Pellets

颗粒
  • 文章类型: Journal Article
    目的:本文研究了冻干微丸中材料厚度对提高封装菌储存稳定性的关键作用。使用扫描电子显微镜(SEM)和X射线显微断层扫描(μCT)对从不同退火持续时间获得的不同厚度的冷冻干燥材料进行定量。然后将材料厚度与封装的细胞的储存稳定性相关联。
    方法:包含蔗糖,麦芽糊精,益生菌细胞在液氮中淬灭形成颗粒。粒料在经历冷冻干燥之前经历不同的退火持续时间。使用SEM和μCT定量材料厚度。通过测量CFU计数来评估富氧和贫氧环境中的储存稳定性,并将其与颗粒结构相关联。
    结果:不同的退火方案产生一系列材料厚度,更广泛的退火导致较厚的材料。储存稳定性与材料厚度呈正相关,表明使用较厚的材料改善了稳定性。未退火的颗粒表现出结构不规则性和不一致的储存稳定性,突出了在冷冻干燥过程中避免退火的不切实际。
    结论:大量退火不仅增强了益生菌产品的储存稳定性,而且对冷冻干燥过程提供了更大的控制,确保均匀和可重复的产品。这项研究强调了冻干颗粒中材料厚度对优化益生菌制剂储存稳定性的重要性。并强调退火作为冷冻干燥淬火颗粒的关键步骤的必要性,以实现所需的结构和稳定性结果。
    OBJECTIVE: This paper investigates the critical role of material thickness in freeze-dried pellets for enhancing the storage stability of encapsulated bacteria. Freeze dried material of varying thicknesses obtained from different annealing durations is quantified using Scanning Electron Microscopy (SEM) and X-ray microtomography (μCT), the material thickness is then correlated to the storage stability of the encapsulated cells.
    METHODS: A formulation comprising of sucrose, maltodextrin, and probiotic cells is quenched in liquid nitrogen to form pellets. The pellets undergo different durations of annealing before undergoing freeze-drying. The material thickness is quantified using SEM and μCT. Storage stability in both oxygen-rich and oxygen-poor environments is evaluated by measuring CFU counts and correlated with the pellet structure.
    RESULTS: The varying annealing protocols produce a range of material thicknesses, with more extensive annealing resulting in thicker materials. Storage stability exhibits a positive correlation with material thickness, indicating improved stability with thicker materials. Non-annealed pellets exhibit structural irregularities and inconsistent storage stability, highlighting the impracticality of avoiding annealing in the freeze-drying process.
    CONCLUSIONS: Extensive annealing not only enhances the storage stability of probiotic products but also provides greater control over the freeze-drying process, ensuring homogeneous and reproducible products. This study underscores the importance of material thickness in freeze-dried pellets for optimizing storage stability for probiotic formulations, and emphasize the necessity of annealing as a critical step in freeze-drying quenched pellets to achieve desired structural and stability outcomes.
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  • 文章类型: Journal Article
    胃肠道线虫(GIN)感染是全球小反刍动物(绵羊和山羊)可持续发展的最大障碍。GINs对合成驱虫药的耐药性导致人们对探索寄生虫控制的替代方法的兴趣日益增加。例如利用具有抗寄生虫特性的生物活性植物。在这次调查中,黑色种子(Nigellasativa),一种二级抗氧化化合物含量高的灌木,和sericealespedeza(Lespedezacuneata),将单宁含量高的多年生豆科植物与抗寄生虫特性相结合,以确定两种含有不同类型次级化合物的生物活性植物是否可以提供比单独的sericealespedeza更强的抗寄生虫作用。在为期49天的审判中,自然寄生的6-7个月大的完整西班牙雄性山羊(n=15/处理)饲喂包含sericealeppedeza叶粉(SL)的颗粒饲料,黑种子粉(BS)和sericealeppedeza叶粉(BS-SL-75%SL,25%BS),或苜蓿(紫花苜蓿,控制寄生;CONP),另一组除虫儿童给予苜蓿颗粒(对照治疗;续)。每周测量动物体重以及血液和粪便样品,以确定细胞体积(PCV)。GIN粪便卵数(FEC),和球虫粪便卵母细胞计数(FOC),分别。在试验结束时对所有动物进行处理(总共60只),从每只山羊的皱胃中回收成虫,用于计数和性别确定。加工后记录尸体重量。接受SL和BS-SL处理的山羊的FEC低于寄生苜蓿(CONP)山羊(P<0.05)。在研究结束时,SL组和BS-SL组的FOC值低于CONT组和CONP组(P<0.05)。随着时间的推移,所有组的PCV值都有上升;SL,BS-SL,与CONP山羊相比,CONT动物表现出更高的PCV值(P<0.05)。与饲喂BS-SL或苜蓿颗粒的山羊相比,饲喂仅SL颗粒的寄生山羊显示出更大的饲料摄入量和动物体重(P<0.05)。然而,这些治疗对山羊尸体的重量没有影响。尽管CONT山羊(苜蓿驱虫)中的H.contortus成虫蠕虫计数低于CONP山羊(苜蓿寄生)(P<0.05),它们与SL或BS-SL动物没有差异.这项研究表明,刺梨叶粉颗粒饮食,单独或与黑种子粉结合使用,作为驱虫药显示出有希望的结果,并且可能被证明是唯一使用常规驱虫药物的有效替代品。在这项研究中,添加黑色种子似乎并未增强sericealeppedeza的有效性。
