Release profile

释放配置文件
  • 文章类型: Journal Article
    本文综述了包膜控释肥料开发的最新成果,其中包括农业的可持续性问题。在过去的几年中,由于食物和供应状况的复杂性逐年增加,研究界对这一特定科学领域的兴趣翻了一番。以及维持现代社会在人口爆发时代的发展。这篇综述涵盖了对所谓的“智能肥料”的新兴研究的及时系统化和综合分析的需求,这些研究根据对营养的需求释放矿物质成分,这些营养分为受控和缓释肥料(CRF和SRF)。除了在这一领域发表的经过精心挑选的基础研究,审查特别侧重于基于材料的分类,强调主体基质在掺杂剂的时间控制释放中的重要性。这大大区分了我们的评论,并使其具有科学新颖性和相关性。审查分为几个部分,处理缓释和控释肥料的类型,并补充了对它们使用的批判性观点。在熟悉该领域的最新成就时,为了方便读者,本评论中有关封装肥料的所有数据均已系统化。还描述了观点和潜在的途径,以推荐和指导在相关学术领域工作的研究人员。
    This review describes the latest achievements in the development of encapsulated controlled-release fertilizers, which encompasses sustainability issues in agriculture. The research community\'s interest in this particular area of science has doubled over the last couple of years due to the yearly increasing complexity of the food and supply situation, as well as maintaining the development of modern society in the era of population outbreak. This review covers demand in timely systematization and comprehensive analysis of emerging research in so-called \"smart fertilizers\" that release mineral components in accordance with the needs for nutrients classified into controlled- and slow-release fertilizers (CRFs and SRFs). Along with the thoroughly selected fundamental studies published in this area, the review specially focuses on the materials-based classification, emphasizing the importance of the host matrix in the time-controlled release of dopant. This substantially differentiates our review and renders scientific novelty and relevancy to it. The review is divided into sections, dealing with the types of slow- and controlled-release fertilizers each, and supplemented with the critical view on their usage. All data regarding encapsulated fertilizers in this review are systematized for the convenience of the readership when becoming familiarized with the latest achievements in this area. Perspectives and potential pathways are also described to recommend and guide researchers working on the related academic fields.
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  • 文章类型: Journal Article
    建议使用过氧化苯甲酰(BPO)和维甲酸联合治疗痤疮;但是,同时给药可能会有刺激性,BPO介导的维甲酸氧化可防止共制剂。在酒渣鼻,过氧化苯甲酰已被证明是有效的;然而,它的使用受到耐受性差的限制。为了克服这些限制,活性成分可以包封在二氧化硅微胶囊内。美国食品和药物管理局已经批准了2种使用该技术的产品,用于寻常痤疮的包封的过氧化苯甲酰和包封的维甲酸产品的组合和用于治疗酒渣鼻的炎性病变的包封的过氧化苯甲酰。活性成分通过二氧化硅壳中的小通道释放,逐渐向皮肤释放活性成分。这项研究描述了在生理相关条件下从二氧化硅壳中包封的维甲酸和包封的过氧化苯甲酰的稳定性和释放曲线,并提供了与传统制剂的区别。
    A combination of benzoyl peroxide (BPO) and tretinoin is recommended for treating acne; however, concurrent administration can be irritating, and coformulation is prevented by BPO-mediated oxidation of tretinoin. In rosacea, benzoyl peroxide has been shown to be efficacious; however, its use has been limited by poor tolerability. To overcome these limitations, the active ingredients can be encapsulated within silica microcapsules. The US Food and Drug Administration has approved 2 products using this technology, a combination of encapsulated benzoyl peroxide and encapsulated tretinoin product for acne vulgaris and encapsulated benzoyl peroxide to treat inflammatory lesions in rosacea. The active ingredients are released through small channels in the silica shell, gradually releasing the active ingredients to the skin. This study describes the stability and release profiles of encapsulated tretinoin and encapsulated benzoyl peroxide from the silica shell in physiologically relevant conditions and provides differentiation from traditional formulations.
