藤黄炮制的研究进展

藤黄为藤黄科植和藤黄的干燥树脂,生藤黄有毒,常须通过炮制,减低毒性。本文对藤黄炮制的研究做了概述。1 炮制工艺研究 王爱芳提出了藤黄的四种炮制工艺:(1)清水制法;(2)荷叶制法;(3)豆腐制法;(4)山羊血制法。以抗炎、杀菌、抗肿瘤和藤黄酸含量为指标,采用正交试验法,综合优选了藤黄高压蒸制工艺。结果表明,以126C蒸制0.5小时为最佳工艺,与上述炮制品比较,具有药理效应强,有效成分含量高及毒性低的特点。     

盐酸雷尼替丁胶囊不稳定的原因分析

笔者对同一批号,不同的包装材料,配方以及放置时间的雷尼替丁胶囊进行多次外观观察及含量测定,发现不同包装材料以及不同配方制法和成品放置长短它的颜色变化不同其含量也不同.经分析研究其不稳定的主要原因有包装材料,配方辅料,制法等有十分重要的关系.     

银杏叶滴丸的制备与含量测定研究

本文介绍银杏叶滴丸的滴制法和紫外分光光度法测定滴丸制剂中总黄酮的含量。     

生物制品品种编写格式样稿破伤风免疫球蛋白

一、名称:包括中文名称、英文名称;二、定义:包括命名、有效成分、形态、用途;三、制法:简要叙述制法和质控要领(种子及种子代次、关键步骤、关键条件、有效成分及其他成分的含量),字数控制在200字左右     

淡豆豉不同制法其成品性状及异黄酮类化学成分含量的比较

目的:比较古法炮制与现今药典制法的淡豆豉其成品性状及异黄酮类化学成分的含量。方法:采用紫外-可见分光光度法对淡豆豉提取物中的总异黄酮进行含量测定;采用高效液相色谱法对淡豆豉提取物中异黄酮游离苷元(大豆素、染料木素)的含量进行测定。色谱柱为Prevail-C18(250 mm×10.0 mm,5μm),流动相为乙腈-水-乙酸(35∶64∶1,V/V/V),检测波长为260 nm,流速为1.0 ml/min,柱温为25℃,进样量为15μl。结果:古法炮制的淡豆豉气香,质地柔软,断面为棕褐色,表皮皱缩,总异黄酮含量为4.140 mg/g,大豆素含量为1.263 0 mg/g,染料木素含量为1.254 mg/g;现今药典制法的淡豆豉气味微弱,质地稍硬,断面为棕黄色,表皮皱缩,总异黄酮含量为3.530 mg/g,大豆素含量为0.349 mg/g,染料木素含量为0.335 mg/g。结论:古法炮制淡豆豉与现今药典制法淡豆豉相比,前者成品性状好、大豆异黄酮类含量高,古法炮制有明显优势。     

不同炮制方法对知母主要化学成分的影响

知母为百合科植物知母（Anemarrhe asphodeloides Bge）干燥根茎，具有清热泻火、生津润燥的功效，临床用于外感热病，高热烦渴，肺热燥咳，骨蒸潮热，内热消渴，肠燥便秘等症。知母含有皂苷、黄酮及木脂素等多种成分，目前其主要炮制方法有盐制法、炒制法、麸制法、酒制法、盐麸制法等。为探讨加工、炮制对知母主要化学成分的影响，笔者考察了不同炮制品的化学成分含量，从而使得知母药材炮制的合理性，科学指导临床用药。     

氯乙油制法改进

氯乙油常用于治疗老年性阴道炎等疾患,原制法为:将氯霉素、乙菧酚,醋酸洗必泰溶于适量丙二醇中,然后与鱼肝油混合即得。该制剂极易分层,主药含量不匀,经实验,现制得乳浊剂剂型。临床应用效果良好,现将改进后的制法简介如下。     

中药炮制减毒方法和机理的探讨

中药炮制减毒的常用方法有净制法、水处理法、炒法、复制法、水火共制法、去油制霜法、水飞法、煅法、培法、提净法等，其原理在于去除毒性成分、改变毒性成分结构、降低毒性成分含量等。通过对炮制减毒方法和机理的探讨，有利于促进中药炮制的规范化和现代化。确保临床用药的安全有效。     

国家食品药品监督管理局国家药品标准(修订)颁布件(ZGB2009-4-11)

经审查,同意对活络油国家药品标准进行修订。修订内容:修订性状、含量限度、贮藏条件,制法中明确加入色素种类及用量。     

《中华人民共和国卫生部药品质量标准》(维吾尔药分册)制剂质量标准的完善与提高

目的　提高《中华人民共和国卫生部药品质量标准》(维吾尔药分册)维药制剂质量标准。方法　从维药制剂的处方与制法,处方中药味的排列顺序,制法项,鉴别项,含量测定项,其他各项指标等方面论述该质量标准需要提高的方面。结果与结论　根据国家食品药品监督管理局关于提高国家药品标准的行动计划,《中华人民共和国卫生部药品质量标准》(维吾尔药分册)维药制剂质量标准必须提高。     