    Gastrointestinal nematode (GIN) infection poses the most significant obstacle to the sustainable development of small ruminant (sheep and goat) farming globally. Resistance of GINs to synthetic anthelmintic drugs has led to rising interest in exploring alternative methods for parasite control, such as the utilization of bioactive plants with anti-parasitic properties. In this investigation, black seed (Nigella sativa), a shrub high in secondary antioxidant compounds, and sericea lespedeza (Lespedeza cuneata), a perennial legume high in tannins with anti-parasitic properties were combined to determine if two bioactive plants containing different types of secondary compounds can provide a stronger anti-parasitic effect than sericea lespedeza alone. In a 49-day trial, naturally parasitized 6-7-month-old intact male Spanish goats (n = 15/treatment) were fed pelletized feeds encompassing sericea lespedeza leaf meal (SL), a combination of black seed meal (BS) and sericea lespedeza leaf meal (BS-SL - 75 % SL, 25 % BS), or alfalfa (Medicago sativa, control parasitized; CONP), with an additional group of dewormed kids given the alfalfa pellets (Control treated; CONT). Weekly measurements of animal weights and samples of blood and feces were collected to determine the packed cell volume (PCV), GIN fecal egg counts (FEC), and coccidia fecal oocyte counts (FOC), respectively. All animals were processed at the end of the trial (60 total), with adult Haemonchus contortus worms recovered from the abomasum of each goat for counting and sex determination. Carcass weights were recorded after processing. Goats given the SL and BS-SL treatments had lower FEC (P<0.05) than the parasitized alfalfa (CONP) goats. At the end of the study, the SL and BS-SL groups\' FOC values were lower (P < 0.05) than the CONT and CONP groups. A rise in PCV values was seen over time for all groups; SL, BS-SL, and CONT animals exhibited higher PCV values (P < 0.05) in comparison to the CONP goats. The parasitized goats fed SL-only pellets showed greater feed intake and animal body weights (P < 0.05) compared to goats fed BS-SL or alfalfa pellets. However, the treatments had no effect on the weight of the goats\' carcasses. Although the H. contortus adult worm counts in the CONT goats (alfalfa-dewormed) were lower (P < 0.05) than in the CONP goats (alfalfa-parasitized), they did not differ from the SL or BS-SL animals. This study indicates that sericea lespedeza leaf meal pellet diet, either by itself or in combination with black seed meal, showed promising results as an anthelmintic and may prove to be an effective alternative to exclusive use of conventional deworming drugs. The addition of black seed did not appear to enhance the effectiveness of sericea lespedeza in this study.