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  • 文章类型: Journal Article
    刺槐花提取物含有各种多酚,它们的葡糖苷有助于潜在的健康益处。摄入这些生物活性化合物并通过胃肠道后,它们的降解可能发生并导致生物活性的丧失。为了克服这个问题,生物活性化合物应该被保护免受环境条件的影响。本研究旨在将黑花提取物封装在基于可生物降解多糖的微粒中,海藻酸盐,和壳聚糖。在摘录中,发现总抗氧化剂含量为每100克干重3.18±0.01克没食子酸当量。此外,脂质的存在(16),酚类物质(27),有机酸(4),L-天冬氨酸衍生物,Questinol,赤霉素,甾醇,和皂苷(2)使用UHPLC-ESI-MS分析确认。体外实验表明,该提取物对HeLa细胞系具有弱的抗α-葡萄糖苷酶活性和中等的抗氧化和细胞毒活性。使用二次气流的挤出方法能够制备用提取物包封的微粒(约270μm)。在藻酸盐和藻酸盐-壳聚糖微粒中实现了超过92%的包封效率。溶胀研究证实,与藻酸盐微粒相比,藻酸盐-壳聚糖微粒的渗透性较低。对于这两种类型的微粒,在37°C下模拟胃肠液中抗氧化剂的释放曲线遵循Korsmeyer-Peppas模型。低于0.5的扩散系数表明抗氧化剂的简单Fick扩散。与藻酸盐微粒相比,藻酸盐-壳聚糖微粒能够更持续地从提取物释放抗氧化剂。获得的结果表明,通过包封在聚合物基质中,提取物中的生物活性化合物的抗氧化活性得到了改善,并且在模拟的胃条件下保护它们免受降解。与藻酸盐系统相比,藻酸盐-壳聚糖显示出从微粒中累积抗氧化剂释放的速度稍慢,并且提取物的抗氧化活性更好。根据这些结果,海藻酸盐-壳聚糖微粒更适合进一步应用于刺槐花提取物的包封。此外,所提出的作为药物递送系统的聚合物基质由于其可生物降解性和无毒性而对人类使用是安全的。
    Black locust flower extract contains various polyphenols and their glucosides contribute to the potential health benefits. After intake of these bioactive compounds and passage through the gastrointestinal tract, their degradation can occur and lead to a loss of biological activity. To overcome this problem, the bioactive compounds should be protected from environmental conditions. This study aimed to encapsulate the black flower extract in the microparticles based on biodegradable polysaccharides, alginate, and chitosan. In the extract, the total antioxidant content was found to be 3.18 ± 0.01 g gallic acid equivalent per 100 g of dry weight. Also, the presence of lipids (16), phenolics (27), organic acids (4), L-aspartic acid derivative, questinol, gibberellic acid, sterol, and saponins (2) was confirmed using the UHPLC-ESI-MS analysis. In vitro assays showed that the extract has weak anti-α-glucosidase activity and moderate antioxidant and cytotoxic activity against the HeLa cell line. The extrusion method with secondary air flow enabled the preparation of microparticles (about 270 μm) encapsulated with extract. An encapsulation efficiency of over 92% was achieved in the alginate and alginate-chitosan microparticles. The swelling study confirmed a lower permeability of alginate-chitosan microparticles compared with alginate microparticles. For both types of microparticles, the release profile of antioxidants in the simulated gastrointestinal fluids at 37 °C followed the Korsmeyer-Peppas model. A lower diffusion coefficient than 0.5 indicated the simple Fick diffusion of antioxidants. The alginate-chitosan microparticles enabled a more sustained release of antioxidants from extract compared to the alginate microparticles. The obtained results indicated an improvement in the antioxidant activity of bioactive compounds from the extract and their protection from degradation in the simulated gastric conditions via encapsulation in the polymer matrixes. Alginate-chitosan showed slightly slower cumulative antioxidant release from microparticles and better antioxidant activity of the extract compared to the alginate system. According to these results, alginate-chitosan microparticles are more suitable for further application in the encapsulation of black locust flower extract. Also, the proposed polymer matrix as a drug delivery system is safe for human use due to its biodegradability and non-toxicity.
