金玉康胶囊治疗轻中度抑郁症的疗效和安全性

目的:评价金玉康胶囊治疗轻中度抑郁症的有效性和安全性。方法:采用多中心、随机、双盲、双模拟、活性药物平行对照设计。入选293例轻中度抑郁症患者,随机分为试验组145例和对照组148例,分别口服金玉康胶囊600 mg·d-1或盐酸氟西汀片20 mg·d-1,疗程均为6周。疗效观察指标包括基线以及治疗不同阶段的17项汉密尔顿抑郁量表(Hamilton rating scale for depression,HAMD17)、汉密尔顿焦虑量表(Hamilton rating scale for anxiety,HAMA)、临床总体印象量表(Clinical Global Impression scale,CGI)评分,以HAMD17作为主要疗效指标。结果:治疗结束时,两组的HAMD17总分与基线相比均明显降低,但两组间差异无显著性;两组的HAMD减分率接近,分别为55．77％和59．95％;以HAMD17减分率判断有效率,两组间差异也无显著性。两组的不良反应发生频率相当;体重在治疗结束时金玉康组较基线有所增加而氟西汀组没有明显变化,组间比较差异有统计学意义(F=5．014,P=0．026)。结论:金玉康胶囊治疗轻中度抑郁症安全、有效。     

盐酸度洛西汀肠溶胶囊治疗抑郁症的疗效和安全性

目的 评价盐酸度洛西汀肠溶胶囊(抗抑郁药)治疗抑郁症的疗效和安全性.方法 采用随机双盲双模拟多中心活性药平行对照临床研究,共入组抑郁症患者246例,试验组(n=123)口服度洛西汀60 mg·d-1;对照组(n=123)口服氟西汀20 mg·d-1,疗程均6周;以17项汉密尔顿抑郁量表(HAMD17)和临床总体印象量表(CGI)进行疗效评价;以不良事件、实验室检查和心电图检查等评价安全性.结果 度洛西汀组与氟西汀组有效率分别为85.47%和85.12%,痊愈率分别为64.10%和61.98%,2组差异无统计学意义(P>0.05);汉密尔顿焦虑量表(HAMA)和CGI的评分,在治疗结束时2组比较差异均无统计学意义.2组药物不良反应发生率分别为35.00%、24.79%,差异无统计学意义(P>0.05).结论 度洛西汀治疗抑郁症安全有效.     

拉莫三嗪与碳酸锂治疗双相抑郁的对照研究

目的:评价拉莫三嗪治疗双相抑郁的疗效和安全性.方法:采用开放,随机,活性药物平行对照设计.入选双相抑郁患者34例,随机分为拉莫三嗪组18例,碳酸锂组16例.分别口服拉莫三嗪50～200mg·d-1,碳酸锂750～1 500 mg·d-1,疗程8周,疗效观察指标包括基线以及治疗终点的17项汉密尔顿抑郁量表(HAMD17)、蒙哥马利抑郁量表(MADRS)、临床总体印象量表(CGI)评分.结果:治疗结束时,两组HAMD17总分与基线相比均明显降低,两组HAMD减分率差异有显著性,分别为24.8%和47.4%;以HAMD17减分率判断的有效率,两组间差异无显著性,分别为33.3%和50%.拉莫三嗪组治疗结束时体重无变化,有2例皮疹报告,其他不良事件两组发生频率相当.结论:拉莫三嗪治疗轻中度的双相抑郁部分有效.安全性较好.     

舒肝解郁胶囊治疗围绝经期女性的抑郁症的研究

目的:探讨舒肝解郁胶囊治疗围绝经期女性抑郁症的疗效和安全性。方法:70例抑郁围绝经期女性抑郁症患者随机分为舒肝解郁胶囊组(治疗组),艾司西酞普兰组(对照组)。治疗时间均为6周。两组治疗前及治疗后的第1、2、4、6周末分别进行汉密尔顿抑郁量表(HAMD)和不良反应量表(TESS)评定,并以HAMD分减分率评定疗效。结果:两组基线HAMD得分无显著差异(P>0.05)。治疗6周后,研究组总有效率91.4%,对照组总有效率88.6%,两组差异无统计学意义(R=0.52,P>0.05)。结论:舒肝解郁胶囊是治疗围绝经期女性抑郁症有效新型中成药。     

