Melting method

  • 文章类型: Journal Article
    非诺贝特(FNF)用于治疗高脂血症。然而,FNF是一种水溶性差的药物,在Lipidil®片剂中,商业产品的剂量相对较高,为160mg。因此,这项研究旨在开发一种溶解和稳定FNF的FNF-固体分散体(SD)。采用使用低熔点FNF的熔融方法。最佳配方(SD2)中FNF的溶出百分比增加了1.2-,1.3-,与Lipidil®相比,5分钟时增加了1.3倍,增加了2.0-,2.1-,与pH1.2介质中的纯FNF相比是2.0倍,蒸馏水,和pH6.8缓冲液,其中包括0.025M十二烷基硫酸钠,分别。SD2制剂在60分钟后在所有溶出介质中显示出近100%的溶出百分比。SD2制剂的物理化学性质表现出FNF的熔点和结晶度的轻微变化。此外,SD2制剂的稳定性维持6个月.特别是,当从SD2制剂中排除淀粉#1500时,确保稳定性是具有挑战性的。总之,由于FNF和赋形剂之间的弱结合力,FNF在SD2制剂中的溶出度得到改善,稳定性得到了保证,在未来的动物实验中有望获得良好的结果。
    Fenofibrate (FNF) is used to treat hyperlipidemia. However, FNF is a poorly water-soluble drug, and the dosage of commercial products is relatively high at 160 mg in a Lipidil® tablet. Therefore, this study aimed to develop an FNF-solid dispersion (SD) that solubilizes and stabilizes FNF. The melting method that uses the low melting point of FNF was employed. The dissolution percentage of FNF in the optimal formulation (SD2) increased by 1.2-, 1.3-, and 1.3-fold at 5 min compared to that of Lipidil® and increased by 2.0-, 2.1-, and 2.0-fold compared to the pure FNF in pH 1.2 media, distilled water, and pH 6.8 buffer, which included 0.025 M sodium lauryl sulfate, respectively. The SD2 formulation showed a dissolution percentage of nearly 100 % in all dissolution media after 60 min. The physicochemical properties of the SD2 formulation exhibited slight changes in the melting point and crystallinity of FNF. Moreover, the stability of the SD2 formulation was maintained for six months. In particular, it was challenging to secure stability when starch#1500 was excluded from the SD2 formulation. In conclusion, the dissolution percentage of FNF in the SD2 formulation was improved owing to the weak binding force between FNF and the excipients, stability was secured, and favorable results are expected in future animal experiments.
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  • 文章类型: Journal Article
    海水淡化在解决水资源短缺和促进可持续发展方面发挥着至关重要的作用。然而,海水中高硼含量的存在构成了重大挑战。本研究介绍了一种渐进的冷冻熔融方法,该方法可以在淡化海水的同时有效地去除硼。实验结果表明,盐度和硼去除率随冻结温度的增加而增加,随冻结时间的增加而降低。在实验熔化方法中,超声波熔融(UM)和振荡熔融(OM)在除硼和脱盐方面优于自然熔融(NM),振荡熔化被证明是最有效的。具体来说,当海水在-20°C下冷冻44小时,然后是55%的冰的OM,盐度和硼去除率分别达到96.79%和97.60%,分别。处理后的海水中硼和盐度浓度仅为0.777‰和0.149mg/L。此外,处理1m3海水的估计理论能耗计算为5.95kWh。这项研究不仅有助于环境的可持续性,而且由于其在脱盐和除硼方面的高效率而具有巨大的潜力。
    Desalination plays a crucial role in addressing water scarcity and promoting sustainable development. However, the presence of high boron content in seawater poses a significant challenge. This study introduces a progressive freezing-melting method that effectively removes boron while desalinating seawater. The experimental results indicated that salinity and boron rate of removal increased with freezing temperature and decreased with freezing duration. Among the experimental melting methods, ultrasonic melting (UM) and oscillatory melting (OM) were superior to natural melting (NM) for boron removal and desalination, with oscillatory melting proving to be the most effective. Specifically, when seawater was frozen at - 20 °C for 44 h followed by OM of 55% of the ice, salinity and boron removal rates reached 96.79% and 97.60%, respectively. The concentrations of boron and salinity in the treated seawater were only 0.777‰ and 0.149 mg/L. Moreover, the estimated theoretical energy consumption for treating 1 m3 of seawater was calculated to be 5.95 kWh. This study not only contributes to environmental sustainability but also holds significant potential due to its high efficiency in desalination and boron removal.