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  • 文章类型: Journal Article
    具有不同物理化学性质的分子的封装(茶碱,蓝色右旋糖酐,研究了口服乳清蛋白(WP)和藻酸盐(ALG)微粒(MP)中的水杨酸和胰岛素)。通过冷胶凝技术制备基于WP/ALG的MP,并在网状化后用WP溶液涂覆。分子影响聚合物溶液的粘度和弹性,导致封装效率的差异(从23%到100%),MP结构和溶胀(>10%)以及就pH而言测试。分子释放是由于MP的扩散和/或侵蚀,并且非常依赖于包封的物质。所有装载的MP均已成功涂覆,但是涂层厚度的变化(从68到146µm)和包封的分子的功能导致分子释放的差异(1小时内5%至80%)。凝胶流变改性,由于WP之间的相互作用,ALG,钙和其他物质,是造成突出差异的原因。为了成功开发具有最佳生物制药特性的载体,在挤出和网状化之前测量流变参数似乎是研究的最重要方面之一。我们的载体似乎更适合阴离子高分子量物质,导致高粘度和弹性,并导致MP,从而在肠道pH值下实现胃抗性和分子的受控释放。
    The encapsulation of molecules with different physicochemical properties (theophylline, blue dextran, salicylic acid and insulin) in whey protein (WP) and alginate (ALG) microparticles (MP) for oral administration was studied. MP based on WP/ALG were prepared by a cold gelation technique and coated with WP solution after reticulation. Molecules influenced polymer solution viscosity and elasticity, resulting in differences regarding encapsulation efficiency (from 23 to 100%), MP structure and swelling (>10%) and in terms of pH tested. Molecule release was due to diffusion and/or erosion of MP and was very dependent on the substance encapsulated. All the loaded MP were successfully coated, but variation in coating thickness (from 68 to 146 µm) and function of the molecules encapsulated resulted in differences in molecule release (5 to 80% in 1 h). Gel rheology modification, due to interactions between WP, ALG, calcium and other substances, was responsible for the highlighted differences. Measuring rheologic parameters before extrusion and reticulation appeared to be one of the most important aspects to study in order to successfully develop a vector with optimal biopharmaceutical properties. Our vector seems to be more appropriate for anionic high-molecular-weight substances, leading to high viscosity and elasticity and to MP enabling gastroresistance and controlled release of molecules at intestinal pH.
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  • 文章类型: Journal Article
    一般来说,NSAID在水中是弱溶解的并且含有亲水和疏水基团。最广泛使用的NSAIDs之一是布洛芬,其具有差的溶解度和高的渗透性。通过创建动态,非共价的,水溶性包合物,环糊精(CD)可以提高低水溶性药物的溶出度,作为药物输送工具,此外,显着有助于药物的化学稳定性和减少药物相关的烦躁。为了改善布洛芬的药理和药代动力学特征,布洛芬的新噻唑烷-4-酮衍生物(4b,4g,4k,4m)与β-CD络合,使用共沉淀和冷冻干燥。新的β-CD复合物(β-CD-4b,β-CD-4g,β-CD-4k,β-CD-4m)使用扫描电子显微镜(SEM)进行表征,差示扫描量热法(DSC),X射线衍射和相溶解度测试。使用YASARA结构软件中包含的AutoDock-VINA算法,我们研究了布洛芬衍生物与β-CD的结合构象并测量了结合能。我们还对布洛芬衍生物和相应的β-CD复合物进行了体内生物学评估,使用镇痛/抗炎试验,以及发布简介。结果支持β-CD复合物(β-CD-4b,β-CD-4g,β-CD-4k,β-CD-4m)与布洛芬衍生物(4b,4g,4k,4m)。此外,β-CD复合物表现出延迟释放曲线,这提供了对药物输送领域的宝贵见解,专注于布洛芬衍生物。
    Generally, NSAIDs are weakly soluble in water and contain both hydrophilic and hydrophobic groups. One of the most widely used NSAIDs is ibuprofen, which has a poor solubility and high permeability profile. By creating dynamic, non-covalent, water-soluble inclusion complexes, cyclodextrins (CDs) can increase the dissolution rate of low aqueous solubility drugs, operating as a drug delivery vehicle, additionally contributing significantly to the chemical stability of pharmaceuticals and to reducing drug-related irritability. In order to improve the pharmacological and pharmacokinetics profile of ibuprofen, new thiazolidin-4-one derivatives of ibuprofen (4b, 4g, 4k, 4m) were complexed with β-CD, using co-precipitation and