米氮平治疗广泛性焦虑症的疗效及安全性

目的:探讨米氮平治疗广泛性焦虑症的疗效和不良反应.方法:对60例广泛性焦虑症患者随机分为试验组及对照组,分别服用米氮平15～30mg·d-1和马普替林50～150mg·d-1,疗程均为6周.于治疗前及治疗后第1,2,4,6周末进行汉密尔顿焦虑量表(HAMD)及不良反应量表(TESS)评定疗效和不良反应.结果:试验组治疗广泛性焦虑症的显效率84.69%,有效率100%;对照组显效率66.67%,有效率88.89%,但两组比较经Ridit分析差异无显著性(P＞0.05).不良反应方面比较米氮平TESS评分显著低于马普替林(p＜0.05).结论:米氮平是治疗广泛性焦虑症的快速、安全、有效的药物.     

度洛西汀与文拉法辛缓释胶囊治疗伴焦虑症状抑郁症疗效的对照研究

目的比较度洛西汀和文拉法辛缓释胶囊治疗伴焦虑症状的抑郁症的临床疗效及副反应。方法符合CCMD-3抑郁症诊断标准,并且汉密尔顿焦虑量表评分≥14分的门诊及住院患者84例,随机分为两组,进行为期6周的治疗,在治疗前及治疗后第一、二、四、六周末用汉密尔顿抑郁量表(HAMD17)、汉密尔顿焦虑量表(HAMA14)评定疗效,以不良反应症状量表(TESS)评定副作用。结果度洛西汀和文拉法辛缓释胶囊治疗伴焦虑症状的抑郁症的显效率分别为76.2%和78.6%,两者差异无统计学意义。两组的HAMD17及HAMA14减分率相当(P>0.05)两者差异无统计学意义。两组的副反应相当,且均较轻。结论度洛西汀和文拉法辛缓释胶囊对伴焦虑症状的抑郁症的疗效均显著,抗抑郁及抗焦虑效果相当,两者副反应均较轻。     

西肽普兰合并曲唑酮治疗老年抑郁症疗效观察

目的:探讨西肽普兰合并曲唑酮治疗老年抑郁症的临床疗效。方法:将74例老年抑郁症患者随机分为治疗组(西肽普兰服用剂量为20～40 mg.d-1合并曲唑酮服用剂量50～150 mg.d-1)及对照组(单用西肽普兰)各37例,疗程6周。分别于治疗后1、2、6周末用汉密尔顿抑郁量表,汉密尔顿焦虑量表评定疗效,以症状量表(TESS)评定治疗中出现的不良反应。结果:2组治疗后汉密尔顿抑郁量表(HAMD)、汉密尔顿焦虑量表(HAMA)总分比较差异有统计学意义(P<0.05),治疗组的不良反应比对照组重,主要表现有头昏、嗜睡,但患者均能耐受。结论:西肽普兰合并曲唑酮治疗抑郁症比对照组临床疗效更好。     

甲磺酸瑞波西汀治疗抑郁症的疗效与安全性

目的:评价瑞波西汀治疗抑郁症的有效性和安全性。方法:73例抑郁症患者随机分成2组,治疗组为36例,给予甲磺酸瑞波西汀胶囊8~12mg.d-1;对照组37例,给予氟西汀胶囊20~40mg.d-1,2组疗程均为6周,治疗前及治疗后1、2、4、6周末采用HAMD、HAMA及TESS量表评定临床疗效和不良反应。结果:2组治疗结束时HAMD与HAMA评分均有显著下降(P<0.01),治疗组显效率为69.4%,对照组显效率为67.6%,2组疗效及不良反应比较无显著性差异(P>0.05)。结论:瑞波西汀与氟西汀治疗抑郁症的疗效和不良反应相似,是一种安全、有效的抗抑郁药。     

太子神悦胶囊治疗轻中度抑郁症的疗效和安全性

目的:评价太子神悦胶囊治疗轻中度抑郁症的疗效和安全性。方法:将研究对象随机分为试验组、阳性药组和安慰剂组,疗程为8周。以治疗终点的汉密尔顿抑郁17项(Hamilton Depression Scale-17 items, HAMD-17)量表减分值作为主要疗效评价指标,在基线、给药后1,2,4,8周末进行评价;安全性评价指标包括实验室检查、心电图检查、生命体征及不良事件发生率。结果:纳入符合标准的抑郁症患者601例。治疗终点3组间减分值比较差异有统计学意义(P<0.000 1),试验组优于安慰剂组(P<0.000 1),试验组非劣于阳性药组(P=0.735 4>0.05),尚不能认为试验组优于阳性药组。治疗期不良事件发生率分别为9.27%,15.97%,10.83%,组间差异无统计学意义(P>0.05)。结论:太子神悦胶囊治疗轻中度抑郁症安全有效。     