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  • 文章类型: Journal Article
    本文研究了不同储存条件对三种类型的农业生物质颗粒的选定理化性质的影响:向日葵壳,麦草和大麻,和木质颗粒。测试是在气候室中进行的,可以模拟真实的储存条件,即具有高空气湿度和可变(±)环境空气温度的条件。结果表明,与木质生物质相比,农业生物质颗粒的降解能力更高。与在高湿度(90%RH)下相比,粒料在变化的±温度下降解的程度较小。水分完全饱和后,农产品颗粒的耐久性平均下降9%,而在向日葵果壳颗粒和木质颗粒的冷冻和除霜后,耐久性降低了2%,和11%的大麻草丸。相比之下,在环境(30°C和90%RH)中,农产品颗粒的下降强度指数下降了20%,在不同的温度条件下下降了15%。没有注意到干物质中所有颗粒的能量参数的变化。另一方面,颗粒在不同环境条件下储存时,水分含量的增加会导致热值降低。
    This article examines the effects of different storage conditions on selected physicochemical properties of three types of agro-biomass pellets: sunflower husks, wheat straw and hemp hurds, and wood pellets. The tests were carried out in a climatic chamber, which allows simulation of real storage conditions, i.e. conditions with high air humidity and variable (±) ambient air temperatures. The results showed higher degradability of agro-biomass pellets compared to woody biomass. The pellets degraded to a less extent at varying  ± temperatures than at high humidity (90% RH). After complete moisture saturation, durability decreases for agro-pellets by an average of 9%, while after freezing and defreezing for sunflower husk pellets and woody pellets durability decreases by 2%, and for hemp hurd pellets by 11%. In contrast, strength-by-dropping index for agro-pellets decreased by 20% after being in the environment (30 °C and 90%RH) and 15% under varying temperature conditions. No change in the energy parameters of all pellets in the dry matter was noted. On the other hand, an increase in the moisture content of pellets when they are stored under different environmental conditions results in a decrease in calorific value.
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  • 文章类型: Journal Article
    残余木质纤维素生物质(RLB)是一种有价值的资源,可以通过作为化石燃料的替代品和作为生产各种增值分子的原料来帮助解决环境问题。为了全面了解南美木质纤维素废物的使用情况,过去四年进行了审查。审查的重点是能源生产,生物燃料生产,获得平台分子(如乙醇,羟甲基糠醛,糠醛,和乙酰丙酸),和其他感兴趣的材料。审查发现,巴西,哥伦比亚,厄瓜多尔的RLB来源最多,甘蔗,油棕,和水稻作物残留物是最突出的。在南美洲,RLB用于生产沼气,合成气,氢气,生物油,生物柴油,烘焙生物质,颗粒,和生物质煤块。研究和生产最多的增值分子是乙醇,其次是糠醛,羟甲基糠醛,和乙酰丙酸.用RLB开发的其他感兴趣的应用包括获得活性炭和纳米材料。南美洲在利用RLB方面取得了重大进展,一些国家在规范其使用方面更加积极主动。然而,关于每个国家RLB的潜力,还有很多需要了解的地方。这篇评论提供了有关南美残留生物量的典型化和价值化的最新观点,并讨论了该地区正在应用的研究和技术水平。这些信息可能有助于未来在南美洲的RLB研究。
    Residual lignocellulosic biomass (RLB) is a valuable resource that can help address environmental issues by serving as an alternative to fossil fuels and as a raw material for producing various value-added molecules. To gain a comprehensive understanding of the use of lignocellulosic waste in South America, a review was conducted over the last 4 years. The review focused on energy generation, biofuel production, obtaining platform molecules (such as ethanol, hydroxymethylfurfural, furfural, and levulinic acid), and other materials of interest. The review found that Brazil, Colombia, and Ecuador had the most RLB sources, with sugarcane, oil palm, and rice crop residues being the most prominent. In South America, RLB is used to produce biogas, syngas, hydrogen, bio-oil, biodiesel, torrefied biomass, pellets, and biomass briquettes. The most studied and produced value-added molecule was ethanol, followed by furfural, hydroxymethylfurfural, and levulinic acid. Other applications of interest that have been developed with RLB include obtaining activated carbon and nanomaterials. Significant progress has been made in South America in utilizing RLB, and some countries have been more proactive in regulating its use. However, there is still much to learn about the potential of RLB in each country. This review provides an updated perspective on the typification and valorization of residual biomass in South America and discusses the level of research and technology being applied in the region. This information can be helpful for future research on RLB in South America.
