左旋盐酸苯环壬酯鼻腔喷雾剂的局部安全性评价

 目的对制备的左旋盐酸苯环壬酯鼻腔喷雾剂进行局部安全性评价。方法以蟾蜍上颚黏膜纤毛为模型考察纤毛毒性,以大鼠鼻黏膜形态学检查评价局部刺激性。结果左旋盐酸苯环壬酯鼻喷剂纤毛毒性及对局部刺激性均较小。结论左旋盐酸苯环壬酯鼻喷剂局部用药较安全,具有良好的应用前景。     

喷雾(冰冻)干燥法制备钠、锂快离子导体

对两种性能较好的快离子导体Na_3Zr_2Si_2P_3O_(12)(Nasicon)和Li_(1.8)Ti_(1.2)·Cr_(0.8)P_3O_(12)用喷雾干燥法和冰冻干燥法制备粉料和陶瓷烧结,并对样品进行了X射线衍射分析,形貌和显微结构观察以及阻抗谱测量等。实验结果表明:两种方法制备的粉料具有颗粒细,均匀性好,合成温度低等优点。在300℃时,两种样品的电阻半分别为10.05 Ω.cm和94.8 Ω.cm。激活能分别为0.25 eV和0.27ev。     

Endoscopic photographic comparison of drug delivery by ear-drops and by aerosol spray

The Otomize (Stafford-Miller Ltd) aerosol spray is a new device for delivering topical ear medication in otitis externa. Both the manufacturers and a recent study have claimed that the spray produces better coverage of the external ear canal than do traditional ear-drops. We performed an endoscopic photographic comparison study to investigate this claim. The area of tympanic membrane and ear canal covered with medication was greater in those ears treated with the aerosol (P < 0.001, paired t-test). The ability of the aerosol to deliver drug to the level of the tympanic membrane suggests a possible role for this device in the treatment of chronic otitis media. The technique of endoscopic photography provides an objective and reproducible means of investigating drug delivery systems for otological conditions.     

心痛灵喷雾剂抗心肌缺血的实验观察

①目的　观察心痛灵喷雾剂对心肌缺血大鼠的药理作用。②方法　通过结扎大鼠冠状动脉前降支制备大鼠心肌缺血模型 ,观察心痛灵喷雾剂对心肌缺血面积和血清磷酸肌酸激酶 (CK)、乳酸脱氢酶 (LDH)、谷草转氨酶 (GOT)的影响 ;静脉注射垂体后叶素制备大鼠心肌缺血模型 ,观察心痛灵喷雾剂对心电图改变的影响。③结果　心痛灵喷雾剂可减少心肌缺血大鼠心肌梗死面积 ,降低血清CK、LDH、GOT活性 ,并减轻静脉注射垂体后叶素引起的缺血性心电图改变 (tD=1.2 2 3～ 13.890 ,P <0 .0 5、0 .0 1)。④结论　心痛灵喷雾剂具有抗心肌缺血的作用     

Preparation of tritium‐labeled Silybin—a protectant for common liver diseases

Silymarin, the seed extract of milk thistle plant, Silybum marianum, has been used traditionally for the treatment of liver diseases and bile duct infection. Silybin 1 is the main bioactive components of silymarin, consisting a pair of diastereomers: Silybin A and Silybin B. In this article, we report the preparation of tritium‐labeled Silybin, which was accomplished by protection of Silybin as tritylated compound 2 and followed by oxidation of the primary alcohol to its corresponding aldehyde 3 . Subsequent reduction with NaB[³H]₄ and deprotection of the trityl group provided the tritium‐labeled Silybin 4 . Copyright © 2006 John Wiley & Sons, Ltd.     

