液体型缓控释注射剂的研究进展

按照注射液中粒子大小对液体型缓、控释注射剂进行分类，概述了缓控释注射剂的发展与基本特点，着重阐述在体凝胶、纳米囊、纳米粒、乳剂及微球、微囊等注射剂的制备方法、释药特性。液体型缓、控释注射剂作为一种新型药物输注系统，是国内外药物制剂研究的一个重要方向，具有广阔的开发前景。     

药物制剂中薄膜包衣微丸的研究与应用

综述近年来薄膜包衣微丸在药物制剂中的研究与应用。微丸属于多单元型药物传递系统，具有众多优点。而将微丸制备技术和薄膜包衣技术相结合制成的具有特殊释药性质的薄膜包衣微丸，已经成为缓、控释制剂研究领域的热点。     

新型缓(控)释骨架片的研究进展

缓控释片剂是口服缓、控释制剂的重要组成．加快研制和推广新剂型和新技术在口服缓控释片中的应用显得相当重要。传统的骨架片按制剂骨架材料的不同可分为不溶性骨架缓控释片、亲水凝胶骨架缓控释片、蜡质骨架缓控释片以及混合材料骨架缓控释片4种。其中。亲水凝胶骨架缓控释片可作为可溶性药物和难溶性药物的载体．是目前口服缓、控释制剂的主要类型之一．约占上市骨架片品种的60％。70％。与一般骨架片相比．新型骨架片主要是在制备工艺方面进行了改进．通过多层骨架缓控释技术、几何异型骨架技术等方式使药物实现定速、定位、定时释放的目的。以下就新型骨架缓控释技术在片剂中的应用和研究现状加以概述：     

缓控释微丸制剂的研究进展

缓控释微丸制剂是一种多单元型给药系统，具有一单元型给药系统不可比拟的优点，成为目前缓控释制剂研究的热点。本文对缓控释微丸制剂包括骨架型微丸、膜控型微丸和骨架膜控两种技术结合制备的微丸的特点、所选用的材料及调节药物释放的方法等方面的研究进展进行了综述．并展望了微丸制剂的发展前景。     

粒径均一单分散载药微球的制备技术及其应用

制备粒径均一、单分散、生物可降解的载药微球对于研发缓控释注射微球具有重要的应用价值.本文重点阐述了在制备粒径均一的单分散微球方面已取得成绩的SPG膜乳化法、微流体技术、电喷雾法和声波激发雾化法的技术原理、应用现状、影响因素、技术要点及尚存在的问题等.     

ZnS-壳聚糖海藻酸钠包裹布洛芬纳米微球的制备和性能研究

目的以壳聚糖-海藻酸钠为基质材料,掺杂入纳米ZnS包裹非甾体抗炎药物布洛芬,制备缓、控释性能优异的载药纳米微球;为研发四代新剂型打下基础。方法利用复凝聚法,通过调整添加基质材料速度、反应温度、搅拌速度等,制备含ZnS的壳聚糖海藻酸钠布洛芬纳米微球,透射电镜观察纳米微球的形态,测试纳米微球的载药量与包封率,拟肠液条件下测试所致纳米微球的释放特性。结果含ZnS壳聚糖海藻酸钠布洛芬纳米载药微球的粒径约为80~100nm,载药量为40.2%药物包封率78.2%,ZnS粒径3nm。在水溶液、0.9%NaCl和磷酸盐缓冲液中的吸水膨胀程度小于不含ZnS的载药纳米微球;体外拟肠条件溶出表明含ZnS的载药纳米微球具有良好的缓控释性能,药代动力学特征为被动扩散。结论掺入了ZnS的壳聚糖海藻酸钠布洛芬纳米微球,形状圆整,包封率理想,具有良好的缓控释性能。     

影响亲水凝胶骨架系统中药物释放的因素

近年来利用骨架系统调节药物释放成为口服缓控释技术的研究热点之一,而亲水性聚合物在缓释骨架的制备中得到了广泛的使用。概述亲水凝胶骨架系统中药物释放的影响因素,包括药物、聚合物、处方和制备过程等,以期为优化亲水凝胶缓释骨架的处方和制备工艺提供参考。     

化学合成的生物降解聚合物在医药领域的应用进展

系统综述了化学合成的生物降解聚合物作为缓控释注射剂,如微球、嵌段共聚物胶束、凝胶等和埋植剂骨架材料的应用进展,并简要介绍了其在医用器械中的应用.     

口服液体缓控释制剂技术的研究进展

目的 针对各类口服液体缓控释技术的释药机理、应用特点及局限性进行综述,为此类制剂的开发提供参考。方法 查阅国内外相关文献,对口服液体缓控释技术进行整理归纳。结果 目前已有基于离子交换树脂和微囊技术的口服液体缓控释制剂上市,此外,微球、固体脂质纳米粒、原位凝胶等技术也应用于口服液体缓控释制剂领域。结论 口服液体缓控释给药系统相比于传统固体缓控释制剂,因其口服可接受性良好,剂量调整灵活,给药依从性优势明显,具有良好的开发应用前景。     

缓控释微丸制备方法的研究进展

缓控释微丸制剂是一种多单元型给药系统,具有单一给药系统无法比拟的优点,成为目前缓控释制剂研究的热点。本文对缓控释微丸制剂的制备方法包括冻干制粒法,挤出滚圆法,离心造粒制丸法等方法的研究进展进行了综述,并对微丸制剂制备方法的未来前景进行展望。     

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。     

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.     

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.     

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.