壳聚糖-海藻酸钠微胶囊对布洛芬的缓释作用

布洛芬作为非甾体抗炎药中的典型代表,具有较好的解热镇痛抗炎作用。但由于其具有胃肠道刺激性、首关效应等缺陷,使用普通制剂很难达到较为理想的临床效果。将壳聚糖-海藻酸钠微胶囊作为载体对布洛芬进行缓释实验,实验结果显示该类微胶囊对布洛芬具有较好的缓释作用,且包封率达到了9 2%。在本文中,将就壳聚糖-海藻酸钠纳米微胶囊对布洛芬的缓释作用进行阐述。     

布洛芬对绿豆下胚轴插条生根的影响(简报)

人工合的解热镇痛抗炎药布洛芬能显著促进绿豆下胚轴生根,增加根数和根干重。     

布洛芬对肝癌细胞HepG2增殖及wnt／β-catenin信号通路的影响

研究非甾类抗炎药布洛芬对肝癌细胞增殖和β-catenin信号通路的影响,探讨布洛芬影响肝癌细胞增殖的可能机制.体外培养HepG2细胞,MTT法检测不同浓度布洛芬分别作用24、48和96 h后细胞增殖情况;应用RT-PCR检测布洛芬处理HepG2 48 h后β-catenin、cyclin D1和c-myc转录水平的变化;western blotting检测布洛芬对HepG2中β-catenin1蛋白表达量的影响;免疫细胞化学法观察布洛芬处理组HepG2细胞β-catenin的亚细胞定位.结果表明0.7mmol/L的布洛芬处理细胞48 h后能明显见到细胞增殖受到抑制,抑制率达到53.8%,且抑制作用有时间、剂量依赖性:经布洛芬处理后细胞的β-catenin、cychn D1和c-myc转录也受到显著抑制;布洛芬处理组细胞β-catenin蛋白表达低于对照组;布洛芬处理后β-catenin在胞核中定位减少,胞浆定位增多.因此,布洛芬能抑制肝癌细胞的增殖,且随着处理时间和药物浓度的增加,其抑制作用逐渐增强,其抑制作用可能与调控β-catenin信号通路,影响β-catenin的表达和定位,调节下游相关靶基因的转录有关.     

“克洛曲(复方克痛宁)研究”获云南省科学技术二等奖

由中国科学院昆明动物研究所熊郁良、王婉瑜研究员主持的该项研究工作，在国际上首次发明了一种高效、广谱，具有镇痛、戒毒双重作用的新型不成瘾药物——克洛曲。该药以蛇毒神经毒为主，辅以起效快的曲马多、布洛芬，组成一个全面作用于中枢、外周神经传导突触后Ach及植物神经系统的新复方制剂，在药效学、药理学及正交试验方面证明均优于国内外现有镇痛药。它克服了神经毒(克痛宁)起效慢、曲马多仅作用于中枢镇痛和可能产生耐药性或会成瘾、布洛芬仅作用于植物神经解热镇痛的缺点，将三条作用途径组成“克洛曲”，充分发挥了各药品的特点，形成起效快、镇痛时间长、高效、广谱、毒性低的新型镇痛药物；该药还具有戒毒作用，且不成瘾，对患者免疫功能及性功能恢复都有显著效果。该工作为毒素研究和应用开创了一条新途径，有关论文在国际会议多次报道并全文刊登，受到好评。 克洛曲作为镇痛药物已经卫生部新药办公室及医药管理局批准并获生产批文，列入部颁试验标准。2000年已在全国上市，并在云南省及全国部分地区作为戒毒辅助用药推广应用。目前正在进一步补充完善材料，拟报批为戒毒特药。该工作1998年经中国科学院组织专家鉴定，达国际先进水平；2000年获云南省科学技术(科学技术进步类)二等奖。     

