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Preparation and characterization of poly(ethylene) oxide/zinc oxide nanofibrous scaffold for chronic wound healing applications. 用于慢性伤口愈合的聚(乙烯)氧化物/氧化锌纳米纤维支架的制备和表征。
Q3 Medicine Pub Date : 2020-01-01 DOI: 10.17219/pim128378
H. Nosrati, M. Khodaei, Mehdi Banitalebi-Dehkordi, M. Alizadeh, Shiva Asadpour, E. Sharifi, J. Ai, Mostafa Soleimannejad
BACKGROUND Skin, the first barrier to pathogens, loses its integrity and function after an injury. The presence of an antibacterial dressing at the wound site may prevent bacterial invasion and also improve the healing process. OBJECTIVES The current study aimed to fabricate a biomimetic membrane with antibacterial properties for healing chronic wounds. MATERIAL AND METHODS The membranes, fabricated through electrospinning, are comprised of polyethylene oxide (PEO) and zinc oxide nanoparticles (ZnO-NPs) as the main biomaterial and antibacterial agent, respectively. Antibacterial activity, cell attachment and viability were tested to evaluate the biological properties of the membranes. The optimal cell compatible concentration of ZnO-NPs was determined for further studies. In vitro characterization of the membranes was performed to confirm their suitable properties for wound healing. RESULTS The antibacterial PEO/ZnO-NP membrane containing 2% of nanoparticles showed no cell toxicity, and human fibroblast cells were able to adhere and proliferate on the scaffold. The in vitro results from the tensile test, wettability, porosity, and protein adsorption revealed appropriate properties of the membrane as a scaffold for skin tissue engineering. CONCLUSIONS Synthetic polymers have been widely used for tissue engineering applications. The proper characteristics of PEO nanofibers, including a high ratio of surface/volume, moderate hydrophilicity and good mechanical properties, make this polymer interesting for skin regeneration. The results demonstrate the potential of the antibacterial PEO/ZnO-NP membrane to be used as an engineered scaffold to improve the wound healing process.
皮肤是病原体的第一道屏障,在受伤后失去了完整性和功能。在伤口部位使用抗菌敷料可以防止细菌入侵,也可以改善愈合过程。目的制备具有抗菌性能的仿生膜,用于慢性伤口的愈合。材料与方法采用静电纺丝法制备的聚氧聚乙烯(PEO)和氧化锌纳米颗粒(ZnO-NPs)分别作为主要生物材料和抗菌剂。通过抗菌活性、细胞附着和活力测试来评价膜的生物学特性。为进一步研究确定ZnO-NPs的最佳细胞相容浓度。对膜进行了体外表征,以确定其适合伤口愈合的性能。结果含2%纳米颗粒的抗菌PEO/ZnO-NP膜无细胞毒性,人成纤维细胞能在支架上粘附和增殖。体外拉伸试验、润湿性、孔隙度和蛋白质吸附的结果表明,该膜具有作为皮肤组织工程支架的合适性能。结论合成聚合物在组织工程中具有广泛的应用前景。PEO纳米纤维具有高的表面/体积比、中等亲水性和良好的机械性能,这使得这种聚合物对皮肤再生很有兴趣。结果表明,抗菌PEO/ZnO-NP膜具有作为工程支架改善伤口愈合过程的潜力。
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引用次数: 7
Preparation and characterization of poly(ethylene oxide)/zinc oxide nanofibrous scaffold for chronic wound healing applications. 慢性伤口愈合用聚环氧乙烷/氧化锌纳米纤维支架的制备与表征。
Q3 Medicine Pub Date : 2020-01-01 DOI: 10.17219/pim/128378
Hamed Nosrati, Mohammad Khodaei, Mehdi Banitalebi-Dehkordi, Morteza Alizadeh, Shiva Asadpour, Esmaeel Sharifi, Jafar Ai, Mostafa Soleimannejad

Background: Skin, the first barrier to pathogens, loses its integrity and function after an injury. The presence of an antibacterial dressing at the wound site may prevent bacterial invasion and also improve the healing process.

Objectives: The current study aimed to fabricate a biomimetic membrane with antibacterial properties for healing chronic wounds.

Material and methods: The membranes, fabricated through electrospinning, are comprised of poly(ethylene oxide) (PEO) and zinc oxide nanoparticles (ZnO-NPs) as the main biomaterial and antibacterial agent, respectively. Antibacterial activity, cell attachment and viability were tested to evaluate the biological properties of the membranes. The optimal cell compatible concentration of ZnO-NPs was determined for further studies. In vitro characterization of the membranes was performed to confirm their suitable properties for wound healing.

Results: The antibacterial PEO/ZnO-NP membrane containing 2% of nanoparticles showed no cell toxicity, and human fibroblast cells were able to adhere and proliferate on the scaffold. The in vitro results from the tensile test, wettability, porosity, and protein adsorption revealed appropriate properties of the membrane as a scaffold for skin tissue engineering.