Regeneration of injured airway epithelium

The airway surface epithelium is frequently injured by microorganisms and viruses due to its permanent contact with the external medium. Following injury, the epithelium is able to repair itself and regenerate through several mechanisms including spreading and migration of basal cells, cell proliferation and differentiation. The cellular and molecular factors involved in wound repair and epithelial regeneration interact closely, implying the participation of cytoskeleton proteins and integrins receptors, matrix metalloproteinases and their inhibitors as well as cytokines and growth factors secreted by airway epithelial and mesenchymal cells. The spatio-temporal modulation of the pro-inflammatory cytokines such as IL-8, and MMPs (MMP-9 and -7) during the different steps of regeneration suggests that the matrix and secretory environment are markedly involved in these mechanisms and that their dysregulation may induce remodeling of the airway mucosa. A better knowledge of the mechanisms involved in airway epithelium regeneration may pave the way to regenerative therapeutics allowing the reconstitution of a functional airway mucosa in numerous respiratory diseases such as cystic fibrosis, chronic obstructive pulmonary diseases and bronchiolitis.     

Multigeneration assessment of nonylphenol and endosulfan using a model Australian freshwater fish, Melanotaenia fluviatilis

Changes over two generations in offspring and reproductive ability were recorded in crimson-spotted rainbowfish (Melanotaenia fluviatilis), a model Australasian freshwater fish, following a 24 h exposure to nominal nonylphenol concentrations of 50, 100, 500, 1000, 2250, and 5000 microg/L and following a 4 h exposure to nominal endosulfan concentrations of 1.0, 5.0, 10, 22, 33, and 50 microg/L. There were also four replicated control treatments: control 1 and 2 and solvent control 1 and 2, as well as "positive" female and male controls: 1 microg/L estradiol 1 and 2 and 1 microg/L testosterone 1 and 2. Results suggested that there may be some parental transfer of toxicants to embryos even over this short exposure period. Fertility of M. fluviatilis was reduced by a 24 h pulse exposure of adults to 100 microg/L nonylphenol and a 4 h exposure to 1.0 microg/L endosulfan. Hatch rates were significantly reduced after exposure to nonylphenol, endosulfan, and estradiol control but not in solvent controls and testosterone control. Significant correlations were found between reproductive and physiological parameters for nonylphenol and endosulfan exposed F0 adult rainbowfish. The major reproductive effects were on hatchability of the F1 generation and the gonadosomatic indices of male F1. The respective nominal NOEC and LOEC's for nonylphenol were 50 and 100 microg/L, and for endosulfan were <1.0 and 1 microg/L. These observed effects have the potential to significantly impact exposed rainbowfish populations through the observed approximately 45% reduction of hatchability and thus larval production.     

舒芬太尼复合咪达唑仑在乳腺癌手术麻醉苏醒中的应用

目的研究舒芬太尼+咪达唑仑在乳腺癌手术麻醉复苏中的应用,术后麻醉苏醒情况及拔管时血流动力学变化。方法选取ASAⅠ级,临床诊断为乳腺癌,拟行乳腺癌改良根治术患者60例,随机分为三组,每组20例,三组均采用气管内插管全身麻醉方式,以维库溴铵诱导插管,1组(F)以芬太尼+异丙酚+咪达唑仑维持麻醉,2组(S)以舒芬太尼+丙泊酚+咪达唑仑维持麻醉,3组(T)以舒芬太尼+丙泊酚+咪达唑仑维持麻醉,于术毕前10min停止丙泊酚输注,追加舒芬太尼+咪达唑仑,观察记录手术结束,取吸痰时,拔管时及拔管后MAP,HR,与基础值进行比较,记录呼患者睁眼时间,拔除气管导管时间和OAA/S评分。结果与术毕时比,F组和S组的MAP和HR在吸痰、拔管时均明显增高(P<0.05)。在睁眼时间、拔管时间两项观察指标中,各组之间差异有统计学意义,T组患者睁眼时间及拔管时间最短,S组次之,F组最慢,OAA/S评分T组评分较F组和S组明显升高(P<0.05)。结论舒芬太尼联合咪达唑仑用于乳腺癌手术患者,能保证很好的麻醉深度,术毕前10min追加舒芬太尼+咪达唑仑,拔管时心血管反应轻,术毕苏醒时间快,清醒状况良好,值得临床推广。     

Caspofungin: pharmacology,safety and therapeutic potential in superficial and invasive fungal infections

