曲美他嗪对扩张型心肌病心力衰竭患者LVEF值的影响

目的探讨曲美他嗪对扩张型心肌病心力衰竭患者LVEF值的影响。方法 24例扩张型心肌病心力衰竭患者,随机分为治疗组和对照组各12例。对照组采用常规治疗,治疗组在此基础上加用曲美他嗪,比较2组治疗前后LVEF值。结果服药4个月后,治疗组LVEF值由(34.1±5.2)%上升至(44.3±8.2)%,较治疗前明显升高(P<0.01),与对照组比较差异有统计学意义(P<0.05)。对照组LVEF值由(33.2±4.9)%上升至(37.4±7.1)%,与治疗前比较差异显著(P<0.01)。结论曲美他嗪治疗扩张型心肌病合并心力衰竭效果显著,可临床推广应用。     

曲美他嗪对扩张型心肌病患者的临床疗效

目的 探讨曲美他嗪对扩张型心肌病（DCM）慢性心力衰竭(CHF)的临床疗效。方法40例扩张型心肌病伴中、重度心力衰竭患者。随机分为两组，对照组19例，常规使用洋地黄、利尿药、血管紧张肽转换酶抑制药、β-受体阻滞药等药物治疗。治疗组21例，在对照组常规治疗基础上，加用曲美他嗪20 mg ，po，tid，均8周为1个疗程。观察曲美他嗪治疗前及治疗8周后,对心功能分级、左心室射血分数（LVEF）、左室舒张末期内径（LVDd）及脑钠肽（BNP）的影响。结果治疗组临床心功能分级明显改善，总有效率90.5%，对照组为52.6%。治疗组LVEF值显著提高、LVDd显著减小，BNP水平明显升高，而血压、心率则无影响。结论曲美他嗪能明显改善扩张型心肌病患者的心功能。     

曲美他嗪对老年性缺血性扩张型心肌病的疗效观察

目的观察在常规治疗的基础上加用曲美他嗪对改善老年性缺血性扩张型心肌病心力衰竭的疗效。方法将40例符合诊断标准的老年性缺血性扩张型心肌病的患者随机分为常规治疗组（对照组）和曲美他嗪治疗组（治疗组），两组疗程均为20周，比较两组治疗前后的临床疗效、心功能分级、LVEF值、心胸比等。结果曲美他嗪治疗组临床心功能分级明显改善，LVEF值显著提高，而血压、心率无影响。结论曲美他嗪治疗能明显改善老年性缺血性扩张型心肌病患者心功能。     

曲美他嗪治疗扩张型心肌病心力衰竭患者的临床应用

目的探讨曲美他嗪治疗扩张型心肌病心力衰竭患者的临床应用效果.方法84例扩张型心肌病心力衰竭患者,采用随机数字表法分为观察组和对照组,每组42例.对照组采用常规治疗,观察组在对照组基础上采用曲美他嗪治疗.比较两组患者治疗前后血清因子[肿瘤坏死因子-α(TNF-α)、可溶性细胞间黏附分子(sICAM-1)]水平、心功能指标[左室射血分数(LVEF)、左室收缩末期内径(LVESD)、左室舒张末期内径(LVEDD)]水平、治疗效果、不良反应发生情况.结果治疗后,两组TNF-α、sICAM-1水平均低于治疗前,且观察组TNF-α、sICAM-1水平均低于对照组,差异具有统计学意义(P<0.05).治疗后,两组LVEF、LVESD、LVEDD水平均优于治疗前,且观察组的LVEF、LVESD、LVEDD水平均优于对照组,差异具有统计学意义(P<0.05).观察组治疗总有效率95.24%高于对照组的80.95%,差异具有统计学意义(χ^2=4.086,P=0.043<0.05).两组不良反应发生率比较,差异无统计学意义(χ^2=0.553,P>0.05).结论曲美他嗪治疗扩张型心肌病心力衰竭能够有效改善血清因子水平,改善心功能,提高治疗效果,安全性良好.     

