正交试验法优选乳结消颗粒混合挥发油提取及包合工艺

摘 要 目的：优选乳结消颗粒中混合挥发油的提取及包合工艺。 方法: 采用正交试验,以提油量为指标,考察加水量、蒸馏时间、药材粉碎度对挥发油提取率的影响;以挥发油包合率和包合物得率综合评分,考察挥发油与β 环糊精（β CD）投料比、加水量和搅拌时间对包合工艺影响,并对挥发油包合物进行TLC 及UV 鉴别。 结果: 挥发油提取最佳工艺为加水10倍量,蒸馏提取3 h;最佳包合工艺采用水饱和法,β CD：挥发油8∶1,10倍量水,包合温度40 ℃,搅拌包合1 h。 结论: 挥发油被β CD 包合形成稳定的包合物,包合工艺稳定可行,为工业化生产提供参考。     

肉桂中挥发油提取及β-环糊精包合工艺研究

目的 研究黄连阿胶胶囊肉桂中挥发油的提取与包合工艺。方法 采用正交试验,以挥发油提取量为指标,优化最佳的提取工艺;以挥发油包合物得率为指标,考察影响挥发油包合工艺主要因素。结果 最佳提取工艺为饮片加水8倍量,浸泡2 h,提取4 h;最佳包合工艺为挥发油与β-环糊精比例为1∶6,加入溶剂量为1.5倍量,胶体碾磨时间为25 min。结论 优选出的工艺合理、可行。     

基于熵权法与响应面法优化香连和胃汤挥发油提取工艺

目的 筛选香连和胃汤中挥发油的最优提取工艺及包合工艺，提高挥发油的利用率。方法 以主要成分百秋李醇、桉油精、乙酸龙脑酯以及挥发油得率为指标，采用GC法测定有效成分含量，DX8trial软件设计试验方案，熵权法处理实验数据，最终筛选出挥发油最佳提取工艺；采用研磨法对挥发油进行包合，通过正交试验设计包合方案，逐一记录挥发油包合率、包合物收得率及包合物含油率3个指标，熵权法对指标进行权重分析，根据权重系数计算3个指标的综合评分，并筛选出最佳包合工艺。结果 挥发油最佳提取工艺：浸泡时间1.5 h，提取时间8 h，加水量为8倍水。最佳包合工艺：采用研磨法进行制备，β-CD-挥发油为6︰ 1，料液比为6︰ 1，研磨时间为0.5 h。结论 通过试验筛选的挥发油最佳提取工艺能提高香连和胃汤中挥发油的得率及有效成分含量，筛选所得最佳包合工艺，能有效包合香连和胃汤中的挥发油。     

当归、枳壳挥发油的提取与包合工艺研究

目的 优选当归和枳壳挥发油的提取工艺及β-环糊精包合工艺.方法 采用单因素考察法,以药材粉碎度、蒸馏时间、浸泡时间、加水量为考察因素,挥发油提取量为指标,优选其提取工艺.以挥发油包合率为指标,对饱和水溶液法、研磨法及超声法进行比较,采用正交实验法,优选出最佳包合工艺;并对包合物进行TLC及IR检验.结果 最佳提取工艺为药材粉碎成粗粉(20目),8倍量水,浸泡0.5h,提取5 h;最佳包合方法是研磨法,挥发油和β-环糊精的比例为1∶8(mL∶g),加4倍量的水,研磨3h.结论 本法确定的最佳提取与包合工艺,可有效地提取与保留当归和枳壳的活性成分挥发油,为其进一步研究打下基础.     

