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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2017 · IF 3.756

Engineering hot-melt extruded solid dispersion for controlled release of hydrophilic drugs

Shuli Zhang,Xuan Meng,Zheng Wang,Aiping Fan,Guocheng Wang,Yanjun Zhao,Yu Tang

It is often challenging to precisely manipulate the release behavior of hydrophilic drugs that is believed to be crucial for a satisfactory therapeutic outcome. The aim of this work was to regulate the dissolution of hydrophilic drug from hot-melt extruded solid dispersion via rational screening of the pore-forming agents. Venlafaxine hydrochloride and Compritol® 888 ATO was selected as the model drug and carrier excipient, respectively. Hydrophilic polyethylene glycol (PEG 6000) and polyvinylpyrolidone (PVP K30) were chosen as the transient pore-forming agents. The X-ray diffraction and thermal analysis showed that both drug and carrier existed in the crystalline form. Both types of polymers could generate pores upon dissolution test and the drug release rate was proportionally correlated to the pore-forming agent content. The mathematical modelling showed that the Ritger-Peppas model gave the best fit to the release curves, which demonstrates a diffusion-dominant release mechanism. The scanning electron microscopy and mercury intrusion porosimetry analysis proved that PVP K30 could generate large pores with low porosity, but PEG 6000 produced smaller pores with relatively high porosity. The in vivo pharmacokinetics study in rat revealed that solid dispersions containing either PEG 6000 or PVP K30 (both at 2.5%, w/w) exhibited an elevated bioavailability compared to the commercial product, Effexor® XR. The current work implied that rational screening of transient pore-forming polymer in solid dispersion could be a robust approach for controlling hydrophilic drug release.

研究领域: 药剂学 · 药物释放系统
✓ 已验证 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2021 · IF 4.384

Application of TPGS as an efflux inhibitor and a plasticizer in baicalein solid dispersion

Meng Tong,Xiaoyan Wu,Shuya Zhang,Di Hua,Shukun Li,Xiangyu Yu,Jing Wang,Zhenhai Zhang

The oral bioavailability and efficacy of baicalein is dramatically limited by its low solubility and effect of efflux. In our study, we chose PVP-VA64 as a carrier and TPGS as a plasticizer and efflux inhibitor to prepare a solid dispersion of baicalein using hot-melt extrusion technology to improve its solubility and bioavailability. The hot-melt process and formulation were optimized, and a BAC-PVP VA64-TPGS solid dispersion (BPT-SD) was prepared. BAC exists in an amorphous or molecular state in BPT-SD. BPT-SD comprised irregular lumps and small particles without BAC or carrier characteristics. The dissolution efficiency of BPT-SD improved under sink conditions. FTIR showed a strong hydrogen bond between BAC and PVP-VA64 in BPT-SD. BPT-SD maintained good physical stability for 6 months. The apparent permeability coefficient of BAC in the Caco-2 cell model confirmed that BPT-SD had higher gastrointestinal membrane permeability. A rat pharmacokinetic study showed that BPT-SD had higher C max and AUC 0- 24h, shorter T max , and 2.88-fold higher bioavailability than BAC. A behavioral experiment in chronic unpredictable mild stress (CUMS) mice confirmed the antidepressant efficacy of BAC. BPT-SD reversed depression-like behavior in CUMS mice and improved BAC bioavailability. BAC preparation into a solid dispersion significantly enhanced dissolution performance and bioavailability.

CAS / MDL: 63449-41-2
研究领域: 药剂学 · 生物医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Energy Materials · 2025 ·Vol. 5 ·期 2 ·N · IF 11.2

High-performance novel anode-supported microtubular protonic ceramic fuel cells via highly efficient and simplified extrusion technology

Zichen Zhuang,Zuzhi Huang,Xiaoyu Zhang,Kui Liu,Guozhu Zheng,Ting Chen,Ruili Sun,Lang Xu,Shaorong Wang