Conclusions: Synthetic polymers have been widely used for tissue engineering applications. The proper characteristics of PEO nanofibers, including a high ratio of surface/volume, moderate hydrophilicity and good mechanical properties, make this polymer interesting for skin regeneration. The results demonstrate the potential of the antibacterial PEO/ZnO-NP membrane to be used as an engineered scaffold to improve the wound healing process.

背景:皮肤是病原体的第一道屏障,在受伤后失去其完整性和功能。在伤口部位使用抗菌敷料可以防止细菌入侵,也可以改善愈合过程。目的:制备具有抗菌性能的仿生膜,用于慢性伤口的愈合。材料与方法:采用静电纺丝法制备的聚环氧乙烷(PEO)和氧化锌纳米颗粒(ZnO-NPs)分别作为主要生物材料和抗菌剂。通过抗菌活性、细胞附着和活力测试来评价膜的生物学特性。为进一步研究确定ZnO-NPs的最佳细胞相容浓度。对膜进行了体外表征,以确定其适合伤口愈合的性能。结果:含2%纳米颗粒的抗菌PEO/ZnO-NP膜无细胞毒性,人成纤维细胞能够在支架上粘附和增殖。体外拉伸试验、润湿性、孔隙度和蛋白质吸附的结果表明,该膜具有作为皮肤组织工程支架的合适性能。结论:合成聚合物在组织工程中具有广泛的应用前景。PEO纳米纤维具有高的表面/体积比、中等亲水性和良好的机械性能,这使得这种聚合物对皮肤再生很有兴趣。结果表明,抗菌PEO/ZnO-NP膜具有作为工程支架改善伤口愈合过程的潜力。
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引用次数: 12
Comprehensive review of the role of acrylic acid derivative polymers in floating drug delivery system. 丙烯酸衍生物聚合物在漂浮给药系统中的作用综述。
Q3 Medicine Pub Date : 2019-07-01 DOI: 10.17219/pim/122016
Beena Kumari, Aparna Khansili, Parmita Phougat, Manish Kumar

In the development of drug delivery systems, an oral drug delivery system is the preferred route of drug administration. Many components play an important role in developing a drug delivery system. Amongst those components, polymers have evolved with these systems. Macromolecule compounds consisting of many monomer units which are joined to each other by different bonds are known as polymers. For drugs that are absorbed primarily in the upper gastrointestinal tract, floating drug delivery systems offer an additional advantage. The purpose behind this review was to focus on different types of floating drug delivery systems and different types of polymers used in floating drug delivery systems, focusing on acrylic acid derivatives and their applications. In this review, the main emphasis is on acrylic acid derivative polymers, their formulation and grades, and various patents on these types of polymers. Based on the literature survey, mainly 2 types of polymers are used in this drug delivery system; i.e., natural and synthetic. Examples of natural polymers are xanthan gum, guar gum or chitosan, and synthetic polymers include acrylic acid derivatives and hydroxylpropyl methylcellulose (HPMC). Eudragit and Carbopol are the most widely used acrylic acid derivatives.

在给药系统的发展中,口服给药系统是给药的首选途径。许多成分在开发给药系统中起着重要作用。在这些成分中,聚合物随着这些系统而发展。由许多单体单元组成的大分子化合物通过不同的键相互连接,称为聚合物。对于主要在上胃肠道吸收的药物,漂浮给药系统提供了额外的优势。本文综述了不同类型的漂浮给药系统和用于漂浮给药系统的不同类型的聚合物,重点介绍了丙烯酸衍生物及其应用。本文主要介绍了丙烯酸衍生物聚合物的配方和牌号,以及这类聚合物的各种专利。根据文献综述,该给药系统主要采用两种聚合物;即天然的和合成的。天然聚合物的例子有黄原胶、瓜尔胶或壳聚糖,合成聚合物包括丙烯酸衍生物和羟丙基甲基纤维素(HPMC)。乌龙茶和卡波酚是应用最广泛的丙烯酸衍生物。
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引用次数: 3
Biomedical application of greenly synthesized silver nanoparticles using the filtrate of Trichoderma viride: Anticancer and immunomodulatory potentials. 绿色木霉滤液绿色合成纳米银的生物医学应用:抗癌和免疫调节潜能。
Q3 Medicine Pub Date : 2019-07-01 DOI: 10.17219/pim/116086
Bukola Christianah Adebayo-Tayo, Gbemisola Elisabeth Ogunleye, Omonike Ogbole

Background: Green route biosynthesis of silver nanoparticles using Trichoderma viride (T. viride) filtrate (TVFSNPs) can serve as an alternative to antibiotics and as an effective drug delivery to combat cancer and act as an immune-stimulator.

Objectives: To biosynthesize silver nanoparticles (SNPs) with T. viride filtrate using green route and to characterize and determine the cytotoxic and immunomodulatory potential of nanoparticles.

Material and methods: Trichoderma viride filtrate was used for biosynthesizing SNPs. The biosynthesized SNPs were characterized using UV-visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX). The cytotoxic properties against Hep‑2C and rotavirus and the immunomodulatory potential were evaluated.

