2004年～2006年我院抗感染药物应用分析

目的：分析掌握我院抗感染药的应用情况,为临床合理应用抗感染药及科学管理提供依据。方法：根据我院“医院药品库存管理系统”的原始数据资料,采用限定日剂量法和销售金额排序法进行分析。结果：2004年～2006年我院抗感染药物的销售金额各占全年化学药销售金额的比例平均为33.29%,低于或接近于国内其他医院。β-内酰胺类销售金额遥遥领先,占抗感染药物销售金额的比例平均为55.8%。青霉素类、头孢菌素类、大环内酯类、氟喹诺酮类、抗结核药是使用频度最高的5大类。在DDDs排序前20位中,排序比〉1的药品占75%。结论：2004年～2006年我院抗感染用药结构基本合理,但仍应当加强管理。     

抗感染药物利用分析

目的 评价抗感染药物的应用现状及趋势.方法 对我院2005-2007年抗感染药物的销售金额、用药频度(DDDs)等进行回顾性分析.结果 我院抗感染药物销售金额2007年有所增长,但其占西药总销售金额的比例呈下降趋势.各年度头孢菌素类销售金额在抗感染药中所占比例均列第1位,平均为49.16%,β-内酰胺类(包括头孢菌素类、青霉素类和其他β-内酰胺类)在抗感染药销售金额中比重最大,占抗感染药总销售额的平均比例为58.83%.DDDs排序前4位的分别是头孢菌素类、大环内酯类、氟喹诺酮类、四环素类,其DDDs之和占年度抗感染药DDDs总和的75.25%、80.27%、80.76%;在DDDs排序前10位药品中,销售金额排序与DDDs排序比＞1的占99.97%.结论 安全、有效、价格低廉的抗感染药物占主导地位,临床用药合理.     

我院2004～2006年抗感染药利用分析

目的:评价我院抗感染药的应用现状及趋势。方法:对我院2004～2006年抗感染药的销售金额、用药频度(DDDs)等进行回顾性分析。结果:我院抗感染药销售金额逐年增长,但其占西药总销售金额的比例呈逐年下降趋势。各年度头孢菌素类销售金额在抗感染药中所占比例均列第1位,平均为36.46%,β-内酰胺类(包括头孢菌素类、青霉素类和其它β-内酰胺类)销售金额平均占抗感染药销售金额的52.62%;DDDs排序列前4位的分别是喹诺酮类、头孢菌素类、大环内酯类和青霉素类,其DDDs之和平均占各年度抗感染药总DDDs的73.89%;在DDDs排序列前10位药品中,销售金额排序与DDDs排序比>1的占76.67%。结论:安全、有效、价格低廉的抗感染药在我院占主导地位。     

我院2002-2004年抗感染药应用分析

目的:分析掌握我院各类抗感染药的使用情况,为临床合理应用抗生素及科学制定采购计划提供依据。方法:根据我院“医院药品库存管理系统”的原始数据资料,采用限定日剂量法和销售金额排序法进行分析。结果:1.我院抗感染药品种数2003年与2004年持平,比2002年有所增加,但增幅不大,头孢菌素类品种数最多;2.抗感染药销售金额平均占西药销售金额的42.03%,头孢菌素类销售金额遥遥领先,平均占抗感染药销售金额的33.58%;3.青霉素类、头孢菌素类、大环内酯类、喹诺酮类、抗结核药、林可霉素类药物是使用频度最高的6大类,提示结核病的流行情况不容乐观。结论:医院3年来抗感染药物品种增多、占总体用药比例偏高,建议加强对病原菌及其耐药性监测,强化合理用药意识。     

我院2001～2005年抗感染药利用分析

目的:了解我院抗感染药的应用状况及趋势。方法:采用金额排序法和用药频度(DDDs)排序法对我院2001～2005年抗感染药应用数据进行统计、分析。结果:我院抗感染药销售金额占药品总销售金额的24.63%～28.47%,销售金额较大的是头孢菌素类和复方β-内酰胺酶抑制剂,占抗感染药销售金额的2/3以上;DDDs较大的是第2代头孢菌素类和青霉素类。结论:头孢菌素类和复方β-内酰胺酶抑制剂在我院的应用占主导地位。     