当归、川芎药对挥发油的提取及包合工艺研究

目的优化当归、川芎药对挥发油提取及包合工艺。方法以挥发油得率为指标,用单因素法对药材的粉碎度、浸泡时间、加水量、提取时间等因素进行考察。另以油利用率、包合物收得率、含油率为指标,用正交实验设计对包合工艺进行优选。结果药材以粉碎后、不浸泡、加10倍量水、煎煮6h为最佳提取工艺。包合最佳工艺为油(mL)与β-CD(g)的比例为1∶6,加30倍量的水,30℃条件下搅拌1h。结论该工艺对挥发油提取、包合效率较高,稳定可靠。     

化痰降气胶囊制备工艺研究

目的：优选化痰降气胶囊最佳制备工艺。方法：采用正交试验法，以浸膏得率及盐酸麻黄碱含量为指标，优选药材乙醇提取工艺；以挥发油含量为提取工艺筛选指标；以挥发油利用率和包合物收率为包合工艺评价指标。结果：药材提取最佳工艺为：以70％乙醇为提取溶媒，加液量8倍，提取2次，时间分别为2h，1h；挥发油最佳提取条件搭配为：10倍水，浸泡1h，提取4h，当归挥发油包合最佳工艺为：每1ml挥发油用10gβ-环湖精（β-CD），100ml水，60℃搅拌包合2h。结论：正交试验法为制备化痰降气胶囊提供依据。     

正交试验优选藏茴香挥发油的提取与包合工艺

目的:优选藏茴香挥发油的提取与包合工艺。方法:以加水量、提取时间、浸泡时间为因素,挥发油提取量为指标,通过正交试验优选挥发油提取工艺;以挥发油与β-环糊精(β-CD)的比例、包合温度、包合时间为因素,挥发油利用率、包合率、综合评分为指标,通过正交试验优选挥发油包合工艺。结果:最佳挥发油提取工艺为加6倍量水浸泡0.5 h,提取挥发油4 h;最佳挥发油包合工艺为挥发油与β-CD的比例为1∶8(V∶m),30℃下搅拌包合2 h。结论:优选的挥发油提取与包合工艺合理、可行,可用于藏茴香挥发油的提取与包合。     

桂龙巴布贴提取工艺考察

摘 要 目的：优选桂龙巴布贴的最佳提取工艺。方法: 采用单因素筛选法,以挥发油得量为指标,对挥发油提取工艺条件进行优选;采用单因素筛选法和正交设计法,以干浸膏得量和乌头类总生物碱含量的综合评分值为指标,对水提取工艺条件进行优选。结果: 挥发油提取工艺最优条件为加入药材量8倍的水,浸泡1 h后,加热回流提取6 h;水提取工艺最优条件为加水8倍量,提取3次,每次1 h。结论:优选得到的提取工艺简单、稳定、可行,为下一步研究奠定了良好的基础。     

正交试验优选浊淋清胶囊中牡丹皮挥发油的提取工艺及β-环糊精包合物的包合工艺

目的:优选浊淋清胶囊中牡丹皮挥发油的提取工艺及β-环糊精包合物的包合工艺。方法:采用正交试验法,以挥发油提取率为指标,粉碎粒度、浸泡时间、加水量为因素优选牡丹皮挥发油提取工艺;以挥发油利用率和包合物收率为指标,β-环糊精与挥发油的比例、包合温度、搅拌时间为因素优选β-环糊精包合工艺。结果:挥发油最佳提取工艺为药材粉碎粒度24目,加15倍量的水,浸泡30min;β-环糊精最佳包合工艺为加8倍量的β-环糊精,加热温度50℃,搅拌包合2h。结论:该工艺简单、快速,挥发油提取率及β-环糊精包合物中挥发油利用率、包合物收得率均较高,适合工业化生产。     

罗勒挥发油提取及β-环糊精包合物的制备

目的优选罗勒挥发油的提取及β-环糊精包合工艺。方法采用正交试验法,以浸泡时间、加水量、蒸馏时间为考察因素,以挥发油的体积为指标,筛选提取工艺。选择挥发油与β-环糊精比例、包合温度、搅拌时间3个因素进行正交试验,以包合率为指标,确定挥发油最佳包合工艺条件。结果最佳提取工艺为浸泡1h,蒸馏6h,10倍量水;最佳包合工艺为挥发油-β-环糊精（1：8）,40℃包合1．5h,包合率达到90．13％。结论提取及包合工艺稳定合理、可行。     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Synthesis and anti-nociceptive and anti-inflammatory effects of gaultherin and its analogs