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  • 文章类型: Journal Article
    最近的COVID-19大流行期间的人类原因为研究人类活动对海鸟的影响提供了独特的机会。秘鲁的封锁阻止了人们访问沿海地区,从而减少海滩上的垃圾处理和微塑料进入海洋的流动。这种活动的停止可能导致沿海地区塑料污染的暂时减少。我们的目的是在沿着普拉亚斯哥斯达黎加佛得角赛道(CPCV)的近岸喂养的新性coo(Nannoppterumbrasililianus)中调查这种现象,位于利马的沿海地带,秘鲁(约1100万人)。
    我们在大流行封锁之前(超过11个月)和期间(超过8个月)收集并分析了CPCV上的新鲜颗粒。
    我们的发现表明,与大流行前的情况(%Oc=7.13,n=800粒)相比,大流行期间颗粒中塑料的发生率显著降低(%Oc=2.47,n=647粒)。在颗粒中发现的最常见的塑料碎片是线状微塑料。此外,我们的研究强调了人类在海滩上的存在与cor颗粒中发现的微塑料(主要是线状)数量之间的直接相关性。我们建议将这些材料重新引入海洋,以前积累在海岸上,可能是由海滩游客向海洋的运动和活动促进的。
    UNASSIGNED: The anthropause during the recent COVID-19 pandemic provided a unique opportunity to examine the impact of human activity on seabirds. Lockdowns in Peru prevented people from visiting coastal areas, thereby reducing garbage disposal on beaches and the movement of microplastics into the ocean. This cessation of activities likely led to a temporary decrease in plastic pollution in coastal regions. We aimed to investigate this phenomenon in inshore-feeding neotropic cormorants (Nannopterum brasilianus) along the Circuito de Playas Costa Verde (CPCV), situated on the coastal strip of Lima, Peru (∼ 11 million people).
    UNASSIGNED: We collected and analyzed fresh pellets along the CPCV before (over 11 months) and during the pandemic lockdowns (over 8 months).
    UNASSIGNED: Our findings revealed a significant reduction in the occurrence of plastic in pellets during the pandemic period (% Oc = 2.47, n = 647 pellets) compared to pre-pandemic conditions (% Oc = 7.13, n = 800 pellets). The most common plastic debris item found in the pellets was threadlike microplastic. Additionally, our study highlights the direct correlation between human presence on beaches and the quantity of microplastics (mainly threadlike) found in cormorant pellets. We suggest that the reintroduction of these materials into the sea, previously accumulated on the coast, is likely facilitated by the movement and activity of beachgoers toward the ocean.
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  • 文章类型: Journal Article
    苦涩的药物,华法林,具有狭窄的治疗指数(NTI),用于儿科和老年病学。本可行性研究的目的是配制适用于剂量个性化的含华法林掩味颗粒,并提高患者的依从性。以及研究核心类型的影响(PharSQ®SpheresM,CELPHERE™CP-507和NaCl)对华法林从Kollicoat®Smartseal掩味包衣的小丸中的释放。将芯成功地装载药物并在具有Wurster插入物的流化床涂布机中涂覆。通过光学显微镜观察到粒度和粒度分布的增加。在唾液模拟的pH中,在Kollicoat®Smartseal水平为2mg/cm2时,无一微丸显示药物释放,确认他们有效的掩味。然而,在胃模拟的pH值,与NaCl核心相比,从PharSQ®SpheresM-和CELPHERE™CP-507包衣的小丸观察到更快的药物释放。其他实验使我们能够解释由于盐析效应而导致的含NaCl颗粒中药物释放较慢的现象。尽管成功了掩味,微丸的药物释放相对较慢(每60分钟不超过91%),允许进一步改进配方。
    The bitter drug, warfarin, has a narrow therapeutic index (NTI) and is used in paediatrics and geriatrics. The aim of this feasibility study was to formulate the taste-masked warfarin-containing pellets to be applicable for dose personalisation and to improve patient compliance, as well as to investigate the effect of the core type (PharSQ® Spheres M, CELPHERE™ CP-507, and NaCl) on the warfarin release from the Kollicoat® Smartseal taste-masking-coated pellets. The cores were successfully drug-loaded and coated in a fluid-bed coater with a Wurster insert. An increase in particle size and particle size distribution was observed by optical microscopy. In saliva-simulated pH, at the Kollicoat® Smartseal level of 2 mg/cm2, none of the pellets demonstrated drug release, confirming their efficient taste-masking. However, in a stomach-simulated pH, a faster drug release was observed from PharSQ® Spheres M- and CELPHERE™ CP-507-coated pellets in comparison with NaCl cores. Additional experiments allowed us to explain the slower drug release from NaCl-containing pellets because of the salting-out effect. Despite the successful taste masking, the drug release from pellets was relatively slow (not more than 91% per 60 min), allowing for further formulation improvements.
