薄荷醇、氮酮、丙二醇联合应用对速美减肥贴透皮速率的影响

中药透皮给药是近年来经皮给药制剂研究的趋势,为了提高经皮给药制剂中药物透进皮肤的量,经皮给药制剂中越来越多地使用透皮吸收促进剂,特别是中药透皮吸收促进剂与化学透皮吸收促进剂联合应用,可增强其促透效果.     

4种透皮吸收促进剂对盐酸苯海拉明透皮性能的影响

目的:研究油酸、1,3-丙二醇、月桂氮酮、丙三醇4种透皮吸收促进剂对盐酸苯海拉明透皮性能的影响。方法:在一定量的盐酸苯海拉明溶液中分别加入4种不同浓度的透皮吸收促进剂,采用改良Franz扩散池进行体外透皮吸收试验,测定不同浓度下不同透皮吸收促进剂的24h累积透过量(Q)。结果:以Q为指标,促透作用油酸>1,3-丙二醇>月桂氮酮>丙三醇,且前三者分别以0.5%、0.5%、0.2%为最佳促透浓度,丙三醇未见有明显的促透作用。结论:4种透皮吸收促进剂在一定浓度下均可增强盐酸苯海拉明局部给药制剂的透皮吸收作用。     

中药复方制剂心安康贴剂的透皮吸收促进剂选择研究

目的：对中药复方制剂心安康贴剂的透皮吸收促进剂的选择进行研究。方法：采用Franz渗透扩散装置的气相色谱法，进行了大鼠皮肤贴剂的体外释放与渗透试验，对氮酮、十六醇、月桂醇硫酸钠，丙二醇4种透皮吸收促进剂单独应用和任意两种舍用的促进效果进行考察。结果：氮酮和丙二醇以2％：15％褥合，促进效果最强。结论：透皮促进剂对中药贴剂中的成分有较好的促透作用。     

氮酮对十四类药物的透皮吸收促进作用

氮酮作为一种新型高效低毒的透皮吸收促进剂，应用于多种透皮吸收制制剂中，取得良好的效果。本文归纳了其在十四类中西药物中，作为促透剂的应用情况。     

不同透皮促进剂对马钱子碱体外透皮吸收的影响

目的考察不同透皮促进剂对马钱子碱体外透皮吸收的影响。方法采用改良Franz扩散池,选用离体猪耳朵皮为屏障,考察不同类型的透皮促进剂对马钱子碱体外透皮吸收速率、增渗倍数等参数的影响。结果除吐温-80外,各透皮促进剂均能提高马钱子碱的透皮速率,促透能力由弱至强依次为桉叶素<油酸<氮酮<肉豆蔻酸异丙酯<柠檬烯。结论本研究可为马钱子碱外用剂型的选择与优化提供指导。     

透皮吸收促进剂应用及研究的新进展

综述了透皮吸收促进剂的应用、促透机制的研究、新型透皮上促进剂的合成与筛选等。     

透皮吸收促进剂在巴布剂中的应用及研究

经皮给药系统不断完善并得到了发展，但许多药物透皮应用时并不能完全满足治疗要求，因此提高其透皮速率是开发透皮给药系统的关键。通过查阅近10年有关透皮吸收促进剂的文献资料，对透皮吸收促进剂及其在巴布剂中的应用情况进行分析、整理和归纳，为巴布剂的透皮吸收实验研究提供参考。     

函数化处理与距离法相结合综合评价几种促透剂的促透效果

目的:探讨函数化处理与距离法相结合在透皮吸收促进剂促透效果综合评价中的应用。方法:研究薄荷醇、月桂氮芯卓酮和石菖蒲挥发油对模型药物对乙酰氨基酚在离体兔背部皮肤上的透皮行为,计算稳态流量、渗透系数、增渗倍数和滞后时间,采用函数化处理与距离法对促透效果进行综合评价。结果:2%薄荷醇促透效果最好,1%月桂氮芯卓酮次之,7%石菖蒲挥发油最差。结论:函数化处理与距离法可作为促透剂综合评价的一种新方法。     

促透剂在透皮吸收制剂中的应用概况

目的为透皮吸收制剂的研究与开发提供信息参考。方法查阅近年来国内外透皮吸收制剂研究论文，总结10种透皮吸收促进剂的研究报告。结果透皮吸收促进剂在透皮吸收制剂研究中的合理选择是影响药物透皮吸收的一个关键因素。结论透皮吸收促进剂在药物透皮吸收制剂研究和新药开发中有着广泛的应用前景。     