曲美他嗪治疗扩张型心肌病心力衰竭临床疗效观察

目的：观察曲美他嗪治疗扩张型心肌病心力衰竭患者临床疗效。方法：扩张型心肌病患者50例,随机分为两组：对照组25例,常规使用洋地黄、利尿药、血管紧张素转换酶抑制药、β－受体阻滞药等药物治疗;治疗组25例,在对照组常规治疗基础上加用曲美他嗪20mg,po,tid,治疗3个月。观察治疗前后两组左室射血分数（LVEF）、心功能、左室收缩末期内径（LVESD）和左室舒张末期内径（LVEDD）变化。结果：治疗组心功能明显改善,总有效率为92．0％,对照组为60．0％。治疗组LVEF值显著提高,P〈0．01,左室收缩、舒张末期内径明显缩小,P〈0．01。结论：曲美他嗪能明显改善扩张型心肌病患者的心功能,逆转心室重构。     

曲美他嗪在扩张型心肌病的应用研究

目的评价曲美他嗪对扩张型心肌病患者左心功能不全的治疗效果。方法选择扩张型心肌病合并左心功能不全患者105例。随机将患者分为曲美他嗪组50例,常规治疗组55例,曲美他嗪组在常规治疗基础上加用曲美他嗪20mg 3次/d,服用12个月,对照组仅用常规治疗。治疗前、治疗后6个月、1年观察患者临床情况及多普勒超声指标的变化。结果曲美他嗪组急性左心衰竭发作率较常规治疗组低(P<0.05),而心源性病死率两组比较差别无统计学意义(P>0.05),治疗后6个月及1年两组LVEF均有改善,但曲美他嗪组改善更显著(P<0.05)。结论短期观察,在常规治疗基础上加用曲美他嗪长期治疗,可明显改善扩张型心肌病患者的左心功能。     

曲美他嗪对扩张型心肌病心力衰竭患者心功能的疗效观察

目的：观察曲美他嗪治疗扩张型心肌病（DCM）合并心力衰竭的临床价值。方法：100例DCM合并心力衰竭患者随机分为观察组和对照组,对照组给予常规抗心力衰竭治疗,观察组在常规治疗的基础上加用曲美他嗪治疗。观察治疗前和治疗24周后患者心功能分级及左室射血分数（LVEF）、左室舒张末期内径（LVEDD）、每分心排量（CO）的变化。结果：治疗24周后,对照组总有效率为72.00%（36/50）,观察组总有效率为88.00%（44/50）,两者比较差异有统计学意义（P〈0.05）;两组治疗后LVEDD、CO、LVEF均较治疗前显著改善（P〈0.01）,且观察组治疗后上述指标明显优于对照组（P〈0.01或P〈0.05）。结论：曲美他嗪可以安全有效地改善DCM合并心力衰竭患者的心功能,值得临床推广。     

卡维地洛治疗扩张型心肌病心力衰竭临床观察

目的：观察卡维地洛治疗扩张型心肌病心力衰竭的疗效。方法：将80例扩张型心肌病心力衰竭患者随机分配到观察组和对照组,对照组采用常规抗心衰治疗,观察组在常规抗心衰治疗的基础上加用卡维地洛进行干预。比较治疗前后观察组和对照组的左心室收缩末期内径（LVESD）,左心室舒张末期内径（LVEDD）,左心室射血分数（LVEF）等反映左心室功能与结构变化的指标,比较观察组和对照组治疗扩张型心肌病心力衰竭的总有效率。结果：对照组对扩张型心肌病心力衰竭患者治疗的总有效率明显低于观察组,P〈0．05。治疗6个月后。观察组患者LVESD明显低于对照组,P〈0．05,而LVEDD与LVEF明显高于对照组。治疗前后组内比较LVESD、LVEDD与LVEF．P〈0．05。差异有统计学意义。结论：对于扩张型心肌病心力衰竭患者,在常规抗心衰治疗的基础上加用卡维地洛能够显著改善左室舒缩功能与心功能状态．有利于左室重构．提高生活质量。     

