穿琥宁氯化钠注射液的工艺研究

目的：为提高穿琥宁氯化钠注射液的质量，优选穿琥宁氯化钠注射液的最佳处方和制备工艺。方法：采用氯化钠调节等渗、磷酸盐缓冲液对调节pH值、活性炭吸附热原、筛选合适的抗氧剂等手段优化穿琥宁氯化钠注射液的制备工艺，采用高效液相色谱法测定穿琥宁氯化钠注射液的含量。结果：每100m1注射液中含0．193gNa2HP0a和0．131gNaH2PO4时注射液最稳定；抗氧剂为0．1％L-半胱氨酸盐酸盐；45℃为主药的溶解温度；浓配液先加热煮沸15min，再稀配、灭菌，注射液澄明度达到要求；整个制备过程通高纯度N2以隔离空气中的O2。结论：优选的处方和制备工艺，可提高穿琥宁氯化钠注射液的质量。     

紫草油制备工艺的改进

目的 改进提取工艺,提高了有效成份的提取率,减少对配制环境的污染,增加药品质量的稳定性.方法 乙醇回流提取代替传统的油炸法,并用高效液相色谱法测定左旋紫草素含量,以左旋紫草素含量为标准,对传统提取方法和改进工艺法进行比较.结果 采用了改进的制备工艺,有效成份的提取率显著提高,提高了产品质量.结论 新制备工艺用7倍量95%乙醇回流提取1h,有效成份提取率可达97%,传统油炸工艺有效成份提取率只有60%左右;且新工艺解决了传统油炸工艺产生的油烟给空气净化系统带来的伤害.     

L—天门冬酰胺酶的提取和纯化工艺改进

目的：改进L－天门冬酰胺酶的提纯工艺，使成品达到中国药典型标准。方法：在工艺流程中改溶菌酶破裂，蔗糖提取为丙酮破裂，稀盐提取，并增加了亲和层析的工序。结果：提取的L－天门冬酰胺酶活力提高到250IU／mg，纯度达到98％以上，产率达到40％，结论：本工艺优于吴氏工艺，成品达到中国药典标准。     

结肠靶向定位滴丸克癌素的提取工艺研究

目的 建立结肠靶向滴丸克癌素的提取工艺方法。方法 采用碱溶酸沉法从槐米中提取芦丁,再进行酸水解得到槲皮素;采用传统乙醇回流法从姜黄中提取总姜黄素,以姜黄中的总姜黄素含量为指标,通过正交表分析确定最佳提取工艺。结果 槲皮素的提取条件为：碱性pH 8~9,酸性pH 3~5条件下提取芦丁;得到精制芦丁加100倍量的2%硫酸酸水解90 min。姜黄的最佳提取工艺为：85%乙醇回流提取3次,每次1 h;得浸膏上硅胶柱收集氯仿洗脱部分得总姜黄素。结论 该工艺可行,可为结肠靶向滴丸克癌素的生产提供参考。     

肌氨肽苷注射液提取工艺研究

目的 研究肌氨肽苷注射液提取工艺，以提高产品收率，确保产品质量稳定。方法 采用正交设计试验，用福林酚法、高效液相色谱法检测提取物中多肽和次黄嘌呤含量，并对制剂产品质量进行考察。结果 选用胃蛋白酶和木瓜蛋白酶进行水解，增加pH值3.0和10.5两步煮沸和低温沉淀，所得提取产物收率高、质量稳定。结论 按照筛选出的生产工艺进行提取，可提高收率，产品质量稳定，工艺合理。     

红果樫木树皮中罗希吐碱的纯化方法

建立红果樫木树皮中罗希吐碱的提取工艺。利用L9（3^4）正交实验确定罗希吐碱的提取条件，比较5种填料（XAD-2树脂，聚酰胺，葡聚糖凝胶LH-20，ODS和阳离子交换树脂）以及液液萃取技术对红果樫木提取物中罗希吐碱的分离效果。提取条件确定为：药材用70％乙醇（v／m=60）超声提取60分钟；提取物溶解于酸水溶液（0，5mol／L HCl调pH1），经等体积正丁醇萃取除去杂质；25％氨水调剩余水溶液pH10，再经等体积正丁醇萃取；正丁醇萃取物溶解于酸水溶液（0．5mol／L HCl调pH1），经阳离子交换树脂色谱分离，水和70％乙醇（pH10，25％氨水调节）为洗脱剂。罗希吐碱存在于70％乙醇洗脱物中，含量可达到53．3％。该工艺为从红果樫木树皮中制备罗希吐碱提取物提供一种简单有效的方法。     

