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Formulation of a film-coated dutasteride tablet bioequivalent to a soft gelatin capsule(Avodart~?): Effect of γ-cyclodextrin and solubilizers

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Asian Journal of Pharmaceutical Sciences 2019年第3期14卷 313-320页

作者： Mi-Hong Min Jin-Hyong Park Mi-Ran Choi Jong-Hyun Hur Byung-Nak Ahn dae-duk kim College of Pharmacy and Research Institute of Pharmaceutical Sciences Seoul National UniversitySeoul08826Republic of Korea Central Research Institute Whanin Pharmaceutical Company4FGBSA107Gwanggyo-roYeongtong-guSuwon16229Republic of Korea

The aim of this study was to optimize a tablet formulation of dutasteride that is bioequivalent to a commercially available soft gelatin capsule(Avodart~?). The effect of cyclodextrin on enhancing the aqueous solubility of dutasteride was investigated, after which the formulation was further optimized with solubilizing polymer and surfactant. Among the cyclodextrins tested, the highest solubility was observed when dutasteride was complexed with γ-cyclodextrin. Moreover, the addition of polyvinylpyrrolidone and Gelucire/TPGS further enhanced the solubility of dutasteride. Differential scanning calorimetry(DSC) and powder X-ray diffraction(pX RD) studies demonstrated that dutasteride existed in the amorphous form in the complex. Optimized dutasteride complexes were selected after a pharmacokinetic study in rats, and film-coated tablets were prepared by the direct compression method. In vitro dissolution profiles for the tablets of dutasteride complexes were similar to those of the reference. Moreover, pharmacokinetic parameters including the C max and AUC values after oral administration in beagle dogs were not significantly different from those of the reference with a relative bioavailability of 92.4%. These results suggest the feasibility of developing a tablet formulation of dutasteride using cyclodextrin complex in addition to a solubilizing polymer and surfactant.

关键词： Dutasteride Tablet Cyclodextrin Complex Formulation

RP-HPLC法测定紫杉醇在大鼠血浆中的含量

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沈阳药科大学学报 2008年第1期25卷 48-51+55页

作者：杨涛崔福德金大德沈阳药科大学药学院首尔国立大学药学院

目的建立紫杉醇在大鼠血浆中的定量分析方法,为药物动力学研究提供分析方法。方法采用RP-HPLC法。Li Chrospher 100反相C18色谱柱(250 mm×4.6 mm,5μm),乙腈-水(体积比50∶50)为流动相,流速为1.0 ***-1,紫外检测波长为227 nm,血浆样品... 详细信息

目的建立紫杉醇在大鼠血浆中的定量分析方法,为药物动力学研究提供分析方法。方法采用RP-HPLC法。Li Chrospher 100反相C18色谱柱(250 mm×4.6 mm,5μm),乙腈-水(体积比50∶50)为流动相,流速为1.0 ***-1,紫外检测波长为227 nm,血浆样品经乙酸乙酯萃取,以内标法定量。结果线性范围为0.025100.0 mg.L-1(r=1.0,n=5),日内RSD小于5%,日间RSD小于10%,定量限25μg.L-1。在以7.5 ***-1的剂量静脉注射紫杉醇到大鼠身上后,药物很快分布到体内(t1/2α=0.16 h),并且快速的消除,消除半衰期仅有1.65 h,药物的平均保留时间tMR为0.52 h。结论所用方法简便、准确、专属性好,能够满足药物动力学研究的需要。

关键词：紫杉醇反相高效液相色谱法血药浓度

Adenosine triphosphate-binding pocket inhibitor for mixed lineage kinase domain-like protein attenuated alcoholic liver disease via necroptosis-independent pathway

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World Journal of Gastroenterology 2025年第6期31卷 44-61页