Protonic ceramic fuel cells (PCFCs) are regarded as efficient energy conversion devices for addressing the challenges of carbon neutrality, which can directly convert the chemical fuel energy into electricity at reduced operating temperatures below 700 °C. However, the insufficient strength and immature preparation processes of PCFCs limit their practical application. In this work, the novel anode-supported microtubular PCFCs with a tube diameter of less than 5 mm were successfully prepared by extrusion technology combined with a dip-coating method. The newly developed BaZr0.4Ce0.4Y0.1Gd0.1O3-δ (BZCYG4411) proton-conducting electrolyte was synthesized using an extremely simple and efficient one-step solid-state reaction method, showing comparable electrical conductivity with BaZr0.4Ce0.4Y0.1Yb0.1O3-δ (BZCYYb4411) and BaZr0.1Ce0.7Y0.1Yb0.1O3-δ (BZCYYb1711) electrolytes, as well as excellent chemical stability. The single cell with Ba2Sc0.1Nb0.1Co1.5Fe0.3O6-δ (BSNCF) cathode exhibited a high peak power density of 906.86 mW cm-2 at 700 °C. Additionally, this microtubular PCFC demonstrated excellent stability after about 103 h durability test at a constant current of 0.5 A cm-2 at 650 °C. This study provides a highly efficient and simplified technology for fabricating high-performance and durable anode-supported microtubular PCFCs.

研究领域: 能源材料科学 · 电化学工程
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International Journal of Applied Ceramic Technology · 2023 ·Vol. 20 ·期 6 ·3455-3469 · IF 2.1

Additive manufacturing of continuous carbon fiber–reinforced silicon carbide ceramic composites

Kai Liu,Lei Qiu,Yuzhen Zhang,Yanying Du,Ce Sun,Song Zhang,Rong Tu,Yanjiao Wu,Huajun Sun,Yusheng Shi

A material extrusion (MEX) technology has been developed for the additive manufacturing of continuous carbon fiber–reinforced silicon carbide ceramic (C f /SiC) composites. By comparing and analyzing the rheological properties of the slurries with different compositions, a slurry with a high solid loading of 48.1 vol% and high viscosity was proposed. Furthermore, several complex structures of C f /SiC ceramic composites were printed by this MEX additive manufacturing technique. Phenolic resin impregnation–carbonization process reduces the apparent porosity of the green body and protects the C f . Finally, the reactive melting infiltration (RMI) process was used to prepare samples with different C f contents from 0 to 2 K (a bundle of carbon fibers consisting of 1000 fibers). Samples with C f content of 1 K show the highest bending strength (161.6 ± 10.5 MPa) and fracture toughness (3.72 ± 0.11 MPa·m 1/2 ) while the thermal conductivity of the samples with the C f content of 1 K reached 11.0 W/(m·K). This study provides a strategy to prepare C f /SiC composites via MEX additive manufacturing and RMI.

CAS / MDL: 9005-38-3
研究领域: 材料科学 · 制造工程
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MOLECULES · 2015 ·Vol. 20 ·期 11 ·20031-20041 · IF 2.416

Pharmacokinetics of Ginkgolide B after Oral Administration of Three Different Ginkgolide B Formulations in Beagle Dogs

Jie Zhao,Ting Geng,Qi Wang,Haihong Si,Xiaoping Sun,Qingming Guo,Yanjing Li,Wenzhe Huang,Gang Ding,Wei Xiao

Ginkgolide B (GB), an important active constituent ofGinkgo bilobaextract, has been used in clinical applications for the treatment of dementia, cerebral insufficiency or related cognitive decline. To investigate the main pharmacokinetic characteristics of three different GB formulations in beagle dogs, a simple, specific and sensitive LC-MS/MS method was established and validated. The separation of the analytes was achieved on an Agilent Eclipse Plus C18column (1.8 μm, 2.1 × 50 mm) with a mobile phase consisting of water and acetonitrile. The flow rate was set at 0.4 mL/min. Quantitation was performed using multiple reaction monitoring (MRM) in negative ion mode, with the transitions atm/z(Q1/Q3) 423.1/367.1 for GB andm/z269.3/170.0 for IS. The linear calibration curve of GB was obtained over the concentration range of 2–200 ng/mL. The intra- and inter-day precisions were <15% and the accuracies were within ±12.7%. The validated method was applied to compare the pharmacokinetic characteristics of GB in healthy beagle dogs after oral administration of three formulations (HME08, GB capsule prepared by hot-melt extrusion technology; LL06, GB pellet prepared by liquid layer technology; conventional GB tablet). The Cmaxvalues of GB from different formulations in beagle dog plasma were 309.2, 192.4 and 66.6 µg/L, and the AUC values were 606.7, 419.1 and 236.2 µg/L·h, respectively. The data suggested that the exposure level of GB from HME08 and LL06 in beagle dog plasma was greatly improved compared with conventional tablets. This study should be helpful for the design and development of oral GB preparations.Keywords:ginkgolide B;hot-melt extrusion;liquid layer;beagle dog plasma;pharmacokinetics;LC-MS/MS

