蚊虫和疾病与驱避蚊剂和人类健康

世界上许多危害很大的疾病，如疟疾、黄热病、登革热等大都是通过蚊蝇小咬等昆虫的侵扰，造成大范围或大面积疾病的传播或引发疫病流行。蚊媒病在预防医学中占有重要位置，据统计，世界上每30秒就有一人由于蚊蝇虫咬引发的疾病造成死亡，每年仅疟疾流行就会导致300万人死亡，登革热的感染每年也多达8000万。     

长效驱蚊霜野外现场驱避效果观察

目的:观察长效驱蚊霜野外驱避效果.方法:选择120名男性健康受试者,随机平均分为4组,第1组(空白对照组)、第2组(施美蚊不叮香露对照组)、第3组(长效驱蚊霜A型试验组)、第4组(长效驱蚊霜B型试验组).所有受试者左前臂裸露并分别涂抹驱蚊剂,每次间隔30 min,在蚊子最多的丛林中站立15 min,观察驱蚊剂的驱避效果.结果:在2 h内试验组驱避蚊虫的有效率为100%,对照组有效率为0.00%,两种驱蚊剂有非常显著的差异(P<0.001).结论:长效驱蚊霜对驱避蚊虫叮咬效果非常显著,驱避效果优于施美蚊不叮香露.     

新型驱蚊虫成分及制剂的研究概况

蚊虫可传播多种疾病,且发病率和病死率较高,严重威胁人类健康。目前以化学合成药为主的驱蚊虫剂在使用中面临诸多严重问题,如对人体产生副作用、造成环境污染、蚊虫种群产生耐药性。因此研究开发新型驱蚊虫活性成分受到全球广泛关注。本文主要综述了石墨烯衍生物、环境友好型植物精油以及部分合成化学品在驱蚊虫方面的研究概况。     

左旋咪唑临床应用及剂型改变

近年来，左旋咪唑应用于免疫调节和免疫治疗的作用非常广泛。多用于治疗免疫功能低下或缺陷以及一些自身免疫性疾病，特别是在对慢性病毒性肝炎的治疗中效果良好。     

新法规下关于中药改剂型为口服凝胶剂的一些思考

目的探讨新法规下关于中药改剂型为口服凝胶剂的合理性研究内容。方法结合申报情况,对照新法规对中药改剂型为口服凝胶剂研究中存在的问题,从剂型选择的必要性、合理性、凝胶特性的研究、辅料的选择及用于口服的安全性、质量研究等方面进行了讨论。结果与结论建议应对其剂型选择的必要性进行充分考虑,对辅料的适用性进行深入研究,建立符合凝胶制剂特性的质量控制指标。     

姜黄素剂型研究进展

目的阐述姜黄素剂型研究的进展。方法围绕姜黄素的溶解性及其体内行为的改善,对其剂型的研究概况进行综述。结果通过对姜黄素各种剂型进行的实验,结果表明,均能在一定程度上提高姜黄素的溶解度和生物利用度。结论姜黄素是天然来源的药物,鉴于其广泛的药理作用,改善姜黄素的溶解度及其生物利用度对改善其体内的吸收有着重要意义。     

氧氟沙星的剂型研究及其应用

氧氟沙星（Ofloxacin,氟嗪酸、康泰必妥）是第三代喹诺酮类抗菌药物,因具有广谱、高效、低毒等特点而被临床各科广泛应用。为了将药物集中于感染病灶,以增加药物的选择性,提高疗效,不少专家和学者根据临床用药需要,结合氧氟沙星的理化特点和药理特性,在片剂、胶囊剂的基础上开发了多种剂型。1滴眼剂代福生等人根据氧氟沙星在水或乙醇中极微溶、而在冰醋酸中易溶的性质,将氧氟沙星配制成滴眼液,并用1mol／L氢氧化钠调节pH至6．0～7．0,以减少对眼的刺激。赵锦文等人以0．1mol／L盐酸为溶媒、磷酸盐作缓冲对的配方,制得的氧氟沙…     