Invasive fungal infections are important causes of morbidity and mortality in hospitalised patients. Current therapy with amphotericin B and antifungal triazoles has overlapping targets and is limited by toxicity and resistance. The echinocandin lipopeptide caspofungin is the first of a new class of antifungal compounds that inhibit the synthesis of 1,3-β-D-glucan. This homopolysaccharide is a major component of the cell wall of many pathogenic fungi and yet is absent in mammalian cells. It provides osmotic stability and is important for cell growth and cell division. In vitro, caspofungin has broad-spectrum antifungal activity against Candida and Aspergillus spp. without cross-resistance to existing agents. The compound exerts prolonged post-antifungal effects and fungicidal activity against Candida spp. and causes severe damage of Aspergillus fumigatus at the sites of hyphal growth. Animal models have demonstrated efficacy against disseminated candidiasis and disseminated and pulmonary aspergillosis, both in normal and in immunocompromised animals. Caspofungin possesses favourable pharmacokinetic properties and is not metabolised through the cytochrome P450 (CYP) enzyme system. It showed highly promising antifungal efficacy in Phase II and III clinical trials in immunocompromised patients with oesophageal candidiasis. Caspofungin was effective in patients with invasive aspergillosis intolerant or refractory to standard therapies. Based on its documented antifungal efficacy and an excellent safety profile, caspofungin has been approved recently by the US Food and Drug Administration for the treatment of invasive aspergillosis in patients who are refractory to or intolerant of other therapies (i.e., amphotericin B, lipid formulations of amphotericin B, and/or itraconazole). Phase III clinical trials in patients with candidaemia and in persistently febrile neutropenic patients requiring empirical antifungal therapy are ongoing. This paper reviews the preclinical and clinical pharmacology of caspofungin and its potential role for treatment of invasive and superficial fungal infections in patients.     

Strain and sex alter effects of stress and nicotine on feeding, body weight, and HPA axis hormones

Gender and genotype result in differential sensitivity to stress and to nicotine. Male and female Sprague–Dawley and Long–Evans rats exhibit different behavioral responses to immobilization stress and to chronically-administered nicotine, suggesting that these animals may be useful to model human variability in stress and nicotine sensitivity. It is possible that differences in sensitivity of the hypothalamo–pituitary–adrenocortical (HPA) axis might account for these sex and strain differences. This experiment examined corticosterone (CORT) and adrenocorticotropin hormone (ACTH) responses of male and female Sprague–Dawley (n=117) and Long–Evans (n=120) rats administered 0, 6, or 12 mg/kg/day nicotine for 14 days; half of each treatment group was exposed to immobilization stress (20 min/day). Feeding and body weight also were measured. Nicotine increased CORT and ACTH levels of Sprague–Dawley females only. Stress increased CORT and ACTH levels of all groups except for Long–Evans females. Nicotine and stress decreased feeding and body weight with greatest effects in Long–Evans females. CORT, feeding, and body weight were positively correlated among stressed females. These findings suggest that strain differences in HPA axis, body weight, and feeding responses to nicotine and to stress are robust among females but not among males. CORT reactivity and female sex hormones may explain these differences.     

Drugs for insomnia

Introduction: Sleep is a vital neurochemical process involving sleep-promoting and arousal centers in the brain. Insomnia is a pervasive disorder characterized by difficulties in initiating or maintaining or non-refreshing (poor quality) sleep and clinically significant daytime distress. Insomnia is more prevalent in women and old age and puts sufferers at significant physical and mental health risks. This review summarizes published data on the current and emerging insomnia drug classes, rationale for development and associated risks/benefits. (Summary of Product Characteristics and Medline search on "hypnotic" or specific drug names and "Insomnia").

Areas covered: GABA_A receptor modulators facilitate sleep onset and some improve maintenance but increase risk of dependence, memory, cognitive and psychomotor impairments, falls, accidents and mortality. Melatonin receptor agonists improve quality of sleep and/or sleep onset but response may develop over several days. They have more benign safety profiles and are indicated for milder insomnia, longer usage and (prolonged release melatonin) older patients. Histamine H-1 receptor antagonists improve sleep maintenance but their effects on cognition, memory and falls remain to be demonstrated. Late-stage pipeline orexin OX1/OX2 and serotonin 5HT2A receptor antagonists may hold the potential to address several unmet needs in insomnia pharmacotherapy but safety issues cast some doubts over their future.

Expert opinion: Current and new insomnia drugs in the pipeline target different sleep regulating mechanisms and symptoms and have different tolerability profiles. Drug selection would ideally be based on improvement in the quality of patients' sleep, overall quality of life and functional status weighed against risk to the individual and public health.     