枯草芽胞杆菌喷雾剂对家兔皮肤创伤愈合的影响

目的 :观察枯草芽胞杆菌喷雾剂对家兔皮肤创伤愈合的影响。方法 :采用家兔皮肤创伤为模型 ,连续给药 6 d,第 11天测定创面面积 ,并于第 17天记录创面愈合数。结果 :枯草芽胞杆菌喷雾剂高剂量组和磺胺嘧啶银组创面面积显著小于空白对照组 ( P<0 .0 5 ) ;枯草杆菌喷雾剂的愈合率显著高于空白对照组( P<0 .0 5 )。结论 :枯草芽胞杆菌喷雾剂能够缩小家兔创面愈合 ,增加创面愈合率     

耳尖放血配合布洛芬治疗儿童外感发热的疗效观察

目的观察耳尖放血配合布洛芬治疗儿童外感发热的临床疗效。方法将60例符合入选标准的外感发热患儿随机分为治疗组和对照组,每组各30例。治疗组采用耳尖放血配合布洛芬治疗,对照组单用布洛芬治疗,观察治疗后2h退热效果及随访24h复发率。结果耳尖放血配合布洛芬比单用布洛芬在治疗后2h的退热效果更佳（P〈0.05）,24h复发率也更低（P〈0.05）。结论耳尖放血配合布洛芬治疗儿童外感发热,退热效果好,复发率低。     

瑶药风湿骨痛喷雾剂的皮肤过敏性试验研究

目的:对瑶药风湿骨痛喷雾剂进行皮肤过敏性试验,为临床安全用药提供依据。方法:豚鼠30只,雌雄各半,按性别、体重随机分成3组,每组10只,于第0、7、14d左侧脱毛致敏,第28 d右侧激发给药,观察其是否产生过敏作用。结果:空白组和给药组对豚鼠无过敏性反应,阳性组出现过敏反应。结论:瑶药风湿骨痛喷雾剂经皮肤给药是安全的。     

手性高效液相色谱法测定S(+)-布洛芬对映体过量

用手性固定相高效液相色谱法(CSP-HPLC)测定了样品或微生物酶不对称水解反应液中S(+)-布洛芬对映体过量(ee)。该法首先将布洛芬转化为二苯酰胺衍生物,然后在N-3,5-二硝基苯甲酰-?-苯甘氨酸[?-DNB-PG]的共价型CSP柱上进行对映体HPLC分离。流动相选择正已烷-异丙醇(98:2),流速1ml/min,对映体分离度1.47。按相同方法同时进行消旋布洛芬的二苯酰胺衍生物的分离,由其对映体峰高比可测定S(+)-布洛芬ee(%)。测定加量回收率相对标准偏差为3.3%。     

花椒总生物碱镇痛、抗炎、止痒作用研究

目的:研究花椒生物碱镇痛、抗炎及止痒作用。方法:分别采用热板法考察其镇痛作用二甲苯致炎法考察其抗炎作用、低分子右旋糖酐-40诱发小鼠皮肤瘙痒研究其止痒作用。结果:中、高浓度的花椒生物碱对小鼠热刺激引起的疼痛具有较强的镇痛作用;高浓度的花椒生物碱能较强抑制二甲苯所致小鼠耳肿胀,并能缓解分子右旋糖酐-40诱发的小鼠皮肤瘙痒。具有较强的抗炎、止痒作用。结论:花椒生物碱具有较强的镇痛、抗炎、止痒作用。     

《英国医学杂志公开版》:非甾体抗炎药或引发心律不齐

<正>网络期刊《英国医学杂志公开版》(BMJ Open)发表的一项最新报告说,非甾体抗炎药可能会引发老年人心律不齐,进而增加心脏病、中风甚至心衰风险。该报告再次提醒人们此类药物可能引发的副作用。非甾体抗炎药是一类具有抗炎、解热和镇痛作用的药物,主要包括阿司匹林、布洛芬、双氯芬酸等,全世界每天有上千万人在服用此类药物。     

The effect of ibuprofen on the intrauterine pressure and menstrual pain of dysmenorrheic patients.