Results: Trichoderma viride filtrate was able to bio-reduce AgNO3 to SNPs. The surface plasmon resonance peak was at 450 nm. The presence of aldehydes, amino acids, ethers, esters, carboxylic acids, hydroxyl groups, and phenol among others indicates the capping and stabilization of proteins in the nanoparticles. The nanoparticles were spherical with a size of 0.1-10.0 nm. The EDX analysis revealed a strong signal of silver (Ag). The TVFSNPs had a cytotoxic effect on Hep2C and rotavirus in a dose-dependent manner and increased the production of immunoglobulin (Ig) A (IgA) and IgM.

Conclusions: Trichoderma viride filtrate contained some biochemicals that can bio-reduce silver nitrate (AgNO3) for SNPs biosynthesis. The anticancer and immunostimulatory potential justifies the biomedical application and biotechnological relevance of T. viride.

背景:利用绿色木霉滤液(TVFSNPs)绿色途径生物合成纳米银可以作为抗生素的替代品和有效的药物递送来对抗癌症,并作为免疫刺激剂。目的:采用绿色途径合成纳米银,并对纳米银的细胞毒性和免疫调节潜能进行表征和测定。材料与方法:采用绿色木霉滤液进行生物合成snp。利用紫外-可见光谱、傅里叶变换红外光谱(FTIR)、扫描电镜(SEM)和能量色散x射线(EDX)对生物合成的snp进行了表征。对Hep‑2C和轮状病毒的细胞毒性和免疫调节潜能进行了评价。结果:绿色木霉滤液能够将AgNO3生物还原为SNPs。表面等离子体共振峰位于450 nm处。醛、氨基酸、醚、酯、羧酸、羟基和苯酚等物质的存在表明纳米颗粒中蛋白质的覆盖和稳定。纳米颗粒呈球形,尺寸为0.1 ~ 10.0 nm。EDX分析显示有很强的银(Ag)信号。TVFSNPs对Hep2C和轮状病毒具有剂量依赖性的细胞毒作用,并增加免疫球蛋白(Ig) a (IgA)和IgM的产生。结论:绿色木霉滤液中含有生物还原硝酸银(AgNO3)的生化物质,可用于SNPs的生物合成。抗癌和免疫刺激的潜力证明了T. viviide的生物医学应用和生物技术相关性。
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引用次数: 7
The use of different dialysis membranes in therapy of patients with multiple myeloma. 不同透析膜在多发性骨髓瘤患者治疗中的应用。
Q3 Medicine Pub Date : 2019-07-01 DOI: 10.17219/pim/122014
Maciej Szymczak, Dorota Zielińska, Aleksandra Musiała

Free light chains accumulation is the reason of kidney injury in patients with multiple myeloma. The removal of free light chains can improve patients prognosis and survival, and in some cases allows for dialysotherapy discontinuation. Unfortunately, conventional dialysis is not effective enough in terms of free light chains removal. New high cut-off (HCO) techniques remove free light chains more effectively than conventional dialysis. In some cases, this technique may turn out better than hemodiafiltration. However, there are some differences between specific techniques in the removal of kappa and lambda light chains. Lambda light chains are better removed by polymethyl methacrylate membranes with a change of filter during dialysis. Kappa light chains are thoroughly removed by polymethyl methacrylate membranes and HCO (35,000 Da) polysulfone membranes. Unfortunately, it is very difficult to differentiate between the effect of HCO dialysis therapy and concomitant chemotherapy because some of the data is not fully conclusive. Using the proper technique for an individual patient may give optimally effective treatment results.

游离轻链积聚是多发性骨髓瘤患者肾损伤的原因。游离轻链的去除可以改善患者的预后和生存,在某些情况下可以停止透析治疗。不幸的是,传统的透析在去除游离轻链方面不够有效。新的高截断(HCO)技术比传统透析更有效地去除游离轻链。在某些情况下,这种技术可能比血液滤过更好。然而,在去除kappa和lambda轻链的具体技术之间存在一些差异。在透析过程中,通过改变过滤器,聚甲基丙烯酸甲酯膜可以更好地去除Lambda轻链。聚甲基丙烯酸甲酯膜和HCO (35000 Da)聚砜膜可彻底去除Kappa轻链。不幸的是,很难区分HCO透析治疗和伴随化疗的效果,因为一些数据不是完全结论性的。对个别患者使用适当的技术可以获得最佳有效的治疗结果。
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引用次数: 0
PALS probing of photopolymerization shrinkage in densely packed acrylate-type dental restorative composites. 高密度丙烯酸酯型牙科修复材料光聚合收缩的PALS探测。
Q3 Medicine Pub Date : 2019-07-01 DOI: 10.17219/pim/118394
Olha Shpotyuk, Adam Ingram, Oleh Shpotyuk, Andrii Miskiv, Nina Smolar

Background: Using positron annihilation lifetime spectroscopy (PALS), microstructural changes in commercial dental restorative composites under light-curing polymerization were identified as a modification in mixed positron/Ps trapping, where the decay of positronium (Ps; the bound state of positrons and electrons) is caused by free-volume holes mainly in the polymer matrix, and positron trapping is defined by interfacial free-volume holes in a mixed filler-polymer environment. In loosely packed composites with a filler content of <70-75%, this process was related to the conversion of Ps-to-positron trapping.