freeze-drying. The new β-CD complexes (β-CD-4b, β-CD-4g, β-CD-4k, β-CD-4m) were characterized using scanning electronic microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction and a phase solubility test. Using the AutoDock-VINA algorithm included in YASARA-structure software, we investigated the binding conformation of ibuprofen derivatives to β-CD and measured the binding energies. We also performed an in vivo biological evaluation of the ibuprofen derivatives and corresponding β-CD complexes, using analgesic/anti-inflammatory assays, as well as a release profile. The results support the theory that β-CD complexes (β-CD-4b, β-CD-4g, β-CD-4k, β-CD-4m) have a similar effect to ibuprofen derivatives (4b, 4g, 4k, 4m). Moreover, the β-CD complexes demonstrated a delayed release profile, which provides valuable insights into the drug-delivery area, focused on ibuprofen derivatives.
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  • 文章类型: Journal Article
    这项研究的目的是评估五种不同蜂蜜(一种新西兰麦卢卡和两种西澳大利亚蜂蜜,Jarrah蜂蜜和沿海薄荷蜂蜜)及其相应的载有蜂蜜的凝胶配方,使用定制设计的Franz型扩散池与高效薄层色谱法(HPTLC)相结合。要验证自定义设置的适用性,使用这种新方法的发布数据与使用商业弗朗兹细胞设备获得的数据进行了比较,这是一个既定的分析工具,用于监测活性成分从局部半固体产品的释放。发现在两种类型的Franz细胞中,纯蜂蜜和载有蜂蜜的制剂中活性化合物的释放曲线相当。例如,当从纯蜂蜜或其相应的预凝胶制剂中释放时,两种Jarrah蜂蜜成分的释放百分比,由RF0.21和0.53处的不同波段表示,并由HPTLC分析,在12小时时没有显着差异(p=0.9986),两个设备中都释放了超过99%的蜂蜜成分。与商用Franz扩散池相比,定制的弗朗兹细胞提供了几个优点,包括简单方便的示例应用程序,只有少量样品的要求,大的扩散表面积,在一个实验中分析20个样品的能力,与购买商业弗朗兹电池相比,成本更低。因此,新开发的方法与HPTLC联用有助于监测纯蜂蜜和载有蜂蜜的半固体制剂中次要蜂蜜成分的释放情况,也可能适用于其他复杂的基于天然产品的产品。
    The aim of this study was to assess the release profile of components in five different honeys (a New Zealand Manuka and two Western Australian honeys, a Jarrah honey and a Coastal Peppermint honey) and their corresponding honey-loaded gel formulations using a custom-designed Franz-type diffusion cell in combination with High-Performance Thin-Layer Chromatography (HPTLC). To validate the suitability of the customised setup, release data using this new approach were compared with data obtained using a commercial Franz cell apparatus, which is an established analytical tool to monitor the release of active ingredients from topical semisolid products. The release profiles of active compounds from pure honey and honey-loaded formulations were found to be comparable in both types of Franz cells. For example, when released either from pure honey or its corresponding pre-gel formulation, the percentage release of two Jarrah honey constituents, represented by distinct bands at RF 0.21 and 0.53 and as analysed by HPTLC, was not significantly different (p = 0.9986) at 12 h with over 99% of these honey constituents being released in both apparatus. Compared to the commercial Franz diffusion cell, the customised Franz cell offers several advantages, including easy and convenient sample application, the requirement of only small sample quantities, a large diffusion surface area, an ability to analyse 20 samples in a single experiment, and lower cost compared to purchasing a commercial Franz cell. Thus, the newly developed approach coupled with HPTLC is conducive to monitor the release profile of minor honey constituents from pure honeys and honey-loaded semisolid formulations and might also be applicable to other complex natural-product-based products.