作者： Han-Ning Xuan Yuan Hyun Sung kim Gye Ryeol Park Jae Eun Ryu Ji Eun kim In Young Kang Hye Young kim Seung Min Lee Ju Hee Oh Eileen L Yoon dae Won Jun Department of Internal Medicine Hanyang University School of MedicineSeoul 04763South Korea Department of Pathology Hanyang University School of MedicineSeoul 04763South Korea Department of Translational Medicine Graduate School of Biomedical Science and EngineeringHanyang UniversitySeoul 04763South Korea Department of Obstetrics and Gynecology Institute of Women’s Medical Life ScienceYonsei Cancer CenterSeverance HospitalYonsei University College of MedicineSeoul 04763South Korea Department of Internal Medicine Sanggye Paik HospitalInje University College of MedicineSeoul 01757South Korea

BACKGROUND Mixed lineage kinase domain-like protein(MLKL)serves as a critical mediator in necroptosis,a form of regulated cell death linked to various liver *** study aims to specifically investigate the role of MLKL’s adenosine triphosphate(ATP)-binding pocket in facilitating necroptosis-independent pathways that may contribute to liver disease *** focusing on this mechanism,we seek to identify potential therapeutic targets that can modulate MLKL activity,offering new strategies for the prevention and treatment of liver-related *** To investigate the possibility of using the ATP-binding pocket-associated,necro-ptosis-independent MLKL pathway as a target for liver *** Cell death following necroptosis stimuli was evaluated using cell proliferation assays,flow cytometry,and electron microscopy in various *** human liver organoid system was used to evaluate whether the MLKL ATP pocket-binding inhibitor could attenuate ***,alcoholic and non-alcoholic fatty liver diseases animal models were used to determine whether MLKL ATP pocket inhibitors could attenuate liver *** While an MLKL ATP pocket-binding inhibitor did not prevent necroptosis-induced cell death in RAW 264.7 cells,it did reduce the necroptosis-led expression of CXCL2,ICAM,and ***,MLKL ATP pocket inhibitor diminishes the expression of CXCL2,ICAM,and VCAM by inhibiting the IκB kinase and nuclear factor kappa-B pathways without inducing necroptosis-induced cell death in two-dimensional cell culture as well as the human-derived liver organoid *** MLKL ATP-binding inhibitor was ineffective in non-alcoholic fatty liver disease animal models,MLKL ATP-binding inhibitor attenuated hepatic inflammation in the alcoholic liver disease *** MLKL ATP pocket-binding inhibitor exerted anti-inflammatory effects through the necroptosis-independent MLKL pathway in an animal model of alcoholic liver disease.

关键词： RAW 264.7 cell Cell death Necroptosis Mixed lineage kinase domain-like protein Non-alcoholic fatty liver disease Mixed lineage kinase domain-like protein adenosine triphosphate binding inhibitor Alcoholic liver disease

Molecules“buckle up”to drive layered hybrid perovskites into single-crystal nanowires in water

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Science China Chemistry 2025年第1期68卷 3-4页

作者： Seokhyoung kim Department of Chemistry Michigan State UniversityEast LansingMI 48824USA

Layered 2D metal halide perovskites(MHPs)are one of the most exciting candidates for next-generation light sources owing to their outstanding optoelectronic *** properties are readily tunable by controlling the halide composition,number of inorganic layers,and the chemistry of organic *** key element that can substantially impact the materials’functionalities is crystal morphology^([1]).