CAS / MDL: 64-77-7
研究领域: 药理学 · 药物分析 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF APPLIED POLYMER SCIENCE · 2021 ·Vol. 138 ·期 39 ·51010 · IF 3.125

Preparation of poly(butylene succinate) vitrimer with thermal shape stability via transesterification reaction

Yue Yin,Jian Yang,Linghui Meng

Poly(butylene succinate) (PBS) refers to a high-performance biodegradable polymer employed to substitute petroleum polymers that cause environmental issues. However, PBS exhibits the defect of flowing above the melting point and rapid dripping for its poor melt strength. Accordingly, this study proposed a novel method to fabricate PBS vitrimer by exploiting reactive extrusion technology to mix diepoxide with PBS and then by employing zinc acetate as a catalyst to crosslink the PBS. Therefore, after the reaction extrusion blending, the blend still has a lower viscosity and high processing performance; in the subsequent curing process, the polymer undergoes a transesterification reaction and the viscosity increases. Via transesterification to form a cross-linked network, the storage modulus, and loss modulus of PBS vitrimer at 140°C reach 55,800% and 3500% of pure PBS, respectively. At this time, the crystallinity of PBS vitrimer is still as high as 56.9% (The crystallinity of pure PBS is 47.4%). And the shape stability of PBS at high temperatures was significantly improved. Moreover, PBS vitrimer could still be reshaped after the cross-linking process. This study proposed a facile method to produce PBS materials exhibiting high thermal shape stability.

研究领域: 材料科学 · 高分子化学
✓ 已验证 DOI 高影响因子
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COMPOSITES SCIENCE AND TECHNOLOGY · 2014 · IF 3.633

Enhancing antibacterial performances of PVDF hollow fibers by embedding Ag-loaded zeolites on the membrane outer layer via co-extruding technique

Huyan Shi,Fu Liu,Lixin Xue,Huafeng Lu,Qingbo Zhou

Ag-loaded zeolites were synthesized and embedded into the outer layer of poly(vinylidene fluoride) (PVDF) dual-layer hollow fiber membrane (D) using a dry-jet wet-spinning co-extruding technique. The distribution of the Ag-loaded zeolites in the outer layer was confirmed by field emission scanning electron microscopy (FE-SEM) and energy-dispersive X-ray spectroscopy (EDX). It was found that the D contained only 54% of the amount of Ag-loaded zeolites that were distributed throughout the cross section of PVDF single-layer hollow fiber membrane (S), as calculated by thermogravimetric analysis (TGA). However, D showed excellent antibacterial efficiency and resistance to bacterial adhesion because of the higher concentration of Ag + in the outer layer of the membrane. The surface morphologies , pure water flux, mean pore size, pore size distribution , and thermal stability of both PVDF membranes were also investigated.

研究领域: 材料科学 · 化学工程 · 环境科学
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FOOD CHEMISTRY · 2024 · IF 8.5

Quality characteristics and fibrous structure formation mechanism of walnut protein and wheat gluten meat analogues during high-moisture extrusion cooking process

Shuwen Lei,Chunyan Zhao,Yue Miao,Hong Zhao,Zhichen Liu,Yuzhuang Zhang,Lei Zhao,Chunxiu Peng,Jiashun Gong

Blending two or more materials to create better high-moisture meat analogues has been actively studied in the food science and technology field. Walnut protein is a high-quality plant-based protein resource, yet its full potential remains underexploited. Thus, this study focused on exploring the quality characteristics and fibrous structure formation mechanism of walnut protein (WP) and wheat gluten (WG) meat analogues during high-moisture extrusion cooking process. Results showed that the optimized WP and WG-blended high-moisture meat analogues exhibited a more pronounced anisotropic and oriented fibrous structure. The blending of WP and WG can protect the molecular chains from the thermal transition, and promote the aggregation of protein molecules mainly by enhancing the interaction between hydrophobic interactions and hydrogen bonds, increasing the apparent viscosity and forming protein subunits with larger molecular weights (>100 kDa) to stabilize the newly formed conformation. Additionally, the content of α-helix was the highest among the secondary structures. This study provides a theoretical basis for the application of WG and WP to produce HMMAs with rich fibrous structures.

CAS / MDL: 60-24-2
研究领域: 食品科学与技术 · 蛋白质化学 · 挤出技术
✓ 已验证 产品关联 DOI PubMed 高影响因子
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