Objectives: To disclose such peculiarities in densely packed composites using the example of he commercially available acrylate-based composite ESTA-3® (ESTA Ltd., Kiev, Ukraine), which boasts a polymerization volumetric shrinkage of only 1.5%.

Material and methods: ESTA‑3® was used as a commercially available acrylate-based dental restorative composite. A fast-fast coincidence system of 230‑ps resolution based on 2 photomultiplier tubes coupled to a BaF2 detector and ORTEC® electronics was used to register lifetime spectra in normal-measurement statistics. The raw PAL spectra were treated using x3-x2-CDA (coupling decomposition algorithm).

Results: The annihilation process in the densely packed dental restorative composites (DRCs), as exemplified by the commercially available acrylate-based composite ESTA‑3®, is identified as mixed positron/ Ps trapping, where o-Ps decay is caused by free-volume holes in the polymer matrix and interfacial filler-polymer regions, and free positron annihilation is defined by free-volume holes between filler particles. The most adequate model-independent estimation of the polymerization volumetric shrinkage can be done using averaged positron annihilation lifetime. A meaningful description of the transformations in Psand positron-trapping sites under light curing can be developed on the basis of a semiempirical model exploring x3‑x2‑CDA. There is a strong monolithization of agglomerated filler nanoparticles in these composites, caused by the photo-induced disappearing of positron traps at the cost of Ps-decaying holes.

Conclusions: Governing the polymerization void-evolution process in densely packed DRC ESTA‑3® occurs mainly in the filler sub-system as positron-to-Ps trapping conversion, which is the reason for the low corresponding volumetric shrinkage.

