正交试验优选复方甘草酸单铵氯化钠注射液制备工艺

目的用正交试验方法优选复方甘草酸单铵氯化钠注射液的制备工艺。方法采用正交试验,选择活性炭用量、中间体pH、微孔滤芯孔径、活性炭吸附温度4个因素,每个因素安排4个水平,按L16（4^5）安排正交试验,用2个指标的加权评分值判定工艺优劣,试验结果进行方差分析。结果活性炭对甘草酸单铵有明显吸附作用,影响成品率的主要因素为活性炭及pH。在主药浓度、吸附时间固定时,加炭0．05％、中间体pH=6．5、吸附温度70℃、滤芯孔径0．22μm的优化条件下,活性炭对甘草酸单铵吸附较少、产品热原检查合格、澄明度、成品率最高。结论配制复方甘草酸单铵氯化钠注射液时要对各影响因素进行控制,避免原料损失,提高成品率及产品质量。     

正交试验优选葡萄糖注射液澄明度

目的:筛选提高葡萄糖注射液澄明度的工艺。方法:采用正交试验法,选择活性炭用量、中间品pH值、煮沸时间3个因素,每个因素安排3个水平,按L9(33)安排正交试验,用2个指标的相加值判定工艺的优劣。结果:用0.5%的活性炭,pH调至4.5,煮沸30 分钟,效果理想。结论:试验结果对提高葡萄糖注射液澄明度有指导意义。     

正交试验法优选右旋糖酐40葡萄糖注射液澄明度的工艺

目的：应用正交试验法优选右旋糖酐４０葡萄糖注射液澄明度的工艺。方法；选择活性髅用量，中间品ｐＨ值与砂棒回流时间等三因素，每个因素取２个水平，按Ｌ８（２＾７）正交安排实验，用２个指标评定工艺的优劣。结果；采用活性炭用量为３．０％，中间品ｐＨ值为４．５，砂棒回流时间４５ｍｉｎ的工艺条件最佳。     

复方氨基酸注射液生产工艺研究

目的对复方氨基酸注射液的制备工艺进行研究,制定切实可行的生产工艺。方法分析影响复方氨基酸注射液成品质量的因素,采用正交试验方法,选择最佳溶解温度、药液pH值、活性炭用量及灭菌条件,以确定最佳生产工艺。结果复方氨基酸注射液成品的含量、可见异物合格率高,成品率得到提高。结论用该工艺生产的复方氨基酸注射液质量稳定,工艺设计合理,切实可行。     

正交试验优选葡萄糖注射液澄明度的工艺

目的：筛选提高葡萄糖注射液澄明度的工艺。方法：采用正交试验法,选择活性炭用量、中间品ｐＨ值、煮沸时间３个因素,每个因素安排３个水平,按Ｌ９（３＾３）安排正交试验,用２个指标的相加值判定工艺的优劣。结果：用０．５％的活性炭,ｐＨ调至４．５,煮沸３０分钟,效果理想。结论：试验结果对提高葡萄糖注射液澄明度有指导意义。     

正交法考察盐酸洛美沙星葡萄糖注射液制备工艺

目的对盐酸洛美沙星葡萄糖注射液生产工艺过程的影响因素进行实验考察,寻求最佳生产工艺。方法通过正交设计考察pH、加炭量、温度和加热时间4个因素对盐酸洛美沙星含量的影响,选用L16（4^5）正交表进行实验。结果活性炭对盐酸洛美沙星有明显吸附作用,在pH值为4．8,加炭量为0．02％,温度为50℃及加热时间为10min的优化条件下,活性炭对盐酸洛美沙星的吸附量最小。结论生产过程中应对上述影响因素进行控制,提高产品质量。     

正交设计法考察盐酸洛美沙星葡萄糖注射液制备工艺

目的：对盐酸洛美沙星葡萄糖注射液生产工艺过程的影响因素进行实验考察，寻求最佳生产工艺。方法：通过正交设计考察pH、加炭量、温度和加热时间4个因素对盐酸洛美沙星含量的影响，选用L16(4^5)正交表进行实验。结果：实验证明活性炭对盐酸洛美沙星有明显吸附作用，在pH值为4．8，加炭量为0．02％，温度为50℃及加热时间为10 min的优化条件下，活性炭对盐酸洛美沙星的吸附量最小。结论：生产过程中应对上述影响因素进行控制，提高产品质量。     