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  • 文章类型: Journal Article
    L-抗坏血酸(AA)是一种高度不稳定的化合物,因此,限制其在药品和化妆品中的使用,特别是在较高的浓度。
    本研究旨在通过将高度敏感的分子(AA)封装在β-环糊精纳米海绵(β-CDNS)中,可以进一步用于制备具有较高AA浓度和增强稳定性的药妆产品。
    NS是通过熔融法合成的。通过冷冻干燥方法将AA包封在β-CDNS中。用红外光谱对所制备的NS进行了表征,SEM,原子力显微镜(AFM),zetasizer,差示扫描量热法(DSC),并对其物理流动特性进行了研究。使用两种方法的组合在Franz装置上进行体外药物释放:样品&分离和透析膜。使用经验证的光谱测定方法进行测定。
    AA在β-CDNS中的包封率表明良好的负载能力(83.57±6.35%)。FTIR,SEM,AFM,DSC结果证实了AA在β-CDNS中的包封。颗粒大小,多分散指数,和zeta电位结果确定了稳定的单分散纳米颗粒的形成。物理流动特性显示出良好的流动特性。在Korsmeyer-Peppas模型之后的4小时内,约有84%的AA从NS中释放。当在30±2℃/65±5%RH下储存时,负载AA的NS保持稳定9个月。
    结论是制备的NS可以保护高度敏感的AA免于降解并提供维生素的延长释放。所制备的载AAβ-CDNS可用于配制其他具有较好稳定性和效果的药妆剂型。
    BACKGROUND: L-Ascorbic acid (AA) is a highly unstable compound, thus, limiting its use in pharmaceutical and cosmetic products, particularly at higher concentrations.
    OBJECTIVE: This study aimed to stabilize the highly sensitive molecule (AA) by encapsulating it in β- cyclodextrin nanosponges (β-CD NS) that can be used further in preparing cosmeceuticals products with higher AA concentrations and enhanced stability.
    METHODS: The NS has been synthesized by the melting method. The AA was encapsulated in β-CD NS by the freeze-drying process. The prepared NS were characterized by FTIR spectrometry, SEM, Atomic Force Microscopy (AFM), zeta sizer, Differential Scanning Calorimetry (DSC), and the physical flow characteristics were also studied. The in vitro drug release was carried out on the Franz apparatus using a combination of two methods: sample & separate and dialysis membrane. The assay was performed using a validated spectrometric method.
    RESULTS: The entrapment efficiency of AA in β-CD NS indicated a good loading capacity (83.57±6.35%). The FTIR, SEM, AFM, and DSC results confirmed the encapsulation of AA in β-CD NS. The particle size, polydispersity index, and zeta potential results ascertained the formation of stabilized monodisperse nanoparticles. The physical flow characteristics showed good flow properties. Around 84% AA has been released from the NS in 4 h following the Korsmeyer-Peppas model. The AA-loaded NS remained stable for nine months when stored at 30±2°C/65±5% RH.
    CONCLUSIONS: It is concluded that the prepared NS can protect the highly sensitive AA from degradation and provide an extended-release of the vitamin. The prepared AA-loaded β-CD NS can be used to formulate other cosmeceutical dosage forms with better stability and effect.