扩张型心肌病应用曲美他嗪治疗临床观察

目的观察应用曲美他嗪治疗扩张型心肌病并慢性充血性心力衰竭临床疗效。方法选取近年来我院扩张型心肌病并慢性充血性心力衰竭患者46例,随机分成治疗组和对照组,两组均为23例,对照组给予利尿剂、洋地黄、单硝酸脂类药物、血管紧张素酶抑制剂和β受体阻滞剂。治疗组在对照组基础上加用曲美他嗪每天3次,一次20 mg,观察6个月。观察治疗前后心功能分级变化、左室射血分数(LVEF),心衰加重再住院率。结果曲美他嗪组治疗后的心功能改善比对照组明显LVEF与对照组相比有明显提高,再住院明显减少。结论曲美他嗪能显著改善扩张型心肌病心功能。     

美托洛尔联合曲美他嗪在冠心病心衰治疗中的临床疗效

目的 探讨美托洛尔联合曲美他嗪在冠心病心衰治疗中的临床疗效.方法 回顾性分析2013年8月至2016年10月期间我院收治的100例冠心病心衰患者的病历资料,将所有患者按照入院顺序分为对照组51例和研究组49例,对照组患者给予常规的临床治疗,研究组在对照组的基础上采用美托洛尔联合曲美他嗪治疗,对比两组患者的治疗效果及治疗前后各观察指标变化.结果 研究组治疗总有效率显著高于对照组,治疗后研究组LVESD、LVEDD、LVEF以及HR指标改善情况显著优于对照组,两组比较差异性显著(P<0.05).结论 美托洛尔联合曲美他嗪联合应用能有效的改善冠心病心衰患者的LVESD、LVEDD、LVEF以及HR,临床疗效显著,具有一定的应用价值.     

Safety assessment of poloxamers 101, 105, 108, 122, 123, 124, 181, 182, 183, 184, 185, 188, 212, 215, 217, 231, 234, 235, 237, 238, 282, 284, 288, 331, 333, 334, 335, 338, 401, 402, 403, and 407, poloxamer 105 benzoate, and poloxamer 182 dibenzoate as used in cosmetics