透皮吸收制剂的探讨

透皮吸收制剂量近年来药剂研究的主要课题之一。透皮制剂吸收的主要途径是药物穿透皮肤的汗孔或毛细血管进入血液循环而达到治疗目的。透皮制剂具有提高药物治疗效能。减少给药次数,降低副作用等特点,影响透皮吸收的因素很多,本文主要从皮肤渗透促进剂、软膏基质、以及皮肤因素三个方面进行了分析。现在透皮吸收制剂的研究正处方兴阶段不断新的理论和新的产品,透皮吸收制剂可望今后在防病、治疗方面发挥更大的作用。     

Effect of natural penetration enhancers on dermal delivery of hydrocortisone acetate

The purpose of the research work was to develop microemulsion (ME) of hydrocortisone acetate (HCA) using natural penetration enhancers and to determine its possibility in effective dermal delivery. Eucalyptus oil, clove oil and lemon grass oil were selected as natural penetration enhancers and pseudo-ternary phase diagrams were plotted using Tween 80 as surfactant and ethanol as cosurfactant. ME of each penetration enhancer was optimized using three factors, three levels Box–Behnken design, with independent variables as penetration enhancer, Tween 80 and ethanol. Formulations were assessed for percentage drug release as dependent variable. Response of these formulations decreased as the concentration of oil ranged from high to low and the response showed positive effect with increase in concentration of Tween 80 and ethanol. The globule size of optimized batches of eucalyptus oil, clove oil and lemon grass oil were found to be 226.1, 129.04 and 818.9 nm respectively. Optimized batches of MEs were then incorporated in carbopol 940 to form ME based gel without affecting their structure. Ex vivo permeation studies showed that amount of drug permeated from ME based gels was less than ME formulation indicating greater retention of HCA into skin layers. Retention of drug in skin layers both dermis and epidermis was higher for all three natural penetration enhancer. Hence natural penetration enhancers can be used for effective delivery of topical corticosteroids to the skin for improved treatment of several skin diseases and can be a better choice over synthetic penetration enhancers in terms of safety.     

山茶油对非甾体抗炎药经皮渗透的促进作用

目的考察山茶油对5种非甾体抗炎药体外经皮渗透的促进作用及其与药物油水分配系数的关系。方法采用两室扩散池装置,以离体大鼠腹部皮肤为渗透屏障,用预处理皮肤法考察山茶油的促渗透作用;用HPLC法测定非甾体抗炎药不同时间在接受池药物浓度,计算累积渗透量及其他渗透动力学参数;用摇瓶法测定药物正辛醇介质分配系数以拟合其与山茶油促渗活性关系。结果山茶油可有效促进非甾体抗炎药的经皮渗透率(除双氯芬酸钠外),尤其对氟比洛芬,促渗效果最明显(P<0.01),其增渗倍数达到3.51;山茶油的促渗活性与非甾体抗炎药的正辛醇介质分配系数呈类似抛物线关系。结论山茶油作为一种低毒、无刺激性的渗透促进剂,能够有效提高药物的经皮渗透效果,具有良好的开发应用前景。     

透皮促进剂对肤康祛斑凝胶体外透皮吸收的影响

目的考察透皮促渗剂对肤康祛斑凝胶的主药熊果苷体外经皮渗透的影响。方法对优化后的肤康祛斑凝胶处方,以大鼠离体皮肤作为渗透屏障,用高效液相色谱法测定凝胶中熊果苷经皮透入接收液含量。考察氮酮、氮酮-薄荷油、氮酮-冰片作为促渗剂对熊果苷透皮吸收的影响。结果肤康祛斑凝胶中熊果苷的体外累积渗透率符合Weibull分布,以氮酮-薄荷油作为促渗剂的处方中,熊果苷累积渗透率最高,渗透促进剂的促透效果为:氮酮-薄荷油>氮酮-冰片>氮酮。结论以氮酮-薄荷油作为促渗剂,对熊果苷有较好的促渗作用。     

中药药效物质基础研究的理论假说与方法

中药(单味药、复方)药效物质基础研究是目前中药现代化的关键。综述了中药药效物质基础研究的主要理论假说与方法,提出应充分重视中医药理论的指导作用;建立可靠、可信的中医症候动物模型;坚持临床疗效为中心等关键点,为研究中药药效物质基础提供依据。     

Investigating the potential of essential oils as penetration enhancer for transdermal losartan delivery: Effectiveness and mechanism of action

The effect of tea tree oil (TTO), cumin oil (CO), rose oil (RO) and aloe vera oil (AVO) on the skin permeation of losartan potassium (LP) was investigated. In vitro skin permeation studies were carried out using rat skin. The mechanism of skin permeation enhancement of LP by essential oils treatment was evaluated by FTIR, DSC, activation energy measurement and histopathological examination. Both concurrent ethanol/enhancer treatment and neat enhancer pretreatment of rat SC with all the oils produced significance increase in the LP flux over the control. The effectiveness of the oils as the penetration enhancers was found to be in the following descending order: AVO > RO > CO > TTO. However, only AVO was the only enhancer to provide target flux required to deliver the therapeutic transdermal dose of LP. FTIR and DSC spectra of the enhancer treated SC indicated that TTO, CO, RO and AVO increased the LP permeation by extraction of SC lipids. The results of thermodynamic studies and histopathological examination of AVO treated SC suggested additional mechanisms for AVO facilitated permeation i.e. transient reduction in barrier resistance of SC and intracellular transport by dekeratinization of corneocytes which may be attributed to the presence of triglycerides as constituents of AVO. It is feasible to deliver therapeutically effective dose of LP via transdermal route using AVO as penetration enhancer.     