Some observations on the effects of bioprocessing on biopolymer stability

A short review is given of some of the effects of the stresses encountered during bioprocessing of protein and carbohydrate-based macromolecular systems. This is of relevance to the effectiveness and safety of protein or peptide drugs themselves (such as insulin and monoclonal antibodies) and for the integrity of delivery systems (such as various carbohydrate-based hydrogel or mucoadhesive polymers). Some carbohydrate polymers are themselves bioactive or immunostimulatory and particular use is being made of polysaccharide and glycoconjugate vaccines whose effectiveness can be severely effected by chain degradation. Stability criteria include molecular weight and conformation and techniques ranging from simple viscomery measurements to sophisticated analytical ultracentrifuge and multi-angle light scattering coupled to size exclusion chromatography and precision viscometry measurements have been useful in this regard. We focus on some recent work on the degradation and aggregation of immunoglobulin G4-based monoclonal antibodies in response to repeated freezing and thawing and long-term storage, looking at the possible connection between conformation change and aggregation, the effects of storage conditions on the stability of chitosan mucoadhesive systems used for nasal and oral delivery. We look at the effects of sterilization conditions (thermal and irradiation) on the stability of a variety of other polysaccharides such as starches, κ-carrageenan, carboxymethylcellulose, alginate, low- and high-methoxy pectins, guar, and xyloglucans and consider the use of a relatively new method for the evaluation of the molecular weight distribution of glycoconjugate vaccines with molecular weights as high as 100?×?10⁶ g/mol.     

Tannins medical / pharmacological and related applications: A critical review

Tannins are natural phenolic compounds that are widespread and almost ubiquitous in the vegetal world. They can be found in fruit, wood and bark of trees, and many types of wild herbs and plants or from sustainable agriculture and forestry. Their traditional use for leather has been doubled for centuries in the popular medical and pharmacological lore by their use to cure or alleviate a variety of infections and diseases. This has indicated to modern researchers that these materials possess a great potential for the use in modern medicine and pharmacy. This review, after an introduction on tannins their structures and their basic chemistry describe what modern researchers have been able to glean and demonstrate of their real, identified and quantified effects on various diseases, from their bactericidal, anticancer and antinflammatory actions to the many other effects that putsnow in more close focus in pharmacology.     

甲基黄酮醇胺盐对大鼠学习记忆的促进作用与其抗氧化作用的关系

目的研究甲基黄酮醇胺盐对大鼠学习记忆的影响，分析该药影响学习记忆与其影响脑内自由基反应的关系。方法ｉｐ甲基黄酮醇胺盐５，１０ｍｇ·ｋｇ－１共７ｄ后，采用Ｍｏｒ－ｒｉｓ水迷宫测试大鼠的学习记忆能力，同时测定训练ｄ５和休息３０ｄ后大鼠脑内过氧化脂质（ＬＰＯ）含量和超氧化歧化酶（ＳＯＤ）活性。结果甲基黄酮醇胺盐两种剂量均可提高大鼠获取空间定位信息能力和信息贮存能力并增强记忆保持和再现过程。用药大鼠脑内ＬＰＯ含量明显低于对照组，与其记忆成绩呈正相关性。而脑内ＳＯＤ活性则高于对照组，与其记忆成绩呈负相关性。结论甲基黄酮醇胺盐对大鼠的学习记忆机能具有促进作用，而它的抗氧化作用可能为其促进学习记忆的作用机制。     

脂蟾毒配基PLGA-TPGS纳米粒的质量评价

目的：以自制材料乙交酯丙交酯共聚物-维生素E聚乙二醇1000琥珀酸酯（polylactide-co-glycolide-D-α-tocopheryl polyethylene glycol 1000 succinate,PLGA-TPGS）为载体制备脂蟾毒配基PLGA-TPGS纳米粒（Resibufogenin-loaded PLGA-TPGS nanoparticles,RPTN）,并以市售材料乙交酯丙交酯共聚物（PLGA）为载体制备脂蟾毒配基PLGA纳米粒（RBG-loaded PLGA nanoparticles,RPN）,体外评价和比较2种纳米粒的质量。方法：采用超声乳化-溶剂挥发法制备RPTN和RPN,用透射电子显微镜和激光粒度仪分别测定二者的外观、粒径、表面电荷。采用反相高效液相色谱法,色谱柱为Hypersil C₁₈（4.6 mm×250 mm,5 μm）,甲醇和0.05%冰醋酸溶液（9∶1）为流动相,检测波长为298 nm,测定RBG在RPTN和RPN中的载药量、包封率和体外释放度。结果：RPTN和RPN的粒径分别为152.3 nm和331.7 nm,载药量和包封率分别为18.4%、79.3%和15.1%、68.6%。体外药物释放30 d时RPTN和RPN的体外累积释放率分别为86.7%和72.3%,RPTN释放较完全。结论：自制载体制备的RPTN比RPN粒径更小,载药量和包封率更大,体外有明显的缓释作用,释放更完全。