微乳对难溶性药物增溶机理的研究

目的:初步探讨微乳对难溶性药物的增溶机理.方法:经处方筛选及相图研究确定(BL-9/正丁醇3∶1)/油/水比例为9∶1∶40的微乳处方;以二氢吡啶类药物为模型药物,测定其在微乳、胶束和油相中的溶解度及油/水分配系数;根据化学结构,采用计算机软件计算药物的特性参数,并结合模型药物的特性分析微乳增溶难溶性药物的机理.结果:微乳对药物的增溶效果远大于油相和胶束,并随药物的脂溶性和空间结构的改变而变化.结论:微乳可用于增溶难溶性药物,且脂溶性越大,空间位阻越小,增溶效果越明显.     

An alkylpolyglucoside surfactant as a prospective pharmaceutical excipient for topical formulations: The influence of oil polarity on the colloidal structure and hydrocortisone in vitro/in vivo permeation

There is a growing need for research into new skin- and environment-friendly surfactants. This paper focuses on a natural surfactant of an alkylpolyglucoside type, which can form both thermotropic and lyotropic liquid-crystalline phases. The aim of this study was to relate some physicochemical properties (characterised by polarisation and transmission electron microscopy, thermal analysis and rheology) of the three formulations based on cetearyl glucoside and cetearyl alcohol, to the results of in vitro and in vivo bioavailability of hydrocortisone (HC). The three formulations contained oils of different polarity (medium chain triglycerides: MG, isopropyl myristate: IPM and light liquid paraffin: LP), respectively. In vitro permeation was followed through the artificial skin constructs (ASC), while the parameters measured in vivo were erythema index: EI (using instrumental human skin blanching assay), transepidermal water loss (TEWL) and stratum corneum hydration (SCH). The vehicles based on cetearyl glucoside and cetearyl alcohol showed a complex colloidal structure of lamellar liquid-crystalline and lamellar gel-crystalline type, depending on oil polarity. Rheological profile of the vehicle was directly related to the in vitro profile of the HC permeation. In vivo results suggested that the vehicle with MG retarded the HC permeation, whereas less polar IPM and non-polar LP enhanced it. It is suggested that the enhancement is achieved either by a direct interaction with lipid lamellae of the SC or indirectly by improving skin hydration.

There were no adverse effects during in vivo study, which indicates a good safety profile of this alkylpolyglucoside surfactant.     

Effect of linoleic acid, linoleic acid anilide, and arachidonic acid on the expression of adhesion molecules on human neutrophils

The effects of linoleic acid, linoleic acid anilide, and arachidonic acid on the expression of CD11b/CD18, CD11c/CD18 integrins and l-selectin on human neutrophils were studied by flow cytometry in a whole blood assay. None of these compounds had any effect on the basal expression of CD11b, CD11c, or l-selectin in the concentration range of 20–100 μM. However, linoleic acid at a concentration of 1000 μM slightly up-regulated CD11b and CD11c by a factor of 2.1 and 1.7, respectively. Linoleic acid, linoleic acid anilide, and arachidonic acid did not affect the formyl-methionyl-leucyl-phenylalanine induced up-regulation of CD11b or CD11c. However, linoleic acid and linoleic acid anilide slightly inhibited the phorbol myristate acetate (PMA)-induced expression of CD11b, which was decreased by 27 and 21% at concentrations of 100 and 1000 μM, respectively. Likewise, arachidonic acid at 40 μM inhibited the PMA-induced expression of CD11b by 19%. Our results suggest that linoleic acid, linoleic acid anilide, and arachidonic acid do not dramatically affect the expression of leukocyte adhesion molecules in a whole blood assay. Received: 17 February 1997  / Accepted: 5 May 1997     

莪术油治疗小儿呼吸道感染的疗效观察

目的:观察莪术油治疗小儿急性呼吸道感染(ARTI)的疗效和安全性。方法:218例RTI患儿随机分两组,治疗组静滴莪术油25ml/(kg·d),1~2次/d,疗程3~7d;对照组静滴头孢拉定50~100mg/(kg·d),3~4次/d,疗程3~7d。结果:两组总有效率分别为89.96%和88.7%(P>0.05)。用药3d后主要症状、体征等客观指标的改善率,治疗组优于对照组(P<0.05)。治疗组未发现不良反应。结论:莪术油葡萄糖注射液治疗小儿呼吸道感染安全有效、使用方便。     