In 12 dysmenorrheic patients we examined the therapeutic action of the Prostaglandin-synthesis inhibitor: Ibuprofen, a non-steroidal analgesic agent. Ibuprofen highly significantly reduced the resting pressure (P less than 0.001), active pressure (P less than 0.001) and frequency (P less than 0.05) of cyclic activity of the uterus, as well as menstrual pain (P less than 0.001). Since these effects occurred after a single oral dose of 800 mg Ibuprofen, without side effects or complications, extensive field trials are recommended with this and other PG-synthesis inhibitors, to assess their therapeutic benefits.     

The effect of ibuprofen on the intrauterine pressure and menstrual pain of dysmenorrheic patients

In 12 dysmenorrheic patients we examined the therapeutic action of the Prostaglandin-synthesis inhibitor: Ibuprofen, a non-steroidal analgesic agent. Ibuprofen highly significantly reduced the resting pressure (P<0.001), active pressure (P<0.001) and frequency (P<0.05) of cyclic activity of the uterus, as well as menstrual pain (P<0.001). Since these effects occurred after a single oral dose of 800 mg Ibuprofen, without side effects or complications, extensive field trials are recommended with this and other PG-synthesis inhibitors, to assess their therapeutic benefits.     

Beneficial Effects of Ibuprofen on Pentylenetetrazol-induced Convulsion

Neurochemical Research - Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) that is commonly used as an anti-inflammatory, anti-pyretic, and analgesic. Although some studies have focused...     

Characteristics and growth kinetics of biomass of Citrobacter freundii strains PYI-2 and Citrobacter portucalensis strain YPI-2 during the biodegradation of Ibuprofen

International Microbiology - Ibuprofen (IBU) is the third most commonly used analgesic drug in the world. It enters the water system as a result of human excretion-based wastewater discharges....     

Study of coat quality of tablets coated by an on-line supercell coater

The aim of this study was to investigate the nature of Supercell coating, an on-line tablet coater that employed a unique pattern of airflow. Tablets coated at different spray rates (4, 6, 8, 10, and 12 mL/min) were analyzed to investigate the influence of different wetting conditions on the quality of coats formed. Scanning electron micrographs showed that tablet coats formed at a spray rate of 4 mL/min consisted of spray-dried droplets that did not coalesce. At a spray rate of 6 mL/min, surface roughness was found to be lower than at the other spray rates, and the coat appeared smoothest, whereby droplets seemed fused together. At higher spray rates, the droplets appeared as branching arms and scale-like structures. This was attributed to the spread of spray droplets by the processing air and mass transfer of wet coating materials between tablets. Further tests showed that coats formed at higher spray rates had higher drug yield, drug uniformity, color uniformity, and density. However, the variability in coat thickness was increased due to the mass transfer of coats and dissolution of tablet core surfaces by the coating material. Since coats of different characteristics can be formed in Supercell coating, the choice of wetting conditions would depend on the type of coat required and the coating materials used. Published: August 10, 2007     

Influence of Process Parameters on Tablet Bed Microenvironmental Factors During Pan Coating

Recent studies have shown the importance of monitoring microenvironmental conditions (temperature, relative humidity) experienced by the tablet bed during a pan coating process, thereby necessitating the need to understand how various process parameters influence these microenvironmental conditions. The process parameters studied in this work include exhaust air temperature, spray rate, inlet airflow rate, gun-to-bed distance, coating suspension percent solids, and atomization and pattern air pressure. Each of these process parameters was found to have an impact on the tablet bed relative humidity (RH), as measured using PyroButton data logging devices. A higher tablet bed RH was obtained with an increase in spray rate and atomization air pressure and with a decrease in exhaust air temperature, inlet airflow rate, gun-to-bed distance, suspension percent solids, and pattern air pressure. Based on this work, it can be concluded that the tablet bed thermodynamic conditions are a cumulative effect of the various process conditions. A strong correlation between the tablet bed RH and the frequency of tablet coating defect (logo bridging) was established, with increasing RH resulting in a higher percent of logo bridging events.     