The synthesis of gaultherin (1) and its analogs was carried out to provide 11 glycosides under phase-transfer catalytic conditions. The activities of all synthesized compounds were evaluated by nitric oxide production inhibitory assay in vitro. Methyl 2-O-(4-O-β-d-galactopyranosyl)-β-d-glucopyranosylbenzoate (5f) showed significantly anti-nociceptive and anti-inflammatory effects by the evaluation in vivo. Structure–activity relationships within these compounds were discussed.     

Modelling and simulation of variability and uncertainty in toxicokinetics and pharmacokinetics

Two important methodological issues within the framework of the variability and uncertainty analysis of toxicokinetic and pharmacokinetic systems are discussed: (i) modelling and simulation of the existing physiologic variability in a population; and (ii) modelling and simulation of variability and uncertainty when there is insufficient or not well defined (e.g. small sample, semiquantitative, qualitative and vague) information available. Physiologically based pharmacokinetic models are especially suited for separating and characterising the physiologic variability from the overall variability and uncertainty in the system. Monte Carlo sampling should draw from multivariate distributions, which reflect all levels of existing dependencies in the intact organism. The population characteristics should be taken into account. A fuzzy simulation approach is proposed to model variability and uncertainty when there is semiquantitative, qualitative and vague information about the model parameters and their statistical distributions cannot be defined reliably.     

成骨细胞的功能与损伤和骨质疏松的防治

骨质疏松是一种全身性骨骼疾病,导致骨折风险增加。成人的骨量通过破骨细胞的骨吸收和成骨细胞的骨形成作用来维持动态平衡,治疗骨质疏松症的理想策略是抑制破骨细胞的骨吸收和/或增强成骨细胞的骨形成功能。目前针对保护成骨细胞及增强其功能的骨质疏松疗法相对较少。因此,本文针对成骨细胞相关功能蛋白、各种细胞损伤机制（内质网应激、氧化应激、机械过载、微小RNA和长链非编码RNA的影响等）及骨质疏松的治疗与预防作一综述,以期为针对增强成骨细胞功能的骨质疏松治疗策略提供新思路。     

益生菌与肿瘤防治

益生菌广泛存在于自然界中,通过维持宿主体内菌群平衡、影响肠屏障功能和调节免疫应答等作用,提高宿主健康水平,被公认为"肠道健康卫士".一些益生菌可以增强机体的免疫功能,抑制致癌物质,影响肿瘤细胞的基因表达,对肿瘤具有拮抗作用.大量研究表明,益生菌在未来的肿瘤防治中有很好的应用和发展前景.     

Self-stimulation and amphetamine: Tolerance to d and l isomers and cross tolerance to cocaine and methylphenidate

The effects of the d and l isomers of amphetamine on self-stimulation responding were tested following acute and chronic administration. Tolerance and post-drug depression of responding occurred in tests with both isomers, indicating no role for p-hydroxynorephedrine (PHN) which is one of the metabolites of d-amphetamine. In the second experiment, d-amphetamine, methylphenidate and cocaine all produced quantitatively and qualitatively similar effects on self-stimulation responding following acute administration. Following chronic administration of d-amphetamine, animals showed tolerance to all three drugs, indicating cross-tolerance among them. These data are consistent with an hypothesis that tolerance and post-drug depression following chronic amphetamine treatment are the result of decreases in postsynaptic receptor sensitivity, which would lead to a decreased effectiveness of all three drugs, regardless of their pre-synaptic mechanisms.     