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  • 文章类型: Journal Article
    大茎植物蒿的田间研究(A.dubia)自2018年以来一直在LAMMC的V种种aičiai分支机构进行。根据三年的实验结果,年干物质(DM)产量从7.94到10.14tha-1不等。生长条件,施氮水平,和收割时间对杜氏芽孢杆菌的生产率有统计学上的显著影响。本文最重要的任务是调查和确定影响杜仲草植物生物量生产力的因素和技术评价,电源,以及植物生物质利用能源转化和生产高质量固体生物燃料颗粒的环境参数。对于实验,使用了六种A.dubia样本的变体,生长于2021年。将植物切割三次,并使用两种施肥选择:(1)不施肥和(2)用180kgha-1的氮肥施肥。这些收获的植物被切碎,碾磨,并压成颗粒。物理机械特性(水分含量,密度,和强度)。在这项研究中,发现颗粒的干重(DM)密度范围为1119.86至1192.44kgm-3。颗粒水分含量范围为8.80至10.49%。在测试颗粒强度之后,结果发现,由植物生物量PK-1-1(首次收获不含氮肥)制成的颗粒对压缩的抵抗力最强,他们承受了560.36N的压力。颗粒的干燃料低热值(LHV)足够高,并且非常接近松木屑颗粒;它从17.46±0.25MJkg-1变化到18.14±0.28MJkg-1。燃烧颗粒的灰分含量范围为3.62±0.02%至6.47±0.09%。有害污染物的排放-CO2,CO,NOx,和未燃烧的碳氢化合物(CxHy)-不超过最大允许水平。总结A.dubia颗粒的燃烧和排放特性的研究结果,可以得出结论,这种生物燃料可以用于生产压制的生物燃料,它的特点是质量足够高,高效燃烧,以及对环境的允许排放。
    Field studies with the large-stemmed plant Artemisia dubia (A. dubia) have been carried out at the Vėžaičiai Branch of LAMMC since 2018. According to three years of experimental results, annual dry matter (DM) yield varied from 7.94 to 10.14 t ha-1. Growing conditions, nitrogen application level, and harvesting time had statistically significant impacts on A. dubia productivity. The most important tasks of this article were to investigate and determine the factors influencing A. dubia plant biomass productivity and the evaluation of technological, power, and environmental parameters of plant biomass utilization for energy conversion and the production of high-quality solid biofuel pellets. For the experiments, six variants of A. dubia samples were used, which were grown in 2021. Plants were cut three times and two fertilization options were used: (1) no fertilization and (2) fertilization with 180 kg ha-1 of nitrogen fertilizer. These harvested plants were chopped, milled, and pressed into pellets. The physical-mechanical characteristics (moisture content, density, and strength) of the A. dubia pellets were investigated. During this study, it was found that the density in the dry mass (DM) of the pellets ranged from 1119.86 to 1192.44 kg m-3. The pellet moisture content ranged from 8.80 to 10.49%. After testing pellet strength, it was found that the pellets which were made from plant biomass PK-1-1 (first harvest without N fertilization) were the most resistant to compression, and they withstood 560.36 N of pressure. The dry fuel lower heating value (LHV) of the pellets was sufficiently high and was very close to that of the pine sawdust pellets; it varied from 17.46 ± 0.25 MJ kg-1 to 18.14 ± 0.28 MJ kg-1. The ash content of the burned pellets ranged from 3.62 ± 0.02% to 6.47 ± 0.09%. Emissions of harmful pollutants-CO2, CO, NOx, and unburnt hydrocarbons (CxHy)-did not exceed the maximum permissible levels. Summarizing the results for the investigated properties of the combustion and emissions of the A. dubia pellets, it can be concluded that this biofuel can be used for the production of pressed biofuel, and it is characterized by sufficiently high quality, efficient combustion, and permissible emissions to the environment.