超临界CO2萃取薏苡仁油工艺条件优化

目的应用超临界CO2萃取技术提取薏苡仁中的薏苡仁油，优化工艺条件。方法利用1L与600L的超临界萃取装置，考察原料水份、压力、时间与温度等参数对薏苡仁油提取得率的影响。结果优化得到用超临界CO2萃取技术从薏苡仁中提取薏苡仁油的工艺参数。结论超临界CO2萃取技术可用于薏苡仁油的提取，适用于工业化生产。     

复方藏红花油治疗跌打损伤(急性软组织损伤)Ⅲ期临床试验总结

目的:评价复方藏红花油治疗跌打损伤(急性软组织损伤)的临床疗效、安全性.方法:采用多中心、单盲随机平行对照方法,将400例跌打损伤(急性软组织损伤)患者分为复方藏红花油组(试验组)300例,正红花油组(对照组)100例,对比分析两组的临床疗效.结果:①试验组总有效率96%,对照组总有效率82.00%,试验组疗效优于对照组(P＜0.01).②两组治疗单项症状均有效.③试验组治疗中医证候有效,且优于对照组.④试验组在治疗过程中未见明显不良反应.结论:复方藏红花油是一种治疗跌打损伤(急性软组织损伤)安全、有效的药物.     

早产儿疾病用维生素E油浴治疗

目的 探讨维生素E油浴应用于早产儿治疗中的作用。方法 对2001年3月～2003年12月我院住院的42例患肺透明膜病的早产儿，28例患新生儿硬肿症的早产儿及随机抽取的50例早产儿，三种情况早产儿分别随机分为治疗组和对照组，对照组给予常规治疗，治疗组在常规治疗的基础上加用维生素E油浴。结果 治疗组治疗的时间均短于对照组（P〈0．05）。结论 维生素E油浴在早产儿治疗中有促进疾病好转和恢复的作用，并且未发现维生素E油浴的不良反应。     

苏州荠芋挥发油的提取工艺研究

目的：考察苏州荠芋挥发油的不同提取方法，以确定最佳提取工艺。方法：采用超临界CO2萃取、水蒸气蒸馏和有机溶剂萃取三种方法提取苏州荠芋挥发油，以所得得油率和所得挥发油的化学成分为指标，对三种方法进行比较。结果：经GC—MS分析结果表明，超临界CO2萃取的得油率为3．46％，要高于其它提取方法。采取超临界CO2萃取和水蒸气蒸馏的苏州荠芋挥发油品质较优。三种方法提取的苏州荠芋挥发油的主要成分基本相似。主要为甲基丁香酚（methyleugenol），占42％左右；其次是单萜类化合物龙脑稀（bomene）、侧伯酮（thujone）、二氢香芹酮（dihydrocarvon）、香荆芥酚（carvacrol）等，占27％左右；再次是倍半萜类化合物橙花烯（nerolidene）和γ-杜松烯等约占19％左右。结论：超临界CO2萃取法为提取苏州荠芋挥发油的理想方法。     

Genetic trace metal disturbances.

Genetic trace metal disturbances can be at three levels. Trace metals play an important role in the metabolism of genetic macromolecules and the information transfer system. Deficiency or excess of trace metals caused either by dietary or genetic factors will affect the normal functioning of the whole organism. The roles of trace metals in carcinogenesis/mutagenesis and ageing are typical of this category. The second level of genetic trace metal disturbances affect the metabolic pathway of the trace metal itself. Biochemical derangement resulting from genetic defects cause aberrant metabolism of the element and thus disease symptoms. Diseases caused by abnormal metabolism of copper, zinc, iron, and molybdenum are discussed. Trace metal disturbances can also be the result of other genetic diseases. This aspect of genetic trace metal disturbances is least investigated. However, information should be important for improving the existing treatment protocol for the more common inborn errors of metabolism, such as phenylketonuria.