抗感染药物利用分析

目的评价抗感染药物的应用现状及趋势。方法对我院2005-2007年抗感染药物的销售金额、用药频度（DDDs）等进行回顾性分析。结果我院抗感染药物销售金额2007年有所增长,但其占西药总销售金额的比例呈下降趋势。各年度头孢菌素类销售金额在抗感染药中所占比例均列第1位,平均为49．16％,β-内酰胺类（包括头孢菌素类、青霉素类和其他β-内酰胺类）在抗感染药销售金额中比重最大,占抗感染药总销售额的平均比例为58．83％。DDDs排序前4位的分别是头孢菌素类、大环内酯类、氟喹诺酮类、四环素类,其DDDs之和占年度抗感染药DDDs总和的75．25％、80．27％、80．76％;在DDDs排序前10位药品中,销售金额排序与DDDs排序比〉1的占99．97％。结论安全、有效、价格低廉的抗感染药物占主导地位,临床用药合理。     

2005～2009年我院抗感染药应用情况分析

目的：了解我院抗感染药的应用状况及趋势。方法：采用金额排序法和用药频度（DDDs）排序法对我院2005～2009年抗感染药应用数据进行统计、分析。结果：我院抗感染药销售金额占药品总销售金额的20.40%～27.14%,销售金额较大的是头孢菌素类和青霉素类,占抗感染药销售金额的2/3以上;DDDs较大的是氟喹诺酮类和青霉素类。结论：头孢菌素类和青霉素类在我院的应用占主导地位。     

2007～2009年我院住院患者抗感染药使用情况分析

目的：评估我院住院患者抗感染药的应用情况,为临床合理用药提供参考。方法：对我院2007～2009年住院患者抗感染药的用药频度（DDDs）、销售金额、限定日费用（DDC）等数据进行统计、分析。结果：3年来我院住院患者抗感染药销售金额持续增长,但占我院全年药品销售比例基本不变,排序第1位的是头孢菌素类;用药频度（DDDs）排序前两位的是头孢菌素类和氟喹诺酮类;β-内酰胺酶抑制剂复合制剂的金额和DDDs上升明显。结论：头孢菌素类抗菌药物在我院住院患者的应用中占主导地位;应加强抗感染药的合理应用和规范化管理,控制细菌耐药率增长。     

2007～2009年我院抗感染药应用调查

目的：分析我院2007～2009年抗感染药的使用情况,为临床合理用药提供依据。方法：采用限定日剂量（DDD）分析法,对本院2007～2009年抗感染药的销售金额和用药频率进行统计、综合分析。结果：2007～2009年间抗感染药销售金额逐年上升,占当年西药销售金额的比例平均为31．9％。头孢菌素类销售金额最高,占抗感染药总量的72％。头孢菌素类、喹诺酮类和青霉素类使用频率最高。DDDs排序前10位中,排序比〉1的药物占70％。结论：我院抗感染药的应用结构基本合理,但仍存在一定的问题,医师应严格执行《抗菌药物临床应用指导原则》的规定。     

2008～2010年我院抗感染药应用情况分析

目的:评价我院抗感染药的应用情况和趋势,为临床合理选择抗感染药提供依据。方法:采用金额排序法、用药频度(DDDs)排序法以及日治疗费用(DDC)法对我院2008～2010年抗感染药进行回顾性分析。结果:2008～2010年我院抗感染药销售金额占药品总销售金额的构成比为26.35%、25.26%、24.6%,头孢菌素类始终居用药第1位。结论:2008～2010年我院抗感染药临床使用量和金额均逐年增长,整体使用情况基本合理,部分品种存在不合理使用现象,需进一步加强监督管理。     

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.