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  • 文章类型: Journal Article
    在这项研究中,一种经济有效且稳定的非均相酸性碳催化剂(CZnLS950),源自木质素磺酸钠(LS),造纸工业的副产品,用于通过热解废食用油(WCO)和从葵花籽中提取的粗天然油生产碳氢化合物燃料,符合循环经济的原则。为了增强其在工业环境中的实用性,催化剂以颗粒形式合成,能够容易地从反应过程中产生的生物燃料中分离。CZnLS950在WCO的热解中表现出显著的催化效率,导致71wt。%温和条件下的液体生物燃料产率。这种性能归因于酸性碳催化剂的独特合成程序,它利用LS和纳米ZnO(20nm)创建具有酸性的分层孔结构(1.1mmol的NH3g-1)。评估了碳催化剂的稳定性和可重复使用性,结果表明,具有良好的稳定性,催化失活较小(〜5wt。%)第四次使用后。提供了对WCO和葵花籽粗天然油热解的不同催化机理的尝试,以了解获得所生产的两种不同生物燃料所涉及的过程。总的来说,这项研究为探索木质素磺酸盐基材料从回收流中获得可再生生物燃料奠定了基础。
    In this study, a cost-effective and stable heterogeneous acidic carbocatalyst (CZnLS950) derived from Na-lignosulfonate (LS), a side product of the paper industry, was employed to produce hydrocarbon fuels through the pyrolysis of waste cooking oil (WCO) and crude natural-oil extracted from sunflower seeds, aligning with the principles of the circular economy. To enhance its practicality in industrial settings, the catalyst was synthesized in pellet form, enabling easy separation from the biofuel produced during the reaction. CZnLS950 exhibited remarkable catalytic efficiency in the pyrolysis of WCO, resulting in a 71 wt. % liquid biofuel yield under mild conditions. This performance is attributed to the unique synthesis procedure of acidic carbocatalyst, which utilizes LS and nano ZnO (20 nm) to create a hierarchical pore structure with acidic properties (1.1 mmol of NH3 g-1). Stability and reusability of the carbocatalyst were evaluated, and the results showed excellent stability with small catalytic deactivation (~5 wt. %) after the fourth use. Attempts at distinct catalytic mechanisms for WCO and sunflower seeds crude natural-oil pyrolysis were provided to understand the processes involved in obtaining the two different biofuels produced. Overall, this study sets the stage for exploring Lignosulfonate-based materials to achieve renewable biofuel from recycling streams.
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  • 文章类型: Journal Article
    背景和目的:肠溶型奥美拉唑是最常用的处方药之一。和欧洲一样,哈萨克斯坦依靠药品生产的本地化作为其主要战略之一,以确保其人口获得负担得起的优质药品。这项研究全面描述了生物等效性延迟释放奥美拉唑的技术发展。材料和方法:在实验室和生产规模的设备上测试了各种方案和技术参数,以建立功能和胃保护层必不可少的技术过程。根据ICH稳定性测试指南和哈萨克斯坦当地规则,稳定性研究是在适合II型气候区的条件下进行的。比较吸收的速率和程度,并随后评估通用药物和参考药物的生物等效性,每种药物的剂量为40mg。结果:在固体剂型的生产现场开发并实施了生产新型肠溶型奥美拉唑胶囊的定量和定性组合物和技术。证实了在pH1.2和6.8的培养基中的溶出曲线。在加速六个月和长期十二个月的研究中,在每个控制点的两种包装材料中开发的配方都通过了平均重量和质量均匀性测试,溶出度试验,耐酸阶段试验,缓冲阶段测试,杂质测定,和微生物纯度测试,并符合所有规范标准。一项针对24名健康志愿者的生物等效性研究与创新药物进行了比较,显示了新仿制药系统的生物等效性。从测试和参考产品获得的Cmax值为1321±249.0ng/mL和1274±233ng/mL,AUC0-t为4521±841ng·h/mL和4371±695ng·h/mL,AUC0-∞为4636±814ng·h/mL和4502±640ng·h/mL。结论:使用负担得起的技术,已开发出20和40mg奥美拉唑的生物等效通用延迟释放制剂.