背景:利用正电子湮灭寿命谱(PALS)技术,确定了光固化聚合下商用牙修复复合材料的微观结构变化是正电子/Ps混合捕获的修饰,其中正电子(Ps;正电子和电子的束缚态主要是由聚合物基体中的自由体积空穴引起的,而正电子的捕获则是由混合填料-聚合物环境中的界面自由体积空穴决定的。目的:以市售的丙烯酸酯基复合材料sta -3®(ESTA Ltd., Kiev, Ukraine)为例,揭示密集堆积复合材料中的这种特性,其聚合体积收缩率仅为1.5%。材料和方法:ESTA‑3®作为一种市售的丙烯酸酯基牙科修复复合材料。在正常测量统计中,使用了一个230 ps分辨率的快速重合系统,该系统基于2个光电倍增管耦合到BaF2探测器和ORTEC®电子设备。原始PAL光谱采用x3-x2-CDA(耦合分解算法)处理。结果:高密度牙科修复复合材料(DRCs)的湮灭过程,如市购的丙烯酸酯基复合材料ESTA‑3®,被确定为混合正电子/ Ps捕获,其中o-Ps衰变是由聚合物基体和填料-聚合物界面区域的自由体积空穴引起的,而自由正电子湮灭由填料颗粒之间的自由体积空穴定义。使用平均正电子湮灭寿命可以对聚合体积收缩进行最适当的模型独立估计。在探索x3‑x2‑CDA的半经验模型的基础上,可以对光固化下pds和正电子捕获位的转换进行有意义的描述。在这些复合材料中,由于光诱导的正电子陷阱以ps衰变空穴为代价而消失,导致了团聚性纳米颗粒的强单块化。结论:高密度DRC ESTA - 3®中聚合空隙演化过程主要发生在填料子系统正电子- ps俘获转换中,这是导致相应体积收缩率较低的原因。
{"title":"PALS probing of photopolymerization shrinkage in densely packed acrylate-type dental restorative composites.","authors":"Olha Shpotyuk,&nbsp;Adam Ingram,&nbsp;Oleh Shpotyuk,&nbsp;Andrii Miskiv,&nbsp;Nina Smolar","doi":"10.17219/pim/118394","DOIUrl":"https://doi.org/10.17219/pim/118394","url":null,"abstract":"<p><strong>Background: </strong>Using positron annihilation lifetime spectroscopy (PALS), microstructural changes in commercial dental restorative composites under light-curing polymerization were identified as a modification in mixed positron/Ps trapping, where the decay of positronium (Ps; the bound state of positrons and electrons) is caused by free-volume holes mainly in the polymer matrix, and positron trapping is defined by interfacial free-volume holes in a mixed filler-polymer environment. In loosely packed composites with a filler content of <70-75%, this process was related to the conversion of Ps-to-positron trapping.</p><p><strong>Objectives: </strong>To disclose such peculiarities in densely packed composites using the example of he commercially available acrylate-based composite ESTA-3® (ESTA Ltd., Kiev, Ukraine), which boasts a polymerization volumetric shrinkage of only 1.5%.</p><p><strong>Material and methods: </strong>ESTA‑3® was used as a commercially available acrylate-based dental restorative composite. A fast-fast coincidence system of 230‑ps resolution based on 2 photomultiplier tubes coupled to a BaF2 detector and ORTEC® electronics was used to register lifetime spectra in normal-measurement statistics. The raw PAL spectra were treated using x3-x2-CDA (coupling decomposition algorithm).</p><p><strong>Results: </strong>The annihilation process in the densely packed dental restorative composites (DRCs), as exemplified by the commercially available acrylate-based composite ESTA‑3®, is identified as mixed positron/ Ps trapping, where o-Ps decay is caused by free-volume holes in the polymer matrix and interfacial filler-polymer regions, and free positron annihilation is defined by free-volume holes between filler particles. The most adequate model-independent estimation of the polymerization volumetric shrinkage can be done using averaged positron annihilation lifetime. A meaningful description of the transformations in Psand positron-trapping sites under light curing can be developed on the basis of a semiempirical model exploring x3‑x2‑CDA. There is a strong monolithization of agglomerated filler nanoparticles in these composites, caused by the photo-induced disappearing of positron traps at the cost of Ps-decaying holes.</p><p><strong>Conclusions: </strong>Governing the polymerization void-evolution process in densely packed DRC ESTA‑3® occurs mainly in the filler sub-system as positron-to-Ps trapping conversion, which is the reason for the low corresponding volumetric shrinkage.</p>","PeriodicalId":20355,"journal":{"name":"Polimery w medycynie","volume":"49 2","pages":"49-56"},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"37985006","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
[Applications of synthetic and semisynthetic polymers (Kollidon K25, Kollidon K90 and Hydroksyethylocellulose) as carriers of ketoprofen in solid oral prolonged release dosage forms. The impact of selected non-ionic surfactants (Tween 80 and Rofam 70) on the release kinetics]. 合成和半合成聚合物(Kollidon K25, Kollidon K90和Hydroksyethylocellulose)作为酮洛芬固体口服缓释剂型载体的应用。所选非离子表面活性剂(Tween 80和Rofam 70)对释放动力学的影响。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.17219/pim/109360
W. Linka, M. Kołodziejczyk, Monika Monika Kamińska
