氧化锌胶浆的制备及临床应用

目的：探索溃疡的治疗方法。研究氧化锌胶浆剂的处方,制备工艺及质量控制。方法：采用CMC-Na为基质制成胶浆剂,用络合滴定法测定氧化锌（ZnO）含量。结果：平均回收率99.08%,RSD=0.17%,方法专一灵敏,稳定性好,临床疗效良好。结论：该制剂适合于临床应用。     

美洛昔康凝胶剂的制备与质量控制

目的：制备关洛昔康凝胶剂，并建立其质量控制方法。方法：拟定处方组成及制备工艺；采用紫外分光光度法测定关洛昔康含量。结果：美洛昔康的线性范围为2．4—19．2μg·ml^-1；平均回收率为100．1％；RSD为0．3％（n=5）。结论：该凝胶剂制备工艺简单，含量测定方法准确可靠，重复性好，可用于该制剂的质量控制。     

聚维酮碘壳聚糖凝胶剂的制备

目的研制聚维酮碘壳聚糖凝胶剂。方法拟订聚维酮碘壳聚糖凝胶剂处方组成及制备工艺，采用电位滴定法测定聚维酮碘含量。结果该制剂pH值为3．5～4．5，聚维酮碘平均回收率为100．17％，RSD为0．68％（n=5）。结论凝胶质量稳定，制备工艺可行，含量测定方法简便、快速、准确。     

盐酸利多卡因胶浆的处方改进及其质量控制

目的：研制一种既有局部麻醉、润滑作用，又能消除消化道泡沫的内窥镜检查用胶浆剂；并能对该制剂进行有效的质量控制。方法：以盐酸利多卡因为局部麻醉剂、二甲硅油为消泡剂、壳聚糖为胶浆基质制备胶浆剂，并对盐酸利多卡因胶浆制定质量控制方法。结果：本制剂对咽喉部麻醉迅速、润滑作用好，消除泡沫作用强，镜检清晰，患者服用方便，不良反应少。结论：本制剂制备工艺简单可行，质量控制方法可靠，临床应用效果满意。     

盐酸丁卡因凝胶剂的研制和质量控制

目的 制备盐酸丁卡因凝胶剂，并建立质量控制标准。方法 以正交试验法筛选基质最佳处方，并建立了酸碱度、含量测定等质量控制标准。结果 含量测定平均回收率为99．86％，RSD为0．36％。结论 制备该凝胶剂工艺简单，质量可控。     

聚维酮碘凝胶的制备与质量控制

目的：制备聚维酮碘凝胶，建立质量控制标准并预测室温贮存期。方法：采用正交试验法筛选最佳基质处方，以卡波姆940为基质制备聚维酮碘凝胶；建立酸碱度、黏度、含量测定和微生物限度质控标准，进行离心试验，耐热耐寒试验；采用经典恒温加热法预测室温贮存期。结果：制备的凝胶剂均匀细腻，pH4．5，黏度32．28Pa·s（n=3），有效碘含量为11．09％（n=3），各温度条件下加热时间与有效碘质量浓度对数变化线性关系良好，25℃时贮存期为740d。结论：该制剂处方合理，制备工艺简单，质量可控。     

巴洛沙星眼用原位凝胶的制备及质量控制

目的：建立巴洛沙星眼用原位凝胶剂的制备及质量控制方法。方法：以泊洛沙姆407为基质,卡波姆940为增稠剂,尼泊金乙酯为抑茵荆,氯化钠为渗透压调节剂,制备巴洛沙星眼用原位凝胶剂;采用HPLC法测定含量。结果：巴洛沙星浓度在5．0～50．0μg·ml^-1范围内线性关系良好（r=0．9996）,平均回收率为100．6％（RSD=1．41％）;家免眼刺激性实验表明本制剂无刺激性,符合《中国药典》对眼用制剂的质量要求。结论：该制剂处方设计合理,制备方法简便,含量测定方法适用于本品质量控制。     

加替沙星滴眼液处方筛选及含量测定

目的：正交试验筛选加替沙星滴眼液的最佳处方．并建立其含量测定方法。方法：以黏度为考察指标．用正交试验考察羟丙甲纤维素（HPMC）型号、浓度、溶液pH对滴眼液黏度的影响，筛选最佳处方组成；采用高效液相色谱法（HPLC）测定加替沙星滴眼液中加替沙星的含量。结果：最佳处方组合为A3B1C3；HPLC线性关系良好。平均回收率为100．1％，RSD为1．2％。结论：该处方设计合理．含量测定方法能有效控制制剂质量。     

盐酸西替利嗪凝胶剂的制备

目的 研制盐酸西替利嗪凝胶。方法 拟订处方组成及制备工艺，建立紫外分光光度法（UV法）用于含量测定。结果 该制剂pH值为6．40～6．50，含量测定方法平均回收率为99．51％，RSD=0．43％。结论 凝胶的制备工艺可行，质量稳定。用UV法测定盐酸西替利嗪的含量，方法可行，重现性好，可用于医院制剂的质量控制。     

盐酸洛美沙星乳膏剂的制备与质控

目的：制备盐酸洛美沙星乳膏剂,制定其质量控制标准。方法：采用紫外分光光度法中的对照品比较法测定盐酸洛美沙星乳膏剂中洛美沙星的含量,以甲醛为溶剂,测定波长287nm。结果：测得盐酸洛美沙星乳膏剂中洛美沙星平均回收率为99．80％,RSD为0．27％（n=6）,乳剂基质对测定无干扰。结论：该乳膏剂处方合理,制备工艺简单,含量测定操作简便,结果准确。     

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.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.