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  • 文章类型: Journal Article
    为了使药物的有效性和安全性达到最佳水平,有必要控制药物释放速率。因此,重要的是发现影响药物递送系统释放曲线的因素。几何形状是片剂形药物递送系统的这些有效因素之一。在这项研究中,已经尝试回答片剂的几何形状如何影响药物释放曲线的一般问题。为此,茶碱从两百片HPMC片剂中的药物释放过程,在口服片剂的生产中被分为八组常见的几何形状,使用有限元分析进行了模拟。使用包括偏最小二乘回归和ANOVA检验的统计方法进行这些模拟结果的分析。结果表明,可以通过了解片剂的几何类型和尺寸来预测药物释放曲线,而无需进行大量的溶出测试。另一个结果是,尽管在许多先前的研究中,几种具有不同几何形状的片剂的药物释放曲线的差异仅通过与表面相关的变量来解释,结果表明,无论几何形状的类型和尺寸如何,不可能准确预测药物释放曲线。此外,结果表明,药物的剂量和片剂的成分没有任何变化,只是因为几何类型的差异,片剂的释放曲线显着不同。这发生在这样一种方式,例如,从具有相同质量和材料但不同几何形状的两个片剂中整个药物质量的释放时间可以相差约7倍。
    In order to achieve the optimal level of effectiveness and safety of drugs, it is necessary to control the drug release rate. Therefore, it is important to discover the factors affecting release profile from a drug delivery system. Geometry is one of these effective factors for a tablet-shaped drug delivery system. In this study, an attempt has been made to answer a general question of how the geometry of a tablet can affect the drug release profile. For this purpose, the drug release process of theophylline from two hundred HPMC-based tablets, which are categorized into eight groups of common geometries in the production of oral tablets, was simulated using finite element analysis. The analysis of the results of these simulations was carried out using statistical methods including partial least squares regression and ANOVA tests. The results showed that it is possible to predict the drug release profile by knowing the geometry type and dimensions of a tablet without performing numerous dissolution tests. Another result was that, although in many previous studies the difference in the drug release profile from several tablets with different geometries was interpreted only by variables related to the surface, the results showed that regardless of the type of geometry and its dimensions, it is not possible to have an accurate prediction of the drug release profile. Also, the results showed that without any change in the dose of the drug and the ingredients of the tablet and only because of the difference in geometry type, the tablets significantly differ in release profile. This occurred in such a way that, for example, the release time of the entire drug mass from two tablets with the same mass and materials but different geometries can be different by about seven times.
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  • 文章类型: Journal Article
    Bacterial infections constitute a threat to public health as antibiotics are becoming less effective due to the emergence of antimicrobial resistant strains and biofilm and persister formation. Antimicrobial peptides (AMPs) are considered excellent alternatives to antibiotics; however, they suffer from limitations related to their peptidic nature and possible toxicity. The present review critically evaluates the chemical characteristics and antibacterial effects of lipid and polymeric AMP delivery systems and coatings that offer the promise of enhancing the efficacy of AMPs, reducing their limitations and prolonging their half-life. Unfortunately, the antibacterial activities of these systems and coatings have mainly been evaluated in vitro against planktonic bacteria in less biologically relevant conditions, with only some studies focusing on the antibiofilm activities of the formulated AMPs and on the antibacterial effects in animal models. Further improvements of lipid and polymeric AMP delivery systems and coatings may involve the functionalization of these systems to better target the infections and an analysis of the antibacterial activities in biologically relevant environments. Based on the available data we proposed which polymeric AMP delivery system or coatings could be profitable for the treatment of the different hard-to-treat infections, such as bloodstream infections and catheter- or implant-related infections.