BACKGROUND Hydrophilic matrices used as oral forms of sustained release drugs are a suitable application medium for short-acting nonsteroidal anti-inflammatory drugs (NSAID) - ketoprofen. A properly selected hydrophilic matrix in oral preparations may significantly increase efficacy and application safety of ketoprofen. OBJECTIVES The aim of the research was to analyze the usefulness of polymers (synthetic Kollidon K25 and K90, semi-synthetic hydroxyethylcellulose) and calcium hydrogen phosphate dihydrate (as an inorganic filler) in manufacturing solid oral matrix forms of ketoprofen and to study of the effect of non-ionic surfactants (Tween 80, Rofam 70) on release kinetics. MATERIAL AND METHODS Ketoprofen, HEC, Kollidon K25, and K90, calcium hydrogen phosphate, magnesium stearate. Incorporation. Studies on the tablet mass. Direct tableting. Studies on the pharmacopoeial parameters and pharmaceutical availability. Approximation of the results. RESULTS The results of the granulometric studies on tablet mass were in accordance with pharmacopoeial standards. The results of morphological and biopharmaceutical studies of the obtained matrices (tablets) were consistent with the pharmacopoeial standards for formulations with HEC, K25 and K90. The release results most closely related to row 0 kinetics were obtained for the matrix containing HEC and K25. Tween 80 added to 0.1N HCl accelerated the release of ketoprofen, while Rofam 70 decelerated it. Tween 80 and Rofam 70 added to the pH 7.4 buffer accelerated the release of ketoprofen. CONCLUSIONS The presented model system of preformulation studies showed the usefulness of HEC and Kolidon K25 in the technology of hydrophilic matrices with ketoprofen. Surfactants added to the medium do not affect the release rate of ketoprofen.
作为口服缓释药物的亲水基质是短效非甾体抗炎药(NSAID) -酮洛芬的合适应用介质。在口服制剂中选择合适的亲水性基质可显著提高酮洛芬的疗效和应用安全性。目的分析聚合物(合成Kollidon K25和K90,半合成羟乙基纤维素)和磷酸氢钙二水合物(作为无机填料)在制备固体口服酮洛芬基质中的作用,并研究非离子表面活性剂(Tween 80, Rofam 70)对酮洛芬释放动力学的影响。材料与方法:sketoprofen, HEC, Kollidon K25, K90,磷酸氢钙,硬脂酸镁。合并。片剂质量的研究。直接压片。药典参数及药物利用度研究。结果的近似。结果颗粒剂质量测定结果符合药典标准。所得基质(片)的形态和生物药剂学研究结果符合HEC、K25和K90制剂的药典标准。对于含有HEC和K25的基质,获得了与第0行动力学最密切相关的释放结果。添加0.1N HCl的吐温80加速了酮洛芬的释放,而Rofam 70则减缓了酮洛芬的释放。在pH 7.4的缓冲液中加入t80和Rofam 70加速了酮洛芬的释放。结论所建立的预处方研究模型系统显示了HEC和Kolidon K25在酮洛芬亲水性基质制备技术中的应用价值。在培养基中加入表面活性剂对酮洛芬的释放率没有影响。
{"title":"[Applications of synthetic and semisynthetic polymers (Kollidon K25, Kollidon K90 and Hydroksyethylocellulose) as carriers of ketoprofen in solid oral prolonged release dosage forms. The impact of selected non-ionic surfactants (Tween 80 and Rofam 70) on the release kinetics].","authors":"W. Linka, M. Kołodziejczyk, Monika Monika Kamińska","doi":"10.17219/pim/109360","DOIUrl":"https://doi.org/10.17219/pim/109360","url":null,"abstract":"BACKGROUND Hydrophilic matrices used as oral forms of sustained release drugs are a suitable application medium for short-acting nonsteroidal anti-inflammatory drugs (NSAID) - ketoprofen. A properly selected hydrophilic matrix in oral preparations may significantly increase efficacy and application safety of ketoprofen. OBJECTIVES The aim of the research was to analyze the usefulness of polymers (synthetic Kollidon K25 and K90, semi-synthetic hydroxyethylcellulose) and calcium hydrogen phosphate dihydrate (as an inorganic filler) in manufacturing solid oral matrix forms of ketoprofen and to study of the effect of non-ionic surfactants (Tween 80, Rofam 70) on release kinetics. MATERIAL AND METHODS Ketoprofen, HEC, Kollidon K25, and K90, calcium hydrogen phosphate, magnesium stearate. Incorporation. Studies on the tablet mass. Direct tableting. Studies on the pharmacopoeial parameters and pharmaceutical availability. Approximation of the results. RESULTS The results of the granulometric studies on tablet mass were in accordance with pharmacopoeial standards. The results of morphological and biopharmaceutical studies of the obtained matrices (tablets) were consistent with the pharmacopoeial standards for formulations with HEC, K25 and K90. The release results most closely related to row 0 kinetics were obtained for the matrix containing HEC and K25. Tween 80 added to 0.1N HCl accelerated the release of ketoprofen, while Rofam 70 decelerated it. Tween 80 and Rofam 70 added to the pH 7.4 buffer accelerated the release of ketoprofen. CONCLUSIONS The presented model system of preformulation studies showed the usefulness of HEC and Kolidon K25 in the technology of hydrophilic matrices with ketoprofen. Surfactants added to the medium do not affect the release rate of ketoprofen.","PeriodicalId":20355,"journal":{"name":"Polimery w medycynie","volume":"22 1","pages":"5-18"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91208799","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Influence of levodropropizine and hydroxypropyl-β-cyclodextrin association on the physicochemical characteristics of levodropropizine loaded in hydroxypropyl-β-cyclodextrin microcontainers: Formulation and in vitro characterization. 左旋丙哌嗪与羟丙基-β-环糊精缔合对羟丙基-β-环糊精微容器内左旋丙哌嗪理化特性的影响:配方及体外表征
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.17219/pim/111887
A. Yousaf, Alina Qadeer, S. Raza, T. Chohan, Y. Shahzad, F. Din, I. Khan, T. Hussain, M. Alvi, T. Mahmood