Poloxamers are polyoxyethlyene, polyoxypropylene block polymers. The impurities of commercial grade Poloxamer 188, as an example, include low-molecular-weight substances (aldehydes and both formic and acetic acids), as well as 1,4-dioxane and residual ethylene oxide and propylene oxide. Most Poloxamers function in cosmetics as surfactants, emulsifying agents, cleansing agents, and/or solubilizing agents, and are used in 141 cosmetic products at concentrations from 0.005% to 20%. Poloxamers injected intravenously in animals are rapidly excreted in the urine, with some accumulation in lung, liver, brain, and kidney tissue. In humans, the plasma concentration of Poloxamer 188 (given intravenously) reached a maximum at 1 h, then reached a steady state. Poloxamers generally were ineffective in wound healing, but were effective in reducing postsurgical adhesions in several test systems. Poloxamers can cause hypercholesterolemia and hypertriglyceridemia in animals, but overall, they are relatively nontoxic to animals, with LD(50) values reported from 5 to 34.6 g/kg. Short-term intravenous doses up to 4 g/kg of Poloxamer 108 produced no change in body weights, but did result in diffuse hepatocellular vacuolization, renal tubular dilation in kidneys, and dose-dependent vacuolization of epithelial cells in the proximal convoluted tubules. A short-term inhalation toxicity study of Poloxamer 101 at 97 mg/m(3) identified slight alveolitis after 2 weeks of exposure, which subsided in the 2-week postexposure observation period. A short-term dermal toxicity study of Poloxamer 184 in rabbits at doses up to 1000 mg/kg produced slight erythema and slight intradermal inflammatory response on histological examination, but no dose-dependent body weight, hematology, blood chemistry, or organ weight changes. A 6-month feeding study in rats and dogs of Poloxamer 188 at exposures up to 5% in the diet produced no adverse effects. Likewise, Poloxamer 331 (tested up to 0.5 g/kg day(-1)), Poloxamer 235 (tested up to 1.0 g/kg day(-1)), and Poloxamer 338 (at 0.2 or 1.0 g/kg day(-1)) produced no adverse effects in dogs. Poloxamer 338 (at 5.0 g/kg day(-1)) produced slight transient diarrhea in dogs. Poloxamer 188 at levels up to 7.5% in diet given to rats in a 2-year feeding study produced diarrhea at 5% and 7.5% levels, a small decrease in growth at the 7.5% level, but no change in survival. Doses up to 0.5 mg/kg day(-1) for 2 years using rats produced yellow discoloration of the serum, high serum alkaline phosphatase activity, and elevated serum glutamicpyruvic transaminase and glutamic-oxalacetic transaminase activities. Poloxamers are minimal ocular irritants, but are not dermal irritants or sensitizers in animals. Data on reproductive and developmental toxicity of Poloxamers were not found. An Ames test did not identify any mutagenic activity of Poloxamer 407, with or without metabolic activation. Several studies have suggested anticarcinogenic effects of Poloxamers. Poloxamers appear to increase the sensitivity to anticancer drugs of multidrug-resistant cancer cells. In clinical testing, Poloxamer 188 increased the hydration of feces when used in combination with a bulk laxative treatment. Compared to controls, one study of angioplasty patients receiving Poloxamer 188 found a reduced myocardial infarct size and a reduced incidence of reinfarction, with no evidence of toxicity, but two other studies found no effect. Poloxamer 188 given to patients suffering from sickle cell disease had decreased pain and decreased hospitilization, compared to controls. Clinical tests of dermal irritation and sensitization were uniformly negative. The Cosmetic Ingredient Review (CIR) Expert Panel stressed that the cosmetic industry should continue to use the necessary purification procedures to keep the levels below established limits for ethylene oxide, propylene oxide, and 1,4-dioxane. The Panel did note the absence of reproductive and developmental toxicity data, but, based on molecular weight and solubility, there should be little skin penetration and any penetration of the skin should be slow. Also, the available data demonstrate that Poloxamers that are introduced into the body via routes other than dermal exposure have a rapid clearance from the body, suggesting that there would be no risk of reproductive and/or developmental toxicity. Overall, the available data do not suggest any concern about carcinogenesis. Although there are gaps in knowledge about product use, the overall information available on the types of products in which these ingredients are used, and at what concentration, indicates a pattern of use. Based on these safety test data and the information that the manufacturing process can be controlled to limit unwanted impurities, the Panel concluded that these Poloxamers are safe as used.     

HPLC法测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱

目的 采用高效液相色谱（HPLC）法同时测定抗妇炎胶囊中木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱10种活性成分。方法 采用InerSustain AQ-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,流动相A：乙腈–无水乙醇（80∶20）,流动相B：0.1%磷酸溶液,梯度洗脱,检测波长220 nm,体积流量1.0 mL/min,柱温30℃,进样量10 μL。结果 木兰花碱、黄柏碱、药根碱、巴马汀、小檗碱、槐果碱、苦参碱、氧化槐果碱、槐定碱和氧化苦参碱分别在2.69～134.50、1.95～97.50、0.63～31.50、0.86～43.00、11.95～597.50、0.59～29.50、6.08～304.00、4.85～242.50、1.66～83.00、19.79～989.50 μg/mL线性关系良好（r≥0.999 3）;平均回收率分别为99.11%、98.23%、96.95%、97.78%、100.02%、97.21%、99.66%、99.52%、98.81%、100.08%,RSD值分别为1.04%、1.23%、1.37%、1.65%、0.70%、1.28%、0.65%、0.81%、1.11%、0.63%。结论 建立的HPLC法可用于抗妇炎胶囊中10种活性成分的测定,作为抗妇炎胶囊质量控制方法。     