儿童用药物剂型的研究进展

儿童处于生长发育的特殊时期,临床用药需要根据患儿的年龄、生理特点确定给药方式和剂量。相对于成人用药,儿童用药依从性差,给药剂量需灵活准确,这给儿童药物的制剂设计带来了挑战。本文通过查阅近年有关儿童用药的文献,概述了国内外儿童用药物剂型的研究与应用进展。     

A bioassay for mosquito repellency against Aedes aegypti: method validation and bioactivities of DEET analogues

Objectives Vector‐borne diseases are still a major mortality factor in Africa and South‐east Asia and effective mosquito repellents are therefore needed. An efficient and safe in‐vitro assay system using artificial blood and skin substitute could facilitate the development of novel repellents, as most assays currently rely on human subjects or vertebrate whole blood. Moreover, examining the skin permeation profiles could provide safer mosquito repellents. The new assay system could serve as an initial system for testing new repellent candidates upon validation with DEET and its analogues. Methods N,N‐Diethyl‐meta‐toluamide (DEET) and five analogues were synthesised and used to validate a novel in‐vitro bioassay using artificial blood and collagen membrane. Repellency against Aedes aegypti was correlated with lipophilicity and skin permeation. Key findings The new in‐vitro assay showed good reproducibility (interday relative standard deviation <10% at high concentrations). Four of the five DEET analogues showed repellency similar or superior to that of DEET. Repellency correlated linearly with lipophilicity but stronger repellents tended to permeate skin better. Conclusions The new in‐vitro assay using blood substitute and collagen membrane significantly simplifies screening of possible mosquito repellents. Lipophilicity as well as skin permeation profiles should be considered before testing of compounds that are candidates for mosquito repellents.     

Tissue disposition of the insect repellent DEET and the sunscreen oxybenzone following intravenous and topical administration in rats

The insect repellent N,N‐diethyl‐m‐toluamide (DEET) and sunscreen oxybenzone (OBZ) have been shown to produce synergistic permeation enhancement when applied concurrently in vitro and in vivo. The disposition of both compounds following intravenous administration (2 mg/kg of DEET or OBZ) and topical skin application (100 mg/kg of DEET and 40 mg/kg of OBZ) was determined in male Sprague‐Dawley rats. Pharmacokinetic analysis was also conducted using compartmental and non‐compartmental methods. A two‐compartment model was deemed the best fit for intravenous administration. The DEET and oxybenzone permeated across the skin to accumulate in blood, liver and kidney following topical skin application. Combined use of DEET and oxybenzone accelerated the disappearance of both compounds from the application site, increased their distribution in the liver and significantly decreased the apparent elimination half‐lives of both compounds (p < 0.05). Hepatoma cell studies revealed toxicity from exposure to all treatment concentrations, most notably at 72 h. Although DEET and oxybenzone were capable of mutually enhancing their percutaneous permeation and systemic distribution from topical skin application, there was no evidence of increased hepatotoxic deficits from concurrent application. Copyright © 2011 John Wiley & Sons, Ltd.     

酮咯酸新型制剂的研究进展

酮咯酸是一种新一代强效镇痛的非甾体类抗炎药.随着给药系统和制剂技术的不断发展,酮咯酸除常规的口服与注射给药外,还开发了经皮肤、眼部、鼻腔及口腔黏膜的给药新途径与新剂型,使酮咯酸具有长效镇痛和局部给药局部起效两大主要特点.酮咯酸新型制剂镇痛效果良好,且能提高患者的顺应性和用药安全性,具有良好的市场前景.     

Percutaneous characterization of the insect repellent DEET and the sunscreen oxybenzone from topical skin application

The synergistic percutaneous enhancement between insect repellent DEET and sunscreen oxybenzone has been proven in our laboratory using a series of in vitro diffusion studies. In this study, we carried out an in vivo study to characterize skin permeation profiles from topical skin application of three commercially available repellent and sunscreen preparations. The correlation between skin disposition and drug metabolism was attempted by using data collected. Both DEET and oxybenzone permeated across the skin after the application and achieved substantial systemic absorption. Combined use of DEET and oxybenzone significantly enhanced the percutaneous penetration percentages (ranging 36-108%) due to mutual enhancement effects. Skin disposition indicated that DEET produced a faster transdermal permeation rate and higher systemic absorption extent, but oxybenzone formed a concentrated depot within the skin and delivered the content slowly over the time. In vivo AUCP/MRT of DEET and oxybenzone was increased by 37%/17% and 63%/10% when the two compounds were used together. No DEET was detected from the urine samples 48 h after the application. Tape stripping seemed to be a satisfactory approach for quantitative assessment of DEET and oxybenzone penetration into the stratum corneum. It was also concluded that pharmacological and toxicological perspectives from concurrent application of insect repellent and sunscreen products require further evaluation to ensure use efficacy and safety of these common consumer healthcare products.     