舒肝解郁胶囊治疗轻中度抑郁症的效果及安全性研究

目的 探讨舒肝解郁胶囊治疗轻中度抑郁症的临床疗效及安全性.方法 2010年5-12月收治的抑郁症76例,随机分为治疗组和对照组各38例,治疗组给予舒肝解郁胶囊治疗,对照组给予盐酸舍曲林治疗.治疗前、治疗1、2、4、6周分别采用汉密尔顿抑郁量表(HAMD)、治疗意外症状量表(TESS)评定治疗效果和药物的安全性.结果 两组在治疗2、4、6周HAMD评分均低于治疗前,治疗1、2周治疗组减分率显著低于对照组(PC),治疗组不良反应发生率低于对照组,差异均有统计学意义(P＜0.05).结论 舒肝解郁胶囊与盐酸舍曲林治疗抑郁症的疗效相当,但不良反应较少,安全性更高.     

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。     

Susceptibility to erythromycin of anaerobes of the genera Bacteroides, Fusobacterium, Sphaerophorus, Veillonella, Clostridium, Corynebacterium, Peptococcus, Peptostreptococcus

The minimal inhibitory concentrations (MIC) of erythromycin were determined by broth dilution tests for 313 anaerobic strains, most of which were clinical isolates. All the gram-positive anaerobes tested (84 Peptococcaceae, including 21 Peptostreptococcus anaerobius and 15 Peptococcus variabilis; 65 Corynebacterium acnes and 29 Clostridium strains, including 13 C. perfringens) were sensitive (MIC values 0.012 through 3.12 microgram erythromycin/ml); so were 111 cultures of gram-negative anaerobes (52 Bacteroides fragilis, 12 B. thetaiotaomicron, 7 B. vulgatus, 13 B. oralis, 4 B. melaninogenicus, 10 Sphaerophorus necrophorus, 2 Veillonella sp., 11 members of other species). Erythromycin at concentrations of 6.25 through 200.0 microgram/ml was active against 24 strains (1 B. fragilis, 4 Fusobacterium fusiforme, 9 Sph. freundi, 10 Sph. varius). The present results are compared to the limited number of reports existing with regard to the susceptibility of anaerobes to erythromycin.     

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.     

New antiretroviral drugs: a review of the efficacy,safety, pharmacokinetics,and resistance profile of tipranavir,darunavir, etravirine,rilpivirine, maraviroc,and raltegravir

Background: The introduction and approval of new antiretroviral agents in the US and Canada bring new opportunities and new challenges. Arguably, for the first time ever, clinicians have the drugs necessary to achieve the goal of suppressing HIV RNA to levels less than 50 copies/mL in even the most treatment-experienced patients and in those with extensive drug-limiting resistance mutations. However, the use of these new agents is complicated by many drug–drug interactions and – to some extent – pre-existing mutations. To derive maximum durability from the use of these newer drugs, a thorough understanding of their indications and limitations is critical. Objective: To thoroughly review the six most recently approved or soon-to-be-approved antiretroviral drugs in the US and Canada: tipranavir, darunavir, etravirine, rilpivirine, maraviroc, and raltegravir. Methods: Discussion of the indications for, and pharmacokinetics, resistance profile, activity, toxicity, and clinical trials results of, the six new agents. Results/conclusions: These six new agents have resulted in marked progress towards the goal of being able to provide HIV-infected individuals with the drugs necessary to achieve decades of durable suppression of HIV without substantial toxicity.     

Disposition of fluvastatin, an inhibitor of HMG-COA reductase, in mouse, rat, dog, and monkey

