天麻指纹图谱的研究进展

天麻是我国名贵的中草药,随着近年来其商品的多样化,掺伪、假冒品不断增多,对其进行更全面、系统的质量控制尤为重要。目前,指纹图谱已成为国际公认的控制中药质量的有效手段之一,主要的研究方法有液相色谱法、薄层色谱法、毛细管电泳色谱、红外光谱、核磁共振、X射线粉末衍射、分子生物学指纹图谱和电化学指纹图谱等,本文对近年来天麻指纹图谱的研究情况进行了归纳总结,为进一步建立该药的质量控制提供了方法和依据。     

基于分子网络研究四逆散抗抑郁症作用的潜在生物学机制

目的 基于分子网络研究四逆散治疗抑郁症的潜在生物学机制。方法 借助于中药系统药理学数据库和分析平台（TCMSP）数据库筛选四逆散的活性成分,筛选条件为口服利用率、药物相似性和血脑屏障透过率,并挖掘四逆散活性成分靶点和抑郁症的治疗靶点。利用韦恩图找到活性成分靶点和疾病靶点的交集靶点,对应相应成分定义为四逆散抗抑郁的有效成分。利用String在线数据库进行交集靶点蛋白质-蛋白质相互作用网络的预测,并利用DAVID数据库进行交集靶点KEGG信号通路的富集分析。最后使用Cytoscape 3.6软件进行活性成分-靶点网络及有效成分-靶点-信号通路的构建和拓扑分析。结果 筛选出了四逆散107个有效成分和28个重要的抗抑郁症靶点。四逆散抗抑郁症的重要靶点显著富集于神经活性配体-受体相互作用、5-羟色胺能突触、多巴胺能突触、逆行内源性大麻素信号传导、钙信号通路等10个信号通路中。结论 本研究从分子网络的角度初步揭示了四逆散治疗抑郁症的潜在作用机制,其主要的生物学机制可能与以神经活性配体-受体相互作用为中心的信号通路有关。     

两种吸入剂对支气管哮喘患者肾上腺皮质功能、糖脂代谢的影响

目的探讨长期应用布地奈德福莫特罗吸入剂(160μg/4.5μg)对支气管哮喘患者的控制作用及对肾上腺皮质功能、糖脂代谢的影响。方法将78例支气管哮喘患者随机分成治疗组和对照组,治疗组给予布地奈德福莫特罗吸入剂(160μg/4.5μg),每日两次,对照组按需应用沙丁胺醇吸入剂,口服茶碱缓释片。观察周期为一年。两组患者在治疗前1天(T0)、一个月(T1)、三个月(T3)、六个月(T6)、12个月(T12),分别给予哮喘控制测试(asthma control test,ACT)评分,呼气峰流速(peak expiratory flow,PEF)日变异率检查,分别抽血测皮质醇、促肾上腺素皮质激素(ACTH),空腹血糖(FPG)、糖化血红蛋白(HbA1c)、甘油三酯、总胆固醇。结果治疗组患者ACT评分高于对照组(P0.05),治疗组患者PEF日变异率小于对照组(P0.05)。治疗组与对照组皮质醇、ACTH、FPG、HbA1c、总胆固醇、甘油三酯之间的差异无统计学意义(P0.05)。结论布地奈德福莫特罗吸入剂对支气管哮喘患者的控制有良好作用,长期应用对患者的肾上腺皮质功能、糖脂代谢无不良影响。     

Assessment of inhaler techniques employed by patients with respiratory diseases in southern Brazil: a population-based study

OBJECTIVE:

To identify incorrect inhaler techniques employed by patients with respiratory diseases in southern Brazil and to profile the individuals who make such errors.

METHODS:

This was a population-based, cross-sectional study involving subjects ≥ 10 years of age using metered dose inhalers (MDIs) or dry powder inhalers (DPIs) in 1,722 households in the city of Pelotas, Brazil.

RESULTS:

We included 110 subjects, who collectively used 94 MDIs and 49 DPIs. The most common errors in the use of MDIs and DPIs were not exhaling prior to inhalation (66% and 47%, respectively), not performing a breath-hold after inhalation (29% and 25%), and not shaking the MDI prior to use (21%). Individuals ≥ 60 years of age more often made such errors. Among the demonstrations of the use of MDIs and DPIs, at least one error was made in 72% and 51%, respectively. Overall, there were errors made in all steps in 11% of the demonstrations, whereas there were no errors made in 13%.Among the individuals who made at least one error, the proportion of those with a low level of education was significantly greater than was that of those with a higher level of education, for MDIs (85% vs. 60%; p = 0.018) and for DPIs (81% vs. 35%; p = 0.010).

CONCLUSIONS:

In this sample, the most common errors in the use of inhalers were not exhaling prior to inhalation, not performing a breath-hold after inhalation, and not shaking the MDI prior to use. Special attention should be given to education regarding inhaler techniques for patients of lower socioeconomic status and with less formal education, as well as for those of advanced age, because those populations are at a greater risk of committing errors in their use of inhalers.     