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  • 文章类型: Journal Article
    含药口香糖(MCG)代表了实现用于牙科预防和治疗的药物的有益平台。本研究旨在研究压缩力对机械的影响,纹理,释放,盐酸溶菌酶(LH)和抗坏血酸(AsA)组合的可压缩MCG的咀嚼感知特性。在实验室单冲压片机上施加不同的力获得了四批MCGs,即,5、7、10和15kN,并通过它们的几何参数进行评估,机械阻力,表面和内部结构特征,纹理轮廓,释放行为,咀嚼过程中的感知属性。发现增加压缩力轻微影响MCG的抗压碎性和脆性,但导致表面平滑和形成较厚的层与高度压实的颗粒排列。根据纹理分析,压缩力的增加导致牙龈更硬,更粘,表明咀嚼可能有困难,因此,损害他们的消费者财产。还发现,就从所获得的口香糖中更好地释放药物而言,较低的压缩力是优选的。志愿者的评估表明,压缩力的增加导致初始硬度和脆性显着提高,并降低了咀嚼过程中整体口香糖质量形成的速率。当使用MCG时,这可能会对感知感觉产生负面影响。根据获得的结果,最佳压缩力选择为7kN,这允许获得具有良好感官的MCGs,机械,纹理,和释放属性。
    Medicated chewing gums (MCGs) represent a beneficial platform for realizing drugs intended for dental prophylaxis and treatment. The present study aimed to investigate the impact of compression force on the mechanical, textural, release, and chewing perception characteristics of compressible MCGs with the combination of lysozyme hydrochloride (LH) and ascorbic acid (AsA). Four batches of MCGs were obtained on a laboratory single-punch tablet machine applying different forces, i.e., 5, 7, 10, and 15 kN, and evaluated by their geometrical parameters, mechanical resistance, surface and internal structure characteristics, texture profile, release behavior, and perception attributes during mastication. It was found that increasing compression force slightly affected resistance to crushing and friability of MCGs, but resulted in surface smoothing and formation of a thicker layer with highly compacted particle arrangement. According to the texture analysis, increasing compression force led to harder and more adhesive gums, indicating possible difficulties in chewing and, therefore, impairment of their consumer properties. Lower compression forces were also found to be preferable in terms of better drug release from the obtained chewing gums. The volunteers\' assessment showed that an increase of compression force led to significantly raising the initial hardness and crumbliness as well as to decreasing the rate of the integral gum mass formation during mastication, which may negatively affect perceptive sensations when using MCGs. Based on the results obtained, the optimal compressing force was selected to be 7 kN, which allows obtaining MCGs with good organoleptic, mechanical, textural, and release properties.
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  • 文章类型: Journal Article
    二氟尼柳是一种众所周知的治疗类风湿性关节炎的药物,骨关节炎,原发性痛经,还有结肠癌.该分子属于非甾体抗炎药(NSAID),因此具有严重的副作用,如心血管疾病的风险发展,肾损伤,和肝脏反应。最后的临床数据表明,二氟尼柳是公认的治疗心脏淀粉样变性的药物之一,具有与临床批准的tafamidis相似的生存益处。二氟尼柳可稳定运甲状腺素蛋白(TTR)四聚体,并防止单体和二聚体的错误折叠在心脏中形成淀粉样蛋白沉积物。为了避免二氟尼柳的严重副作用,已经开发了各种输送系统。在本次审查中,关注二氟尼盐装载输送系统的最新发展,其技术,释放配置文件,和有效性。
    Diflunisal is a well-known drug for the treatment of rheumatoid arthritis, osteoarthritis, primary dysmenorrhea, and colon cancer. This molecule belongs to the group of nonsteroidal anti-inflammatory drugs (NSAID) and thus possesses serious side effects such as cardiovascular diseases risk development, renal injury, and hepatic reactions. The last clinical data demonstrated that diflunisal is one of the recognized drugs for the treatment of cardiac amyloidosis and possesses a survival benefit similar to that of clinically approved tafamidis. Diflunisal stabilizes the transthyretin (TTR) tetramer and prevents the misfolding of monomers and dimers from forming amyloid deposits in the heart. To avoid serious side effects of diflunisal, the various delivery systems have been developed. In the present review, attention is given to the recent development of diflunisal-loaded delivery systems, its technology, release profiles, and effectiveness.
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