水杨酸咪唑栓的稳定性考察

目的考察光、温度、湿度等多种因素对水杨酸咪唑栓稳定性的影响。方法建立质量标准,分别进行各影响因素试验、加速试验、室温留样检查观察和分析水杨酸咪唑栓的性状、含量及其他项目。结果本制剂对高湿度、低温(4℃)稳定,但光照对本品外观颜色有一定影响,在高温40～80℃放置会软化变形。结论本品应避光,35℃以下温度保存。     

Action of methylxanthines and imidazole on the contractility of the terminal ileum of the guinea pig

Methylxanthines (aminophylline and caffeine) and imidazole, substances with an opposite action on phosphodiesterase (PDE), were found to contract the terminal ileum and to potentiate nerve-mediated responses — contractions elicited by electrical stimulation (ES) at 3 Hz and 30 Hz. Imidazole-induced contractions which were partly reduced by atropine, potentiated both responses to ES to about the same extent, and enhanced contractility of the preparation to histamine and potassium. The action of imidazole on the terminal ileum could be related to its influence on PDE in the smooth muscle.The effects of aminophylline and caffeine were found to be more complex, possibly involving some mechanisms other than inhibition of PDE. They produced atropine-sensitive contractions of the terminal ileum, which were potentiated by physostigmine and strongly depressed by hemicholinium. In the presence of atropine, they potentiated ES-induced contractions, particularly those elicited by ES at 30 Hz, which are thought to be of adrenergic orig origin. Both actions appeared to be due to presynaptic effects—activation of cholinergic and adrenergic neurons in the intestinal wall, possibly by enhanced influx of calcium, and facilitated release of acetylcholine and noradrenaline. Aminophylline, in concentrations which potentiated nerve-mediated contractions elicited by ES, did not affect direct smooth muscle-contracting action of drugs. Higher concentrations of aminophylline, above 0.1 mM, were found to inhibit histamine- and noradrenaline-induced contractions presumbly due to inhibition of PDE in the smooth muscle and subsequent elevation of cAMP levels.     

Diversion of prostaglandin endoperoxide metabolism by selective inhibition of thromboxane A2 biosynthesis in lung, spleen or platelets.

Infusion of arachidonic acid through the guinea pig lung or the cat spleen causes a release of thromboxane A2 and prostaglandins, as measured by bioassay. After incubation of human platelets with arachidonate similar metabolites are formed, as demonstrated chromatographically. Infusion of imidazole (50-75 microgram/ml) through the lung or spleen specifically inhibits thromboxane A2 production and diverts the pathway to the prostaglandins, mainly prostaglandin F2alpha. In human platelets imidazole causes a dose-dependent inhibition of thromboxane A2 formation (ID50 5.5 X 10(-4) M). This inhibition is accompanied by a dose-dependent increase in prostaglandin F2alpha. Since thromboxane A2 induces platelet aggregation and is a potent vasoconstrictor, diversion of pathways to prostaglandins with opposite or less potent action might be of relevance in the treatment of cardiovascular diseases.     

In vitro antifungal activities of new imidazole salts towards dermatophytes

The in vitro activities of two new miconazole and econazole salts with the sulphosalicylic acid against 71 clinical isolates of dermatophytes were evaluated in comparison with those of miconazole, miconazole nitrate, econazole and econazole nitrate. Miconazole sulphosalicylate and econazole sulphosalicylate were equally effective in inhibiting the fungal growth compared with miconazole, econazole, and their nitrates.     

氟罗沙星溶液光降解反应机理的探讨

目的：研究氟罗沙星溶液光降解反应机理。方法：通过过氧化氢和咪唑对氟罗沙星溶液光降解影响的试验和咪唑对培氟沙星溶液光降解的影响的试验，推断氟罗沙星溶液光降解的可能机理。结果：过氧化氢对氟罗沙星光降解有促进作用，咪唑对氟罗沙星和培氟沙星光降解有抑制作用。结论：推断氟罗沙星的光降解反应明显有自由基的参与；而C8-位的氟取代基是喹诺酮类药物光降解反应中自由基反应的关键基团。     

Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents

Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds.     

芬太尼联合咪唑安定麻醉用于妇科手术效果研究

目的 对芬太尼联合咪唑安定麻醉用于妇科手术中的麻醉效果及安全性进行研究。方法 以我院2011年6月~2012年6月间妇科手术治疗的78例患者为研究对象,采用随机数字表法分为观察组和对照组,每组39例。分别使用芬太尼联合咪唑安定及丙泊酚联合芬太尼进行麻醉,对两组研究的麻醉效果及安全性进行比较及统计学分析。结果 观察组患者的麻醉效果及安全性均优于对照组,差异具有统计学意义（P〈0.05）。结论 芬太尼联合咪唑安定麻醉用于妇科手术的麻醉中具有麻醉效果好、安全性高等优势。     

Imidazole antimycotics affect the activity of various ion channels and insulin secretion in mouse pancreatic B-cells

In the present paper the effects of antimycotics with imidazole structure on the activity of various ion currents of mouse pancreatic B-cells and insulin secretion from isolated islets have been studied. Clotrimazole (0.1– 10 μM, bath solution without albumin) reversibly inhibited the whole-cell K⁺ _ATP current studied with the patch-clamp technique and concomitantly depolarized the membrane potential. Two other structurally related compounds, econazole and ketoconazole, exhibited similar effects on the whole-cell K⁺ _ATP current. Clotrimazole also inhibited the current through single K⁺ _ATP channels measured in the inside-out configuration. According to these results it seems unlikely that a cytoplasmic factor is involved in the action of clotrimazole on K⁺ _ATP currents. Clotrimazole (10 μM) also reduced the current through voltage-dependent Ca²⁺ and K⁺ channels and altered inactivation kinetics. Moreover, clotrimazole reversibly abolished a recently described inward current which is induced by hypotonic cell swelling. The results show that clotrimazole altered the activity of all ion currents in B-cells investigated in this study. Clotrimazole (3–100 μM, solution with albumin) irreversibly inhibited insulin secretion from isolated islets. With econazole and ketoconazole similar effects on hormone release were observed. The changes in the activity and kinetics of voltage-dependent Ca²⁺ and K⁺ currents are likely to contribute to the observed inhibition of insulin secretion. However, we cannot entirely rule out that imidazole antimycotics also interfere with a step in stimulus-secretion coupling distal to changes in membrane potential. Received: 9 July 1997 / Accepted: 29 July 1997