BACKGROUND Poorly water-soluble drugs do not dissolve well in aqueous-based gastrointestinal fluid; therefore, they are not well absorbed. Thus, employing a suitable solubility enhancing technique is necessary for such a drug. Drug/HP‑β‑CD complexation is a promising way to improve solubility and dissolution of a poorly water-soluble drug. Levodropropizine was used as a model drug in this study. OBJECTIVES The purpose of this research was to enhance the aqueous solubility and dissolution rate of levodropropizine by employing the inclusion complexation technique. MATERIAL AND METHODS A microparticle formulation was prepared from levodropropizine and hydroxypropyl-β-cyclodextrin (HP‑β‑CD) in a 1:1 molar ratio through the spray-drying technique. The host-guest relationship between levodropropizine and HP‑β‑CD was also investigated using the molecular docking computational methodology. The aqueous solubility and dissolution rate of levodropropizine in formulations were assessed and compared with those of the drug alone. X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR) were applied for the solid-state characterization of the prepared samples. RESULTS According to the research outcomes, the levodropropizine/HP‑β‑CD formulation had enhanced the aqueous solubility (351.12 ±13.26 vs 92.76 ±5.00 mg/mL) and dissolution rate (97.83 ±3.36 vs 3.12 ±1.76% in 10 min) of levodropropizine, compared to the plain drug powder. The levodropropizine/ HP‑β‑CD formulation had converted the crystalline drug into its amorphous counterpart. Furthermore, no covalent interaction was found to exist between levodropropizine and HP‑β‑CD. The spray-dried particles were discrete. Each particle had a shriveled appearance. CONCLUSIONS The levodropropizine/HP‑β‑CD formulation is, therefore, recommended for the more effective administration of levodropropizine through the oral route.
背景:水溶性差的药物不能很好地溶解在水基胃肠道液体中;因此,它们不能很好地吸收。因此,对这种药物采用合适的溶解度增强技术是必要的。药物/HP‑β‑CD络合是一种很有前途的方法来改善水溶性差的药物的溶解度和溶出度。本研究以左旋丙哌嗪为模型药物。目的采用包合技术提高左丙哌嗪的溶解度和溶出度。材料与方法以左丙丙哌嗪和羟丙基-β-环糊精(HP -β- CD)为原料,采用喷雾干燥技术,以1:1的摩尔比制备sa微粒制剂。利用分子对接计算方法研究了左旋丙哌嗪与HP‑β‑CD的主客关系。评价了左旋丙哌嗪在制剂中的溶解度和溶出度,并与单用左旋丙哌嗪进行了比较。采用x射线衍射(XRD)、差示扫描量热法(DSC)、扫描电镜(SEM)和傅里叶变换红外光谱(FTIR)对制备的样品进行了固态表征。结果左旋丙哌嗪/HP‑β‑CD制剂的溶解度(351.12±13.26 vs 92.76±5.00 mg/mL)和溶出度(97.83±3.36 vs 3.12±1.76%,10 min)均高于普通药粉;左旋丙哌嗪/ HP‑β‑CD制剂将晶体药物转化为非晶态药物。此外,左旋丙哌嗪与HP‑β‑CD之间不存在共价相互作用。喷雾干燥的颗粒是离散的。每个粒子都有一个收缩的外观。结论左旋丙嗪/HP‑β‑CD是口服左旋丙嗪更有效的给药方式。
{"title":"Influence of levodropropizine and hydroxypropyl-β-cyclodextrin association on the physicochemical characteristics of levodropropizine loaded in hydroxypropyl-β-cyclodextrin microcontainers: Formulation and in vitro characterization.","authors":"A. Yousaf, Alina Qadeer, S. Raza, T. Chohan, Y. Shahzad, F. Din, I. Khan, T. Hussain, M. Alvi, T. Mahmood","doi":"10.17219/pim/111887","DOIUrl":"https://doi.org/10.17219/pim/111887","url":null,"abstract":"BACKGROUND Poorly water-soluble drugs do not dissolve well in aqueous-based gastrointestinal fluid; therefore, they are not well absorbed. Thus, employing a suitable solubility enhancing technique is necessary for such a drug. Drug/HP‑β‑CD complexation is a promising way to improve solubility and dissolution of a poorly water-soluble drug. Levodropropizine was used as a model drug in this study. OBJECTIVES The purpose of this research was to enhance the aqueous solubility and dissolution rate of levodropropizine by employing the inclusion complexation technique. MATERIAL AND METHODS A microparticle formulation was prepared from levodropropizine and hydroxypropyl-β-cyclodextrin (HP‑β‑CD) in a 1:1 molar ratio through the spray-drying technique. The host-guest relationship between levodropropizine and HP‑β‑CD was also investigated using the molecular docking computational methodology. The aqueous solubility and dissolution rate of levodropropizine in formulations were assessed and compared with those of the drug alone. X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR) were applied for the solid-state characterization of the prepared samples. RESULTS According to the research outcomes, the levodropropizine/HP‑β‑CD formulation had enhanced the aqueous solubility (351.12 ±13.26 vs 92.76 ±5.00 mg/mL) and dissolution rate (97.83 ±3.36 vs 3.12 ±1.76% in 10 min) of levodropropizine, compared to the plain drug powder. The levodropropizine/ HP‑β‑CD formulation had converted the crystalline drug into its amorphous counterpart. Furthermore, no covalent interaction was found to exist between levodropropizine and HP‑β‑CD. The spray-dried particles were discrete. Each particle had a shriveled appearance. CONCLUSIONS The levodropropizine/HP‑β‑CD formulation is, therefore, recommended for the more effective administration of levodropropizine through the oral route.","PeriodicalId":20355,"journal":{"name":"Polimery w medycynie","volume":"75 1","pages":"35-43"},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83842081","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Influence of sodium starch glycolate, croscarmellose sodium and crospovidone on disintegration and dissolution of stevia-loaded tablets. 乙醇酸淀粉钠、交联棉糖钠和交联维酮对甜菊糖苷片崩解度的影响。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.17219/pim/111516