    Background and Objectives: The enteric form of omeprazole is one of the most commonly prescribed medications. Similarly to Europe, Kazakhstan relies on the localization of pharmaceutical drug production as one of its primary strategies to ensure that its population has access to affordable and good-quality medicines. This study comprehensively describes the technologically available development of bioequivalent delayed-release omeprazole. Materials and Methods: Various regimes and technological parameters were tested on laboratory- and production-scale equipment to establish a technical process where a functional and gastro-protective layer is essential. According to the ICH guidance on stability testing and Kazakhstan local rules, stability studies were conducted under conditions appropriate for climate zone II. The comparison of the rate and extent of absorption with subsequent assessment of the bioequivalence of the generic and reference drugs after a single dose of each drug at a dose of 40 mg was performed. Results: The quantitative and qualitative composition and technology of producing a new generic enteric form of omeprazole in capsules were developed and implemented at the manufacturing site of solid forms. Dissolution profiles in media with pH 1.2 and 6.8 were proven. During the accelerated six-month and long-term twelve-month studies, the developed formulation in both packaging materials at each control point passed the average weight and mass uniformity test, dissolution test, acid-resistance stage test, buffer stage test, impurity assay, and microbiological purity test and met all the specification criteria. A bioequivalence study in 24 healthy volunteers compared against the innovative drug showed the bioequivalency of the new generic system. The obtained values from the test and reference products were 1321 ± 249.0 ng/mL and 1274 ± 233 ng/mL for Cmax, 4521 ± 841 ng·h /mL and 4371 ± 695 ng·h /mL for AUC0-t, and 4636 ± 814 ng·h /mL and 4502 ± 640 ng·h /mL for AUC0-∞. Conclusions: Using affordable technologies, a bioequivalent generic delayed-release formulation of 20 and 40 mg omeprazole has been developed.
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  • 文章类型: Journal Article
    通过压实小丸制备的多单位剂型提供了优于小丸填充胶囊的重要制造和顺应性优点。然而,压实可能会对微丸的释放控制机制产生负面影响,和亚基在摄入后可能不容易获得。在此提出将缓冲层应用于起始单元作为获得具有令人满意的机械强度的片剂的策略。快速崩解和维持单个亚基的预期释放曲线,同时避免使用微丸和赋形剂的混合物来促进压实并限制所涉及的力的影响。缓冲层PEG1500,一种柔软的可溶性材料,在充分控制加工温度的前提下,证明是可行的。缓冲的耐胃颗粒显示出在相对较低的压实压力下固结,在片剂崩解后保留了其固有的释放性能。通过施加外部Kollicoat®IR膜克服了与使用PEG1500相关的粘附问题。通过实验设计(DoE),证明了所提出方法的鲁棒性,并对配方和制片条件进行了优化。所制造的压片垫涂层颗粒系统将允许输送相对高负载的调释单元,因此,为多单位剂型的口服给药提供了一种通用且可扩展的策略。
    Multiple-unit dosage forms prepared by compacting pellets offer important manufacturing and compliance advantages over pellet-filled capsules. However, compaction may negatively affect the release control mechanism of pellets, and subunits may not be readily available after intake. Application of a cushioning layer to the starting units is here proposed as a strategy to obtain tablets with satisfactory mechanical strength, rapid disintegration and maintenance of the expected release profile of individual subunits while avoiding the use of mixtures of pellets and excipients to promote compaction and limit the impact of the forces involved. Cushion-coating with PEG1500, a soft and soluble material, was proved feasible provided that the processing temperature was adequately controlled. Cushioned gastro-resistant pellets were shown to consolidate under relatively low compaction pressures, which preserved their inherent release performance after tablet disintegration. Adhesion problems associated with the use of PEG1500 were overcome by applying an outer Kollicoat® IR film. Through design of experiment (DoE), robustness of the proposed approach was demonstrated, and the formulation as well as tableting conditions were optimized. The tableted cushion-coated pellet systems manufactured would allow a relatively high load of modified-release units to be conveyed, thus setting out a versatile and scalable approach to oral administration of multiple-unit dosage forms.
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