关键词： nanowires perovskite halide

Half-Covered'Glitter-Cake'AM@SE Composite:A Novel Electrode Design for High Energy Density All-Solid-State Batteries

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Nano-Micro Letters 2025年第5期17卷 463-478页

作者： Min Ji kim Jin-Sung Park Jin Woong Lee Sung Eun Wang Dowoong Yoon Jong Deok Lee Jung Hyun kim Taeseup Song Ju Li Yun Chan Kang dae Soo Jung Energy and Environmental Division Korea Institute of Ceramic Engineering and TechnologyJinjuGyeongnam 52851Republic of Korea Department of Materials Science and Engineering Korea UniversityAnam-DongSeongbuk-GuSeoul 136-713Republic of Korea Department of Nuclear Science and Engineering Massachusetts Institute of TechnologyCambridgeMA 20139USA Department of Materials Science and Engineering Ajou UniversitySuwon 16499Republic of Korea Department of Energy Systems Research Ajou UniversitySuwon 16499Republic of Korea Department of Energy Engineering Hanyang UniversitySeoul 04763Republic of Korea Department of Materials Science and Engineering Massachusetts Institute of TechnologyCambridgeMA 02139USA

All-solid-state batteries(ASSBs)are pursued due to their potential for better safety and high energy ***,the energy density of the cathode for ASSBs does not seem to be satisfactory due to the low utilization of active materials(AMs)at high *** small amount of solid electrolyte(SE)powder in the cathode,poor electrochemical performance is often observed due to contact loss and non-homogeneous distribution of AMs and SEs,leading to high tortuosity and limitation of lithium and electron transport ***,we propose a novel cathode design that can achieve high volumetric energy density of 1258 Wh L^(-1)at high AM content of 85 wt%by synergizing the merits of AM@SE core–shell composite particles with conformally coated thin SE shell prepared from mechanofusion process and small SE *** core–shell structure with an intimate and thin SE shell guarantees high ionic conduction pathway while unharming the electronic *** addition,small SE particles play the role of a filler that reduces the packing porosity in the cathode composite electrode as well as between the cathode and the SE separator *** systematic demonstration of the optimization process may provide understanding and guidance on the design of electrodes for ASSBs with high electrode density,capacity,and ultimately energy density.

关键词： All-solid-state batteries Cathodes Sulfide-based solid electrolytes Interfaces Mechanofusion

Role of glutathione transferase in phase separation of FUS and TAF15 in neurons

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Neural Regeneration Research 2025年第7期20卷 1999-2000页

作者： Kiyoung kim Department of Medical Science Soonchunhyang UniversityAsanKorea

Amyotrophic lateral sclerosis(ALS)is a progressive neurodegenerative disorder characterized by the degeneration of motor neurons in the brain and spinal cord,leading to muscle weakness,paralysis,and ultimately death(Cleveland and Rothstein,2001).Frontotemporal lobar degeneration(FTLD)is a neurodegenerative disease affecting the frontal and temporal lobes of the brain,leading to changes in behavior,personality,and language(Van Langenhove et al.,2012).Both ALS and FTLD are classified as proteinopathies in which abnormal protein aggregation and accumulation in neurons contribute to the disease *** in sarcoma(FUS)is a DNA/RNA-binding protein involved in various cellular processes,including transcriptional regulation,RNA splicing,and DNA *** in the FUS gene have been linked to familial ALS,highlighting the importance of FUS in the disease pathogenesis(Vance et al.,2009).In ALS and FTLD,aberrant post-translational modifications(PTMs)of FUS,such as phosphorylation,acetylation,and methylation,have been implicated in the promotion of FUS aggregation and neurotoxicity(Choi et al.,2023).Therefore,understanding the regulatory mechanisms of FUS PTMs is crucial for developing targeted therapies against these diseases.

关键词： degeneration FUS aggregation

Carboplatin restores neuronal toxicity in FUS-linked amyotrophic lateral sclerosis

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Neural Regeneration Research 2025年第8期20卷 2319-2320页

作者： Kiyoung kim Department of Medical Science Soonchunhyang UniversityAsanKorea

Amyotrophic lateral sclerosis(ALS),also known as Lou Geh rig's disease,is a progressive neurodegenerative disorder that affects motor neurons in the brain and spinal *** leads to muscle weakness,paralysis,and ultimate... 详细信息

关键词： paralysis sclerosis respiratory

Recovery of the injured neural system through gene delivery to surviving neurons in Parkinson’s disease