Comparison of a laboratory and a production coating spray gun with respect to scale-up

A laboratory spray gun and a production spray gun were investigated in a scale-up study. Two Schlick spray guns, which are equipped with a new antibearding cap, were used in this study. The influence of the atomization air pressure, spray gun-to tablet bed distance, polymer solution viscosity, and spray rate were analyzed in a statistical design of experiments. The 2 spray guns were compared with respect to the spray width and height, droplet size, droplet velocity, and spray density. The droplet size, velocity, and spray density were measured with a Phase Doppler Particle Analyzer. A successful scale-up of the atomization is accomplished if similar droplet sizes, droplet velocities, and spray densities are achieved in the production scale as in the laboratory scale. This study gives basic information for the scale-up of the settings from the laboratory spray gun to the production spray gun. Both spray guns are highly comparable with respect to the droplet size and velocity. The scale-up of the droplet size should be performed by an adjustment of the atomization air pressure. The scale-up of the droplet velocity should be performed by an adjustment of the spray gun to tablet bed distance. The presented statistical model and surface plots are convenient and powerful tools for scaling up the spray settings if the spray gun is changed from laboratory spray gun to the production spray gun. Published: January 19, 2007     

The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol

Background  

Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of two studies on the pharmacokinetic properties of a novel ibuprofen (200 mg) and paracetamol (500 mg) fixed-dose combination tablet.     

延胡索乙素与白芷总香豆素、总挥发油配伍药效学比较研究

目的：评价延胡索乙素、白芷总香豆素及总挥发油配伍的药效学比较研究。方法：小鼠醋酸扭体法、热板镇痛法、甩尾法三种模型比较元胡止痛片（A组）、延胡索乙素（B组）、白芷总香豆素（C组）、白芷总挥发油（D组）、延胡索乙素与白芷总香豆素配伍（E组）、延胡索乙素与白芷总挥发油配伍（F组）及延胡索乙素与白芷总香豆素、白芷总挥发油配伍（G组）后的镇痛作用。结果：A、G组镇痛效果最佳,B、E、F组具显著的镇痛作用,C、D组与模型组相比,有一定的镇痛作用,但较弱。结论：延胡索乙素与白芷总香豆素、总挥发油配伍使用,具有显著的镇痛作用,类似于元胡止痛片中元胡白芷的配伍作用,但成分更为明确,标准可控,使用量小,属于分子中药组方范畴。元胡的主要有效成分延胡索乙素与白芷的主要成分白芷总香豆素、总挥发油均具有镇痛作用,符合中药元胡及白芷的功效,本实验采用药物有效成分进行配伍,成分明确,结果可控。     

Modeling weight variability in a pan coating process using Monte Carlo simulations

The primary objective of the current study was to investigate process variables affecting weight gain mass coating variability (CV _m) in pan coating devices using novel video-imaging techniques and Monte Carlo simulations. Experimental information such as the tablet location, circulation time distribution, velocity distribution, projected surface area, and spray dynamics was the main input to the simulations. The data on the dynamics of tablet movement were obtained using novel video-imaging methods. The effects of pan speed, pan loading, tablet size, coating time, spray flux distribution, and spray area and shape were investigated. CV _m was found to be inversely proportional to the square root of coating time. The spray shape was not found to affect the CV _m of the process significantly, but an increase in the spray area led to lower CV _ms. Coating experiments were conducted to verify the predictions from the Monte Carlo simulations, and the trends predicted from the model were in good agreement. It was observed that the Monte Carlo simulations underpredicted CV _ms in comparison to the experiments. The model developed can provide a basis for adjustments in process parameters required during scale-up operations and can be useful in predicting the process changes that are needed to achieve the same CV _m when a variable is altered.