止痒袋泡洗剂联合止痒散外用治疗肛周湿疹的临床疗效

为探讨痒袋泡洗剂联合止痒散外用治疗肛周湿疹的临床疗效．将200例肛门湿疹患行随机分为对照组和治疗组,各100例。对照组单纯使用丁酸氧化可的松乳膏局部外涂治疗,治疗组在以止痒袋泡洗剂局部外洗治疗后,外涂止痒散,两组均以2同为一疗程。结果显示,治疗组痊愈72例（72．0%）,有效24例,无效4例．总在效率96．0％;对照组痊愈44例（44．0％）．有效47例,无效9例,总有效率91．0%。两组总在效率差异无统计学意义．P〉0．05;但治疗组治愈率明显高于对照组．P〈0．05。停约8周后,治疗组痊愈者复发32例（44．4%,32／72）．对照组复发33例（75．0%．33/14）．对照组复发率明显高于治疗组．P〈0．05。治疗组未出现不良反应,对照组有1例出现肛周局部烧灼感,未予处理,停药后症状消失。结果表明,止痒袋泡洗剂联合止痒散外用治疗肛周湿疹治愈率高,无不良反应。复发率低,值得临床推广应用。     

肠风散的镇痛作用及皮肤安全性研究

为研究肠风散的镇痛作用及皮肤急性毒性、皮肤刺激性和皮肤过敏反应,采用醋酸扭体法和热板法观察肠风散的镇痛作用;用ELISA法测定肛肠病术后疼痛模型大鼠血清白介素-6（IL-6）和白介素-10（IL-10）含量,研究镇痛作用机理;观察小鼠皮肤急性毒性反应、豚鼠皮肤刺激性和过敏反应,研究肠风散局部使用的皮肤安全性。结果显示,肠风散大、中剂量（分别为100％和50％）局部外涂能明显提高小鼠足底痛阈（P〈0．05或P〈0．01）,亦能明显抑制冰醋酸所致小鼠扭体反应（P〈0．05）;肠风散大、中剂量（分别为100％和50％）局部外涂能使肛肠病术后疼痛模型大鼠血清IL-6含量显著降低、IL-10含量明显升高（P〈O．05或P〈O．01）;肠风散经皮给药,未见明显急性毒性、皮肤刺激性及过敏反应。结果表明,肠风散局部给药具有一定的镇痛作用,局部皮肤给药安全性较高。     

理气开郁法板块方镇痛作用的动态分析

目的：探讨理气开郁法中药板块方的镇痛作用特点。方法：将150只清洁级昆明种小鼠,按体重随机区组法分为15组,包括对照组,柴郁汤、芍甘汤、痛泻要方、金铃子散高中低剂量各组,吗啡和布洛芬组,采用45℃、50℃、55℃水浴引致小鼠疼痛模型,动态测定痛阈潜伏期,用药前测定基础痛阈。采用重复测量设计的方差分析。结果：柴郁汤、芍甘汤和痛泻要方的镇痛作用以高剂量更明显;柴郁汤对45℃、50℃、55℃水浴的痛阈潜伏期均有延长作用,柴郁汤高、中剂量在多个时间点上显示出较好的镇痛作用。结论：柴郁汤的镇痛作用较强,作用特点类似于中枢镇痛药或兼有中枢性镇痛作用;芍药甘草汤、痛泻药方、金铃子散属于作用于外周的镇痛药。     

Dry powder inhalation: past,present and future

Introduction: Early dry powder inhalers (DPIs) were designed for low drug doses in asthma and COPD therapy. Nearly all concepts contained carrier-based formulations and lacked efficient dispersion principles. Therefore, particle engineering and powder processing are increasingly applied to achieve acceptable lung deposition with these poorly designed inhalers.

Areas covered: The consequences of the choices made for early DPI development with respect of efficacy, production costs and safety and the tremendous amount of energy put into understanding and controlling the dispersion performance of adhesive mixtures are discussed. Also newly developed particle manufacturing and powder formulation processes are presented as well as the challenges, objectives, and new tools available for future DPI design.

Expert opinion: Improved inhaler design is desired to make DPIs for future applications cost-effective and safe. With an increasing interest in high dose drug delivery, vaccination and systemic delivery via the lungs, innovative formulation technologies alone may not be sufficient. Safety is served by increasing patient adherence to the therapy, minimizing the use of unnecessary excipients and designing simple and self-intuitive inhalers, which give good feedback to the patient about the inhalation maneuver. For some applications, like vaccination and delivery of hygroscopic formulations, disposable inhalers may be preferred.     

Box-Behnken效应面法优化磷酸西格列汀片处方设计

目的：筛选磷酸西格列汀片直接压片法的最佳处方。方法：采用Box-Behnken效应面法（BBD）优化磷酸西格列汀片的处方设计,以原料药粒径、MCC占填充剂比例及崩解剂用量为考察因素,以休止角、均匀度、溶出度为评价指标,制备样品作质量考察。结果：最优处方原药粒径100 nm,MCC占填充剂比例为45%,崩解剂用量为2.7%。根据最优处方制备的小试样品,均匀度为（2.53±0.18）%,休止角为（38.9±0.5）°,10 min溶出度为（82.3±2.2）%,与理论值的差距＜10%。3批中试样品,各评价指标与理论值的差距均＜10%,符合质量要求。结论：通过BBD法优化的磷酸西格列汀片处方,具有良好的流动性、混合均匀度,制得片剂具有快速溶出特征。     

四逆散干预焦虑症作用机制的网络药理学分析

目的探讨四逆散干预焦虑症的功效作用网络及药效作用机制。方法运用网络药理学方法,多个数据库联合分析四逆散和焦虑症的作用靶点,通过Cytoscape筛选靶点并对其基因功能和信号通路进行分析,运用Bio GPS数据库对所得靶点进行器官定位。结果分析结果表明槲皮素、山柰酚、芍药苷等成分作用于SRC、EGFR、PIK3R1等靶点,通过ERBB2信号通路、EGFRv III信号通路、VEGFA-VEGFR2信号通路等共同发挥作用,器官定位结果表明作用的核心病位为肝。结论四逆散干预焦虑症体现了中药多成分、多靶点、多通路的作用特点。