In vitro permeation characterization of repellent picaridin and sunscreen oxybenzone

Picaridin and oxybenzone are two active ingredients found in repellent and sunscreen preparations, respectively. We performed a series of in vitro diffusion studies to evaluate the transmembrane permeation of picaridin and oxybenzone across human epidermis and poly(dimethylsiloxane) (PDMS) membrane. Permeation of picaridin (PCR) and oxybenzone (OBZ) across human epidermis was suppressed when both active ingredients were used concurrently; increasing concentration of the test compounds further reduced the permeation percentage of picaridin and oxybenzone. While permeation characteristics were correlative between human epidermis and PDMS membrane, permeability of PDMS membrane was significantly larger than that of human epidermis. The findings were different from concurrent use of repellent DEET and sunscreen oxybenzone in which a synergistic permeation enhancement was observed. Further comparative studies are therefore needed to understand permeation mechanisms and interactions between picaridin and oxybenzone.     

Development and characterization of micellar systems for application as insect repellents

N,N-diethyl-meta-toluamide (DEET) is a widely used insect repellent due to its high efficacy. In this work, micellar systems based on poly(ethylene oxide)–poly(propylene oxide)–poly(ethylene oxide) triblock copolymer were developed and studied for the purpose of controlling the release and cutaneous permeation of DEET, using concentrated solutions of the copolymer Pluronic F127 to form thermoreversible gels. The formulations presented thermoreversible gelation above 5 °C and altered rheological behavior at 15 and 25 °C. The presence of the drug drastically changed the sol–gel transition temperatures. The micrographs suggest that DEET induced the formation of anisotropic structures, and Maltese Crosses were observed. The formulation containing 10 wt% DEET and 15 wt% Pluronic F127 presented sustained drug release for up to 7 h. DEET release profile followed the Higuchi kinetics model. There was a reduction of approximately 35% in the amount of DEET absorbed through the skin after 6 h. About 62% of DEET from the formulation consisting of Pluronic F127 and DEET remain retained on the skin. The anisotropic structure may constitute a barrier to diffusion and thereby controlling the drug release effectively. These tests suggest that the tested samples exhibit safety profile greater than some commercially available products.     

肝舒胶囊的成型工艺研究

目的探讨肝舒胶囊的成型条件。方法从粉末和颗粒的吸湿性、流动性等几个方面进行考察。结果采用3%羧甲基淀粉钠为辅料所制颗粒的临界相对湿度约为61%,休止角为29.68°,堆密度为0.65 g/mL,可选用0号胶囊进行装量。结论本成型工艺可行,利于制粒,制成的颗粒流动性好,利于填充。     

注射用前列地尔的处方与工艺研究

目的：确定注射用前列地尔的制备处方及工艺。方法：选择适宜赋形剂,对冻干工艺进行筛选。结果：以右旋糖酐为赋形剂,经过18小时的冻干过程,制得成型性好,质量可靠的注射用前列地尔。结论：注射用前列地尔处方工艺可行。     

Pharmacokinetic and pharmacodynamic comparison of a new controlled-release formulation of metoprolol with a traditional slow-release formulation

The plasma concentration-time profile and haemodynamic effects of metoprolol after the administration of metoprolol CR¹ (a new multiple-unit controlled-release formulation) and metoprolol SR² (a traditional slow-release formulation) once daily, were investigated in 12 healthy men. Data were collected over one 24-h dose interval at steady state after five days of treament.The study was a randomized, three-way, crossover comparison of metoprolol CR, 100 mg, metoprolol SR, 100 mg, and placebo. The reduction in exercise heart rate in relation to placebo treatment was used as a measure of ₁-blockade.