A. Yousaf, Faiza Naheed, Y. Shahzad, T. Hussain, T. Mahmood
BACKGROUND Sugar substitutes are used by diabetic, obese and calorie-conscious people. As artificial sweeteners are harmful to the body, natural sweeteners are more suitable. Sugar substitutes are available on the market in tablet forms, which are added to hot or cold drinks. Rapid disintegration and dissolution of sugar substitute-loaded tablet is desired. However, the tablets should be hard enough to maintain their integrity during mechanical shocks. OBJECTIVES The objective of this research was to develop rapidly disintegrating and dissolving stevia-loaded tablets with appropriate wetting, hardness and friability. MATERIAL AND METHODS Several tablets were prepared using different superdisintegrants using the direct compression method. Flowability tests of the powder blends were performed before compression; these test took into account such physical parameters as bulk density, tapped density, angle of repose, compressibility index, and Hausner's ratio. Evaluation of the compressed cores was accomplished with weight variation, hardness, thickness, friability, disintegration time, wetting time, and dissolution. RESULTS The disintegration time and wetting time of the tablets were in the following order: sodium starch glycolate > croscarmellose sodium > crospovidone containing tablets. A powder blend consisting of stevia extract, crospovidone, lactose, and magnesium stearate at the optimized ratio of 15/2.5/32/0.5 (w/w/w/w) showed the best flow, rapid disintegration (38 ±0.894 s), wetting (30 ±1 s), and dissolution (~ 95% in 1 min). Moreover, this formulation showed more rapid wetting (30 ±1 s vs 91 ±1.9 s), disintegration (38 ±0.894 s vs 143 ±1.276 s) and dissolution (~ 95% vs 60% in 1 min) than a commercial product. CONCLUSIONS The tablet consisting of stevia, crospovidone, lactose, and magnesium stearate at the weight ratio of 15/2.5/32/0.5 showed excellent results with regards to dissolution and disintegration; accordingly, this formulation could be a potential sugar substitute for diabetic, obese and/or calorie-conscious individuals.
背景:糖尿病、肥胖和对卡路里敏感的人都在使用糖替代品。由于人造甜味剂对人体有害,天然甜味剂更合适。市场上有片剂形式的糖替代品,可以添加到热饮或冷饮中。糖替代片的快速崩解和溶出是必需的。然而,平板电脑应该足够坚硬,以在机械冲击下保持其完整性。目的:研制湿性、硬度、脆度适宜的甜菊糖快速崩解溶出片。材料与方法采用不同的强力崩解剂,采用直接压缩法制备不同的片剂。在压缩前进行了粉末共混物的流动性试验;这些试验考虑了堆密度、攻丝密度、休止角、压缩指数、豪斯纳比等物理参数。压缩岩心的评价指标包括重量变化、硬度、厚度、脆性、崩解时间、润湿时间和溶解度。结果各片剂的崩解时间和润湿时间依次为:乙醇酸淀粉钠片、交联棉糖钠片、交联维酮片。以15/2.5/32/0.5 (w/w/w/w)的最佳配比为甜叶菊提取物、交叉烷醇酮、乳糖和硬脂酸镁的混合粉末,其流动性最佳,崩解速度快(38±0.894 s),湿润速度快(30±1 s),溶出速度快(1 min ~ 95%)。此外,该配方具有更快的润湿(30±1 s vs 91±1.9 s),崩解(38±0.894 s vs 143±1.276 s)和溶解(~ 95% vs 60%在1分钟内)比商业产品。结论以15/2.5/32/0.5的质量比,由甜菊糖、交叉烷维酮、乳糖、硬脂酸镁组成的片剂具有良好的溶出和崩解效果;因此,这种配方可能是糖尿病、肥胖和/或热量敏感人群的潜在糖替代品。
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引用次数: 3
Relationship between compression pressure, mechanical strenghth and release properties of tablets. 片剂的压缩压力、机械强度与释放性能的关系。
Q3 Medicine Pub Date : 2019-01-01 DOI: 10.17219/pim/111888
O. Adeleye
Tablets are a complex drug delivery system consisting of the active pharmaceutical ingredients and excipients. Tablet production involves a series of unit operations in which drugs and excipients are subjected to mechanical stresses, such as compression pressure, thus imposing changes in the properties of these materials. Variations in the compression pressure and other processing parameters may affect the mechanical strength and release properties of the final tablet. It is generally expected that an increase in compression pressure should lead to an increase in mechanical strength and a decrease in release properties of tablets, but this may not be true in some practical situation, since tablet production is the result of complex interaction between many factors involving the drug, excipient, the formulation, and processing variables. The degree and extent of interaction of these variables are not absolutely dependent on one factor. The aim of this review is to study the interaction between compression pressure, mechanical strength and release properties of immediate and controlled release tablets. The effect of compression pressure on tablets is complemented by such factors as the material properties of the drug and excipient, the formulation and processing factors, which in turn affects mechanical strength and release properties.
片剂是一种由活性药物成分和赋形剂组成的复杂给药系统。片剂生产涉及一系列单元操作,其中药物和赋形剂受到机械应力,例如压缩压力,从而使这些材料的性质发生变化。压缩压力和其他工艺参数的变化可能会影响最终片剂的机械强度和释放性能。一般认为,压缩压力的增加会导致片剂机械强度的增加和释放性能的降低,但在某些实际情况下可能并非如此,因为片剂的生产是许多因素复杂相互作用的结果,这些因素包括药物、赋形剂、配方和工艺变量。这些变量相互作用的程度和范围并不完全取决于一个因素。本综述旨在研究速释片和控释片的压缩压力、机械强度与释药性能的相互作用。压缩压力对片剂的影响还与药物和赋形剂的材料性质、制剂和加工因素等因素相辅相成,进而影响片剂的机械强度和释放性能。
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引用次数: 7
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Polimery w medycynie
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