount of the thiol conjugates was found to enhance the elasticity, cohesiveness, adhesiveness and mucoadhesion of the gel formulations but not their hardness and compressibility when compared to gels prepared using their respective parent formulations. Slower release rate of CLM from gels was achieved when the polymer concentrations were increased in the gel formulations. PC and its thiol conjugate were found to prolong the release of CLM longer than 70 h unlike gel formulations prepared using CHI and its thiol conjugate which were able to release CLM up to 12 h. Stability of CLM was preserved during the 3 month stability analysis under controlled room temperature and accelerated conditions.     

Pattern of MHC class I and immune proteasome expression in Walker 256 tumor during growth and regression in Brattleboro rats with the hereditary defect of arginine-vasopressin synthesis

Dynamics of the expression of MHC class I, immune proteasomes and proteasome regulators 19S, PA28, total proteasome pool and proteasome chymotrypsin-like activity in Walker 256 tumor after implantation into Brattleboro rats with the hereditary defect of arginine-vasopressin synthesis was studied. The tumor growth and regression in Brattleboro rats were accompanied by changes in the proteasome subunit level unlike the tumor growth in WAG rats with normal expression of arginine-vasopressin gene. In the tumor implanted into Brattleboro rats the immune proteasome level was maximal between days 14 and 17, when the tumor underwent regression. Conversely, the expression of proteasome regulators tended to decrease during this period. Immune proteasomes are known to produce antigen epitopes for MHC class I to be presented to CD8+ T lymphocytes. Enhanced expression of immune proteasomes coincided with the recovery of MHC class I expression, suggesting the efficient presentation of tumor antigens in Brattleboro rats.     

Annual TSP and Trace Metal Distribution in the Urban Atmosphere of Islamabad in Comparison with Mega-Cities of the World

The objective of this work was to assess the current concentrations of total suspended particles (TSP) and trace metals in the urban atmosphere of Islamabad, Pakistan, where local industries, transportation, and urbanization are adversely affecting air quality. Air sampling was done using a high-volume sampler and the metals were estimated in TSP by Flame Atomic Absorption Spectrophotometry. An annual mean TSP of 151.9 μ g/m³ was determined for the period May 2003–April 2004, which exceeded the World Health Organization's (WHO's) primary and secondary standards of air quality. The TSP metal concentrations were compared with those reported in literature for other regions of the world and with air quality standards laid down by regulatory agencies. The levels of Na, Fe, Zn, Pb, Mn, Cr, Co, and Cd for the present study were higher than most of the levels reported for other typical industrial and urban areas of the world. The airborne Ni concentrations were higher than the WHO and the U.S. Environmental Protection Agency's standards. Cluster and Principal Component Analyses of the data were used to identify the sources of the metals and establish their mutual correlations in the local atmosphere.     

郴州市高血压患者中药物抵抗型高血压的筛查和城乡比较研究

目的:通过调查郴州市城区和乡村高血压患者用药现状,筛查出药物抵抗型高血压患者,以提高药物抵抗型高血压患者的治疗率和控制率,为高血压患者个体化降压治疗方案和健康教育方案的制定提供依据。方法:随机选择郴州市区及乡村地区各200名高血压患者,以问卷的形式进行调查。结果:郴州市区药物抵抗型高血压在高血压患者中所占比例及知晓比例分别为6%、9.5%,乡村地区所占比例及知晓比例分别为7%、4%。结论:郴州市药物抵抗型高血压在高血压患者中所占比例为6.5%,农村药物抵抗型高血压患者知晓比例较低;药物抵抗型高血压患者个体化降压治疗方案有待于改进。     

郴州市高血压患者中药物抵抗型高血压的筛查和城乡比较研究

目的：通过调查郴州市城区和乡村高血压患者用药现状,筛查出药物抵抗型高血压患者,以提高药物抵抗型高血压患者的治疗率和控制率,为高血压患者个体化降压治疗方案和健康教育方案的制定提供依据。方法：随机选择郴州市区及乡村地区各200名高血压患者,以问卷的形式进行调查。结果：郴州市区药物抵抗型高血压在高血压患者中所占比例及知晓比例分别为6%、9.5%,乡村地区所占比例及知晓比例分别为7%、4%。结论：郴州市药物抵抗型高血压在高血压患者中所占比例为6.5%,农村药物抵抗型高血压患者知晓比例较低;药物抵抗型高血压患者个体化降压治疗方案有待于改进。     

几种差异序列分析方法的比较及其研究前景

分离和鉴定不同生物基因的差异序列,有助于功能基因的分离,揭开物种间进化的规律,阐明某些疾病相关基因的作用机理。本文简述了几种近年来常用的筛选差异基因的方法,特别是最新发表的杂交监控差异分析法(HMDA)的原理、适用范围及其特点,重点探讨了HMDA法在真核基因组差异序列筛选中的技术性突破及其研究前景。     

Evaluation of FORS-D Analysis: A Comparison with the Statistically Significant Stem-loop Potential

The stem-loop potential of a nucleic acid segment (expressed as a FONS value), decomposes into base composition-dependent and base order-dependent components. The latter, expressed as a FORS-D value, is derived by subtracting the value of the base composition-dependent component (FORS-M) from the FONS value. FORS-D analysis is the use of FORS-D values to estimate the potential of local base order to contribute to a stem-loop structure, and it has been used to investigate the relationship between stem-loop structure and other selective pressures on genomes. In the present study, we evaluated the reliability of FORS-D analysis by comparing it with statistically significant stem-loop potential, another robust method developed by Le and Maizel for examining stem-loop structure. We found that FORS-M values calculated using 10 randomized sequences are as reliable as those calculated using 100 randomized sequences. The resulting FORS-D values have a similar trend and distribution as statistically significant stem-loop potential, implying that FORS-D analysis is as reliable as the latter in measuring the distribution of base order-dependent stem-loop potential. Since the calculation of the FORS-M values is time consuming, the integrated program Bodslp developed by us will become a convenient tool for large-scale FORS-D analysis. The results also suggest that for some purposes the online program SigStb developed by Le and Maizel may be used as an alternative tool for FORS-D analysis. C. Y. Zhang and J. F. Wei contributed equally to this paper.