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Neural Regeneration Research 2025年第10期20卷 2855-2861页

作者： Chanchal Sharma Sehwan kim Hyemi Eo Sang Ryong kim School of Life Science Kyungpook National UniversityDaeguKorea BK21 FOUR KNU Creative BioResearch Group Kyungpook National University DaeguKorea Brain Science and Engineering Institute Kyungpook National UniversityDaeguKorea

A critical unaddressed problem in Parkinson’s disease is the lack of therapy that slows or hampers *** medications effectively manage symptoms,they offer no long-term benefit because they fail to address the underlying neuronal *** highlights that the elusive goals of halting progression and restoring damaged neurons limit the long-term impact of current *** clinical trials using gene therapy have demonstrated the safety of various vector delivery systems,dosages,and transgenes expressed in the central nervous system,signifying tangible and substantial progress in applying gene therapy as a promising Parkinson’s disease ***,at diagnosis,many dopamine neurons remain in the substantia nigra,offering a potential window for recovery and *** propose that modulating these surviving dopamine neurons and axons in the substantia nigra and striatum using gene therapy offers a potentially more impactful therapeutic approach for future ***,innovative gene therapies that focus on preserving the remaining elements may have significant potential for enhancing long-term outcomes and the quality of life for patients with Parkinson’s *** this review,we provide a perspective on how gene therapy can protect vulnerable elements in the substantia nigra and striatum,offering a novel approach to addressing Parkinson’s disease at its core.

关键词： adeno-associated virus gene therapy neuroprotection neurorestoration neurotrophic factor nigrostriatal dopamine pathway pro-survival protein

High mobility group box 1 in the central nervous system:regeneration hidden beneath inflammation

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Neural Regeneration Research 2025年第1期20卷 107-115页

作者： Hanki kim Bum Jun kim Seungyon Koh Hyo Jin Cho Xuelian Jin Byung Gon kim Jun Young Choi Department of Brain Science Ajou University School of MedicineSuwonSouth Korea Department of Biomedical Sciences Ajou University Graduate School of MedicineSuwonSouth Korea Department of Neurology Ajou University School of MedicineSuwonSouth Korea Department of Geriatrics The Affiliated Suqian First People’s Hospital of Nanjing Medical UniversitySuqianJiangsu ProvinceChina

High-mobility group box 1 was first discovered in the calf thymus as a DNA-binding nuclear protein and has been widely studied in diverse fields,including neurology and ***-mobility group box 1 in the extracellular space functions as a pro-inflammatory damage-associated molecular pattern,which has been proven to play an important role in a wide variety of central nervous system disorders such as ischemic stroke,Alzheimer’s disease,frontotemporal dementia,Parkinson’s disease,multiple sclerosis,epilepsy,and traumatic brain *** drugs that inhibit high-mobility group box 1 as a damage-associated molecular pattern,such as glycyrrhizin,ethyl pyruvate,and neutralizing anti-high-mobility group box 1 antibodies,are commonly used to target high-mobility group box 1 activity in central nervous system *** it is commonly known for its detrimental inflammatory effect,high-mobility group box 1 has also been shown to have beneficial pro-regenerative roles in central nervous system *** this narrative review,we provide a brief summary of the history of high-mobility group box 1 research and its characterization as a damage-associated molecular pattern,its downstream receptors,and intracellular signaling pathways,how high-mobility group box 1 exerts the repair-favoring roles in general and in the central nervous system,and clues on how to differentiate the pro-regenerative from the pro-inflammatory *** targeting high-mobility group box 1 in the central nervous system may benefit from differentiating between the two functions rather than overall suppression of high-mobility group box 1.

关键词： central nervous system damage-associated molecular pattern ethyl pyruvate glycyrhizzin high mobility group box 1 inflammation neural stem cells neurodevelopment oligodendrocyte progenitor cells redox status regeneration