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  • 文章类型: Journal Article
    Dissolving microneedles (DMNs) have been used as an alternative drug delivery system to deliver therapeutics across the skin barrier in a painless manner. In this study, we propose a novel heat-melting method for the fabrication of hydrophobic poly(lactic-co-glycolic acid) (PLGA) DMNs, without the use of potentially harmful organic solvents. The drug-loaded PLGA mixture, which consisted of a middle layer of the DMN, was optimized and successfully implanted into ex vivo porcine skin. Implanted HMP-DMNs separated from the patch within 10 min, enhancing user compliance, and the encapsulated molecules were released for nearly 4 weeks thereafter. In conclusion, the geometry of HMP-DMNs was successfully optimized for safe and effective transdermal sustained drug delivery without the use of organic solvents. This study provides a strategy for the innovative utilization of PLGA as a material for transdermal drug delivery systems.
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  • 文章类型: Journal Article
    The study mainly aimed to improve the solubility of honokiol (HK) by preparing honokiol nanosuspensions (HNS). In this study, HNS were obtained using Kolliphor®P407 (P407) as a stabilizer through melting method combined with high pressure homogenization (HPH). The crystalline state of HNS was confirmed through differential scanning calorimetry (DSC) and X-ray Diffraction (XRD). In vitro, the dissolution rate of HNS was significantly improved than that of pure HK. In vivo, higher anti-inflammatory activity was achieved after free HK had been made into HNS. There was no significant difference between the degree of edema (DE) of HNS group and that of aspirin group. Consequently, melting method combined with HPH was a potent technique to prepare HNS. Furthermore, nanosuspension was a valid formulation that could be utilized to enhance the anti-inflammatory effect of HK.
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  • 文章类型: Journal Article
    Over the last half-century, solid dispersions (SDs) have been intensively investigated as a strategy to improve drugs solubility and dissolution rate, enhancing oral bioavailability. In this review, an overview of the state of the art of SDs technology is presented, focusing on their classification, the main preparation methods, the limitations associated with their instability, and the marketed products. To fully take advantage of SDs potential, an improvement in their physical stability and the ability to prolong the supersaturation of the drug in gastrointestinal fluids is required, as well as a better scientific understanding of scale-up for defining a robust manufacturing process. Taking these limitations into account will contribute to increase the number of marketed pharmaceutical products based on SD technology.
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  • 文章类型: Journal Article
    Lithium fluoride doped with Mg and Dy was fabricated for the first time using melting method. The optimum concentrations of impurities and thermal treatment were studied to achieve high thermoluminescence (TL) sensitivity. TL sensitivity of the fabricated phosphor is close to that of TLD-100 powder. Tm-Tstop technique was used to identify the number of overlapped TL glow peaks. Initial rise, isothermal decay and computerized glow curve deconvolution (CGCD) methods were applied to obtain kinetic parameters of the prepared TL material. Three component glow peaks were distinguished at temperatures 395, 448 and 510 K. Other TL properties such as fading, linearity of dose response and reusability are also presented and discussed.
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  • 文章类型: Journal Article
    The study aimed to develop a modified-solid dispersion method using a swellable hydrophilic polymers accompanied by a conventional carrier to enhance the dissolution of a drug that possesses poor water solubility. Two swellable polymers (hydroxypropyl methylcellulose and polyethylene oxide) were swelled in melted polyethylene glycol 6000 (PEG 6000) in different ratios and under different conditions. The type, amount, and, especially, incorporation method of the swellable polymers were crucial factors affecting the dissolution rate, crystallinity, and molecular interaction of the drug. Interestingly, the method in which the swellable polymer was thoroughly mixed with the melted PEG 6000 as the first step was more effective in increasing drug dissolution than the method in which the drug was introduced to the melted PEG 6000 followed by the addition of the swellable polymer. This system has potential for controlling drug release due to high swelling capabilities of these polymers. Therefore, the current study can be considered to be a promising model for formulations of controlled release systems containing solid dispersions.
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