氟他胺灭活排污方法研究

目的：本对氟他胺生产过程废水中氟他胺灭活进行研究。方法：针对氟他胺具酰胺结构的情况，用75%乙醇、纯化水为溶剂，加入不同碱量静放4h、100℃回流1h，3h后用高效液相色谱法测定残留含量。结果：实验表明，以水为溶剂，加入与氟他胺等重量的氢氧化钠，在100℃温度下回流3h后，氟他胺活性彻底被消除。     

雀梅藤中大麦芽碱含量测定方法学考察

摘要：目的:建立雀梅藤中大麦芽碱含量测定方法学且优化其提取工艺。方法:HPLC法,色谱柱为JADE-PAK?KM-C18（250 mm×4.6 mm, 5μm）,流动相为甲醇-0.02 mol·ml-1磷酸二氢钾（10%磷酸调节pH至2）（10∶90）,流速为1.0 ml·min-1,检测波长为220 nm,柱温为30℃,进样量为10μl。采用正交试验L9（3~4）对溶媒、溶剂量、氨水量及提取时间等因素进行考察,以大麦芽碱含量作为评价指标,优化其提取工艺并进行验证。结果:大麦芽碱在0.025 0～0.950 0 mg·ml-1浓度范围内线性良好（r=0.999 7）,精密度、重复性较好（RSD<2%）,平均回收率为100.8%（RSD=1.96%,n=6）。优化后雀梅藤大麦芽碱最佳提取工艺为100 ml氯仿、1.5 ml氨水、提取15 min,验证试验表明大麦芽碱的平均含量为1.172 9 mg·g-1（RSD=0.79%,n=3）。结论:所优化的提取工艺稳定可靠,所建方法学简便、准确、高效,可用于雀梅藤的质量控制。     

正交设计法优选金果榄提取工艺

目的：优选金果榄的最佳提取工艺。方法：以盐酸药根碱与盐酸巴马汀含量和浸膏率为评价指标，采用高效液相色谱法测定含量，采用正交试验考察乙醇浓度、乙醇用量、回流时间、回流次数对提取效果的影响。结果：金果榄的最佳提取工艺为6倍量的95%乙醇回流3次，每次0．5h。结论：该提取工艺设计合理。结果可靠。为提取金果榄提供理论基础。     

减肥食品或保健品中非法添加盐酸西布曲明、盐酸芬氟拉明、酚酞的快速检测方法研究

目的：建立减肥食品或保健品中同时检测盐酸西布曲明、盐酸芬氟拉明、酚酞的薄层色谱方法。方法：样品经甲醇提取后，采用硅胶G薄层板，以甲苯-乙酸乙酯-异丙醇-浓氨试液（12：6：3：0．5）为展开剂，4％氢氧化钠溶液及稀碘化铋钾为显色剂。结果：在选定的色谱条件下，盐酸西布曲明、盐酸芬氟拉明、酚酞3种组分能得到较好的分离。结论：本法快速、简便、专属性强，可作为同时检测盐酸西布曲明、盐酸芬氟拉明、酚酞的快速检测方法。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Glycofection: The Ubiquitous Roles of Sugar Bound on Glycoplexes

Glycofection (transfection by using sugar-substituted polylysine) was assessed in order to provide an alternative to viral vectors for the transfer of genes into vascular smooth muscle cells. A rabbit vascular smooth muscle cell line (Rb-1 cells) was selectively transfected by using glycoplexes (glycosylated polylysine/pSV2LUC complexes) in the presence of 10 mu M of the fusogenic peptide GALA. A sugar-specific transfection was obtained when the glycofection was conducted for 1 h with glycoplexes containing either alpha Gal, alpha -Glc, alpha -GalNAc, beta -GlcNAc, or beta -GalNAc residues. The gene expression was high after transfection, with glycoplexes bearing alpha Gal, alpha -GalNAc, or beta -GalNAc residues that were weakly internalized, and low with glycoplexes carrying Lact or Rha residues that were well taken up by cells. These results suggest that 1) glycofection can be a good approach for a selective transfer of genes intovascular smooth muscle cells, 2) an efficient uptake of the glycoplexes is not the unique limiting step for an efficient transfection, and 3) the sugar-dependent trafficking of the glycoplexes inside the cells may account for the transfection efficiency.     

直肠癌下切缘病理组织学分析

目的探讨直肠癌逆向浸润与下切缘的安全距离的关系。方法对36例直肠癌Miles手术和Dixon手术后标本的肿瘤下缘1.0cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查,观察直肠癌逆向浸润或转移的距离。结果36例直肠癌标本距癌肿下缘1.0 cm、2.0cm、3.0cm的肠壁及对应的系膜病理组织学检查均为阴性,结论直肠癌远恻逆向浸润或转移未见超过1.0cm,因此认为保肛手术时切除肿瘤远侧肠管(包括系膜)2.0cm是安全的。