Acamprosate and naltrexone treatment effects on ethanol and sucrose seeking and intake in ethanol-dependent and nondependent rats

Rationale  Two pharmacotherapies are approved for treating alcohol craving (acamprosate and naltrexone), but both have shown mixed findings in animals and humans. Objectives  The present experiments utilized a “reinforcer blocking” approach (i.e., rats were able to consume ethanol during treatment) to better understand the efficacy of these treatments for ethanol seeking and drinking using ethanol-dependent and nondependent rats. Materials and methods  In “nondependent” experiments, drugs (acamprosate 50, 100, and 200 mg/kg; naltrexone 0.1, 0.3, and 1.0 mg/kg) were administered over 3-week periods prior to operant sessions with a low response requirement to gain access to reinforcers for 20 min. For “dependent” experiments, rats were made dependent in vapor/inhalation chambers. Results  Acamprosate and naltrexone had similar effects on intake in nondependent and dependent rats; neither drug was selective for ethanol over sucrose drinking. In nondependent animals, naltrexone was more efficacious at more doses than acamprosate, and acamprosate’s effects were limited to a dose that also had adverse effects on body weight. Both pharmacotherapies showed more selectivity when examining reinforcer seeking. In nondependent rats, acamprosate and naltrexone had response-attenuating effects in ethanol, but not sucrose, groups. In dependent animals, acamprosate had selective effects limited to a decrease in sucrose seeking. Naltrexone, however, selectively decreased ethanol-seeking in nondependent rats. Conclusions  The naltrexone-induced decreases in seeking suggested a change in incentive motivation which was selective for ethanol in nondependent rats. The “nondependent” paradigm may model early stages of “problem drinking” in humans, and the findings suggest that naltrexone could be a good intervention for this level of alcohol abuse and relapse prevention.     

Antiinfective and encrustation-inhibiting materials--myth and facts

Catheters, urethral and ureteral stents and other urological implants are frequently affected by encrustration and infection due to their permanent contact with urine. Indwelling urinary catheters provide a haven for microorganisms and thus require extensive monitoring. Several surface modification techniques have been proposed to improve the performance of devices including the immobilization of biomolecules, the incorporation of hydrophilic grafts to reduce protein adsorption, the creation of hydrophobic surfaces, the creation of microdomains to regulate cellular and protein adhesion, new polymers and antimicrobial coatings. Physico-chemical explanation to elucidate the mechanism of such encrustation or infection inhibiting materials is still not available. Our series of experiments showed a marked decrease of silver-activity in biological fluids which corresponds with the controversial clinical results obtained with silver coated urinary catheters. Rifampicin/minocycline coated catheters had very low activity against Gram-negative rods, enterococci and Candida spp., the main causing organisms of urinary catheter infection. Surface engineered materials and antimicrobial drug delivery systems will be the next generation of sophisticated urinary catheters and stents, if both efficacy as well as efficiency has been proved clinically.     

Alprazolam and lorazepam single and multiple-dose effects on psychomotor skills and sleep

Summary The effects of alprazolam 0.5 mg and lorazepam 2 mg on cognitive and psychomotor skills were assessed in twelve normal volunteer subjects in a randomised, double-blind, crossover design. Single and multiple dose effects were monitored using a battery of tests comprising critical flicker fusion threshold (CFFT), choice reaction time (CRT), simulated car tracking, and subjective ratings of perceived sedation (LARS) and of sleep behaviour (LSEQ). Compared with placebo baseline scores, treatment with lorazepam 2 mg (both single and multiple doses) resulted in a widespread impairment of CRT, tracking accuracy, and CFFT. Single doses of alprazolam 0.5 mg reduced CFFT with respect to the placebo baseline. Single and multiple dose treatment with both drugs resulted in subjective reports of sedation, a reduction of sleep onset latency, and improved sleep quality. Only lorazepam 2 mg significantly disrupted the integrity of behaviour on waking from sleep. These results suggest important pharmacodynamic differences between the two drugs in the doses used.