The physiological disposition of fluvastatin, a potent inhibitor of hydroxymethylglutaryl-CoA reductase and thus cholesterol synthesis, has been studied in the mouse, rat, dog, and monkey using 14C- or 3H-labeled drug. Oral doses of fluvastatin were absorbed at a moderate to rapid rate. The extent of absorption was dose-independent and was essentially complete in all four species studied. However, the drug was subject to extensive presystemic hepatic extraction followed by direct excretion via the bile, thus minimizing the systemic burden and yielding high liver/peripheral tissue concentration gradients for fluvastatin and its metabolites. Only at high doses far exceeding the intended human daily dose of ca 0.6 mg kg-1 did fluvastatin bioavailability approach unity, apparently due to saturation of the first-pass effect. Dose-normalized blood levels of fluvastatin and total radioactivity were higher in the dog than in the other species, suggesting a smaller distribution volume in the former. Fluvastatin was partially metabolized before excretion, the extent of metabolism being smallest in the dog and greatest in the mouse. The half-life of intact fluvastatin ranged from 1-2h in the monkey to 4-7h in the dog. Regardless of the dose or dose route, the administered radioactivity was recovered predominantly in feces, with the renal route accounting for less than 8 per cent of the dose. No tissue retention of radioactivity was observed, and material balance was essentially achieved within 96h after dosing.     

Strength of drug habits: For heroin,morphine, methadone,alcohol, barbiturates,pentobarbital, benzedrine,cocaine, and marijuana

The drug habits for 78 confirmed opiate addicts were studied on eight scales from the Process Association Test of Addiction (PATA) for many drug names. Through cluster analysis eight stages of addiction were defined: “to be clean”, “to learn about drugs”, “to hustle”, “to chip” (also “to be high”), to be psychologically dependent or “to need a shot”, “to be hooked”, “to kick a habit” and “to be in treatment”. Associations stimulated by the words heroin and morphine were very similar over the eight stages of addiction in opiate addicts. The subjects were especially inclined to associate morphine and heroin with the most severe level of addiction, “to be hooked”. Associations to both methadone and cocaine were elevated at the “hooked” stage, but in other respects associations to these drugs were opposite. Thus, associations to cocaine were focused on the stage of psychological dependence and the lower intermediate stage of addiction, “to chip” and “to be high”, whereas associations to methadone suggested a turning away from addiction as indicated by avoidance associations (“to come down” and “to kick a habit”) as well as associations to “treatment” and “to be clean”. Marijuana, Benzedrine, “goofball” (barbiturates) and alcohol habits were prominent at an intermediate stage of addiction (“to chip” and “to be high”). Avoidance associations were common for Benzedrine and “goofballs” (also pentobarbital) but not for marijuana or alcohol. “Hustling” associations were frequent for marijuana but not for alcohol.     

Simultaneous measurement of bupivacaine, etidocaine, lidocaine, meperidine, mepivacaine, and methadone

A gas-liquid chromatographic method for the simultaneous measurement of bupivacaine, etidocaine, lidocaine, meperidine, mepivacaine, and methadone in serum is described. The drugs and the internal standard, prilocaine, are extracted from 1 ml of serum. The procedure involves a two-step extraction and injection of the extract into a gas chromatograph equipped with a 10-ft OV-11 glass column and a nitrogen-phosphorus detector. The temperature gradient program results in a run time of 16 min and retention times for meperidine, prilocaine (internal standard), lidocaine, etidocaine, mepivacaine, methadone, and bupivacaine of 3.8, 5.4, 6.0, 8.7, 11.0, 11.7, and 14.8 min, respectively. Standard curves for all drugs were linear over the 80 to 2,000-ng/ml range and recovery of all components averaged 97 +/- 2% with the lowest detection limit of 10 ng/ml for all drugs except meperidine and methadone, which were 20 ng/ml. The within-day coefficients of variation ranged from 12 to 8% at 500 ng/ml. The day-to-day coefficients of variation of the slope and intercept values ranged from 2 to 0% and 130 to 3%, respectively. Response factors of the nitrogen-specific collector varied with the drug analyzed and resulted in peak area variation at constant offset and attenuation of 30%. This method is intended and adequate for therapeutic monitoring of chronically treated pain patients who are being given various combinations of local anesthetic and/or narcotic agents.     

马蹄金中铁、钙、镁、铜、锌、锰、镍的形态分析

目的：研究马蹄金全草中微量元素的存在形态。方法：采用超声波提取。电感耦合等离子发射光谱法（ICP—AES）对马蹄金不同形态中Fe、Ca、Mg、Cu、Zn、Ma、Ni等元素进行分析。结果：Fe元素在马蹄金中含量最高，而Cu元素含量最低；Ca的提取率最高，Fe的提取率最低；Ca、Mg、Cu、Zn、Mn、Ni6种元素的可溶态均大于悬浮态；且渣中的微量元素含量较高。结论：马蹄金中的微量元素是以无机态为主，多种形态共存的复杂体系。