渗透促进剂增加复方骨质增生贴剂透皮渗透的研究

目的 探讨氮酮、杜香萜烯两种渗透促进剂对复方骨质增生贴剂透皮渗透的影响。方法 制备不同浓度氮酮、杜香萜烯及不含渗透促进剂的复方骨质增生贴剂，通过进行体外透皮实验，研究氮酮和杜香萜烯对该贴剂中的主要有效成分阿魏酸的渗透促进作用。结果 不同浓度的氮酮和杜香萜烯均有渗透促进作用，在本实验中氮酮优于杜香萜烯，且氮酮的最佳浓度为3％，此时氮酮的增渗倍数最高，为8．1倍。结论 以阿魏酸累积渗透量为指标，选择3％氮酮作为复方骨质增生贴剂的渗透促进剂更为适宜。     

水溶性氮酮对人眼小梁细胞增殖活性与形态结构的影响

目的观察经皮渗透促进剂氮酮对体外培养的人眼小梁细胞增殖活性和超微结构的影响，寻找氮酮作用于眼部的安全浓度。 方法进行人眼小梁细胞的体外培养，四氮唑盐（MTT）法观察不同浓度氮酮作用不同时间对小梁细胞增殖的影响；倒置相差显微镜和透射电镜下观察氮酮对小梁细胞形态和超微结构的影响；荧光染色法观察氮酮对小梁细胞活性的影响。结果10 8～10 5 g·L 1氮酮作用24 h不影响小梁细胞的增殖。10 8～10 6 g·L 1氮酮对小梁细胞形态和超微结构无影响。荧光染色法显示10 3 和10 4 g·L 1氮酮作用后的细胞呈不同程度变性坏死。结论10 8～10 6 g·L 1氮酮不会影响小梁细胞的形态结构和增殖活性，低浓度氮酮在理论上对小梁细胞是安全的。     

补骨脂酊透皮吸收的实验研究

补骨脂酊是治疗白癜风的常用制剂，为提高其治疗效果，对含高效透皮吸收增强剂氮酮的酊剂之透皮吸收进行了研究，发现氮酮有增加补骨脂酊中补骨脂素和异补骨脂素透皮吸收的作用，氮酮浓度为２％时，体外经皮渗透１２小时，其透过百分率增加约４５％。对所取得之数据进行抛物线拟合，求得最佳氮酮浓度为２．１５％。皮肤残存量结果表明体外实验中皮肤残存量较体内大，体内皮肤残存量含２％氮酮之酊剂较不含氮酮之酊剂高。实验证明中药     

月桂氮酮对灭痤乳膏中盐酸克林霉素透皮吸收作用的影响

目的：研究不同浓度的月桂氮酮对盐酸克林霉素小鼠离体皮肤渗透性的影响。方法：用改良的Franze扩散池，选用不同浓度月桂氮酮(0，l％，2％和5％)作促渗剂，采用高效液相色谱法(HPLC法)测定盐酸克林霉素累积释放量(Q)、稳态流量(J)及渗透系数(Kp)。结果：与不含月桂氮酮的灭痤乳膏中盐酸克林霉素的Q值相比较，含1％月桂氮酮增加了67％，而含2％月桂氮酮则无显差异，当月桂氮酮浓度达5％时，Q反而降低了45％。结论：l％月桂氮酮对灭痤乳膏中盐酸克林霉素具有明显促渗作用。     

月桂氮■酮的抑菌作用观察

月桂氮酮（氮酮）作为一种高效透皮吸收促进剂，已广泛应用于医药化妆品等领域，本实验中发现，氮酮在２０μｇ／ｍｌ浓度下，对Ｇ＋细菌及芽孢具有显著的抑制作用。     

氮酮对19种药物的促透皮吸收作用

氮酮对１９种药物的促透皮吸收作用河北医学院第二医院（０５００００）刘宝库，李守勤氮酮（Ａｚｏｎｅ）由美国Ｎｅｌｓｏｎ公司１９７６年开发成功。１９８７年郑颉首次向国内介绍［１］，国内氮酮产品相继面市。氮酮促透皮吸收作用的研究和应用工作方兴未艾，促进了制...     

月桂氮Zuo酮对咪康唑霜透皮扩散作用的影响

本文研究了月桂氮Ｚｕｏ酮对咪康唑霜皮扩散作用的影响。考察了氮酮在不同浓度下、以离体鼠皮为透皮屏障、咪康唑霜对涂有霉菌琼脂培养基的扩散作用。实验结果表明：含５种不同浓度氮酮的咪康唑霜，其抑菌圈直径均小于不含氮酮的样品，且随着氮酮浓度递升（１．２、１．８、２．４％），其抑菌圈直径与不含氮酮样品相对照，在统计学上的显著性（Ｐ＜０．０５）或极显著性差异（Ｐ＜０．０１）。     

氮酮对双氯灭痛透皮吸收的影响

以透皮吸收模型观察了氮酮浓度对双氯灭痛透皮吸收的影响。结果表明，搽剂中氮酮浓度为１％是其透皮吸收促进作用的适宜浓度，氮酮对软膏中双氯灭痛的透皮吸收无促进作用。     

月桂氮酮对无环鸟苷霜体外透皮吸收作用的影响

考察不同浓度月桂氮酮对无环鸟苷霜的透皮促渗作用，进行合理的处方筛选。以离休兔皮为渗透屏障，采用改良Franz扩散池，研究不同浓度氮酮对无环鸟昔的透皮促渗作用。无环鸟苷霜的透皮吸收为零级动力学过程，氮酮对无环鸟苷的透皮促渗作用无浓度依赖性，经试验测得2％氮酮对无环鸟苷的促渗作用最强。     

桉叶油和氮酮对替硝唑凝胶剂体外透皮释药的研究

目的：研制替硝唑凝胶剂，考察混合促进剂桉叶油和氮酮对替硝唑透皮吸收作用的影响。方法：采用改良Franz直立式释放池，以离体鼠皮为透皮屏障，使用不同浓度的混合桉叶油和氮酮，测量替硝唑的透皮吸收量。结果：含2％桉叶油和2％氮酮的替硝唑凝胶与不含桉叶油和氮酮的替硝唑凝胶之间，其透皮速率增加了291％。结论：不同浓度的混合促进剂可不同程度地促进替硝唑的透皮吸收效果，其中以2％桉叶油加氮酮组成的混合促进剂作用最显著。     

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.

---

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.     

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.     

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.