Nasal nicotine spray: a rapid nicotine delivery system

Plasma nicotine concentrations following administration by two types of nasal nicotine spray were compared in ten subjects. Absorption was particularly rapid during the first 2.5 min, the average rise in blood nicotine concentrations during this time being 8.6 ng/ml for the two products, followed by a small further rise to an average peak increase of 10.5 ng/ml 5 min after the dose of 2 mg nicotine base (mean 27.8 micrograms/kg). Despite a four-fold Cmax variation between subjects, the levels of individual subjects were fairly consistent across the two products. There were no significant differences between the two products in blood nicotine concentrations or cardiovascular responses, and the correlation between the AUCs from the two products was 0.68 (P = 0.01). Eight subjects reported subjective feelings of light-headedness or slight dizziness, which are not typical after slower absorption from nicotine gum or skin patches. Blood nicotine levels within the smoking range were soon built up with repeated doses, even in the subject with the least efficient nasal absorption. In a second study of ad libitum use under clinical conditions both products appeared sufficiently acceptable for therapeutic use as an aid to smoking cessation. There was no tendency to escalate to excessive use over 4 weeks, and blood nicotine concentrations in nine subjects averaged only 44% of their prior smoking levels. Only one subject had levels equivalent to prior smoking and possible reasons why this was not more common are discussed.     

施地瑞玛生理性海水鼻腔喷雾器治疗小儿干燥性鼻炎的临床观察

目的:探讨施地瑞玛生理性海水鼻腔喷雾器治疗小儿干燥性鼻炎的疗效。方法:将58例患儿随机分成2组,2组均不使用其他药物。治疗组给予施地瑞玛生理性海水鼻腔喷雾器喷鼻;对照组给予生理性盐水滴鼻液滴鼻,观察2组治疗前后症状、体征及有效率。结果:根据2组的主要症状、体征及疗效,治疗组优于对照组(P<0.05)。结论:生理性海水鼻腔喷雾器治疗小儿干燥性鼻炎,可以缩短病程,改善鼻腔功能,疗效确切,且使用安全、舒适、方便,可以作为治疗小儿干燥性鼻炎的理想药物。     

An automated on-line method for simultaneous analysis of phenothiazines in human serum by high-performance liquid chromatography/sonic spray ionization mass spectrometry using backflush column switching

An automated on-line method for simultaneous analysis of five phenothiazine drugs by high-performance liquid chromatography (HPLC)/sonic spray ionization mass spectrometry (SSI-MS) has been established, using backflush column switching. A 400-μl portion of serum sample diluted 81-fold with distilled water was subjected to the on-line system. In the system, an Oasis HLB cartridge was used as the precolumn for extraction; large molecules such as proteins in serum were discarded by use of distilled water containing 0.1% formic acid as a mobile phase. After switching a valve, the analytes trapped in the precolumn were eluted in the backflush mode and separated by a Chromolith Performance RP-18e column, which is composed of C₁₈-bonded monolithic silica. The column effluents were then introduced into the SSI-MS. The present method provided successful separation and determination of six phenothiazines including an internal standard. Satisfactory linearities, reproducibility, and sensitivity were obtained at concentration levels that matched the toxic levels of phenothiazines. All drug peaks appeared within 18 min, and the system could be reequilibrated in only about 8 min for the next run. Because of the simplicity and rapidness of the method, it is likely to be useful in the fields of emergency medicine and forensic toxicology.     

Effect of Antihepatotoxic Agents Against Microcystin-LR Toxicity in Cultured Rat Hepatocytes

Primary cultures of adult rat hepatocytes were used to investigate the effects of two putative therapeutic agents, dithioerythritol and silymarin on microcystin-LR-induced hepatotoxicity. Cell injury was assessed by the extent of cellular [¹⁴C]adenine nucleotides and lactate dehydrogenase (LDH) release into the medium and the extent of hepatocyte detachment from monolayers. Microcystin-LR (1 µM) induced a significant release of both ¹⁴C-labeled nucleotides and LDH from hepatocytes as well as significant detachment of cells from monolayers. Although both dithioerythritol (0.63–5 mM) and silymarin (25–200 µM) reduced the amount of marker release and cell detachment from microcystin-LR-treated wells, silymarin provided significantly greater protection than dithioerythritol at one-tenth the concentration. Furthermore, silymarin and dithioerythritol treatment prevented morphological deformations and detachment of cells.     

流化床喷雾制粒机若干机理的研究

研究了流化床喷雾制粒机的起始流化速率，粉粒平稳流化及其控制方法，喷雾制粒机理和骤变失稳现象，指出起始流化速度的实验值远大于理论值，但是可以通过对床层压降的监控，实现平稳流化的操作控制，颗粒以团骤方式长大，而温骤变失稳是本文流化制粒失效的主要形式，讨论了多种过程参量对制粒和骤变失稳的影响，其结果有助于指导实际生产。