Arformoterol: (R,R)-eformoterol, (R,R)-formoterol, arformoterol tartrate, eformoterol-sepracor, formoterol-sepracor, R,R-eformoterol, R,R-formoterol

Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral centres and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. In 1995, Sepracor acquired New England Pharmaceuticals, a manufacturer of metered-dose and dry powder inhalers, for the purpose of preparing formulations of levosalbutamol and arformoterol. Phase II dose-ranging clinical studies of arformoterol as a longer-acting, complementary bronchodilator were completed successfully in the fourth quarter of 2000. Phase III trials of arformoterol began in September 2001. The indications for the drug appeared to be asthma and chronic obstructive pulmonary disease (COPD). However, an update of the pharmaceutical product information on the Sepracor website in September 2003 listed COPD maintenance therapy as the only indication for arformoterol. In October 2002, Sepracor stated that two pivotal phase III studies were ongoing in 1600 patients. Sepracor estimates that its NDA submission for arformoterol, which is projected for the first half of 2004, will include approximately 3000 adult subjects. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. In addition, Sepracor stated that the two pivotal phase III studies in 1600 patients were still progressing. In 1995, European patents were granted to Sepracor for the use of arformoterol in the treatment of asthma, and the US patent application was pending.     

欧洲刺柏（Juniper）

活性成分与药理作用欧洲刺柏药用部位是其浆果，具有促水排泄、防腐、抗胃肠胀气和抗风湿作用，还可改善胃功能。用作促水排泄药可增加尿量（水丢失），但不增加钠排泄。成分萜品烯-4-醇可增加肾小球滤过率，但刺激肾。欧洲刺柏浆果对单纯疱疹病毒体外显示抗病毒活性，并具抗真菌活性。动物实验显示，欧洲刺柏浆果提取物具有堕胎、抗生育、抗炎、抗胚胎植入、降血压、升血压和降血糖作用。欧洲刺柏浆果油具有兴奋子宫的活性，以及利尿、胃肠道抗菌和刺激作用，该油对平滑肌有阻止解痉作用。     

Oral Presentations (LDD, LPES, LNM, LPAT, LNT, LPPT, LPM)

Probiotic microorganisms have been shown to provide specific health benefits when consumed as food supplements or as food components. The main problem of such products is the poor survival of the probiotic bacteria in the low pH of gastric fluid. However the use of synthetic excipients for enteric coating to prevent the exposure of microorganisms to gastric fluid is limited in food supplementary industry. Therefore the aim of this study was to develop an enteric coating formulation containing shellac as a natural polymer. Shellac possesses good resistance to gastric juice; the major disadvantage of this polymer is its low solubility in the intestinal fluid [1, 2]. Thus films containing different ratios of shellac and water-soluble polymers (sodium alginate, hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidon (PVP)) or plasticizers (glycerol and glyceryl triacetate (GTA)) were prepared in order to analyse the films’ melting temperatures (T_m), the changes in enthalpy (ΔH), their capability of taking up water, and their solubility in different media. The release characteristics of the films were studied by loading pellets with Enterococcus faecium M74 and coating them with formulations containing different amounts of shellac and polymer or plasticized shellac. Using dissolution tests, performed according to USP XXXI paddle method, the resistance of the coatings to simulated gastric fluid (SGF, pH 1.2) and the release of cells in simulated intestinal fluid (SIF, pH 6.8) was investigated.The trials showed that an increasing amount of plasticizer results in a decrease of T_m and ΔH of the films whereat glycerol had a superior plasticization effect to GTA. The compatibility of films made of water-soluble polymers and shellac was also concentration dependent. HPMC and PVP showed superior compatibility with shellac compared to sodium alginate, since films containing shellac and more than 10% [w/w] sodium alginate tended to separate into two phases. In the end five formulations containing shellac and either 5% [w/w] glycerol, 10% [w/w] PVP, 20% [w/w] PVP, 10% [w/w] HPMC, or 5% [w/w] sodium alginate emerged as feasible for enteric coating purposes.