甘草酸二铵注射液与三种注射液配伍的稳定性

目的考察甘草酸二铵注射液分别与酚妥拉明、利巴韦林、门冬氨酸钾镁注射液配伍的稳定性。方法采用紫外分光光度法,考察在不同温度下(4、25、37℃)各配伍液0~6 h内吸收度和吸收曲线的变化,测定其pH值及不溶性微粒数,并观察其外观。结果在5%葡萄糖注射液中,甘草酸二铵注射液分别与上述3种药物配伍后,其pH值、外观、吸收度等几乎无变化。结论在上述实验条件下,甘草酸二铵注射液分别与以上3种药物配伍稳定。     

活性炭去除注射液中热原的工艺条件考察

目的:考察注射液生产工艺中活性炭吸附热原的适宜条件。方法:从活性炭加入比例、pH变化、吸附温度、加入次数和活化处理方式等5个方面进行分析,运用动态浊度法进行检测,研究最佳工艺条件。结果:活性炭去除热原的适宜工艺条件为添加比例0.3%、pH 5.0、温度50℃、二次吸附和105℃干燥活化处理。结论:建立了活性炭去除注射液中热原的常用方法。     

正交试验设计法对甲硝唑注射液配制方法的探讨

本文用正交试验设计法对甲硝唑注射液配制方法进行了探讨。实验结果表明,活性炭用量、煮沸时间和配制方法均对甲硝唑注射液有显著性影响(F>0.01),溶液pH值和消毒温度对甲硝唑注射液有显著影响(F>0.05)。选择最佳配制方法为:活性炭用量0.1％,吸附时间为煮沸10分钟,溶液pH值5.0～5.5,灭菌温度110℃30分钟。     

Neuroscience and Hormesis: Overview and General Findings

This article provides a summary of an assessment of the occurrence and impact of hormesis in the neurosciences, including the areas of neuroprotection, neurite outgrowth, and drugs for Alzheimer's disease, Parkinson's disease, anxiety, pain, seizures, stroke, as well as in the areas of behavioral pharmacology, addictive drugs, stress biology including the Yerkes–Dodson law, and p-glycoprotein efflux activity. The findings indicate that the hormetic dose response has a common, if not dominant, presence in each of these diverse areas of neuroscience and further strengthens the conclusion that hormesis is highly generalizable, being independent of biological model, endpoint, and chemical class.     

Self-injection of barbiturates and benzodiazepines in baboons

Self-injection of three barbiturates, six benzodiazepines, and chlorpromazine was examined in baboons. Intravenous injections of drug were dependent upon completion of 160 lever presses (a 160-response fixed-ratio schedule). A 3-h time-out period followed each injection, permitting a maximum of eight injections per day. Prior to testing each dose of drug, self-injection performance was established with cocaine. Subsequently, a test dose was substituted for cocaine. Amobarbital, pentobarbital, and secobarbital maintained the highest levels of self-injection, which were similar to those maintained by cocaine. Clonazepam, clorazepate, diazepam, flurazepam, medazepam, and midazolam maintained relatively modest levels of self-injection, while chlorpromazine maintained only low levels, which were in the range of vehicle control. Of the six benzodiazepines, midazolam produced the highest levels of self-injection. At the highest self-injected doses, the barbiturates produced anesthesia in contrast to the benzodiazepines, which produced only sedation. None of the drugs affected food intake except for chlorpromazine, which produced dose-related decreases. The differences among the drug classes (i.e., barbiturate, benzodiazepine, phenothiazine) with respect to the maintenance of self-injection correspond well with the results of previous animal and human drug self-administration studies.     