非诺洛芬钙凝胶剂的制备及其体外透皮吸收研究

目的：对非诺洛芬钙凝胶剂制备,以及该剂型对小鼠皮肤的渗透作用进行研究。方法：建立了凝胶剂含量测定的三波长紫外法。结果：高分子辅料的种类、比例及透皮吸收促进剂的用量均对凝胶剂的物理性质有影响。首次发现,凝胶剂中加入２％按叶油为透皮吸收促进剂,其体外累积渗透量和渗透速率均最大。非诺洛芬钙凝胶剂的体外渗药动力学可用Ｈｉｇｕｃｈｉ方程来表述。结论：凝胶基质的最佳配比为５％Ｃａｐ与２０％ＰＶＡ（２∶１）混合。２％桉叶油可明显增加非诺洛芬钙凝胶剂的透皮吸收。     

Mechanism of In Vitro Percutaneous Absorption Enhancement of Carvedilol by Penetration Enhancers

The effect of penetration enhancers like tulsi (basil) oil, eucalyptus oil, clove oil, black cumin oil, oleic acid and Tween 80 on the percutaneous absorption of model lipophilic drug-carvedilol was investigated using excised rat abdominal skin. Transdermal flux, permeability coefficient and enhancement factor were calculated for each penetration enhancer. Black cumin oil (5% v/v) was selected on the basis of its highest enhancement in permeation and was evaluated further for its mode of action using DSC, FTIR and histological studies. The results indicated that the oil shows its action by extraction of lipids from stratum corneum as well as by loosening the hydrogen bonds between ceramides subsequently leading to fluidization of the lipid bilayer.     

Mechanism of in vitro percutaneous absorption enhancement of carvedilol by penetration enhancers

The effect of penetration enhancers like tulsi (basil) oil, eucalyptus oil, clove oil, black cumin oil, oleic acid and Tween 80 on the percutaneous absorption of model lipophilic drug-carvedilol was investigated using excised rat abdominal skin. Transdermal flux, permeability coefficient and enhancement factor were calculated for each penetration enhancer. Black cumin oil (5% v/v) was selected on the basis of its highest enhancement in permeation and was evaluated further for its mode of action using DSC, FTIR and histological studies. The results indicated that the oil shows its action by extraction of lipids from stratum corneum as well as by loosening the hydrogen bonds between ceramides subsequently leading to fluidization of the lipid bilayer.     

桉油对丙酸氮倍他索乳膏经皮渗透和吸收的作用

目的：考察促进剂桉油对丙酸氯倍他索（CBT）乳膏经皮渗透的促进作用,通过比较透过量和皮层中量,分析在该制剂中是否透合使用桉油,方法：采用直立式扩散池,考察了桉油在0．5％,1．0％,5．0％浓度下0．05％CBT乳膏经皮渗透2,4,6,8,10,24h后单位面积累积透过量Q(ug.cm^-2)和稳态透皮流量J（ug.cm^-2.h^-1);HPLC法测定经皮渗透24h后每克皮肤组织中CBT的量D（ug.g^-1),结果：4种浓度的桉油均显著促进CBT乳膏透皮吸收（P＜0．01）,其J值约是对照组的3－5倍（P＜0．01）,随浓度增加,陂层量D并不随之相应增加,结论：桉油可加快CBT经皮渗透速度,也能增加皮层中CBT量,但有饱和性,建议CBT 乳膏膏以少加（＜50％）或不加桉油为好。     

某院581例药品不良反应报告分析

目的：了解该院药品不良反应（ADR）的发生特点,促进临床合理用药。方法对该院2012—2013年上报的581例ADR 报告进行统计和分析。结果581例 ADR 报告中,男性290例,女性291例,基本持平;静脉给药方式引发的 ADR 最多,占总例数的72．81％,抗感染药物引起的 ADR 最多,占总例数的26．68％,其次为中药制剂,占总例数的17．21％;ADR 表现以皮肤及附件损伤最为常见,占总例数的28．92％;ADR 报告分类多为一般,占总数的91．57％。结论临床应重视药品不良反应的报告和监测工作,慎用中药制剂,合理使用抗感染药物,以减少 ADR 的发生。