基于HMGR、SQS1、β-AS基因CNVs的甘草道地性机制研究

本文利用real-time PCR方法对不同产地甘草的3-羟基-3-甲基戊二酰CoA还原酶 (3-hydroxy-3-methylglutaryl-CoA reductase, HMGR)、鲨稀合成酶1 (squalene synthetase 1, SQS1)、β-香树脂醇合成酶 (β-amyrin synthase, β-AS) 基因的拷贝数进行了研究, 发现不同产地的HMGR基因存在1～3个拷贝数变异, SQS1基因存在1～2个拷贝数变异, 未发现β-AS基因拷贝数变异。甘草HMGR、SQS1、β-AS基因拷贝数存在5种自然组合类型: A型 (2+1+1)、B型 (1+1+1)、C型 (3+2+1)、D型 (2+2+1) 和E型 (3+1+1), 其中内蒙古杭锦旗甘草存在A、B两种类型, A与B的比例为1∶1.3; 内蒙古赤峰甘草也存在A、B两种类型, 但A与B比例为3∶1; 宁夏盐池甘草存在A、B、C、D 4种类型, A/B/C/D比例为1∶5.1∶1∶2, A/B比例为1∶5.1; 甘肃民勤甘草存在A、B、E 3种类型, A/B/E比例为4.1∶2.1∶1, A/B比例为2∶1。本研究证明中药功能基因基因组拷贝数变异 (copy number variations, CNVs) 与产地具有相关性, 可能是道地药材形成的机制之一。     

Planning Future Strategies for Domestic and International NeuroAIDS Research, July 24–25, 2008

The National Institute of Mental Health in cooperation with the National Institute on Drug Abuse and the National Institute of Neurological Disorders and Stroke organized a meeting on July 24–25, 2008 to develop novel research directions for neuroAIDS research. The deliberations of this meeting are outlined in this brief report. Several critical research areas in neuroAIDS were identified as areas of emphasis. Opportunities for collaborations between large NIH-funded projects were also discussed. NeuroAIDS Research Participants. Cristian Achim, University of California, San Diego, San Diego, CA; Sunil Ahuja, University of Texas Health Science Center at San Antonio, San Antonio, TX; James Becker, University of Pittsburgh Medical School, Pittsburgh, PA; Bruce Brew, University of New South Wales, Sydney, Australia; Janice Clements, Johns Hopkins University, Baltimore, MD; Ronald Ellis, University of California, San Diego, San Diego, CA; Leon Epstein, Northwestern University Feinberg School of Medicine, Chicago, IL; Lynda Erinoff, National Institute on Drug Abuse, National Institutes of Health, Bethesda, MD; Dana Gabuzda, Dana Farber Cancer Institute, Harvard Medical School Boston, MA; Harris Gelbard, University of Rochester Medical Center School of Medicine, Rochester, NY; Benjamin Gelman, University of Texas Galveston, TX; David Goldstein, Duke University, Durham, NC; Colin Hall, University of North Carolina, Chapel Hill, NC; Rohan Hazra, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD; Robert Heaton, University of California, San Diego, San Diego, CA; Robin Huebner, Division of AIDS, National Institute of Allergy and Infectious Diseases, National Institute of Health, Bethesda, MD; Kamel Khalili, Temple University, Philadelphia, PA; Dennis Kolson, University of Pennsylvania, Philadelphia PA; Diane Lawrence, National Institute on Drug Abuse, National Institutes of Health, Bethesda, MD; Scott Letendre, University of California, San Diego, San Diego, CA; Thomas Marcotte, University of California, San Diego, San Diego, CA; Michael McGrath, University of California, San Francisco, San Francisco, CA; Susan Morgello, Mount Sinai Medical Center, New York, NY; Avindra Nath, Johns Hopkins University, Baltimore, MD; Vinayaka Prasad, Albert Einstein School of Medicine, Bronx, NY; Richard Price, University of California, San Francisco, San Francisco, CA; Lynn Pulliam, University of California, San Francisco, San Francisco, CA; Dianne Rausch, HIV Pathogenesis, Neuropsychiatry and Treatment Branch, Center for Mental Health Research on AIDS, National Institute of Mental Health, National Institutes of Health Bethesda, MD; Kevin Robertson, University of North Carolina at Chapel Hill, Chapel Hill, NC; Ned Sacktor, The Johns Hopkins University, Baltimore, MD; Gerald Sharp Division of AIDS, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD; Elyse Singer, University of California, Los Angeles, Los Angeles, CA; Stephen Spector, University of California, San Diego, LaJolla, CA; Beth Stevens, Harvard Medical School, Children’s Hospital, Kirby Neurobiology Center, Boston, MA; Mario Stevenson, University of Massachusetts Medical Center, Worcester, MA; Ellen Stover, National Institute of Mental Health, National Institutes of Health, Bethesda, MD; Ronald Swanstrom, University of North Carolina at Chapel Hill-Chapel Hill, NC; Victor Valcour, University of California, San Francisco, San Francisco, CA; David Volsky, Columbia University Medical Center, New York, NY; Brian Wigdahl, Drexel University College of Medicine, Philadelphia, PA; May Wong, National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD; Constantin Yiannoutsos, Indiana University, Indianapolis, IN; Christine Zink, The Johns Hopkins University, Baltimore, MD     

［~3H］二氢埃托啡在大鼠脑分布的定量放射自显影

本文用体外定量受体放射自显影分析法观察了［３Ｈ］二氢埃托啡（ＤＨＥ）在大鼠脑中定位分布和结合特点。结果表明，［３Ｈ］ＤＨＥ特异结合较高的部位主要为纹状体，伏隔核，大脑皮质Ⅰ层和Ⅲ层，丘脑，缰核，杏仁核。脚间核和蓝斑，ＤＨＥ主要作用于ｕ－阿片受体．     

Some phytochemical, pharmacological and toxicological properties of ginger (Zingiber officinale Roscoe): a review of recent research.

Ginger (Zingiber officinale Roscoe, Zingiberacae) is a medicinal plant that has been widely used in Chinese, Ayurvedic and Tibb-Unani herbal medicines all over the world, since antiquity, for a wide array of unrelated ailments that include arthritis, rheumatism, sprains, muscular aches, pains, sore throats, cramps, constipation, indigestion, vomiting, hypertension, dementia, fever, infectious diseases and helminthiasis. Currently, there is a renewed interest in ginger, and several scientific investigations aimed at isolation and identification of active constituents of ginger, scientific verification of its pharmacological actions and of its constituents, and verification of the basis of the use of ginger in some of several diseases and conditions. This article aims at reviewing the most salient recent reports on these investigations. The main pharmacological actions of ginger and compounds isolated therefrom include immuno-modulatory, anti-tumorigenic, anti-inflammatory, anti-apoptotic, anti-hyperglycemic, anti-lipidemic and anti-emetic actions. Ginger is a strong anti-oxidant substance and may either mitigate or prevent generation of free radicals. It is considered a safe herbal medicine with only few and insignificant adverse/side effects. More studies are required in animals and humans on the kinetics of ginger and its constituents and on the effects of their consumption over a long period of time.     

Effects of methylphenidate on multiple components of attention in children with attention deficit hyperactivity disorder

Rationale Methylphenidate (MPH) has been shown to be effective in the treatment of attention deficits in children with attention deficit hyperactivity disorder (ADHD). Although a variety of studies have been performed, there is little available information as to which components of attentional functioning are disturbed in ADHD.Objectives The aim of the present study was to monitor the effect of MPH on various measures of attention in children with ADHD.Methods In a double-blind, placebo-controlled, crossover study, the attentional functioning of 58 children diagnosed with ADHD without psychiatric comorbidity was examined. Assessment of attention was performed on their usual MPH treatment and following withdrawal of the drug. Furthermore, the attentional performance of 58 healthy children was assessed. The test battery consisted of reaction time tasks, including measures of alertness, vigilance, divided attention, flexibility, and aspects of selective attention such as focused attention, inhibition, and integration of sensory information.Results In comparison to the test performance of healthy children, children with ADHD displayed impairments of vigilance, divided attention, flexibility, and aspects of selective attention including focused attention, inhibition, and integration of sensory information. Statistical comparison of attentional functioning of children with ADHD on and off MPH treatment revealed that the medication resulted in an improved task accuracy regarding vigilance, divided attention, inhibition, focused attention, integration of sensory information, and flexibility. Conclusion The present findings indicate that various aspects of attention are markedly impaired in children with ADHD. Treatment with MPH was accompanied by improvements in attention functions of small to moderate sizes. Although MPH-induced improvements were observed in a broad range of attention measures, children with ADHD who were on MPH treatment nevertheless displayed serious deficits in a number of components of attention.     

Cell wall active antifungal agents

The recent American approval of Cancidas^?, a semi-synthetic echinocandin, for salvage treatment of aspergillosis has demonstrated that the cell wall is a clinically viable target for treating fungal infections. Recently, a variety of new, sulfated members of the echinocandin lipopeptide family have been reported, which, like other echinocandins, are glucan synthesis inhibitors. In addition, two new classes of lipopeptide glucan synthesis inhibitors, the aerothricin lipopeptidolactones and the Sankyo lipopeptides, have been identified, as well as a novel member of the papulacandin family of liposaccharide glucan synthesis inhibitors. The first new structural class of glucan synthesis inhibitors discovered in over 20 years, the so-called sterol glycosides, is reviewed. Five different structural types within this class have been characterised. Finally, several novel compounds with cell wall antifungal activity based on inhibition of chitin synthase are reviewed.     

抗心律失常药物对蟾酥致小鼠心律失常的影响

比较苯妥英钠、利多卡因(钠通道阻滞药)、普萘洛尔(β肾上腺素受体拮抗药)、胺碘酮(延长动作电位时程药)和维拉帕米(钙通道阻滞药)对蟾酥诱导小鼠心律失常的抑制作用及对离体小鼠心脏的蟾酥致死量的影响。采用动态心电图记录蟾酥诱导小鼠心律失常。观察模型组和各给药组心电图的P-R间期、QRS时程、Q-T间期、T波幅度和HR的变化,统计各心律失常发生率、存活率及心律失常评分。采用离体小鼠心脏灌流,记录心脏的蟾酥致死量。与模型组相比,苯妥英钠组的QRS时程缩短且心率减慢;室性心律失常的发生率降低,存活率增高;显著增加离体小鼠心脏的蟾酥累积致死量。利多卡因组与模型组相比,P-R间期和QRS时程缩短;室性心律失常发生率降低;显著增加离体小鼠心脏的蟾酥累积致死量。普萘洛尔组与模型组相比,P-R间期、QRS时程和Q-T间期缩短;室上性及室性心律失常的发生率降低。胺碘酮显著减慢模型小鼠的心率并且降低模型小鼠室性心律失常的发生率。维拉帕米显著延长模型小鼠P-R间期,抑制Q-T间期延长;减少室上性及室性心律失常的发生;显著减少离体小鼠心脏的蟾酥累积致死量。整体动物实验中,苯妥英钠对蟾酥诱导小鼠的心律失常最有效,其次是利多卡因和普萘洛尔,...     

Endocrine disruption mechanism of o,p'-DDT in mature male tilapia (Oreochromis niloticus)

The aim of the present study was to evaluate, in vivo, the potential of o,p'-DDT to disrupt the endocrine system of mature male tilapia. In particular, the possibility that o,p'-DDT effects were mediated directly via the estrogen receptor (ER). Compounds with known ability to bind to the ER were employed: estradiol to induce and tamoxifen to inhibit the estrogenic effects result of the activation of the ER. In addition, an aromatase inhibitor, 4-hydrxyandrostenedione (4-OHA), was used to assess the ability of o,p'-DDT to induce estrogenic effects in a surrounding of low estradiol concentration. The effects of estradiol and o,p'-DDT were studied alone or in the presence of tamoxifen or 4-OHA at the end of a 12-day period of exposure. The main endpoints measured were plasma alkaline-labile phosphorous (ALP; an indirect indicator of vitellogenin), estradiol, testosterone and o,p'-DDT. It was found that o,p'-DDT was able to induce the vitellogenesis (measured as plasma ALP increase) and decrease the circulating levels of estradiol and testosterone. Interestingly, o,p'-DDT kept this ability in whole fish with low concentrations of estradiol which would exclude endogenous estradiol as indirect mediator of the estrogenic effects induced by o,p'-DDT. In addition, the plasma concentration of o,p'-DDT, instead of that of estradiol, was closely related to the plasma ALP increase induced by o,p'-DDT. This indicates that o,p'-DDT could have directly activated the vitellogenesis. The antiestrogenic action of tamoxifen to inhibit the vitellogenesis and the decrease on plasma estradiol induced by o,p'-DDT indicates that o,p'-DDT can bind directly to the ER. In conclusion, this in vivo study shows that o,p'-DDT has the potential to disrupt the endocrine system and strongly supports that the estrogenic actions of o,p'-DDT involve binding to the ER.